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Yohimbine | CAS No: 146-48-5 | GMP-certified suppliers
A medication that treats erectile dysfunction of vascular, diabetic, or psychogenic origin and acts as a sympatholytic and mydriatic for autonomic and urological applications.
Therapeutic categories
Primary indications
- Indicated as a sympatholytic and mydriatic
- Impotence has been successfully treated with yohimbine in male patients with vascular or diabetic origins and psychogenic origins
Product Snapshot
- Yohimbine is available as oral sugar-coated tablets
- It is used primarily for sympatholytic and mydriatic applications, as well as treatment of impotence related to vascular, diabetic, or psychogenic origins
- Yohimbine is approved for use in the Canadian market with approved, investigational, and veterinary indications
Clinical Overview
Pharmacodynamically, yohimbine exerts its effects by blocking presynaptic alpha-2 adrenergic receptors, leading to increased release of norepinephrine. This blockade results in enhanced parasympathetic (cholinergic) activity concomitant with a reduction in sympathetic (adrenergic) tone. The mechanism believed to contribute to its therapeutic use in impotence involves an increase in sympathetic drive via central alpha-2 adrenergic receptor blockade, potentially enhancing penile inflow and/or reducing outflow. Additionally, interactions with neurotransmitters such as dopamine, serotonin, and cholinergic systems may play contributory roles. Peripheral vascular effects mirror those of reserpine but are milder and transient. Yohimbine’s mild antidiuretic action is postulated to occur through hypothalamic stimulation and posterior pituitary hormone release.
Absorption, distribution, metabolism, and excretion parameters are not extensively documented in detail; however, yohimbine is a substrate for cytochrome P450 enzymes including CYP2D6 and CYP3A4, implicating potential drug-drug interactions and variable metabolic clearance in certain populations. It also interacts with P-glycoprotein transport pathways.
Safety considerations include the potential for increased anxiety and mood stimulation at higher doses. Yohimbine does not significantly stimulate cardiac beta-adrenergic receptors and may lower blood pressure, although controlled data quantifying this effect are limited. The compound’s serotonergic receptor antagonism and dopaminergic receptor activity necessitate cautious use in patients susceptible to serotonin syndrome or dopaminergic-related adverse effects.
Yohimbine is globally recognized and approved for specific indications; it is also categorized among drugs used in erectile dysfunction, autonomic agents, and adrenergic antagonists. Notable usage contexts include both approved therapeutic applications and investigational or veterinary uses.
For API sourcing and quality, pharmaceutical-grade yohimbine should adhere to stringent purity criteria, free from plant-derived contaminants and consistent in enantiomeric composition due to its chiral centers. Reliable suppliers ensure compliance with pharmacopeial standards and thorough characterization using validated analytical methods. Monitoring cytochrome P450 substrate activity is important for formulation scientists assessing potential metabolic liabilities and drug interaction risks.
Identification & chemistry
| Generic name | Yohimbine |
|---|---|
| Molecule type | Small molecule |
| CAS | 146-48-5 |
| UNII | 2Y49VWD90Q |
| DrugBank ID | DB01392 |
Pharmacology
| Summary | Yohimbine acts primarily as a presynaptic alpha-2 adrenergic receptor antagonist, enhancing sympathetic neurotransmission by increasing norepinephrine release. It modulates multiple neurotransmitter systems, including dopaminergic, serotonergic, and cholinergic receptors, contributing to its effects on vascular and autonomic function. Therapeutically, yohimbine is utilized for its sympatholytic and mydriatic properties, with applications in treating erectile dysfunction linked to vascular, diabetic, or psychogenic factors. |
|---|---|
| Mechanism of action | Yohimbine is a pre-synaptic alpha 2-adrenergic blocking agent. The exact mechanism for its use in impotence has not been fully elucidated. However, yohimbine may exert its beneficial effect on erectile ability through blockade of central alpha 2-adrenergic receptors producing an increase in sympathetic drive secondary to an increase in norepinephrine release and in firing rate of cells in the brain noradrenergic nuclei. Yohimbine-mediated norepinephrine release at the level of the corporeal tissues may also be involved. In addition, beneficial effects may involve other neurotransmitters such as dopamine and serotonin and cholinergic receptors. |
| Pharmacodynamics | Yohimbine is an indolalkylamine alkaloid with chemical similarity to reserpine. Yohimbine blocks presynaptic alpha-2 adrenergic receptors. Its action on peripheral blood vessels resembles that of reserpine, though it is weaker and of short duration. Yohimbine's peripheral autonomic nervous system effect is to increase parasympathetic (cholinergic) and decrease sympathetic (adrenergic) activity. It is to be noted that in male sexual performance, erection is linked to cholinergic activity and to alpha-2 adrenergic blockade which may theoretically result in increased penile inflow, decreased penile outflow or both. Yohimbine exerts a stimulating action on the mood and may increase anxiety. Such actions have not been adequately studied or related to dosage although they appear to require high doses of the drug. Yohimbine has a mild anti-diuretic action, probably via stimulation of hypothalmic center and release of posterior pituitary hormone. Reportedly Yohimbine exerts no significant influence on cardiac stimulation and other effects mediated by (beta)-adrenergic receptors. Its effect on blood pressure, if any, would be to lower it; however, no adequate studies are at hand to quantitate this effect in terms of Yohimbine dosage. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-2A adrenergic receptor | Humans | antagonist |
| Alpha-2B adrenergic receptor | Humans | antagonist |
| Alpha-2C adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Rapidly absorbed following oral administration. Bioavailability is highly variable, ranging from 7 to 87% (mean 33%). |
|---|---|
| Half-life | Elimination half-life is approximately 36 minutes. |
| Metabolism | Yohimbine appears to undergo extensive metabolism in an organ of high flow such as the liver or kidney, however, the precise metabolic fate of yohimbine has not been fully determined. |
Formulation & handling
- Yohimbine is a small molecule alkaloid formulated exclusively for oral administration in tablet form.
- The compound exhibits moderate water solubility and a LogP of 2.1, indicating balanced lipophilicity favorable for oral absorption.
- Yohimbine can be taken with or without food, suggesting no significant food sensitivity or special administration conditions.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is entering a mature market phase in Canada following recent patent expiration. This status allows for increased generic competition and broader market availability. |
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| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Yohimbine involves multiple packagers primarily serving the Canadian market with various dosage forms. Several originator companies have developed branded products, such as Yocon Tablet and Yohimbine Hydrochloride tablets, with availability noted mainly in Canada, while limited presence is indicated in the US and EU markets. Given the established brand portfolio and the presence of many generic packagers, patent expirations have likely led to existing generic competition in the supply chain. |
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Yohimbine is a type of Alpha blockers
Alpha blockers are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the medical field. These medications are primarily utilized for their ability to block the alpha-adrenergic receptors, which are present in various parts of the body, including blood vessels and smooth muscle tissues. Alpha blockers work by preventing the receptor activation by the neurotransmitter norepinephrine, resulting in relaxation of the smooth muscles and dilation of the blood vessels.
These drugs find extensive applications in the treatment of several medical conditions. One of the most common applications of alpha blockers is in managing hypertension (high blood pressure) by promoting vasodilation, thereby reducing the resistance to blood flow. Additionally, they are employed in the treatment of benign prostatic hyperplasia (BPH) to relieve urinary symptoms by relaxing the smooth muscles in the prostate and bladder neck.
Some examples of popular alpha blockers include doxazosin, prazosin, and tamsulosin. Each of these medications may have specific indications and variations in their mechanism of action.
It is important to note that alpha blockers may cause certain side effects, such as dizziness, low blood pressure, and nasal congestion. Hence, it is crucial for healthcare professionals to carefully monitor patients receiving these medications and adjust the dosage accordingly.
In summary, alpha blockers are a vital subcategory of pharmaceutical APIs, playing a significant role in the management of conditions like hypertension and benign prostatic hyperplasia. Their mechanism of action involves blocking alpha-adrenergic receptors, leading to vasodilation and relaxation of smooth muscles. However, it is crucial to exercise caution while using these medications due to potential side effects.
Yohimbine (Alpha blockers), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Yohimbine API manufacturers & distributors
Compare qualified Yohimbine API suppliers worldwide. We currently have 3 companies offering Yohimbine API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aquatic Remedies Pvt Ltd | Producer | India | India | CoA | 35 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Vital Laboratories Pvt. L... | Producer | India | India | CoA, USDMF, WC | 22 products |
When sending a request, specify which Yohimbine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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