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QuickView for Pergolide (compound)


PubChem
Name: Pergolide
PubChem Compound ID: 11392877
Description: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.
Molecular formula: C19H26N2S
Molecular weight: 314.489 g/mol
DrugBank
Identification
Name: Pergolide
Name (isomeric): DB01186
Drug Type: small molecule
Description: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.
Synonyms:
Pergolide Methanesulfonate; Pergolida [INN-Spanish]; Pergolidum [INN-Latin]; Pergolide Mesylate
Brand: Permax
Category: Antidyskinetics, Antiparkinson Agents, Dopamine Agonists, Neuroprotective Agents, Central Nervous System Agents
CAS number: 66104-22-1
Pharmacology
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 It was withdrawn from the US and Canadian markets in 2007 due to an increased risk of cardiac valvulopathy.
Pharmacology:
Pergolide stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D1 and D5 subreceptors and are associated with dyskinesias. The dopaminergic D2 re...
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Mechanism of Action:
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 sto...
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Absorption: Significant amount may be absorbed (evidence on bioavailability still lacking).
Protein binding: 90%
Biotransformation: Extensively hepatic.
Route of elimination: The major route of excretion is the kidney.
Half Life: 27 hours
Toxicity: Oral, rat LD50: 15 mg/kg. Symptoms of overdose include nausea, vomiting, convulsions, decreased blood pressure, and CNS stimulation.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food to reduce gastric irritation and nausea
Drug interaction:
TamsulosinPergolide, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Pergolide is initiated, discontinued, or dose changed.
ZolmitriptanConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, pergolide, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
TelithromycinTelithromycin may reduce clearance of Pergolide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Pergolide if Telithromycin is initiated, discontinued or dose changed.
TipranavirTipranavir may increase the plasma concentration of Pergolide. Concomitant therapy should be avoided.
TranylcypromineIncreased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
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