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Namespace Prefixes

Prefix	IRI
n2	http://linked.opendata.cz/resource/drugbank/drug/
dcterms	http://purl.org/dc/terms/
n13	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/drugbank/
n23	http://linked.opendata.cz/resource/AHFS/
foaf	http://xmlns.com/foaf/0.1/
n22	http://linked.opendata.cz/resource/mesh/concept/
n4	http://linked.opendata.cz/resource/drugbank/company/
n12	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/national-drug-code-directory/
n27	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/chemspider/
n25	http://bio2rdf.org/drugbank:
adms	http://www.w3.org/ns/adms#
n19	http://linked.opendata.cz/resource/drugbank/patent/
n11	http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
n20	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/wikipedia/
rdf	http://www.w3.org/1999/02/22-rdf-syntax-ns#
n16	http://linked.opendata.cz/resource/drugbank/medicinal-product/
n6	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/pharmgkb/
owl	http://www.w3.org/2002/07/owl#
n21	http://linked.opendata.cz/ontology/mesh/
n3	http://linked.opendata.cz/ontology/drugbank/
n28	http://www.drugs.com/cdi/
n9	http://linked.opendata.cz/resource/drugbank/property/
n18	http://www.rxlist.com/cgi/generic2/
n8	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/kegg-compound/
n26	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/bindingdb/
xsdh	http://www.w3.org/2001/XMLSchema#
n7	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/pubchem-compound/
n15	http://linked.opendata.cz/resource/atc/
n29	http://linked.opendata.cz/resource/drugbank/drug/DB01186/identifier/pubchem-substance/
n14	http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item: n2:DB01186
rdf:type: n3:Drug
n3:description: Pergolide is a long-acting dopamine agonist approved in 1982 for the treatment of Parkinson’s Disease. It is an ergot derivative that acts on the dopamine D2 and D3, alpha2- and alpha1-adrenergic, and 5-hydroxytryptamine (5-HT) receptors. It was indicated as adjunct therapy with levodopa/carbidopa in the symptomatic treatment of parkinsonian syndrome. It was later found that pergolide increased the risk of cardiac valvulopathy. The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007.
n3:generalReferences: # Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E: Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med. 2007 Jan 4;356(1):29-38. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17202453 # Breitenstein C, Korsukewitz C, Floel A, Kretzschmar T, Diederich K, Knecht S: Tonic dopaminergic stimulation impairs associative learning in healthy subjects. Neuropsychopharmacology. 2006 Nov;31(11):2552-64. Epub 2006 Jul 26. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16880771
n3:group: approved withdrawn
n3:halfLife: 27 hours
n3:indication: Indicated as adjunctive treatment to levodopa/carbidopa in the management of the signs and symptoms of Parkinson's disease. It was withdrawn from the US and Canadian markets in 2007 due to an increased risk of cardiac valvulopathy.
owl:sameAs: n11:DB01186 n25:DB01186
dcterms:title: Pergolide
adms:identifier: n6:PA450873 n7:47811 n8:C07425 n12:0187-0839-01 n13:DB01186 n20:Pergolide n26:50017543 n27:43503 n29:46507604
n3:mechanismOfAction: The dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 receptor causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders.
n3:packager: n4:271B50DA-363D-11E5-9242-09173F13E4C5 n4:271B50DB-363D-11E5-9242-09173F13E4C5 n4:271B50D8-363D-11E5-9242-09173F13E4C5 n4:271B50D6-363D-11E5-9242-09173F13E4C5 n4:271B50D7-363D-11E5-9242-09173F13E4C5 n4:271B50D5-363D-11E5-9242-09173F13E4C5 n4:271B50D9-363D-11E5-9242-09173F13E4C5 n4:271B50D4-363D-11E5-9242-09173F13E4C5 n4:271B50DC-363D-11E5-9242-09173F13E4C5
n3:patent: n19:5114948
n3:routeOfElimination: The major route of excretion is the kidney.
n3:synonym: Pergolida Pergolide Methanesulfonate Pergolidum Pergolide Mesylate
n3:toxicity: Oral, rat LD50: 15 mg/kg. Symptoms of overdose include nausea, vomiting, convulsions, decreased blood pressure, and CNS stimulation.
n14:hasAHFSCode: n23:28-36-20-04
n3:foodInteraction: Take with food to reduce gastric irritation and nausea
n3:proteinBinding: 90%
n3:synthesisReference: "DrugSyn.org":http://www.drugsyn.org/Pergolide.htm
n21:hasConcept: n22:M0016279
foaf:page: n18:pergol.htm n28:pergolide-mesylate.html
n3:IUPAC-Name: n9:271B50E2-363D-11E5-9242-09173F13E4C5
n3:InChI: n9:271B50E8-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula: n9:271B50E7-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight: n9:271B50E4-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight: n9:271B50E5-363D-11E5-9242-09173F13E4C5
n3:SMILES: n9:271B50E6-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility: n9:271B50E0-363D-11E5-9242-09173F13E4C5
n3:logP: n9:271B50DE-363D-11E5-9242-09173F13E4C5 n9:271B50E1-363D-11E5-9242-09173F13E4C5 n9:271B50F9-363D-11E5-9242-09173F13E4C5
n3:logS: n9:271B50DF-363D-11E5-9242-09173F13E4C5
n14:hasATCCode: n15:N04BC02
n3:H-Bond-Acceptor-Count: n9:271B50EE-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count: n9:271B50EF-363D-11E5-9242-09173F13E4C5
n3:InChIKey: n9:271B50E9-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-: n9:271B50EA-363D-11E5-9242-09173F13E4C5
n3:Polarizability: n9:271B50EC-363D-11E5-9242-09173F13E4C5
n3:Refractivity: n9:271B50EB-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count: n9:271B50ED-363D-11E5-9242-09173F13E4C5
n3:absorption: Significant amount may be absorbed (evidence on bioavailability still lacking).
n3:affectedOrganism: Humans and other mammals
n3:casRegistryNumber: 66104-22-1
n3:category
n3:containedIn: n16:271B50DD-363D-11E5-9242-09173F13E4C5
n3:Bioavailability: n9:271B50F4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter: n9:271B50F6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule: n9:271B50F7-363D-11E5-9242-09173F13E4C5
n3:Melting-Point: n9:271B50F8-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings: n9:271B50F3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge: n9:271B50F2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five: n9:271B50F5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name: n9:271B50E3-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-: n9:271B50F0-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-: n9:271B50F1-363D-11E5-9242-09173F13E4C5