Pergolide mesylate is a synthetic ergot derivative and is used in the treatment of Parkinsonism as well as hyperprolactinaemia.
It is an ergoline derivative, and a selective dopamine agonist with a high affinity for the D2 receptor site, and a lesser affinity for the D1 receptor site.
Pergolide is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 1 to 2 hours. At least 10 metabolites of pergolide have been detected in the urine and faeces, including N-despropylpergolide, pergolide sulfoxide, and pergolide sulfone.
Adverse effects include somnolence, dyskinesias, nausea, dry mouth, constipation, and hallucinations. Profound somnolence resulting in unplanned daytime sleep episodes has occurred in an increasing number of patients receiving pergolide as treatment of Parkinson’s disease. Dyskinesias were reported in 62.4% of patients who received pergolide during a clinical trial, as compared with 24.6% of patients who received placebo. Retroperitoneal fibrosis has been reported in several patients following long-term pergolide therapy. There are some reports of erythromelalgia of the lower extremities in Parkinsonian patients on pergolide therapy. Pleuropulmonary fibrosis was reported in several patients following long-term pergolide therapy.
Overdose with pergolide may result in vomiting, sweating, dizziness, agitation, dyskinesias, hallucinations, involuntary movements, palpitations, and hypotension. Treatment is symptomatic.
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