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Namespace Prefixes

PrefixIRI
n14http://www.rxlist.com/cgi/generic3/
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n9http://linked.opendata.cz/resource/AHFS/
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n18http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/chemspider/
n11http://linked.opendata.cz/resource/mesh/concept/
n20http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/chebi/
n21http://bio2rdf.org/drugbank:
n12http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/wikipedia/
n22http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/pharmgkb/
admshttp://www.w3.org/ns/adms#
n23http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/pubchem-compound/
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n5http://linked.opendata.cz/ontology/drugbank/
n6http://linked.opendata.cz/resource/drugbank/property/
n4http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/kegg-drug/
n19http://linked.opendata.cz/resource/drugbank/drug/DB01158/identifier/drugbank/
xsdhhttp://www.w3.org/2001/XMLSchema#
n8http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB01158
rdf:type
n5:Drug
n5:description
Bretylium blocks the release of noradrenaline from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The primary mode of action for bretylium is thought to be inhibition of voltage-gated K(+) channels. Recent evidence has shown that bretylium may also inhibit the Na,K-ATPase by binding to the extracellular K-site.
n5:group
approved
n5:halfLife
The terminal half-life in four normal volunteers averaged 7.8±0.6 hours (range 6.9-8.1). During hemodialysis, this patient's arterial and venous bretylium concentrations declined rapidly, resulting in a half-life of 13 hours.
n5:indication
For use in the prophylaxis and therapy of ventricular fibrillation. Also used in the treatment of life-threatening ventricular arrhythmias, such as ventricular tachycardia, that have failed to respond to adequate doses of a first-line antiarrhythmic agent, such as lidocaine.
owl:sameAs
n16:DB01158 n21:DB01158
dcterms:title
Bretylium
adms:identifier
n4:D00645 n7:46505320 n12:Bretylium n18:2337 n19:DB01158 n20:3172 n22:PA448662 n23:2431
n5:mechanismOfAction
Bretylium inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. The mechanisms of the antifibrillatory and antiarrhythmic actions of bretylium are not established. In efforts to define these mechanisms, the following electrophysiologic actions of bretylium have been demonstrated in animal experiments: increase in ventricular fibrillation threshold, increase in action potential duration and effective refractory period without changes in heart rate, little effect on the rate of rise or amplitude of the cardiac action potential (Phase 0) or in resting membrane potential (Phase 4) in normal myocardium, decrease in the disparity in action potential duration between normal and infarcted regions, and increase in impulse formation and spontaneous firing rate of pacemaker tissue as well as increase ventricular conduction velocity.
n5:synonym
(2-Bromobenzyl)ethyldimethylaminium N-Ethyl-N,N-dimethyl-2-bromobenzenemethanaminium 2-Bromo-N-ethyl-N,N-dimethylbenzenemethanaminium
n5:toxicity
Oral, mouse: LD<sub>50</sub> = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Bretylium serum levels were 8000 ng/mL.
n8:hasAHFSCode
n9:24-04-04-20
n5:salt
n5:synthesisReference
Copp, F.C. and Stephenson, D.; US. Patent 3,038,004; June 5, 1962; assigned to Burroughs Wellcome & Co.
n10:hasConcept
n11:M0131477
foaf:page
n14:bretosy.htm
n5:IUPAC-Name
n6:271B4B81-363D-11E5-9242-09173F13E4C5
n5:InChI
n6:271B4B87-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n6:271B4B86-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n6:271B4B83-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n6:271B4B84-363D-11E5-9242-09173F13E4C5
n5:SMILES
n6:271B4B85-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n6:271B4B7F-363D-11E5-9242-09173F13E4C5 n6:271B4B96-363D-11E5-9242-09173F13E4C5
n5:logP
n6:271B4B80-363D-11E5-9242-09173F13E4C5 n6:271B4B7D-363D-11E5-9242-09173F13E4C5
n5:logS
n6:271B4B7E-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Acceptor-Count
n6:271B4B8D-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n6:271B4B8E-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n6:271B4B88-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n6:271B4B89-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n6:271B4B8B-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n6:271B4B8A-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n6:271B4B8C-363D-11E5-9242-09173F13E4C5
n5:affectedOrganism
Humans and other mammals
n5:casRegistryNumber
59-41-6
n5:category
n5:Bioavailability
n6:271B4B92-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n6:271B4B94-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n6:271B4B95-363D-11E5-9242-09173F13E4C5
n5:Melting-Point
n6:271B4B97-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n6:271B4B91-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n6:271B4B90-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n6:271B4B93-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n6:271B4B82-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-acidic-
n6:271B4B8F-363D-11E5-9242-09173F13E4C5