Library

X
feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
Filter
  • 1985-1989  (839)
  • 1988  (121)
  • 1986  (144)
  • 1985  (574)
  • Physics  (480)
  • pharmacokinetics  (359)
  • 101
    Electronic Resource
    Electronic Resource
    Plasma drug and antiplatelet profiles of the original acetylsalicylic acid preparations used in the AMIS, PARIS and German-Austrian trials for secondary prevention of myocardial infarction (1988)
    Springer
    European journal of clinical pharmacology 33 (1988), S. 541-547 
    Details
    ISSN: 1432-1041
    Keywords: acetylsalicylic acid ; infarct prevention ; platelet aggregation ; pharmacokinetics ; healthy volunteers ; secondary heart attack prevention ; AMIS ; PARIS ; German-Austrian trials
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a cross-over study 6 healthy male subjects were given for 9 days the acetylsalicylic acid (ASA) preparations used in the Aspirin Myocardial Infarction Study (AMIS), Persantine-Aspirin Reinfarction Study (PARIS) and German-Austrian secondary heart attack prevention trials, exactly according to the original study protocols. Plasma concentrations of ASA and its main metabolites salicylic acid (SA) and salicyluric acid (SUA), as well as platelet function (collagen-induced platelet aggregation; tissue extract-induced change in platelet shape) were studied repeatedly on the first day of each medication period and were again examined on the sixth and ninth days. Differences in the plasma concentrations of ASA and its metabolites were found only on the first day, probably as a result of different absorption rates. Collagen-induced platelet aggregation was more rapidly inhibited the faster the preparation was absorbed. Each ASA preparation inhibited tissue extract-induced platelet shape change from the first dose, although statistically significant inhibition was seen only with the AMIS preparation. It is concluded that differences in the antithrombotic efficiency of ASA cannot be explained by differences in the pharmacokinetic and antiplatelet profiles of the various ASA preparations tested.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542484
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 102
    Electronic Resource
    Electronic Resource
    Intrathecal ACNU — a new therapeutic approach against malignant leptomeningeal tumors (1988)
    Springer
    Journal of neuro-oncology 6 (1988), S. 221-226 
    Details
    ISSN: 1573-7373
    Keywords: leptomeningeal tumor ; intrathecal chemotherapy ; ACNU ; nitrosourea ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Pharmacokinetics, toxicity and therapeutic efficacy of intrathecal ACNU, 3-((4-amino-2-methyl-5-pyrimidinyl)methyl)-1-(2-chloroethyl)-1-nitrosourea, were studied in rats to determine if it is a new and effective method for the treatment of malignant leptomeningeal tumors. Pharmacokinetics of intracisternally administered ACNU was studied by macroscopial autoradiography using 14C-labeled ACNU. It was demonstrated that intracisternally administered ACNU distributed in the subarachnoid space and subpial layer of the brain in high concentration and was rapidly eliminated into the systemic circulation. The diffusional transport of ACNU into the deeper part of the brain was limited. More than 3.0 mg/kg of intracisternal ACNU induced progressive loss of the weight of body in normal rats, and 80% of the rat given 6.0 mg/kg died. Increase of capillary permeability, neuronal loss and gliosis were observed in the marginal layer of the brain facing to the subarachnoid space in the rat given more than 3.0 mg/kg of ACNU. Systemic and local toxicity was not observed in the rat given less than 1.5 mg/kg. Therapeutic effect of intrathecal ACNU against leptomeningeal tumors was evaluated in the rat with meningeal carcinomatosis induced by intracisternal inoculation of Walker 256 carcinosarcoma cells. The median survival time of the rat treated with 1.5 mg/kg of intracisternal ACNU once on day 2 or on day 5 after tumor inoculation was significantly prolonged by 173%, and 214% at maximum, respectively, as compared with that of the untreated animal. These findings suggest that intrathecal ACNU may be of value for clinical trial against leptomeningeal tumors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00163704
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 103
    Electronic Resource
    Electronic Resource
    The use of mass balance principles to describe regional drug distribution and elimination (1988)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 16 (1988), S. 13-29 
    Details
    ISSN: 1573-8744
    Keywords: pharmacokinetics ; mass balance ; regional distribution ; regional elimination
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Mass balance principles were used to derive a number of terms that are helpful in describing the rate and extent of regional drug uptake. Regional drug uptake was defined as the net movement of drug from the blood perfusing a region into the extravascular space of the region due to the distribution and/or elimination of the drug. By analogy with the traditional physiological definition of flux, net drug flux was defined as the difference in mass per unit time of drug respectively entering and leaving a region via the arterial and venous blood vessels. The timeintegral of net drug flux, net drug mass, was defined as the mass of drug that has entered a region via the arterial blood vessels but has not left the region via the venous blood vessels. For regions in which no drug elimination occurs, the mean regional drug concentration was defined as the net drug mass divided by the mass of the region. When a number of criteria are satisfied, the net drug flux is approximately the rate of drug uptake and the net drug mass is approximately the extent of drug uptake. Several examples are given to demonstrate the broad range of applications of mass balance principles. First, the method was used to characterize the differences between drug distribution and elimination in a hypothetical region using drug concentrations simulated from compartmental models of either distribution alone or distribution with elimination. Second, the whole body distribution net flux was described during a constant rate infusion of iodohippurate (IOH) into a sheep from the difference between the whole body net flux and renal net flux of IOH. Third, the time course of the mean myocardial lignocaine (lidocaine) concentrations in a sheep after an intravenous bolus of lignocaine were described. The time course of the lignocaine-induced depression of myocardial contractility followed more closely the mean myocardial lignocaine concentrations than that of either the arterial or coronary sinus blood concentrations. It is concluded that the use of mass balance principles provides a simple, empirical, and physiologically based method for the determination of the rate and extent of both drug distribution and elimination in regions as simple as single organs or as complex as the whole body.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061860
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 104
    Electronic Resource
    Electronic Resource
    The uptake and elution of lignocaine and procainamide in the hindquarters of the sheep described using mass balance principles (1988)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 16 (1988), S. 31-40 
    Details
    ISSN: 1573-8744
    Keywords: lignocaine ; procainamide ; pharmacokinetics ; mass balance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Mass balance principles were used to describe the uptake and elution of lignocaine (lidocaine) and procainamide in the hindquarters of the sheep. Each of four sheep received a right atrial infusion of either lignocaine · HCl (2.7 mg/min) or procainamide · HCl (5.5mg/min) for 180 min. Paired arterial and inferior vena cava (draining the hindquarters) blood samples were taken at 20-min intervals during the infusion and for 180 min after the infusion. Lignocaine and procainamide mean total body clearances were 2.9 L/min (SD 1.1) and 1.3 L/min (SD 0.2), respectively. An index of the uptake and elution of these drugs in the hindquarters was estimated from the net drug mass per unit hindquarter blood flow;indirect evidence suggested that hindquarter blood flow was constant. All the net mass/flow of procainamide that was taken into the hindquarters during the infusion also eluted after the infusion, demonstrating reversible distribution into the tissues. However, uptake of procainamide was still occurring when blood concentrations were constant, indicating that the concentrations of procainamide in the hindquarters were not in equilibrium with the inferior vena cava concentrations. Lignocaine did not reach constant blood concentrations during the infusion and showed no tendency to reach arteriovenous equilibration; an arteriovenous difference of 22%(SD5%) across the hindquarters was measured during the last 60 min of the infusion. By 180 min after the lignocaine infusions, 79% (SD 8%) of the lignocaine net mass/flow had not eluted from the hindquarters when arterial and venous lignocaine concentrations were not significantly different. This drug could remain uneluted due to metabolism and/or avid tissue binding, and presents difficulties in the interpretation of pharmacokinetic data whether based on arterial or venous blood sampling.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061861
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 105
    Electronic Resource
    Electronic Resource
    On the dose dependency of Cyclosporin a absorption and disposition in healthy volunteers (1988)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 16 (1988), S. 331-353 
    Details
    ISSN: 1573-8744
    Keywords: Cyclosporin A ; pharmacokinetics ; dose dependency ; oral absorption ; disposition ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of Cyclosporin A (CyA, SandimmuneR) was studied in 12 healthy male volunteers after oral dosing of 350 mg, 700 mg, and 1400 mg as a drinking solution. Blood samples were collected over 96 hr and analyzed by high pressure liquid chromatography. Concentration data were evaluated with model-independent and model-based linear pharmacokinetic concepts. Individual CyA concentration-time profiles in whole blood were well described by a two-compartment open model with zero-order absorption for all three doses. Comparison of pharmacokinetic parameters across doses indicates that both absorption and disposition are dose-dependent. Nonlinear disposition is suggested by the significant increase of the terminal half-life from 8.9±4.9hr to 11.9±4.9hr (mean±SD) after a 350 mg and a 1400 mg dose, respectively. Changes in the metabolic activity of the liver with concentration might be responsible for this phenomenon. In addition, the modeling approach indicated that bioavailability decreases with increasing dose. Moreover, the dependence of the rate of CyA absorption (zero-order rate constant) versus dose was well described by a hyperbola. The limited solubility of the drug in the gastrointestinal tract might be responsible for this behavior. The lag time (0.2–0.8 hr) was independent of dose. This value is similar to the time of gastric emptying in fasting volunteers. The duration of absorption for 11 of 12 subjects was in the range 2.5–3.5 hr over all doses and agrees well with the small intestine transit time. Some subjects showed a marked secondary peak at one or two doses, which could be adequately fitted by a model with two successive zero-order inputs. This double-peak behavior was ascribed to the influence of the food on gastric emptying. Dose dependency of disposition and absorption counterbalance each other in the usual dose range. This leads to an almost proportional increase of area under the blood CyA concentration-time profile with increasing dose.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01062550
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 106
    Electronic Resource
    Electronic Resource
    Pharmacokinetic modeling of the anticonvulsant response of oxazepam in rats using the pentylenetetrazol threshold concentration as pharmacodynamic measure (1988)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 16 (1988), S. 203-228 
    Details
    ISSN: 1573-8744
    Keywords: oxazepam ; pharmacokinetics ; pharmacodynamics ; anticonvulsant response ; pentylenetetrazol threshold ; kinetic-dynamic model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract This investigation developed strategies along which the anticonvulsant effect of oxazepam in the rat could be pharmacokinetically modeled. After determination of the pharmacokinetics of oxazepam, which could be described with a two-compartment model (halflives of distribution and elimination 6 and 52 min, respectively), the drug was administered iv to groups of animals to achieve a serum concentration range of 0.1–2.5 mg/L at 10, 45, and 120 min after administration. At these time points pentylenetetrazol (PTZ) was infused slowly until the first myoclonic jerk occurred. The anticonvulsant response, expressed as the elevation of the serum or brain threshold concentration of PTZ, was modeled versus the serum (both total and free) and brain oxazepam concentration, according to the sigmoid E max model. The total serum and brain oxazepam EC50 values are about 0.5 mg/L and 1.1 mg/kg, respectively, and E max 120 mg/L PTZ. No marked differences in pharmacodynamic parameters between the three time groups were found, which indicates that serum and brain are pharmacokinetically indistinguishable from the effect compartment, that there is no (inter) activity of oxazepam metabolites and absence of development of acute tolerance during the investigated time frame. An interfering role of metabolites was also excluded by a direct radioreceptor assay of oxazepam, yielding very similar results as the specific Chromatographic assay. It is concluded that the concentration-anticonvulsant effect relationship of oxazepam can satisfactorily be described by the sigmoid E max model, when utilizing the employed experimental strategies.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01062261
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 107
    Electronic Resource
    Electronic Resource
    An Implantable Pump for Intrarenal Infusion of Immunosuppressants in a Canine Autotransplant Model (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 781-785 
    Details
    ISSN: 1573-904X
    Keywords: pharmacokinetics ; 6-mercaptopurine ; targeted drug delivery ; renal transplantation ; intraarterial infusion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract We developed a canine renal allograft model utilizing implantable infusion pumps and biocompatible catheters to investigate the pharmacokinetics of local immunosuppressive drug administration. Seven mongrel dogs underwent bilateral nephrectomy and autotransplantation of one kidney to the iliac vessels. The proximal end of an infusion catheter directed into the iliac artery was tunneled to a subcutaneously placed programmable pump. A second, sampling catheter was placed with its tip in the iliac vein. Simultaneous regional (iliac vein) and systemic (jugular vein) venous concentrations of 6-mercaptopurine (6-MP), the immunosuppressive metabolite of azathioprine, were determined during a continuous 24-h intraarterial infusion (10 mg/kg/24 hr). The gradient between regional and systemic 6-MP concentrations was maximal initially when the pump was turned on, continuously decreased until steady state was reached, and disappeared immediately after the pump was turned off. The mean ratio of steady-state iliac vein to systemic 6-MP concentrations was 5.0 ± 1.4, demonstrating a pharmacokinetic advantage of continuous intraarterial 6-MP infusion to the autotransplanted kidney. The novel canine renal allograft model described herein overcomes the technical limitations of earlier models and represents a foundational step in the design of intrarenal infusion patterns of immunosuppressive agents which we expect to prolong survival of the allotransplanted kidney with minimal systemic drug exposure and side effects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015940802451
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 108
    Electronic Resource
    Electronic Resource
    Liquid Chromatographic Analysis of Di(2-ethylhexyl) Phthalate: Application to Pharmacokinetic Studies in the Mongrel Dog (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 10-15 
    Details
    ISSN: 1573-904X
    Keywords: di(2-ethylhexyl) phthalate ; liquid chromatographic (LC) analysis ; pharmacokinetics ; renal failure ; mongrel dog
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A high-performance liquid chromatographic (HPLC) assay was developed for the determination of di(2-ethylhexyl) phthalate (DEHP) in serum or plasma. Plasma DEHP concentrations that were measured by HPLC in specimens obtained from hemodialysis patients were in good agreement with corresponding concentrations that were measured by gas chromatography with selected ion monitoring (GC-SIM) (r 2 = 0.996). Plasma DEHP concentrations were measured after intravenous DEHP administration (1.2–4.4 mg DEHP/kg body weight) to determine the effect of bilateral ureteral ligation on DEHP elimination in the mongrel dog. DEHP plasma clearance (∼6.3 ml/min/kg), steady-state distribution volume (∼0.2l/kg), and terminal half-life (∼50 min) were unchanged in two dogs following bilateral ureteral ligation. DEHP terminal half-life and steady-state distribution volume were substantially smaller (25- to 70-fold) than reported previously in the rat or dog.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015872309411
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 109
    Electronic Resource
    Electronic Resource
    Peripheral pharmacokinetic parameters of levodopa/carbidopa and the on-off phenomenon in parkinsonian patients (1988)
    Springer
    Neurological sciences 9 (1988), S. 255-259 
    Details
    ISSN: 1590-3478
    Keywords: Parkinson disease ; levodopa ; pharmacokinetics ; on-off phenomenon
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Sommario I principali parametri farmacocinetici periferici della associazione levodopa/carbidopa sono stati studiati in 11 volontari sani ed in 16 pazienti affetti da morbo di Parkinson in differenti stadi di malattia, con e senza fluttuazioni delle performances motorie. Dopo somministrazione per via orale di una dose standard del farmaco (levodopa 250 mg., carbidopa 25 mg.), i valori della concentrazione plasmatica massima, del tempo di comparsa del picco e dell'area sotto la curva concentrazione/tempo sono risultati simili in tutti i gruppi esaminati. La farmacocinetica periferica dell'associazione levodopa/carbidopa non è risultata essere differente nei parkinsoniani che presentavano delle fluttuazioni delle performances motorie in confronto ai pazienti con stabile risposta clinica alla terapia.
    Notes: Abstract The principal peripheral pharmacokinetic parameters of the levodopa/carbidopa association were investigated in 11 healthy volunteers and in 16 patients at various stages of Parkinson disease, with and without the on-off phenomenon. After oral administration of a standard dose of drug (levodopa 250 mg + carbidopa 25 mg) the peak plasma concentrations, peak onset time and area under the curve/time proved to be similar across the groups. There was no difference in peripheral pharmacokinetics of the association between parkinsonian patients with swings in response and those without.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02334049
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 110
    Electronic Resource
    Electronic Resource
    Quantitative Structure–Activity Study on Human Pharmacokinetic Parameters of Benzodiazepines Using the Graph Theoretical Approach (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 201-208 
    Details
    ISSN: 1573-904X
    Keywords: quantitative structure–activity analysis (QSAR) ; topological approach ; benzodiazepines ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The graph theoretical indices for a series of 13 benzodiazepines were calculated using a graph-path topological method. The total molecule, the ring fragments, and combinations of ring fragments were subjected to a quantitative structure–activity analysis using eight pharmacokinetic parameters. The metabolic clearance and the blood-to-plasma concentration ratios were most highly correlated with the graph theoretical indices, with R values of 0.975 and 0.938, respectively. These correlations were found when the diazepine + benzo fragment and phenyl fragment were used to calculate the graph-path indices. Terminal disposition half-life was correlated with the benzo + diazepine fragment, with R = 0.969. Truncating the graph-path codes by eliminating cycles in the total molecule markedly improved the correlation coefficients. When compared to the graph-path indices for the total molecule, the correlation coefficients for the terminal disposition half-life and metabolic clearance data rose from 0.721 to 0.935 and from 0.770 to 0.968, respectively, using the graph-path indices of the truncated molecule. Intrinsic clearance of unbound drug also was poorly correlated with the total molecule (r 〈 0.7) but rose significantly using the graph-path indices of the truncated moleucle (r = 0.971 and 0.975 for the well-stirred and parallel-tube models, respectively.)
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015933527583
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 111
    Electronic Resource
    Electronic Resource
    Stereoselective Binding of Disopyramide to Plasma Proteins (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 316-318 
    Details
    ISSN: 1573-904X
    Keywords: disopyramide ; pharmacokinetics ; plasma proteins ; stereoisomers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015986906627
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 112
    Electronic Resource
    Electronic Resource
    Cimetidine Elimination from the Cerebrospinal Fluid of the Rat (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 628-633 
    Details
    ISSN: 1573-904X
    Keywords: cimetidine ; cerebrospinal fluid ; clearance ; choroid plexus ; pharmacokinetics ; transport
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The major goal of this study was to develop a small animal model that could be used to assess quantitatively the clearance of cimetidine from the cerebrospinal fluid (CSF) under relatively physiologic conditions. In addition, we addressed questions related to the pathways involved in the elimination of cimetidine from the CSF. We administered high and low bolus doses of cimetidine together with inulin, as a marker of bulk flow, into the lateral ventricle of anesthetized rats and sampled CSF from the cisterna magna. Principles of linear pharmacokinetic systems were applied to the data to obtain clearances from the CSF. The clearance of inulin was 2.02 ± 0.22 µl/min, which is in excellent agreement with the CSF production rate of 2.2 µl/min in anesthetized rats. The clearance of cimetidine from the CSF following the administration of a low dose was 11.8 ± 3.1 µl/min, which is in good agreement with the cimetidine CSF clearance in the rat obtained previously in studies using the technique of ventriculocisternal perfusion. A 32% decrease in the CSF clearance of cimetidine (P 〈 0.05) was observed when the high dose was administered, suggesting that CSF elimination is saturable. The clearance of inulin was unaffected by the high dose of cimetidine. This study demonstrates that the technique of lateral ventricle injection and sampling from the cisterna magna is useful in quantitatively assessing the elimination of compounds from the CSF in the rat under relatively physiologic conditions.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015918802935
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 113
    Electronic Resource
    Electronic Resource
    Liquid Chromatographic Assay and Pharmacokinetics of Quazepam and Its Metabolites Following Sublingual Administration of Quazepam (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 365-368 
    Details
    ISSN: 1573-904X
    Keywords: quazepam ; metabolites ; reversed phase ; high-performance liquid chromatography ; solid-phase extraction ; plasma ; sublingual ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A reverse-phase liquid chromatographic method is described for simultaneous quantification of quazepam, and two of its metabolites, 2-oxoquazepam and N-desalkyl-2-oxoquazepam. The method uses a solid-phase extraction procedure to prepare plasma samples. After extraction, the methanolic extract is evaporated; the residue is then reconstituted in a small volume of mobile phase and chromatographed. The total chromatography time for a single sample is about 20 min. A sensitivity of 1 ng/ml for quazepam and its metabolites is attained when 1 ml of plasma is extracted. Analytical recovery of quazepam and its metabolites added to plasma ranged from 87 to 96%. The maximum within-day and day-to-day coefficients of variation for each compound at concentrations of 20 and 60 ng/ml were 7.6 and 11.2%, respectively. The method was applied to sublingual pharmacokinetic studies of quazepam in healthy volunteers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015907611170
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 114
    Electronic Resource
    Electronic Resource
    Comparative Pharmacokinetics of Methylprednisolone Phosphate and Hemisuccinate in High Doses (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 509-513 
    Details
    ISSN: 1573-904X
    Keywords: methylprednisolone phosphate ; methylprednisolone hemisuccinate ; pharmacokinetics ; saliva analysis ; endogenous hydrocortisone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of methylprednisolone and two methylprednisolone esters, the phosphate and the hemisuccinate, were investigated after intravenous administration of the esters to 12 healthy male subjects in two different doses (250 and 1000 mg). Methylprednisolone was formed more rapidly from phosphate than from hemisuccinate. During the first 30 min methylprednisolone levels were three to four times higher after phosphate administration than after hemisuccinate. The mean residence time of the hemisuccinate was significantly longer and the total-body clearance lower than those of the phosphate. Whereas very little of the phosphate (mean, 1.7%) was eliminated unchanged into the urine, there were significant amounts of hemisuccinate (mean, 14.7%) excreted renally and therefore not bioavailable. Methylprednisolone saliva levels paralleled plasma levels; the average saliva/plasma ratio was 0.22. Neither phosphate nor hemisuccinate could be detected in saliva. An average of 7.2% of the administered dose was eliminated in the form of methylprednisolone in urine. Renal clearance was 24 ml/min and not dose or prodrug dependent. For both doses endogenous hydrocortisone levels were lowered after 24 hr. For the 1000-mg dose the depression was still significant after 48 hr. The results indicate that methylprednisolone phosphate results in a faster and more efficient conversion to its active form, methylprednisolone, than methylprednisolone hemisuccinate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015921408870
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 115
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and Bioavailability of Hydromorphone: Effect of Various Routes of Administration (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 718-721 
    Details
    ISSN: 1573-904X
    Keywords: hydromorphone ; intranasal ; transdermal ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics and bioavailability of hydromorphone following various routes of administration, i.e., intravenous, oral, intranasal, and transdermal, were investigated in rabbits. Hydromorphone plasma concentrations were determined by reverse-phase high-performance liquid chromatography (HLPC). Comparison of area under the concentration versus time curve (AUC) between intravenous and oral administrations showed a low bioavailability of hydromorphone after oral administration. The nasal absorption of hydromorphone was studied by the in situ nasal recirculation technique, and the results showed that hydromorphone is well absorbed from the nasal mucosa. The transdermal permeation of hydromorphone was also evaluated for 24 hr and a steady-state plasma concentration (0.135 µg/ml) was achieved during the 6- to 24-hr periods following the application of a transdermal patch on the inner pinna of the rabbit's ear.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015959912021
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 116
    Electronic Resource
    Electronic Resource
    Exogenous Methemoglobin as a Cyanide Antidote in Rats (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 749-752 
    Details
    ISSN: 1573-904X
    Keywords: methemoglobin ; cyanide antidote ; cyanide poisoning ; pharmacokinetics ; rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The effects of the administration of methemoglobin (MetHb) prepared in vitro were evaluated in Sprague–Dawley rats given increasing doses of potassium cyanide (KCN). Median lethal dose (LD50) studies were conducted by giving intraperitoneal injections of KCN (in 0.3- to 0.5-ml volumes), then 2 min later administering intravenous (iv) doses of 1000, 1500, or 2500 mg/kg of MetHb through the tail vein. Control rats received an equivalent volume of saline. The resulting LD50 values for KCN were 7.4 ± 1.1, 11.7 ± 1.1, 13.9 ± 1.0, and 14.2 ± 1.0 mg/kg (mean ± SD) for the control (no MetHb) and 1000-, 1500-, and 2500-mg/kg dose groups, respectively. Additional groups of rats were given 1000, 1500, or 2500 mg/kg MetHb and submitted for necropsy. The gross finding of darkened kidneys was present in both dose groups, but became consistent and more prominent in the 2500-mg/kg dose group. Evidence of pathologic changes was not present in other organs. Single-dose pharmacokinetic studies were conducted using iv doses of 1600 and 2500 mg/kg MetHb. The elimination half-life was similar in both doses (62.6 min), but the volume of distribution (95.3 ± 7.2 and 126.3 ± 5.2 ml/kg, mean ± SE) and clearance (1.1 ± 0.1 and 1.5 ± 0.1 ml/min/kg) were significantly different (P 〈 0.05) for the 1600-and 2500-mg/kg dose groups, respectively. From these data we conclude that although MetHb is cleared from the vascular system rapidly, it may be an effective and nontoxic antidote for doses of cyanide up to twice that of the control LD50.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015928432494
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 117
    Electronic Resource
    Electronic Resource
    Capillary Gas Chromatography and Thermionic N-P-Specific Detection of 13-Bis(2-chloroethyl)-l-nitrosourea (BCNU) or l-(2-Chloroethyl)-3-cyclohexyl-l-nitrosourea (CCNU) in Stability and Pharmacokinetic Studies (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 220-225 
    Details
    ISSN: 1573-904X
    Keywords: capillary gas chromatography ; analysis ; stability ; pharmacokinetics ; carmustine ; lomustine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract An expedient, rapid, and sensitive capillary gas chromatographic method for the analysis of l,3-bis(2-chloroethyl)-l-nitrosourea (BCNU) or l-(2-chloroethyl)-3-cyclohexyl-l-nitrosourea (CCNU) in plasma is described. Separation of the underivatized nitrosourea compounds was performed on a 0.33-mm-i.d., 25-m fused-silica, SE-30 capillary column, and detection was carried out using a thermionic N–P-specific detector. The compounds were extracted from plasma with benzene with a yield of 〉87%. The assay was linear in the ranges of 0.001 to 0.5 and 0.5 to 25 µg/ml for CCNU or 0.003 to 0.50 and 0.5 to 25 µg/ml for BCNU, with correlation coefficients from 0.9914 to 0.9999 and coefficients of variation (CV) of 〈3.3%. Other antineoplastic agents did not interfere in the assay. The method was employed to study the pharmacokinetics of BCNU in rabbits. The plasma concentration-time curves were fit to a two-compartment model with a mean (SE) α, β, and total-body clearance of 2.898 (0.913) hr−1, 0.1228 (0.0179) hr−1, and 7.211 (2.862) liters/hr · kg, respectively. Further, the stability of BCNU and CCNU in solution was examined at different temperatures. Both compounds were stable in benzene or acetone (4 to 37°C) but labile in plasma even if refrigerated. The apparent rate constants for degradation of BCNU and CCNU were 0.09921 and 0.02853 hr−1 at 4°C and 5.998 and 2.553 hr−1 at 37°C, respectively.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015989612562
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 118
    Electronic Resource
    Electronic Resource
    Dextromethorphan Pretreatment Induces Antipyrine Clearance in the Rat (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 437-439 
    Details
    ISSN: 1573-904X
    Keywords: antipyrine ; dextromethorphan ; drug metabolism ; enzyme induction ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Numerous agents that undergo extensive first-pass metabolism have been shown to inhibit oxidative drug metabolism. To examine whether this effect is related to the chemical structure or pharmacokinetic characteristics of the inhibiting agent, we determined the effect of dextromethorphan (a compound which exhibits pharmacokinetic similarities to, but is chemically dissimilar from, previously studied agents) on the disposition of antipyrine. A single oral dose of dextromethorphan hydrobromide, 100 mg/kg, 1 hr prior to antipyrine administration had no significant effect on the pharmacokinetics of this model substrate. The administration of dextromethorphan at the same dose twice daily for 3 days and an additional dose 1 hr prior to antipyrine administration resulted in a 33% increase in the clearance of antipyrine. These data indicate that dextromethorphan is capable of inducing hepatic microsomal enzymes. Studies are needed to determine if this effect also occurs upon chronic administration in humans. These data suggest that the pharmacokinetic characteristic of extensive first-pass metabolism is not necessarily associated with inhibition of drug metabolism.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015940518439
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 119
    Electronic Resource
    Electronic Resource
    Mean Residence Time Concepts for Pharmacokinetic Systems with Nonlinear Drug Elimination Described by the Michaelis–Menten Equation (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 156-164 
    Details
    ISSN: 1573-904X
    Keywords: mean residence time ; moment analysis ; pharmacokinetics ; Michaelis–Menten elimination ; compartmental models
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Equations for the mean residence time (MRT) of drug in the body and related functions are derived for drugs which are intravenously administered into a one- or two-compartment system with Michaelis–Menten elimination. This MRT is a function of the steady-state volume of distribution and time-average clearance obtained from the dose and area under the curve (dose/AUC). The differences between the MRT calculated by the proposed method and by using the moment theory method (AUMC/AUC) are demonstrated both mathematically and by computer simulations. The validity of the proposed method for calculation of MRT and its relationship to the moment theory result have also been assessed by examining the percentage of the administered dose eliminated and the percentage of the total area attained at MRT and at AUMC/AUC in relation to the dose. The equations evolved should be helpful in clarifying residence time derivations and in defining the disposition characteristics and differences between linear and nonlinear systems. Direct methods are provided for calculation of Michaelis–Menten parameters based on the relationship between MRT and dose.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015960806202
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 120
    Electronic Resource
    Electronic Resource
    Calculations and Application of Mean Residence Times for Drugs Which Demonstrate One-Compartment Distribution and Michaelis-Menten Elimination (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 196-196 
    Details
    ISSN: 1573-904X
    Keywords: mean residence time ; pharmacokinetics ; Michaelis-Menten elimination ; one-compartment model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015977209836
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 121
    Electronic Resource
    Electronic Resource
    Pharmacokinetics, behavioral, and neurophysiological aspects of the action of 2-ethyl-6-methyl-3-hydroxypyridine in rats (1988)
    Springer
    Bulletin of experimental biology and medicine 106 (1988), S. 1104-1107 
    Details
    ISSN: 1573-8221
    Keywords: nootropic drugs ; pharmacokinetics ; behavior ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00840370
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 122
    Electronic Resource
    Electronic Resource
    The lymphatic route. 1) Albumin and hyaluronidase modify the normal distribution of interferon in lymph and plasma (1986)
    Springer
    Cellular and molecular life sciences 42 (1986), S. 432-433 
    Details
    ISSN: 1420-9071
    Keywords: Interferon ; immunomodulator ; catabolism ; pharmacokinetics ; administration routes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary When human recombinant interferon-α2 diluted in saline was injected s.c. into rabbits, the total amount recovered in thoracic lymph was less than 0.4%. Recoveries increased from 2- to 8-fold if interferon was injected in 4% albumin or with hyaluronidase, respectively. Albumin added to interferon acts as an interstitial fluid expander, thus favoring interferon absorption through lymphatics rather than blood capillaries. This strategy may increase the therapeutic index of interferon.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02118644
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 123
    Electronic Resource
    Electronic Resource
    Atoms to astronomy: Computer graphics at the Jet Propulsion Laboratory (1986)
    Springer
    The visual computer 2 (1986), S. 159-163 
    Details
    ISSN: 1432-2315
    Keywords: Education ; Animation ; Computer graphics ; Physics ; Solar system
    Source: Springer Online Journal Archives 1860-2000
    Topics: Computer Science
    Notes: Abstract Within the Jet Propulsion Laboratory in Pasadena, California, state of the art computer graphics animation is done in the Computer Graphics Laboratory. The topics of the animations cover many scientific disciplines. Specific features of the system developed there, both hardware and software, are discussed. The prime mover of the effort is Dr. James F. Blinn of Pasadena; his role and experiences are elaborated. Their current largest project is The Mechanical Universe; the system is used for its production.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01900326
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 124
    Electronic Resource
    Electronic Resource
    The effects of domperidone on the absorption of levodopa in normal subjects (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 721-723 
    Details
    ISSN: 1432-1041
    Keywords: domperidone ; levodopa ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of simultaneous oral administration of 20, 40, or 80 mg domperidone on the pharmacokinetics of an oral 500 mg dose of levodopa was studied in eight normal women. No significant differences in maximum plasma levodopa concentration, the time of its attainment, or the area under the plasma levodopa concentration versus time profile occurred. Domperidone significantly reduced the incidence of adverse gastrointestinal effects due to levodopa administration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00615966
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 125
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of verapamil in patients with hypertension (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 155-163 
    Details
    ISSN: 1432-1041
    Keywords: hypertension ; verapamil ; norverapamil ; pharmacokinetics ; dosing frequency
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twelve hypertensive patients (WHO Stage I-II) were given oral verapamil (Isoptin) b.d. or t.d.s. as long-term treatment. The pharmacokinetics of verapamil and norverapamil were studied both after single and b.d. and t.d.s. doses of verapamil 240, 360 or 480 mg daily adjusted according to the blood pressure response. The apparent oral clearance of verapamil was decreased after both the twice and thrice daily dosage regimens (1.38 and 1.841/min, respectively) as compared to the single dose (4.39 l/min). The plasma half-life of verapamil was increased from 3.34 h (single dose) to 4.65 h (b.i.d.). Decreased elimination of norverapamil was also found after multiple doses of verapamil, as shown by an increase in the adjusted AUC of norverapamil (adjusted to a verapamil dose of 80 mg), namely from 574.9 h·ng·ml−1 (single dose) to 1172 h·ng·ml−1 (b.d.) and to 841 h·ng·ml−1 (t.d.s.). The plasma half-life of norverapamil increase from 5.68 h to 7.34 h during twice daily dosing. During thrice daily verapamil, no increase in plasma half-life was found either for verapamil or norverapamil, probably due to the relatively short sampling time (6 h). The plasma concentration of verapamil and the reduction in supine systolic and diastolic blood pressure were correlated. The mean decrease in supine systolic blood pressure was 5.8 mm Hg per 100 ng verapamil/ml plasma, and for diastolic pressure 2.9 mm Hg per 100 ng verapamil/ml plasma. The mean steadystate plasma concentrations of verapamil were similar after twice and thrice daily dosing regimens, which agrees with the clinical observation that blood pressure control in hypertensive patients is as good after verapamil b.d. and t.d.s.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606652
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 126
    Electronic Resource
    Electronic Resource
    The effect of ranitidine and cimetidine on imipramine disposition (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 285-290 
    Details
    ISSN: 1432-1041
    Keywords: imipramine ; ranitidine ; cimetidine ; pharmacokinetics ; metabolism ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic characteristics of imipramine were studied after a single, oral, 100 mg dose was taken by 12 healthy male subjects following 3 days of pretreatment with placebo, cimetidine (300 mg every 6 h), and ranitidine (150 mg every 12 h) in a randomized, double blind, crossover trial. After each imipramine dose plasma samples were collected for 72 h and assayed for imipramine, desipramine, 2-hydroxyimipramine and 2-hydroxydesipramine by HPLC. Cimetidine preadministration statistically prolonged imipramine t1/2 compared to ranitidine (22.7 vs. 13.0 h) or placebo (10.8 h). Mean imipramine area under the curve (AUC) following cimetidine pretreatment was more than double that following placebo (2.633 vs. 0.966 µg·h·ml−1) or ranitidine (1.14 µg·h·ml−1) pretreatment. Imipramine apparent oral clearance was reduced in all 12 subjects after cimetidine. Compared to ranitidine or placebo, cimetidine pretreatment was associated with an increased imipramine/desipramine AUC ratio, suggesting cimetidine-induced impairment of demethylation of imipramine. Ranitidine was not observed to alter imipramine pharmacokinetics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981125
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 127
    Electronic Resource
    Electronic Resource
    Femoxetine and cimetidine: Interaction in healthy volunteers (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 299-302 
    Details
    ISSN: 1432-1041
    Keywords: femoxetine ; cimetidine ; pharmacokinetics ; drug interaction ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The possibility of a pharmacokinetic interaction between femoxetine and cimetidine has been evaluated in 8 healthy volunteers. Two volunteers received single doses of femoxetine, and 6 were given multiple doses of femoxetine for 7 days with and without concurrent cimetidine. No influence of cimetidine was observed on the kinetics of single doses of femoxetine, but after multiple doses the plasma concentration of femoxetine was significantly increased. Similarly, the AUC at steady state tended to be increased, but not to a significant extent. Concurrent cimetidine did not cause a reduction in the AUC of the active desmethyl metabolite. It is recommended that femoxetine is given in reduced doses (e.g. 400 mg) when administered with cimetidine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981127
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 128
    Electronic Resource
    Electronic Resource
    Transsynovial distribution and protein binding of pirazolac in patients with rheumatoid arthritis (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 307-311 
    Details
    ISSN: 1432-1041
    Keywords: pirazolac ; rheumatoid arthritis ; transsynovial distribution ; synovial fluid drug level ; pharmacokinetics ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Following a washout period of 7 days, twenty-one patients suffering from rheumatoid arthritis and 3 from osteo-arthritis, who all required articular puncture were given a non-steroidal anti-inflammatory drug pirazolac 450 mg b.d. for 7 days. After discontinuation of the treatment the subjects were divided into 4 groups each of 6 patients. The non protein bound fraction of pirazolac in synovial fluid (0.86%) was significantly higher than that in plasma (0.53%). The average pirazolac concentration in plasma within the dosing interval fluctuated between 30.9 µg/ml and 59 µg/ml, and in synovial fluid between 16.6 µg/ml and 29.9 µg/ml. The half-life of pirazolac calculated from the measured and interpolated data from all patients was 30.9 h in plasma and 66.2 h in synovial fluid. The absolute free concentrations in plasma and synovial fluid (approx. 250 ng/ml) were in the range of the IC50-values for inhibition of cyclooxygenase in mouse peritoneal macrophages.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981129
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 129
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of ceftazidime in patients with biliary tract disease (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 327-331 
    Details
    ISSN: 1432-1041
    Keywords: ceftazidime ; cholecystectomy ; pharmacokinetics ; biliary tree tissue level
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After administration of ceftazidime as a 1 g i.v. bolus injection, its concentration was measured by HPLC at frequent intervals in serum, bile and tissue from different parts of the biliary tract in 32 patients undergoing operation for biliary tract disease. In bile from the functioning gallbladder and common bile duct, a high concentration of ceftazidime was found, mean 18.5 and 26.6 mg/l, respectively. In bile from the non-functioning gallbladder, a very low concentration was found (〈1.5 mg/l). Ceftazidime in the gallbladder wall varied considerably with the type and degree of inflammation judged histologically; the mean level was 21.3 mg/kg. The elimination half-life of ceftazidime was 1.74 h, apparent volume of distribution 20.01 and total plasma clearance 133 ml/min. In bile from T-tube specimens a high concentration was found, the mean peak values being 27.2 mg/l. However, biliary excretion of the drug was low at less than 0.5% of the administered dose. These concentrations of ceftazidime were sufficient to inhibit the in-vitro growth of pathogens, namely theEnterobacteriaecae commonly responsible for biliary tract infection.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981132
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 130
    Electronic Resource
    Electronic Resource
    Digoxin-diltiazem interaction: A pharmacokinetic evaluation (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 351-353 
    Details
    ISSN: 1432-1041
    Keywords: digoxin ; diltiazem ; interaction ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of digoxin were studied before and after a 2 week course of diltiazem, 30 mg four times daily, in 7 healthy volunteers. Each subject received an IV dose of digoxin before starting diltiazem and again on day 15 of the study. Diltiazem was continued until all sera and urine were collected. During the control and diltiazem phases, respectively, the terminal elimination rate constants were 0.0231±0.007 h−1 and 0.0254±0.007 h−1, the volumes of distribution were 10.5±3.95 l/kg and 10.2±3.26 l/kg, and the total body clearances were 3.72±0.78 ml·min−1·kg−1 and 4.09±0.94 ml·min−1·kg−1. None of these pharmacokinetic parameters of digoxin were significantly different before or during diltiazem administration. Overall, there does not appear to be an interaction between digoxin and diltiazem.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981136
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 131
    Electronic Resource
    Electronic Resource
    Pharmacokinetic parameters of bevantolol in volunteers (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 375-377 
    Details
    ISSN: 1432-1041
    Keywords: bevantolol ; pharmacokinetics ; beta-blocking drugs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of the new beta-adrenoceptor blocking drug bevantolol and some aspects of its beta-blocking effect have been studied in healthy volunteers. Bevantolol had a short serum half-life (86±33 min) and high systemic availability after oral administration. The observed changes in heart rate, systolic blood pressure during excercise and plasma renin activity were all compatible with beta-adrenoceptor blockade. After 200 mg p.o. in the morning, the effects lasted for less than 24 h.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541549
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 132
    Electronic Resource
    Electronic Resource
    Treatment of liver disease with malotilate. A pharmacokinetic and pharmacodynamic phase II study in cirrhosis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 407-416 
    Details
    ISSN: 1432-1041
    Keywords: malotilate ; cirrhosis ; bioavailability ; liver fibrosis ; metabolite kinetics ; pharmacokinetics ; portal-systemic shunting ; urinary metabolites
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Malotilate, a sulphur-containing compound with antifibrotic and hepatoprotective properties in several animal models, has been investigated in cirrhotic patients. Nine patients with cirrhosis of various aetiologies and severity, and 4 healthy volunteers, participated in a pharmacokinetic study. After a single dose of 500 mg malotilate p.o. peak malotilate plasma concentration measured by GC-MS was 35 times higher in patients (median 0.70 µg/ml) than in controls (median 0.019 µg/ml). The median apparent oral clearance was approximately 50 times lower in cirrhotics (median 2.2l/min) than in healthy volunteers (118l/min). The apparent oral clearance was significantly correlated with indicators of portalsystemic shunting, such as the 2-h postprandial serum bile acids and the bioavailability of oral nitroglycerine. Urinary output of the glucuronidated metabolite-(M3), measured by HPLC, was normal in patients, whereas recovery of metabolite-M6 (resulting from ring opening and loss of sulphur) was reduced. Six patients in an open 6-month trial received malotilate 200 mg t.i.d. for 2 months and 400 mg t.i.d. for 4 months. The thrombocyte count increased and serum ferritin level fell in all patients, and serum cholinesterase rose and IgA decreased in 5 of 6. The other indicators of liver function did not show a significant change. Dry skin was the only possible adverse effect. It is concluded that first-pass elimination of malotilate is dramatically reduced in cirrhotics, and that a smaller amount of the drug reaches the liver in such patients. Malotilate was well tolerated, even in patients with advanced disease.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607952
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 133
    Electronic Resource
    Electronic Resource
    Fluocortolone: Pharmacokinetics and effect on plasma cortisol level (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 433-438 
    Details
    ISSN: 1432-1041
    Keywords: fluocortolone ; pharmacokinetics ; adrenal suppression ; cortisol suppression
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of fluocortolone and its effect on plasma cortisol levels are described after oral administration of 20, 50 and 100 mg to 9 healthy adults. The concentrations of fluocortolone and cortisol in plasma were measured simultaneously by HPLC with UV detection. Fluocortolone was rapidly absorbed after all doses, giving the maximum plasma level after 1.4–2.1 h. After ingestion of 20, 50 and 100 mg, the peak levels were 199, 419 and 812 ng/ml, respectively. The maximum plasma levels and areas under the plasma level-time curves increased in proportion to the dose. Post-maximum plasma levels declined monoexponentially with a half-life of 1.76 h. Plasma half-life (t1/2=1.76 h), volume of distribution (1.03 l/kg) and oral clearance (6.9 ml/min/kg) were independent of the dose. The intensity and duration of adrenal suppression was dose dependent. Maximum suppression was observed 8 hours after fluocortolone. Clearcut suppression of cortisol levels after 24 hours was only seen following 100 mg fluocortolone.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607956
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 134
    Electronic Resource
    Electronic Resource
    Biliary excretion and pharmacokinetics of ceftriaxone after cholecystectomy (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 445-451 
    Details
    ISSN: 1432-1041
    Keywords: ceftriaxone ; cholecystectomy ; cephalosporins ; biliary excretion ; T-drain bile ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Three groups of patients with biliary tract disease treated by cholecystectomy were given ceftriaxone. In Group 1 single doses of 150 mg and 1500 mg were given on Days 1 and 5 after cholecystectomy. In Group 2 2 g was given daily for 6 days and the cholecystectomy was on Day 2. Patients in Group 3 received 2 g every 12 h for 3 to 5 doses before cholecystectomy. Plasma samples, urine and T-drain bile were collected at various times from Groups 1 and 2 patients. Gallbladder bile and plasma were collected from Group 3 patients at the time of cholecystectomy. The mean (±SEM) T-drain bile-to-plasma concentration ratio of ceftriaxone in Groups 1 and 2 was 6.7±0.92. The mean (±SEM) gallbladder bile-to-plasma concentration ratio was 33±4.2. No clinically significant differences were detected between the kinetics of ceftriaxone in the cholecystectomy patients compared to normal volunteers. The usual dosage of ceftriaxone appeared adequate for prophylaxis or treatment of biliary tract infection by susceptible organisms.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607958
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 135
    Electronic Resource
    Electronic Resource
    Methotrexate in erythrocytes of patients with psoriasis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 453-456 
    Details
    ISSN: 1432-1041
    Keywords: methotrexate ; psoriasis ; pharmacokinetics ; p.o. ; i.m. administration ; methotrexate steady-state ; erythrocyte concentration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Methotrexate (MTX) concentrations in erythrocytes in 32 psoriatics treated weekly with MTX p.o. or i.m. have been studied. When treatment had been constant for at least 5 weeks, there was only small variation in erythrocyte MTX (ery-MTX) in the week between two courses of treatment. The ery-MTX was correlated with the weekly dose of MTX. For patients treated with MTX i.m.r=0.87, and in patients given divided oral dosesr was 0.68. There was no difference in ery-MTX between the two routes of administration. No correlation was observed between ery-MTX and the total MTX dose or the length of treatment. During constant MTX administration small variations in ery-MTX were observed. Small changes in the weekly dose of MTX resulted in marked changes in ery-MTX in 4 of the 5 patients studied.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607959
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 136
    Electronic Resource
    Electronic Resource
    Acute effects of clometacin on renal prostaglandin biosynthesis in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 499-501 
    Details
    ISSN: 1432-1041
    Keywords: clometacin ; prostaglandin ; renal excretion ; plasma renin activity ; pharmacokinetics ; non steroidal antiinflammatory agents ; cyclooxygenase inhibitor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 6 healthy subjects the effect of clometacin on renal function, sodium and water excretion, plasma renin activity and urinary excretion of prostaglandins has been studied. After four days of treatment with clometacin, the excretion of urinary prostaglandins E2, F2 α and 6 keto F1 α and thromboxane B2 were reduced by 61.2, 41.2, 59 and 42%, respectively. 62% reduction in plasma renin activity was also observed. There was no significant change in mean blood pressure, heart rate, body weight, creatinine clearance or urinary excretion of sodium. It is concluded that clometacin is an efficient cyclooxygenase inhibitor in healthy individuals with a normal sodium intake, and that caution is required when giving clometacin to patients at risk of developing renal failure during treatment with a cyclooxygenase inhibitor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607969
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 137
    Electronic Resource
    Electronic Resource
    Kinetics of the fab fragments of digoxin antibodies and of bound digoxin in patients with severe digoxin intoxication (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 527-533 
    Details
    ISSN: 1432-1041
    Keywords: digoxin intoxication ; antibody treatment ; pharmacokinetics ; clearance ; distribution volume
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 17 patients with severe digoxin intoxication were successfully treated with 320 to 480 mg Fab fragments of digoxin-specific IgG from sheep. The infusion period ranged between 0.5 and 7 h. Serum and urine concentrations of digoxin bound to Fab fragments, and in 11 cases unbound Fab fragments in serum, were determined during and after the infusion. The renal clearance of bound digoxin and therefore of the antibody was 13.6 ml/min. The median extrarenal clearance of the Fab fragments was 10.9 ml/min. The half-life of the serum concentrations starting at 12 h was 14.3 h, and the value was increased to 25.4 h when regression began at 24 h; the corresponding apparent distribution volumes were 25.9 and 541. These figures exceed the volume of the extracellular space and suggest intracellular penetration of the Fab fragments. The dosage of the antibody should be sufficiently high to bind digoxin in the most severe cases of poisoning. The maximum serum concentrations of bound antibody were 30 mg/l after 3 h and 20 mg/l after 5 h. A loading dose of 160 mg followed by an infusion of 0.5 mg/min was sufficient to absorb digoxin re-diffusing into the serum during the first 8 h. In some cases free digoxin reappeared in the serum 8–12 h after beginning the treatment. This might be prevented by infusing a further ampoule at a rate of 0.1 mg/min or less.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542410
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 138
    Electronic Resource
    Electronic Resource
    Diurnal variation in the pharmacokinetics of intravenous theophylline and etophylline in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 635-636 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; etophylline ; diurnal variations ; i.v. application ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542428
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 139
    Electronic Resource
    Electronic Resource
    Renal effects of pinacidil in hypertensive patients on chronic beta-blocker therapy (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 641-647 
    Details
    ISSN: 1432-1041
    Keywords: pinacidil ; hypertension ; vasodilators ; renal function and — haemodynamics ; beta-blockers ; guanidines ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The acute and chronic effects of pinacidil on blood pressure (BP) and renal function were investigated in 10 patients with moderate arterial hypertension insufficiently controlled by chronic beta-blockade. Acute i. v. administration of pinacidil caused a significant fall in BP of 29.9/18.3 mm Hg and, despite beta-blockade, a concomitant rise in heart rate (HR) of 21%. Renal vascular resistance (RVR) showed a marked reduction as a consequence of the fall in BP, and a transient rise in renal plasma flow (RPF). Diuresis and renal clearance of sodium and uric acid showed a parallel fall. The excretion rates of albumin and β2-microglobulin were also significantly reduced. Pharmacokinetic studies indicated that glomerular filtration was responsible for elimination of the parent drug, and that proximal tubular secretion was the pathway of excretion of the main metabolite, pinacidil pyridine-N-oxide. During therapy for 4 months there was no further significant reduction in BP, despite increases in the daily dose of pinacidil. The effects on HR were less conspicious after 4 months; renal haemodynamic parameters and body weight were not significantly changed. The initial level of RVR and the initial acute reduction in this parameter appeared to be major determinants of the long-term BP response. The drug was well tolerated apart from one patient who developed slight fluid retention. However, concomitant administration of a diuretic will probably be necessary during routine use of this therapeutic combination.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00608209
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 140
    Electronic Resource
    Electronic Resource
    Dosage adjustment for ceftazidime in patients with impaired renal function (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 597-605 
    Details
    ISSN: 1432-1041
    Keywords: ceftazidime ; renal failure ; dosage adjustment ; predicted serum level ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Ceftazidime has good antibacterial activity against many Gram-negative micro-organisms including Ps. aeruginosa. The aim of the present study was to calculate a dosage adjustment regimen for renal failure patients and to test it in a second group of patients. A study was made of the pharmacokinetics of ceftazidime 1 g given as a single bolus i.v. injection in 20 patients in an intensive care unit with varying degrees of renal function, including patients on regular haemodialysis. The serum half-life of elimination (t1/2β) varied from 1.6 to 45 h depending on renal function. During haemodialysis the mean t1/2 was 4.7 h. A good correlation between the renal clearance of creatinine and ceftazidime was observed. In most patients protein binding was lower than previously observed. From the pharmacokinetic data, a dosage adjustment regimen for patients with renal insufficiency was calculated, which studies in 7 further patients showed to be effective.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542421
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 141
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of fluocortolone in man (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 615-617 
    Details
    ISSN: 1432-1041
    Keywords: fluocortolone ; pharmacokinetics ; protein binding ; synthetic corticoid ; clearance ; volume of distribution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of the synthetic corticoid fluocortolone was determined in 9 healthy female volunteers after a single oral dose of 20 mg. The maximal plasma level fluocortolone (Cmax) of 202±70 ng/ml occurred within 85±32 min of oral intake after which it declined monoexponentially. Total plasma clearance was 6.48±2.07 ml/min·kg and the clearance of unbound fluocortolone was 60.38±26.67 ml/min·kg. Plasma protein binding was 83 to 95%. The volume of distribution at steady-state was 1.01±0.34 l/kg for total fluocortolone and 11.21±3.77 l/kg for unbound drug. The results of the study characterize the kinetics of unbound fluocortolone for the first time. In addition, the kinetics of total fluocortolone presented here confirm values calculated previously.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542423
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 142
    Electronic Resource
    Electronic Resource
    Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 177-182 
    Details
    ISSN: 1432-1041
    Keywords: glibenclamide ; bioavailability ; pharmacokinetics ; dissolution ; hypoglycaemia ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A study has been carried out investigating four different marketed oral preparations of glibenclamide, correlating the effectiveness of the drug in these preparations in lowering plasma glucose concentrations with (i) the in vitro dissolution of the drug, measured by the British Pharmacopoeal and Desaga methods, and (ii) the in vivo bioavailability, assessed in 12 healthy human volunteers. The two dissolution methods yielded different rank orders of ease of dissolution of the drug from the various preparations; the findings of neither dissolution method correlated adequately with the results of the in vivo bioavailability studies, which correctly predicted the abilities of the preparations to reduce plasma glucose concentrations. Relative to an oral glibenclamide solution the bioavailabilities of the drug from three tablet preparations were 0.69, 0.49 and 0.24. The mean elimination half-life of the drug was 1.5 h and assuming complete bioavailability of the drug from oral solution the mean systemic clearance was 0.095 l kg−1h−1, and the mean apparent volume of distribution was 0.20 l kg−1. It is concluded that it may be unsafe to use in vitro dissolution data as a basis for assessing the bioequivalences of different glibenclamide preparations intended for oral use.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606655
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 143
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and effects on blood pressure of a single oral dose of milrinone in healthy subjects and in patients with renal impairment (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 549-553 
    Details
    ISSN: 1432-1041
    Keywords: milrinone ; renal impairment ; hypertension ; pharmacokinetics ; healthy subjects ; antihypertensive effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Milrinone, a new, nonglycosidic inotropic agent with peripheral vasodilating properties, was given as a single oral 5 mg dose to 7 healthy subjects, 7 patients with moderate renal impairment (CRI I, creatinine clearance 30–63 ml/min) and 7 patients with severe renal impairment (CRI II, creatinine clearance 9–29 ml/min). All except one of the patients with renal impairment had hypertension. The mean urinary recovery of milrinone was 82% in healthy subjects, the renal clearance was 288 ml/min and the plasma half-life (t1/2) was 0.94 h. In CRI the mean plasma t1/2 was prolonged (CRI I 1.78 h, CRI II 3.24 h). There was a significant linear relationship between creatinine clearance and the elimination rate constant, and between creatinine clearance and the renal clearance of milrinone. During the study day there was a tendency to a decrease in supine BP from 1 to 6–8 h after dosing, with the maximal decrease at 2–3 h (healthy subjects 118/71→107/56, CRI 159/95→136/79 mmHg). The same degree of change was seen in standing BP. A slight rise in standing HR was seen from 2–6 h after dosing. Changes in BP and HR are difficult to evaluate since the study was not placebo-controlled. The plasma elimination rate of milrinone was decreased in CRI and dose adjustment may be necessary. Placebo-controlled studies of milrinone in hypertensive patients would be required to validate its possible antihypertensive effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635891
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 144
    Electronic Resource
    Electronic Resource
    The pharmacokinetics of timegadine and two of its metabolites after multiple oral dosing, and the effects of concomitant administration of ibuprofen (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 581-586 
    Details
    ISSN: 1432-1041
    Keywords: timegadine ; ibuprofen ; anti-inflammatory ; pharmacokinetics ; enzyme induction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A 250 mg tablet of timegadine was given twice daily for 15 days to 13 healthy volunteers. On Day 16 a single morning dose of timegadine was supplemented by two 200 mg tablets of a proprietary brand of ibuprofen. Serum concentrations of timegadine were measured by high pressure liquid chromatography, and steady state was achieved between Days 5 and 8. Serum concentrations of two metabolites of time-gadine, MI and MII were measured by thin layer chromatography by Leo Pharmaceutical Products, Denmark. Ibuprofen did not significantly affect the serum half-time of timegadine, but did reduce the maximum measured serum timegadine concentration, the area under the serum concentration versus time curve and the time to achieve maximum measured serum concentration. Serum liver enzymes remained within the normal ranges and there were no changes in hepatic microsomal enzyme activity as assessed by urinary excretion ofD-glucaric acid.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635896
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 145
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of teicoplanin in patients on continuous ambulatory peritoneal dialysis (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 501-504 
    Details
    ISSN: 1432-1041
    Keywords: teicoplanin ; continuous ambulatory peritoneal dialysis ; pharmacokinetics ; antibiotic
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the pharmacokinetics of teicoplanin, a new glycopeptide antibiotic active against Gram-positive aerobic and anaerobic bacteria, in five patients with end-stage renal disease on continuous ambulatory peritoneal dialysis (CAPD). Although teicoplanin was eliminated in the peritoneal fluid, relatively little was recovered (6.8±1.2% of the given dose). The following values were obtained: elimination half-time 102–347 h; total body clearance 4.16–7.38 ml·h−1·kg−1, peritoneal clearance 0.31–0.37 ml·h−1·kg−1. Because the elimination of teicoplanin is about four times less in patients undergoing CAPD compared with subjects with normal renal function, the dose of teicoplanin should be reduced appropriately in such cases.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613532
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 146
    Electronic Resource
    Electronic Resource
    The action of cisapride on gastric emptying and the pharmacodynamics and pharmacokinetics of oral diazepam (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 205-208 
    Details
    ISSN: 1432-1041
    Keywords: cisapride ; diazepam absorption ; drug interaction ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of the benzamide cisapride (C) (8 mg) i.v. have been compared to placebo (P) in a double blind randomised study. The effects on gastric emptying, the absorption and effects of oral diazepam, and BP and pulse were observed. Cisapride increased the rate of gastric emptying of 500 ml liquid containing diazepam 10 mg (t1/2 C: 7.4 min, P: 14.9 min). The initial rate of absorption of diazepam contained in the drink was increased by C (AUC 0–1 h C: 328 µg h 1−1, P: 253 µg h 1−1, but there was no change in overall bioavailability. This change in diazepam kinetics was associated with a significantly greater impairment in reaction time in the first 45 min after drinking but not in self rated sedation. Cisapride produced a significant tachycardia (e.g. after 10 min C: 82 beats/min, P: 69 beats/min) which probably reflects a peripheral vasodilator action. Cisapride may therefore alter the pharmacokinetics and dynamics of concurrently administered drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614304
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 147
    Electronic Resource
    Electronic Resource
    Isosorbide dinitrate in plasma and dialysate during haemodialysis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 187-190 
    Details
    ISSN: 1432-1041
    Keywords: isosorbide dinitrate ; haemodialysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 10 patients with end stage renal disease on regular haemodialysis the plasma concentrations and dialyzer clearance of isosorbide dinitrate (ISDN) were determined after an oral dose of a retarded release formulation of 60 mg ISDN. The maximal plasma concentration of ISDN 2–7 h after oral administration was higher (14 ng/ml) than has been reported in healthy volunteers. The haemodialyzer clearance of ISDN was 92.4 ml/min at a blood flow of 200 ml/min and dialysate flow of 500 ml/min. During a 5-h haemodialysis an average of 0.3 mg ISDN was removed from the patient's circulation, representing about 0.5% of the administered dose and about 3% of the available drug in the circulation. No influence of haemodialysis on the plasma level of ISDN was found.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614300
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 148
    Electronic Resource
    Electronic Resource
    Effects of probenecid on enprofylline kinetics in man (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 221-223 
    Details
    ISSN: 1432-1041
    Keywords: enprofylline ; probenecid ; pharmacokinetics ; renal elimination ; active secretion ; drug interaction ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Enprofylline 1 mg/kg, a new potent antiasthmatic xanthine derivative, which is mainly eliminated by renal excretion, was given intravenously to 6 normal subjects with and without oral pretreatment with 1 g probenecid. The latter caused a drop in the average total body clearance of enprofylline from 21 to 9.8 l/h, and in the average renal clearance from 17 to 8.0 l/h. The average half-life increased from 1.8 to 3.0 h. The volumes of distribution, Vz and Vss, both fell by about 25%, indicating that probenecid had restricted the distribution of enprofylline in the body. The plasma protein binding of enprofylline was not altered by probenecid. The results confirm the opinion that active tubular secretion accounts for a large proportion of the total elimination of enprofylline.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614308
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 149
    Electronic Resource
    Electronic Resource
    Alfentanil kinetics in renal insufficiency (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 245-247 
    Details
    ISSN: 1432-1041
    Keywords: alfentanil ; uraemia ; i.v. administration ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Alfentanil 100 µg/kg was administered as an i.v. bolus to 9 patients with severe chronic renal dysfunction (creatinine clearance 1.0±1.2 ml/min) requiring regular haemodialysis. Plasma alfentanil concentrations were measured by a specific radioimmunoassay. Individual plasma concentration-time curves were fitted to a two-compartment open model. Mean distribution and elimination half-lives were 3.7 min and 58 min, respectively. The apparent volumes of distribution of the central compartment and the total volume of distribution at steady-state were 91 ml/kg and 304 ml/kg, respectively. Alfentanil plasma clearance was 5.3±2.5 ml/min/kg. All the patients tolerated alfentanil well and no side-effects nor delayed recovery were observed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614313
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 150
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of intravenous and intraperitoneal moxalactam in chronic ambulatory peritoneal dialysis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 299-302 
    Details
    ISSN: 1432-1041
    Keywords: moxalactam ; continous ambulatory peritoneal dialysis ; pharmacokinetics ; intraperitoneal administration ; i.v. injection
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of moxalactam has been investigated in 10 subjects undergoing continuous ambulatory peritoneal dialysis (CAPD). A single 1 g dose was injected i.v. and a 1 g dose was given intraperitoneally in the CAPD fluid during a 4 h dwell-time. Moxalactam was assayed by HPLC. After i.v. injection, the serum kinetics of moxalactam were: plasma t 1/2=17.9 h; volume of distribution at steady-state, 0.27 l/kg; total plasma clearance, 12.8 ml/min; peritoneal clearance, 2.1 ml/min. Dialysate moxalactam concentrations rose rapidly but only 20% of the dose was eliminated by the peritoneal route. After intraperitoneal instillation, moxalactam appeared in the serum rapidly and the peak serum concentration ranged from 21 to 49 µg/ml after between 4 and 5 h. The absorption of moxalactam from the peritoneal space was 57±16%. The data suggest that moxalactam has bidirectional exchange characteristics through the peritoneal membrane. Instillation of moxalactam in CAPD fluid may permit rapid absorption and the appearance of a therapeutic serum concentration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541532
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 151
    Electronic Resource
    Electronic Resource
    Cefodizime penetration into skin suction blister fluid following a single intravenous dose (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 295-298 
    Details
    ISSN: 1432-1041
    Keywords: cefodizime ; skin suction blister fluid ; pharmacokinetics ; protein binding ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cefodizime pharmacokinetics was investigated, evaluating drug concentrations in serum, skin suction blister fluid (SBF), saliva and urine in six healthy male subjects who were administered a 1-g dose intravenously. Serum levels in five subjects can be described according to a two-compartment open model; terminal half-life is 181±14 min. Volume of distribution (Vdβ) amounts to 15.3±1.61, serum clearance to 59±6 ml/min, renal clearance to 33±3 ml/min. Of the administered dose, 54% is renally excreted unchanged within 27 h. Unbound drug fraction in serum is 19.0% and in SBF 38.4%. Thus renal clearance of free cefodizime amounts to 172 ml/min, Vdss to 68.91 (free drug). Whereas cefodizime has not been detected in saliva samples, SBF concentration 3–9 h post administration parallel serum levels, amounting to 40% of the respective serum concentration. At 9 h, unbound cefodizime concentrations in SBF amount to 1.4±0.4 µg/ml, this value being well above the MIC90% values of many clinically relevant bacteria.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541531
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 152
    Electronic Resource
    Electronic Resource
    Methods of comparing pharmacokinetics of slow release preparations: a comparison of “Theo-Dur” and “Phyllocontin” in patients with asthma (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 313-317 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; aminophylline ; slow release formulations ; bronchial asthma ; pharmacokinetics ; methods of comparison
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of two slow release theophylline preparations “Theo-Dur” (T) containing theophylline only and “Phyllocontin” (P) containing aminophylline have been compared in 12 patients with asthma. Each patient received both treatments in random order. The dose of treatment administered 12 hourly was increased or decreased to produce plasma theophylline concentrations of 10–20 mg/l at clinic visits normally 7 to 8 h after dosing. Pharmacokinetic studies were carried out after at least one week's treatment with this dose. After the first study day patients were crossed over to the second treatment at a dosage providing a similar amount of theophylline. They returned for a second study day after at least one week. Comparison of the dose corrected AUC, time to peak concentrations, within patient coefficients of variation (CV), number of concentration time points falling within 25% of Cmax and percentage fluctuations in plasma concentration showed no significant differences between the two preparations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541535
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 153
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of ergotamine in healthy volunteers following oral and rectal dosing (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 331-334 
    Details
    ISSN: 1432-1041
    Keywords: ergotamine ; pharmacokinetics ; volunteers ; mass spectrometry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twenty-four healthy volunteers participated in a study on the disposition of ergotamine following oral and rectal administration. Plasma samples were collected surrounding each dose of medication and a new mass spectrometry method was used for quantitation of the samples. A mean peak plasma concentration of 454 pg/ml was measured an average of 50 min following a 2 mg rectal dose. In contrast, the 2 mg oral dose produced a mean peak plasma concentration of 21 pg/ml an average of 69 min following the dose. Area under the concentration time curve indicated a relative bioavailability of 5% for the oral dosage form. Conflicting data on ergotamine disposition highlight the factors which may be responsible for determining bioavailability and pharmacologic activities of the compound.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541538
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 154
    Electronic Resource
    Electronic Resource
    Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 323-329 
    Details
    ISSN: 1432-1041
    Keywords: methylprednisolone ; prednisolone ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition and plasma binding of methylprednisolone were examined in seven normal volunteers following the administration of 5, 20 and 40 mg of intravenous methylprednisolone sodium succinate. Methylprednisolone exhibits linear plasma protein binding averaging 77%. The mean plasma methylprednisolone clearance of 337 ml·h−1. kg−1 was independent of dose. The steroid appears to moderately distribute into tissue spaces with a mean volume of distribution of 1.41·kg−1. Methylprednisolone disposition parameters were compared with the non-transcortin bound parameters for prednisolone. The prednisolone plasma clearance based on the transcortin free-drug is similar to methylprednisolone total plasma clearance. However, the corrected volume of distribution of prednisolone is only one-half that of methylprednisolone. The disposition rate of these two steroids is thus similar, in spite of their metabolic control by different enzymatic pathways and major influence of saturable transcortin binding on prednisolone elimination.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541537
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 155
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of isosorbide-5-nitrate in renal failure (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 349-350 
    Details
    ISSN: 1432-1041
    Keywords: isosorbide-5-nitrate ; renal failure ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of the antianginal drug isosorbide-5-nitrate (IS-5-N) was studied in 20 patients with varying degrees of chronic renal failure after repeated oral doses of standard 20 mg tablets t.d.s. Blood samples were taken in the steady state on the 2nd and 28th days, and the plasma level was assayed by HPLC. There was no statistically significant difference in C max ss , t1/2 and AUC 0–8 ss between the 2nd and 28th days, nor was a difference found between patients with mild and severe renal failure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541542
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 156
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of oral terguride in patients with a prolactinoma (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 363-365 
    Details
    ISSN: 1432-1041
    Keywords: terguride ; prolactin ; pharmacokinetics ; mean residence time ; prolactinoma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of oral terguride 1 mg was evaluated in a single-dose study in 8 patients with a prolactinoma and one with acromegaly. A radioreceptor assay was used to measure the plasma levels of terguride. The peak plasma concentration (2.3±0.7 ng/ml, mean±SEM) was attained within 1 h of drug administration. Moment analysis gave a mean residence time of 4.3±0.6 h. Plasma prolactin was also determined by radioimmunoassay. The plasma prolactin was reduced to 30±3% of its pretreatment value after 4 h.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541546
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 157
    Electronic Resource
    Electronic Resource
    Effect of cimetidine on digoxin disposition in peptic ulcer patients (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 489-491 
    Details
    ISSN: 1432-1041
    Keywords: cimetidine ; digoxin ; drug interference ; urinary excretion ; ulcer patients ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cimetidine inhibits the renal tubular secretion of creatinine and digoxin is partly excreted by the same pathway. In order to investigate a possible interaction between the two drugs, a randomized cross-over acute study has been conducted. Six patients with duodenal ulcers were given a single dose of digoxin (Dig) 0.75 mg i.v. with and without oral cimetidine 1200 mg/day. Cimetidine significantly reduced creatinine clearance from 157 to 132 ml/min. There was no significant difference in inulin clearance, 99.2 vs 97.5 ml/min, Dig elimination half life 53.9 vs 56.9 h, apparent volume of distribution 11.3 vs 11.6 l/kg, systemic clearance 2.42 vs 2.35 ml/min/kg, renal clearance 1.48 vs 1.62 ml/min/kg or urinary excretion of digoxin 49.5 vs 51.6% of dose without or with cimetidine. These results suggest that cimetidine does not influence the disposition of digoxin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607966
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 158
    Electronic Resource
    Electronic Resource
    Pharmacodynamics and pharmacokinetics of three different doses of urapidil infused in hypertensive patients (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 549-552 
    Details
    ISSN: 1432-1041
    Keywords: urapidil ; pharmacodynamics ; pharmacokinetics ; hypertension
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The study was designed to follow the haemodynamic effects and pharmacokinetics under steady-state conditions of three different doses of urapidil infused continuously. Nine male hypertensive patients received three randomly assigned intravenous infusions of 32.5, 65 and 130 mg urapidil, over 14 h during 6 consecutive days, in a change-over fashion. Blood pressure and heart rate were measured over a period of 28 h after the infusion began and were compared with a reference profile obtained prior to the treatment periods. Urapidil and its main metabolite, parahydroxylated urapidil, were also determined for 28 h after the infusion began using HPLC. The 32.5 mg dose of urapidil caused a maximum decrease in systolic blood pressure of 33±8 mmHg, the 65 mg dose a maximum decrease of 39±12 mmHg and the 130 mg dose a maximum decrease of 50±12 mmHg. The 32.5 and 65 mg doses resulted in similar serum urapidil concentrations, with maximum levels in the 100 to 200 ng/ml range, and the 130 mg dose caused a maximum level approximately four times that achieved with the 32.5 mg dose. The serum concentration of parahydroxy urapidil was proportional to the corresponding dose of urapidil. Four patients reported mild headache, fatigue, weakness, pressure in the head, perspiration and orthostatic dysregulation. The side-effects were probably drug related but required no specific therapy. In summary, the 32.5 mg dose of urapidil resulted in a pronounced decrease in blood pressure. The average pressure reduction over the 14-h infusion period showed further dose-dependent increases after the 65 and 130 mg doses. In severe hypertension, the 130 mg dose can be employed, since it does result in a further, significantly larger decrease in blood pressure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542413
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 159
    Electronic Resource
    Electronic Resource
    Potential pulmonary uptake and clearance of morphine in postoperative patients (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 567-574 
    Details
    ISSN: 1432-1041
    Keywords: morphine ; lung clearance ; pharmacokinetics ; physiological model ; diabetes mellitus ; postoperative state
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of lung uptake and lung clearance on the disposition of morphine was studied in surgical patients. In the postoperative period morphine was given intravenously by a two-rate infusion regimen. Under steady-state conditions samples of mixed central venous blood (pulmonary artery) and peripheral arterial blood (radial artery) were taken simultaneously and at the same time cardiac output was measured. The concentration differences between venous and arterial blood were used to calculate the extraction ratio of morphine across the lung. In all patients there was marked pulmonary uptake, but the concentration differences in most of them were small under steady-state conditions. The extraction ratio (mean ±SD) across the lung was 0.06±0.10, implying insignificant lung clearance. However, in two patients, both with diabetes mellitus, there was a significant concentration gradient, indicating that the lung could contribute to the total body elimination of morphine. On the other hand, the total clearance was similar in diabetic and nondiabetic patients (1190 and 1150 ml/min, respectively), implying that pulmonary clearance would have no significant influence on the kinetics of morphine. A physiologically based pharmacokinetic model was used to describe the disposition of morphine in postoperative patients. The model allowed simulation of pulmonary diffusion, uptake and elimination and supported conclusions based on model-independent experimental data.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542416
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 160
    Electronic Resource
    Electronic Resource
    Comparative single dose and steady-state pharmacokinetics of bevantolol in young and elderly subjects (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 699-704 
    Details
    ISSN: 1432-1041
    Keywords: bevantolol ; pharmacokinetics ; young and elderly subjects ; metabolite ; accumulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of bevantolol were examined following single and repeated oral doses to young and elderly volunteers. Following administration of a single 200-mg bevantolol tablet mean maximum plasma bevantolol concentrations in young and elderly subjects were 1690 ng/ml and 1810 ng/ml, respectively. Maximum bevantolol concentrations occurred approximately 1.1 h postdose in both young and elderly subjects. There were no significant differences in mean steady state bevantolol concentrations on Day 14 between young and elderly subjects. However, disproportionate increases in Cmax, and in AUC, but not in tmax values were observed between Days 1 and 14. On Days 1 and 14, most young and elderly subjects exhibited monoexponential decline in bevantolol plasma concentrations after absorption phase. In those subjects Day 14 elimination half-lives in young and elderly were 1.9 and 2.2 h, respectively. In subjects who exhibited biexponential decline in bevantolol, an age effect in elimination became apparent, on Day 14 elimination half-lives were 5.7 and 11.2 h in young and elderly subjects, respectively. Bevantolol Metabolite III concentrations were observed in plasma of some subjects during the first 6 h after dosing. At steady-state AUC (0-ldc) values for the metabolite were less than 2% those of bevantolol. Bevantolol plasma levels accumulate to a small extent with repeated 200 mg daily doses. This is probably due to the contribution of a late and more persistent terminal elimination phase that was discernable in only certain individuals.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00608218
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 161
    Electronic Resource
    Electronic Resource
    Cefmenoxime kinetics during continuous ambulatory peritoneal dialysis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 713-717 
    Details
    ISSN: 1432-1041
    Keywords: cefmenoxime ; peritoneal dialysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of the aminothiazolyliminomethoxy cephalosporin, cefmenoxime, were determined after a 30 min intravenous infusion of 15 mg/kg body weight in 6 adult subjects undergoing continuous ambulatory peritoneal dialysis. Concentrations of cefmenoxime in serum, urine and dialysate were determined by high-pressure liquid chromatography. The mean peak serum concentration was 92.8±11.6 µg/ml and the harmonic mean for the elimination half-life was 5.46 h. The volume of distribution at steady-state was 14.60±3.01 l/kg. Total body clearance of the drug was 31±7.7 ml/min with 8±5% and 5.75±2.72% of the administered dose being eliminated by renal and peritoneal clearance, respectively. Peritoneal clearance for all exchanges (n=24) was 1.93±68 ml/min. These data suggest that peritoneal losses of this drug are minimal and doses conventionally employed in advanced renal failure can be utilized in the management of systemic infections.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00608221
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 162
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of cimetidine after subchronic administration (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 741-744 
    Details
    ISSN: 1432-1041
    Keywords: cimetidine ; subchronic administration ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of cimetidine on its own pharmacokinetics after subchronic administration was assessed in 8 healthy volunteers, aged 26–29 years. On control Day 1, each subject received cimetidine 300 mg i.v., and serum and urine samples were obtained. Each subject was initiated on cimetidine 600 mg b.i.d. orally for 2 weeks. There were 3 further study days repeated after 1 and 2 weeks of cimetidine dosing and 1 week after stopping cimetidine. There was no significant difference in the mean total body clearance of cimetidine among the 4 study days. Mean elimination t1/2β and Vβ were similarly unchanged. However mean renal clearance (CLR) and fe were significantly increased following 2 weeks of drug dosing (CLR 5.41 ml·min−1 kg−1; fe 0.61) compared to control (CLR 4.00 ml·min−1·kg−1; fe 0.48). Although the non renal clearance was reduced from control values of 4.29 to 3.51 ml·min−1·kg−1 following 2 weeks of dosing the difference was not significant. Dosage adjustment of cimetidine appears unnecessary after short-term dosing in the presence of normal renal function.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00608228
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 163
    Electronic Resource
    Electronic Resource
    Study of the elimination kinetics of torasemide, a novel loop diuretic, in renal insufficiency (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 49-51 
    Details
    ISSN: 1432-1041
    Keywords: torasemide ; pharmacokinetics ; kidney insufficiency
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma concentration of torasemide was determined as a function of time in 8 patients with impaired renal function (creatinine clearance ⩽25 ml/min). The elimination half-life (1.3 to 3.8 h), the volume of distribution (0.12 to 0.29 l/kg), and the total body clearance (0.02 to 0.10 l/kg·h) were similar to those observed in normal volunteers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541467
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 164
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of oral glycerol-1-nitrate (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 169-175 
    Details
    ISSN: 1432-1041
    Keywords: glycerol-1-nitrate ; plasma concentration ; pharmacokinetics ; urinary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma kinetics and urinary excretion of glycerol-1-nitrate (G-1-N), a water soluble metabolite of glycerol trinitrate with anti-anginal potential, have been investigated in healthy human volunteers following oral doses of 10, 20 and 40 mg tablets and 20 mg as drops. In all volunteers G-1-N was rapidly absorbed. The mean concentration-time curves peaked 40 min after administration of tablets at 144 ng/ml (10 mg), 308 ng/ml (20 mg) and 573 ng/ml (40 mg). After the drops the peak of 324 ng/ml occurred at 1 h. The areas under the G-1-N concentration-time curve and the G-1-N peak heights were linear with dose. Tablets and drops can be regarded as bioequivalent with respect to area under the curve and elimination half-life. The bioavailability of the 20 mg tablet relative to the 20 mg drops was 98.6% in terms of area under the curve. The mean apparent half-life of G-1-N elimination from plasma was 2.69±0.67 h (n=46). The mean residence time of G-1-N in the body was 4.65 h compared to 0.28 h for glycerol trinitrate after buccal administration. Female volunteers were found to have significantly lower areas under the curve than male volunteers. The difference was probably due to differences in body weight. Renal excretion does not play an important role in the elimination of oral G-1-N from the body. An overall average of 5.42% of the G-1-N dose was excreted in the urine; free drug accounted for 4.02% and conjugated drug for 1.40%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606654
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 165
    Electronic Resource
    Electronic Resource
    Penbutolol pharmacokinetics: the influence of concomitant administration of cimetidine (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 555-560 
    Details
    ISSN: 1432-1041
    Keywords: cimetidine ; penbutolol ; pharmacokinetics ; drug metabolism ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A possible interaction of penbutolol and cimetidine was investigated in healthy volunteers treated orally for 7 days. The plasma levels of unmetabolised penbutolol showed a slight but non-significant increase. The biphasic elimination kinetics of penbutolol (half-lives 0.8 and 17 h) was not affected by coadministration of cimetidine. Plasma levels of penbutolol were not significantly altered by chronic treatment with cimetidine, whereas the levels of 4-hydroxypenbutolol and 4-hydroxypenbutolol glucuronide were significantly reduced.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635892
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 166
    Electronic Resource
    Electronic Resource
    Comparison of a controlled-release tablet of salbutamol given twice daily with a standard tablet given four times daily in the management of chronic obstructive lung disease (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 431-436 
    Details
    ISSN: 1432-1041
    Keywords: salbutamol ; asthma ; controlled release tablets ; chronic obstructive lung disease ; pharmacokinetics ; therapeutic effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a double-blind cross-over study 20 patients with reversible airways obstruction were treated either with conventional 4 mg tablets of salbutamol a.i.d., or 8 mg controlled release (CR) tablets of salbutamol b.d. Each treatment was given for 2 weeks. The morning PEFR was significantly higher with the CR tablets (p〈0.05) but although the evening PEFR was also better the difference was not significant. Wheeze was significantly lower (p〈0.05) and extra “rescue” inhalation of bronchodilators was required less often and on fewer occasions during treatment with the CR tablets. Comparison of the 12-h mean plasma salbutamol profile showed a peak and trough every 6 h with the standard tablets, and a flatter profile with a single, lower and delayed peak during the 12 h between CR tablets. Although the minimum and average plasma salbutamol levels were similar in the groups on the two preparations, the maximum plasma level was significantly lower and there was significantly less fluctuation on CR tablets (p〈0.02). The CR and standard tablets had equivalent bio-availability.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613520
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 167
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of naproxen in elderly patients (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 463-468 
    Details
    ISSN: 1432-1041
    Keywords: naproxen ; osteoarthritis ; elderly patients ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of naproxen have been examined in 13 elderly patients (mean age 84.2 years) and in 9 younger patients (mean age 53.9 years) at the end of a 21 day course of therapy with naproxen 500 mg b.d. The mean pre-dose concentration on days 19, 20 and 21 was significantly higher in the elderly patients than in the controls (60.1 vs. 43.3 µ g · ml−1). The AUC (0–24) was significantly higher in the elderly subjects only when normalized for body weight (9.1 vs. 5.4 µg·ml−1·h kg−1 p⩽0.02). The AUC was significantly higher in the elderly group compared to the control group also in the normalized form. The apparent clearance of naproxen was reduced in the elderly compared to the control patients (315 vs. 628 ml·h−1). The percentage protein binding of naproxen was the same in both groups (99.8%) but the free concentration of naproxen was significantly higher in the elderly patients than in the control patients (141 vs. 89.8 ng·ml−1). Although there was no excess of side effects in the elderly patients it is suggested that when naproxen is given to elderly patients, therapy should be started at the lower end of the dosage range.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613525
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 168
    Electronic Resource
    Electronic Resource
    Dose-dependent pharmacokinetics of dexamethasone (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 225-230 
    Details
    ISSN: 1432-1041
    Keywords: dexamethasone ; pharmacokinetics ; dose dependancy ; suppression of cortisol ; healthy females
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The dose dependency of the pharmacokinetics of dexamethasone and its influence on the endogenous secretion of cortisol has been studied in healthy females. The maximum plasma level occurred between 1.6 and 2.0 h after doses of 0.5–3.0 mg independent of the type of administration. AUC, distribution volume, plasma clearance and cmax did not increase in proportion to the dose but only by the factor of about 0.6–0.7 after the oral administration of 0.5–1.5 mg. Comparatively high values were reached after 3.0 mg i.m. This may be due to reduced bioavailability of the oral doses. Within the first 12 h after the administration of 0.5–3.0 mg, endogenous cortisol secretion was influenced independent of dose. However, the suppressive effect after 24 h was dose dependent and amounted to approximately 24% for 0.5 mg p. o., 62% for 1.5 mg p. o. and 90% for 3.0 mg i. m. In the case of administration every second day, the integral reduction within 24 h after the administration of 0.5 mg dexamethasone was 44 to 65% and for 1.5 mg between 59 and 62%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614309
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 169
    Electronic Resource
    Electronic Resource
    Renal excretion and pharmacokinetics of methotrexate and 7-hydroxy-methotrexate following a 24-h high dose infusion of methotrexate in children (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 231-238 
    Details
    ISSN: 1432-1041
    Keywords: methotrexate ; hydroxymethotrexate ; lymphoid malignancy ; renal excretion ; metabolism ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In children with lymphoid malignancies 18 courses of methotrexate (18–200 mg/kg) administered as a 24-h infusion were monitored. Plasma concentrations and renal excretion rates of methotrexate (MTX) and 7-hydroxymethotrexate (7-OHMTX) were determined. A low correlation was found between the administered dose of MTX and the body exposure to MTX or 7-OHMTX. Although 84% of the MTX eventually recovered from the urine was excreted during the 24 h of the infusion, the renal clearance of MTX was markedly lower during the time of the infusion than after it. There were courses with a low and others with a high renal clearance of MTX during the infusion, despite the same urine flow. A low MTX renal clearance was correlated with a high body exposure to MTX. As the same variations were also seen in the same patient during successive courses, pharmacokinetical characterization of patients appears questionable. The renal clearance of 7-OHMTX was significantly lower than the renal clearance of MTX, and the body exposure to 7-OHMTX ranged from 2–40% of the MTX body exposure. Treatment courses with a low or a high body exposure to 7-OHMTX were not associated with different urinary recoveries of the metabolite. Differences in MTX hydroxylation could not be substantiated. Because the concentration of 7-OHMTX is high soon after the end of an infusion, a specific method of MTX determination should be chosen for controlling treatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614310
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 170
    Electronic Resource
    Electronic Resource
    Curve-fitting in pharmacokinetics — A comparison between gamma-and biexponential fits (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 243-244 
    Details
    ISSN: 1432-1041
    Keywords: gamma distributions ; exponentials ; clearance ; mean residence time ; curve fitting ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Seven sets of plasma concentration-time data were fitted to both a conventional biexponential equation and a gamma equation. The values of clearance (CL) and mean residence time (MRT) were calculated from the fitted parameters and compared with the values calculated by the trapezoid rule. Both the biexponential and gamma equations provided adequate fits to the data. The values of CL and MRT calculated from the biexponential fits correlated very closely with the values calculated by the trapezoid rule, but there were large discrepancies between the values calculated from the gamma fits and the trapezoid rule. The biexponential model appears to be less sensitive to scatter in the data.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614312
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 171
    Electronic Resource
    Electronic Resource
    Ceftriaxone pharmacokinetics during peritoneal dialysis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 303-307 
    Details
    ISSN: 1432-1041
    Keywords: ceftriaxone ; peritoneal dialysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The purpose of this study was to investigate the pharmacokinetics of intraperitoneally (IP) administered ceftriaxone (CRO) in patients maintained on chronic peritoneal dialysis. A single 2 g dose of CRO was administered IP to six adult patients who did not have peritonitis at the time of study. After a 5 hour dwell, the peritoneal fluid was exchanged with CRO-free fluid. Exchanges were carried out every 4 to 8 h, over a 24- to 28-h period. The peak total plasma CRO concentration was 104 µg/ml. An average of 74.1% of the IP dose of CRO was absorbed. Plasma protein binding was nonlinear; mean free fraction ranged from 12.8 to 17.9% at low and high concentrations. Dialysate concentrations at the end of subsequent exchanges ranged from means of 19.9 to 2.9 µg/ml. Total CRO clearance from plasma was 10.1 ml·kg−1·h−1 and the mean terminal t1/2 was 12.7 h. Dialytic clearance averaged 0.69 ml·kg−1·h−1, only 6.9% of total clearance. A model which incorporates known characteristics of CRO binding and distribution in anuric patients was used to simulate plasma and peritoneal concentrations of CRO during multiple dose IP drug administration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541533
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 172
    Electronic Resource
    Electronic Resource
    Circadian changes in the absorption and elimination of theophylline in patients with bronchial obstruction (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 309-312 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; asthma ; absorption ; elimination ; pharmacokinetics ; circadian changes ; bronchial obstruction ; slow release preparation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Circadian variation in the serum concentration of theophylline has been reported in most patients receiving slow release oral preparations. To examine further the mechanism and clinical relevance of this change, an investigation has been made into the diurnal fluctuation in elimination kinetics during i.v. administration of theophylline and its serum concentration profile on oral treatment with a slow release preparation, in 8 hospitalized patients receiving it for bronchial obstruction. After reaching steady-state on a constant intravenous infusion, the total body clearance of theophylline (CL) was determined every 4–6 h from the steady-state concentration and the infusion rate. No systematic trend indicative of circadian changes in elimination kinetics was observed. The intraindividual fluctuation in CL during the observation period was small (coefficient of variation 4–11%). In contrast, on oral dosing a smaller area under the serum concentration-time curve was found during the night time (22.00–06.00). The results show that the circadian variation described in serum theophylline concentrations is due to delayed absorption at night. The elimination kinetics of theopyhlline do not change.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541534
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 173
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of isoniazid: Influence of age (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 335-340 
    Details
    ISSN: 1432-1041
    Keywords: isoniazid ; pharmacokinetics ; age dependent differences ; pulmonary tuberculosis patients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The distribution of the acetylator phenotype of isoniazid was studied in 458 patients of different ages, and the influence of age on its apparent distribution volume, clearance and half-life was investigated in slow and rapid acetylators. The doses of isoniazid for the patients were determined according to the inactivation index method, as described by Vivien. Apparent distribution volume showed no difference between slow and rapid acetylators but it did decrease significantly with age. Clearance and half-life varied significantly in slow acetylators, and these variations led to a decrease in the necessary dose of isoniazid.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541539
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 174
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of nimodipine in patients with aneurysmal subarachnoid haemorrhage (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 421-425 
    Details
    ISSN: 1432-1041
    Keywords: nimodipine ; subarachnoid haemorrhage ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Patients with a ruptured supratentorial aneurysm undergoing early surgery after the subarachnoid haemorrhage were treated postoperatively with nimodipine to prevent delayed ischaemic dysfunction. It was given first as a continuous intravenous infusion 2 mg/h (mean dose 0.5 µg/kg/min) for at least 7 days, and then orally (45 mg × 6) for at least a further 7 days. During the i.v. infusion, the mean plasma concentration was 26.6±1.8 ng/ml. The plasma clearance ranged from 0.57 to 1.77 l/kg/h and was negatively correlated with the age of the patient. Immediately prior to successive oral doses, the mean plasma concentration was 13.2 ng/ml (range〈3–38.8 ng/ml). The peak level was usually found after 1 h; it ranged from 7.0–96.0 ng/ml. Mean bioavailability was 15.9%. The nitropyridine metabolite was found in measurable concentrations only after oral treatment with nimodipine. In some cases, the concentration of metabolite exceeded that of the parent compound. The three patients investigated who developed delayed ischaemic dysfunction had plasma concentrations well within the range in patients who did not, so it seems unlikely that the therapeutic failure could be attributed to individual deviations in the pharmacokinetics of the drug.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607954
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 175
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and quantitative characterization of cefotiam excretion after intravenous administration to patients after cholecystectomy (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 439-444 
    Details
    ISSN: 1432-1041
    Keywords: cefotiam ; pharmacokinetics ; clearance ; urinary excretion ; biliary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six patients, aged 52 to 71 years, with T-tube drainage of the common bile duct and a urinary catheter after cholecystectomy, were studied in order to evaluate the urinary and biliary excretion and pharmacokinetics of cefotiam in the early postoperative period. Each patient received cefotiam 1 g i.v. as a bolus injection. Cefotiam in plasma, urine, and bile were determined by HPLC. A 2-compartment open model with elimination from the central compartment satisfactorily fitted the plasma levels of the drug. The renal clearance of cefotiam (CLR=133 ml/min) was an order of magnitude greater than its biliary clearance (CLB=11.8 ml/min). Glomerular filtration was the main mechanism for elimination of cefotiam. The values of CLR and CLB in relation to the total plasma clearance (CL=138. ml/min) demonstrated the negligible role of metabolism in elimination of cefotiam in these patients.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607957
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 176
    Electronic Resource
    Electronic Resource
    Influence of dose and route of administration on disposition of metronidazole and its major metabolites (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 467-473 
    Details
    ISSN: 1432-1041
    Keywords: metronidazole ; metabolism ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of dose and route of administration on the kinetics of metronidazole and its major metabolites has been investigated in 8 healthy volunteers given 0.5 and 2.0 g i.v. and p.o. Metronidazole elimination kinetics from plasma could be described by an open two-compartment model. The systemic oral bioavailability of both doses was approximately 1. The total systemic clearance of the intravenous 2.0 g dose was 9% lower than that of the 0.5 g dose (p〈0.05). There were no significant dose-related differences in volume or rate of distribution. The elimination half-life was similar after the four treatments with metronidazole. The major elimination pathways, renal excretion and hepatic oxidation and glucuronidation, accounted for more than 2/3 of the total systemic clearance. Clearance both by hepatic oxidative metabolism and renal excretion was significantly lower after 2.0 than after 0.5 g i.v., whereas there was no significant difference after the oral doses. The results indicate that a high therapeutic dose of metronidazole may be eliminated at a reduced rate, but this is probably not of clinical importance. No single saturable elimination pathway was identified.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607962
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 177
    Electronic Resource
    Electronic Resource
    Rate-limiting diffusion processes following intrathecal administration of morphine (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 575-579 
    Details
    ISSN: 1432-1041
    Keywords: morphine ; pharmacokinetics ; intrathecal-intravenous administration ; flip-flop kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Morphine concentrations in plasma in five patients following intrathecal (i.t.) administration and in five other patients following intravenous (i.v.) administration were measured by a specific RIA sensitive to 0.1 ng/ml. Pharmacokinetic analysis showed a similar apparent total body clearance of morphine following both i.t. and i.v. administration, and complete bioavailability of i.t. morphine to the systemic circulation. This indicates that morphine is probably not metabolised in the CNS and that all of an i.t. dose diffuses from CSF to the plasma compartment. However a marked decrease in the i.t. terminal rate constants, involving a flip-flop phenomenon, contributed to the prolonged terminal half-life of i.t. morphine. The slow diffusion of morphine from the i.t. space to the plasma compartment can account for the prolonged analgesia following i.t. administration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542417
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 178
    Electronic Resource
    Electronic Resource
    Clonazepam pharmacokinetics and therapeutic efficacy in neonatal seizures (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 585-589 
    Details
    ISSN: 1432-1041
    Keywords: clonazepam ; neonates ; convulsions ; therapeutic effect ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Eighteen newborns (gestational age 28 to 42 weeks and post-natal age 0.5 to 44 days) suffering from convulsions not controlled by phenobarbital were treated with clonazepam 0.1 mg/kg (8 cases) or 0.2 mg/kg (10 cases) administered by slow intravenous infusion. The plasma half-lives in these ‘phenobarbital pretreated neonates’ were of the same order of magnitude as those reported in adults (20–43 h). Post-natal age did affect clearance, which was 50–70% less than in adults and older children. At the end of the infusion period, plasma clonazepam ranged from 28 to 117 ng/ml in the 0.1 mg/kg group and from 99 to 380 ng/ml in the 0.2 mg/kg group. In the former an immediate therapeutic response was observed in 7 out of 8 cases, and in the latter a significant and somehow delayed effect on convulsion was present only in 6 cases. The data suggest that optimal therapeutic response might already have been achieved with the 0.1 mg/kg dose. Higher doses and toxic concentrations of clonazepam may be detrimental to complete control of seizures and may expose the newborn to an unnecessary risk of adverse events.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542419
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 179
    Electronic Resource
    Electronic Resource
    Lack of effect of cimetidine on pharmacodynamics and kinetics of single oral doses of R- and S-acenocoumarol (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 619-623 
    Details
    ISSN: 1432-1041
    Keywords: acenocoumarol ; cimetidine interaction ; stereoselectivity ; healthy subjects ; pharmacokinetics ; anticoagulant effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics and dynamics of single doses (5 mg p.o.) of the optical isomers of acenocoumarol (R-AC and S-AC) were followed in healthy subjects and the effect on them of cimetidine 800 mg/day was also investigated. The AC enantiomers differed greatly in their pharmacokinetics. The mean residence time (MRT) of R-AC was about 10 times longer than that of S-AC, 15 h vs 1.2 h. There was no difference in the volume of distribution. Depression of blood clotting activity (Thrombotest) was observed only after administration of R-AC. The inactivity of S-AC as a vitamin K antagonist must be ascribed to its short MRT. Cimetidine did not affect the acute oral kinetics of R- and S-AC, nor did it affect the anticlotting activity of R-AC. The urinary excretion pattern of the 6- and 7-hydroxylated AC metabolites was not altered during cimetidine treatment. Although the present studies showed no effect of cimetidine on the pharmacokinetics and dynamics of acenocoumarol, the findings of Serlin et al. [3] suggest that cimetidine should not be administered during acenocoumarol therapy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542424
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 180
    Electronic Resource
    Electronic Resource
    Comparative pharmacokinetic study of adriamycin and 4'epi-adriamycin after their simultaneous intravenous administration (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 629-631 
    Details
    ISSN: 1432-1041
    Keywords: adriamycin ; epirubicin ; anthraquinone glycosides ; pharmacokinetics ; chemotherapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma pharmacokinetics of adriamycin and 4'epi-adriamycin have been studied in 6 patients with ovarian carcinoma after simultaneous intravenous administration of equal amounts of the two anthracyclines. A highly selective liquid chromatographic analytical method permitted quantification of plasma concentrations of the two drugs as well as their corresponding 13-hydroxy metabolites. The plasma concentrations of each drug followed a three-compartment open model, with great interindividual variation in the pharmacokinetic parameters. On average, the area under the plasma concentration time curve (AUC) and the maximum plasma concentration (Cmax) were 1.6- and 1.2-times larger for adriamycin than for 4'epi-adriamycin. 4'Epi-adriamycin was eliminated faster than adriamycin by 4 of the 6 patients, the average terminal half-life of the latter being 1.4-times longer. The plasma concentrations of the 13-hydroxy metabolites did not exceed 20 ng/ml. Their AUC values averaged 23% of those of the intact drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542426
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 181
    Electronic Resource
    Electronic Resource
    The effect of posture on the pharmacokinetics of intravenous benzylpenicillin (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 731-734 
    Details
    ISSN: 1432-1041
    Keywords: benzylpenicillin ; intravenous administration ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the pharmacokinetics of intravenously administered benzylpenicillin in normal subjects during bedrest and during ambulation. The values of total body clearance, mean residence time, and renal clearance found during ambulation were 487.4±100.5 ml/min, 36.23±13.45 min, and 309.4±93.4 ml/min (means ± SD). The corresponding values for bedrest were 543.6±122.6 ml/min, 35.27±10.21 min, and 324.1±145.3 ml/min. There were no significant differences between any of these pharmacokinetic variables with the change in posture. These results differ from previously reported results for the effects of posture on the pharmacokinetics of penicillins administered by extravascular routes, and suggest that the absorption of benzylpenicillin may be dependent on posture.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00608225
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 182
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of trimazosin and its effects on blood pressure, renal function and proteinuria during short-term therapy of patients with impaired renal function and hypertension (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 63-68 
    Details
    ISSN: 1432-1041
    Keywords: trimazosin ; proteinuria ; chronic renal insufficiency ; hypertension ; glomerular filtration rate ; renal vascular resistance ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics and short-term (10 weeks) effects of trimazosin, an alpha1-adrenoreceptor antagonist, on renal function and blood pressure in patients with moderate chronic renal insufficiency and hypertension, have been studied for the first time. Eight patients in whom the blood pressure was not normalized with a diuretic alone underwent pharmacokinetic studies and assessment of the renal function during a 10-week period of trimazosin therapy. Trimazosin significantly lowered blood pressure (recumbent and upright) without significantly altering renal function. Renal vascular resistance was decreased by 14%. Fractional sodium excretion, proteinuria and laboratory serum tests remained unchanged. Neither body weight nor pulse rate were affected. Moderate renal insufficiency did not modify the pharmacokinetics of the drug. Thus, trimazosin, as second-step antihypertensive agent, appeared to be safe and effective in patients with moderate renal insufficiency and hypertension, without exerting favourable or adverse renal effects during short-term therapy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870988
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 183
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of amikacin in cystic fibrosis: A study of bronchial diffusion (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 79-83 
    Details
    ISSN: 1432-1041
    Keywords: amikacin ; aminoglycoside ; cystic fibrosis ; pharmacokinetics ; bronchial diffusion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 36 pharmacokinetic studies of amikacin were performed to evaluate the bronchial diffusion of amikacin in 9 children with cystic fibrosis, 3 to 15 years old. Amikacin was administered i.v. according to a variable dosage regimen. Four children without cystic fibrosis were enrolled as controls. The mean half life was 1.1, the volume of distribution averaged 0.26 l/kg, and the mean plasma clearance was 131 ml/min/1.73 m2, which no differed from that of the controls. The mean peak plasma concentration was always above the MIC but its level depended on the unit dose: 18.5 mg/l, 25,95 mg/l and 31,46 mg/l for doses of 5, 7.5 and 12.5 mg/kg, respectively. Between consecutive amikacin infusions, the plasma level was above the MIC for 21% and 46% of the time after the 5 and 7.5 mg/kg doses. The maximum concentration in sputum between H1 and H2 was always below the MIC, except after 15 mg/kg. The ratio AUC sputum/AUC plasma was between 0.028 and 0.61, and it increased from the beginning to the end of the course of treatment. No side effects were observed on hearing, or vestibular and renal function. The results are used to suggest more appropriate dosing regimens.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870991
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 184
    Electronic Resource
    Electronic Resource
    The pharmacokinetics ofα-human atrial natriuretic polypeptide in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 101-103 
    Details
    ISSN: 1432-1041
    Keywords: atrial natriuretic polypeptide ; α-hANP ; pharmacokinetics ; radioimmunassay
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have analysed the pharmacokinetics ofα-human atrial natriuretic polypeptide (α-hANP) in healthy subjects, using a two-compartment open model following bolus intravenous injection. The plasma half-times for the fast and slow components were 1.7±0.07 min and 13.3±1.69 min respectively. V1 (the volume of the central compartment), Vz (volume of distribution) and Vss (volume of distribution at steady-state) were 5370±855 ml (89.5±14.3 ml·kg−1), 32000±4620 ml (533±77.0 ml·kg−1), and 11900±1530 ml (198±25.5 ml·kg−1) respectively. The mean plasma clearance was 1520±121 ml·min−1 (25.4±2.0 ml·min−1·kg−1.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870995
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 185
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of single and multiple doses of flusoxolol (Ro 31-1411) in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 113-115 
    Details
    ISSN: 1432-1041
    Keywords: flusoxolol ; multiple-dose ; pharmacokinetics ; Ro 31-1118 ; optical isomer
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Flusoxolol (Ro 31-1411) is the pharmacologically active optical isomer of Ro 31-1118, a potent cardioselective β-adrenoceptor antagonist with partial agonist activity. It was given to 6 healthy volunteers in a single dose, 40 mg, and then in multiple doses, 40 mg daily for 8 days. Plasma concentration data were best described by a linear two-compartment pharmacokinetic model with first order absorption, and the results confirmed linear kinetics. Pharmacokinetic data for flusoxolol were comparable to those for the racemate Ro 31-1118.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870998
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 186
    Electronic Resource
    Electronic Resource
    Biliary excretion of ceftriaxone (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 123-124 
    Details
    ISSN: 1432-1041
    Keywords: ceftriaxone ; biliary excretion ; cholecystectomy ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00871001
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 187
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of oral cyclosporin a (Sandimmun) in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 211-216 
    Details
    ISSN: 1432-1041
    Keywords: cyclosporin A ; absorption ; pharmacokinetics ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Extensive pharmacokinetic (PK) profiles after oral dosing of 300 mg cyclosporin A (CsA) were determined in whole blood by radioimmunoassay (RIA) in 14 healthy male volunteers, using two-compartment models with either first order (M1) or zero order (M0) absorption. According to zero order absorption the mean of the following PK parameters was determined: terminal half-life=12.1±5.0 h, apparent volume of distribution at steady-state=5.6 ±2.1 l · kg−1, apparent clearance=0.51±0.11 l · h−1 · kg−1. The time lag between drug ingestion and first blood level was short, 0.38±0.11 h. Drug absorption lasted for 2.8±1.6 h. The end of absorption was indicated in each individual by a sharp drop in blood levels. The observations support the assumption that CsA is absorbed in the upper part of the small intestine with a clear-cut termination (absorption window). This assumption may explain the high degree of variability in the bioavailability of CsA.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606661
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 188
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of betaxolol in middle aged patients (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 231-233 
    Details
    ISSN: 1432-1041
    Keywords: betaxolol ; pharmacokinetics ; middle aged subjects ; oral and i.v. administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of betaxolol was studied in 8 middle-aged (40–60 years) subjects after oral (20 mg) and intravenous (10 mg) administration. The principal parameters were almost identical to those observed in young healthy volunteers. The recommended therapeutic regimen, a single daily dose of 20 mg, appears well suited for middle aged, hypertensive patients.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606665
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 189
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of piroximone (MDL 19.205) in healthy volunteers (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 239-242 
    Details
    ISSN: 1432-1041
    Keywords: piroximone ; cardiotonic drug ; pharmacokinetics ; bioavailability ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six healthy, male subjects received single intravenous and oral doses of piroximone. Plasma piroximone concentrations were assayed up to 8 h after each dose by HPLC. Urinary excretion of the parent compound was also determined. Following the oral dose, piroximone reached peak plasma concentrations within 30 to 90 min. The t1/2 of the terminal decay phase was 2.8 h, the mean apparent volume of distribution was 2.5 l/kg, and the mean total body clearance was 755 ml/min. Mean urinary recovery of parent drug within 24 h was 50% after the intravenous dose and 41% after the oral dose. Renal clearance accounted for approximately 50% of total body clearance. Oral bioavailability, estimated from AUC or urinary recovery, was 80%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606667
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 190
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of tiapride in patients with tardive dyskinesia and Huntington's disease (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 191-194 
    Details
    ISSN: 1432-1041
    Keywords: tiapride ; Huntington's disease ; pharmacokinetics ; tardive dyskinesia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of tiapride were determined at steady-state in 5 patients with tardive dyskinesia and 2 patients with Huntington's disease given tiapride 100 mg t.i.d. for 7 days. The maximum serum concentration of tiapride of 1.47±0.35 µg/ml was reached after 1.4±0.67 h. The half-life time of elimination was 229±41 min. About 50% of the dose of tiapride was excreted unchanged by the kidney. Neither protein binding nor glucuronide, sulphate or acetyl conjugation was observed. Renal clearance in the patients appeared to be lower but the other pharmacokinetic parameters did not differ from previous findings in healthy young volunteers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606657
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 191
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of primaquine in patients withP. Vivax malaria (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 205-210 
    Details
    ISSN: 1432-1041
    Keywords: primaquine ; malaria ; acute and chronic dosing ; carboxylic acid metabolite ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of primaquine (PQ) and its major carboxylic acid metabolite (PQC) have been studied in seven Indian patients withP. vivax malaria following PQ 15 mg/day p.o. for 14 days. After a single oral dose on Day 1, a mean peak blood concentration of 50.7 ng/ml PQ was attained after 2.3 h, which declined monoexponentially with a half-life of 5.6 h. The mean total body clearance was 37.6 l/h and the volume of distribution was 2921. The mean renal excretion (0–24 h) of the drug was only 0.54% of the dose and renal clearance was 0.189 l/h. Following chronic administration, none of the pharmacokinetic parameters was affected, and a steady state blood concentration of 2.5–4.2 ng/ml PQ was attained. After the first dose of PQ, PQC had a mean area under the blood concentration — time curve 11-fold higher than that of the parent drug. In contrast to the rapid distribution and elimination of PQ, the metabolite showed a longer mean residence time and accumulation in the body. The mean Cmax and AUC of the metabolite on Day 14 were 48 and 40% higher than the corresponding Day 1 values. The metabolite could not be detected in urine at any time in any patient. PQ and its metabolite did not show any accumulation in blood cells.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606660
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 192
    Electronic Resource
    Electronic Resource
    Interaction of oxaprozin with acetaminophen, cimetidine, and ranitidine (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 371-374 
    Details
    ISSN: 1432-1041
    Keywords: oxaprozin ; drug interaction ; acetaminophen ; cimetidine ; ranitidine ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twelve healthy male volunteers participated in a single-dose four-way crossover study to evaluate potential drug interactions with oxaprozin, a nonsteroidal antiinflammatory agent of the propionic class. The four modes of administration were:a. oxaprozin, 1200 mg alone;b. oxaprozin during concurrent acetaminophen, 500 mg 4 times daily;c. oxaprozin with cimetidine, 300 mg 4 times daily;d. oxaprozin with ranitidine, 150 mg every 12 hours. Acetaminophen, cimetidine, or ranitidine were begun 24 hours prior to oxaprozin dosage and continued for the 10-day duration of each trial. No significant differences existed among the four treatment conditions in peak plasma oxaprozin concentration (86 µg/ml), volume of distribution (0.23 l/kg), time of peak concentration (3.7 h after dosage), or elimination half-life (54 h). Oxaprozin oral clearance was significantly lower (by 20%) during both the cimetidine and ranitidine trials versus control (0.047 vs 0.047 vs 0.059 ml/min/kg), but clearance during acetaminophen was not significantly different from control. Thus acetaminophen, cimetidine or ranitidine has only a small influence on the pharmacokinetics of a single oral dose of oxaprozin. The reduction in oxaprozin clearance due to cimetidine or ranitidine is statistically significant but small in magnitude.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981141
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 193
    Electronic Resource
    Electronic Resource
    Pharmacokinetic approach to equilibrium between ketanserin and ketanserin-ol (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 339-342 
    Details
    ISSN: 1432-1041
    Keywords: ketanserin ; ketanserin-ol ; pharmacokinetics ; reduction-oxidation equilibrium ; healthy volunteers ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The metabolic reduction-oxidation equilibrium between ketanserin and ketanserin-ol was studied after oral dosing of both substances to two healthy volunteers. Comparison of plasma Cmax and AUCs indicated that the equilibrium was shifted towards ketanserin-ol. There is evidence that ketanserin-ol elimination is the slowest step dictating the terminal half-life of ketanserin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981134
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 194
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of a long-acting bromocriptine preparation (Parlodel LA) and its effect on release of prolactin and growth hormone (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 615-618 
    Details
    ISSN: 1432-1041
    Keywords: bromocriptine ; long-acting formulation ; pharmacokinetics ; prolactin inhibition ; growth hormone secretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and endocrine actions of a long-acting form of bromocriptine (Parlodel) were examined in a controlled study in 10 healthy volunteers receiving a single i.m. injection of 50 mg. Six further subjects took bromocriptine 1.25 mg t.i.d. for 3 days p.o. In the subjects given the slow release preparation, the plasma bromocriptine concentrations increased sharply to a maximum of 1.65 mg/l 2 h after injection. This fast release process was followed by slow clearance with a half-life of 16 days. The substance was still detectable in plasma 35 days postinjection. Plasma prolactin (PRL) fell rapidly from a mean of 5.6 ng/ml to reach significantly lower levels at 60 and 120 min. Inhibition was maintained for up to 35 days, when plasma PRL was still significantly below the values recorded at baseline and in the control group. Plasma GH peaked at 3.6 ng/ml at 120 min and subsequently declined slowly to stabilize between 1.4 and 2.2 ng/ml for about 12 h, falling to below the 1 ng/ml limit for the remainder of the study period. In contrast, individuals receiving oral bromocriptine exhibited a significant elevation following the first dose and an equivalent increment after the morning dose on Day 3. Thus, the results show a prolonged inhibitory effect on PRL of this long-acting bromocriptine preparation in parallel with its slow plasma clearance. The stimulant effect on GH secretion is short lived, presumably due to desensitisation of specific receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635902
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 195
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of terbutaline during pregnancy (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 619-623 
    Details
    ISSN: 1432-1041
    Keywords: terbutaline ; pregnancy ; pharmacokinetics ; preterm labour ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Terbutaline in plasma was determined in three groups of women by gas chromatography-mass spectrometry. Eight women received a single i.v. dose of 0.25 mg terbutaline sulphate during pregnancy and 3–6 months after delivery. Mean plasma clearance was 29% higher during pregnancy than after delivery. There was a subsequent decrease in mean terminal half-life from 5.3 to 3.7 h and in mean residence time from 5.3 to 3.4 h. There was no change in volume of distribution. A second group of pregnant women in premature labour (n=8) received oral terbutaline 5 mg t.d.s. The dosing was repeated after delivery. The mean steady state plasma concentration of terbutaline was about 30% lower during pregnancy than after delivery. A third group of women in preterm labour (n=8) was treated with an i.v. infusion of terbutaline. The concentrations of terbutaline found on cessation of uterine contractions ranged between 12.8 and 31.5 ng/ml. At present there is no basis for formulation of a “therapeutic plasma level” of terbutaline for the treatment of preterm labour.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635903
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 196
    Electronic Resource
    Electronic Resource
    Single dose prophylaxis with metronidazole in infants during abdominal surgery: A pharmacokinetic study (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 625-628 
    Details
    ISSN: 1432-1041
    Keywords: metronidazole ; prophylaxis ; single dose ; pharmacokinetics ; abdominal surgery ; infants
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma metronidazole was measured following a single interavenous dose of 20 mg/kg (Flagyl 5 mg/ml) in 12 infants less than 1 year of age undergoing abdominal surgery. In all patients sufficient plasma concentrations, well above the MIC values for anaerobic bacteria, were found for at least 16 h. A prolonged half-life was demonstrated in the group less than 8 weeks of age (t1/2/18.4 h). The group over 8 weeks of age demonstrated a t1/2 comparable to that seen in adults (t1/2 7 h).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635904
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 197
    Electronic Resource
    Electronic Resource
    Antiemetic effect and pharmacokinetics of high dose metoclopramide in cancer patients treated with cisplatin-containing chemotherapy regimens (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 33-40 
    Details
    ISSN: 1432-1041
    Keywords: metoclopramide ; high dose ; antiemetic efficacy ; cancer patients ; pharmacokinetics ; cisplatin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Fifteen cancer patients receiving cisplatin-containing chemotherapy participated in two antiemetic studies. In Study 1 they received standard antiemetics in low doses on demand, and in Study 2 the same patients participated in an open randomized cross-over study between metoclopramide 1 and 2 mg/kg i.v.×5. Serum metoclopramide was determined by HPLC. Self-reporting of nausea using a visual analogue scale (VAS) was compared with observer rated scores. Tolerability and volume vomited were assessed by nurse observers. The biological half-life of metoclopramide was 9.9 h, the volume of distribution was 9.9 l/kg and the clearance was 0.68 l/h/kg. The pharmacokinetics of high dose metoclopramide was linear in the range 0.15–2 mg/kg×5, with very little accumulation. Compared to standard antiemetics, both high dose regimens of metoclopramide had a significant effect on nausea, but no effect on the volume vomited. Self reports of nausea were significantly correlated with observer rated values. Tolerance of high dose metoclopramide was good except in 3 patients who left the study because of restlessness and trismus. It is concluded that high dose metoclopramide probably can be administered for several consecutive days without appreciable accumulation of the drug. Self-reporting of nausea by patients on VAS is a simple and feasible method of evaluation. The finding that metoclopramide affects nausea but not vomiting supports the hypothesis that nausea and vomiting should be evaluated separately in assessing antiemetic efficacy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870982
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 198
    Electronic Resource
    Electronic Resource
    Initial and long-term outpatient experience with pirmenol for control of ventricular arrhythmias (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 15-22 
    Details
    ISSN: 1432-1041
    Keywords: pirmenol ; ventricular arrhythmias ; antiarrhythmic drug ; initial- and long-term experience ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Pirmenol, a new class IA antiarrhythmic agent, has shown promise in short-term trials, but long-term efficacy has not been documented. We thus evaluated 11 patients with frequent (≥60/h) premature ventricular complexes (PVC) given oral pirmenol for 25–727 days. Ten of 11 patients entering the long-term open trial had shown ≥70% (mean 83%) PVC suppression during in-hospital pirmenol dose ranging. Long-term pirmenol was given in divided doses of 100–600 mg/day. Mean PVC frequency during baseline was 13,078/24h (range, 3,218–32,718); couplets averaged 481/24h (1–2,829) and runs 45/24h (0–334). Ambulatory monitoring was performed at 1, 3, 6, and 12 months, then semiannually. Mean absolute PVC suppression at 1 month averaged 75% (p≤0.02). Median individual percentage PVC suppression was 94%. During the first 3 months, 8 patients (73%) continued to show a favorable response (≥70% suppression), and 3 had arrhythmia recurrence and were dropped. One responder was withdrawn after the onset of paroxysmal atrial fibrillation, and another early responder was withdrawn after 3 months because of arrhythmia relapse. Six patients have been treated for over 1 year, with 99% mean PVC suppression. Mean couplet and run frequencies at 1 month decreased by means of 76% (p≤0.05) and 92% (p=0.001) respectively. At 1 year, couplets were suppressed 99.8% and runs by 99.7% in the 6 patients remaining on pirmenol. Mean QT interval increased slightly (7.1%,p〈0.05); mean PR and QRS intervals were unchanged. Plasma pirmenol concentrations averaged 1.49 µg/ml at clinic evaluations, 1.72 µg/ml in responders vs 1.08 µg/ml in nonresponders. Inade-quate plasma drug concentrations may be one cause for arrhythmia recurrence. Adverse effects were minimal. Thus, oral pirmenol is a safe and effective agent for long-term outpatient management of complex ventricular arrhythmias in selected patients.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870979
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 199
    Electronic Resource
    Electronic Resource
    Kinetics of allopurinol and oxipurinol after chronic oral administration. Interaction with benzbromarone (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 53-58 
    Details
    ISSN: 1432-1041
    Keywords: allopurinol ; benzbromarone ; oxipurinol ; pharmacokinetics ; repeated dose ; drug interaction ; urate excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Previous studies have described a pharmacokinetic interaction between probenecid, a uricosuric drug, and oxipurinol, the major metabolite of allopurinol. In single dose studies, no interaction was found to occur between benzbromarone, another uricosuric agent, and oxipurinol. A cross over study was conducted in 12 volunteers to compare the kinetics of allopurinol and oxipurinol following treatment for 7 days with allopurinol alone or combined with benzbromarone 20 or 100 mg. The pharmacokinetic parameters of allopurinol were not modified by the uricosuric therapy, but those of oxipurinol were markedly altered by concurrent administration even of the lower dose of benzbromarone; the average plasma level fell by 30% and the renal elimination rate was increased by 50%. A parallel increase in the renal elimination rate of uric acid was observed (significant only with the higher dose of benzbromarone) and a positive linear correlation between the fractional excretion of uric acid and that of oxipurinol was established.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870986
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 200
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of N-acetylcysteine in man (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 217-222 
    Details
    ISSN: 1432-1041
    Keywords: N-acetylcysteine ; bioavailability ; slow-release formulation ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary N-Acetylcysteine was given intravenously and as three fast dissolving and one slow-release formulation, on separate occasions, as a single dose of 600 mg to 10 fasting (5 men and 5 women) healthy volunteers. Blood and urine were sampled for the following 12 h. Renal clearance constituted around 30% of total body clearance, which was 0.21 l/h/kg. Volume of distribution was 0.33 l/kg, consistent with distribution mainly to extracellular water. The late elimination half-life was 2.27 h and the mean residence time 1.62 h. The slow-release tablet resulted in a flattened plasma concentration-time curve typical of slow release formulations, while the other three oral formulations were rapidly absorbed. The oral availability of N-acetylcysteine varied between 6 and 10%, with the slow-release tablet having the lowest and the fast dissolving tablet the highest availability.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606662
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...