Yohimbine
From Wikipedia, the free encyclopedia
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Yohimbine
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| Systematic (IUPAC) name | |
| 17α-hydroxy-yohimban-16α- carboxylic acid methyl ester |
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| Identifiers | |
| CAS number | |
| ATC code | G04 |
| PubChem | |
| ChemSpider | |
| Chemical data | |
| Formula | C21H26N2O3 |
| Mol. mass | 354.44 g/mol (base) 390.90 g/mol (hydrochloride) |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status |
OTC |
| Routes | ? |
Yohimbine is a tryptamine alkaloid and is the active chemical constituent of the medicinal herb Pausinystalia yohimbe (formerly Corynanthe yohimbe), also known as yohimbe or yohimbe bark. Yohimbine is a stimulant drug and purportedly has aphrodisiac qualities.
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[edit] Function
[edit] Aphrodisiac
The NIH states that yohimbine hydrochloride is the standardized form of yohimbine that is available as a prescription medicine in the United States, and has been shown in human studies to be effective in the treatment of male impotence.[1]
Yohimbine Hydrochloride, USP—a standardized form of yohimbine—is a prescription medicine that has been used to treat erectile dysfunction.[2] Controlled studies suggest that it is not always an effective treatment for impotence, and evidence of increased sex drive (libido) is anecdotal only.[3]
It cannot be excluded that orally administered yohimbine can have a beneficial effect in some patients with ED. The conflicting results available may be attributed to differences in drug design, patient selection, and definitions of positive response. However, generally, available results of treatment are not impressive.
– Review of literature on Yohimbine studies 2000., (Morales, 2000b)
Yohimbine has been shown to be effective in the reversal of sexual satiety and exhaustion in male rats.[4] Yohimbine has also been shown to increase the volume of ejaculated semen in dogs, with the effect lasting at least five hours after administration.[5] Yohimbine has been shown to be effective in the treatment of orgasmic dysfunction in men.[6]
[edit] Other uses
Yohimbine hydrochloride has also been used for the treatment of sexual side effects caused by some antidepressants (SSRIs), female hyposexual disorder, as a blood pressure boosting agent in autonomic failure, xerostomia, and as a probe for noradrenergic activity.
Yohimbine has been used to facilitate recall of traumatic memories in the treatment of posttraumatic stress disorder (PTSD).[7] Use of yohimbine outside therapeutic settings may not be appropriate for persons suffering from PTSD.[8]
According to one study, oral yohimbine supplementation may actuate significant fat loss in athletes.[9] Some internet shops sell expensive formulations of yohimbine for transdermal delivery to effect a local reduction of adipose tissue, although there is no experimental evidence that it is effective. Demand for products of this kind is frequently found in the bodybuilding community.
In veterinary medicine, yohimbine is used to reverse anesthesia from the drug xylazine in small and large animals.
[edit] Pharmacology
Yohimbine has high affinity for the α2A-adrenergic, α2B-adrenergic, and α2C-adrenergic receptors, moderate affinity for the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2B, and D2 receptors, and weak affinity for the D3 receptor.[10] Yohimbine also has unknown but significant affinity for the 5-HT2A receptor. Yohimbine behaves as an antagonist at all receptors except for the 5-HT1A, 5-HT1D, and 5-HT2A receptors, where it acts as a weak partial agonist.[10]
[edit] Production
Yohimbine is the principal alkaloid of the bark of the West African evergreen Pausinystalia yohimbe Pierre (formerly Corynanthe yohimbe), family Rubiaceae (Madder family). There are 31 other yohimbane alkaloids found in Yohimbe. In Africa, yohimbe has traditionally been used as an aphrodisiac.[2] However, it is very important to note that while the terms yohimbine, yohimbine hydrochloride, and yohimbe bark extract are related, they are not interchangeable.[1]
The main active chemical present in yohimbe bark is yohimbine HCl (indole alkaloid), found in the bark of the Pausinystalia yohimbe tree.
However, the levels of yohimbine that are present in yohimbe bark extract are variable and often very low.[1] Therefore, although yohimbe bark has been used traditionally to reduce male erectile dysfunction, there is not enough scientific evidence to form a definitive conclusion in this area.
[edit] Adverse effects
Yohimbine has significant side effects, such as anxiety reactions. According to the Mayo Clinic, yohimbine can be dangerous if used in excessive amounts.[11]
Higher doses of oral yohimbine may create numerous side effects, such as rapid heart rate, high blood pressure, overstimulation, insomnia and/or sleeplessness. Some effects in rare cases were panic attacks, hallucinations, headaches, dizziness, and skin flushing.[12]
More serious adverse effects may include seizures and renal failure. Yohimbine should not be consumed by anyone with liver, kidney, heart disease, or a psychological disorder.[12]
The range between an effective dose and a dangerous dose is very narrow; too large of a dosage can be harmful and toxic.[12] This may also lead to precipitation of panic disorder type reactions.
[edit] References
- ^ a b c [1] National Institutes of Health
- ^ a b [2] National Center for Complementary and Alternative Medicine
- ^ "Pharmacology of Penile Erection — Andersson 53 (3): 417 — Pharmacological Reviews". http://pharmrev.aspetjournals.org/cgi/content/full/53/3/417#SEC4_4_6_2. Retrieved on 2007-12-23.
- ^ Fernández-Guasti A, Rodríguez-Manzo G. Pharmacological and physiological aspects of sexual exhaustion in male rats. Scand J Psychol. 2003 Jul;44(3):257-63. PMID 12914589
- ^ Yonezawa A, Yoshizumii M, Ebiko M, Amano T, Kimura Y, Sakurada S. (2005). "Long-lasting effects of yohimbine on the ejaculatory function in male dogs". Biomed Res 26 (5): 201–6. doi:. PMID 16295696.
- ^ Adeniyi AA, Brindley GS, Pryor JP, Ralph DJ. (2007). "Yohimbine in the treatment of orgasmic dysfunction". Asian J Androl 9 (3): 403–7. doi:. PMID 17486282.
- ^ "Approaches to the Treatment of PTSD (1995)". http://www.traumatherapie.de/users/vanderkolk/kolk2.html.
- ^ "Yohimbine use in a natural setting: effects on posttraumatic stress disorder". http://www.ncbi.nlm.nih.gov/pubmed/7604149.
- ^ "Yohimbine: the effects on body composition and exercise performance in soccer players". http://www.ncbi.nlm.nih.gov/pubmed/17214405.
- ^ a b Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Cogé F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A. (2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.". Synapse 35 (2): 79-95. PMID 10611634.
- ^ [3] Mayo Clinic
- ^ a b c Prescription for Nutritional Healing, fourth edition Phyllis A. Balch, CNC
[edit] External links
- Erectile Dysfunction and Yohimbine
- Erowid Yohimbe Vault
- "Yohimbe bark extract" (MedlinePlus)
- Effectiveness Rating and Review of Yohimbe by Pharmacists
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