Metabolism

The full metabolism of yohimbine in human is unknown. Yet the existence of tow metabolites, 10-hydroxyyohimbine and 11-hydroxyyohimbine. 11-hydroxyyohimbine, the main metabolite, largely present in plasma, exhibits a longer elimination half-life than yohimbine, 6.0h versus 1h respectively.

​Elimination
Orally administered yohimbine is rapidly eliminated from plasma (elimination half-life 0.6 1/- 0.26h). This clearance of yohimbine from plasma is constant over approximately 10 elimination half-lives. Yohimbine is probably eliminated primarily through metabolism since its rapid plasma clearance is not the result of renal elimination or sequestration by red blood cells. 
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Indication and filed of application
Penile erectile dysfunction of organic or psychogenic origin. Erectile dysfunction due to diabetes and drug side-effect.
Dosage and method of use 18mg of yohimbine daily (1 tablet Zumba 3 times a day), between meals, for a period of 3-4 weeks. If gastric or neurological intolerance develop, reduce the dose to 1 tablet per day, increasing progressively the dose slowly to 18mg per day. 
​ Contra-indications

Hepatic and renal insufficiency. Hypertension.

Precaution measures

In high doses, yohimbine may cause a blood pressure fall upon long standing.

Undesirable effects

Rarely and in high doses: nervousness, irritability, insomnia, tremor, head ache, nausea, diarrhea, orthostatic hypotension, tachycardia, priapism.

Interactions

Should not be administered in combination with alpha-mimetic drugs and especially those having a central nervous effect.

Overdosage

The dosage should be limited to 18mg per day, taken in 3 times 6mg. Accidents are extremely rare and have been reported for doses corresponding to 10times the therapeutic dose. 

Stability

Not to be used beyond the date indication of the package. To be stored at dry and cool place. 

Presentation

6mg tablets. Box of 60 tables in blister pack.

Sale category:OTC product 

Trademark holder:  Philomedica Ltd.

ZUMBA®

Yohimbine stimulates activity in animal. It produces a vasodilation of the cavernous body of the penis. Administered orally for 2-4 weeks, in doses below those causing die-effects, yohimbine restores erectile functionality in man.

Galenic form

Film coated tablets

Composition Yohimine hydrochloride 6mg 

Properties and effects 

Yohimbine is a selective alpha2-adrenoreceptor antagonist agent. At high doses it possesses a sympatholytic effect resulting from the inhibition of the postsynaptic alpha2-adrenoreceptors. 

Cardiovascular effects

In high doses, yohimbine produces hypertension accompanied by tachycardia. Yohimine counteracts the hypotension caused by tricyclic antidepressants. 
​Digestive apparatus
Yohimbine is an antagonist of the inhibition of intestinal contractions and of the gastric secretion triggered by alpha-agonists.

​Pharmacokinetics
Yohimbine is rapidly eliminated from plasma (t12 1/- 0.6h), has low renal excretion rate (lower than 1%), a high plasma clearance and its oral bioavailability is low and variable (about 30%). These data suggest that the low bioavailability of yohimbine may result from a first-pass effect. In the management of impotence, the delayed action of yohimbine administered orally may have a long half-life ( -elimination phase) that has not been detected, or its activity may reside in metabolite(s) displaying a biological half-life longer than the drug itself.

Absorption
The drug is rapidly absorbed (absorption half-time 0.17 +/- 0.11h). the bioavailability of orally administered yohimbine is approximately 30%, but varies within broad limits.