About: Cabergoline     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...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 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours. (en)
http://linked.open...ugbank/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. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Cabergoline (en)
adms:identifier
http://linked.open...mechanismOfAction
  • The dopamine D<sub>2</sub> receptor is a 7-transmembrane G-protein coupled receptor associated with G<sub>i</sub> proteins. In lactotrophs, stimulation of dopamine D<sub>2</sub> causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca<sup>2+</sup> 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 D<sub>2</sub> 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, &alpha;<sub>1</sub>,- and &alpha;<sub>2</sub>- adrenergic, and 5-HT<sub>1</sub>- and 5-HT<sub>2</sub>-serotonin receptors. (en)
http://linked.open...drugbank/packager
http://linked.open...outeOfElimination
  • 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. (en)
http://linked.open.../drugbank/synonym
  • Cabergoline (en)
  • 1-Ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea (en)
  • (8R)-6-Allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide (en)
  • Cabergolina (en)
  • Cabergolinum (en)
  • 1-((6-Allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea (en)
  • 1-[(6-Allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea (en)
  • (8beta)-N-[3-(dimethylamino)Propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide (en)
http://linked.open...drugbank/toxicity
  • Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Absorption is not affected by food. (en)
  • Take with food to improve tolerance. (en)
http://linked.open...nk/proteinBinding
  • Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner. (en)
http://linked.open...ynthesisReference
  • "DrugSyn.org":http://www.drugsyn.org/Cabergoline.htm (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
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http://linked.open...bank/Refractivity
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http://linked.open...ugbank/absorption
  • First-pass effect is seen, however the absolute bioavailability is unknown. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 81409-90-7 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • * renal cl=0,008 L/min * nonrenal cl=3.2 L/min (en)
http://linked.open...gbank/containedIn
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http://linked.open...bank/Rule-of-Five
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http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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