Pergolide

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Permax; Belgium: Permax; Czech Republic: Permax; Denmark: Permax; Estonia: Permax; France: Celance; Germany: Celance, Parkotil, Pergolid; Greece: Celance; Ireland: Celance, Pergolide; Italy: Nopar, Pergolide; Luxembourg: Permax; Netherlands: Pergolide, Permax; Poland: Permax; Portugal: Pergolida, Permax; Spain: Pergolida, Pharken; UK: Celance.

North America

Canada: Permax; USA: Permax.

Latin America

Brazil: Celance.

Asia

Japan: Pergolide, Pergolin, Permax, Veceral.

Drug combinations

Chemistry

Pergolide Mesylate: C~19~H~26~N~2~S CH~4~O~3~S. Mw: 410.59. (1) Ergoline, 8-[(methylthio)methyl]-6-propyl-, monomethanesulfonate, (8β)-; (2) 8β-[(Methylthio)methyl]-6-propylergoline monomethanesulfonate. CAS-66104-23-2; CAS-66104-22-1 (pergolide)(1979).

Pharmacologic Category

Antiparkinsonian Agents; Ergot-derivative Dopamine Receptor Agonists. (ATC-Code: N04BC02).

Mechanism of action

A dopamine receptor agonist. Relieves symptoms of parkinsonism, presumably by directly stimulating postsynaptic dopamine receptors in corpus striatum. Reduces serum prolactin concentrations by inhibiting release of prolactin from anterior pituitary gland. Causes transient increases in serum somatotropin (growth hormone) concentrations and decreases in serum luteinizing hormone concentrations.

Therapeutic use

Symptomatic management of parkinsonian syndrome.

Pregnancy and lactiation implications

Use with caution during pregnancy or lactation (drug expected to interfere with lactation).

Unlabeled use

Contraindications

Known hypersensitivity to pergolide or other ergot derivatives.

Warnings and precautions

May cause drowsiness or sleepiness. Concurrent use of other CNS depressants may cause additive sedative effects. Orthostatic and/or sustained hypotension reported. Hallucinations reported. May cause and/or exacerbate pre-existing states of confusion or hallucinations. Pulmonary fibrosis, pleuritis, pleural effusion, pleural fibrosis, pericarditis, pericardial effusion, cardiac valvulopathy (involving 1 or more valves), or retroperitoneal fibrosis reported rarely. A symptom complex resembling neuroleptic malignant syndrome (e.g. elevated temperature, muscular rigidity, altered consciousness, autonomic instability) reported in association with rapid dosage reduction of, withdrawal of, or changes in antiparkinsonian therapy. May potentiate adverse dopaminergic effects of levodopa and may cause or exacerbate pre-existing dyskinesias. Arrhythmias (e.g. atrial premature contractions, sinus tachycardia) reported. Use with caution in patients prone to cardiac dysrhythmias. Cardiac valvulopathy and other cardiac adverse effects reported. Increased incidence of confusion, somnolence, and peripheral edema reported in patients ≥65 years of age. Substantially eliminated by kidneys; risk of toxic reactions may be greater in impaired renal function.

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