Talk:Yohimbine
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Summary sheet: Yohimbine |
Yohimbine | |||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||
Common names | Yohimbine, Yocon, Yocoral or quebrachine | ||||||||||||||||||||||||||
Systematic name | methyl (1S,15R,18S,19R,20S)-18-hydroxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate | ||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||
Psychoactive class | Stimulant | ||||||||||||||||||||||||||
Chemical class | Indole alkaloid | ||||||||||||||||||||||||||
Routes of Administration | |||||||||||||||||||||||||||
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Yohimbine (also known as quebrachine) is a naturally-occurring stimulant substance of the indoloquinolizidine class. It has various uses including as an aphrodisiac and a weight loss agent. Most often, yohimbine is used in the form of hydrochloride.
Yohimbine, an alpha-2 adrenergic receptor antagonist, is an indole alkaloid found in numerous botanical sources. It is the predominant alkaloid in extracts from the bark of the Pausinystalia johimbe tree, and can also be found in Rauwolfia root.[1] Many of its effects are attributed to its α2-adrenergic receptor antagonist activity, which increases central sympathetic outflow and raises blood pressure, heart rate, and norepinephrine levels.[2]
Yohimbine is also used as a mydriatic and sympatholytic and has been suggested as an antidote to clonidine and xylazine overdose.[3]
While some reviewers noted that this extract did help them maintain an erection, lose weight or increase their energy level, many noted that the side effects they experienced outweighed any benefits they received. Some took a dosage that was considerably lower than recommended and still had unwanted side effects.
Chemistry
This chemistry section is incomplete. You can help by adding to it. |
Yohimbine is an indole alkaloid molecule of the indoloquinolizidine chemical class. Analyses of yohimbe bark indicate that the average total indole alkaloid content is approximately 3–6%, with approximately 10–15% of the alkaloids being yohimbine. In addition to yohimbine and its isomers (α-yohimbine, β-yohimbine, allo-yohimbine), these alkaloids include ajmaline, dihydroyohimbine, corynantheidine, dihydrocorynantheine, and corynanthine (rauhimbin).[2] Most often, yohimbine is used in the form of hydrochloride.
Yohimbine has been used for a variety of medical purposes, including as a treatment for erectile dysfunction, sexual dysfunction caused by selective serotonin reuptake inhibitors (SSRIs), and as a treatment for xerostomia (dry mouth). It has also been used as a performance-enhancing supplement in bodybuilding and athletics, as well as a weight loss supplement. However, there is limited scientific evidence to support the effectiveness of yohimbine for these purposes.
Yohimbine is believed to work by blocking alpha-2 adrenergic receptors, which can increase blood flow and improve circulation. However, it can also cause side effects such as anxiety, high blood pressure, and rapid heart rate. It may also interact with certain medications, such as antidepressants and medications for high blood pressure.
Despite its potential medical uses, yohimbine is not regulated by the FDA and is considered a dietary supplement. As with all supplements, it is important to discuss the use of yohimbine with a healthcare provider before taking it.
Yohimbine has been found to be effective in treating erectile dysfunction in men. It is believed to work by blocking alpha-2 adrenergic receptors, which can increase blood flow and improve circulation. This can improve the symptoms of erectile dysfunction. However, more research is needed to fully understand the effectiveness and safety of yohimbine for this purpose.
Studies have also found that yohimbine may be effective in treating sexual dysfunction caused by SSRIs. It is believed to work by increasing the release of neurotransmitters such as dopamine and norepinephrine, which can improve sexual function. However, more research is needed to confirm these findings.
In addition to its potential medical uses, yohimbine is also used as a performance-enhancing supplement in bodybuilding and athletics, as well as a weight loss supplement. However, there is limited scientific evidence to support the effectiveness of yohimbine for these purposes.
As with all supplements, it is important to discuss the use of yohimbine with a healthcare provider before taking it. Yohimbine can cause side effects such as anxiety, high blood pressure, and rapid heart rate. It may also interact with certain medications, such as antidepressants and medications for high blood pressure.
Pharmacology
The primary and most researched mechanism of yohimbine is antagonism of a class of receptors known as alpha-2 adrenergic receptors, thus it increases noradrenaline levels by preventing their uptake into subsequent neurons. Blocking alpha-2 adrenoceptors increases blood pressure, releases insulin, and decreases blood sugar levels. Yohimbine also, however, blocking alpha-1 adrenergic receptors, albeit with lower affinity. It also has been shown to weak inhibit monoamine oxidase.[4]
In high concentrations yohimbine behaves as an antagonist at dopamine D2 and D3 receptors, serotonin 5-HT1B, 5-HT1D, and 5-HT2B receptors, and as a partial agonist at 5-HT1A.[5]
Subjective effects
This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it. |
Compared to other stimulants, yohimbine can be described as less recreational. For many users, it is unpleasant, and often even with a small dosage causes anxiety and irritability.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects
-
Yohimbine pretty much gives body energy while doing very little for mind.
- Appetite suppression[6]
- Dizziness[4]
- Frequent urination[7]
- Headaches[4]
- Hyperthermia
- Increased blood pressure[7]
- Increased heart rate[4]
- Increased perspiration
- Increased salivation - The mechanism by which yohimbine increases submaxillary secretion appears to involve inhibition of presynaptic a2-ARs located on the chorda tympani, which inhibit cholinergic transmission.[8]
- Incoordination[4]
- Nausea[4]
- Pupil dilation[4]
- Seizures[4] - In extremely high dose, yohimbine can induce seizures.
- Stamina enhancement
- Stimulation - In terms of its effects on the physical energy levels of the user, yohimbine is usually considered to be mildly to moderately energetic and stimulating in a fashion that is considerably weaker in comparison to that of traditional recreational stimulants such as amphetamine or cocaine, but stronger than caffeine.
- Tactile enhancement
- Vasoconstriction
Cognitive effects
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- Analysis enhancement[9]
- Anxiety[4] - Yohimbine exerts a stimulating action on the emotions and may increase anxiety.
- Cognitive dysphoria
- Cognitive euphoria - Generally, this effect is rare and less pronounced than with classical stimulants.
- Disinhibition - Yohimbine can increase impulsivity.[10]
- Dream potentiation - Many users report that yohimbine in a dosage of up to 1 mg has a positive effect on the brightness of sleep and its memory.
- Ego inflation
- Emotion enhancement - Yohimbine makes whatever cognitive, especially emotional, sensation more intense. That sensation intensified could be positive or negative, it just depends on the context.
- Increased libido
- Irritability
- Motivation enhancement - Yohimbine can get motivation and mood levels up.
- Thought acceleration
- Wakefulness
Experience reports
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and harm potential
This toxicity and harm potential section is a stub. As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. |
Yohimbine has a low toxicity relative to dose. Various studies have shown that in reasonable doses in a careful context, it presents few negative cognitive, psychiatric or toxic physical consequences, though some exist. The side effects of yohimbine are clearly dose-dependent, are generally apparent at doses much higher than the claimed therapeutic doses. Generally all reported side effects of yohimbine are reversible and resolve spontaneously within a relatively short time after termination of the drug therapy[8], and most individuals who experience the inadvertent use of toxic doses will recover after a relatively short period of expectant restoration, which is measured in hours. Deaths from yohimbine overdosing are uncommonly reported but nonetheless published.[10] Higher doses (200 – 5,000 mg) result in stronger side effects and can be toxic to the brain. Extremely high doses (above 5,000 mg) can be lethal.[11]
Not recommended for individuals who have bleeding conditions as it can increase the risk of bleeding. For this reason, it is also dangerous for individuals who recently had a surgery. For those already taking this supplement, it is advised to stop intake two weeks before the scheduled surgery.
It is strongly recommended that one be familiar with harm reduction practices when using this drug.
Dependence and abuse potential
Yohimbine is not known to be not habit-forming and the desire to use it can actually decrease with use. It is most often self-regulating.
Tolerance to the effects of yohimbine are quickly built after repeated and frequent usage. After that, it takes about 7 days for the tolerance to be reduced to half and 14 days to be back at baseline (in the absence of further consumption). Yohimbine does not produce cross-tolerance with most other stimulants.
Dangerous interactions
Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).
Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
- 25x-NBOMe & 25x-NBOH - 25x compounds are highly stimulating and physically straining. Combinations with Yohimbine should be strictly avoided due to the risk of excessive stimulation and heart strain. This can result in increased blood pressure, vasoconstriction, panic attacks, thought loops, seizures, and heart failure in extreme cases.
- Alcohol - Combining alcohol with stimulants can be dangerous due to the risk of accidental over-intoxication. Stimulants mask alcohol's depressant effects, which is what most people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects will be left unopposed, which can result in blackouts and severe respiratory depression. If mixing, the user should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - Combinations with DXM should be avoided due to its inhibiting effects on serotonin and norepinephrine reuptake. There is an increased risk of panic attacks and hypertensive crisis, or serotonin syndrome with serotonin releasers (MDMA, methylone, mephedrone, etc.). Monitor blood pressure carefully and avoid strenuous physical activity.
- MDMA - Any neurotoxic effects of MDMA are likely to be increased when other stimulants are present. There is also a risk of excessive blood pressure and heart strain (cardiotoxicity).
- MXE - Some reports suggest combinations with MXE may dangerously increase blood pressure and increase the risk of mania and psychosis.
- Dissociatives - Both classes carry a risk of delusions, mania and psychosis, and these risk may be multiplied when combined.
- Stimulants - Yohimbine may be dangerous to combine with other stimulants like cocaine as they can increase one's heart rate and blood pressure to dangerous levels.
- Tramadol - Tramadol is known to lower the seizure threshold[12] and combinations with stimulants may further increase this risk.
- MAOIs - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, and some antidepressants.[13]
Legal status
This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
According to 1, yohimbine is uncontrolled in the United States, meaning it is legal to buy, sell or possess without a license or prescription. However, it is illegal to market it as a treatment for erectile dysfunction without getting FDA approval 2. Yohimbine is also unscheduled in the U.K., making it legal to buy, sell or possess 1.
However, yohimbine is banned in some other countries, such as Australia 1, Canada 2, New Zealand, Germany and Austria. In these countries, yohimbine can only be obtained with a prescription or not at all.
See also
External links
References
- ↑ Yohimbine | https://www.sciencedirect.com/science/article/pii/B9780128012383988627
- ↑ 2.0 2.1 Interactions between Nutraceuticals/Nutrients and Therapeutic Drugs | https://www.sciencedirect.com/science/article/pii/B9780128021477000607
- ↑ Encyclopedia of Toxicology. Yohimbine | https://www.sciencedirect.com/science/article/pii/B9780123864543007995
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 4.7 4.8 Encyclopedia of Toxicology | https://www.sciencedirect.com/science/article/pii/B9780123864543007995
- ↑ 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. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/10611634
- ↑ Yohimbine and rauwolscine reduce food intake of genetically obese (obob) and lean mice. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/6145164
- ↑ 7.0 7.1 Reference Module in Biomedical Sciences | https://www.sciencedirect.com/science/article/pii/B9780128012383988627
- ↑ 8.0 8.1 Yohimbine: a clinical review | https://www.sciencedirect.com/science/article/pii/S0163725801001565
- ↑ Differential effects of noradrenergic drugs on anxiety and arousal in healthy volunteers with high and low anxiety. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/9004342
- ↑ 10.0 10.1 An Overview of Yohimbine in Sports Medicine | https://www.sciencedirect.com/science/article/pii/B9780128054130000156
- ↑ Case study: two fatal case reports of acute yohimbine intoxication. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/23846025
- ↑ Talaie, H.; Panahandeh, R.; Fayaznouri, M. R.; Asadi, Z.; Abdollahi, M. (2009). "Dose-independent occurrence of seizure with tramadol". Journal of Medical Toxicology. 5 (2): 63–67. doi:10.1007/BF03161089. eISSN 1937-6995. ISSN 1556-9039. OCLC 163567183.
- ↑ Gillman, P. K. (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of Anaesthesia. 95 (4): 434–441. doi:10.1093/bja/aei210 . eISSN 1471-6771. ISSN 0007-0912. OCLC 01537271. PMID 16051647.