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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB01205
rdf:type
n3:Drug
n3:description
Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central nervous system.
n3:dosage
n7:271B55AC-363D-11E5-9242-09173F13E4C5 n7:271B55AD-363D-11E5-9242-09173F13E4C5 n7:271B55AE-363D-11E5-9242-09173F13E4C5 n7:271B55AF-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Ngo AS, Anthony CR, Samuel M, Wong E, Ponampalam R: Should a benzodiazepine antagonist be used in unconscious patients presenting to the emergency department? Resuscitation. 2007 Jul;74(1):27-37. Epub 2007 Feb 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17306436 # Olkkola KT, Ahonen J: Midazolam and other benzodiazepines. Handb Exp Pharmacol. 2008;(182):335-60. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18175099 # Maeda S, Miyawaki T, Higuchi H, Shimada M: Effect of flumazenil on disturbance of equilibrium function induced by midazolam. Anesth Prog. 2008 Fall;55(3):73-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18788841
n3:group
approved
n3:halfLife
Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Compared to adults, the elimination half-life in pediatric patients was more variable, averaging 40 minutes (range: 20 to 75 minutes).
n3:indication
For the complete or partial reversal of the sedative effects of benzodiazepines in cases where general anesthesia has been induced and/or maintained with benzodiazepines, and where sedation has been produced with benzodiazepines for diagnostic and therapeutic procedures. Also for the management of benzodiazepine overdose as an adjunct for appropriate supportive and symptomatic measures.
owl:sameAs
n28:DB01205 n31:DB01205
dcterms:title
Flumazenil
adms:identifier
n6:46507438 n15:26263 n16:5103 n17:PA449659 n18:3373 n19:D00697 n20:0004-6911-06 n21:C07825 n22:3256 n23:DB01205 n30:Flumazenil
n3:mechanismOfAction
Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in man.
n3:packager
n8:271B559C-363D-11E5-9242-09173F13E4C5 n8:271B559D-363D-11E5-9242-09173F13E4C5 n8:271B559A-363D-11E5-9242-09173F13E4C5 n8:271B559B-363D-11E5-9242-09173F13E4C5 n8:271B55A9-363D-11E5-9242-09173F13E4C5 n8:271B55A7-363D-11E5-9242-09173F13E4C5 n8:271B55A8-363D-11E5-9242-09173F13E4C5 n8:271B559F-363D-11E5-9242-09173F13E4C5 n8:271B559E-363D-11E5-9242-09173F13E4C5 n8:271B55A5-363D-11E5-9242-09173F13E4C5 n8:271B55A6-363D-11E5-9242-09173F13E4C5 n8:271B55A3-363D-11E5-9242-09173F13E4C5 n8:271B55A4-363D-11E5-9242-09173F13E4C5 n8:271B55A1-363D-11E5-9242-09173F13E4C5 n8:271B55A2-363D-11E5-9242-09173F13E4C5 n8:271B55A0-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination
Flumazenil is completely (99%) metabolized. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the radioactivity appearing in urine and 5% to 10% in the feces.
n3:synonym
Flumazenilo Anexate Lanexat Flumazenilum Flumazepil
n3:toxicity
In clinical studies, most adverse reactions to flumazenil were an extension of the pharmacologic effects of the drug in reversing benzodiazepine effects.
n3:volumeOfDistribution
* 0.9 to 1.1 L/kg
n9:hasAHFSCode
n24:28-92-00
n3:proteinBinding
Protein binding is approximately 50%, mostly (66%) to albumin. Protein binding is reduced in patients with hepatic cirrhosis.
n11:hasConcept
n12:M0008585
foaf:page
n14:flumazenil.htm n25:flumazenil.html
n3:IUPAC-Name
n4:271B55B4-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B55BA-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B55B9-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B55B6-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B55B7-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B55B8-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B55C9-363D-11E5-9242-09173F13E4C5 n4:271B55B2-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B55CB-363D-11E5-9242-09173F13E4C5 n4:271B55B3-363D-11E5-9242-09173F13E4C5 n4:271B55B0-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B55B1-363D-11E5-9242-09173F13E4C5
n9:hasATCCode
n10:V03AB25
n3:H-Bond-Acceptor-Count
n4:271B55C0-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B55C1-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B55BB-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B55BC-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B55BE-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B55BD-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B55BF-363D-11E5-9242-09173F13E4C5
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
78755-81-4
n3:category
n3:clearance
* 1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]
n3:containedIn
n26:271B55AA-363D-11E5-9242-09173F13E4C5 n26:271B55AB-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B55C5-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B55C7-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B55C8-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B55CA-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B55C4-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B55C3-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B55C6-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B55B5-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B55C2-363D-11E5-9242-09173F13E4C5