Yohimbine

Yohimbine - differently called — cvebrakhin - vegetable alkaloid with the stimulating action, the aphrodisiac received from Yohimbe plant. It is applied by bodybuilders to weight loss, drying of muscles, increase in a libido.

Substance C21H26O3N2 formula. In pure form represents colourless crystals with a temperature of melting of 235 — 237 °C. Studying of this group of alkaloids was stimulated search of the operating beginning of the known veterinary medicine, the so-called "Horse activator".

Yohimbine is the main alkaloid of a tree of Pausinystalia johimbe Pierre ex Beille, family of Rubiaceae growing in the central part of Africa still Yohimbine receive from bark of the South American plants White a quebracho (Aspidosperma quebracho-blanco Schltr.) and Rauvolfiya snake (Rauvolfia serpentina Benth. ex Kurz), Apocynaceae families. Cora Yokhimbe contains 0,5 — 1,5% of alkaloids of an indolny row. The main alkaloid is ιξυθμαθν, the others — isomers of a yokhimbin.

Physiological effects of Yohimbine

Yohimbine began to be used as means for treatment of erectile dysfunction and a stimulator of a men's potentiality. Yohimbine renders on a human body expressed simpatolic and stimulating action.

At the expense of a capability to inhibit MAO (monoaminooxidase) has anti-depressive effect.

Yohimbine has high affinity to alfa2-adrenoceptors, moderate affinity to alfa1-adrenoceptors, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2B, both D2 to receptors, and weak affinity to 5-HT1E, 5-HT2A, 5-HT5A, 5-HT7, and D3 to receptors. Yohimbine has antagonism (blocks) to alfa1-adrenoceptors, alfa2-adrenoceptors, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, both D2 to receptors, and agonistichesk interacts (initiates) with 5-HT1A receptors.

Action of yohimbine was in details researched in Kenneth Grasing work, MD and coauthors which was carried out for the purpose of studying of harm (shipping) and properties of substance in quite high dose (22 mg). Healthy young people participated in an experiment, influence on mood, warm activities, arterial pressure, etc. was studied.

Good tolerance, fast speed of assimilation and removal of substance was established. In case of the use together with greasy food decrease in concentration in blood was observed. Scientists showed that even high doses don't lead to development of side effects, moderately increasing pulse rate, breath, at the same time lowering arterial pressure. Yohimbine had significant effect on mentality, initiating a number of the psychostimulating effects: excitement, improvement of mood, and so forth

Influence on a dream: Yohimbine increases dream brightness, but only in very small doses if the dose more than 1 mg appears feeling of alarm during sleep. Yohimbine is much more effective in case of acceptance in early hours, in a REM sleep phase.

Yohimbine in sports delivery

Yohimbine possesses the expressed lipolytic action, this property allowed to receive yohimbine special popularity in a sports delivery. Fat-burning action of yohimbine is proved by authoritative researches. Besides yohimbine makes exciting impact on a CNS, improving cognitive functions, mental concentration, allows to train more longly and more intensively.

It is known that the majority of work as stimulators of secretion of an adrenaline which is excited, in turn, by an alpha and beta adrenoreceptors. At exaltation of beta receptors there is a fat destruction, and at exaltation of alpha receptors the boomerang effect is observed: inhibition of release of an adrenaline and accumulation of fat in fatty depots. Blocking alpha receptors, yohimbine allows fat to be blasted freely with energy allocation. Do not forget take Meldonium for better results.

There are also additional reasons which dictate need of blocking of alfa2-adrenoreceptors. It allows to reduce the arterial pressure which often increases at the use and also to strengthen a blood stream in fatty tissue at the expense of what transport of fatty acids to the place of destruction accelerates. Difficulty of disposal of fat in some places is explained with large number of alfa2-adrenoreceptors therefore yohimbine can precisely help to remove fatty deposits in the most problem places.

Recommendations about acceptance

The safe dose of yohimbine constitutes 10-20 mg. Time of semi-removal about 6 hours. Use additive together with food.

Legal status

Yohimbine isn't prohibited to sale, but is added by the resolution of the Chief state doctor of the Russian Federation to the list forbidding inclusion of yohimbine in unicomponent composition of dietary supplements.

Opinion of the expert:

The legislator's prohibition on restriction in production of yohimbine as unicomponent dietary supplement is caused by potential harm for health. Negative action of yohimbine, perhaps, is suppressed due to addition of the second active component. These legislative restrictions are proved or not - it is difficult to tell. In practice the producer can easily bypass this prohibition, it is enough add one more component. The large pharmaceutical enterprises observe this restriction.

Sports food with yohimbine

• Hydroxycut Hardcore X from MuscleTech
• Lipo-6x from Nutrex
• Fyre from Syntrax
• Tight! Xtreme from S.A.N.

Side effects of yohimbine

In researches high safety and good tolerance of additive, even was shown at the use of a single dose of 22 mg.

Sometimes, when using yohimbine and fat reducer on its basis are possible: fluctuations of arterial pressure and tachycardia (due to the stimulating influence on heart, expansion of a vascular bed), excitement, sleeplessness or a sleepiness, a headache, giddiness, erubescence (at the expense of vasodilatation). The risk of development of side effects increases at a combination to other stimulators (complex additives).

Contraindications to use of yohimbine: a hypertonia, an ischemic heart disease, diseases of a liver and/or kidneys, tachycardia, alienations, a hypersensibility to yohimbine.

Intoxication symptoms:

Approximately in 20 – 30 minutes after oral administration of an overdose there are a delicacy, generalized paresthesias, a lack of coordination and memories, and also a severe headache in a combination with giddiness, a tremor, heartbeat and feeling of alarm. The headache, a hypertensia and tachycardia can be also stored within several hours. From laboratory indicators high body height of level of Noradrenalinum is observed (it is normal of 150 - 550 pg/ml).

Besides, there can be nausea, vomiting, a mydriasis, salivation and a dacryagogue.

Alternative source

Yohimbine I a hydrochloride a2-adrenoblocker, influences mainly presynaptic central and peripheric a2-adrenoreceptors. Drug increases physical activity, physical working capacity, enlarges the CARDIAC CONTRACTIONS RATE, in small doses raises the ABP (due to stimulation of the vasomotor center), in larger — the ABP reduces (for the account and - adrenoceptor blocking action), strengthens inflow of a blood to organs of a small pelvis, including to genitals. Rastormazhivayet the spinal centers of an erection and ejaculation, improving thereby a cavernous bodies. Improves a psychoemotional background and sex feelings, promotes elimination of feeling of discomfort, uncertainty, restraint and pavor. Raises a libido and a potency. Weakens effect of serotonin which excess content in an organism causes a depression, nervousness. Has antidiuretic effect, will mobilize fatty acids from hypodermic fatty tissue.

It is quickly and completely soaked up from a GIT. At oral administration the beginning of action — in 15 — 30 min. In 10 min. after intake gets through GEB and it is found in cerebrospinal fluid. The maximum concentration in a blood plasma is reached in 1,3 h. About 17% of the entered yohimbine of a hydrochloride are defined in brain tissues during 6 h. Drug in a liver is metabolized.

Removal:

The elimination half-life of yohimbine after use of a single dose differs in different researches and makes from 0,25 to 2,5 hours. An elimination half-life of a 11-gidroksiyokhimbin longer – about 6 hours. After reusable use yohimbine it is removed in time range from less than 1 to more than 8 hours.

Drug inside, in the form of tablets on 5 — 10 mg of 1 — 3 time a day is used, without chewing and washing down with a glass of water. Duration of course use is 3 — 10 weeks.

Contraindications to use of yohimbine of a hydrochloride are: hypersensitivity, liver and/or renal failure, arterial hypertension, arterial hypotension, coronary heart disease, concomitant use of adrenomimetik, including Clophelinum. With care it is necessary to apply at a peptic ulcer of a stomach or a duodenum, mental diseases.

At reception of yohimbine development of side effects is possible: giddiness, headache, uneasiness, pavor, migraine, tremor of arms, vomiting, diarrhea, gastralgia, depression of the ABP, orthostatic hypotension, rising of the ABP, tachycardia, priapism.