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  • 1
    Electronic Resource
    Electronic Resource
    Plasma and urinary excretion kinetics of oral baclofen in healthy subjects (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 181-184 
    Details
    ISSN: 1432-1041
    Keywords: baclofen ; renal function ; healthy subjects ; pharmacokinetics ; probenecid ; tubular secretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Baclofen, a centrally acting muscle relaxant, is used in the treatment of spasticity. Its pharmacokinetics has been derived from plasma and urine data in four healthy subjects, whose renal function was simultaneously measured. After oral administration of a single 40 mg dose, baclofen was mainly excreted unchanged by the kidney, 69 (14) %. The half-life, calculated from extended least squares modelling (ELSMOS) both of plasma and urine data was 6.80 (0.68) h, which is longer than reported in most studies based solely on plasma data. The renal excretion rate constant had the high mean value of 0.35 (0.24) h−1, and the apparent renal clearance of baclofen equalled the creatinine clearance. Passive tubular reabsorption is relatively unimportant, since no dependence was observed on variables urine flow or pH. Although active tubular secretion may contribute to its renal clearance, as shown by the effect of coadministration of probenecid, glomerular filtration appears to be the dominant transport mechanism.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558228
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  • 2
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and mechanism of renal excretion of short acting sulphonamides and N4-acetylsulphonamide derivatives in man (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 283-292 
    Details
    ISSN: 1432-1041
    Keywords: sulphonamides ; N4-acetylsulphonamide derivatives ; pharmacokinetics ; renal excretion ; tubular secretion ; structure-excretion relationship ; deacetylation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of short acting sulphonamides and a series of N4-acetylsulphonamide derivatives has been investigated. Sulphonamides with a sulphur atom two atomic bond distances from the N1 atom are excreted by active tubular secretion, e.g. sulphamethizole, sulphaethidole and sulphathiazole. When the sulphur atom is replaced by an oxygen or nitrogen atom, active renal excretion no longer occurs. N4-acetylsulphonamides are excreted by active tubular secretion. The renal clearance values of the N4-acetylsulphonamides are not influenced by the substituent at the N1 position. Two groups of N4-acetylsulphonamides can be distinguished. One has a T1/2 of 4–6 h and a renal clearance value of 20–60 ml/min and the second has a T1/2 of 10–20 h and a renal clearance of less than 10 ml/min. N4-acetylsulphonamides are deacetylated to the extent of about 5%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00618779
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  • 3
    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
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  • 4
    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
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of intramuscular nicomorphine and its metabolites in man (1991)
    Springer
    European journal of clinical pharmacology 41 (1991), S. 375-378 
    Details
    ISSN: 1432-1041
    Keywords: Nicomorphine ; 6-nicotinoylmorphine ; morphine ; intramuscular administration ; metabolism ; absorption ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After i.m. injection nicomorphine is relatively slowly absorbed from the muscular depot and is found in the serum for approximately 1 h. The rate of absorption differs between patients and governs the overall pharmacokinetic profile of the compound. The relative AUCs were nicomorphine 18%, 6-nicotinoylmorphine 17%, and morphine 65%. Nicomorphine and 6-nicotinoylmorphine have significantly higher AUCs after i.m. injection than after i.v. injection, while the AUC of morphine and the total AUC show no difference between the two modes of administration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00314971
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  • 6
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of antibiotics in critically ill patients (1990)
    Springer
    Intensive care medicine 16 (1990), S. S235 
    Details
    ISSN: 1432-1238
    Keywords: Pharmacokinetics ; Antibiotics ; Aminoglycosides ; Protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Differences in pharmacokinetic data of aminoglycosides, ceftazidime and ceftriaxone between intensive care patients and volunteers or patients who are less severely ill, are described. Similar differences are observed for midazolam. In severely ill patients with normal renal function a wide interpatient variability of aminoglycoside half-life (t1/2) and increased distribution volume (Vd) are observed. This results in inadequate serum levels. A pharmacokinetic approach of drug dosing, based on serum concentrations in individual patients, is advised. For ceftazidime and ceftriaxone similar changes of t1/2 and Vd are observed. Since protein binding is frequently reduced in severely ill patients, the influence of altered binding of highly bound drugs on Vd and drug clearance is discussed. As both may be increased by reduced protein binding, the change of t1/2 to be expected is unpredictable. Dosing regimens should be based on pharmacokinetic data derived from patients whose severity of disease is comparable to that of the patients to be treated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01709707
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  • 7
    Electronic Resource
    Electronic Resource
    Cannabivarichromene, a new cannabinoid with a propyl side chain in cannabis (1973)
    Springer
    Cellular and molecular life sciences 29 (1973), S. 260-261 
    Details
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Zusammenfassung Es wurde ein neuer Vertreter aus der Gruppe der psychotrop wirkenden Inhaltsstoffe im Haschisch indischer Herkunft gefunden. Es handelt sich um Cannabivarichromen, als Homologa mit einer Propyl-Seitenkette des Cannabichromens.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01926461
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  • 8
    Electronic Resource
    Electronic Resource
    Kinetics of l-tryptophan in depressive patients: A possible correlation between the plasma concentrations of l-tryptophan and some psychiatric rating scales (1981)
    Springer
    Psychopharmacology 75 (1981), S. 350-353 
    Details
    ISSN: 1432-2072
    Keywords: l-tryptophan kinetics ; Depression ; Plasma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The plasma concentration and flux of l-tryptophan are abnormal in primary depressive patients, according to the literature. The plasma concentrations of l-tryptophan over a 6-h period after ingestion of 5 g l-tryptophan were investigated and did not differ significantly between depressive patients and controls during the absorption, distribution, and elimination phases. There was no correlation between the plasma concentrations with anxiety or depression scores, or with the excretion in urine of 17-hydroxycorticosteroids and xanthurenic acid during the 24 h after l-tryptophan. Treatment with either 125 mg pyridoxine (three times daily with meals) and l-tryptophan (3 g at 10 PM) or with maprotiline (100 mg at 10 PM) had no influence on the plasma concentrations of l-tryptophan after 2 or 4 weeks of treatment. This excludes l-tryptophan deficiency as a pathogenic factor of depression in the patients studied. No kinetic differences could be demonstrated in the depressive patients, making differences in body compartments or flux of l-tryptophan unlikely to be of pathogenic importance to depression.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00435851
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  • 9
    Electronic Resource
    Electronic Resource
    Treatment of a patient with impaired renal function with gentamicin-PMMA-beads (1981)
    Springer
    Archives of orthopaedic and trauma surgery 99 (1981), S. 137-141 
    Details
    ISSN: 1434-3916
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung 150 Gentamycin-PMMA-Kugeln wurden implantiert (+ 160 mg Gentamicin i.v. preop.) in eine 73jährige Frau, die an einer starken Einschränkung der Nierenfunktionen litt. Relativ häufig wurden die Plasma-Konzentrationen vom Gentamycin und die renalen Funktionen bestimmt. Die Konzentration von Gentamycin im Plasma erreichte einen Plateauwert von 3 μg/ml. Es trat keine Akkumulation von Gentamycin im Plasma auf.
    Notes: Summary 150 Gentamicin-PMMA-beads were implanted (+ 160 mg gentamicin i.v. preop.) in a woman aged 73 years and with severely impaired kidney function. Frequent determination of gentamicin plasma concentrations and renal functions were possible. The plasma concentration reached a plateau at approx. 3 μg/ml. No accumulation of gentamicin in plasma occurred.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00389749
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  • 10
    Electronic Resource
    Electronic Resource
    Interindividual variation in the capacity-limited renal glucuronidation of probenecid by humans (1993)
    Springer
    Pharmacy world & science 15 (1993), S. 197-202 
    Details
    ISSN: 1573-739X
    Keywords: Clearance, renal ; Glucuronates ; Metabolism ; Pharmacokinetics ; Probenecid ; Protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A dose of 1,000 mg probenecid was administered orally to 14 human volunteers in order to quantify the maximal rate of formation and excretion of probenecid acyl glucuronide in the urine. Probenecid showed dose-dependent pharmacokinetics. Plasma protein binding of probenecid was high, being somewhat higher in males (90.7±1.4%) than in females (87.9±1.4%; p=0.0019). It was shown that probenecid is metabolized by cytochrome P-450 into at least two phase I metabolites. Each of the metabolites accounted for less than 12% of the dose administered; the main metabolite probenecid acyl glucuronide, representing 42.9±13.2% of the dose, was only present in urine and not in plasma. The renal excretion rate-time profile of probenecid acyl glucuronide showed a plateau value in the presence of an acidic urine pH. This plateau value was maintained for about 10 h at the dose of 1,000 mg. The height of the plateau value depended on the individual and varied between 250 and 800μg/min (15–50 mg/h). It was inferred that probenecid acyl glucuronide is formed in the kidney during blood-to-lumen passage through the tubular cells. We conclude that the plateau value in the renal excretion rate of probenecid glucuronide reflects itsV max of formation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01880626
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