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Phenoxybenzamine | CAS No: 59-96-1 | GMP-certified suppliers
A medication that manages malignant pheochromocytoma, benign prostatic hypertrophy, and malignant essential hypertension by providing sustained alpha-adrenergic blockade and vasodilation.
Therapeutic categories
Primary indications
- For the treatment of phaeochromocytoma (malignant), benign prostatic hypertrophy and malignant essential hypertension
Product Snapshot
- Phenoxybenzamine is an oral small molecule formulated as capsules
- It is primarily indicated for the treatment of malignant phaeochromocytoma, benign prostatic hypertrophy, and malignant essential hypertension
- The product is approved for marketing and use in the US regulatory market
Clinical Overview
Pharmacodynamically, phenoxybenzamine acts as a long-acting, irreversible alpha-receptor blocker. It induces a sustained "chemical sympathectomy" by inhibiting alpha-1 and alpha-2 adrenergic receptors primarily on vascular smooth muscle. This blockade results in relaxation of the muscle fibers lining blood vessels, promoting vasodilation, increased blood flow to the skin, mucosa, and abdominal viscera, and a reduction in both supine and erect blood pressures. It has no significant activity on the parasympathetic nervous system. In clinical use, phenoxybenzamine effectively controls hypertensive episodes and associated sweating in patients with pheochromocytoma. When tachycardia is pronounced, beta-adrenergic blockers may be co-administered to manage this compensatory response.
Regarding absorption, distribution, metabolism, and excretion (ADME), phenoxybenzamine is typically administered orally, exhibiting prolonged duration of action due to its covalent binding to alpha receptors. Detailed human pharmacokinetic data are limited, but its irreversible receptor binding underpins its extended pharmacodynamic effect.
Safety considerations include the risk of orthostatic hypotension due to peripheral vasodilation and reflex tachycardia. Other adverse effects may result from nonspecific alpha blockade. Careful dose titration and monitoring are necessary to avoid complications such as excessive hypotension. Phenoxybenzamine is approved globally but is reserved primarily for specific indications given the availability of more selective alpha blockers.
The drug is marketed under various international brand names and is utilized mainly in tertiary care settings for managing pheochromocytoma and resistant hypertension.
For procurement, sourcing of phenoxybenzamine API requires verification of purity and stability given its reactive nature and irreversible receptor binding profile. Compliance with pharmacopeial standards and thorough quality control testing, including residual solvent and impurity profiling, are critical to ensure consistent clinical performance.
Identification & chemistry
| Generic name | Phenoxybenzamine |
|---|---|
| Molecule type | Small molecule |
| CAS | 59-96-1 |
| UNII | 0TTZ664R7Z |
| DrugBank ID | DB00925 |
Pharmacology
| Summary | Phenoxybenzamine is a long-acting, non-selective alpha-adrenergic antagonist that irreversibly blocks alpha-1 and alpha-2 receptors, leading to vasodilation through smooth muscle relaxation. Its pharmacodynamic effects include sustained reduction of blood pressure and increased blood flow to peripheral tissues. It is primarily used to manage hypertension and symptoms associated with pheochromocytoma by producing chemical sympathectomy. |
|---|---|
| Mechanism of action | Phenoxybenzamine produces its therapeutic actions by blocking alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure. |
| Pharmacodynamics | Phenoxybenzamine is indicated for the control of episodes of hypertension and sweating that occur with a disease called pheochromocytoma. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phenoxybenzamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathectomy" by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Phenoxybenzamine works by blocking alpha receptors in certain parts of the body. Alpha receptors are present in the muscle that lines the walls of blood vessels. When the receptors are blocked by Phenoxybenzamine, the muscle relaxes and the blood vessels widen. This widening of the blood vessels results in a lowering of blood pressure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-1A adrenergic receptor | Humans | antagonist |
| Alpha-2A adrenergic receptor | Humans | antagonist |
| Alpha-2C adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Twenty to 30 percent of orally administered phenoxybenzamine appears to be absorbed in the active form. |
|---|---|
| Half-life | 24 hours |
Formulation & handling
- Phenoxybenzamine is a small molecule compound formulated for oral administration as capsules.
- Its low water solubility and high LogP suggest potential challenges with bioavailability and formulation excipients.
- Handling should consider stability under standard storage conditions without special sensitivity to food or injectable use.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has patent protection expiring in the US within the next 12 months, indicating an upcoming transition towards a more mature market with potential generic competition. Post-expiry, the API is expected to experience increased market accessibility and pricing adjustments. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Phenoxybenzamine is primarily manufactured by a limited number of originator companies, with Wellspring Pharmaceutical Corp noted as a key manufacturer. Branded products are available mainly in the US market, with multiple brand samples such as Dibenzyline and Phenoxybenzamine Hydrochloride. Patent expiration has allowed or suggests the presence of generic competition within the market. |
|---|
Safety
| Toxicity | Symptoms of overdose are largely the result of block of the sympathetic nervous system and of the circulating epinephrine. They may include postural hypotension resulting in dizziness or fainting, tachycardia, particularly postural, vomiting; lethargy, and shock. |
|---|
- Overdose may induce postural hypotension, tachycardia, vomiting, lethargy, and shock due to sympathetic nervous system blockade
- Handle with care to avoid exposure that could lead to systemic adrenergic effects
- Monitor for signs of cardiovascular instability during processing and formulation
Phenoxybenzamine 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.
Phenoxybenzamine (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.
Phenoxybenzamine API manufacturers & distributors
Compare qualified Phenoxybenzamine API suppliers worldwide. We currently have 2 companies offering Phenoxybenzamine 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 |
|---|---|---|---|---|---|
| Chemisch-pharmazeutisches... | Producer | Germany | Germany | CoA, EDMF/ASMF, FDA, GMP, MSDS | 7 products |
| NAVINTA | Producer | United States | Unknown | CoA, USDMF | 15 products |
When sending a request, specify which Phenoxybenzamine 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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