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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB00363
rdf:type
n3:Drug
n3:description
A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent. [PubChem]
n3:dosage
n20:271B6022-363D-11E5-9242-09173F13E4C5 n20:271B6023-363D-11E5-9242-09173F13E4C5 n20:271B6024-363D-11E5-9242-09173F13E4C5 n20:271B6025-363D-11E5-9242-09173F13E4C5 n20:271B6026-363D-11E5-9242-09173F13E4C5 n20:271B6027-363D-11E5-9242-09173F13E4C5 n20:271B6028-363D-11E5-9242-09173F13E4C5 n20:271B6029-363D-11E5-9242-09173F13E4C5 n20:271B602A-363D-11E5-9242-09173F13E4C5 n20:271B602B-363D-11E5-9242-09173F13E4C5 n20:271B602C-363D-11E5-9242-09173F13E4C5 n20:271B602D-363D-11E5-9242-09173F13E4C5 n20:271B602E-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Alvir JM, Lieberman JA, Safferman AZ, Schwimmer JL, Schaaf JA: Clozapine-induced agranulocytosis. Incidence and risk factors in the United States. N Engl J Med. 1993 Jul 15;329(3):162-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8515788 # Vaddadi KS, Soosai E, Vaddadi G: Low blood selenium concentrations in schizophrenic patients on clozapine. Br J Clin Pharmacol. 2003 Mar;55(3):307-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12630982 # Naheed M, Green B: Focus on clozapine. Curr Med Res Opin. 2001;17(3):223-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11900316 # Lane HY, Chang YC, Chang WH, Lin SK, Tseng YT, Jann MW: Effects of gender and age on plasma levels of clozapine and its metabolites: analyzed by critical statistics. J Clin Psychiatry. 1999 Jan;60(1):36-40. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10074876
n3:group
approved
n3:halfLife
8 hours (range 4-12 hours)
n3:indication
For use in patients with treatment-resistant schizophrenia.
n3:manufacturer
n4:271B6012-363D-11E5-9242-09173F13E4C5 n4:271B6013-363D-11E5-9242-09173F13E4C5 n4:271B6010-363D-11E5-9242-09173F13E4C5 n4:271B6011-363D-11E5-9242-09173F13E4C5 n4:271B600E-363D-11E5-9242-09173F13E4C5 n4:271B600F-363D-11E5-9242-09173F13E4C5 n4:271B600D-363D-11E5-9242-09173F13E4C5
owl:sameAs
n12:DB00363 n25:DB00363
dcterms:title
Clozapine
adms:identifier
n14:2716 n15:DB00363 n16:22869 n17:3766 n24:46506474 n26:PA449061 n27:2818 n28:D00283 n29:57664-345-88 n30:38 n31:C06924 n32:38 n34:Clozapine
n3:mechanismOfAction
Clozapine's antipsychotic action is likely mediated through a combination of antogistic effects at D2 receptors in the mesolimbic pathway and 5-HT2A receptors in the frontal cortex. D2 antagonism relieves positive symptoms while 5-HT2A antagonism alleviates negative symptoms.
n3:packager
n4:271B5FFA-363D-11E5-9242-09173F13E4C5 n4:271B5FFB-363D-11E5-9242-09173F13E4C5 n4:271B5FFE-363D-11E5-9242-09173F13E4C5 n4:271B5FFF-363D-11E5-9242-09173F13E4C5 n4:271B5FFC-363D-11E5-9242-09173F13E4C5 n4:271B5FFD-363D-11E5-9242-09173F13E4C5 n4:271B6002-363D-11E5-9242-09173F13E4C5 n4:271B6003-363D-11E5-9242-09173F13E4C5 n4:271B6000-363D-11E5-9242-09173F13E4C5 n4:271B6001-363D-11E5-9242-09173F13E4C5 n4:271B6006-363D-11E5-9242-09173F13E4C5 n4:271B6007-363D-11E5-9242-09173F13E4C5 n4:271B6004-363D-11E5-9242-09173F13E4C5 n4:271B6005-363D-11E5-9242-09173F13E4C5 n4:271B600A-363D-11E5-9242-09173F13E4C5 n4:271B600B-363D-11E5-9242-09173F13E4C5 n4:271B6008-363D-11E5-9242-09173F13E4C5 n4:271B6009-363D-11E5-9242-09173F13E4C5 n4:271B600C-363D-11E5-9242-09173F13E4C5
n3:patent
n18:5178878 n18:6024981
n3:routeOfElimination
Approximately 50% of the administered dose is excreted in the urine and 30% in the feces.
n3:synonym
Clozapine Clozapin Clozapina Clozapinum
n3:toxicity
Clozapine carries a black-box warning for agranulocytosis.
n9:hasAHFSCode
n10:28-16-08-04
n3:foodInteraction
Take without regard to meals. Limit caffeine intake (may reduce clozapine matabolism). Avoid alcohol.
n3:proteinBinding
97% (bound to serum proteins)
n3:synthesisReference
Schmutz, J. and Hunziker, F.; US. Patent 3,539,573; November 10, 1970 .
n22:hasConcept
n23:M0004649
foaf:page
n7:clo1089.shtml n19:clozapine.htm n35:clozapine.html
n3:IUPAC-Name
n5:271B6033-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B6039-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B6038-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B6035-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B6036-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B6037-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B6031-363D-11E5-9242-09173F13E4C5 n5:271B6049-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B602F-363D-11E5-9242-09173F13E4C5 n5:271B6032-363D-11E5-9242-09173F13E4C5 n5:271B604B-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B6030-363D-11E5-9242-09173F13E4C5
n3:pKa
n5:271B604C-363D-11E5-9242-09173F13E4C5
n9:hasATCCode
n33:N05AH02
n3:H-Bond-Acceptor-Count
n5:271B603F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B6040-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B603A-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B603B-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B603D-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B603C-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B603E-363D-11E5-9242-09173F13E4C5
n3:absorption
Rapid and almost complete
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
5786-21-0
n3:category
n3:containedIn
n21:271B6014-363D-11E5-9242-09173F13E4C5 n21:271B6015-363D-11E5-9242-09173F13E4C5 n21:271B6018-363D-11E5-9242-09173F13E4C5 n21:271B6019-363D-11E5-9242-09173F13E4C5 n21:271B6016-363D-11E5-9242-09173F13E4C5 n21:271B6017-363D-11E5-9242-09173F13E4C5 n21:271B601C-363D-11E5-9242-09173F13E4C5 n21:271B601D-363D-11E5-9242-09173F13E4C5 n21:271B601A-363D-11E5-9242-09173F13E4C5 n21:271B601B-363D-11E5-9242-09173F13E4C5 n21:271B6020-363D-11E5-9242-09173F13E4C5 n21:271B6021-363D-11E5-9242-09173F13E4C5 n21:271B601E-363D-11E5-9242-09173F13E4C5 n21:271B601F-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n5:271B6045-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B6047-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B6048-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n5:271B604A-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B6044-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B6043-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B6046-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B6034-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B6041-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B6042-363D-11E5-9242-09173F13E4C5