Bibliothek

X
feed icon rss

Ihre E-Mail wurde erfolgreich gesendet. Bitte prüfen Sie Ihren Maileingang.

Leider ist ein Fehler beim E-Mail-Versand aufgetreten. Bitte versuchen Sie es erneut.

Vorgang fortführen?

Exportieren
Filter
  • 2000-2004
  • 1990-1994  (1.463)
  • 1985-1989
  • 1950-1954  (442)
  • 1940-1944  (182)
  • 1935-1939  (599)
  • 1925-1929
  • 1900-1904
  • 1990  (1.463)
  • 1954  (442)
  • 1942  (182)
  • 1936  (599)
  • General Chemistry  (2.251)
  • Rat  (174)
  • Biochemistry  (136)
  • pharmacokinetics  (125)
Datenquelle
Materialart
Erscheinungszeitraum
  • 2000-2004
  • 1990-1994  (1.463)
  • 1985-1989
  • 1950-1954  (442)
  • 1940-1944  (182)
    • +
Jahr
Schlagwörter
  • 101
    Digitale Medien
    Digitale Medien
    The synaptic connections of basket cell axons in the developing rat hippocampal formation (1990)
    Springer
    Experimental brain research 81 (1990), S. 500-508 
    Details
    ISSN: 1432-1106
    Schlagwort(e): Dentate gyrus ; Ammon's horn ; Synapses ; Golgi-gold labeled terminals ; Light and electron microscopy ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary Recent studies have indicated that hippocampal basket cells in both the dentate gyrus and Ammon's horn develop their somal and dendritic features during the first two postnatal weeks in rats. Their axon terminals form exclusively symmetric synapses that are found as early as 5 postnatal days in both regions. The present study used Golgi-electron microscopic material from 10 and 16 day old rats to demonstrate that the axon terminals of basket cells form synapses not only with somata, dendrites, and dendritic spines as reported for adult material but also with axon initial segments. However, the terminals forming synapses with axon initial segments and dendritic spines represent only a minor portion of the total number of basket cell terminals. Quantitative results indicate that 36–62% of the total number of these terminals form axosomatic synapses and 32–50% form axodendritic synapses depending on the analyzed cell. These data indicate that hippocampal basket cells have an axonal distribution similar to that found for cortical basket cells.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02423498
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 102
    Digitale Medien
    Digitale Medien
    Axotomized, adult basal forebrain neurons can innervate fetal frontal cortex grafts: A double fluorescent tracer study in the rat (1990)
    Springer
    Experimental brain research 81 (1990), S. 545-551 
    Details
    ISSN: 1432-1106
    Schlagwort(e): Axonal tracing ; Neural transplants ; Fluoro-Gold ; Nuclear Yellow ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The ability of axonal regeneration of identified adult basal forebrain (BFB) neurons was examined after homotopic grafting of fetal neocortical tissue to a lesion cavity in the frontal neocortex. Using a four step experimental procedure, adult rats first received an injection of the fluorescent dye Fluoro-Gold (FG) into the sensorimotor cortex in order to label those neurons with projections to the area by retrograde axonal transport. After one week the injection area was removed by aspiration, leaving a cavity in the neocortex. One week later a block of fetal (E14) frontal cortical tissue was placed in the cavity. The animals were then allowed to survive for 6 weeks before a second fluorescent tracer, Nuclear Yellow (NY), was injected into the transplant. The animals were sacrificed 24 h later and analyzed by fluorescence microscopy. Both single labeled, FG and NY containing neurons and double labeled neurons containing both tracers were found in the BFB. The results demonstrate that adult BFB neurons can reestablish cortical projections into fetal cortical grafts (double labeled neurons), and they suggest that other BFB neurons, not initially innervating the lesioned cortical area, have sprouted into the transplant (NY labeled neurons).
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02423503
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 103
    Digitale Medien
    Digitale Medien
    Topography of the facial musculature within the facial (VII) motor nucleus of the neonatal rat (1990)
    Springer
    Experimental brain research 81 (1990), S. 649-653 
    Details
    ISSN: 1432-1106
    Schlagwort(e): Motoneurons ; Musculotopic organization ; Whisker follicle ; Brainstem ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary WGA-HRP, HRP and fluorescent tracers were used to determine the representation of the facial muscles in the facial motor nuclear complex (FMNC) of the newborn rat. Tracer injections of the superficial cervical and anterior mandibular portions of platysma, the orbicularis oculi muscle, the nasolabial musculature and the posterior auricular musculature revealed an adultlike topographic organization across FMNC subnuclei. Tracer delivery to individual vibrissa follicle loci of the whiskerpad also demonstrated an adult-like musculotopic organization within the lateral subnucleus.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02423515
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 104
    Digitale Medien
    Digitale Medien
    The expression of different cytochemical markers in normal and axotomised dorsal root ganglion cells projecting to the nucleus gracilis in the adult rat (1990)
    Springer
    Experimental brain research 105 (1990), S. 331-344 
    Details
    ISSN: 1432-1106
    Schlagwort(e): Dorsal root ganglion ; Nucleus gracilis ; Sciatic nerve ; Nerve injury ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Rat lumbar dorsal root ganglion neurones projecting to the nucleus gracilis in the brainstem were retrogradely labelled with Fluoro-Gold and analysed immunocytochemically for their expression of substance P-, calcitonin gene-related peptide-, galanin-, galanin message-associated peptide-, neuropeptide Y-, nitric oxide synthase- and carbonic anhydrase-like immunoreactivity as well as affinity to Griffonia (bandeiraea) simplicifolia lectin I — isolectin B4, RT97 and to choleragenoid. The analysis was made both in uninjured rats and in rats which had been subjected to unilateral sciatic nerve transection and partial resection 3 weeks earlier. The data showed that 6% of the L4 and L5 lumbar dorsal root ganglion cells that projected to the nucleus gracilis showed substance P-like immunoreactivity. Following nerve injury, none of the nucleus gracilis-projecting dorsal root ganglion cells showed substance P-like immunoreactivity. Nineteen per cent of the investigated cell population showed calcitonin gene-related peptide-like immunoreactivity in uninjured rats, but no nucleus gracilisprojecting calcitonin gene-related peptide-positive cells were found after nerve injury. Galanin- and galanin message-associated peptide-like immunoreactivity were found in 2% and 3%, respectively, of the Fluoro-Gold-labelled cell population normally and in 22% and 14%, respectively, after injury. No neuropeptide Y-positive cells were found in the Fluoro-Gold-labelled cell population normally, but after nerve injury, 96% of this population became neuropeptide Y-positive. Nitric oxide synthaselike immunoreactivity was found in 2% of the Fluoro-Gold-labelled cells normally and in 10% after injury. Two per cent of the Fluoro-Gold-labelled cells in the normal cases were stained by Griffonia (bandeiraea) simplicifolia lectin I — isolectin B4. After injury, however, no such double labelling was found. Thirty-four per cent of the Fluoro-Gold-labelled cell population was carbonic anhydrase positive normally, and 42% after injury. Seventy-five per cent of the Fluoro-Gold-labelled cells showed RT97 immunoreactivity normally and 12% after injury. Choleragenoid-like immunoreactivity was found in 99% of the Fluoro-Gold-labelled dorsal root ganglion cells normally and 81% after injury. Immunohistochemical visualisation of choleragenoid transganglionically transported from the injured sciatic nerve combined with neuropeptide Y immunocytochemistry showed that primary afferent fibres and terminals in the nucleus gracilis contain neuropeptide Y following peripheral nerve transection. Taken together, the results indicate that peripherally axotomised nucleus gracilis-projecting neurones undergo marked alterations in their cytochemical characteristics, which may be significant for the structural and functional plasticity of this system after injury.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00233034
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 105
    Digitale Medien
    Digitale Medien
    In the hippocampus in vivo, nitric oxide does not appear to function as an endogenous antiepileptic agent (1990)
    Springer
    Experimental brain research 105 (1990), S. 391-401 
    Details
    ISSN: 1432-1106
    Schlagwort(e): NADPH diaphorase ; Hilus ; l-Nitro-arginine ; 8-Bromo-cGMP ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Using a reverberatory epilepiform discharge of hippocampal-parahippocampal circuits termed “maximal dentate activation”, this study investigated whether the local release of nitric oxide within these circuits functions as an antiepileptic agent. Two nitric oxide synthase inhibitors (l-nitro-arginine methyl ester and 7-nitro-indazole) and a guanylate cyclase inhibitor (methylene blue) were tested, and none had a significant effect on the time to onset or duration of maximal dentate activation. A membrane-permeable analogue of cyclic guanosine monophosphate (cGMP), 8-bromo-cGMP, caused an increase in the time to onset and a decrease in the duration of maximal dentate activation. The number of neurons expressing NADPH diaphorase activity (a marker for nitric oxide synthase) was also examined after repeated elicitation of maximal dentate activation. After 18 seizures there was a significant, but transient, decrease in the number of hilar/subgranular neurons that were NADPH diaphorase-positive. The decrease was only seen at 1 h after the last seizure. There was no induction of NADPH diaphorase activity. These results are not consistent with the hypothesis that, in hippocampal-parahippocampal circuits in vivo, nitric oxide is released in response to neuronal activity and then acts to terminate the neuronal activity.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00233039
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 106
    Digitale Medien
    Digitale Medien
    The influence of insulin-induced hypoglycemia on the calcium transients accompanying reversible forebrain ischemia in the rat (1990)
    Springer
    Experimental brain research 105 (1990), S. 363-369 
    Details
    ISSN: 1432-1106
    Schlagwort(e): Ischemia ; Hypoglycemia ; Calcium transient ; Insulin ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The primary objective of this study was to explore why preischemic hypoglycemia, which restricts tissue acidosis during the ischemic insult, does not ameliorate cell damage incurred as a result of transient ischemia. The question arose whether hypoglycemia (plasma glucose concentration 2–3 mM) delays resumption of extrusion of Ca2+ from cells during recirculation. Measurements of extracellular Ca2+ concentration during forebrain ischemia of 15 min duration proved that this was the case. Thus, normoglycemic animals resumed Ca2+ extrusion upon recirculation after a delay of 1.5–2.0 min, and hypoglycemic ones after an additional delay which could amount to 3–4 min. We attempted to explore the cause of this delay. At first sight, the results suggested that resumption of oxidative phosphorylation upon recirculation was substrate limited. However, glucose infusion during ischemia or just after recirculation failed to accelerate Ca2+ extrusion from the cells. A comparison between non-injected and insulin-injected animals at equal plasma glucose concentrations suggested that insulin was responsible for the delay. On analysis, the delay proved to be related to a sluggish recovery of cerebral blood flow. The results suggest that when cell damage is evaluated after transient ischemia in hypo- and normoglycemic subjects, attention should be directed to the period of cell calcium ‘overload’. Unobserved differences in the duration of the calcium transient may also confound interpretation of data on the effects of insulin.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00233036
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 107
    Digitale Medien
    Digitale Medien
    Dye coupling between dorsal raphe neurones (1990)
    Springer
    Experimental brain research 105 (1990), S. 383-390 
    Details
    ISSN: 1432-1106
    Schlagwort(e): Dorsal raphe nucleus ; Biocytin ; Dye coupling ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Neurones in the dorsal raphe nucleus (DRN) were impaled and filled with biocytin in coronal slices of midbrain taken from young adult rats. The electrophysiological properties and gross morphology of the cells were similar to those reported previously for serotonergic neurones in the DRN. Of 27 cases in which filled neurones were recovered in histological material, almost half (48%) showed labelling of two or three cells, although only one cell had been recorded from. Coupled cells were identified as close or distantly coupled, depending on the distance from the soma of the presumed impaled cell (23.5±15 μm, n=7 and 150±26.5 μm, n=10 respectively). Whereas close-coupled cells may have been artefactually “coupled” by the penetrating electrode, coupling between distant cells is most likely to be a result of transfer of biocytin through gap junctions. Camera lucida reconstructions of pairs of labelled cells revealed extensive overlap of dendritic fields and numerous crossings between dendrites. When examined at high magnification under a light microscope, many of the crossing dendrites were found to travel in different focal planes. Nevertheless, for each pair of cells, at least one point of close apposition was observed between dendrites or between the axon and a dendrite of the presumed impaled and coupled cell. The incidence of dye coupling between neurones in the DRN may reflect a relatively high level of electrotonic coupling between the neurones. This form of coupling may be important in determining the synchronous nature of firing of neurones in the DRN.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00233038
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 108
    Digitale Medien
    Digitale Medien
    Peripheral nervous control of cold-induced reduction in the respiratory quotient of the rat (1990)
    Springer
    International journal of biometeorology 34 (1990), S. 24-27 
    Details
    ISSN: 1432-1254
    Schlagwort(e): Cold-induced thermogenesis ; Peripheral nervous system ; Respiratory quotient ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Geographie , Physik
    Notizen: Abstract Cold-exposed rats show a reduction in the respiratory quotient which is indicative of a relative shift from carbohydrates to lipids as substrates for oxidative metabolism. In the present study, the effects of food deprivation and cold exposure on the respiratory quotient were observed. In addition, the involvement of the three main branches of the peripheral nervous system (sympathetic, parasympathetic, and somatic) was investigated by means of synaptic blockade with propranolol, atropine, and quinine, respectively. Both propranolol and quinine blocked the cold-induced decrease in respiratory quotient and increase in heat production, whereas atropine had only minor and very brief effects. It is concluded that both the sympathetic and somatic branches are involved in the metabolic changes associated with cold-induced thermogenesis and that the increase in metabolic heat production involves a shift from carbohydrate to lipid utilization irrespective of which of the two branches is activated.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01045816
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 109
    Digitale Medien
    Digitale Medien
    Pharmacokinetic properties of the antimuscarinic drug [3H]-hexahydro-sila-difenidol in the rat (1990)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 342 (1990), S. 146-152 
    Details
    ISSN: 1432-1912
    Schlagwort(e): Pharmacokinetics ; [3H]-Hexahydro-siladifenidol ; Sila-drug ; Rat ; Autoradiography
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The pharmacokinetics of tritiated hexahydrosila-difenidol ([3H]-HHSiD) were examined in rats. Furthermore, the distribution of radioactivity was studied by means of whole body autoradiography. After i. v. administration of 2.9 mg/kg HHSiD plus [3H]-HHSiD to anaesthetized rats bearing a catheter implanted in the ductus choledochus and receiving a mannitol infusion, HHSiD was rapidly distributed and metabolized. Only 5% of the radioactivity was recovered in blood after 23 s and 0.4% after 2.5 h. 64% of the plasma radioactivity could be extracted with hexane from the samples taken 23 s after administration. 52% of the radioactivity was eliminated within 2.5 h, 13% by urinary and 39% by biliary excretion. Following oral administration of 8.6 mg/kg HHSiD plus [3H]-HHSiD there was an absorption of approximately one fourth of the administered radioactivity within 4 h. By means of whole body autoradiography (i. v. injection) as well as by tissue distribution measurement the highest levels of radioactivity were found in bile, urine, lung, kidney, adrenals, liver and pancreas. Thus, after i. v. administration to rats HHSiD is rather quickly distributed, metabolized and excreted. This explains its low antimuscarinic potency in vivo.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00166957
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 110
    Digitale Medien
    Digitale Medien
    Regulation of renal phosphate reabsorption during development: implications from a new model of growth hormone deficiency (1990)
    Springer
    Pediatric nephrology 4 (1990), S. 387-391 
    Details
    ISSN: 1432-198X
    Schlagwort(e): Renal phosphate reabsorption ; Growth hormone deficiency ; Growth hormone releasing factor antagonist ; Renal development ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract It has been hypothesized that the high rate of renal phosphate (Pi) reabsorption in the immature animal is a consequence of the increased demand for Pi associated with the rapid rate of growth. Although growth hormone (GH) has been proposed to play a role in this process, investigations of the relationship between GH, growth and the renal Pi transport have been hampered by the lack of methods available to specifically alter circulating GH levels. This review summarizes the findings from recent studies using a newly developed peptidic antagonist to GH-releasing factor (GRF-AN) as a method of specifically inhibiting GH release. Systemic injection of GRF-AN was effective in suppressing the pulsatile release of GH, and in significantly attenuating the rate of growth, in both immature and adult rats. However, the inhibition of growth was associated with a reduction in net Pi retention only in immature rats, resulting in a doubling in the urinary excretion of Pi. GRF-AN treatment of immature rats lead to a decrease in the maximum tubular capacity to transport Pi-down to the level seen in adult rats. However, GRF-AN treatment did not alter renal Pi reabsorption in adult rats. We conclude that chronic administration of an antagonist to GRF in rats provides a new model of GH deficiency with which to study the interrelationships between growth, GH and other physiological systems. Furthermore, the findings suggest that the pulsatile release of GH, directly or indirectly, contributes to the high rate of renal Pi reabsorption in young, growing animals and may play a critical role in regulating Pi homeostasis during development.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00862524
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 111
    Digitale Medien
    Digitale Medien
    NMR studies of phosphate metabolism in the isolated perfused kidney of developing rats (1990)
    Springer
    Pediatric nephrology 4 (1990), S. 392-398 
    Details
    ISSN: 1432-198X
    Schlagwort(e): Nuclear magnetic resonance ; Phosphate metabolism ; Renal development ; Isolated perfused kidney ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract During growth, the capacity for renal phosphate (Pi) reabsorption varies as a function of Pi demand. These changes occur in the absence of changes in extracellular concentration of Pi and are also observed in renal cells cultured in defined media. These findings suggest a direct regulatory effect of intracellular Pi on its transport systems. We postulate that a low intracellular Pi concentration ([Pi]i) occurs in the developing kidney as a consequence of differences in Pi metabolism between growing and mature cells and that a low [Pi]i, in turn, leads to adaptive changes in renal Pi transport. In order to assess this hypothesis, we used31P-nuclear magnetic resonance (NMR) to measure the intracellular concentrations of NMR-visible Pi and phospho-metabolites and the rates of Pi turnover due to adenosine triphosphate (ATP) synthesis, in isolated perfused kidneys of 3- to 4-week-old and 12- to 13-week-old rats. The [Pi]i was lower (1.7±0.1 vs 2.7±0.1 mM,P〈0.05) in kidneys of growing than of adult rats, while the ATP (2.9±0.3 vs 2.8±0.5 mM) and adenosine diphosphate (ADP)(−0.2 mM) concentrations were similar at the two ages, consistent with a high phosphorylation potential in the kidneys of the younger animals. Radiofrequency irradiation of the γ-P of ATP resulted in reduction in the intensity of the Pi resonance of 62±5% in the newborn and 38±3% in the adult (P〈0.05). The corresponding 1.6-fold higher fractional turnover rate of the Pi pool in the younger than in the older rats accounts for the similar rates of ATP synthesis at the two ages (30±7 vs 35±4 μmol/min per g,P〉0.3), despite the smaller intracellular Pi pool present in the younger than in the older animals. The low [Pi]i may stimulate the synthesis of 1,25 hydroxivitamin D3 and the expression of Pi transport related proteins. The high phosphorilation potential drives the ATP flux necessary for growth related transport and biosynthetic processes.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00862525
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 112
    Digitale Medien
    Digitale Medien
    ACTH-induced behaviors and their modulation by serotonergic agonists differ in neonatal and weanling rat pups (1990)
    Springer
    Psychopharmacology 100 (1990), S. 151-158 
    Details
    ISSN: 1432-2072
    Schlagwort(e): ACTH ; Behavior ; Serotonergic agonists ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Four-day-old (P4) and 21–22-day-old (P21–22) rat pups received an intracisternal injection of either ACTH1-16NH2 or saline followed by a subcutaneous (SC) injection of saline, the serotonergic (5HT)1A agonists 8-OH-DPAT or ipsapirone, the 5HT1B agonist TFMPP or the 5HT2 agonist DOI. The ontogeny of ACTH-induced behaviors including grooming, yawn and stretch as well as various serotonin-related behaviors were recorded via time-sampling at 20 s intervals for a test duration of 50 min. ACTH induced slight but significant increases in grooming at P4, along with a significant increase in yawning. At this age the 5HT1B agonist TFMPP induced substantial increases in grooming, with no effect of the other agonists on this behavior. All of the serotonergic agonists, however, decreased ACTH-induced yawning at P4. At P21–22 ACTH induced more robust grooming than that observed at P4, although different in nature from adult-typical ACTH-induced grooming. This ACTH-induced grooming at P21–22 was attenuated by all of the serotonergic agonists. ACTH-induced yawning at P21–22 was not affected by the serotonergic agonists while ACTH-induced stretching was increased by the 5HT1B agonist TFMPP at this age. These data provide additional evidence of differential mediation of various ACTH-induced behaviors, and support other reports of ontogenetic alterations in the response to serotonergic manipulations during the neonatal to weanling age period.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244398
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 113
    Digitale Medien
    Digitale Medien
    Influence of dose and route of administration on the kinetics of fluoxetine and its metabolite norfluoxetine in the rat (1990)
    Springer
    Psychopharmacology 100 (1990), S. 509-514 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Fluoxetine ; Norfluoxetine ; Kinetics ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Fluoxetine (FL) is being used in neuropharmacology as a tool for studying various functional roles of serotoninergic neurons. Its kinetics was studied in rats, a species widely used in neurochemical studies, after IV (2.5–10 mg/kg) and oral (5–20 mg/kg) administration. When injected IV the drug followed apparent first-order kinetics up the 10 mg/kg dose. Its volume of distribution was large and total body clearance was relatively high compared to liver blood flow. The mean elimination half-lives (t 1/2) of FL and its active metabolite norfluoxetine (NFL) were about 5 and 15 h, respectively. The mean blood:plasma concentration ratios of FL and NFL approached unity and plasma protein binding was 85–90% for both compounds. After oral doses the kinetics of FL were complex. At the lowest dose tested (5 mg/kg) the drug was efficiently extracted by the liver (extraction ratio about 60%), resulting in bioavailability of only about 38%. Plasma areas under the curve (AUC) of the metabolite were approximately the same as after IV injection of the same dose; consequently the metabolite-to-parent drug ratio after oral administration (about 5) was approximately twice that after IV injection of FL (about 2.5). At higher doses, however, the oral bioavailability (e.g.C max and AUC) appeared greater than expected, possibly because of transient saturation of FL first-pass metabolism in the case of the 10 mg/kg dose and concomitant saturation of elimination kinetics at the higher dose (20 mg/kg). The apparent eliminationt 1/2 of FL markedly increased and the metabolite-to-parent drug ratio declined with the higher dose, this also being consistent with saturable elimination. Brain concentrations reflected the plasma kinetics of FL and NFL and the metabolite-to-parent drug ratio varied with dose and time of administration and was modified at the highest dose tested. FL and its metabolite NFL distributed almost evenly in discrete brain areas and subcellular distribution was similar for both compounds. Neurochemical studies of FL should consider the formation of the active metabolite NFL and extrapolation of data across animal species requires consideration of dose dependence in the rat.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244004
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 114
    Digitale Medien
    Digitale Medien
    Regional neurotransmitter responses after acute and chronic electroconvulsive shock (1990)
    Springer
    Psychopharmacology 101 (1990), S. 60-65 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Microdialysis ; Electroconvulsive shock ; Noradrenaline ; Dopamine ; Regional responses ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Regional neurotransmitter changes after acute and chronic electroconvulsive shock (ECS) were studied using the technique of repeated microdialysis. Microdialysis was carried out on alternate sides of the brains of anaesthetised rats before and during the first and the eighth ECS or sham (control) treatments. Extracellular fluid release of monoamines and their metabolites was measured in the frontal cortex, striatum and nucleus accumbens using HPLC with electrochemical detection. The first ECS produced selective regional responses, shown by increased concentrations of noradrenaline (NA) and dopamine (DA) in frontal cortex, by unchanged DA content in striatum, and by a small rise in NA and a fall in DA concentrations in nucleus accumbens. Concentrations of metabolites increased after ECS in all regions studied, and for homovanillic acid and dihydroxyphenylacetic acid, the temporal pattern of these changes did not resemble that of DA. Comparison of neurotransmitter responses as per cent of baseline release after the first and eighth ECS treatments showed they were identical. Basal release of monoamines and metabolites before the first ECS or sham treatment was similar in all regions studied. Prior to the eighth treatment, basal release of NA in the frontal cortex and DA in the striatum was elevated in the ECS-treated animals, while basal release of NA in the nucleus accumbens was reduced in both ECS-and sham-treated animals. These data suggest that acute and chronic ECS have different and region-specific effects on neurotransmitter release, although the overall pattern of these responses is not changed by chronic treatment. The catecholamine-releasing actions of ECS, and the changes in basal release of neurotransmitters seen after chronic treatment may contribute to its therapeutic effects.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02245791
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 115
    Digitale Medien
    Digitale Medien
    Oxiracetam andd-pyroglutamic acid antagonize a disruption of passive avoidance behaviour induced by the N-methyl-d-aspartate receptor antagonist 2-amino-5-phosphonovalerate (1990)
    Springer
    Psychopharmacology 101 (1990), S. 130-131 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Nootropic drugs ; d-Pyroglutamic acid ; Oxiracetam ; NMDA receptor ; Passive avoidance ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Intracerebroventricular administration (6 µg/2 µl) ofd-2-amino-5-phosphonovalerate (AP-5), a specific antagonist of the NMDA receptors, prior to training impaired the passive avoidance in a retention test in rat. Pretreatment with oxiracetam andd-pyroglutamic acid at doses ranging from 50 to 500 mg/kg SC dose-dependently prevented the disruptive effect of AP-5. This finding indicates that an interaction with excitatory amino acid NMDA type receptors may be important in behavioural effects of the two pyrrolidinone derivatives.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02245803
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 116
    Digitale Medien
    Digitale Medien
    Anxiogenic-like effect of infusing 1-(3-chlorophenyl) piperazine (mCPP) into the hippocampus (1990)
    Springer
    Psychopharmacology 101 (1990), S. 138-140 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Anxiety ; 1-(3-Chlorophenyl)piperazine (mCPP) ; Hippocampus ; 5-HT1C receptor ; Social activity ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract 1-(3-Chlorophenyl) piperazine (mCPP) was previously shown to have an anxiogenic-like effect, i.e., it decreased total interaction in a rat social interaction test. Evidence indicated mediation by activation of 5-HT1C receptors with an ED50 of approximately 500 µg/kg IP (Kennett et al. 1989). A comparable effect is now shown on infusing 4 µg of the drug ICV or infusing 0.5 µg into the hippocampus. Both responses were dose dependent. Infusion of 1 µg mCPP into the amygdala had no effect. None of the above treatments significantly reduced locomotion. Results are consistent with the postulated role of the hippocampus in anxiety.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02245806
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 117
    Digitale Medien
    Digitale Medien
    Involvement of 5-HT1C-receptors in drug-induced penile erections in rats (1990)
    Springer
    Psychopharmacology 101 (1990), S. 57-61 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Penile erections ; 5-HT1C receptors ; Functional antagonism ; 5HT1C-receptor selectivity ratio ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Drug-induced penile erections (PE) were initially suggested to be 5-HT1B receptor mediated. However, since the discovery of the 5-HT1C receptor a number of compounds, considered to be 5-HT1B selective, appear to bind more strongly to the 5-HT1C receptor and this prompted a re-evaluation of the receptor subtype involved in PE induction. PE could be induced by the 5-HT agonists mCPP (0.22–2.2 mg/kg), TFMPP (0.46–1.0 mg/kg) and MK 212 (0.1–1.0 mg/kg). The 5-HT agonist DOI (0.022–0.22 mg/kg) did not induce PE in placebo-pretreated rats but in rats pretreated with various 5-HT2 antagonists it did. These compounds have in common a strong affinity for the 5-HT1C receptor. mCPP (0.46 mg/kg)-induced PE could be antagonized by the 5-HT antagonists metergoline, cyproheptadine, mesulergine, mianserin, ritanserin and ketanserin. Their ED50s were 0.04, 0.4, 0.03, 0.06, 0.4 and 2 mg/kg, respectively. The potency of both the agonists to induce, and the antagonists to inhibit, PE was found to be dependent on their selectivity for the 5-HT1C receptor versus the 5-HT2 receptor. Spiperone (0.1–1.0 mg/kg) and GR 38032F (1–10 mg/kg) did not antagonise mCPP-induced PE. 8-OH-DPAT and 5MeODMT counteracted mCPP (0.46 mg/kg)-induced PE. Their ED50s were 0.03 and 0.4 mg/kg, respectively. DOI counteracted mCPP induced PE only at doses above 1 mg/kg, whereas CGS 12066B (1.0–10 mg/kg) was inactive. The results suggest that PE are induced by activation of the 5-HT1C receptor and are functionally inhibited by activation of 5-HT1A or 5-HT2 receptors.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02253718
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 118
    Digitale Medien
    Digitale Medien
    Free choice ethanol intake of laboratory rats under different social conditions (1990)
    Springer
    Psychopharmacology 101 (1990), S. 233-239 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Ethanol ; Drug taking behavior ; Isolation ; Stress ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract To study the effects of different kinds of social deprivation on voluntary ethanol (ETOH) intake male Wistar rats were housed by (a) individual caging, (b) “contact” caging (partial social deprivation), and (c) group caging (four individuals per cage). In the latter condition the individuals were separated once a week from each other for 24 h. The rats simultaneously received water 5%, 10% and 20% ETOH for a period of 14 weeks. Additional control animals received water. Isolated individuals drank significantly more alcohol than group-housed or contact-caged rats. After a few days they preferred the 20% solution. Circadian measures revealed a discontinuous intake of high doses (〉 0.5 g/kg/h) during short time periods. Contact-caged rats consumed much less ETOH, but both the preference for 20% ETOH and the circadian course of intake were similar to those occurring after isolation. ETOH intake of group-housed individuals was low. These individuals preferred the 5% solution and continuously consumed small ETOH doses. During the period of short-term isolation they drank even more ETOH than long-term isolated individuals. In contrast to the latter, the enhancement of intake decreased after some weeks. It is suggested that the differences between the housing groups not only reflect different degrees of isolation stress, but may also be explained by a contribution of different reinforcing or aversive psychotropic effects of ETOH. Reduction of isolation stress is probably most important in the situation of short term separation, whereas dose-dependent reinforcement via social stimulation or sedation may affect the drug taking behavior under the other social conditions.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244132
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 119
    Digitale Medien
    Digitale Medien
    Dizocilpine (MK-801), ketamine and phencyclidine: low doses affect brain field potentials in the freely moving rat in the same way as activation of dopaminergic transmission (1990)
    Springer
    Psychopharmacology 101 (1990), S. 317-323 
    Details
    ISSN: 1432-2072
    Schlagwort(e): MK-801 (Dizocilpine) ; Phencyclidine ; l-Dopa ; Field potentials ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The effects of dizocilpine (MK-801), (±)-5-methyl-10,11-dihydro-5Hdibenzo-[a,d]-cyclohepten-5,10-imine maleate, after IP injection into freely behaving rats, have been compared with the action of ketamine-chloride and phencyclidine (PCP). MK-801 produced strongly dose-dependent effects which could be followed quantitatively over a time of 4 h. During this time spectral analysis of the field potentials continuously recorded from frontal cortex, hippocampus, striatum, and reticular formation revealed a particular pattern of changes which was very stable over time, and, after low doses of 0.05 and 0.1 mg/kg, matched that produced by phencyclidine (2 and 4 mg/kg) or ketamine chloride (10 and 20 mg/kg). With higher doses of MK-801 a continuous change from power decreases to power increases was observed. These increases were accompanied by strong behavioral effects in terms of impaired locomotor control. All three non-competitive NMDA antagonists showed a high degree of similarity with respect to the changes of the frequency content of the field potentials over time. The same pattern of electrical changes could be observed after the application ofl-dopa (50 mg/kg) or amphetamine (0.2 mg/kg). This can be interpreted in the sense that the same population of cells within the recording area which is under dopaminergic control is at the same time under glutamate control. This leads to the hypothesis that it might be possible to bypass the missing dopaminergic control during parkinsonism by noncompetitive NMDA-receptor blocking drugs.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244048
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 120
    Digitale Medien
    Digitale Medien
    Initial sensitivity, acute tolerance and alcohol consumption in four inbred strains of rats (1990)
    Springer
    Psychopharmacology 101 (1990), S. 390-395 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Sensitivity ; Acute tolerance ; Drinking ; Strains ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Initial sensitivity and acute tolerance to ethanol were determined in a jumping test in separate groups of spontaneously hypertensive (SH) and normotensive Wistar-Kyoto (WKY) rats, and of Dahl salt-sensitive (SS) and salt-resistant (SR) rats. One week later, voluntary consumption of ethanol was studied in all groups. SH rats were found to be more sensitive than WKY, but there was no difference in acute tolerance development between these two strains. SH rats, however, drank significantly more alcohol than the WKY in both the two-bottle choice paradigm and the limited access model. Similarly, SS rats drank significantly more alcohol than the SR rats, although SS rats were found to be more sensitive to ethanol than SR. There was again no difference in acute tolerance development between these two strains. These observations suggest that difference in alcohol consumption in these strains cannot be accounted for by significant differences in acute tolerance or in initial sensitivity to ethanol.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244059
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 121
    Digitale Medien
    Digitale Medien
    Panax ginseng extract modulates sleep in unrestrained rats (1990)
    Springer
    Psychopharmacology 101 (1990), S. 486-488 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Circadian rhythm ; Ginseng extract ; Panax ginseng ; Rat ; Slow wave sleep (SWS)
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The amount of wakefulness and slow wave sleep (SWS) during the 12-h light period slightly but significantly decreased and increased, respectively, in freely behaving rats after continued 1-week intake of Panax ginseng extract through drinking water (15 mg/day). Paradoxical sleep was little affected. No sleep parameters were modulated by the treatment during the dark period. The diurnal SWS enhancement disappeared and recovered to the baseline level after 2 weeks of continued treatment. It is speculated that the well known health-improving effect of the ginseng may be, at least in part, related to an enhancement of sleep.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244226
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 122
    Digitale Medien
    Digitale Medien
    A matching law analysis of the effects of dopamine receptor antagonists (1990)
    Springer
    Psychopharmacology 101 (1990), S. 560-567 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Herrnstein's equation ; Dopamine antagonists ; Reinforcement ; Motor capacity ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Herrnstein's matching equation was used to analyze drug effects on performance in random interval reinforcement schedules. Pimozide caused effects compatible with both motor and motivational impairments, in a 5-component multiple schedule, a 3-schedule 3-day cycle (ALT-3), and a 2-schedule 2-day cycle (ALT-2). However, at low doses, both sulpiride and SCH-23390, tested in the ALT-3 and ALT-2 procedures, caused effects compatible with selective motivational impairments. In experiments using the non-multiple schedules, motivational effects increased during the course of the experimental session, under all three drugs. The interpretation of “motor” and “motivational” deficits in the ALT-2 procedure was validated by experiments in which the response-force and deprivation level were systematically varied. The results support the view that dopamine may be involved in the maintenance of rewarded behaviour, but do not differentially implicate the D1 or the D2 receptor subtype.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244238
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 123
    Digitale Medien
    Digitale Medien
    Amnesic trace locked into the benzodiazepine state of memory (1990)
    Springer
    Psychopharmacology 102 (1990), S. 28-36 
    Details
    ISSN: 1432-2072
    Schlagwort(e): State-dependence ; Benzodiazepines ; Memory ; Drug dependence ; Drug tolerance ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Rats were trained in a food-rewarded lever-pressing task until they could complete an FR10 requirement within the first 120 s of the session, and were tested for the retention of this response requirement after having reached this criterion. The pharmacological treatment instituted at the time of tests was either the same as or different from that used during acquisition. In this state-dependency (StD) procedure, saline-to-drug as well as drug-to-saline state changes produced robust failures to transfer with chlordiazepoxide (CDP) and also with yohimbine. Diazepam substituted for, while Ro 15-1788 antagonised, CDP; none of several non-benzodiazepine compounds substituted for CDP. Neither food deprivation nor extensive overtraining after CDP prevented the failure of transfer when animals were tested for drug-to-saline transfer. Another series of experiments evaluated the effects of CDP and diazepam in a rat conflict procedure. The doses at which CDP and diazepam produced anti-conflict effects were similar to those at which failure to transfer occurred in saline-to-drug state changes, and higher than those at which such failure occurred in drug-to-saline state changes. With benzodiazepines, StD of memory retrieval conceivably constitutes a parsimonious explanation of the anxiolytic and untoward (amnesic, drug dependence) actions of these drugs.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02245740
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 124
    Digitale Medien
    Digitale Medien
    Ethanol effects on delayed spatial matching as modeled by a negative exponential forgetting function (1990)
    Springer
    Psychopharmacology 102 (1990), S. 391-398 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Delayed matching-to-position ; Signal detection theory ; Exponential model ; Ethanol ; Chlordiazepoxide ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Performance on delayed matching-to-position as a function of ethanol was investigated in rats and dose effects assessed by fitting an exponential decay model of forgetting to signal detection sensitivity scores. Three ethanol doses (0.25, 0.50, and 0.75 g/kg) and one isovolume saline control were examined. For further comparison, one dose of chlordiazepoxide (CDP; 5 mg/kg) and its saline control were also given. Forgetting functions were reasonably well described by the decay model under all treatment conditions. In addition, the functions's decay constant (−b) proved to be differentially sensitive to both drug and dose effects. Reduced decay estimates were obtained following the two lowest ethanol doses, the reduction being statistically significant for the 0.25 g/kg dose. In contrast, the function estimate of initial sensitivity, the intercept parameter (SI0), was not significantly affected by ethanol. Consistent with the low-dose ethanol effects, CDP significantly decreased the value of the decay parameter while leaving the intercept parameter unaffected. But unlike ethanol, the variance accounted for by the model for the individual data was less following CDP administration. Drug effects were interpreted using the exponential decay model of forgetting, and the results suggest independent discriminative control over SI0 and b. The significant effect of the low-dose sedative-hypnotics upon b, with no attendant effects upon SI0, is suggested to result from enhanced, spontaneous, delay interval mediation.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02244109
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 125
    Digitale Medien
    Digitale Medien
    Discriminative stimulus properties of 8-OH-DPAT in rats are not altered by pretreatment with para-chlorophenylalanine (1990)
    Springer
    Psychopharmacology 101 (1990), S. 39-42 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Drug discrimination test ; 5-HT1A autoreceptor ; 8-OH-DPAT ; pCPA ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The role of 5-HT1A autoreceptors in the discriminative stimulus properties of 8-OH-DPAT (0.1 mg/kg, SC) in rats, was investigated. Drug lever appropriate responding to 8-OH-DPAT (0.1 mg/kg, SC) and ipsapirone (3 mg/kg, SC) was measured before and after treatment with para-chlorophenylalanine (pCPA) at a dose (150 mg/kg IP, −3 and −2 days) which causes severe depletion of brain 5-HT stores. The recognition of the drug stimulus was not significantly altered by pCPA. These results indicate that activation of 5-HT1A autoreceptors is of minimal importance to the 8-OH-DPAT cue.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02253715
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 126
    Digitale Medien
    Digitale Medien
    Effects of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) on locomotor activity and rearing of mice and rats (1990)
    Springer
    Psychopharmacology 102 (1990), S. 485-491 
    Details
    ISSN: 1432-2072
    Schlagwort(e): Locomotor activity ; Serotonin ; 8-OH-DPAT ; Mouse ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The effects of 8-OH-DPAT on locomotor activity have not yet been clearly defined. Tricklebank et al. (1984) and Dourish et al. (1985) provide evidence that 8-OH-DPAT increases activity, whereas Mittman and Geyer (1989), Hillegaart et al. (1989) and Carli et al. (1989) suggest that it is reduced by the drug. In the present study, the effects of 8-OH-DPAT on locomotor activity and rearing were examined in habituated and unhabituated mice and rats. The effects of the drug were followed for up to 2 h in the mouse and up to 4 h in the rat. In unhabituated mice and rats, doses of 0.1 mg/kg or more of 8-OH-DPAT blocked activity during the period post-injection when control levels of activity were highest. However, after about 60 min in mice and 150 min in the rat a marked hyperactivity was observed, which was followed by a period of increased rearing. In habituated mice this biphasic effect on locomotor activity was also observed, but there was no increase in rearing. In habituated rats there was no decrease in locomotor activity, rather a biphasic increase was observed. The effects of 8-OH-DPAT on locomotor activity immediately post-injection are interpreted as being a result of the stereotyped, uncoordinated “ambulation” which forms a part of the 5-HT syndrome, and which results in a level of activity intermediate between that of unhabituated and habituated rats. The mechanism by which 8-OH-DPAT produces elevated locomotor activity and increased rearing seen 60 min or more post-injection is not yet known, but may be a result of brain concentrations of the drug falling to a low, but still effective level.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02247129
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 127
    Digitale Medien
    Digitale Medien
    The effect of exercise on atropine pharmacokinetics (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 395-397 
    Details
    ISSN: 1432-1041
    Schlagwort(e): atropine ; exercise ; pharmacokinetics ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Seven healthy males (19–32 y) underwent each of four separate conditions in a repeated measures design. Five of these subjects underwent an additional trial. In four of five trials subjects received 2.0 mg atropine sulfate intramuscularly in the anterolateral portion of the left thigh: at rest (T1); following completion of a single exercise (Ex) bout (T2), (Each bout consisted of 25 min of stationary cycling at 40% VO2 max with 5 min of seated rest), prior to three Ex bouts (T3) and following one and prior to three Ex bouts (T5). Trial 4 (T4) was the same as T3 with the substitution of a saline placebo. Serum samples were collected over a 12 h period and atropine concentration was determined by RIA. Ex trials were compared to T1. Ex prior to atropine (T2) significantly decreased the mean volume of distribution (Vz, 278 vs 2321). Ex in T3 significantly decreased the serum half life (t1/2, 4.2 vs 3.5 h), Vz (278 vs 1981), and clearance (CL, 763 vs 638 ml·min−1) and significantly increased the peak concentration (Cp, 6.7 vs 12.3 ng·ml−1) and area under the curve (AUC, 44.1 vs 53.1 ng·ml−1). In T5, Ex significantly decreased the t1/2 (3.4 h), Vz (182 l) and CL (575 ml·min−1) and significantly increased the absorption rate constant (ka, 0.482 vs 1.1 min−1), elimination rate constant (ke, 0.0012 vs 0.0015 min−1), Cp (14 ng·ml−1) and AUC (53.3 ng·h·ml−1). These results demonstrate that moderate Ex either prior to and/or immediately following drug administration has the capacity to significantly modify atropine pharmacokinetics.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315417
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 128
    Digitale Medien
    Digitale Medien
    Plasma and cerebrospinal fluid concentrations of indomethacin in humans (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 343-346 
    Details
    ISSN: 1432-1041
    Schlagwort(e): indomethacin ; cerebrospinal fluid ; pharmacokinetics ; protein binding ; analgesic activity
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Plasma and cerebrospinal fluid (CSF) concentrations of indomethacin have been determined in 52 patients hospitalized for nerve-root compression pain. Samples of blood and CSF were collected at the same time in each subject, 0.5 to 12 h after a single intramuscular injection of 50 mg indomethacin. Analgesic effect was assessed by the absolute and percentage variation in Huskisson's visual analogue scale between dosing and sampling. According to its high lipid solubility, indomethacin rapidly crossed the blood-brain barrier, being detected in CSF 0.5 h after administration. After attainment of equilibrium within 2 h, the CSF level exceeded the free plasma level. Since the drug was extensively bound to serum albumin (99.7±0.1%), this phenomenon may represent a slight degree of binding of indomethacin in CSF. The analgesic activity was not related to either the plasma or CSF concentration of indomethacin.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315572
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 129
    Digitale Medien
    Digitale Medien
    Excretion of tolbutamide metabolites in young and old subjects (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 523-524 
    Details
    ISSN: 1432-1041
    Schlagwort(e): tolbutamide ; hydroxytolbutamide ; carboxytolbutamide ; urinary excretion ; age ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Tolbutamide (1 g/70 kg) was administered as a single intravenous dose to 31 healthy, non-smoking, drug-free males between 23 and 87 years old and the total amounts of hydroxy and carboxytolbutamide excreted in 24 h were measured. There was a significant decrease in the urinary recovery of both metabolites with age. The reason for these findings is not known at the present time and may be associated with the decrease in creatinine clearance observed in these subjects or other changes in the pharmacokinetics of tolbutamide which are currently being investigated.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336696
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 130
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of intravenous 2-mercaptopropionylglycine in man (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 499-503 
    Details
    ISSN: 1432-1041
    Schlagwort(e): 2-mercaptopropionylglycine ; body clearance ; half-life ; pharmacokinetics ; protein binding
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of 2-mercaptopropionylglycine (2-MPG) was studied in ten healthy volunteers after a single i. v. injection of 250 mg (1532 μmol). The total and non-protein-bound concentrations versus time curves were best described by a three-exponential function with terminal half-lives of 55 and 59 h respectively. Body clearance based upon the total concentration was estimated to be 105 and 231 ml/min based on the non-protein-bound 2-MPG. The corresponding values for Vss were 99 l and Vss,n 173 l, and for Vγ485 l and Vγ,n 1121 l respectively. 75% of the dose was excreted in the urine, mainly during the first 6 h after injection. The proportion of non-protein-bound 2-MPG diminished exponentially during the first 15 h and then levelled off at about 30%. There was a nonlinear increase in the non-protein-bound fraction of 2-MPG as the total plasma concentration of the drug increased.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336691
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 131
    Digitale Medien
    Digitale Medien
    Effect of posture on total phenytoin plasma concentration (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 526-527 
    Details
    ISSN: 1432-1041
    Schlagwort(e): phenytoin ; posture ; pharmacokinetics ; plasma levels
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336698
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 132
    Digitale Medien
    Digitale Medien
    Two-stage penetration of a single oral dose of sulphadimethoxine into skin blister fluid (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 487-490 
    Details
    ISSN: 1432-1041
    Schlagwort(e): sulphadimethoxine ; plasma concentration ; skin blister fluid concentration ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The time-dependent concentration curves of sulphadimethoxine in plasma and cantharidin-induced skin blister fluid have been evatuated following a single oral dose of 1 g. In contrast to other drugs, sulphadimethoxine exhibited two-stage penetration into the blister fluid, the second peak concentration being higher than the first. The maximum plasma concentration of 94.1 mg·l−1 was observed after 4 h, and in skin blister fluid the first peak of 25.6 mg·l−1 was found after 7 h, and the second of 58.0 mg·l−1 occurred after 30 h. The penetration of sulphadimethoxine into skin blister fluid, defined as the ratio of the AUC there to that in plasma was 0.748. The results suggest that sulphadimethoxine penetrates into skin blister fluid to a great extent from plasma and achieves concentrations exceeding the MIC for susceptible pathogens, but it requires a relatively long time to do so.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280941
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 133
    Digitale Medien
    Digitale Medien
    The pharmokinetics of isradipine in hypertensive subjects (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 209-211 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Isradipine ; hypertension ; pharmacokinetics ; pharmacodynamics ; clinical trial
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary In conjunction with a multicentre clinical trial of the calcium antagonist isradipine in hypertension, pharmacokinetic and pharmacodynamic studies were conducted in 9 subjects. An initial dose of 5 mg (capsule formulation) of isradipine was given orally. The mean Cmax, tmax and AUC(0–8) were 6.0 ng · ml−1, 1.5 h and 15.1 h · ng · ml−1 respectively. Seven subjects repeated the study at steady state after 10 week's dose titration with isradipine. Cmax, tmax and AUC(0–8) were 3.7 ng · ml−1, 1.2 h and 12.2 h · ng · ml−1 respectively indicating that the drug does not accumulate over time. Control of blood pressure paralleled plasma isradipine concentrations which suggested that the drug should be given at least twice daily. Pharmacokinetic studies performed in conjunction with clinical trials can provide valuable information about the patterns of drug response.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00265988
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 134
    Digitale Medien
    Digitale Medien
    A lack of pharmacokinetic interaction between ranitidine and piroxicam (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 583-586 
    Details
    ISSN: 1432-1041
    Schlagwort(e): ranitidine ; piroxicam ; interaction ; pharmacokinetics ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The effects of piroxicam (40 mg) on the pharmacokinetics of ranitidine (150 mg) and of ranitidine (150 mg bid) on the pharmacokinetics of piroxicam (20 mg) were assessed in two 2-way crossover studies in two groups of 18 healthy male subjects. In the first study there were no statistically significant differences between the pharmacokinetic variables for ranitidine in the presence or absence of piroxicam. The mean maximum plasma concentration (Cmax) was 467 ng·ml−1 for ranitidine alone and 466 ng·ml−1 in the presence of piroxicam; mean area under the plasma concentration vs time curve (AUC) was 2460 h·ng ml−1 and 2551 h·ng ml−1 respectively; and the mean terminal half-life (t 1/2) was 3.6 h and 3.8 h respectively. In the second study there were no statistically significant differences between the pharmacokinetic variables for piroxicam in the presence or absence of ranitidine. The mean Cmax was 2.1 μ·ml−1 in the presence of placebo and 2.0 μg·ml−1 in the presence of ranitidine respectively; mean AUC was 133 h·μg ml−1 and 137 h·μg ml−1 respectively, and the mean t 1/2 was 53.6 h and 54.5 h respectively.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316100
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 135
    Digitale Medien
    Digitale Medien
    Clinical implications of slow sulphoxidation of thioridazine in a poor metabolizer of the debrisoquine type (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 613-614 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Thioridazine ; debrisoquine polymorphism ; pharmacokinetics ; adverse effects
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316110
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 136
    Digitale Medien
    Digitale Medien
    Effect of mequitazine on the pharmacokinetics of theophylline in asthmatic patients (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 255-258 
    Details
    ISSN: 1432-1041
    Schlagwort(e): theophylline ; mequitazine ; drug interaction ; pharmacokinetics ; asthma
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The effect of an oral anti-allergic drug, mequitazine, on the pharmacokinetics of theophylline has been investigated in seven asthmatic patients. They received chronic theophylline therapy (a sustained-release theophylline tablet 200–400 mg b.d. at 12 h intervals) and coadministered mequitazine 6 mg for 3 weeks. Plasma theophylline concentration-time curves and the urinary excretion of theophylline and its major metabolites before and after coadministration of mequitazine were compared. No significant change in the pharmacokinetic parameters of theophylline or in the urinary recovery of unchanged drug and its metabolites was observed. Thus, mequitazine did not influence the pharmacokinetics of theophylline and it should be safe for coadministration to asthmatic patients on chronic theophylline therapy.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315026
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 137
    Digitale Medien
    Digitale Medien
    Clinical pharmacokinetics of intravenous and oral 9-amino-1,2,3,4-tetrahydroacridine, tacrine (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 259-263 
    Details
    ISSN: 1432-1041
    Schlagwort(e): tacrine ; amyotrophic lateral sclerosis ; postoperative sedation ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of 9-amino-1,2,3,4-tetrahydroacridine; tacrine, THA, was studied after intravenous administration and following the first and last oral doses of a seven week clinical trial involving 8 patients with amyotrophic lateral sclerosis, ALS. Two surgical patients given intravenous THA for reversal of postoperative sedation were also included. Plasma concentration of THA and in some cases the metabolite, 1-hydroxy-THA, were assayed using a selective and sensitive method with high performance liquid chromatography. After an intravenous dose of 30 mg THA, the plasma concentrations were fitted to a two-compartment model. Plasma clearance showed a threefold interindividual variation with a mean of 2.42 l·h−1. Volume of distribution, Vα varied 100–680 l with a mean of 349 l. The plasma half-lives of distribution and elimination were 1.8 and 98.2 min, respectively. Oral bioavailability showed large interindividual differences and ranged 6–36% in the four subjects studied. After seven weeks treatment with oral THA, plasma concentrations immediately prior to medication were below 10 ng/ml in three patients and above 100 ng/ml in two patients. At the same occasion the plasma metabolite concentrations considerably exceeded those of THA. THA medication was associated with side effects in the majority of the patients.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315027
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 138
    Digitale Medien
    Digitale Medien
    Altered flecainide disposition in healthy volunteers taking quinine (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 269-273 
    Details
    ISSN: 1432-1041
    Schlagwort(e): flecainide ; quinine ; pharmacokinetics ; metabolism inhibition ; drug interaction ; renal transport
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of flecainide and its two sequential metabolites, both free and conjugated, its pharmacodynamics, and the influence of simultaneously administered quinine, have been studied in 10 healthy subjects. The study comprised two, 48-h open phases at an interval of 1 week. Flecainide acetate 150 mg was given as a 30-min i.v. infusion and quinine sulphate orally 500 mg×3 over 24 h. Quinine administration did not change the apparent volume of distribution or the renal clearance of flecainide, but it significantly reduced its systemic clearance (9.2 vs 7.6 ml · kg−1 · min−1), thus increasing the elimination half-life (9.6 vs 11.5 h). The amount of flecainide transformed to its first, meta-O-dealkylated metabolite (MODF) fell with no change in the renal excretion of the latter, either in its free or conjugated forms. This finding, in association with a fall in amount of the second, meta-O-dealkylated lactam metabolite (MODLF) recovered in its conjugated forms in the urine, suggests that quinine inhibits both the first and the second steps of the sequential metabolism of flecainide. When the subjects received quinine in addition to flecainide, the PR interval in the ECG was slightly more prolonged than with flecainide alone. Due to the study design, an effect of quinine per se and the consequence of increased serum flecainide levels could not be distinguished.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315029
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 139
    Digitale Medien
    Digitale Medien
    Comparative enantioselective pharmacokinetic studies of celiprolol in healthy volunteers and patients with impaired renal function (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 573-576 
    Details
    ISSN: 1432-1041
    Schlagwort(e): celiprolol ; renal failure ; pharmacokinetics ; enantioselective kinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of the ß1-selective adrenergic antagonist (R,S)-celiprolol has been studied after oral administration of 200 mg celiprolol-HCl to 8 healthy volunteers and 8 patients with various degrees of impaired renal function. No significant difference was found between the two enantiomers in the control group or in the patients. In healthy volunteers an average of 9.8% of the dose of R-(+)-celiprolol and 9.5% of S-(-)-celiprolol was recovered unchanged in the urine. Renal impairment reduced the urinary excretion of both enantiomers to the same extent according to the severity of the uraemia, producing higher AUCs. Nevertheless, the terminal half-lives of the R- and S-enantiomers were not significantly different between the groups. Dosage reduction in patients with renal impairment does not seem to be necessary.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316098
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 140
    Digitale Medien
    Digitale Medien
    Relationship between pharmacokinetics and hemodynamic tolerance to isosorbide-5-mononitrate (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. S53 
    Details
    ISSN: 1432-1041
    Schlagwort(e): nitrates ; pharmacokinetics ; pharmacodynamics ; nitrate tolerance ; isosorbide-5-mononitrate
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Healthy male volunteers received three different dose regimens of a controlled-release form of isosorbide-5-mononitrate (IS-5-MN; 60 mg per tablet). Dose regimen I consisted of a single daily dose of 60 mg given for 5 days. Dose regimen 11 was started with a dose of 60 mg, followed by 30 mg 12 h later and thereafter every 8 h. The last dose, on the 5th day was again 60 mg. In dose regimen III60 mg followed by 30 mg 6 h later were administered every day for 5 days. The peripheral arterial and venous effects of IS-5-MN during the first and last dosing interval were followed by changes in the finger pulse curve, standing systolic blood pressure, heart rate, and venous distensibility. Plasma concentrations of IS-5-MN were measured frequently following the first and the last dose. Following dose regimen I all hemodynamic effects produced by the first dose were maintained during the study. The maximal plasma concentrations were about 400 ng/ml and the trough value, lower than 100 ng/ml. Following dose regimen II the hemodynamic effects of IS-5-MN and sublingual glyceroltrinitrate were completely abolished on the 5th day. Trough plasma concentrations were approximately 300 ng/ml during the entire study period. Following dose regimen III pronounced hemodynamic effects were seen on the 1st day. However, a significant attenuation of the hemodynamic effects was measured on the 5th day, when trough plasma concentrations were between 100 and 230 ng/ml. There was a significant negative correlation between the magnitude of hemodynamic effect remaining on the 5th day (measured by the area under the finger pulse curve) and the trough plasma concentration. Thus, the maintenance of minimum plasma concentrations of IS-5MN of 300 ng/ml or higher produces a rapid development of hemodynamic nitrate tolerance, whereas no tolerance was found when the plasma concentrations were allowed to decline below 100 ng/ml before the next dose was given. A significant attenuation of hemodynamic effects was found when minimum plasma concentrations were between 100 and 230 ng/ml. The degree of attenuation in this concentration range increased with increasing trough plasma concentrations.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01417565
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 141
    Digitale Medien
    Digitale Medien
    Testicular effects of di-n-butyl phthalate (DBP): Biochemical and histopathological alterations (1990)
    Springer
    Archives of toxicology 64 (1990), S. 148-152 
    Details
    ISSN: 1432-0738
    Schlagwort(e): Di-n-butyl phthalate ; Testes ; Rat ; Toxicity
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Di-n-butyl phthalate (DBP) was administered to young male rats by gavage at the doses of 250, 500 and 1000 mg/kg body weight/day for 15 days. A significant decrease in testes weight was observed at 500 and 1000 mg/kg doses of DBP. Histopathological examination revealed marked degeneration of seminiferous tubules. The activities of testicular enzymes associated with postmeiotic spermatogenic cells, such as sorbitol dehydrogenase and acid phosphatase, were decreased significantly, while that of lactate dehydrogenase was significantly increased, coincident with degeneration of spermatogenic cells. The activities of enzymes associated with premeiotic spermatogenic cells, Sertoli cells or interstitial cells, β-glucuronidase, γ-glutamyl transpeptidase and glucose-6-phosphate dehydrogenase were significantly increased. Thus the alterations in activity of these testicular cell specific enzymes suggest that DBP exposure during early life could affect the testicular functions.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01974401
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 142
    Digitale Medien
    Digitale Medien
    Seasonal effects on the daily variations of gentamicin — induced nephrotoxicity (1990)
    Springer
    Archives of toxicology 64 (1990), S. 205-209 
    Details
    ISSN: 1432-0738
    Schlagwort(e): Chronotoxicology ; Renal toxicity ; Gentamicin ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The effect on kidney damage of the season of year at which gentamicin was administered to rats was studied. Rats received a single intramuscular dose of 200 mg/kg gentamicin at four different times of the day (08.00, 14.00, 20.00 or 02.00 hours. Studies were carried out in January–February, March–April, June–July and October–November. The nephrotoxicity was assessed by the increase of three urinary enzymes: two brush border enzymes, gamma-glutamyl transferase and alanine aminopeptidase, and a lysosomial enzyme: N-acetyl-β-d-glucosaminidase. The results show that when the injection is administered at 20.00 hours in the January–February and the October–November studies and at 08.00 hours in the March–April study and at 14.00 hours in the June–July study there is a significant increase in the excretion of these enzymes. The renal toxicity of gentamicin therefore has circadian variations as well as seasonal variations. The peak enzyme level is displaced from the start to the end of the rest period of rats depending upon the time of year.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02010726
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 143
    Digitale Medien
    Digitale Medien
    Single-dose toxicokinetics ofN-nitrosomethylethylamine andN-nitrosomethyl (2,2,2-trideuterioethyl)amine in the rat (1990)
    Springer
    Archives of toxicology 64 (1990), S. 109-115 
    Details
    ISSN: 1432-0738
    Schlagwort(e): N-Nitrosomethylethylamine ; Deuterium isotope effect ; N-Nitrosomethyl(2,2,2-trideuterioethyl)amine ; Toxicokinetics ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract To investigate the origins of an organotropic shift toward increasing esophageal carcinogenicity and DNA alkylation caused by β-trideuteration of the hepatocarcinogen,N-nitrosomethylethylamine (NMEA), the single-dose toxicokinetics of NMEA andN-nitrosomethyl(2,2,2-trideuterioethyl)amine (NMEA-d 3) has been characterized in 8-week-old male Fischer 344 rats by analysis using high performance liquid chromatography of serial blood samples. An i.v. bolus dose of 0.6 μmol/kg to rats revealed biphasic first order elimination with a terminal half-life of 9.46 ± 0.69 min for unchanged NMEA and 28.9 ± 2.4 min for total radioactivity. Extensive conversion to polar metabolites was observed in the chromatograms. The systemic blood clearance and apparent steadystate volume of distribution for unchanged NMEA were 39.9 ± 4.6 ml/min/kg and 496 ± 36 ml/kg, respectively. There was negligible plasma protein binding and no detectable NMEA was excreted unchanged in the urine. Larger doses given by gavage indicated a systemic bioavailability of 25 ± 1%. Similar doses of NMEA-d 3 given to other groups of rats revealed no significant differences in any of the toxicokinetic parameters. NoN-nitrosomethyl (2-hydroxyethyl)amine was found as a detectable metabolite of NMEA or NMEA-d 3 in any of the blood or urine samples which were analyzed. When considered together, the data suggest that previously observed differences in organ specificity for the carcinogens, NMEA and NMEA-d 3, are not due to differences in the total amounts of nitrosamine reaching particular tissues, but may have other localized causes such as differences in the enzymes responsible for metabolism which are present in each tissue. Such differences may make too small a contribution to the total systemic clearance to be detectable in that parameter, but at the level of the fraction of a dose that alkylates DNA they may be important.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01974395
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 144
    Digitale Medien
    Digitale Medien
    Alteration of rat liver microsomal monooxygenase activities by gasoline treatment (1990)
    Springer
    Archives of toxicology 64 (1990), S. 677-679 
    Details
    ISSN: 1432-0738
    Schlagwort(e): Gasoline ; Rat ; Liver ; Microsomal mono- oxygenase activity
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Previous work has shown an increase in rat liver enzyme activities after chronic exposure to gasoline vapor. In the present study, male Sprague-Dawley rats were pretreated with unleaded gasoline at 1 and 5 ml/kg, i.p., and selected hepatic microsomal monooxygenase activities were determined at 18, 48, and 72 h. At 18 h, moderate increases were observed in P450 content (1.3-fold), cytochromec-reductase activity (1.25-fold), and inN-nitrosodimethylamine demethylation rate (1.25- to 1.6-fold). Pentoxyresorufin dealkylase activity (an activity displayed primarily by P450IIB1) was significantly elevated at 18 and 48 h (30- to 60-fold), and ethoxyresorufin dealkylase activity (an activity displayed by P450 IA1) was elevated (2- to 4-fold). Immunoblot analysis revealed no change in P450IIE1 at these time points, but an elevation in P450IIB1 in agreement with the pentoxyresorufin dealkylase activity measurements.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01974697
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 145
    Digitale Medien
    Digitale Medien
    Distribution of three common chlorophenoxyacetic acid herbicides into the rat brain (1990)
    Springer
    Archives of toxicology 64 (1990), S. 61-65 
    Details
    ISSN: 1432-0738
    Schlagwort(e): Chlorophenoxy acids ; Herbicides ; Pesticides ; Blood-brain barrier ; Protein binding ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The distribution of three common14C-labelled chlorophenoxyacetic acid herbicides (2,4-dichlorophenoxyacetic acid or 2,4-D, 2-methyl-4-chlorophenoxyacetic acid or MCPA, 2,4,5-trichlorophenoxyacetic acid or 2,4,5-T) into the different brain areas was studied in rats pretreated with toxic doses of the herbicides (238–475 mg/ kg). Also, their binding to proteins in rat plasma was determined in vitro by increasing the concentrations of chlorophenoxyacetic acids in the incubate from 0 to 1 mg/ml. Both 2,4-D and MCPA pretreatments increased brain concentrations of14C-labelled herbicides more markedly than 2,4,5-T pretreatments did. No essential differences were found in the distribution between the different brain areas. Protein-unbound fractions of 2,4-D and MCPA in the plasma were clearly higher than those of 2,4,5-T but the highest herbicide concentration increased the protein-unbound fraction of 2,4,5-T more (7-13-fold) than of 2,4-D and MCPA (5-fold). The results suggest that the greater increase in the penetration into the brain of 2,4-D and MCPA than of 2,4,5-T during their intoxication is due to some factors other than the changes in their binding to plasma proteins and mere enhanced diffusion through the blood-brain barrier.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01973378
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 146
    Digitale Medien
    Digitale Medien
    Placental transfer of metals of coal fly ash into various fetal organs of rat (1990)
    Springer
    Archives of toxicology 64 (1990), S. 153-156 
    Details
    ISSN: 1432-0738
    Schlagwort(e): Fly ash ; Metals ; Distribution ; Organs ; Rat ; Fetus
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Fly ash (100 mg/kg body weight) was administered intratracheally to 14-day pregnant rats for 6 consecutive days. On day 20 of gestation the translocation of metals present in the fly ash to various maternal and fetal organs was studied. Fly ash administration to pregnant mothers retarded the growth of fetal heart and kidney as determined by their weights. Fly ash instillation increased organ levels of nearly all the metals studied in both mother and fetus. Most of the metals present in coal fly ash were transferred in significant amounts through placenta to several fetal organs. However, the pattern of their distribution into various fetal organs was different for different metals.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01974402
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 147
    Digitale Medien
    Digitale Medien
    Pulmonary toxicity of inhaled styrene in acetone-, phenobarbital- and 3-methylcholanthrene-treated rats (1990)
    Springer
    Archives of toxicology 64 (1990), S. 365-369 
    Details
    ISSN: 1432-0738
    Schlagwort(e): Styrene inhalation ; Phenobarbital ; Methylcholanthrene ; Acetone ; Microsomal drug-metabolizing enzymes ; Glutathione ; Thioethers ; Lung ; Liver ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Pulmonary changes in glutathione (GSH) indicated by the concentration of non-protein sulphydryls showed a decrease of 43% in rats exposed for 5 h per day three times to 500 cm3/m3 (2100 mg/m3) styrene vapour. In these rats, only a marginal decrease was observed in the pulmonary cytochrome P450 oxidative metabolism. Following a single 24-h inhalation exposure to 500 cm3/m3 styrene, the decreases in GSH were 66% in lung but only 16% in liver. On the other hand, a multifold increase in the disposition of thioether compounds was found in urine. Pulmonary cytochrome P450-dependent metabolism was decreased, shown by low residual activities of 7-ethoxyresorufin (〈20%), 7-ethoxycoumarin (53%) and 7-pentoxyresorufin O-dealkylases (76%). Epoxide hydrolase and GSH S-transferase enzyme activities which catalyze styrene detoxification were not decreased. Styrene exposure (24 h) of acetone-, phénobarbitalor 3-methylcholanthrene-pretreated rats resulted in pulmonary effects different from each other and from those of styrene alone. Acetone potentiated the lung effect and elevated 1.5-fold urine thioether output. Inducer pretreatment seemed to be a factor aggravating styrene toxicity; in effect this was clearest in acetone-induced rats. In general, GSH depletion accompanied by inhibition of cytochrome P450-dependent oxidative drug metabolism were the earliest biochemical lesions manifested in styrene-exposed lung.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01973457
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 148
    Digitale Medien
    Digitale Medien
    Bioinequivalence of marketed diltiazem preparations (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 189-190 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Diltiazem ; bioinequivalence ; plasma concentration ; dissolution ; pharmacokinetics ; commercial brands
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary A bioequivalence study of three brands of regular diltiazem — Angizem (A), Dilzem (B) and Herbesser (C) has been carried out in 5 healthy, male volunteers. After a single oral dose of 60 mg of each preparation, the mean AUC(0–8 h) and Cmax of preparation B was significantly higher than of brands A and C. The tmax of A and B was significantly lower than of C. B had a higher dissolution rate in vitro (98.8% dissolved in 45 min) than A and C. Thus, there was bioinequivalence of the three brands of diltiazem, due partly to differences in dissolution and perhaps in part to a first pass effect.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280058
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 149
    Digitale Medien
    Digitale Medien
    Chronokinetic study of netilmicin in man (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 199-201 
    Details
    ISSN: 1432-1041
    Schlagwort(e): netilmicin ; pharmacokinetics ; diurnal variation ; circadian rhythm
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Netilmicin 1.5 mg/kg body weight was administered intravenously every 8 h for 2 days to 8 patients with normal renal function. Significant elevation of mean and trough plasma concentrations was found at 05.00 h and 09.00 h. This was considered to be due to circadian variation, with possible accumulation during the night. The clinical importance of this phenomenon in relation to the development of aminoglycoside toxicity awaits further investigation.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280062
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 150
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and metabolism of iodo-doxorubicin and doxorubicin in humans (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 507-513 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Anthracyclines ; cancer patients ; iodo-doxorubicin ; doxorubicin ; pharmacokinetics ; metabolism
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of doxorubicin (DOX), iodo-doxorubicin (I-DOX) and their metabolites in plasma has been examined in five patients each receiving 50 mg/m2 of both anthracyclines as a bolus injection. Terminal half-life, mean residence time (MRT), peak plasma concentration Cmax, and area under the curve (AUC) appeared smaller for I-DOX, whereas its plasma clearance (CLp) and volume of distribution at steady state (Vss) were larger than for DOX. The major metabolite of I-DOX was iodo-doxorubicinol (I-AOL) followed by doxorubicinol aglycone (AOLON). The AUC of I-AOL was 6-times larger than that of its counterpart AOL, which is the major metabolite of DOX. AOLON generated after I-DOX administration is a further important metabolite, as its AUC was 10-times larger than that of AOLON generated from DOX. The other aglycones, such as doxorubicin aglycone (AON) and the 7-deoxy-aglycones were only minor metabolites after either I-DOX or DOX injection. The ratio AUCI-AOL/AOL/AUCI-DOX/DOX was 27 in the case of I-DOX and 0.4 after DOX. The terminal half-lives of the cytostatic metabolites I-AOL and AOL were similar, although a longer MRT for AOL was calculated. Both metabolites had much longer MRTs than their parent drugs. The MRTs of the aglycones AOLON and AON were greater than those of the 7-deoxy-aglycones after both I-DOX and DOX. Approximately 6% DOX and less than 1% I-DOX were excreted by the kidneys during the initial 48 h. About 5% of I-DOX was excreted via the kidneys as I-AOL. Aglycones were not detected in significant amounts. The plasma concentrations of all compounds measured were highest during the first few minutes after administration of I-DOX and DOX. The I-AOL concentration was comparable to that of I-DOX immediately after the injection, due to very rapid metabolism within the central compartment (vascular space) by the aldoketo reductase system in the erythrocytes. The plasma concentration-time curves of (7d)-aglycones showed a second peak between 2 and 9 h after injection, suggesting enterohepatic circulation of metabolites lacking the daunosamine sugar moiety.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280945
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 151
    Digitale Medien
    Digitale Medien
    Rapid and slow benzbromarone elimination phenotypes in man: benzbromarone and metabolite profiles (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 577-581 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Benzbromarone ; elimination phenotypes ; pharmacokinetics ; metabolism ; genetic variation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Following oral administration of the uricosuric drug benzbromarone two major metabolites appear in the circulation, 1'-hydroxy-benzbromarone (M1), and a second product (M2) of unknown structure. The plasma concentrations of the parent drug and of M1 and M2 have now been compared in two different elimination phenotypes, 10 subjects who eliminated the drug rapidly (S1–10) and one individual (S11) whose elimination capacity was impaired, presumably due to genetic variation (S11). The AUC (0–96) of the parent drug in S11 was 145 gmg · ml−1 h, and in the other individuals it averaged 18.3 (11.4–24.5) μg · ml−1 h. The plasma elimination half life of benzbromarone was 3.34 (1.77–5.24) h in the rapid eliminators, and 13.08 h in the subject with the elimination defect. The mean plasma elimination half life of the metabolites in S1–10 amounted to 20.1 (11.9–41.2) h for M1, and 17.2 (12.9–30.7) h for M2. In S11 the plasma elimination half life of M1 was prolonged to 76.6 h, and of M2 to 75.4 h. Thus, the elimination defect in S11 was not restricted to the parent drug, but it also involved the two major metabolites M1 and M2. This might be a consequence of a hepatic enzyme deficiency, or be due to impairment of drug excretion.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316099
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 152
    Digitale Medien
    Digitale Medien
    Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 603-605 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Galanthamine ; Alzheimer's disease ; stereoselectivity ; cholinesterase inhibition ; side effects ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The effect of galanthamine (GAL) and its 2 major metabolites on human cholinesterases has been explored. Epigalanthamine, a diastereomer of GAL, was 130-times less potent in vitro in its effect on acetylcholinesterase (AChE) in erythrocytes than the parent compound, and it did not differ significantly from the ketone galanthaminone. In vivo, the maximal 36–55% inhibition of AChE was approached 30 min after oral administration of 10 mg GAL. The duration of the catalytic inhibition corresponded to an elimination half-life of approximately 5–7 h. GAL was well tolerated in 8/8 healthy volunteers, and 3/4 Alzheimer patients tolerated the drug up to a daily dose of 40 mg.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316106
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 153
    Digitale Medien
    Digitale Medien
    Effect of ponsinomycin on cyclosporin pharmacokinetics (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 165-167 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Cyclosporin A ; ponsinomycin ; pharmacokinetics ; drug interaction ; macrolide antibiotic ; renal transplantation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The influence of treatment with ponsinomycin, a new macrolide antibiotic, on the pharmacokinetics of cyclosporin A has been studied in 10 renal transplant patients. The pharmacokinetics of cyclosporin A was investigated at steady state, before and during treatment with ponsinomycin. On average, the blood levels of cyclosporin A were doubled by the macrolide, possibly due to a decrease in elimination or/and to an increase in absorption. Ponsinomycin should be use very carefully in patients treated with cyclosporin A.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280052
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 154
    Digitale Medien
    Digitale Medien
    A multiple dose pharmacokinetic and tolerance study of once daily 200 mg sustained-release flurbiprofen capsules in young and very elderly patients (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 267-270 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Flurbiprofen ; sustained-release formulation ; tolerance ; pharmacokinetics ; adverse reaction
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetic profile of 200 mg sustained-release flurbiprofen capsules was compared in nine elderly (mean age 84.2 years) and 10 young (mean age 38.1 years) patients with arthritis. After a single capsule, a 48 h plasma concentration profile was performed. The patients then took 1 capsule daily for a further 13 days with plasma levels of the drug being measured pre-dose on alternate days. Following ingestion of the last capsule, a further 48 hour plasma concentration profile was performed. These results were compared with each other and with computer predicted data obtained from dosing with 200 mg conventional flurbiprofen (as 100 mg b.d.). In both young and elderly patients, the two 48 h plasma concentration profiles confirmed the sustained-release characteristics of the capsule. There was no evidence of dose-dumping, although, in one elderly patient with a partial gastrectomy, higher plasma concentrations were observed. Inter- and intra-patient variability was acceptable. A steady-state was achieved within the predicted four days in both groups and there was no evidence of accumulation with the daily dosing interval. A mean steady-state level of approximately 6 μg/ml was achieved for both populations. Computer predicted data for 200 mg conventional flurbiprofen (as 100 mg b.d.) showed a pre-dose/peak range of 1–12 μg/ml. The pre-dose/peak ranges for the young and old patients were 4–10 μg/ml and 4–8 μg/ml respectively. One young patient developed a hypersensitivity reaction of moderate severity; one young and four elderly patients developed a low haemoglobin concentration during the study. No other changes in haematological or biochemical parameters were seen.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315108
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 155
    Digitale Medien
    Digitale Medien
    Influence of food on the bioavailability of metoprolol from an OROS system; a study in healthy volunteers (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 315-316 
    Details
    ISSN: 1432-1041
    Schlagwort(e): metoprolol ; oral osmotic drug delivery system (OROS) ; food intake ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The influence of food intake on the bioavailability of metoprolol from an OROS system has been investigated. No significant difference was found between OROS administration to fasting subjects or after breakfast in any of the kinetic parameters (AUC, Cmax, tmax, C24 and lag time). Therefore, metoprolol OROS can be administered with breakfast.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315121
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 156
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and effects of levodopa in advanced Parkinson's disease (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 385-389 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Levodopa ; Parkinson's disease ; pharmacokinetics ; pharmacodynamics ; modeling
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Five patients with severe Parkinson's disease were characterized with respect to their pharmacokinetic and pharmacodynamic responses to levodopa given: orally, intravenously (three different infusion rates) and intraduodenally. The best therapeutic infusion rate in the intravenous study was used for the intraduodenal infusion of levodopa. A lag time between plasma concentration and effect following oral administration was seen in three of the five patients and this disequilibrium was estimated as the rate constant ke0 using model-independent analysis. The plasma concentration-effect relationship was similar for the three modes of administration and in all patients the therapeutic plasma concentration for full mobility was 〉4–5 μg·ml−1. The disequilibrium half-life for development of effect after oral administration was calculated to be about 30 min. The patients remained clinically stable during the period of the intraduodenal infusion.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315415
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 157
    Digitale Medien
    Digitale Medien
    Pharmacokinetics after a single oral dose of bopindolol in patients with cirrhosis (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 569-572 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Bopindolol ; cirrhosis ; antipyrine ; pharmacokinetics ; side effects
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The plasma concentration-time curve of the hydrolysis product of bopindolol has been investigated in 14 patients with cirrhosis and in 15 healthy volunteers given a single oral dose of 2 mg bopindolol. Cirrhosis was confirmed by history and clinical examination or liver biopsy. The time to maximum concentration, maximum concentration and AUC of hydrolyzed bopindolol were similar in the patients and controls. However, the elimination half-life was 6.0 h in controls and 9.5 h in cirrhotics. Antipyrine clearance was markedly decreased in patients with cirrhosis, but no correlation was found with the pharmacokinetic parameters of hydrolysed bopindolol. Although the AUC was not significantly altered in patients with cirrhosis, the longer half-life of hydrolysed bopindolol suggests impairment of its disposition in liver disease, which could lead to significant accumulation of drug during chronic dosing.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316097
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 158
    Digitale Medien
    Digitale Medien
    Digoxin infusion versus bolus injection in rapid atrial fibrillation: relation between serum level and response (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 335-341 
    Details
    ISSN: 1432-1041
    Schlagwort(e): digoxin ; atrial fibrillation ; infusion ; pharmacokinetics ; simulation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Using available data on time-concentration and time-effect relationships in normal persons the results of infusion of digoxin in various time periods were simulated and compared with administration of digoxin by bolus injections, using a three-compartment pharmacokinetic model to which a separate small side-effect compartment was subsequently added. The validity of the simulations was tested in 11 patients with rapid atrial fibrillation. Serum digoxin concentrations, ventricular rate and side effects were monitored in a double-blind study comparing an infusion of 1.5 mg digoxin over 6 h with administration of three bolus injections of 0.5 mg digoxin 8 h apart. In agreement with the predictions of the model, the maximal fall in ventricular rate was reached after 8–9 h in the infusion group and after 19–20 h in the bolus injection group, without any detectable difference in side effects. There were certain discrepancies between the results of the clinical study and the predictions of the model, e.g. in serum digoxin concentrations, perhaps due to impaired clearance in the patients. However, it is concluded that the tested model is valid in elderly patients with rapid atrial fibrillation.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315571
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 159
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and pharmacodynamics of the ace inhibitor benazepril hydrochloride in the elderly (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 379-385 
    Details
    ISSN: 1432-1041
    Schlagwort(e): benazepril ; benazeprilat ; ACE inhibitor ; pharmacokinetics ; pharmacodynamics ; elderly ; adverse effects
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics and pharmacodynamics of a single oral dose benazepril·HCl 10 mg have been studied in 15 healthy volunteers aged 65 to 80 y. The kinetics of unchanged benazepril and its active metabolite benazeprilat did not differ significantly in males and females, so the combined kinetic data from all 15 elderly subjects were compared with a historical control group of 19–32 year-old healthy men treated in the same way. The disposition of benazepril was not affected by age. The time to maximum plasma concentration, tmax (0.5 h) and elimination half-life (0.6 h) in the elderly were the same as in young subjects. The kinetics of benazeprilat was slightly changed in the elderly; although its tmax (1.5 h) was not affected, Cmax and the AUC were 20–40% greater. The elimination half-life of benazeprilat during the first 24 h after doing in the elderly was increased by about 20% to 3.2 h. The renal plasma clearance of benazeprilat (18.1 ml·min−1) was about 20% smaller than in the young subjects. An average of 18.5% of the dose was recovered as benazeprilat in the 24 h urine from the elderly subjects, which was similar to the recovery in the young subjects. Both benazepril and benazeprilat were highly bound to serum proteins (96 and 95%, respectively). Mean systolic and diastolic blood pressures in the elderly were reduced by a maximum of 37/16 mm Hg at 6 h, in association with a small rise in pulse rate. Treatment was generally well tolerated. Three of the 15 subjects reported clinical adverse experiences judged to be possibly drug related, namely headache, abdominal pain and cold extremities.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315579
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 160
    Digitale Medien
    Digitale Medien
    Uricosuric effect of different doses of irtemazole in normouricaemic subjects (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 489-491 
    Details
    ISSN: 1432-1041
    Schlagwort(e): irtemazole ; dose-response relationship ; pharmacokinetics ; uricosuric drugs ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Irtemazole 12.5 to 50 mg in 6 healthy, normouricaemic subjects caused a maximal decrease in plasma uric acid (after 8 to 12 h) of 46.5%. The uricosuric effect began during the first 60 min after drug administration and it lasted for 7 to 24 h. Renal uric acid excretion returned to its base line value after 8 to 16 h and uric acid clearance after 10.0 to 12.0 h. Doses of irtemazole between 12.5 and 37.5 mg produced a dose-related rise in the uricosuric effect. There was no essential difference between the uricosuric effect of 37.5 mg and 50 mg irtemazole. The D50 dose (that producing a half-maximal effect) was between 16.3 mg and 34.2 mg, (average 24.7 mg). The value of irtemazole in the management of hyperuricaemia and gout remains to be determined.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336689
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 161
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of S(+)- and R(−)-ibuprofen in volunteers and first clinical experience of S(+)-ibuprofen in rheumatoid arthritis (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 493-497 
    Details
    ISSN: 1432-1041
    Schlagwort(e): ibuprofen ; rheumatoid arthritis ; enantiomer ; stereoselectivity ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary S(+)-, R(−)- or racemic ibuprofen was administered orally to volunteers in doses of 150 mg, 300 mg and 500 mg pure S(+)-, 300 mg pure R(−)- and 600 mg racemic ibuprofen. The pharmacokinetic parameters in humans showed that S(+)-ibuprofen was not inverted to R(−)-ibuprofen, whereas R(−)-ibuprofen was inverted to S(+)-ibuprofen to a variable degree. S(+)-ibuprofen and R(−)-ibuprofen given alone more rapidly reached significantly higher maximal plasma concentrations than after the same doses of the racemic compound. The elimination half-lives and clearance values for all three forms of ibuprofen were comparable. The mean residence time of S(+)-ibuprofen after R(−)- and racemic ibuprofen was significantly longer than after administration of the pure S(+)-enantiomer. Judged by the AUC, the bioavailability of S(+)-ibuprofen was independent of the dose within the range tested. Administration of S(+)-ibuprofen to 6 rheumatic patients showed that the pharmacokinetic behaviour of S(+)-ibuprofen in patients was similar to that found in volunteers. S(+)-ibuprofen proved to be an effective analgesic antirheumatic drug in the dose range 1 to 1.5 g/day.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336690
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 162
    Digitale Medien
    Digitale Medien
    Indirect assessment of the enterohepatic recirculation of piroxicam and tenoxicam (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 547-549 
    Details
    ISSN: 1432-1041
    Schlagwort(e): piroxicam ; tenoxicam ; cholestyramine ; pharmacokinetics ; enterohepatic circulation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary To assess the extent of enterohepatic recycling of piroxicam and tenoxicam, their pharmacokinetics have been compared in the absence and presence of concomitant treatment with cholestyramine. In a randomized crossover study 6 healthy volunteers received piroxicam and tenoxicam 20 mg p.o., alone or with cholestyramine 24 g/day for 4 days. Cholestyramine increased piroxicam & tenoxicam elimination approximately 2-fold (t1/2 50.3 vs 28.1 h and 73.6 vs 35.8 h, respectively). It also increased the apparent clearance (Cl/f) of piroxicam and tenoxicam by 58% and 112%. When cholestyramine was administered, the t1/2 of piroxicam & tenoxicam were correlated (r=0.89), which suggests that their hepatic biotransformation is under a common control. It is concluded that: piroxicam and tenoxicam are eliminated to a large and comparable extent through the biliary route, and the administration of cholestyramine may help to accelerate their elimination in cases of overdosage.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278579
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 163
    Digitale Medien
    Digitale Medien
    The pharmacokinetics of d-sotalol and d,l-sotalol in healthy volunteers (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 579-582 
    Details
    ISSN: 1432-1041
    Schlagwort(e): d-sotalol ; d,l-sotalol ; pharmacokinetics ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of d-sotalol has been studied in six healthy volunteers given single doses of 0.25, 0.50, 1, 2 mg·kg−1 i.v. and one 100 mg oral dose in comparison with the kinetics of 1 mg·kg−1 i.v. of dlsotalol. There was no significant difference in the disposition of the d-enantiomer and the racemate. The terminal half-life averaged 7.2 h, and the kinetics was linear, with a mean total clearance of 0.13 l·h−1·kg−1. Renal clearance of d-sotalol represented 56 to 77% of total clearance. The absolute systemic availability of oral d-sotalol was close to 100% and the elimination half-life of the oral-d-enantiomer was similar to that of the i.v. form (7.5 h).
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278585
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 164
    Digitale Medien
    Digitale Medien
    Subjective symptoms and pharmacokinetics/dynamics of metoprolol CR in elderly subjects — a comparison with atenolol (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 571-578 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Atenolol ; metoprolol CR ; elderly subjects ; subjective symptoms ; pharmacokinetics ; pharmacodynamics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary In a double-blind, randomised, cross-over study, the pharmacokinetic/dynamic effects and subjective symptoms of a new controlled-release (CR) formulation of metoprolol (50 and 100 mg) have been compared with atenolol (50 mg) and placebo in 20 elderly healthy subjects. The metoprolol CR formulation displayed an even plasma concentration-time profile over the dosage interval while atenolol produced a peak at 2–4 h. All three active treatments produced significant β1-blockade at 24 h compared to placebo. Four hours after dose intake, the degree of β1-blockade was significantly greater with conventional atenolol 50 mg than with either dose of metoprolol CR. Subjective well-being was examined with a self-administered questionnaire (MSE-profile), including three dimensions: Contentment, Vitality and Sleep. No significant differences were detected between placebo and either dose of metoprolol CR. At 2 h, following atenolol, a deterioration in Vitality was observed compared to placebo and metoprolol CR 100 mg. At the end of the dosage interval there was no longer any significant difference between the treatments. Perceived leg fatigue during exercise, evaluated 4 h after dosing, was more pronounced during treatment with atenolol than metoprolol CR 50 mg. The results suggest that the metoprolol CR formulation was not associated with significant effects on subjective well-being, whereas atenolol caused a deterioration at the time of the peak plasma concentration of the drug.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278584
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 165
    Digitale Medien
    Digitale Medien
    Single- and multiple-dose pharmacokinetics of R-(−)- and S-(+)-prenylamine in man (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 587-593 
    Details
    ISSN: 1432-1041
    Schlagwort(e): prenylamine ; racemic drug ; stereoselectivity ; metabolism ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of S-(+)- and R-(−)-prenylamine was studied in eight healthy volunteers given single and repeated oral doses of the racemic drug. Distinct differences in various pharmacokinetic parameters were found between the S- and R-enantiomer. The maximum plasma concentrations and AUCs of the R-enantiomer exceeded those of the S-enantiomer five-fold; the apparent oral clearance of the S-form was five-times and the renal clearance three-times higher than of the R-form. Acid catalyzed hydrolysis of urine samples released more S-prenylamine, indicating stereoselective glucuronidation of unchanged prenylamine. Plasma protein binding also differed between the two enantiomers, generally with a higher unbound fraction of the S-form, whereas analysis of the bound fractions showed that prenylamine was bound to different plasma proteins with inverse stereoselectivity.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278587
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 166
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of isradipine in patients with chronic liver disease (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 599-603 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Isradipine ; cirrhosis ; systemic ; calcium antagonist ; aminopyrine breath test ; serum bile acids ; galactose elimination ; pharmacokinetics ; bioavailability
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of the dihydropyridine calcium antagonist isradipine has been examined in 8 healthy volunteers, 7 patients with non-cirrhotic chronic liver disease (CLD), and 8 patients with biopsy-proven cirrhosis (CIR). Isradipine was simultaneously given orally (12C 5 mg) and i.v. (13C 1 mg). Systemic availability was significantly increased from 17% and 16% in controls and CLD, respectively, to 37% in CIR. The corresponding systemic clearances averaged 1.1, 0.9 and 0.61 · min−1, the reduction in cirrhotics being significant. Both aminopyrine demethylation capcity, a measure of hepatic microsomal function, and indocyanine green disappearance, a measure of hepatic perfusion, were correlated with the reduction in systemic clearance, and the reduction in oral clearance was correlated with the reciprocal of the serum bile acid concentration. The loss of first-pass extraction should be considered when this calcium antagonist is given perorally in patients with hepatic cirrhosis.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278589
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 167
    Digitale Medien
    Digitale Medien
    Absorption kinetics of oral and rectal flecainide in healthy subjects (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 595-598 
    Details
    ISSN: 1432-1041
    Schlagwort(e): flecainide ; pharmacokinetics ; absorption ; non-parenteral administration ; healthy subjects ; rectal administration
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The absorption kinetics of different pharmaceutical formulations of orally and rectally administered flecainide have been assessed in a cross-over study in 7 healthy volunteers. The subjects received single doses of flecainide after a washout period of at least one week. A tablet, an oral solution, a rectal solution and a 10 min i.v. infusion during 10 min each containing 100 mg flecainide were administered to the subjects in a randomized order. The mean absolute bioavailability was 98%, 78% and 81% for the rectal and oral solutions and the tablet. The lag time after administration of the oral solution was 0.33 h and it was 0.86 h after the tablet and 0.18 h after the rectal solution. The mean time to the peak serum concentration (tmax) after the rectal solution (0.67 h) was shorter than after either the tablet (4 h) or oral solution (1 h). The maximum serum concentration (Cmax) was 0.29 mg · 1−1 after the rectal solution, 0.14 mg · 1−1 after the tablet and 0.17 mg · 1−1 after the oral solution. All the volunteers showed significantly higher serum flecainide concentrations during the first 20 min of the absorption phase after rectal administration of 100 mg flecainide as a solution compared to its oral administration. In conclusion: based on the absolute bioavailability, Cmax, tmax, and lag times, rectal administration of flecainide solution gave a better absorption profile than after oral tablet or solution.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278588
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 168
    Digitale Medien
    Digitale Medien
    Albendazole kinetics in patients with echinococcosis: Delayed absorption and impaired elimination in cholestasis (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 605-608 
    Details
    ISSN: 1432-1041
    Schlagwort(e): albendazole ; albendazole sulphoxide ; absorption ; elimination ; benzimidazole ; pharmacokinetics ; echinococcosis ; cholestasis
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of albendazole and its main metabolite, albendazole sulphoxide, have been examined after giving a single oral dose of 200 mg albendazole to 19 patients with either Echinococcus multilocularis or E. granulosus, 5 of whom had significant extrahepatic obstruction due to the underlying disease. The AUC of albendazole sulphoxide was increased in the latter patients (mean 122 μmol · h · l−1 compared to 17 μmol · h · l−1 in the non-obstructed group). Obstructed patients had delayed absorption, ka averaging 0.39 compared to 1.41 h−1 in non-obstructed patients. The corresponding elimination rate constant, ke was also prolonged, averaging 0.041 and 0.13 h−1 in the two groups, respectively. Four patients were restudied after complete or partial resolution of the cholestasis. The pharmacokinetic parameters in them had returned towards values comparable to those in the non-obstructed patients.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278590
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 169
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and endocrine effects of terguride in healthy subjects (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 609-615 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Terguride ; partial dopamine agonist ; pharmacokinetics ; endocrine effects ; pituitary hormones ; 6β-OH cortisol
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Plasma levels of the partial dopamine agonist, terguride, were measured by RIA in healthy volunteers after a single i. v. dose of 50 μg and on the first and seventh day of an oral treatment with 250 μg, 500 μg and 750 μg b. d. Basal and releasing hormone (TRH, GHRH, CRF, LHRH) — stimulated pituitary hormone secretion (PRL, TSH, GH, FSH, LH) and cortisol were also determined by RIA. Following the i. v. injection, plasma terguride levels declined biphasically, with half-lives of 0.2 and 1.5 h; total clearance was 17 ml·min−1·kg−1. the oral bioavailability of terguride over all doses was about 20%. Basal and TRH-stimulated prolactin levels were dose-dependently depressed, but the secretion of other hormones remained unaffected. Tolerance of terguride was excellent and there was no negative effect on performance or mood, nor on mixed-function oxygenase activity, assessed as urinary 6β-OH cortisol.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278591
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 170
    Digitale Medien
    Digitale Medien
    The effects of frusemide and probenecid on the pharmacokinetics of phenprocoumon (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 261-265 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Frusemide ; probenecid ; phenprocoumon ; anticoagulant ; drug interaction ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary We have studied the pharmacokinetics of phenprocoumon with and without co-administration of frusemide and probenecid in two groups of 17 healthy volunteers. Frusemide 40 mg b.i.d. for 7 days did not interact with phenprocoumon to a significant extent. Probenecid 500 mg q.i.d. for 7 days significantly accelerated the overall elimination of phenprocoumon, as indicated by a decrease in AUC from 295 to 157 μg · h · ml−1, and a reduction in the fraction of the dose excreted by the kidneys. The data are consistent with inhibition of the glucronidation of phenprocoumon by probenecid. Its accelerated elimination may be a consequence of the increased formation of hydroxylated metabolites.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315107
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 171
    Digitale Medien
    Digitale Medien
    The effect of perindopril and hydrochlorothiazide alone and in combination on blood pressure and on the renin-angiotensin system in hypertensive subjects (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 327-332 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Hypertension ; perindopril ; hydrochlorothiazide ; ACE inhibition ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacodynamic effects and acceptability of perindopril (4 mg daily) and hydrochlorothiazide (25 mg daily) given alone or in combination for 1 month were investigated in a double-blind, placebo controlled, parallel group study. The pharmacokinetics of perindopril and its active metabolite perindoprilat and the time course of angiotensin converting enzyme inhibition were studied for 72 h following the last dose of treatment in the two appropriate groups. Similar decreases in blood pressure were seen 24 h after the last dose of perindopril or hydrochlorothiazide (11/7 mm Hg supine) given alone at these doses. The effect of these drugs given together was additive on diastolic blood pressure and synergistic on systolic blood pressure (24.5/12.6 mm Hg supine) taking into account the placebo response. The significant increase in plasma renin activity produced by perindopril alone was potentiated by concurrent administration of hydrochlorothiazide. The formation of perindoprilat was slightly reduced in the group also receiving hydrochlorothiazide and there was a very small reduction in ACE inhibition in this group. Perindopril, whether given alone or in combination with hydrochlorothiazide, was well tolerated and produced no clinically significant change in routine haematology or serum biochemistry. The additive or synergistic effects of perindopril and hydrochlorothiazide on blood pressure must be due to their complementary physiological actions and not to a pharmacokinetic interaction.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315404
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 172
    Digitale Medien
    Digitale Medien
    Comparison of the diuretic effect and absorption of a single dose of furosemide and free and the fixed combinations of furosemide and triamterene in healthy male adults (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 595-597 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Furosemide ; triamterene ; drug combination ; absorption ; urine sodium ; urine potassium ; fixed combination ; healthy volunteers ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The absorption and diuretic effect of furosemide 40 mg alone (F), and of the free (F+T) and the fixed (FT) combinations of furosemide 40 mg and triamterene 50 mg have been compared in 12 healthy young men. A slight reduction in the area under the concentration-time curve (AUC) of plasma furosemide was found for the fixed combination (AUC480) F 2.58 μg · h · ml−1; F+T 2.46 μg · h · ml−1; FT 1.97 μg · h · ml−1. There was a significant reduction in the AUC480 of plasma triameterene (F+T 204.9 μg · h · l−1; FT 130.2 μg · h · l−1). Sodium excretion after F+T and FT was more pronounced than after F (F+T 302 mmol; FT 311 mmol; F 259 mmol). When compared to F alone, there was a reduction in the 24-hour potassium excretion after F+T as well as after FT (F 121 mmol; F+T 104 mmol; FT 107 mmol). It is concluded that the absorption of triamterene was significantly reduced after ingestion of the fixed combination tablet. However, in healthy male adults this had no influence on its natriuretic and potassium-sparing effect as compared to the free combination.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316104
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 173
    Digitale Medien
    Digitale Medien
    Ivermectin binds avidly to plasma proteins (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 607-608 
    Details
    ISSN: 1432-1041
    Schlagwort(e): ivermectin ; pharmacokinetics ; plasma protein binding
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Human pharmacokinetic data on the new antiparasitic agent, ivermectin, are scanty. For the evaluation of its disposition a specific HPLC assay with sensitive fluorescence detection was developed. Applying equilibrium dialysis, plasma protein binding of ivermectin was measured in five healthy individuals and it averaged 93.2±4.4% (SD). Such strong binding should be taken into consideration, especially in patients with malnutrition or with diseases in which a decrease in plasma proteins and consequently a higher free fraction of ivermectin could be expected.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00316107
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 174
    Digitale Medien
    Digitale Medien
    Effect of cimetidine and ranitidine on the hepatic and renal elimination of nicotine in humans (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 165-169 
    Details
    ISSN: 1432-1041
    Schlagwort(e): nicotine ; cimetidine ; ranitidine ; pharmacokinetics ; H2-receptor antagonists ; hepatic oxidation ; renal secretion ; tobacco smoking ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary In a randomized, double-blind, cross-over experiment, 6 healthy consenting male subjects were administered cimetidine 600 mg or ranitidine 300 mg or placebo p.o. q12h×2 days. Nicotine bitartrate was administered i.v. on day 2 (1 ug/kg/min)×30 min. After cimetidine mean nicotine total and metabolic clearances were decreased by 30% and 27% while after ranitidine the clearances were decreased by 10% and 7% respectively. Since smokers regulate their smoke intake based in large part on their nicotine blood levels these results suggest that the diminished nicotine total clearance in the presence of cimetidine could be important in assisting smoking reduction or cessation.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00265978
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 175
    Digitale Medien
    Digitale Medien
    Sex-difference and the effects of smoking and oral contraceptive steroids on the kinetics of diflunisal (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 175-179 
    Details
    ISSN: 1432-1041
    Schlagwort(e): diflunisal ; smoking ; pharmacokinetics ; sex-differences ; oral contraceptive steroids
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The single dose pharmacokinetics of diflunisal were studied in 4 groups of 6 young volunteers: control men, control women, women taking low estrogen oral contraceptive steroids (OCS), and women smokers (10–20 cigarettes/day). The plasma clearance of diflunisal was significantly higher in men (0.169 ml·min−1·kg−1) and in women on OCS (0.165 ml·min−1·kg−1) as compared to control women (0.108 ml·min−1·kg−1). Partial metabolic clearances of diflunisal by the three conjugative pathways (phenolic and acyl glucuronide formation, sulphate conjugation) were all increased in men and women OCS users as compared to control women. Statistically significant increases, however, were only observed for the partial metabolic clearance of diflunisal by phenolic glucuronidation between men and women (2.91 vs. 1.85 ml·min−1 respectively), and for the partial clearance by acyl glucuronidation between OCS users and control women (4.81 vs. 3.01 ml·min−1 respectively). Smoking resulted in a moderate increase (35%) in plasma diflunisal clearance. However, a significant reduction in total urinary recovery of diflunisal and its glucuronide and sulphate conjugates was found in smokers (70.5% in smokers as compared to 84.2–87.2% in the 3 other study groups). Consequently, smoking may have induced hydroxylation, a minor oxidative metabolic pathway of diflunisal recently discovered in man.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00265980
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 176
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of oral cyclosporin A in diabetic children and adolescents (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 181-184 
    Details
    ISSN: 1432-1041
    Schlagwort(e): cyclosporin A ; diabetic children ; pharmacokinetics ; dose adjustment
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Cyclosporin A (CsA) pharmacokinetics was studied in 19 diabetic children (mean age: 10.6 y). They were divided into prepubertal (I) and pubertal (II) groups according to plasma oestradiol or testosterone concentrations. The kinetic study was performed after a 72 h wash out period and a single oral dose of 7.5 mg/kg CsA. CsA in blood was measured by HPLC. The kinetic parameters: Cmax, tmax, t1/2, AUC, CL/f, Vz/f and tss were calculated. No significant difference was found between the two groups. A significant negative correlation was found between Vz and both total cholesterol (r=0.46), VLDL+LDL−cholesterol (r=−0.49) and VLDL+LDL−phospholipids (r=−0.58). CsA kinetics at steady-state were simulated by superimposition of single dose kinetics derived from each single dose. Measured steady-state blood concentrations were correlated (r=0.80) with the values predicted by the simulation. The results suggest that CsA adjustment dosage of the CsA may be performed after a single oral dose using blood levels measured by HPLC. This procedure requires validation in further studies.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00265981
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 177
    Digitale Medien
    Digitale Medien
    Impairment of estramustine phosphate absorption by concurrent intake of milk and food (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 189-193 
    Details
    ISSN: 1432-1041
    Schlagwort(e): estramustine phosphate ; prostatic cancer ; gastrointestinal absorption ; food intake ; calcium ; drug interaction ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The effect of milk and food on the pharmacokinetics of estramustine phosphate was investigated in six patients with prostatic cancer. In a randomized three-way cross-over study, the patients were given single doses of the drug together with low calcium water, low calcium food and milk. The evaluation was based upon the plasma concentration of two metabolites, estromustine and estrone, as parent drug could not be detected in plasma. The tmax and lag time of estromustine were significantly increased by milk and food intake and Cmax and AUC were significantly decreased. In comparison with water, the AUC of estromustine was 41% when the drug was taken with milk and 67% after simultaneous intake of standardized food. Corresponding figures for the peak values were 32 and 57%, respectively. The effect of milk and food intake on the pharmacokinetics of estrone was similar. Studies in vitro demonstrated that the dissolution of estramustine phosphate disodium was markedly impaired in the presence of calcium. It was concluded that the rate and extent of absorption of estramustine phosphate were decreased when the drug was taken with milk or food due to the formation of a poorly absorbable calcium complex. To obtain high and reproducible absorption of Estracyt®, the drug should not be taken together with milk, milk products or other calcium-rich food or drugs.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00265983
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 178
    Digitale Medien
    Digitale Medien
    Oral pharmacokinetics of pirenzepine in patients with chronic renal insufficiency, failure, and maintenance haemodialysis (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 405-406 
    Details
    ISSN: 1432-1041
    Schlagwort(e): pirenzepine ; renal insufficiency ; haemodialysis ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetic properties of pirenzepine following administration of a single, 50 mg oral dose were evaluated in three groups of subjects: group I, end stage renal disease requiring maintenance haemodialysis (CLCR 0 to 10 ml·min−1); group II, moderate renal insufficiency (CLCR 10 to 30 ml·min−1); and group III, mild renal dysfunction (CLCR 30 to 70 ml·min−1). Additionally, subjects in group I received a 50 mg dose on a non-dialysis day and at least one week later, a 50 mg dose during haemodialysis. There was a linear relationship (r = 0.97) between pirenzepine renal clearance and renal function as measured by creatinine clearance. The harmonic mean terminal half-life for pirenzepine was 17.3 h in subjects with end stage renal disease, 18.0 h in subjects with moderate renal insufficiency and 14.7 h in subjects with mild renal dysfunction. Haemodialysis reduced the level of circulating pirenzepine by approximately 25%. The mean arterial to venous plasma pirenzepine ratio during hemodialysis was 1.29 (range 1.02–1.56). Based on subjective reporting of adverse experiences and clinical observation, pirenzepine appeared to have had a wide margin of safety in these patients. Dry mouth was the most frequently reported adverse experience attributable to pirenzepine administration. A reduction in dose or dosing frequency may be warranted only in end state renal disease (CLCR 0 to 10 ml·min−1).
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315586
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 179
    Digitale Medien
    Digitale Medien
    Biliary secretion of felodipine metabolites in man after intravenous [14C]felodipine (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 421-424 
    Details
    ISSN: 1432-1041
    Schlagwort(e): felodipine ; bile ; dihydropyridines ; biliary secretion ; healthy volunteers ; drug metabolism ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The biliary secretion of [14C]felodipine in 4 healthy human subjects was studied by use of the multiple marker dilution principle with double lumen tubes placed in the stomach and intestine. Insignificant amounts of14C activity were recovered from gastric aspirates. The individual recovery from intestinal aspirates varied from 2.9 to 8.5% of the dose of radioactivity over the period of 4.5 h after dosing. Less than 0.1% was identified as unchanged felodipine. The results show that biliary secretion is a minor route of elimination of felodipine or its metabolites. Bile collection for 4.5 h had no significant effect on the pharmacokinetics of felodipine, although the 72 h urinary recovery of radioactivity tended to be lower when bile was collected (59%) than in the control experiment (66%).
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336677
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 180
    Digitale Medien
    Digitale Medien
    Pharmacokinetics, cerebrospinal fluid concentration, and safety of intravenous rifampin in pediatric patients undergoing shunt placements (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 515-517 
    Details
    ISSN: 1432-1041
    Schlagwort(e): rifampicin ; cerebrospinal fluid ; children shunt infections ; adverse effects ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The objectives of this study were to characterize the pharmacokinetics and determine the cerebrospinal fluid concentrations and safety of intravenous rifampin in pediatric patients undergoing shunt placement. Nine patients (mean age 5.6 y) received a single dose of rifampin, 20 mg · kg−1, administered intravenously 1 h prior to surgery. The peak serum concentrations ranged from 13.5–26.7 μg · ml−1; cerebrospinal fluid concentrations ranged from 0.12–3.0 (mean: 1.4) μg · ml−1. The mean total clearance, apparent distribution volume, and elimination half-life were 0.291 · kg−1 · h−1, 1.11 · kg−1, and 2.8 h. The concentrations of rifampin achieved in the cerebrospinal fluid exceeded the minimum inhibitory concentrations by 100-to 1000-fold against Staphylococcus epidermidis. However, 5 of 9 patients developed cutaneous reactions during intravenous rifampin prophylactic therapy. Because of the high frequency of adverse effects and more than adequate rifampin concentrations achieved in the cerebrospinal fluid, rifampin doses lower than that used in this study may be evaluated in future studies.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF02336694
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 181
    Digitale Medien
    Digitale Medien
    Comparative bioavailability of a cisapride suppository and tablet formulation in healthy volunteers (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 629-631 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Cisapride ; pharmacokinetics ; bioavailability ; suppository ; tablet
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The comparative bioavailability of cisapride as a 30 mg suppository and three 5 mg oral tablets was investigated in 12 non-smoking, healthy male volunteers. The two formulations were administered on two separate occasions following an overnight fast, according to a randomized cross-over design. The plasma concentration of cisapride was measured over 48 h after drug administration. The 30 mg suppository exhibited a mean time to the peak plasma concentration of 3.8 h, while the tablets showed a significantly earlier peak time of 1.5 h. The maximum plasma concentration of cisapride after the 30 mg suppository (50.3 ng · ml−1) was significantly lower than after the tablets (74.3 ng · ml−1). The AUCs following the two treatments did not differ significantly from each other. The comparative bioavailability of the 30 mg cisapride suppository in relation to the three 5 mg oral tablets was 85%, with a 95%-confidence interval of 67% to 102% (not adjusted for dose). Normalizing the mean AUC by dose, the relative bioavailability of the suppository was 43% of that of the tablet. The elimination half-life of cisapride was not significantly different following the administration of the two formulations (9.3 h for the suppository and 9.8 h for the tablet).
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00278595
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 182
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of various single intravenous and oral doses of omeprazole (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 195-197 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Omeprazole ; metabolites ; bioavailability ; pharmacokinetics ; dose-dependent kinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The influence of dose on the kinetics of omeprazole and two of its metabolites, hydroxyomeprazole and the sulphone, has been studied. Ten healthy subjects were given omeprazole 10 and 40 mg iv and 10, 40 and 90 mg orally. No significant dose-related difference in any parameter calculated from the iv experiments was detected. Following the oral solutions, however, there was a dose-dependent increase in systemic availability, probably due to saturable first-pass elimination. The AUC of the sulphone also seemed to increase non-linearly with increasing dose, and that of the hydroxyomeprazole increased in proportion to dose. The slight dose-dependency of the bioavailability of the solution is considered to be of no or limited clinical relevance. Furthermore, since omeprazole is given orally as slowly absorbed enteric coated granules in the dose of 20 mg o.d., the potential for dose-dependent kinetics in clinical practice would be much less than in the present study.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280061
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 183
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 193-194 
    Details
    ISSN: 1432-1041
    Schlagwort(e): methocarbamol ; haemodialysis ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary We determined plasma methocarbamol concentrations over 24 h following a 1.5 g methocarbamol dose (off-dialysis day) to 8 chronic haemodialysis patients and compared these results to those from 17 healthy male volunteers. The harmonic mean elimination half-life was similar between the two groups, 1.24 and 1.14 h, respectively. tmax and the weight-adjusted Cmax were 1.1 h and 27.0 mg · m−1 for haemodialysis patients and 1.1 and 23.1 mg · l−1 for normals. Relative systemic availability was assessed by comparing weight-normalized AUC × k10 products. These results indicate no significant differences with respect to methocarbamol absorption, with the relative systemic availability in patients being 113%. These data suggest that absorption and elimination of methocarbamol is similar between normal subjects and patients undergoing maintenance haemodialysis.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280060
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 184
    Digitale Medien
    Digitale Medien
    Pharmacokinetic study of methotrexate, folinic acid and their serum metabolites in children treated with high-dose methotrexate and leucovorin rescue (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 377-383 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Methotrexate ; folinic acid ; 7-hydroxymethotrexate ; pharmacokinetics ; 5-methyltetrahydrofolic acid ; leucovorin
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of methotrexate (MTX), 7-hydroxymethotrexate (7-OHMTX), 2,4-diaminomethylpteroic acid (APA), folinic acid, and 5-methyltetrahydrofolate (5-MTHF) have been studied during 21 high-dose MTX (HDMTX) infusions (5 g·m−2 in 24 h) with leucovorin (LCV) rescue, a component of the therapy of 5 children with acute lymphoblastic leukemia (ALL). The median steady-state concentration of MTX was 66 μmol·l−1. Three elimination half-lifes were determined for MTX: 1.8 h, 6.4 h and a terminal 15 h. The median systemic MTX clearance was 110 mg·m−2·min−1. The 7-OHMTX level increased during each infusion and a Cmax of 19 μmol·l−1 was achieved at the end. Its initial half-life was 5 h and the terminal half-life was 12 h. Thus, the peak serum concentration ratio of 7-OHMTX to MTX was reached 24 h after the end of the infusion at a median ratio of 8. The MTX metabolite APA was detected in concentrations less than 0.06 μmol·l−1. The median folinic acid level during rescue, 48 h after starting the infusion, was 7.0 μmol·l−1 and 18 h following the last dose of LCV it was 0.44 μmol·l−1, leading to ratios of folinic acid to MTX of 31 and 6, respectively. The median 5-MTHF level during rescue was 0.44 μmol·l−1 with a median ratio of 5-MTHF to MTX of 2. Twenty infusions with 48 h MTX levels of less than 0.5 μmol·l−1 were without marked toxicity. Only one patient with a 48 h MTX concentration of 5.5 μmol·l−1 and a ratio of 5-MTHF to MTX of 0.08 suffered from ulcerating mucositis and septicaemia despite increased and prolonged LCV rescue.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315414
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 185
    Digitale Medien
    Digitale Medien
    Pharmacokinetic interaction between cyclosporin and diltiazem (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 237-242 
    Details
    ISSN: 1432-1041
    Schlagwort(e): cyclosporin A ; diltiazem ; pharmacokinetics ; kidney transplantation ; drug metabolism ; cytochrome P-450 ; drug interactions ; human liver microsomes
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Previous reports have indicated that administration of the calcium antagonist diltiazem results in major changes in the pharmacokinetics of cyclosporin A (CyA). A new clinical trial was undertaken in 22 renal transplant patients receiving a constant dose of cyclosporin to further explore this interaction. Coadministration of diltiazem for one week produced an increase in the blood concentration of CyA and its metabolites 17 and 18 in almost all patients, but no increase in CyA metabolites 1 and 21. The mean whole blood CyA trough level determined by HPLC rose from 117 ng·ml−1 to 170 ng·ml−1 after one week on diltiazem, and the mean trough level of metabolite 17 rose similarly from 184 ng·ml−1 before to 336 ng·ml−1. Based on experiments with microsomes from human liver the effect of diltiazem was due to noncompetitve inhibition of CyA-metabolism by diltiazem, and the increased concentration of metabolite 17 might have been due to stronger inhibition of its secondary metabolism steps.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315023
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 186
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and pharmacodynamics of conventional and controlled-release formulations of metipranolol in man (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 243-247 
    Details
    ISSN: 1432-1041
    Schlagwort(e): metipranolol ; pharmacokinetics ; pharmacodynamics ; β-adrenoreceptor blockade ; radioreceptor assay ; controlled release form
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics and β-adrenoceptor blocking effects of conventional and sustained-release metipranolol have been studied in 6 healthy male volunteers given a single oral dose of 40 mg. Plasma drug concentrations determined by TLC and a radioreceptor assay, and the inhibition of exercise-induced tachycardia, were monitored for 48 h. Relevant amounts of active metabolites other than deacetylmetipranolol were not found. Compared to conventionally formulated metipranolol, the controlled-release product had a prolonged mean residence time (10.7 vs 5.5 h), the peak drug concentration was halved and the time to peak drug concentrations was delayed. Relatively constant plasma concentrations (cideal = 6.5 ng/ml) and a clinically significant reduction of exercise-induced tachycardia were maintained throughout a 24 h dosing interval. An individual deacetylmetipranolol plasma concentration-effect relationship was evaluated using the Emax model. Mean parameters were Emax 26% and C50 2.9 ng/ml.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315024
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 187
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of oral noscapine (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 275-279 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Noscapine ; pharmacokinetics ; bioavailability ; dose dependency ; oral administration ; inter- and intra-individual variability ; adverse events
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The relative bioavailability in 20 healthy volunteers of 100 mg, 200 mg and 300 mg tablets of noscapine and 200 mg as a solution has been assessed in a four-way cross-over study, with repeated administration of the 200 mg dose to assess intraindividual variability. There was a disproportionate increase in the AUC of noscapine tablets, as a 3-fold increase in dose produced a 9-fold rise in AUC. This dose-dependency could mainly be attributed to saturable first-pass metabolism of the drug. Administration of noscapine as a solution resulted in a significantly higher maximal concentration at an earlier time-point and a higher AUC than the corresponding dose as tablets. Repeated administration of noscapine tablets and solution yielded higher AUC on the second dosing occasion. No cause for this carry-over effect was found, and the contribution of remaining noscapine was negligible. The terminal half-life of noscapine, which was independent of formulation or dose size was 4.5 h. Both inter- and intraindividual variability in noscapine kinetics were very high, e.g. 73% and 51% CV of the AUC for the 200 mg tablet.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315110
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 188
    Digitale Medien
    Digitale Medien
    Effect of exercise on propranolol pharmacokinetics (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 391-394 
    Details
    ISSN: 1432-1041
    Schlagwort(e): propranolol ; beta-blockers ; pharmacokinetics ; exercise
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The effect of submaximal exercise on the pharmacokinetics of low dose intravenous propranolol was studied in 15 healthy human subjects. There was a wide individual variation in the results for each subject and a large difference in the degree of changes with exercise. The effect of exercise on the pharmacokinetics of propranolol, a flow limited drug, is marked but variable. This phenomenon may have profound effects on patients taking the drug regularly who exercise intermittently and drug doses may have to be adjusted.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315416
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 189
    Digitale Medien
    Digitale Medien
    Yohimbine bioavailability in humans (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 409-411 
    Details
    ISSN: 1432-1041
    Schlagwort(e): yohimbine ; pharmacokinetics ; bioavailability
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Pharmacokinetic profiles were determined in seven healthy young male subjects following single oral and intravenous doses of 10 mg of yohimbine hydrochloride. The drug was rapidly eliminated (t1/2β 0.58 h orally and t1/2β 0.68 h intravenously). Following intravenous administration the data fit a two-compartment pharmacokinetic model, with a very rapid distribution phase (t1/2a was approximately 6 min). Both the oral and the intravenous yohimbine clearance values were high but oral clearance values were much higher (mean 9.77 ml·min−1·kg−1 intravenous versus 55.9 ml·min−1·kg−1 oral). The oral bioavailability showed great variability, ranging from 7% to 87% (mean value was 33%). The imcomplete oral bioavailability of yohimbine may reflect either incomplete absorption from the gastrointestinal tract or an hepatic first pass effect. Although yohimbine is rapidly absorbed when given orally, the bioavailability is quite variable and considerable individualization of dosing may be necessary when the drug is used orally for clinical indications.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315421
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 190
    Digitale Medien
    Digitale Medien
    A randomized double-blind study of bisoprolol versus atenolol in mild to moderate essential hypertension (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 21-24 
    Details
    ISSN: 1432-1041
    Schlagwort(e): bisoprolol ; atenolol ; hypertension ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary We have compared the efficacy and pharmacokinetics of bisoprolol, a new cardioselective beta-adrenoceptor antagonist, with atenolol in a randomized double-blind crossover study in 12 patients (mean age 53.5 y) with mild to moderate essential hypertension. After a two week placebo wash-out period without any antihypertensive therapy, the patients were given bisoprolol 10 mg daily or atenolol 50 mg daily, increasing to 20 mg or 100 mg respectively if the sitting diastolic blood pressure did not fall below 90 mm Hg after two weeks of therapy. Crossover occurred after six weeks of active therapy followed by two weeks of placebo wash-out. After 6 weeks of therapy both drugs significantly reduced sitting and standing diastolic blood pressures (bisoprolol by 15% and 16% respectively, atenolo by 11% in both cases). However, while sitting and standing systolic pressures were significantly reduced by bisoprolol (13% and 16% respectively), only standing systolic pressures were significantly reduced by atenolol (11%), and this reduction was significantly less than with bisoprolol (p〈0.05). Both drugs similarly reduced mean sitting and standing heart rates. There were no significant differences between the single-dose and steady-state kinetics of either bisoprolol or atenolol. The mean plasma elimination half-life (t1/2) increased from 12.9 to 13.2 h during steady state on bisoprolol and from 7.2 to 11.5 h on atenolol. The apparent volume of distribution (Vz) was greater for bisoprolol than for atenolol after single dosing (235 1 vs 146 1) and at steady state (216 1 vs 137 1), but clearances were similar for both drugs. The maximum plasma concentration (Cmax) of bisoprolol increased from 45 μg·l−1 to 72 μg·l−1 during steady state and the Cmax of atenolol increased from 321 μg·l−1 to 410 μg·l−1 Adverse effects occurred in only one patient (lethargy while taking atenolol). These results suggest that bisoprolol has similar efficacy, safety, and pharmacokinetics to atenolol in patients with mild to moderate essential hypertension.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314797
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 191
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of (+)-rolipram and (−)-rolipram in healthy volunteers (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 71-75 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Rolipram ; enantiomers ; pharmacokinetics ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Plasma levels of S-(+)-rolipram and R-(−)-rolipram in six healthy male volunteers were measured by radioimmunoassay after intravenous injection of 0.1 mg and oral administration of 1.0 mg of the pure enantionmers. Following i.v. treatment, plasma levels of both isomers declined in three phases, with half-lives of 0.2 h, 0.6–0.9 h and 6–8 h. Total clearance was 6 ml · min−1 · kg−1. Oral administration of 1.0 mg gave a peak concentration of 16 ng · ml−1 after 0.5 h. Bioavailability of (+)-rolipram was 77% and of the (−) enantiomer it was 74%. There was no significant difference in Cmax, half-life, total clearance or bioavailability between the two enantiomers.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314807
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 192
    Digitale Medien
    Digitale Medien
    Effect of haemodialysis on the pharmacokinetics of cetirizine (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 67-69 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Cetirizine ; haemodialysis ; pharmacokinetics ; renal failure
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of Cetirizine, a histamine H1-receptor antagonist, were investigated in five renal failure patients undergoing chronic haemodialysis therapy. The patients received one 10 mg cetirizine dihydrochloride capsule 3 h before haemodialysis. Concentrations of cetirizine in serum and dialysate were determined by HPLC. The maximum serum cetirizine concentration and the time to reach that maximum were 285 μg·1−1 and 2.0 h, respectively. The terminal disposition half-life of cetirizine in these patients was 19.3 h. The haemodialysis clearance of cetirizine was 14.0 ml · min−1. Although this is approximately 33% of the apparent total body clearance of cetirizine in subjects with normal renal function, the fraction of the dose removed by dialysis was only 9.4%. Thus, since haemodialysis does not produce a clinically significantly alteration in cetirizine elimination, no supplemental dose should be necessary after dialysis.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314806
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 193
    Digitale Medien
    Digitale Medien
    Influence of midazolam on the plasma concentrations of mepivacaine after lumbar epidural injection in children (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 91-92 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Midazolam ; Mepivacaine ; local anaesthetic ; lumbar epidural anesthesia ; children ; drug interaction ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Twenty children undergoing surgery received a lumbar block using 0.4 ml/kg mepivacaine 2.0%. They were randomized into two groups, one of which received midazolam 0.4 mg/kg rectally as premedication. Midazolam administration did not significantly influence the plasma concentrations of mepivacaine.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314812
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 194
    Digitale Medien
    Digitale Medien
    Acetaminophen pharmacokinetics in women receiving conjugated estrogen (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 97-98 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Acetaminophen ; estrogen ; pharmacokinetics ; drug interaction
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314814
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 195
    Digitale Medien
    Digitale Medien
    The excretion of enalapril and enalaprilat in human breast milk (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 99-99 
    Details
    ISSN: 1432-1041
    Schlagwort(e): enalapril ; milk ; enalaprilat ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00314815
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 196
    Digitale Medien
    Digitale Medien
    Plasma levels of morphine and morphine glucuronides in the treatment of cancer pain: relationship to renal function and route of administration (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 121-124 
    Details
    ISSN: 1432-1041
    Schlagwort(e): morphine ; cancer ; morphine-6-glucuronide ; renal function ; drug metabolism ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary There is growing evidence that renally-impaired patients receiving morphine therapy are at greater risk of developing opiate toxicity, due to the accumulation of an active metabolite, morphine-6-glucuronide (M6G), which is usually excreted by the kidneys. This study examined the relationships between morphine dosage, renal function, and trough plasma concentrations of morphine and its glucuronide metabolites in 21 patients (aged mean: 68.5 years; 11 males) receiving either oral or subcutaneous morphine for terminal cancer pain. The median daily morphine dosages (mg · kg−1) were: orally 1.87 (range 0.37–6.82) and subcutaneously 1.64 (range 0.22–3.60). The median plasma concentrations of morphine, morphine-3-glucuronide (M3G), and M6G (ng · ml−1) were: 36.0, 1035.2, and 142.3, respectively. The plasma concentrations of morphine, M3G and M6G were each significantly related to the daily morphine dosage (n=21, Spearman r=0.79, 0.91, and 0.88 respectively). Accumulation of the morphine glucuronides was dependent on renal function. The plasma concentrations of M3G and M6G, when divided by the morphine concentration, were significantly related to the caluclated creatinine clearance of the patient. Patients receiving oral morphine had higher plasma concentration ratios of glucuronide/morphine than those receiving subcutaneous therapy, presumably due to first-pass glucuronidation. The results of this study confirm that accumulation of the pharmacologically active M6G is related to renal function, which probably explains the observation that morphine dosage requirements are generally reduced in patients with renal impairment.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00265969
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 197
    Digitale Medien
    Digitale Medien
    Pharmacokinetics and pharmacodynamics of cicaprost in healthy volunteers after oral administration of 5 to 20 μG (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 149-153 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Cicaprost ; PGI2-mimetic drug ; pharmacokinetics ; pharmacodynamics ; volunteers ; dose titration ; adverse effects
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary In a Phase I study, the tolerability, pharmacodynamics and pharmacokinetics of cicaprost have been investigated in 6 male volunteers given 5, 10, 15 and 20 μg as tablets of the β-cyclodextrin clathrate. Individual inhibition of platelet aggregation and changes in facial colour (measured by chromametry) were dose-dependent and reached a maximum 30 to 60 min post-dose. The maximum inhibition of platelet aggregation was about 40%. After 3 to 4 h pre-treatment values had returned. Blood pressure remained within the normal range. The peak plasma level of cicaprost was reached within 15 to 90 min after drug intake. Both Cmax-and AUC were individually dose-dependent. The terminal half-life in plasma of cicaprost was approx. 1 h, and its total clearance amounted to 4–7 ml·min−1·kg−1. The time courses of the plasma levels and of the pharmacodynamic actions were in agreement. Interindividual differences were observed in the occurrence of unwanted effects (e.g. headache). Thus, cicaprost is an orally available PGI2-mimetic, for which effects on platelet aggregation and vascular perfusion have been demonstrated in healthy volunteers after doses of 5 to 15 μg.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00280049
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 198
    Digitale Medien
    Digitale Medien
    Excessive motor impairment two hours after Triazolam in the elderly (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 229-232 
    Details
    ISSN: 1432-1041
    Schlagwort(e): benzodiazepines ; elderly subjects ; excessive drug effect ; psychomotor performance ; pharmacokinetics ; adverse reaction ; age
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of triazolam 0.25 mg p.o. and psychomotor coordination were compared in nine healthy, elderly volunteers and nine middle aged controls. Motor coordination, as measured by pursuit rotor performance, was impaired in the elderly even before triazolam administration, and in contrast to the controls it deteriorated to a critical level after the drug. Factors associated with the major decrease in psychomotor performance in the elderly volunteers were poor baseline performance, an additional independent-age factor, and the plasma concentration of free triazolam. Although short acting benzodiazepines may have a less detrimental effect on performance on the morning following their intake, there may be serious motor incoordination and falls may occur if the patients have to rise during the night, particularly when the plasma concentration is high, i.e. about 2 h after dosing.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315021
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 199
    Digitale Medien
    Digitale Medien
    Pharmacokinetics of a valpromide isomer, valnoctamide, in healthy subjects (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 289-291 
    Details
    ISSN: 1432-1041
    Schlagwort(e): valnoctamide ; valpromide ; valproic acid ; pharmacokinetics ; healthy subjects ; tranquiliser
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of a single 400 mg oral dose of valnoctamide (VCD) has been investigated in seven healthy, adult, male volunteers. VCD was not biotransformed rapidly to its corresponding acid valnoctic acid (VCA), unlike its isomer valpromide (VPD). It had a mean residence time of 13.2 h and a terminal half-life of 9.3 h. Throughout the study, only low plasma levels of VCA could be detected. Thus, unlike VPD, which is a prodrug of the corresponding acid, (valproic acid, VPA). VCD appears to act as a drug in its own right, and it does not undergo similar hydrolysis. The pharmacokinetic difference may account for the different pharmacological activities of the two isomers.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315032
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
  • 200
    Digitale Medien
    Digitale Medien
    The pharmacokinetics of cotinine in plasma and saliva from non-smoking healthy volunteers (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 281-287 
    Details
    ISSN: 1432-1041
    Schlagwort(e): Cotinine ; non-smokers ; saliva levels ; plasma levels ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Cotinine is a major metabolite of nicotine in man. Its disposition kinetics has been followed in plasma and saliva from nine nonsmokers, 23 to 56 years of age. Cotinine 5, 10 and 20 mg was given intravenously and orally to each subject, and plasma, saliva and urine samples were collected for 96 h. The kinetics of cotinine was best described by a multi-compartment model with three distinct phases both in plasma and saliva. Regardless of the mode of administration, there was no indication of dose-dependent kinetics. Mean total plasma clearance was 63.8 ml·h−1·kg−1 and mean renal clearance was 4.7 ml·h−1·kg−1, i.e. only 10% of the dose was excreted unchanged in the urine. The volume of distribution, as calculated from the plasma curves, was slightly greater than the body weight, 1.1 l·kg−1. The concentration of cotinine was 20 to 40% higher in unstimulated mixed saliva than in plasma during the absorption, distribution and elimination phases. As the clearance and distribution values in saliva were directly proportional to the corresponding values in plasma, similar terminal half-life values were obtained in the two body fluids, 15.5 and 16.8 h for plasma and saliva, respectively. Thus the kinetics of cotinine is linear after intravenous and after oral dosing, and salivary concentrations give the same information about cotinine disposition in the body as do plasma concentrations.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00315031
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
    BibTip Andere fanden auch interessant ...
    Artikel (Nationallizenzen)
    Volltext
Schließen ⊗
Diese Webseite nutzt Cookies und das Analyse-Tool Matomo. Weitere Informationen finden Sie hier...