药品详细

Acebutolol(醋丁洛尔)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

醋丁洛尔

英文名

Acebutolol

分子式

C₁₈H₂₈N₂O₄

化学名

N-(3-acetyl-4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}phenyl)butanamide

分子量

Average: 336.4259
Monoisotopic: 336.204907394

CAS号

37517-30-9

ATC分类

C07A 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A cardioselective beta-adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action. [PubChem]

生产厂家

Amneal pharmaceutical
Mylan pharmaceuticals inc
Promius pharma llc
Watson laboratories inc

封装厂家

Alphapharm Party Ltd.
Amneal Pharmaceuticals
Bryant Ranch Prepack
Caremark LLC
Kaiser Foundation Hospital
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
Mylan
Patheon Inc.
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.
Professional Co.
Promius Pharma

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Acetanilides
Acetophenones and Derivatives

Substructures

Hydroxy Compounds
Aliphatic and Aryl Amines
Phenols and Derivatives
Amino Ketones
Ethers
Benzene and Derivatives
Acetanilides
Carboxylic Acids and Derivatives
Amino Alcohols
Aromatic compounds
Anisoles
Carboxamides and Derivatives
Benzoyl Derivatives
Alcohols and Polyols
Acetophenones and Derivatives
Phenyl Esters
Anilines
Ketones

适应症

药理

Indication

For the management of hypertension and ventricular premature beats in adults.

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.

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.

Absorption

Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In

Volume of distribution

Not Available

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.

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.

Clearance

Not Available

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.

Affected organisms

Humans and other mammals

Pathways

Pathway	Name	SMPDB ID
	Acebutolol Pathway	SMP00296

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	119-123 °C	PhysProp
water solubility	259 mg/L	Not Available
logP	1.71	HANSCH,C ET AL. (1995)
Caco2 permeability	-5.83	ADME Research, USCD

Predicted Properties

Property	Value	Source
water solubility	1.72e-01 g/l	ALOGPS
logP	1.43	ALOGPS
logP	1.53	ChemAxon
logS	-3.3	ALOGPS
pKa (strongest acidic)	13.91	ChemAxon
pKa (strongest basic)	9.57	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	5	ChemAxon
hydrogen donor count	3	ChemAxon
polar surface area	87.66	ChemAxon
rotatable bond count	10	ChemAxon
refractivity	94.87	ChemAxon
polarizability	38.51	ChemAxon

药物相互作用

Drug	Interaction
Acetohexamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Chlorpropamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Clonidine	Increased hypertension when clonidine stopped
Dihydroergotamine	Ischemia with risk of gangrene
Dihydroergotoxine	Ischemia with risk of gangrene
Disopyramide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Epinephrine	Hypertension, then bradycardia
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Fenoterol	Antagonism
Formoterol	Antagonism
Gliclazide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Glipizide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Glisoxepide	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Glyburide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Ibuprofen	Risk of inhibition of renal prostaglandins
Indacaterol	Beta-adrenergic antagonists, especially those that are not cardioselective, may interfere with the effect of indacaterol when administered concurrently. Beta-blockers may exacerbate bronchospasms in patients with COPD.
Indomethacin	Risk of inhibition of renal prostaglandins
Insulin Aspart	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Insulin Detemir	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Insulin Glargine	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Insulin Glulisine	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Insulin Lispro	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Isoproterenol	Antagonism
Lidocaine	The beta-blocker, acebutolol, may increase the effect and toxicity of lidocaine.
Methysergide	Ischemia with risk of gangrene
Orciprenaline	Antagonism
Pipobroman	Antagonism
Pirbuterol	Antagonism
Piroxicam	Risk of inhibition of renal prostaglandins
Prazosin	Risk of hypotension at the beginning of therapy
Repaglinide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Salmeterol	Antagonism
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Terbutaline	Antagonism
Tolazamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Tolbutamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Verapamil	Increased effect of both drugs

食物相互作用

Take without regard to meals; absorption rate and maximal concentration are slightly reduced but the extent of absorption is not affected.

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