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Active ingredient: Pergolide - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Neuroprotective Agents
  • Antiparkinson Agents
  • Antidyskinetics
  • Dopamine Agonists
  • Central Nervous System Agents

Dosage Forms

  • Tablet

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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