Acebutolol

Acebutolol (trade names Sectral, Prent) is a beta blocker for the treatment of hypertension and arrhythmias.

Pharmacology:

Acebutolol is a cardioselective beta blocker with ISA (intrinsic sympathomimetic activity; see article on pindolol). It is therefore more suitable than non cardioselective beta blockers, if a patient with asthma or chronic obstructive pulmonary disease (COPD) needs treatment with a beta blocker. (For these reasons, it may be a beta-blocker of choice in inclusion in Polypill strategies). In doses lower than 800mg daily its constricting effects on the bronchial system and smooth muscle vessels are only 10% to 30% of those observed under propranolol treatment, but there is experimental evidence that the cardioselective properties diminish at doses of 800mg/day or more.

The drug has lipophilic properties, and therefore crosses the blood–brain barrier. Acebutolol has no negative impact on serum lipids (cholesterol and triglycerides). No HDL decrease has been observed. In this regard, it is unlike many other beta blockers which have this unfavourable property.

The drug works in hypertensive patients with high, normal, or low renin plasma concentrations, although acebutolol may be more efficient in patients with high or normal renin plasma concentrations. In clinically relevant concentrations, a membrane-stabilizing effect does not appear to play an important role.

Pharmacokinetics:

Acebutolol is well absorbed from the GI tract, but undergoes substantial first-pass-metabolization, leading to a bioavailability of only 35% to 50%. Peak plasma levels of acebutolol are reached within 2 to 2.5 hours after oral dosing. Peak levels of the main active metabolite, diacetolol, are reached after 4 hours. Acebutolol has a half-life of 3 to 4 hours, and diacetolol a half-life of 8 to 13 hours.

Acebutolol undergoes extensive hepatic metabolization resulting in the desbutyl amine acetolol which is readily converted into diacetolol. Diacetolol is as active as acebutolol (equipotency) and appears to have the same pharmacologic profile. Geriatric patients tend to have higher peak plasma levels of both acebutolol and diacetolol and a slightly prolonged excretion. Excretion is substantially prolonged in patients with renal impairment, and so a dose reduction may be needed. Liver cirrhosis does not seem to alter the pharmacokinetic profile of the parent drug and metabolite.

Acebutolol Basic information:

Product Name: Acebutolol

Synonyms: (.+/-.)-3'-Acetyl-4'-[2-hydroxy-3-(1-methylethylamino)propoxy]butyranilide;(.+/-.)-3'-Acetyl-4'-[2-hydroxy-3-(isopropylamino)propoxy]butyranilide;(.+/-.)-N-(3-Acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)butanamide;1-(2-Acetyl-4-n-butyramidophenoxy)-2-hydroxy-3-isopropylaminopropane;3'-Acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide;5'-Butyramido-2'-(2-hydroxy-3-isopropylaminopropoxy)acetophenone;Butanamide, N-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-, (.+/-.)-;dl-Acebutolol

CAS: 37517-30-9

MF: C18H28N2O4

MW: 336.43

EINECS: 253-539-0

Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals;Adrenoceptor

Mol File: 37517-30-9.mol

Acebutolol Structure

Acebutolol Chemical Properties

mp 119-123°C

storage temp. -20°C Freezer

Water Solubility 259 mg/L

CAS DataBase Reference 37517-30-9(CAS DataBase Reference)

NIST Chemistry Reference Acebutolol(37517-30-9)

Acebutolol Usage And Synthesis

Chemical Properties Crystalline Solid

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

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

Specification:

Test  Item	Analysis  Specification	Result
Description	White crystalline powder	Conforms
Melting range	129°C~132°C	130.8°C-131°C
Loss on drying	≤0.5%	0.20 %
Specific rotation	-58°~-62°(C=1,in CH3OH)	-61.05°
Sulphated ash	≤0.1%	0.08 %
Heavy metals	≤10ppm	Conforms
Chlorides	≤0.02%	Conforms
Sulfates	≤0.02%	Conforms
Fluorine	14.7%~17.9%	15.2%
Residual solvent	Methanol ≤0.2% Isopropanol ≤0.2% Ethyl acetate≤0.2% Chloroform ≤0.2%	0.0% 0.0% 0.0% 0.0%
Related substances (HPLC)	Single impurity ≤0.2% Total impurities ≤0.5%	0.05% 0.08%
Assay	≥99.5%	99.92%
Conclusion	Accordance with the reference

Package & Storage :

ckaging Detail	0.5kgs/Al-Bottle 1.0kgs/Al- Bottle 2.0kgs/Al- Bottle 5.0 kgs/Al-Bottle 25.0 kgs/drum or upon customers' request.
Storage	Store in a well-closed container away from moisture
Shelf Life	2 years if sealed and store away from direct sun light.
Delivery Detail	within 3 days after get the payment

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Notice: This product is only suitable for laboratory use, or the use of animals. It can not be used directly on the human body