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Betaxolol | CAS No: 63659-18-7 | GMP-certified suppliers
A medication that manages hypertension and cardiac conditions by selectively blocking beta-1 adrenergic receptors to reduce blood pressure and cardiovascular risk.
Therapeutic categories
Primary indications
- For the management of hypertension
Product Snapshot
- Betaxolol is available in oral small molecule formulations such as tablets and ophthalmic solutions or drops
- It is primarily indicated for the management of hypertension
- The product is approved or investigational in key regulatory markets including the US and Canada
Clinical Overview
Pharmacodynamically, betaxolol competitively and selectively blocks beta-1 adrenergic receptors located chiefly in cardiac tissue. By preventing catecholamine binding at these receptors, it reduces heart rate, myocardial contractility, and cardiac output, thereby lowering systolic and diastolic blood pressure. The blockade also suppresses renin release from the kidneys, reducing vasoconstriction mediated via the renin-angiotensin system. Betaxolol lacks intrinsic sympathomimetic activity (ISA) and membrane stabilizing properties and is lipophilic, facilitating its tissue penetration.
The mechanism of action centers on antagonism of beta-1 receptors in the heart and vascular smooth muscle, leading to decreased myocardial oxygen consumption. While selective, betaxolol can also inhibit beta-2 adrenergic receptors at higher concentrations, potentially causing bronchospasm in susceptible patients. This highlights the importance of cautious use in individuals with reactive airway diseases.
Key pharmacokinetic and metabolism data note that betaxolol is a substrate for cytochrome P450 enzymes including CYP1A2 and CYP2D6; such metabolism considerations may impact drug-drug interaction profiles. Betaxolol’s safety profile necessitates monitoring for bradycardia, hypotension, and potential exacerbation of bronchospastic conditions. It is categorized under beta-1 selective blockers without partial agonist effects, serving as an important option in cardiovascular therapeutics.
Betaxolol is marketed under various reputable pharmaceutical brands globally and forms part of several antihypertensive formulations. For API sourcing, quality assurance includes verifying the absence of impurities and ensuring compliance with pharmacopeial standards. Analytical characterization should confirm beta-1 selectivity and potency, alongside batch-to-batch consistency, given the drug’s critical cardiovascular indications.
Identification & chemistry
| Generic name | Betaxolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 63659-18-7 |
| UNII | O0ZR1R6RZ2 |
| DrugBank ID | DB00195 |
Pharmacology
| Summary | Betaxolol is a beta-1 selective adrenergic antagonist that reduces cardiac workload by blocking beta-1 receptors in the heart and vascular smooth muscle, leading to decreased heart rate, cardiac output, and blood pressure. It also inhibits renin release, contributing to vasodilation and further blood pressure reduction. Betaxolol’s beta-1 selectivity minimizes bronchial effects associated with beta-2 receptor blockade. |
|---|---|
| Mechanism of action | Betaxolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Betaxolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm. |
| Pharmacodynamics | Betaxolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Betaxolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as betaxolol that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Betaxolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | antagonist |
| Beta-2 adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Absorption of an oral dose is complete. There is a small and consistent first-pass effect resulting in an absolute bioavailability of 89% ± 5% that is unaffected by the concomitant ingestion of food or alcohol. |
|---|---|
| Half-life | 14-22 hours |
| Protein binding | 50% |
| Metabolism | Primarily hepatic. Approximately 15% of the dose administered is excreted as unchanged drug, the remainder being metabolites whose contribution to the clinical effect is negligible. |
Formulation & handling
- Betaxolol is a small molecule beta-blocker available in oral tablet and ophthalmic solution/suspension formulations.
- It exhibits low water solubility and moderate lipophilicity (LogP 2.54), which should be considered during formulation development.
- No significant food interactions have been reported, simplifying oral dosing regimens.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's patents expired in the United States on January 30, 2014, indicating a mature market phase in both the US and Canada. Generic versions are likely available, reflecting established market presence. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Betaxolol includes multiple originator and generic companies, indicating a diverse supply base. Branded Betaxolol products are primarily available in the US and Canadian markets. Given the patent expiry date in 2014, generic competition is established and ongoing in these regions. |
|---|
Safety
| Toxicity | Oral LD<sub>50</sub>s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats. Predicted symptoms of overdose include bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia. |
|---|
- Handle with care to avoid exposure due to potential systemic toxicity at doses exceeding 350 mg/kg in animal models
- Use appropriate personal protective equipment to prevent inhalation or dermal absorption, as systemic effects may include cardiovascular and respiratory symptoms
- Ensure containment measures are in place to mitigate risks associated with accidental spills or inhalation
Betaxolol is a type of Beta blockers
Beta blockers are a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the medical field. These medications work by blocking the effects of adrenaline and other stress hormones on the beta receptors in the body. This action helps to reduce the heart rate and blood pressure, making them effective in treating various cardiovascular conditions.
Beta blockers are commonly prescribed to manage conditions such as hypertension (high blood pressure), angina (chest pain), arrhythmias (irregular heart rhythms), and certain types of heart failure. They can also be used in the prevention of migraines and to alleviate symptoms associated with anxiety disorders.
By targeting the beta receptors, these APIs provide a significant impact on the sympathetic nervous system, reducing the fight-or-flight response and promoting a state of calmness. This mechanism of action allows beta blockers to be effective in controlling heart-related conditions.
Some well-known beta blockers include metoprolol, propranolol, atenolol, and carvedilol. These APIs are available in various forms such as tablets, capsules, and injectables, allowing for flexibility in administration and dosage.
It is important to note that the use of beta blockers should be done under medical supervision due to potential side effects and contraindications. Common side effects may include fatigue, dizziness, cold hands and feet, and sexual dysfunction. Patients with certain conditions like asthma or diabetes may require cautious monitoring while using beta blockers.
In conclusion, beta blockers are a vital subcategory of pharmaceutical APIs used to treat cardiovascular conditions by blocking the effects of stress hormones. Their effectiveness and versatility make them a valuable tool in managing various medical conditions, enhancing the well-being of patients.
Betaxolol (Beta 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.
Betaxolol API manufacturers & distributors
Compare qualified Betaxolol API suppliers worldwide. We currently have 6 companies offering Betaxolol 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 |
|---|---|---|---|---|---|
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Indoco Remedies | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 19 products |
| Lusochimica | Producer | Italy | Italy | CoA, JDMF, USDMF | 23 products |
| Pioneer AGRO Ind. | Producer | India | India | CoA, GMP, WC | 12 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Watson Pharma | Producer | India | India | CoA, GMP, WC | 5 products |
When sending a request, specify which Betaxolol 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 Betaxolol 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.
