A Comprehensive Monograph on Yohimbine (DB01392)

1.0 Executive Summary

This monograph provides a comprehensive scientific and clinical assessment of yohimbine (DrugBank ID: DB01392), an indole alkaloid derived from botanical sources. The primary pharmacological action of yohimbine is potent antagonism of alpha-2 (α2​) adrenergic receptors, which disrupts a key negative feedback loop in the sympathetic nervous system, leading to a significant increase in norepinephrine release. This sympathomimetic activity underpins its physiological effects.

Historically, yohimbine was a first-line treatment for erectile dysfunction, and clinical evidence from randomized controlled trials supports its modest efficacy over placebo for this indication. However, with the advent of more effective and safer therapeutic classes, such as phosphodiesterase-5 inhibitors, its use in this capacity has become obsolete, and it is no longer recommended by major clinical guidelines. In contemporary settings, yohimbine is widely marketed and consumed as a dietary supplement, primarily for fat loss and athletic performance enhancement. These popular uses, however, are not supported by robust or consistent clinical evidence. The proposed mechanism for lipolysis is biologically plausible, but human trials have yielded conflicting results, and no significant ergogenic effects on performance have been consistently demonstrated.