Esmolol

Esmolol

File:Esmolol structure.svg
Systematic (IUPAC) name
methyl (RS)-3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate
Clinical data
Pregnancy category	AU: C US: C (Risk not ruled out)
Routes of administration	iv
Pharmacokinetic data
Bioavailability	-
Protein binding	60%
Metabolism	Erythrocytic
Biological half-life	9 minutes
Excretion	Renal
Identifiers
CAS Number	103598-03-4
ATC code	C07AB09 (WHO)
PubChem	CID 59768
Chemical data
Formula	C16H25NO4
Molar mass	295.374 g/mol[[]]

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

It is a class II antiarrhythmic.

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 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. Esmolol is also the drug of choice when aortic dissection is suspected.

Metabolism

Esmolol is rapidly hydrolyzed by plasma esterases and not by plasma cholinesterases. Esmolol's short duration of action is based on the ester-methyl side chain which allows for quick hydrolysis. Esmolol's structure is reflected in its name, Es-molol as in ester-methyl. 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.

References

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