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Acebutolol | CAS No: 37517-30-9 | GMP-certified suppliers
A medication that manages hypertension and ventricular premature beats in adults by selectively reducing cardiac beta-1 adrenergic activity to support cardiovascular health.
Therapeutic categories
Primary indications
- For the management of hypertension and ventricular premature beats in adults
Product Snapshot
- Acebutolol is available as oral tablets and capsules as well as an intravenous injection solution
- It is primarily used for the management of hypertension and ventricular premature beats in adults
- The product is approved in key regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, acebutolol exhibits selective antagonism at beta-1 adrenergic receptors located predominantly in cardiac tissue. By blocking these receptors, acebutolol reduces the effects of endogenous catecholamines such as epinephrine, leading to decreased heart rate, myocardial contractility, and consequently lowered blood pressure. Its mild intrinsic sympathomimetic activity (ISA) differentiates it from nonselective beta-blockers, resulting in reduced antagonism at peripheral beta-2 receptors, which are mainly found in bronchial tissues. This selectivity translates into a lower risk of bronchoconstriction compared with nonselective agents like propranolol, although the risk is somewhat higher than with other selective beta-blockers such as atenolol.
The mechanism of action further involves inhibition of renin release from the kidneys, attenuating the renin-angiotensin-aldosterone system (RAAS), which contributes to vasoconstriction and elevated blood pressure. Acebutolol also exhibits stabilizing and quinidine-like effects on cardiac rhythm, which can be beneficial in arrhythmia management.
Key ADME characteristics include hepatic metabolism, with acebutolol acting both as a substrate and inhibitor of cytochrome P450 CYP2D6 enzymes. It is also a substrate for P-glycoprotein. Such interactions necessitate consideration during co-administration with drugs metabolized via these pathways. The pharmacokinetic profile supports once or twice daily dosing, but specific parameters such as bioavailability or half-life are product-dependent and should be confirmed during development.
Safety and toxicity considerations include potential bradycardia, hypotension, and in some cases, exacerbation of bronchospastic conditions due to beta-1 selectivity not being absolute. Careful patient monitoring is advised, especially in populations with respiratory comorbidities or conduction abnormalities. Acebutolol may also prolong the QT interval, necessitating caution in patients with predisposing conditions.
Notable brand names for acebutolol include Sectral, though usage may vary regionally.
From an API sourcing perspective, quality aspects critical for acebutolol include stringent control of polymorphic form and purity to ensure batch-to-batch consistency. Due to its involvement with CYP2D6 metabolism, impurities or degradation products affecting metabolic pathways require thorough evaluation. Suppliers should provide comprehensive documentation including certificates of analysis confirming compliance with pharmacopeial specifications and material safety data. Given global regulatory requirements, sourcing from manufacturers adhering to Good Manufacturing Practices (GMP) and supported by validated analytical methods is essential to ensure quality and supply chain reliability.
Identification & chemistry
| Generic name | Acebutolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 37517-30-9 |
| UNII | 67P356D8GH |
| DrugBank ID | DB01193 |
Pharmacology
| Summary | Acebutolol is a selective beta-1 adrenergic receptor antagonist with mild intrinsic sympathomimetic activity, primarily used to reduce heart rate and blood pressure by blocking beta-1 receptors in cardiac tissue. It also inhibits renin release from the kidneys, contributing to vascular relaxation. Compared to nonselective beta blockers, acebutolol has reduced beta-2 receptor antagonism, resulting in lower bronchoconstrictive effects. |
|---|---|
| Mechanism of action | Acebutolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Acebutolol blocks these receptors, lowering the heart rate and blood pressure. This drug then has the reverse effect of epinephrine. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. |
| Pharmacodynamics | Acebutolol is a cardioselective, beta-adrenoreceptor blocking agent, which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range. In general, beta-blockers reduce the work the heart has to do and allow it to beat more regularly. Acebutolol has less antagonistic effects on peripheral vascular ß2-receptors at rest and after epinephrine stimulation than nonselective beta-antagonists. Low doses of acebutolol produce less evidence of bronchoconstriction than nonselective agents like propranolol but more than atenolol. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | partial agonist |
| Beta-2 adrenergic receptor | Humans | partial agonist |
ADME / PK
| Absorption | Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. |
|---|---|
| Half-life | The plasma elimination half-life is approximately 3 to 4 hours. The half-life of its metabolite, diacetolol, is 8 to 13 hours. |
| Protein binding | 26% |
| Metabolism | Subject to extensive first-pass hepatic biotransformation (primarily to diacetolol). |
| Route of elimination | Elimination via renal excretion is approximately 30% to 40% and by non-renal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall. |
Formulation & handling
- Acebutolol is a small molecule API suitable for oral and intravenous formulations, available as capsules, tablets, and injectable solutions.
- The compound exhibits moderate water solubility and lipophilicity (LogP 1.53), supporting formulation in diverse dosage forms.
- Food intake may reduce absorption rate and peak plasma concentration, but does not necessitate strict administration timing relative to meals.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has passed patent expiry in both the US and Canada, indicating a mature market with generic competition. Regulatory approval pathways in these regions support ongoing availability through multiple manufacturers. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Acebutolol includes multiple packagers primarily serving the US and Canadian markets. Several originator companies have contributed to branded products, which have established presence mainly in North America. The availability of multiple branded formulations and the presence of numerous packagers suggest that patent expirations have allowed for existing generic competition. |
|---|
Safety
| Toxicity | Symptoms of overdose include extreme bradycardia, advanced atrioventricular block, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm, and hypoglycemia. |
|---|
- Overdose may result in severe cardiovascular effects including extreme bradycardia, atrioventricular conduction abnormalities, and hypotension
- Neurological symptoms such as seizures have been observed in toxicity cases
- Use caution in individuals with compromised respiratory function due to risk of bronchospasm
Acebutolol 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.
Acebutolol (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.
Acebutolol API manufacturers & distributors
Compare qualified Acebutolol API suppliers worldwide. We currently have 3 companies offering Acebutolol 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 |
|---|---|---|---|---|---|
| Cambrex | Producer | Italy | Unknown | CoA, USDMF | 104 products |
| Hikal | Producer | India | India | CoA, GMP, WC | 26 products |
| Moehs | Producer | Spain | Spain | CoA, USDMF | 50 products |
When sending a request, specify which Acebutolol 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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