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Namespace Prefixes

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Statements

Subject Item: n2:DB00248
rdf:type: n3:Drug
n3:description: Cabergoline, an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor. It is used to treat hyperprolactinemic disorders and Parkinsonian Syndrome. Cabergoline possesses potent agonist activity on dopamine D2 receptors.
n3:dosage: n14:271B652D-363D-11E5-9242-09173F13E4C5 n14:271B652E-363D-11E5-9242-09173F13E4C5
n3:generalReferences: # Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson's disease] Neurologia. 2003 May;18(4):202-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12721865 # Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson's disease. Drugs. 2004;64(18):2125-41. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15341508 # Bracco F, Battaglia A, Chouza C, Dupont E, Gershanik O, Marti Masso JF, Montastruc JL: The long-acting dopamine receptor agonist cabergoline in early Parkinson's disease: final results of a 5-year, double-blind, levodopa-controlled study. CNS Drugs. 2004;18(11):733-46. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15330687 # Miyagi M, Arai N, Taya F, Itoh F, Komatsu Y, Kojima M, Isaji M: Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents. Biol Pharm Bull. 1996 Nov;19(11):1499-502. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8951172
n3:group: approved
n3:halfLife: The elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.
n3:indication: For the treatment of hyperprolactinemic disorders, either idiopathic or due to prolactinoma (prolactin-secreting adenomas). May also be used to manage symptoms of Parkinsonian Syndrome as monotherapy during initial symptomatic management or as an adjunct to levodopa therapy during advanced stages of disease.
n3:manufacturer: n5:271B652A-363D-11E5-9242-09173F13E4C5 n5:271B652B-363D-11E5-9242-09173F13E4C5 n5:271B6528-363D-11E5-9242-09173F13E4C5 n5:271B6529-363D-11E5-9242-09173F13E4C5 n5:271B6527-363D-11E5-9242-09173F13E4C5
owl:sameAs: n13:DB00248 n23:DB00248
dcterms:title: Cabergoline
adms:identifier: n16:54746 n17:46508571 n18:49884-673-14 n19:PA448708 n25:C08187 n26:D00987 n27:37 n28:37 n29:DB00248 n30:3286 n31:49452 n32:Cabergoline
n3:mechanismOfAction: The dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 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. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1,- and α2- adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.
n3:packager: n5:271B6520-363D-11E5-9242-09173F13E4C5 n5:271B6521-363D-11E5-9242-09173F13E4C5 n5:271B651F-363D-11E5-9242-09173F13E4C5 n5:271B6524-363D-11E5-9242-09173F13E4C5 n5:271B6525-363D-11E5-9242-09173F13E4C5 n5:271B6522-363D-11E5-9242-09173F13E4C5 n5:271B6523-363D-11E5-9242-09173F13E4C5 n5:271B6526-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination: After oral dosing of radioactive cabergoline to five healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine.
n3:synonym: (8R)-6-Allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide (8beta)-N-[3-(dimethylamino)Propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide Cabergolina Cabergoline Cabergolinum 1-[(6-Allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea 1-((6-Allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea 1-Ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea
n3:toxicity: Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.
n7:hasAHFSCode: n24:28-36-20-04
n3:foodInteraction: Absorption is not affected by food. Take with food to improve tolerance.
n3:proteinBinding: Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner.
n3:synthesisReference: "DrugSyn.org":http://www.drugsyn.org/Cabergoline.htm
n9:hasConcept: n10:M0136060
foaf:page: n21:cabergoline.html n22:cabergoline.htm
n3:IUPAC-Name: n4:271B6533-363D-11E5-9242-09173F13E4C5
n3:InChI: n4:271B6539-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula: n4:271B6538-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight: n4:271B6535-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight: n4:271B6536-363D-11E5-9242-09173F13E4C5
n3:SMILES: n4:271B6537-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility: n4:271B6549-363D-11E5-9242-09173F13E4C5 n4:271B6531-363D-11E5-9242-09173F13E4C5
n3:logP: n4:271B654B-363D-11E5-9242-09173F13E4C5 n4:271B652F-363D-11E5-9242-09173F13E4C5 n4:271B6532-363D-11E5-9242-09173F13E4C5
n3:logS: n4:271B6530-363D-11E5-9242-09173F13E4C5
n7:hasATCCode: n8:N04BC06 n8:G02CB03
n3:H-Bond-Acceptor-Count: n4:271B653F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count: n4:271B6540-363D-11E5-9242-09173F13E4C5
n3:InChIKey: n4:271B653A-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-: n4:271B653B-363D-11E5-9242-09173F13E4C5
n3:Polarizability: n4:271B653D-363D-11E5-9242-09173F13E4C5
n3:Refractivity: n4:271B653C-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count: n4:271B653E-363D-11E5-9242-09173F13E4C5
n3:absorption: First-pass effect is seen, however the absolute bioavailability is unknown.
n3:affectedOrganism: Humans and other mammals
n3:casRegistryNumber: 81409-90-7
n3:category
n3:clearance: * renal cl=0,008 L/min * nonrenal cl=3.2 L/min
n3:containedIn: n11:271B652C-363D-11E5-9242-09173F13E4C5
n3:Bioavailability: n4:271B6545-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter: n4:271B6547-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule: n4:271B6548-363D-11E5-9242-09173F13E4C5
n3:Melting-Point: n4:271B654A-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings: n4:271B6544-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge: n4:271B6543-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five: n4:271B6546-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name: n4:271B6534-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-: n4:271B6541-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-: n4:271B6542-363D-11E5-9242-09173F13E4C5