Pharmacokinetics and systemic availability of the antihypertensive agent indoramin and its metabolite 6-hydroxyindoramin in healthy subjects.
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.
D000042:Absorption; D000293:Adolescent; D000328:Adult; D001682:Biological Availability; D005260:Female; D006801:Humans; D007211:Indoles / Q000493:pharmacokinetics*; D007217:Indoramin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D008297:Male
D007211:Indoles; D007217:Indoramin; C049268:6-hydroxyindoramin