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Yohimbe School
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Yohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe (Yohimbe). It is also found naturally in Rauwolfia serpentina (Indian Snakeroot), Alchornea floribunda (Niando), along with several other active alkaloids. Yohimbine has been used as both an over-the-counter dietary supplement in herbal extract form and prescription medicine in pure form for the treatment of sexual dysfunction. Yohimbine was explored as a remedy for type 2 diabetes in animal and human models carrying polymorphisms of the α2A-adrenergic receptor gene.[1]
Contents
1 Indications
1.1 Sexual
1.2 Fat loss
1.3 Other uses
2 Pharmacology
3 Production
4 Adverse effects
5 See also
6 References
7 External links
Indications
Sexual
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.[2]
Yohimbine Hydrochloride, USP—a standardized form of yohimbine—is a prescription medicine that has been used to treat erectile dysfunction.[3] Controlled studies suggest that it is not always an effective treatment for impotence, and evidence of increased sex drive (libido) is anecdotal only.[4]
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.[5]
Yohimbine blocks the pre- and post-synaptic alpha-2 adrenoceptors. Blockade of post-synaptic alpha-2 adrenoceptors leads to minor corpora cavernosa smooth muscle relaxation. In fact the majority of adrenoceptors in the corpora cavernosa are alpha-1. Blockade of pre-synaptic alpha-2 adrenoceptors leads to increased release of neurotransmitters in the central nervous system and in the corpora cavernosa penis such as nitric oxide, noradrenaline, and dopamine. Whether nitric oxide released in the corpora cavernosa has a relaxing effect, noradrenaline has a much powerful constricting effect by stimulating the unblocked alpha-1 adrenoceptors. Concomitant use of an alpha-1 blocking agent will prevent constriction caused by the increased adrenergic stimulation.[6]
In addition to yohimbine, Pausinystalia yohimbe contains approximately 55 other alkaloids, of which yohimbine accounts for 1% to 20% of total alkaloids. Among them corynanthine is an alpha-1 adrenoceptor blocker. Hence the use of Yohimbe extract in sufficient dosages may provide concomitant alpha-1 and alpha-2 adrenoceptors blockade and thus may better enhance erections than yohimbine alone.[6]
Yohimbine has been shown to be effective in the reversal of sexual satiety and exhaustion in male rats.[7] Yohimbine has also been shown to increase the volume of ejaculated semen in dogs, with the effect lasting at least five hours after administration.[8] Yohimbine has been shown to be effective in the treatment of orgasmic dysfunction in men.[9]
Fat loss
According to one study, oral yohimbine supplementation may actuate significant fat loss in athletes.[10] Numerous bodybuilding supplement companies sell formulations of yohimbine for transdermal delivery to effect a local reduction of adipose tissue, although the experimental evidence for its efficacy is limited.[11][12]
Other uses
Yohimbine 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.
The addition of yohimbine to fluoxetine or venlafaxine has also been found to potentiate the antidepressant action of both of these agents.[13]
Yohimbine has been used to facilitate recall of traumatic memories in the treatment of post traumatic stress disorder (PTSD).[14] Use of yohimbine outside therapeutic settings may not be appropriate for persons suffering from PTSD.[15] In pharmacology, yohimbine is used as a probe for α2-adrenoceptor. In veterinary medicine, yohimbine is used to reverse anesthesia from the drug xylazine in small and large animals.
Pharmacology
Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1-adrenergic, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2B, and D2 receptors, and weak affinity for the 5-HT1E, 5-HT2A, 5-HT5A, 5-HT7, and D3 receptors.[16][17] It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a partial agonist at 5-HT1A.[16][18][19][20] Its intrinsic activities at the other sites listed are unclear/unknown, but it is probably mostly antagonistic at them.
Production
Yohimbine is the principal alkaloid of the bark of the West African evergreen Pausinystalia yohimbe (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.[3] However, it is very important to note that while the terms yohimbine, yohimbine hydrochloride, and yohimbe bark extract are related, they are not interchangeable.[2]
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.[2] 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.
The tree is currently threatened with extinction in its native habitat due to international demand.[citation needed] Its conservation is difficult because the bioactivity of the tree has led many Western governments to declare it a proscribed species.
Adverse effects
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.[21]
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.[21]
The therapeutic index of yohimbine is quite low; the range between an effective dose and a dangerous dose is very narrow.[21] A typical dose for sexual dysfunction would be 15-30mg, whereas 100mg would be considered dangerous. This may also lead to the precipitation of panic disorder type reactions, heart attack, and possibly death.
Yohimbine in combination with modafinil is frequently associated with nausea, dangerous acute rapid heart beat, and acute increased blood pressure. Yohimbine exhibits some degree of MAOI activity while modafinil has been shown to increase levels of various monamines, and therefore could result in severe risk of dangerous side effects.
See also
Ajmalicine
Corynanthine
Rauwolscine
Reserpine
Deserpidine
Rescinnamine
References
^ Rosengren, A. H.; Jokubka, R.; Tojjar, D.; Granhall, C.; Hansson, O.; Li, D.-Q.; Nagaraj, V.; Reinbothe, T. M. et al. (2009). "Overexpression of Alpha2A-Adrenergic Receptors Contributes to Type 2 Diabetes". Science 327 (5962): 217–20. DOI:10.1126/science.1176827. PMID 19965390.
^ a b c "Yohimbe: MedlinePlus Supplements". nlm.nih.gov. November 19, 2010. Retrieved December 13, 2010.
^ a b Yohimbe. National Center for Complementary and Alternative Medicine.
^ Andersson KE (September 2001). "Pharmacology of penile erection". Pharmacological Reviews 53 (3): 417–50. PMID 11546836.
^ Andersson, Karl-Erik; Steers, William D. (1998). "The pharmacological basis of sexual therapeutics". In Morales, Alvaro. Erectile dysfunction: issues in current pharmacotherapy. London: Martin Dunitz. pp. 97–124 [114]. ISBN 978-1-85317-577-0.
^ a b Saenz De Tejada, I; Kim, NN; Goldstein, I; Traish, AM (2000). "Regulation of pre-synaptic alpha adrenergic activity in the corpus cavernosum". International Journal of Impotence Research 12 Suppl 1: S20–25. PMID 10845761.
^ Fernández-Guasti A, Rodríguez-Manzo G (July 2003). "Pharmacological and physiological aspects of sexual exhaustion in male rats". Scandinavian Journal of Psychology 44 (3): 257–63. DOI:10.1111/1467-9450.00343. PMID 12914589.
^ Yonezawa A, Yoshizumii M, Ebiko M, Amano T, Kimura Y, Sakurada S (October 2005). "Long-lasting effects of yohimbine on the ejaculatory function in male dogs". Biomedical Research 26 (5): 201–6. DOI:10.2220/biomedres.26.201. PMID 16295696.
^ Adeniyi AA, Brindley GS, Pryor JP, Ralph DJ (May 2007). "Yohimbine in the treatment of orgasmic dysfunction". Asian Journal of Andrology 9 (3): 403–7. DOI:10.1111/J.1745-7262.2007.00276.x. PMID 17486282.
^ Ostojic SM (2006). "Yohimbine: the effects on body composition and exercise performance in soccer players". Research in Sports Medicine 14 (4): 289–99. DOI:10.1080/15438620600987106. PMID 17214405.
^ www.mesomorphosis.com/articles/volk/yohimbine-02.htm
^ Yohimbe Info and Products at Bodybuilding.com
^ Dhir, A; Kulkarni, SK (2007). "Effect of addition of yohimbine (alpha-2-receptor antagonist) to the antidepressant activity of fluoxetine or venlafaxine in the mouse forced swim test". Pharmacology 80 (4): 239–43. DOI:10.1159/000104877. PMID 17622775.
^ van der Kolk, Bessel A. (1995). "The Treatment of Post Traumatic Stress Disorder". In Hobfoll, Stevan E.; De Vries, Marten W.. Extreme stress and communities: impact and intervention. Boston: Kluwer Academic Publishers. pp. 421–44. ISBN 978-0-7923-3468-2.
^ Morgan CA, Grillon C, Southwick SM et al. (February 1995). "Yohimbine facilitated acoustic startle in combat veterans with post-traumatic stress disorder". Psychopharmacology 117 (4): 466–71. DOI:10.1007/BF02246220. PMID 7604149.
^ a b Millan MJ, Newman-Tancredi A, Audinot V et al. (February 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. DOI:10.1002/(SICI)1098-2396(200002)35:2<79::AID-SYN1>3.0.CO;2-X. PMID 10611634.
^ "PDSP Ki Database".
^ Arthur JM, Casañas SJ, Raymond JR (June 1993). "Partial agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". Biochemical Pharmacology 45 (11): 2337–41. DOI:10.1016/0006-2952(93)90208-E. PMID 8517875.
^ Kaumann AJ (June 1983). "Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors". Naunyn-Schmiedeberg's Archives of Pharmacology 323 (2): 149–54. DOI:10.1007/BF00634263. PMID 6136920.
^ Baxter GS, Murphy OE, Blackburn TP (May 1994). "Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle". British Journal of Pharmacology 112 (1): 323–31. PMC 1910288. PMID 8032658.
^ a b c Prescription for Nutritional Healing, fourth edition Phyllis A. Balch, CNC
Heres the link as well: en.wikipedia.org/wiki/Yohimbine
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Alpha-2 receptors are common in sites of the body that tend to preferentially accumulate fat; abdomen, breasts, buttocks and thighs. When exposed to circulating catecholamines, such as norepinephrine and epinephrine, alpha-2 receptor sites inhibit lipolysis (the release of fatty acids), while the beta receptors stimulate lipolysis. Generally speaking, epinephrine, norepinephrine, glucagon, adrenocorticotropic hormone (ACTH), and growth hormone stimulate the release of fatty acids from adipose tissue into the blood stream. Once in the blood stream, fatty acids are usually rapidly oxidized if the fatty acid blood concentration is not elevated from fatty acid input resulting from a meal.
Generally, when fatty acid blood concentration is high, it favors fat storage, which results from over-eating and inactivity. Although, keeping in mind that fatty acids are always used for energy, it is the balance between the amount of fatty acids ingested versus their use for energy that determines how much ends up stored as fat. Of course, this is a rather simplistic explanation of fatty acid metabolism. There is much more involved in these fat storage/utilization dynamics, and those who want more insight on these dynamics should click on the link below to get more information on ISSA's SPN course book. In that book, I am able to delve into these dynamics in much more detail.
Hypothetically speaking, blocking the alpha-2 receptors might be useful during weight loss to free up the catecholamines like norepinephrine, making more available to stimulate beta receptor sites, resulting in a higher rate of lipolysis. Also, yohimbine, through its alpha 2-adrenergic receptor antagonist activity, has been shown to increase levels of norepinephrine in the blood stream.
Galitzky and coworkers observed during their 14- day study of yohimbine treatment that lipid-mobilizing effects were sustained during this study period. This research collaborated their earlier observations found using yohimbine as a lipid-mobilizing agent, as well as from the research of Lafontan and coworkers.
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I took one once and I felt like shit bru, was jittery and naar and I couldnt eat.
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DO NOT TAKE NO FOR AN ANSWER
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Byron182 wrote: I get very horny on the stuff and get wet dreams some of the days . Not sure if its the clen or yoh that gives me the heat flashes. Maybe the dreams are linked to the zetofen and deep sleep...
Eish bud, didn't really want to know that haha :pinch:
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Byron182 wrote: I get very horny on the stuff and get wet dreams some of the days . Not sure if its the clen or yoh that gives me the heat flashes. Maybe the dreams are linked to the zetofen and deep sleep...
Hahahahahhahahahhahahahhahahahahhahahahahhahahahahahhahahahahhahahaha ROTF! :lol: :silly: :lol:
+1 for making my day bru
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rvp01 wrote: Ha ha ha ha ha as long as they not western dreams bro (the kind when you wake up and you still shooting) :lol: it's probably from the yohimbine bud
:lol: :lol: :lol:
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With hard work and dedication you can achieve anything!
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