Brands, Medical Use, Clinical Data
Drug Category
- Neuroprotective Agents
- Antiparkinson Agents
- Antidyskinetics
- Dopamine Agonists
- Central Nervous System Agents
Dosage Forms
Brands / Synonyms
Pergolida [Inn-Spanish]; Pergolide Mesylate; Pergolide Methanesulfonate; Pergolidum [Inn-Latin]; Permax; Permax
Indications
Indicated as adjunctive treatment to levodopa/carbidopa in the management of the signs and symptoms of Parkinson’s disease.
Pharmacology
Pergolide is an ergot derivative dopamine receptor agonist at both D1 and D2 receptor sites. Pergolide is 10 to 1,000 times more potent than bromocriptine on a milligram per milligram basis in various in vitro and in vivo test systems. Pergolide mesylate inhibits the secretion of prolactin in humans; it causes a transient rise in serum concentrations of growth hormone and a decrease in serum concentrations of luteinizing hormone. In Parkinson’s disease, pergolide mesylate is believed to exert its therapeutic effect by directly stimulating postsynaptic dopamine receptors in the nigrostriatal system.
Mechanism of Action
Pergolide is a potent dopamine receptor agonist. It directly stimulates post-synaptic dopamine receptors at both D1 and D2 receptor sites in the nigrostriatal system.
Absorption
Significant amount may be absorbed (evidence on bioavailability still lacking).
Toxicity
Oral, rat LD50: 15 mg/kg. Symptoms of overdose include nausea, vomiting, convulsions, decreased blood pressure, and CNS stimulation.
Biotrnasformation / Drug Metabolism
Not Available
Contraindications
Pergolide mesylate is contraindicated in patients who are hypersensitive to this drug or other ergot
derivatives.
Drug Interactions
Dopamine antagonists, such as the neuroleptics (phenothiazines, butyrophenones, thioxanthines ) or metoclopramide,
ordinarily should not be administered concurrently with Permax (a dopamine agonist); these agents may diminish the
effectiveness of Permax. Because pergolide mesylate is approximately 90% bound to plasma proteins, caution should be
exercised if pergolide mesylate is coadministered with other drugs known to affect protein binding.
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