QuickView for Acebutolol (compound)

Summary
General Info

PubChem

PubChem Compound 155082

Name:	Acebutolol
PubChem Compound ID:	155082
Description:	A cardioselective beta-1 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.
Molecular formula:	C₁₈H₂₈N₂O₄
Molecular weight:	336.426 g/mol
Synonyms:	Butanamide, N-(3-acetyl-4-((2R)-2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)-; 68107-81-3

DrugBank

Identification

Name:	Acebutolol
Name (isomeric):	DB01193
Drug Type:	small molecule
Description:	A cardioselective beta-1 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.
Synonyms:	Acebutololo; Acetobutolol; Acebutolol HCL; dl-Acebutolol; Acebutolol Hydrochloride
Brand:	Sectral, Monitan, Prent, Neptal
Category:	Adrenergic beta-Antagonists, Anti-Arrhythmia Agents, Antihypertensive Agents
CAS number:	37517-30-9

Pharmacology

Indication:	For the management of hypertension and ventricular premature beats in adults.
Pharmacology:	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-re... show more » 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. show less «
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 pre... show more » 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. show less «
Absorption:	Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In
Protein binding:	26%
Biotransformation:	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.
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

Interactions

Food interaction:

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

Drug interaction:

Ibuprofen	Risk of inhibition of renal prostaglandins
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Epinephrine	Hypertension, then bradycardia
Insulin Glargine	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.

Ibuprofen	Risk of inhibition of renal prostaglandins
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Epinephrine	Hypertension, then bradycardia
Insulin Glargine	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Lidocaine	The beta-blocker, acebutolol, may increase the effect and toxicity of lidocaine.
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Clonidine	Increased hypertension when clonidine stopped
Insulin Aspart	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Glipizide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Insulin Glulisine	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Glisoxepide	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Insulin Detemir	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Repaglinide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Acetohexamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Salmeterol	Antagonism
Insulin	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Chlorpropamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Terbutaline	Antagonism
Tolazamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Methysergide	Ischemia with risk of gangrene
Glyburide	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.
Gliclazide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Fenoterol	Antagonism
Disopyramide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Pipobroman	Antagonism
Orciprenaline	Antagonism
Formoterol	Antagonism
Dihydroergotamine	Ischemia with risk of gangrene
Dihydroergotoxine	Ischemia with risk of gangrene
Isoproterenol	Antagonism
Verapamil	Increased effect of both drugs
Pirbuterol	Antagonism
Tolbutamide	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Prazosin	Risk of hypotension at the beginning of therapy
Insulin Lispro	The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
Piroxicam	Risk of inhibition of renal prostaglandins
Indomethacin	Risk of inhibition of renal prostaglandins

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Targets

Beta-1 adrenergic receptor

Beta-2 adrenergic receptor

Enzymes

Cytochrome P450 2D6

Transporters

Solute carrier family 22 member 1

Multidrug resistance protein 1