Biopharmaceutics and metabolism of yohimbine in humans

The biopharmaceutics of yohimbine (YO) and the pharmacokinetics of 10-hydroxy-yohimbine (10-OH-YO) and 11-hydroxy-yohimbine (11-OH-YO) were investigated in healthy subjects following i.v. (5 mg) and oral (8 mg) dosing. One subject was found as a slow hydroxylator of YO. The mean (±S.D.) oral absolut...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 1999-10, Vol.9 (1), p.79-84
Main Authors: Le Corre, Pascal, Dollo, Gilles, Chevanne, François, Le Verge, Roger
Format: Article
Language:English
Subjects:
10-Hydroxy-yohimbine
11-Hydroxy-yohimbine
Administration, Oral
Adrenergic alpha-Antagonists - blood
Adrenergic alpha-Antagonists - metabolism
Adrenergic alpha-Antagonists - pharmacokinetics
Adult
Area Under Curve
Biological and medical sciences
Catecholaminergic system
Healthy subjects
Humans
Injections, Intravenous
Male
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Oral bioavailability
Pharmacokinetics
Pharmacology. Drug treatments
Yohimbine
Yohimbine - analogs & derivatives
Yohimbine - blood
Yohimbine - metabolism
Yohimbine - pharmacokinetics
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Summary:The biopharmaceutics of yohimbine (YO) and the pharmacokinetics of 10-hydroxy-yohimbine (10-OH-YO) and 11-hydroxy-yohimbine (11-OH-YO) were investigated in healthy subjects following i.v. (5 mg) and oral (8 mg) dosing. One subject was found as a slow hydroxylator of YO. The mean (±S.D.) oral absolute bioavailability of YO was 22.3±21.5%. Total plasma clearance ( CL) and renal clearance ( CL r) of YO following i.v. dosing were 0.728±0.256 ml/min and 0.001±0.002 ml/min, respectively. Based on the steady-state volume of distribution ( V ss), YO had a relatively low distribution ( V ss=32.2±12.1 l). The overall renal excretion of YO, 10-OH-YO and 11-OH-YO, expressed as percent of the dose of YO administered, were not different following i.v. and oral dosing, and were around 0.1, 0.2 and 14%, respectively. Following i.v. dosing of YO, the mean apparent terminal half-life of 11-OH-YO (347±63 min) was almost four times higher than that of YO (91.0±33.6 min) suggesting an elimination rate-limited kinetics for 11-OH-YO.
ISSN:0928-0987
1879-0720
DOI:10.1016/S0928-0987(99)00046-9