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Alfuzosin | CAS No: 81403-80-7 | GMP-certified suppliers
A medication that alleviates lower urinary tract symptoms associated with benign prostatic hyperplasia by improving urine flow and reducing prostate gland enlargement.
Therapeutic categories
Primary indications
- Alfuzosin is used to treat the signs and symptoms of benign prostatic hyperplasia (BPH)
Product Snapshot
- Alfuzosin is available as an oral extended-release tablet formulation
- It is primarily used for the management of benign prostatic hyperplasia (BPH) symptoms
- Alfuzosin is approved and marketed in key regulatory regions including the United States and Canada
Clinical Overview
Pharmacologically, alfuzosin belongs to the quinazolinamine class, defined by a heterocyclic aromatic quinazoline core with amine substitutions. It exerts its therapeutic effect by selectively binding to alpha-1 adrenergic receptors located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. The receptor blockade reduces smooth muscle contraction in these tissues, thereby increasing urine flow and alleviating symptoms associated with BPH.
In addition to its effects on the lower urinary tract, alfuzosin antagonizes the vasoconstrictive action of catecholamines such as epinephrine and norepinephrine on peripheral vasculature. This vasodilation can result in postural hypotension and syncope, necessitating cautious use in patients concurrently treated with nitrates or antihypertensive agents and those with a history of decreased blood pressure related to similar medications.
Alfuzosin is metabolized primarily via cytochrome P450 CYP3A4 isoenzymes and serves as a substrate for P-glycoprotein, potentially influencing its pharmacokinetic profile and drug-drug interaction risks. The drug has been associated with potential QTc interval prolongation, warranting consideration in patients with risk factors for cardiac arrhythmias.
First approved by the U.S. Food and Drug Administration in 2003, alfuzosin is marketed globally under multiple pharmaceutical brands. Its use is well established in clinical guidelines for managing BPH symptoms.
From an API procurement and quality standpoint, suppliers must ensure compliance with Good Manufacturing Practices (GMP) and provide detailed certificates of analysis confirming identity, purity, and absence of relevant impurities. Given the potential for cytochrome P450-mediated interactions, batch consistency and impurity profiling are critical for maintaining product safety and efficacy.
Identification & chemistry
| Generic name | Alfuzosin |
|---|---|
| Molecule type | Small molecule |
| CAS | 81403-80-7 |
| UNII | 90347YTW5F |
| DrugBank ID | DB00346 |
Pharmacology
| Summary | Alfuzosin is an alpha-1 adrenergic receptor antagonist that selectively targets receptors in the lower urinary tract, including the prostate and bladder neck. Its inhibition of these receptors results in smooth muscle relaxation, improving urine flow and alleviating symptoms associated with benign prostatic hyperplasia (BPH). Additionally, alfuzosin's blockade of peripheral alpha-1 receptors can induce vasodilation, impacting vascular tone. |
|---|---|
| Mechanism of action | Alpha(1)-adrenoreceptors are found in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra; their activation may lead to contraction of smooth muscle and urinary symptoms in patients with BPH. Alfuzosin selectively binds to and inhibits alpha(1)-adrenergic receptors in the lower urinary tract. This leads to the relaxation of smooth muscle in both the prostate and bladder neck, resulting in the improvement in urine flow and a reduction of urinary symptoms. |
| Pharmacodynamics | By selectively inhibiting alpha adrenergic receptors in the lower urinary tract, alfuzosin causes smooth muscle relaxation in the bladder neck and prostate, improving urine flow, thereby reducing BPH symptoms. Additionally, alfuzosin reduces the vasoconstrictor effect of catecholamines (epinephrine and norepinephrine), leading to peripheral vasodilation. This leads to a risk of postural hypotension/syncope, and prescribing information warns that caution should be exercised in patients who take nitrates, antihypertensives, or have experienced decreased blood pressure after using other medications. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-1 adrenergic receptors | Humans | antagonist |
| Alpha-1A adrenergic receptor | Humans | antagonist |
| Alpha-1B adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Alfuzosin is readily absorbed in the gastrointestinal tract and the absolute bioavailability under fed conditions is 49%. In patients over 75 years of age, alfuzosin is absorbed more rapidly and peak plasma levels are higher. One source mentions a bioavailability of 64%. After multiple doses under fed conditions, Cmax is achieved in 8 hours. Cmax and AUC0-24 values are about 13.6 ng/mL and 194 ng·h/mL, respectively. Steady-state plasma concentrations are achieved after the second dose and are 1.2 to 1.6 times higher than after a single dose. With the extended-release formulation, alfuzosin release is sustained over 20 hours with a rate of dissolution ranging between 2 and 12 hours. |
|---|---|
| Half-life | The apparent elimination half-life of alfuzosin after oral administration is about 10 hours. The terminal half-life is 3-5 hours. |
| Protein binding | The protein biding of alfuzosin is moderate and ranges from 82% to 90%. Alfuzosin is 68.2% bound to human serum albumin and 52.5% bound to human serum alpha-glycoprotein. |
| Metabolism | Alfuzosin undergoes extensive hepatic metabolism; only 11% of the administered dose is detected unchanged in the urine. Alfuzosin is metabolism occurs via three metabolic pathways: oxidation, O-demethylations, and N-dealkylation. Metabolites of alfuzosin are not pharmacologically active and CYP3A4 is main hepatic cytochrome enzyme responsible for its metabolism. |
| Route of elimination | It is partially metabolised and excreted mainly in the bile and faeces. Following oral administration of a radiolabeled alfuzosin solution, the detection of radioactivity after one week was 69% in the feces and 24% in the urine. |
| Volume of distribution | The volume of distribution of alfuzosin after intravenous administration in healthy volunteers is about 3.2 L/kg. Alfuzosin distributes heavily to the tissues of the prostate. |
| Clearance | Exercise caution if renal clearance is < 30 mL/min. The clearance of alfuzosin is increased in renal insufficiency (with or without dialysis), due to an increase in the free fraction. |
Formulation & handling
- Alfuzosin is a small molecule oral API primarily formulated as extended-release tablets.
- The API requires administration post-meal to optimize absorption and reduce variability associated with food.
- Formulation stability considerations focus on maintaining solid-state integrity with moderate water solubility and a logP indicating balanced hydrophilicity and lipophilicity.
Regulatory status
| Lifecycle | The API's patent protection in the United States expired in 2018, with Canadian patent protection ending in 2017, indicating that the product is in a mature market phase in both regions. Generic competition is likely established in the US and Canadian markets. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Alfuzosin is dominated by a single originator company with multiple associated packagers primarily serving the US and Canadian markets. Branded products are present mainly in North America, reflecting a regional focus. Patent expiry dates indicate that generic competition is likely established or imminent in these territories. |
|---|
Safety
| Toxicity | The oral LD50 of alfuzosin is 2300 mg/kg in male mice and 1950 mg/kg in female mice. An overdose of alfuzosin can cause hypotension. Cardiovascular support should be initiated immediately. The patient should be kept in the supine position to aid in restoring pressure and managing heart rate. Fluid resuscitation should also be considered in severe cases; sometimes, vasopressors are required. Renal function should be monitored frequently. Dialysis may not be of benefit to alfuzosin protein binding of up to 90%. |
|---|
- Alfuzosin exhibits moderate acute oral toxicity with an LD50 of approximately 2000–2300 mg/kg in mice
- Overexposure may result in hypotension, necessitating cardiovascular monitoring and support during handling incidents
- High plasma protein binding (~90%) limits the efficacy of dialysis in cases of significant exposure
Alfuzosin 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.
Alfuzosin (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.
Alfuzosin API manufacturers & distributors
Compare qualified Alfuzosin API suppliers worldwide. We currently have 7 companies offering Alfuzosin API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, GMP, WC | 164 products |
| Farmak | Producer | Czech Republic | Czech Republic | CEP, CoA, FDA, GMP, USDMF | 19 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| MSN Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 119 products |
| Sanofi | Producer | France | Unknown | CoA, USDMF | 93 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
| Unichem Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 62 products |
When sending a request, specify which Alfuzosin 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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