Acebutolol
Acebutolol is a moderately ß1-selective adrenoceptor antagonist with intrinsic sympathomimetic activity, first synthesized in 1967. Acebutolol is prepared by chemical synthesis and the racemate is used clinically. It lowers the blood pressure and slows the heart rate. Acebutolol is available for both oral and intravenous use and as an oral combination product with hydrochlorothiazide. Drugs that blocks the ß1 receptor have been developed to eliminate the unwanted bronchoconstrictor effects (ß2) of propranolol seen among the asthmatic patients. It antagonize ß1 receptors at doses 50 to 100 times less than those required to block ß2 receptors. This cardioselectivty is more pronounced at low doses and is lost at high doses.
Primary Characteristics
Acebutolol is also known as Acebutolol Hydrochloride.
It is of Synthetic origin and belongs to Propylaminopropane.
It belongs to Beta-1 adrenergic antagonist pharmacological group on the basis of mechanism of action and also classified in Antihypertensive Agents pharmacological group.
Molecular Weight: 372.9 · pKa: 9.4 · Solubility in Water: very high · Solubility in Alcohol: low · Non-proprietary name: Acebutolol.
Pharmacokinetics
Absorption: Acebutolol has an oral bioavailability is 25% (±25%), pre-systemic (first-pass) metabolism accounts for 40% (±10%).
Distribution: Acebutolol has a volume of distribution is 1-2 l/kg. plasma protein binding is 11-19%.
Elimination: it is metabolised via Liver & Gut, plasma half-life is 5-9 hr, renal excretion is 12-14%.
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Indications
Acebutolol is primarily indicated in conditions like Angina, Angina pectoris, Cardiac arrhythmia, Hypertension, To prevent recurrence of neural tube defect.
Acebutolol is also indicated for secondary conditions like Hypertension in pregnancy, Hypertrophic cardiomyopathy, Migraine, Schizophrenia, Thyrotoxicosis.
Contraindications
Acebutolol is contraindicated in conditions like Cardiogenic shock, Bronchospasm, Bradycardia.
Dosage
Acebutolol's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 400 – 400 mg | — | Every 24h | PO | For Angina pectoris. |
| 200 mg | 200 mg | Every 12h | PO | For Angina pectoris. |
| 300 mg | 300 mg | Every 8h | PO | For Angina pectoris. Maximum 1200mg/day in divided doses. |
| 300 mg | 300 mg | Every 12h | PO | For Hypertension |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Acebutolol produces potentially life-threatening effects which include Severe bradycardia, Severe bronchospasm, Severe hypoglycemia, Severe angina on withdrawal, Severe MI on withdrawal. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Acebutolol are Bradycardia, Hypotension, Death .
Acebutolol is known to cause more or less tolerable side effects which are usually transient. These include Dizziness, Tiredness .
Warnings / Precautions
Interference in Pathology
Acebutolol may interfere in the diagnosis of Estimation of Urinary Catecholamines , Zimmerman method for assaying 17-kotasteroids .
Available Brands
None recorded.
Storage Conditions
Drug Classification
- 1.12.3.1 — Beta blocking agents