PMID: 3653231Jan 1, 1987Paper

Pharmacokinetics and systemic availability of the antihypertensive agent indoramin and its metabolite 6-hydroxyindoramin in healthy subjects

European Journal of Clinical Pharmacology
D M PierceR A Franklin

Abstract

We have studied the pharmacokinetics and absolute systemic availability of indoramin (50 mg) given orally in solution or as a tablet with reference to intravenously administered drug (0.15 mg/kg) in 9 healthy volunteers. After intravenous administration the median apparent volume of distribution was 6.3 l X kg-1, plasma clearance was 20.0 ml X min-1 X kg-1, and terminal half-time was 4.1 h. When given by tablet indoramin was absorbed with moderate rapidity, with a median tmax of 1.5 h. The median systemic availability was 24%. After oral administration in solution the drug was more rapidly absorbed, with a median tmax of 1.0 h (p less than 0.01). The median systemic availability was 43% (15-85%). Plasma concentrations of an active metabolite, 6-hydroxyindoramin, after single oral doses in either dosage form, were of a similar order to those of unchanged drug and fell with similar rapidity. After intravenous administration, however, concentrations of the metabolite were negligible.

References

Jan 1, 1976·Clinical Pharmacokinetics·G Johnsson, C G Regàrdh
Sep 1, 1979·European Journal of Clinical Pharmacology·D N BatemanM D Rawlins
Jun 1, 1976·British Journal of Clinical Pharmacology·G H DraffanC T Dollery
Oct 1, 1975·Clinical Pharmacology and Therapeutics·G R Wilkinson, D G Shand
Jan 1, 1984·European Journal of Clinical Pharmacology·H M NorburyS J Warrington
Jan 1, 1983·European Journal of Clinical Pharmacology·H M NorburyS J Warrington
Jan 1, 1983·European Journal of Clinical Pharmacology·R A FranklinD Stevenson
Apr 1, 1982·Clinical Pharmacology and Therapeutics·R G McAllister, E B Kirsten
Jan 1, 1982·Current Medical Research and Opinion·G N VolansT Frost

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Citations

Jan 1, 1988·European Journal of Clinical Pharmacology·D M PierceR A Franklin
Dec 1, 1990·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·D M Pierce
Mar 1, 1988·Biopharmaceutics & Drug Disposition·D M PierceR A Franklin
Jan 1, 1987·European Journal of Clinical Pharmacology·D M PierceR A Franklin

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