Esmolol

drugbox
IUPAC_name = methyl 3- [4-(2-hydroxy-3-propan
-2-ylamino-propoxy)phenyl] propanoate
CAS_number = 103598-03-4
ATC_prefix=C07
ATC_suffix=AB09
PubChem=59768
DrugBank=



C=16 | H=25 | N=1 | O=4>
molecular_weight = 295.374 g/mol
metabolism = Erythrocytic
bioavailability = -
volume_of_distribution = 3.5 l kg-1
protein_bound = 60%
elimination_half-life = 9 minutes
excretion = Renal
pregnancy_AU = C
pregnancy_US = C
pregnancy_category =
legal_status =
routes_of_administration = iv

Esmolol (trade name Brevibloc) is a cardioselective beta1 receptor blocker with rapid onset,cite journal |author=Deng CY, Lin SG, Zhang WC, "et al" |title=Esmolol inhibits Na+ current in rat ventricular myocytes |journal=Methods Find Exp Clin Pharmacol |volume=28 |issue=10 |pages=697–702 |year=2006 |month=December |pmid=17235414 |doi=10.1358/mf.2006.28.10.1037498 |url=http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summaryn_pr?p_JournalId=6&p_RefId=1037498] 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.

References


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