About: Esmolol     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • 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 stabilizing 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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes. The acid metabolite has an elimination half-life of about 3.7 hours. (en)
http://linked.open...ugbank/indication
  • For the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Also used in noncompensatory sinus tachycardia where the rapid heart rate requires specific intervention. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Esmolol (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Similar to other beta-blockers, esmolol blocks the agonistic effect of the sympathetic neurotransmitters by competing for receptor binding sites. Because it predominantly blocks the beta-1 receptors in cardiac tissue, it is said to be cardioselective. In general, so-called cardioselective beta-blockers are relatively cardioselective; at lower doses they block beta-1 receptors only but begin to block beta-2 receptors as the dose increases. At therapeutic dosages, esmolol does not have intrinsic sympathomimetic activity (ISA) or membrane-stabilizing (quinidine-like) activity. Antiarrhythmic activity is due to blockade of adrenergic stimulation of cardiac pacemaker potentials. In the Vaughan Williams classification of antiarrhythmics, beta-blockers are considered to be class II agents. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Consistent with the high rate of blood-based metabolism of esmolol hydrochloride, less than 2% of the drug is excreted unchanged in the urine. The acid metabolite has an elimination half-life of about 3.7 hours and is excreted in the urine with a clearance approximately equivalent to the glomerular filtration rate. Excretion of the acid metabolite is significantly decreased in patients with renal disease, with the elimination half-life increased to about ten-fold that of normals, and plasma levels considerably elevated. (en)
http://linked.open.../drugbank/synonym
  • ESMOLOL (en)
  • (+-)-Esmolol (en)
  • Methyl P-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate (en)
  • (+-)-Methyl P-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate (en)
  • Methyl 4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)benzenepropanoate (en)
  • 3-[4-(2-Hydroxy-3-isopropylamino-propoxy)-phenyl]-propionic acid methyl ester (en)
http://linked.open...drugbank/toxicity
  • Symptoms of overdose include cardiac arrest, bradycardia, hypotension, electromechanical dissociation and loss of consciousness. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • 55% bound to human plasma protein, while the acid metabolite is 10% bound. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • "DrugSyn.org":http://www.drugsyn.org/Esmolol.htm (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Rapidly absorbed, steady-state blood levels for dosages from 50-300 µg/kg/min (0.05-0.3 mg/kg/mm) are obtained within five minutes. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 103598-03-4 (en)
http://linked.open...rugbank/clearance
  • * 20 L/kg/hr [Men] (en)
http://linked.open...gbank/containedIn
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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