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Namespace Prefixes

PrefixIRI
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n5http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB00187
rdf:type
n3:Drug
n3: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.
n3:dosage
n23:271B5513-363D-11E5-9242-09173F13E4C5 n23:271B5514-363D-11E5-9242-09173F13E4C5 n23:271B5515-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3: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.
n3: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.
n3:manufacturer
n19:271B550C-363D-11E5-9242-09173F13E4C5 n19:271B550D-363D-11E5-9242-09173F13E4C5 n19:271B550B-363D-11E5-9242-09173F13E4C5 n19:271B550E-363D-11E5-9242-09173F13E4C5
owl:sameAs
n21:DB00187 n27:DB00187
dcterms:title
Esmolol
adms:identifier
n8:46506146 n9:PA449500 n10:59768 n11:C06980 n14:0641-2965-45 n15:DB00187 n17:4856 n18:53916 n24:Esmolol
n3: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.
n3:packager
n19:271B5504-363D-11E5-9242-09173F13E4C5 n19:271B5505-363D-11E5-9242-09173F13E4C5 n19:271B5502-363D-11E5-9242-09173F13E4C5 n19:271B5503-363D-11E5-9242-09173F13E4C5 n19:271B5508-363D-11E5-9242-09173F13E4C5 n19:271B5509-363D-11E5-9242-09173F13E4C5 n19:271B5506-363D-11E5-9242-09173F13E4C5 n19:271B5507-363D-11E5-9242-09173F13E4C5 n19:271B550A-363D-11E5-9242-09173F13E4C5
n3:patent
n22:6310094 n22:2410446
n3:routeOfElimination
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.
n3:synonym
(+-)-Esmolol Methyl P-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate 3-[4-(2-Hydroxy-3-isopropylamino-propoxy)-phenyl]-propionic acid methyl ester Methyl 4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)benzenepropanoate ESMOLOL (+-)-Methyl P-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate
n3:toxicity
Symptoms of overdose include cardiac arrest, bradycardia, hypotension, electromechanical dissociation and loss of consciousness.
n5:hasAHFSCode
n6:24-24-00
n3:proteinBinding
55% bound to human plasma protein, while the acid metabolite is 10% bound.
n3:salt
n3:synthesisReference
"DrugSyn.org":http://www.drugsyn.org/Esmolol.htm
foaf:page
n13:esmolol.html n25:esmolol.htm
n3:IUPAC-Name
n4:271B551A-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5520-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B551F-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B551C-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B551D-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B551E-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5530-363D-11E5-9242-09173F13E4C5 n4:271B5518-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5531-363D-11E5-9242-09173F13E4C5 n4:271B5516-363D-11E5-9242-09173F13E4C5 n4:271B5519-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5517-363D-11E5-9242-09173F13E4C5
n5:hasATCCode
n26:C07AB09
n3:H-Bond-Acceptor-Count
n4:271B5526-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5527-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5521-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5522-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5524-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5523-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5525-363D-11E5-9242-09173F13E4C5
n3: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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
103598-03-4
n3:clearance
* 20 L/kg/hr [Men]
n3:containedIn
n16:271B5512-363D-11E5-9242-09173F13E4C5 n16:271B5510-363D-11E5-9242-09173F13E4C5 n16:271B5511-363D-11E5-9242-09173F13E4C5 n16:271B550F-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B552C-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B552E-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B552F-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B552B-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B552A-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B552D-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B551B-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5528-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5529-363D-11E5-9242-09173F13E4C5