Esmolol

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Esmolol
Systematic (IUPAC) name
methyl 3-[4-(2-hydroxy-3-propan -2-ylamino-propoxy)phenyl]propanoate
Identifiers
CAS number	103598-03-4
ATC code	C07 AB09
PubChem	59768
Chemical data
Formula	C₁₆H₂₅N O_4>
Mol. weight	295.374 g/mol
Pharmacokinetic data
Bioavailability	-
Protein binding	60%
Metabolism	Erythrocytic
Half life	9 minutes
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status
Routes	iv

Esmolol (tradename 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.

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.

[edit] 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.

[edit] 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.

Beta blockers (C07) edit