Esmolol detailed information

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Esmolol detailed information
Clinical data
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration
iv
ATC code
Pharmacokinetic data
Bioavailability-
Protein binding60%
MetabolismErythrocytic
Elimination half-life9 minutes
ExcretionRenal
Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC16H25NO4>
Molar mass295.374 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]




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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