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Yohimbine bioavailability in humans.

S K Guthrie1, M Hariharan, L J Grunhaus

  • 1College of Pharmacy, University of Michigan, Ann Arbor.

European Journal of Clinical Pharmacology
|January 1, 1990
PubMed
Summary
This summary is machine-generated.

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Yohimbine hydrochloride is quickly eliminated from the body. Oral bioavailability of yohimbine hydrochloride is highly variable, suggesting personalized dosing for clinical use.

Area of Science:

  • Pharmacology
  • Clinical Pharmacokinetics

Background:

  • Yohimbine hydrochloride is an alpha-2 adrenergic antagonist used for various clinical indications.
  • Understanding its pharmacokinetic profile is crucial for safe and effective therapeutic use.

Purpose of the Study:

  • To determine the pharmacokinetic profiles of yohimbine hydrochloride after single oral and intravenous doses.
  • To assess the oral bioavailability and elimination characteristics of yohimbine hydrochloride.

Main Methods:

  • Single oral and intravenous doses of 10 mg yohimbine hydrochloride administered to seven healthy young male subjects.
  • Pharmacokinetic parameters including elimination half-life, clearance, and bioavailability were calculated.
  • Data analyzed using a two-compartment pharmacokinetic model for intravenous administration.

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Main Results:

  • Yohimbine hydrochloride exhibited rapid elimination with a short elimination half-life (t1/2 beta ~0.6 h).
  • Intravenous administration followed a two-compartment model with a rapid distribution phase (t1/2a ~6 min).
  • Oral bioavailability was highly variable (7%-87%, mean 33%), with significantly higher oral clearance compared to intravenous clearance.

Conclusions:

  • Yohimbine hydrochloride is rapidly absorbed and eliminated, but its oral bioavailability is notably variable.
  • Potential reasons for variable oral bioavailability include incomplete gastrointestinal absorption or significant hepatic first-pass metabolism.
  • Individualized dosing strategies may be necessary for oral yohimbine hydrochloride therapy due to its unpredictable bioavailability.