Pharmacokinetics of oral indoramin

Abstract

A randomized crossover study was carried out in 7 healthy subjects to investigate the pharmacokinetics of indoramin from two oral formulations (film-coated and uncoated 50 mg tablets) and to determine the effect of a standard mean on the plasma concentration time curve of the film-coated form. The results indicated that peak plasma concentrations occurred in 1 to 4 hours after treatment with a single dose of 2 tablets, with an overall elimination half-life of 5 hours. No significant differences could be shown between treatments in any of the pharmacokinetic variables determined. However, administration of film-coated indoramin after a standard meal narrowed the range of peak concentrations but the time at which peak concentrations of the drug occurred did not appear to be related to whether or not indoramin was given after the meal.

Pharmacokinetic Interaction Between Indoramin and Ethanol

“…Both indoramin and ethanol caused sedation. 4 The increased bioavailability of oral indoramin in the presence of ethanol may reflect some enhanced absorption, but it is also consistent with inhibition of first-pass metabolism of a flowlimited drug. The clinical implications are discussed.…”

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

“…kg -1 and a disposition half-time of approximately 4 h (Draffan et al 1976;Norbury et al 1983). After oral administration indoramin is subject to extensive first-pass metabolism (Draffan et al 1976), leading to somewhat low and variable plasma concentrations (Volans et al 1982;Norbury et al 1984). Its mean systemic availability (+ SD) in 5 middleaged female volunteers has been previously estimated at 8.3 + 2.9% (Norbury et al 1984).…”