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Yohimbine

Yohimbine is an alkaloid originally found in the bark of the Yohimbe tree that grows in southern Africa. It has been used as an aphrodisiac and to treat sexual dysfunction for centuries but has gained recent notoriety as a fat loss supplement. Numerous recent studies have indicated that yohimbine is effective at blocking alpha adrenoreceptors, something that as will be detailed later is highly efficient at promoting fat loss. For this reason yohimbine has become quite popular and relatively widely available.

The primary mechanism by which yohimbine works is by blocking alpha adrenoreceptors. These receptors, when stimulated, prevent the release of norepinephrine. Norepinephrine is one of the primary lipolytic hormones in the body and stimulates the alpha and beta adrenoreceptors. There are several feedback mechanisms that cause norepinephrine release to be stunted. Yohimbine works to combat this. Stimulation of the beta adrenoreceptors, via norepinephrine, can cause lipolysis (the break down of fat). By blocking the alpha adrenoreceptors more norepinephrine is able to be released and lipolysis can continue.

The reason why the inhibition of the alpha adrenoreceptor works so well in terms of promoting fat loss is that it is responsible for regulating lipolysis during the times that are bodies are at rest and not during strenuous activity, i.e. the majority of the day. Therefore by stimulating the mechanism that allows us to burn fat during most of the day we become even more efficient at burning fat. Interestingly enough it also is true that the majority of males have a higher ratio of alpha adrenoceptors in the body fat that they hold in their abdominal areas, while women have a higher ratio in the body fat around their hips and thighs. This would bode well for those individuals having trouble reducing their fat deposits in those areas that are seemingly universal among the sexes.

Other than the effects that yohimbine has on lipolysis, it has also been successfully used to treat sexual dysfunction in men (1) and can help with sexual arousal in women if combined with L-arginine glutamate (2) as it is a vasodilator. It has also been shown to slightly raise testosterone levels in males (3), however this rise is negligible. There are also anecdotal reports by some users that they experience an increased "pump" in the gym while using the supplement, however of course there is no scientific research or studies to back up this assertion.


Use and Dosing for Yohimbine>

Clinically, doses of approximately .2mg per kilogram per day have been shown to be effective is reducing body fat for both men and women (4, 5). This type of dosing should also result few side effects for the user. The half life of yohimbine is only about one to two hours, however because the half life of the metabolite 11-hydroxy-yohimbine is six to eight hours (and this metabolite has a similar action as yohimibine itself) a user should only have to take doses of the supplement two or three times per day to see the full effects.

It is recommended that yohimbine be taken on an empty stomach as if it was to be taken with meals this may reduce it's lipolytic effects (5). Of course, as is discussed below, due to some of the side effects associated with yohimbine it is advisable that a user do not take it close to when they are going to sleep as it can cause insomnia.

In terms of length of use there is no direct information stating that yohimbine becomes less effective the longer a user administers it, however anecdotally most users report that the effects of the compound tend to dissipate over time and doses must be increased to continue at previous levels. This would seem to indicate that some receptor down-regulation, which is likely to occur.

For this reason it would seem obvious that users need to cycle their use of yohimbine. Since there are no studies suggesting the most efficient way to do this, it is primarily up to the user to experiment with the most effective method to be used.


Risks and Side Effects while using Yohimbine>

The side effects associated with yohimbine are mostly related to the elevated levels of norepinephrine that it causes. Anxiety, increased heart rate and a rise in blood pressure are all side effects that are common at higher doses, with insomnia be related to these.

Other possible side effects include dizziness, anxiety, hyperstimulation, and nausea among others (6). There are conflicting studies that suggest that in some cases yohimbine can cause antidiuresis, decreased frequency of urination (7) or an increased frequency of urination (6). The reason for the discrepancy is not explained in the scientific literature, but there could be numerous variables in the studies that would be cause for this difference in the information.

Also due to yohimbine being able to downregulate your body's response to norepinephrine many male users will complain of not being able to achieve orgasm during sexual activity. This is somewhat ironic in the fact that yohimbine can help with erectile difficulties, but can cause problems in "completing the act".

Of course, with all supplements like yohimbine it is recommended that a user begin taking a much smaller dosage than is required to begin with so that they are able to gage their reaction to it. Many will find that they are able to use doses far smaller than thought and achieve good results. As well, one does not want to start off with high doses if the side effects are unbearable. All side effects associated with yohimbine dissipate once administration of the supplement ceases.

As always, any potential drug interactions should be discussed with a doctor. It should be noted however that yohimbine is often prescribed to individuals who are taking selective serotonine re-uptake inhibitors and suffer from erectile dysfunction as a side affect of this medication. It is also often advised that yohimbine can cause adverse reactions if combined with monoamine oxydase inhibitors (MAOIs). They same is true of some anti-depressant medications. Again, if you are using other types of medications consult with your doctor before beginning yohimbine.


References


1. Tam SW, Worcel M, Wyllie M. Yohimbine: a clinical review. Pharmacol Ther. 2001 Sep;91(3):215-43

2. Meston CM, Worcel M. The effects of yohimbine plus L-arginine glutamate on sexual arousal in postmenopausal women with sexual arousal disorder. Arch Sex Behav. 2002 Aug;31(4):323-32

3. Guay AT, Spark RF, Jacobson J, Murray FT, Geisser ME. Yohimbine treatment of organic erectile dysfunction in a dose-escalation trial. Int J Impot Res. 2002 Feb;14(1):25-31

4. Berlan M, Galitzky J, Riviere D, Foureau M, Tran MA, Flores R, Louvet JP, Houin G, Lafontan M. Plasma catecholamine levels and lipid mobilization induced by yohimbine in obese and non-obese women. Int J Obes. 1991 May;15(5):305-15

5. Galitzky J, Taouis M, Berlan M, Riviere D, Garrigues M, Lafontan M. Alpha 2-antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male volunteers. Eur J Clin Invest. 1988 Dec;18(6):587-94

6. Webber R. Erectile dysfunction. Clinical Evidence. 2003 (10): 1003�1011

7. Farjam A, Greven J. Effects of the alpha 2-adrenoceptor antagonists yohimbine and idazoxan on kidney function in intact and diabetes insipidus rats. Urol Int. 1989;44(5):255-9.







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