Esmolol detailed information

Esmolol detailed information

Clinical data
Pregnancy category	AU: C US: C (Risk not ruled out)
Routes of administration	iv
ATC code	C07AB09 (WHO)
Pharmacokinetic data
Bioavailability	-
Protein binding	60%
Metabolism	Erythrocytic
Elimination half-life	9 minutes
Excretion	Renal
Identifiers
IUPAC name methyl 3-[4-(2-hydroxy-3-propan -2-ylamino-propoxy)phenyl]propanoate
CAS Number	103598-03-4
PubChem CID	59768
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C16H25NO4>
Molar mass	295.374 g/mol

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Overview

Esmolol (trade name Brevibloc) is a cardioselective beta₁ receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic parasympathomimetic or membrane stabilising activity at therapeutic dosages.

Esmolol decreases the force and rate of heart contractions by blocking beta-adrenergic receptors of the sympathetic nervous system, which are found in the heart, lungs and other organs of the body. Esmolol prevents the action of two naturally occurring substances: epinephrine and norepinephrine.

Dosing

Esmolol is given by slow intravenous injection. It is commonly used in patients during surgery to prevent or treat tachycardia, and is also used in treatment of acute supraventricular tachycardia.

Metabolism

Esmolol is rapidly hydrolysed by the esterases in the cytosol of red blood cells. Plasma cholinesterases and red cell membrane acetylcholinesterase do not have any action. This metabolism results in the formation of a free acid and methanol. The amount of methanol produced is similar to endogenous methanol production. Its elimination half-life is about 9 minutes.

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