Yohimbine
Encyclopedia
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.
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.
Yohimbine Hydrochloride, USP—a standardized form of yohimbine—is a prescription medicine that has been used to treat erectile dysfunction. Controlled studies suggest that it is not always an effective treatment for impotence, and evidence of increased sex drive (libido) is anecdotal only.
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.
Pausinystalia Yohimbe (Yohimbe) doesn't contain just Yohimbine. It contains around 55 other alkaloids and 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 then Yohimbine alone.
Yohimbine has been shown to be effective in the reversal of sexual satiety and exhaustion in male rats. Yohimbine has also been shown to increase the volume of ejaculated semen in dogs, with the effect lasting at least five hours after administration. Yohimbine has been shown to be effective in the treatment of orgasmic dysfunction in men.
delivery to effect a local reduction of adipose tissue
, although the experimental evidence for its efficiency is limited.
, 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.
Yohimbine has been used to facilitate recall of traumatic memories in the treatment of post traumatic stress disorder (PTSD). Use of yohimbine outside therapeutic settings may not be appropriate for persons suffering from PTSD.
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.
, 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. 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. Its intrinsic activities
at the other sites listed are unclear/unknown, but it is probably mostly antagonistic at them.
(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
. However, it is very important to note that while the terms yohimbine, yohimbine hydrochloride, and yohimbe bark extract are related, they are not interchangeable.
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. 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. Its conservation is difficult because the bioactivity of the tree has led many Western governments to declare it a proscribed species.
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
.
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.
The therapeutic index
of yohimbine is quite low; the range between an effective dose and a dangerous dose is very narrow. This may also lead to precipitation of panic disorder type reactions.
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.
Alkaloid
Alkaloids are a group of naturally occurring chemical compounds that contain mostly basic nitrogen atoms. This group also includes some related compounds with neutral and even weakly acidic properties. Also some synthetic compounds of similar structure are attributed to alkaloids...
with stimulant
Stimulant
Stimulants are psychoactive drugs which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others...
and aphrodisiac
Aphrodisiac
An aphrodisiac is a substance that increases sexual desire. The name comes from Aphrodite, the Greek goddess of sexuality and love. Throughout history, many foods, drinks, and behaviors have had a reputation for making sex more attainable and/or pleasurable...
effects found naturally
Natural resource
Natural resources occur naturally within environments that exist relatively undisturbed by mankind, in a natural form. A natural resource is often characterized by amounts of biodiversity and geodiversity existent in various ecosystems....
in Pausinystalia yohimbe
Pausinystalia yohimbe
Pausinystalia yohimbe , formerly known as Corynanthe yohimbe, is a psychoactive plant which contains the tryptamine alkaloid yohimbine. It is widely distributed over-the-counter as an herbal aphrodisiac.- References :...
(Yohimbe). It is also found naturally in Rauwolfia serpentina
Rauwolfia serpentina
Rauvolfia serpentina, or 'snakeroot' or 'sarpagandha' is a species of flowering plant in the family Apocynaceae.-Medicinal uses:It is one of the 50 fundamental herbs used in traditional Chinese medicine, where it has the name shégēn mù or yìndù shémù .Rauwolfia serpentina contains a number of...
(Indian Snakeroot), Alchornea floribunda
Alchornea floribunda
Alchornea floribunda is a plant native to Sudan, Uganda, Cameroon, Central African Republic, the Republic of Congo, Equatorial Guinea , Gabon, São Tomé and Príncipe, the Democratic Republic of Congo, Côte d'Ivoire, Ghana, Guinea, Liberia, Nigeria and Sierra Leone...
(Niando), along with several other active alkaloids. Yohimbine has been used as both an over-the-counter
Over-the-counter drug
Over-the-counter drugs are medicines that may be sold directly to a consumer without a prescription from a healthcare professional, as compared to prescription drugs, which may be sold only to consumers possessing a valid prescription...
dietary supplement
Dietary supplement
A dietary supplement, also known as food supplement or nutritional supplement, is a preparation intended to supplement the diet and provide nutrients, such as vitamins, minerals, fiber, fatty acids, or amino acids, that may be missing or may not be consumed in sufficient quantities in a person's diet...
in herbal extract
Herbal extract
Tincture is a liquid solution of herbs and a fluid menstruum, usually ethanol. The dried or fresh herbs are combined with alcohol, then the solid matter is removed leaving only the oils of the herbs mixed with the alcohol...
form and prescription
Prescription drug
A prescription medication is a licensed medicine that is regulated by legislation to require a medical prescription before it can be obtained. The term is used to distinguish it from over-the-counter drugs which can be obtained without a prescription...
medicine
Medicine
Medicine is the science and art of healing. It encompasses a variety of health care practices evolved to maintain and restore health by the prevention and treatment of illness....
in pure form for the treatment
Therapy
This is a list of types of therapy .* Adventure therapy* Animal-assisted therapy* Aquatic therapy* Aromatherapy* Art and dementia* Art therapy* Authentic Movement* Behavioral therapy* Bibliotherapy* Buteyko Method* Chemotherapy...
of sexual dysfunction
Sexual dysfunction
Sexual dysfunction or sexual malfunction refers to a difficulty experienced by an individual or a couple during any stage of a normal sexual activity, including desire, arousal or orgasm....
. Yohimbine was explored as a remedy for type 2 diabetes in animal and human models carrying polymorphisms of the α2A-adrenergic receptor gene.
Sexual
The NIHNational Institutes of Health
The National Institutes of Health are an agency of the United States Department of Health and Human Services and are the primary agency of the United States government responsible for biomedical and health-related research. Its science and engineering counterpart is the National Science Foundation...
states that yohimbine hydrochloride is the standardized form of yohimbine that is available as a prescription medicine in the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
, and has been shown in human studies to be effective in the treatment of male impotence.
Yohimbine Hydrochloride, USP—a standardized form of yohimbine—is a prescription medicine that has been used to treat erectile dysfunction. Controlled studies suggest that it is not always an effective treatment for impotence, and evidence of increased sex drive (libido) is anecdotal only.
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.
Pausinystalia Yohimbe (Yohimbe) doesn't contain just Yohimbine. It contains around 55 other alkaloids and 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 then Yohimbine alone.
Yohimbine has been shown to be effective in the reversal of sexual satiety and exhaustion in male rats. Yohimbine has also been shown to increase the volume of ejaculated semen in dogs, with the effect lasting at least five hours after administration. Yohimbine has been shown to be effective in the treatment of orgasmic dysfunction in men.
Fat loss
According to one study, oral yohimbine supplementation may actuate significant fat loss in athletes. Numerous bodybuilding supplement companies sell formulations of yohimbine for transdermalTransdermal
Transdermal is a route of administration wherein active ingredients are delivered across the skin for systemic distribution. Examples include transdermal patches used for medicine delivery, and transdermal implants used for medical or aesthetic purposes....
delivery to effect a local reduction of adipose tissue
Adipose tissue
In histology, adipose tissue or body fat or fat depot or just fat is loose connective tissue composed of adipocytes. It is technically composed of roughly only 80% fat; fat in its solitary state exists in the liver and muscles. Adipose tissue is derived from lipoblasts...
, although the experimental evidence for its efficiency is limited.
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, xerostomiaXerostomia
Xerostomia is the medical term for the subjective complaint of dry mouth due to a lack of saliva. Xerostomia is sometimes colloquially called pasties, cottonmouth, drooth, or doughmouth. Several diseases, treatments, and medications can cause xerostomia. It can also be exacerbated by smoking or...
, and as a probe for noradrenergic activity.
The addition of yohimbine to fluoxetine
Fluoxetine
Fluoxetine is an antidepressant of the selective serotonin reuptake inhibitor class. It is manufactured and marketed by Eli Lilly and Company...
or venlafaxine
Venlafaxine
Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class. First introduced by Wyeth in 1993, now marketed by Pfizer, it is licensed for the treatment of major depressive disorder , as a treatment for generalized anxiety disorder, and comorbid indications in...
has also been found to potentiate the antidepressant action of both of these agents.
Yohimbine has been used to facilitate recall of traumatic memories in the treatment of post traumatic stress disorder (PTSD). Use of yohimbine outside therapeutic settings may not be appropriate for persons suffering from PTSD.
In pharmacology, yohimbine is used as a probe for α2-adrenoceptor.
In veterinary medicine
Veterinary medicine
Veterinary Medicine is the branch of science that deals with the prevention, diagnosis and treatment of disease, disorder and injury in non-human animals...
, yohimbine is used to reverse anesthesia
Anesthesia
Anesthesia, or anaesthesia , traditionally meant the condition of having sensation blocked or temporarily taken away...
from the drug xylazine
Xylazine
Xylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. An analogue of clonidine, it is an agonist at the α2 class of adrenergic receptor....
in small and large animals.
Pharmacology
Yohimbine has high affinity for the α2-adrenergic receptorAlpha-2 adrenergic receptor
The alpha-2 adrenergic receptor is a G protein-coupled receptor associated with the Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-, α2B-, and α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well...
, moderate affinity for the α1-adrenergic
Alpha-1 adrenergic receptor
The alpha-1 adrenergic receptor is a G protein-coupled receptor associated with the Gq heterotrimeric G-protein. It consists of three highly homologous subtypes, including α1A-, α1B-, and α1D-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. It behaves as an antagonist
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a partial agonist
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
at 5-HT1A. Its intrinsic activities
Intrinsic activity
Intrinsic activity or efficacy refers to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind to its molecular target, and the EC50, which is a measure of the...
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 yohimbePausinystalia yohimbe
Pausinystalia yohimbe , formerly known as Corynanthe yohimbe, is a psychoactive plant which contains the tryptamine alkaloid yohimbine. It is widely distributed over-the-counter as an herbal aphrodisiac.- References :...
(formerly Corynanthe yohimbe), family Rubiaceae
Rubiaceae
The Rubiaceae is a family of flowering plants, variously called the coffee family, madder family, or bedstraw family. The group contains many commonly known plants, including the economically important coffee , quinine , and gambier , and the horticulturally valuable madder , west indian jasmine ,...
(Madder family). There are 31 other yohimbane alkaloids found in Yohimbe. In Africa, yohimbe has traditionally been used as an aphrodisiac
Aphrodisiac
An aphrodisiac is a substance that increases sexual desire. The name comes from Aphrodite, the Greek goddess of sexuality and love. Throughout history, many foods, drinks, and behaviors have had a reputation for making sex more attainable and/or pleasurable...
. However, it is very important to note that while the terms yohimbine, yohimbine hydrochloride, and yohimbe bark extract are related, they are not interchangeable.
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. 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. Its conservation is difficult because the bioactivity of the tree has led many Western governments to declare it a proscribed species.
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.Higher doses of oral yohimbine may create numerous side effects, such as rapid heart rate
Tachycardia
Tachycardia comes from the Greek words tachys and kardia . Tachycardia typically refers to a heart rate that exceeds the normal range for a resting heart rate...
, high blood pressure, overstimulation, insomnia
Insomnia
Insomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...
and/or sleeplessness. Some effects in rare cases were panic attacks, hallucinations, headaches, dizziness
Dizziness
Dizziness refers to an impairment in spatial perception and stability. The term is somewhat imprecise. It can be used to mean vertigo, presyncope, disequilibrium, or a non-specific feeling such as giddiness or foolishness....
, and skin flushing
Flushing (physiology)
For a person to flush is to become markedly red in the face and often other areas of the skin, from various physiological conditions. Flushing is generally distinguished, despite a close physiological relation between them, from blushing, which is milder, generally restricted to the face, cheeks or...
.
More serious adverse effects may include seizures and renal failure
Renal failure
Renal failure or kidney failure describes a medical condition in which the kidneys fail to adequately filter toxins and waste products from the blood...
. Yohimbine should not be consumed by anyone with liver
Liver disease
Liver disease is a broad term describing any single number of diseases affecting the liver.-Diseases:* Hepatitis, inflammation of the liver, caused mainly by various viruses but also by some poisons , autoimmunity or hereditary conditions...
, kidney, heart disease
Heart disease
Heart disease, cardiac disease or cardiopathy is an umbrella term for a variety of diseases affecting the heart. , it is the leading cause of death in the United States, England, Canada and Wales, accounting for 25.4% of the total deaths in the United States.-Types:-Coronary heart disease:Coronary...
, or a psychological disorder.
The therapeutic index
Therapeutic index
The therapeutic index is a comparison of the amount of a therapeutic agent that causes the therapeutic effect to the amount that causes death or toxicity ....
of yohimbine is quite low; the range between an effective dose and a dangerous dose is very narrow. This may also lead to precipitation of panic disorder type reactions.
Yohimbine in combination with modafinil
Modafinil
Modafinil is an analeptic drug manufactured by Cephalon, and is approved by the U.S. Food and Drug Administration for the treatment of narcolepsy, shift work sleep disorder, and excessive daytime sleepiness associated with obstructive sleep apnea...
is frequently associated with nausea, dangerous acute rapid heart beat, and acute increased blood pressure. Yohimbine exhibits some degree of MAOI activity while modafinil
Modafinil
Modafinil is an analeptic drug manufactured by Cephalon, and is approved by the U.S. Food and Drug Administration for the treatment of narcolepsy, shift work sleep disorder, and excessive daytime sleepiness associated with obstructive sleep apnea...
has been shown to increase levels of various monamines, and therefore could result in severe risk of dangerous side effects.
See also
- AjmalicineAjmalicineAjmalicine, also known as δ-yohimbine or raubasine, is an antihypertensive drug used in the treatment of high blood pressure. It has been marketed under numerous brand names including Card-Lamuran, Circolene, Cristanyl, Duxil, Duxor, Hydroxysarpon, Iskedyl, Isosarpan, Isquebral, Lamuran, Melanex,...
- CorynanthineCorynanthineCorynanthine, also known as rauhimbine, is an alkaloid found in the Rauwolfia and Pausinystalia genera of plants. It is one of the two diastereoisomers of yohimbine, the other being rauwolscine...
- RauwolscineRauwolscineRauwolscine, also known as isoyohimbine, α-yohimbine, and corynanthidine, is an alkaloid found in various species within the genera Rauwolfia and Pausinystalia . It is a stereoisomer of yohimbine...
- ReserpineReserpineReserpine is an indole alkaloid antipsychotic and antihypertensive drug that has been used for the control of high blood pressure and for the relief of psychotic symptoms, although because of the development of better drugs for these purposes and because of its numerous side-effects, it is rarely...
- DeserpidineDeserpidineDeserpidine is an antihypertensive drug related to reserpine.-References:...
- RescinnamineRescinnamineRescinnamine is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug.It is an alkaloid obtained from Rauwolfia serpentina and other species of Rauwolfia....
External links
- "Yohimbe bark extract" (MedlinePlusMedlinePlusMedlinePlus is a free Web site that provides consumer health information for patients, families, and Health care providers. The site brings together information from the United States National Library of Medicine, the National Institutes of Health , other U.S. government agencies, and...
) - Effectiveness Rating and Review of Yohimbe by Pharmacists