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  • 1975-1979  (2)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 9 (1976), S. 345-354 
    ISSN: 1432-1041
    Keywords: 3H-digitoxin ; metabolism ; spironolactone ; enzyme induction ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of spironolactone on the metabolism of intravenously administered3H-digitoxin (80 µCi) was investigated in eight patients. In three of them the labelled glycoside was given on a second occasion after spironolactone treatment had been discontinued for at least 65 days. Of total urinary radioactivity 79 % was unaltered drug and 12 % consisted of water soluble compounds. No digitoxigenin or digoxigenin and only trace amounts (〈2 %) of digoxin and the bis- and monoglycosides of digoxigenin were found. After spironolactone total urinary radioactivity was unchanged but the fraction eliminated as unchanged digitoxin fell from 79 to 66 % and the water soluble compounds increased from 12 to 26 % (p〈0.05). In addition spironolactone caused a 20 % reduction in the half-life of serum radioactivity (p〈0.01) and a 16 % reduction in the volume of distribution (p〈0.05). Induction of hepatic enzymes by spironolactone is proposed to explain the alteration in the metabolism of digitoxin in man. Both the altered metabolic pattern and the reduction in the volume of distribution appear to contribute to the reduction in half-life.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Summary Azlocillin, a new semisynthetic penicillin with a wide spectrum of antimicrobial activity and a member of the ureidopenicillin group, was administered to ten adults in a dosage of 2 g by intravenous bolus injection. The determination of antibiotic activity in serum and urine demonstrated an average concentration of 58.9µg/ml after one hour, 28.1µg/ml after two hours, and 6.1µg/ml after four hours. The total urinary excretion was 60% within six hours. The pharmacokinetic parameters were calculated for the one and two compartment models, respectively. Mathematical analysis according to an open two-compartment model resulted in better curve adjustment as judged from the sum of the deviant squares. The resulting parameters for volume of distribution and rate of elimination show only minor differences however. Similar results were seen on comparison with the respective data for ampicillin.
    Notes: Zusammenfassung Azlocillin, ein neues halbsynthetisches Penicillin mit breitem Wirkungsspektrum aus der Gruppe der Ureidobenzyl-Penicilline, wurde in einer Dosis von 2 g 10 Er-wachsenen mit normaler Nierenfunktion intravenös verabreicht. Die Bestimmung der Serum- und Urinkonzentrationen ergab nach 1 Stunde eine mittlere Serumkonzentration von 58,9 mcg/ml, nach 2 Stunden 28,1 mcg/ml und nach 4 Stunden 6,1 mcg/ml, die Gesamtausscheidung über die Niere betrug innerhalb von 6 Stunden 60%. Darüber hinaus wurden Halbwertzeit, Verteilungsvolumen, Fläche unter der Serumkonzentrationskurve sowie renale und totale Clearance ermittelt. Die mathematische Analyse ergibt eine bessere Anpassung der experimentell ermittelten Werte an ein 2-Kompartment-Modell, die Berechnung der entsprechenden Parameter nach dem 1-Kompartment-Modell zeigt jedoch nur geringfügige, kaum ins Gewicht fallende Unterschiede. Ein Vergleich mit den entsprechenden Daten für Ampicillin und Carbenicillin läßt eine ähnliche Kinetik erkennen.
    Type of Medium: Electronic Resource
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