Biopharmaceutics and metabolism of yohimbine in humans

Eur J Pharm Sci. 1999 Oct;9(1):79-84. doi: 10.1016/s0928-0987(99)00046-9.


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.

Publication types

  • Clinical Trial

MeSH terms

  • Administration, Oral
  • Adrenergic alpha-Antagonists / blood
  • Adrenergic alpha-Antagonists / metabolism
  • Adrenergic alpha-Antagonists / pharmacokinetics*
  • Adult
  • Area Under Curve
  • Humans
  • Injections, Intravenous
  • Male
  • Yohimbine / analogs & derivatives
  • Yohimbine / blood
  • Yohimbine / metabolism
  • Yohimbine / pharmacokinetics*


  • Adrenergic alpha-Antagonists
  • 11-hydroxyyohimbine
  • Yohimbine