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Acebutolol

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Acebutolol Basic information

Product Name:
Acebutolol
CAS:
37517-30-9
MF:
C18H28N2O4
MW:
336.43
EINECS:
253-539-0
Mol File:
37517-30-9.mol
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Acebutolol Chemical Properties

Melting point:
119-123°C
Boiling point:
472.9°C (rough estimate)
Density 
1.1748 (rough estimate)
refractive index 
1.5700 (estimate)
storage temp. 
-20°C Freezer
pka
pKa 9.40 (Uncertain)
Water Solubility 
259 mg/L
CAS DataBase Reference
37517-30-9(CAS DataBase Reference)
NIST Chemistry Reference
Acebutolol(37517-30-9)
EPA Substance Registry System
Butanamide, N-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]- (37517-30-9)
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Acebutolol Usage And Synthesis

Chemical Properties

Crystalline Solid

Uses

Cardioselective ?adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic (class II)

Uses

Cardioselective β-adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic (class II).

Definition

ChEBI: An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.

brand name

Sectral (Dr. Reddy’s).

General Description

Acebutolol is one of the very few β-blockers whosemetabolite plays a significant role in its pharmacological actions.This drug is absorbed well from the gastrointestinaltract, but it undergoes extensive first-pass metabolic conversionto diacetolol by hydrolytic conversion of the amidegroup to the amine, followed by acetylation of the amine. After oral administration, plasma levels of diacetololare higher than those of acebutolol. Diacetolol is also aselective β1-blocker with partial agonistic activity; it has littlemembrane-stabilizing activity. It has a longer half-life (8–12hours) than the parent drug and is excreted by the kidneys.

Clinical Use

Acebutolol (Sectral) is a cardioselective 1-adrenoceptor blocking agent that also has some minor membrane stabilizing effects on the action potential. Acebutolol is effective in the management of the patient with essential hypertension, angina pectoris, and ventricular arrhythmias. Antiarrhythmic effects are observed with the patient both at rest and taking exercise.

Side effects

Adverse effects include bradycardia, gastrointestinal upset, dizziness, and headache.

Metabolism

About half of an orally administered dose of acebutolol (Sectral) is absorbed. Approximately 25% of the drug is bound to plasma proteins, and its plasma halflife is about 4 hours.Metabolism of acebutolol produces a metabolite with -blocking activity whose half-life is 10 hours.

Precautions

Acebutolol should not be administered in cardiogenic shock, uncontrolled heart failure, or severe bradycardia or to patients with known hypersensitivity to the drug.

Acebutolol Preparation Products And Raw materials

Raw materials

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AcebutololSupplierMore

J & K SCIENTIFIC LTD.
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010-82848833- ;010-82848833-
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LGM Pharma
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Syntechem Co.,Ltd
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China Langchem Inc.
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0086-21-58956006,021-38701807;021-58950017
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Shanghai Kewel Chemical Co., Ltd.
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021-64609169-
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kewelchemexp@yahoo.com
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