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Esmolol
Systematic (IUPAC) name
methyl (RS)-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 C 16H25NO4  
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,[1] a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.

It is a class II antiarrhythmic.[2]

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. 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

  1. ^ Deng CY, Lin SG, Zhang WC, et al. (December 2006). "Esmolol inhibits Na+ current in rat ventricular myocytes". Methods Find Exp Clin Pharmacol 28 (10): 697–702. doi:10.1358/mf.2006.28.10.1037498. PMID 17235414. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summaryn_pr?p_JournalId=6&p_RefId=1037498.  
  2. ^ Jaillon P, Drici M (December 1989). "Recent antiarrhythmic drugs". Am. J. Cardiol. 64 (20): 65J–69J. doi:10.1016/0002-9149(89)91203-4. PMID 2688391.  







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