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Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
n25http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/drugbank/
dctermshttp://purl.org/dc/terms/
n12http://linked.opendata.cz/resource/mesh/concept/
foafhttp://xmlns.com/foaf/0.1/
n4http://linked.opendata.cz/resource/drugbank/company/
n23http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/national-drug-code-directory/
n24http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/chemspider/
n7http://bio2rdf.org/drugbank:
n27http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/chebi/
admshttp://www.w3.org/ns/adms#
n14http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
n9http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/wikipedia/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
n21http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/pharmgkb/
n13http://linked.opendata.cz/resource/drugbank/medicinal-product/
owlhttp://www.w3.org/2002/07/owl#
n11http://linked.opendata.cz/ontology/mesh/
n3http://linked.opendata.cz/ontology/drugbank/
n20http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/pdb/
n22http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/kegg-compound/
n17http://www.drugs.com/cdi/
n16http://www.rxlist.com/cgi/generic2/
n5http://linked.opendata.cz/resource/drugbank/property/
n26http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/bindingdb/
n18http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/pubchem-compound/
xsdhhttp://www.w3.org/2001/XMLSchema#
n19http://linked.opendata.cz/resource/drugbank/drug/DB00382/identifier/pubchem-substance/

Statements

Subject Item
n2:DB00382
rdf:type
n3:Drug
n3:description
A centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. Tacrine has been discontinued for the United States market.
n3:generalReferences
# Qizilbash N, Whitehead A, Higgins J, Wilcock G, Schneider L, Farlow M: Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. Dementia Trialists' Collaboration. JAMA. 1998 Nov 25;280(20):1777-82. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9842955 # Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20480924
n3:group
withdrawn
n3:halfLife
2 to 4 hours
n3:indication
For the palliative treatment of mild to moderate dementia of the Alzheimer's type.
n3:manufacturer
n4:271B3E76-363D-11E5-9242-09173F13E4C5
owl:sameAs
n7:DB00382 n14:DB00382
dcterms:title
Tacrine
adms:identifier
n9:Tacrine n18:1935 n19:46505487 n20:760 n21:PA451576 n22:C01453 n23:59630-190-12 n24:1859 n25:DB00382 n26:8961 n27:9389
n3:mechanismOfAction
The mechanism of tacrine is not fully known, but it is suggested that the drug is an anticholinesterase agent which reversibly binds with and inactivates cholinesterases. This inhibits the hydrolysis of acetylcholine released from functioning cholinergic neurons, thus leading to an accumulation of acetylcholine at cholinergic synapses. The result is a prolonged effect of acetylcholine.
n3:packager
n4:271B3E75-363D-11E5-9242-09173F13E4C5 n4:271B3E74-363D-11E5-9242-09173F13E4C5
n3:synonym
THA Tetrahydroaminacrine 1,2,3,4-tetrahydroacridin-9-amine Tacrinum Tetrahydroaminoacridine Tacrine Tacrin
n3:toxicity
Overdosage with cholinesterase inhibitors can cause a cholinergic crisis characterized by severe nausea/vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. The estimated median lethal dose of tacrine following a single oral dose in rats is 40 mg/kg, or approximately 12 times the maximum recommended human dose of 160 mg/day.
n3:volumeOfDistribution
* 349 ± 193 L
n3:proteinBinding
55%
n3:salt
n3:synthesisReference
S. Shirley Yang, Wayne Boisvert, Nouman A. Muhammad, Jay Weiss, "Controlled release tacrine drug delivery systems and methods for preparing same." U.S. Patent US5576022, issued February, 1993.
n11:hasConcept
n12:M0021008
foaf:page
n16:tacrine.htm n17:tacrine.html
n3:IUPAC-Name
n5:271B3E7E-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B3E84-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B3E83-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B3E80-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B3E81-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B3E82-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B3E93-363D-11E5-9242-09173F13E4C5 n5:271B3E7C-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B3E95-363D-11E5-9242-09173F13E4C5 n5:271B3E7A-363D-11E5-9242-09173F13E4C5 n5:271B3E7D-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B3E7B-363D-11E5-9242-09173F13E4C5
n3:pKa
n5:271B3E96-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n5:271B3E8A-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B3E8B-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B3E85-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B3E86-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B3E88-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B3E87-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B3E89-363D-11E5-9242-09173F13E4C5
n3:absorption
Tacrine is rapidly absorbed. Absolute bioavailability of tacrine is approximately 17%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
321-64-2
n3:category
n3:containedIn
n13:271B3E78-363D-11E5-9242-09173F13E4C5 n13:271B3E79-363D-11E5-9242-09173F13E4C5 n13:271B3E77-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n5:271B3E8F-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B3E91-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B3E92-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n5:271B3E94-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B3E8E-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B3E8D-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B3E90-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B3E7F-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B3E8C-363D-11E5-9242-09173F13E4C5