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Tamsulosin | CAS No: 106133-20-4 | GMP-certified suppliers
A medication that treats benign prostatic hyperplasia symptoms by improving urinary flow and is also used off-label for ureteral stones, prostatitis, and female voiding dysfunction.
Therapeutic categories
Primary indications
- Tamsulosin is indicated for the treatment of signs and symptoms of benign prostatic hyperplasia
- Tamsulosin is also used off label for the treatment of ureteral stones, prostatitis, and female voiding dysfunction
Product Snapshot
- Tamsulosin is formulated as oral capsules and tablets, including immediate, extended, and delayed-release forms
- It is primarily indicated for benign prostatic hyperplasia and used off-label for conditions such as ureteral stones and prostatitis
- Tamsulosin holds approved status in the US and Canadian pharmaceutical markets
Clinical Overview
Pharmacodynamically, tamsulosin exhibits a high degree of selectivity for alpha-1A receptors, binding these receptors 3.9 to 38 times more selectively than alpha-1B receptors and 3 to 20 times more than alpha-1D receptors. This receptor subtype specificity differentiates it from earlier non-selective alpha-1 blockers, reducing the risk of adverse effects related to vascular smooth muscle relaxation such as orthostatic hypotension.
The mechanism of action involves competitive antagonism at postsynaptic alpha-1 adrenoceptors, with approximately 70% of these receptors in the prostate identified as alpha-1A subtype. Inhibiting these receptors induces smooth muscle relaxation, alleviating urinary symptoms associated with prostatic enlargement. Off-label uses include facilitation of ureteral stone passage, management of prostatitis, and treatment of female voiding dysfunction.
Pharmacokinetic properties indicate that tamsulosin undergoes hepatic metabolism primarily via cytochrome P450 isoenzymes CYP2D6 and CYP3A4. It is eliminated mainly through renal excretion of metabolites. This metabolism profile necessitates consideration of potential drug-drug interactions, especially with CYP inhibitors or inducers.
Safety and toxicity profiles typically reflect its receptor selectivity, with fewer cardiovascular adverse events compared to less selective alpha-1 antagonists. Common adverse effects may include dizziness and ejaculatory dysfunction. Monitoring is advised in patients with severe hepatic impairment or history of orthostatic hypotension.
Tamsulosin was first approved by the FDA in 1997 and is an established agent in urologic pharmacopeia. Brand availability varies by region and formulation.
For API sourcing, strict adherence to pharmacopeial standards and impurity profiling is essential due to the compound’s chiral nature and sensitivity to manufacturing conditions. Suppliers should provide comprehensive Certificates of Analysis and evidence of compliance with relevant regulatory guidelines to ensure consistent quality for pharmaceutical development.
Identification & chemistry
| Generic name | Tamsulosin |
|---|---|
| Molecule type | Small molecule |
| CAS | 106133-20-4 |
| UNII | G3P28OML5I |
| DrugBank ID | DB00706 |
Pharmacology
| Summary | Tamsulosin is an alpha-1 adrenergic receptor antagonist with high selectivity for the alpha-1A and alpha-1D subtypes, primarily located in prostatic and bladder tissues. By blocking these receptors, it relaxes smooth muscle in the prostate and bladder neck, improving urinary flow and reducing bladder outlet obstruction. The drug’s receptor subtype specificity contributes to its targeted pharmacodynamic effects and a lower incidence of cardiovascular side effects. |
|---|---|
| Mechanism of action | Tamsulosin is a blocker of alpha-1A and alpha-1D adrenoceptors.[Label,A1078] About 70% of the alpha-1 adrenoceptors in the prostate are of the alpha-1A subtype. By blocking these adrenoceptors, smooth muscle in the prostate is relaxed and urinary flow is improved. The blocking of alpha-1D adrenoceptors relaxes the detrusor muscles of the bladder which prevents storage symptoms. The specificity of tamsulosin focuses the effects to the target area while minimizing effects in other areas. |
| Pharmacodynamics | Tamsulosin is an alpha adrenoceptor blocker with specificity for the alpha-1A and alpha-1D subtypes, which are more common in the prostate and submaxillary tissue. The final subtype, alpha-1B, are most common in the aorta and spleen. Tamsulosin binds to alpha-1A receptors 3.9-38 times more selectively than alpha-1B and 3-20 times more selectively than alpha-1D. This selectivity allows for a significant effect on urinary flow with a reduced incidence of adverse reactions like orthostatic hypotension. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-1A adrenergic receptor | Humans | antagonist |
| Alpha-1D adrenergic receptor | Humans | antagonist |
| Alpha-1B adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Oral tamsulosin is 90% absorbed in fasted patients. The area under the curve is 151-199ng/mL\*hr for a 0.4mg oral dose and 440-557ng/mL*hr for a 0.8mg oral dose. The maximum plasma concentration is 3.1-5.3ng/mL for a 0.4mg oral dose and 2.5-3.6ng/mL for a 0.8mg oral dose. Taking tamsulosin with food increases the time to maximum concentration from 4-5 hours to 6-7 hours but increases bioavailability by 30% and maximum plasma concentration by 40-70%. |
|---|---|
| Half-life | The half life in fasted patients is 14.9±3.9 hours. The elimination half life is 5-7 hours and the apparent half life is 9 to 13 hours in healthy subjects. In patients who require tamsulosin, the apparent half life is 14-15 hours. |
| Protein binding | Tamsulosin is 94%-99% protein bound, mostly to alpha-1-acid glycoprotein. |
| Metabolism | Tamsulosin is mostly metabolized in the liver by cytochrome P450 (CYP) 3A4 and 2D6, with some metabolism by other CYPs.[Label,A1078] CYP3A4 is responsible for the deethylation of tamsulosin to the M-1 metabolite and the oxidative deamination to the AM-1 metabolite, while CYP2D6 is responsible for the hydroxylation of tamsulosin to the M-3 metabolite and the demethylation of tamsulosin to the M-4 metabolite. In addition, tamsulosin can be hydroxylated at a different position by an unknown enzyme to form the M-2 metabolite. The M-1, M-2, M-3, and M-4 metabolites can be glucuronidated, and the M-1 and M-3 metabolites can undergo sulfate conjugation to form other metabolites before excretion. |
| Route of elimination | 97% of an orally administered does is recovered in studies, which 76% in the urine and 21% in the feces after 168 hours. 8.7% of the dose is excreted as unmetabolized tamsulosin.[Label,A1078] |
| Volume of distribution | 16L after intravenous administration. |
| Clearance | 2.88L/h. |
Formulation & handling
- Tamsulosin is a small molecule drug formulated exclusively for oral administration in various immediate and extended-release capsule and tablet forms.
- Due to its low water solubility and moderate lipophilicity (LogP 2.04), formulation strategies should focus on enhancing bioavailability.
- Administering after meals, consistently timed at 30 minutes postprandial, is recommended to minimize plasma level fluctuations and ensure dosing consistency.
Regulatory status
| Lifecycle | The API is marketed in the United States and Canada, with primary patent protections having expired between 2010 and 2015 in the US, and between 2013 and 2023 in Canada. As a result, the API is in a mature market phase with potential for generic competition in both regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Tamsulosin includes multiple originator and generic manufacturers with global operations, particularly prominent in the US and Canadian markets. Several branded products are available, including combination therapies, indicating a diverse branded presence. Patent expiry dates, mostly in the early 2010s with a key patent expiring in Canada by late 2023, suggest that generic competition is established and ongoing in primary markets. |
|---|
Safety
| Toxicity | In the event of overdose, patients may experience hypotension and should lie down in a supine position to maintain blood pressure and heart rate. If further measures are required intravenous fluids should be considered. If further progression is required, vasopressors may be used and renal function should be monitored. Dialysis is unlikely to assist in treating overdose because tamsulosin is extensively protein bound. The oral LD50 in rats is 650mg/kg.[MSDS] Tamsulosin is not indicated for use in women and no studies have been performed in pregnancy, though animal studies have not shown fetal harm. Tamsulosin is excreted in the milk of rats but there is no available data on what the effect of this tamsulosin exposure may be. Animal studies have shown male and female rat fertility is affected by tamsulosin due to impairment of ejaculation and fertilization. In men, tamsulosin is associated with abnormal ejaculation. Tamsulosin is not mutagenic but may be carcinogenic at levels above the maximum recommended human dose. Female rats experience a slight increase in the rates of mammary gland fibroadenomas and adenocarcinomas. |
|---|
- Tamsulosin exhibits low acute toxicity with an oral LD50 in rats of 650 mg/kg
- Overdose may induce hypotension requiring cardiovascular monitoring
- The compound is extensively protein bound, limiting removal by dialysis in cases of overdose
Tamsulosin 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.
Tamsulosin (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.
Tamsulosin API manufacturers & distributors
Compare qualified Tamsulosin API suppliers worldwide. We currently have 27 companies offering Tamsulosin API, with manufacturing taking place in 10 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 |
|---|---|---|---|---|---|
| ALP PHARM | Producer | China | China | CoA, USDMF | 33 products |
| Aquatic Remedies Pvt Ltd | Producer | India | India | CoA | 35 products |
| Astellas Pharma | Producer | Japan | Japan | CEP, CoA, GMP | 3 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Bioindustria | Producer | Italy | Italy | CEP, CoA, FDA, GMP | 12 products |
| Chemo Iberica | Producer | Spain | Spain | CoA, USDMF | 12 products |
| Chinoin | Producer | Hungary | Unknown | CoA, JDMF | 21 products |
| Cipla | Producer | India | Unknown | CEP, CoA | 164 products |
| Curia | Producer | United States | Spain | CoA, EDMF/ASMF, GMP, MSDS | 106 products |
| Divis Labs. | Producer | India | India | CoA, FDA, GMP, ISO9001, Other, USDMF, WC | 47 products |
| Dongbang FTL | Producer | South Korea | South Korea | CoA, JDMF | 13 products |
| Fermion | Producer | Finland | Finland | BSE/TSE, CoA, GDP, GMP, JDMF, Other, MSDS, USDMF | 29 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hamari Chemicals | Producer | Japan | Japan | CoA, JDMF | 12 products |
| Lek Pharma | Producer | Slovenia | India | CoA, USDMF | 32 products |
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, USDMF | 757 products |
| Sun Pharma | Producer | India | India | CEP, CoA, USDMF, WC | 219 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Tooba Pharmaceuticals Pri... | Producer | India | India | BSE/TSE, CoA, FDA, GMP, HALAL, ISO14001, ISO9001, MSDS, WHO-GMP | 7 products |
| Unichem Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 62 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 133 products |
| Yonsung Fine Chem. | Producer | South Korea | South Korea | CoA, JDMF | 13 products |
| Zentiva K.S. | Producer | Czech Republic | Czech Republic | CEP, CoA, GMP | 1 products |
| Zhejiang Jinhua Conba | Producer | China | China | CoA, USDMF | 6 products |
When sending a request, specify which Tamsulosin 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.).
Use the list above to find high-quality Tamsulosin API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
