. . . . . . . . "approved"@en . . . . "Take with food to reduce gastric irritation and nausea"@en . "66104-22-1"@en . . . . "Pergolida"@en . . . "Pergolide Methanesulfonate"@en . . " "@en . "The dopamine D₂ receptor is a 7-transmembrane G-protein coupled receptor associated with G_i 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. "@en . "Humans and other mammals"@en . . "# 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"@en . "Pergolidum"@en . . . "27 hours"@en . . . . . . . . . . . . "Pergolide Mesylate"@en . "Pergolide is a long-acting dopamine agonist approved in 1982 for the treatment of Parkinson\u2019s 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 The drug was withdrawn from the US market in March 2007 and from the Canadian market in August 2007. "@en . . . . . . "Pergolide"@en . . . . "The major route of excretion is the kidney."@en . "withdrawn"@en . "Significant amount may be absorbed (evidence on bioavailability still lacking)."@en . . . . . "\"DrugSyn.org\":http://www.drugsyn.org/Pergolide.htm"@en . . . "90%"@en . . . . . . "Oral, rat LD₅₀: 15 mg/kg. Symptoms of overdose include nausea, vomiting, convulsions, decreased blood pressure, and CNS stimulation."@en . . "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. "@en . . . . . .