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Esmolol



Esmolol
Systematic (IUPAC) name
methyl 3-[4-(2-hydroxy-3-propan
-2-ylamino-propoxy)phenyl]propanoate
Identifiers
CAS number 103598-03-4
ATC code C07AB09
PubChem 59768
Chemical data
Formula C16H25NO4> 
Mol. mass 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 (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.

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 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.

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Esmolol". A list of authors is available in Wikipedia.
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