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Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n26http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/pubchem-substance/
n13http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/kegg-drug/
n22http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/drugbank/
n15http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/iuphar/
foafhttp://xmlns.com/foaf/0.1/
n19http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/guide-to-pharmacology/
n24http://bio2rdf.org/drugbank:
n20http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/chemspider/
admshttp://www.w3.org/ns/adms#
n21http://www.drugs.com/mtm/
n10http://www.rxlist.com/cgi/generic/
n8http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/chebi/
n12http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n14http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/pharmgkb/
n6http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/wikipedia/
n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n16http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/kegg-compound/
n7http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/bindingdb/
n25http://linked.opendata.cz/resource/drugbank/drug/DB00637/identifier/pubchem-compound/
n18http://linked.opendata.cz/resource/atc/
n17http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB00637
rdf:type
n3:Drug
n3:description
Astemizole is a long-acting, non-sedating second generation antihistamine used in the treatment of allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice.
n3:generalReferences
# Wang X, Hockerman GH, Green HW 3rd, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL: Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J. 2006 Jul;20(9):1531-3. Epub 2006 May 24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16723379 # Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr: A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16816845
n3:group
withdrawn approved
n3:halfLife
1 day
n3:indication
Astemizole was indicated for use in the relieving allergy symptoms, particularly rhinitis and conjunctivitis. It has been withdrawn from the market however due to concerns of arrhythmias.
owl:sameAs
n12:DB00637 n24:DB00637
dcterms:title
Astemizole
adms:identifier
n6:Astemizole n7:24226 n8:2896 n13:D00234 n14:PA448498 n15:2603 n16:C06832 n19:2603 n20:2160 n22:DB00637 n25:2247 n26:46508569
n3:mechanismOfAction
Astemizole competes with histamine for binding at H<sub>1</sub>-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H<sub>1</sub>-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier and preferentially binds at H1 receptors in the peripehery rather than within the brain, CNS depression is minimal. Astemizole may also act on H<sub>3</sub>-receptors, producing adverse effects.
n3:synonym
Astemizol 1-(P-Fluorobenzyl)-2-((1-(2-(P-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole Astemizolum Astemison 1-(P-Fluorobenzyl)-2-((1-(P-methoxyphenethyl)-4-piperidyl)amino)benzimidazole Astémizole
n3:toxicity
LD<sub>50</sub>=2052mg/kg in mice
n3:foodInteraction
Take on an empty stomach, food decreases absorption by 60%.
n3:proteinBinding
96.7%
n3:synthesisReference
Godelieve Irma Christine Maria Heylen, Cornelus Gerardus Maria Janssen, Jurzak Mirek, Henricus Petrus Martinus Maria Van Assouw, "Radiolabeled astemizole and method of making." U.S. Patent US07541476, issued June 02, 2009.
foaf:page
n10:astem.htm n21:astemizole.html
n3:IUPAC-Name
n4:271B5DD5-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5DDB-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5DDA-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5DD7-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5DD8-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5DD9-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5DD3-363D-11E5-9242-09173F13E4C5 n4:271B5DEA-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5DD4-363D-11E5-9242-09173F13E4C5 n4:271B5DD1-363D-11E5-9242-09173F13E4C5 n4:271B5DEC-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5DD2-363D-11E5-9242-09173F13E4C5
n17:hasATCCode
n18:R06AX11
n3:H-Bond-Acceptor-Count
n4:271B5DE1-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5DE2-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5DDC-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5DDD-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5DDF-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5DDE-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5DE0-363D-11E5-9242-09173F13E4C5
n3:absorption
Rapidly absorbed from the gastrointestinal tract.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
68844-77-9
n3:category
n3:Bioavailability
n4:271B5DE6-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5DE8-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5DE9-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B5DEB-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5DE5-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5DE4-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5DE7-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5DD6-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5DE3-363D-11E5-9242-09173F13E4C5