Pergolide is an oral dopamine receptor agonist used predominantly in the therapy of Parkinson disease. Pergolide therapy is associated with low rate of transient serum enzyme elevations during treatment and has been implicated in rare cases of acute liver injury.
Pergolide (per' goe lide) is an ergot derivative similar to bromocriptine which acts as a dopamine receptor agonist. Pergolide, unlike bromocriptine, has agonist activity on both D1 and D2 dopamine receptors and acts directly on the substantia nigra. Pergolide was approved for use in the United States in 1988 and has been in use since in the therapy of symptomatic Parkinson disease, usually in combination with levodopa/carbidopa. Pergolide is available in tablets of 0.05, 0.25 and 1.0 mg in generic forms and under the brand name of Permax. The typical initiating dose of pergolide is 0.05 mg once daily for the first 2 days, with gradual increase thereafter based upon tolerance and effect. The average therapeutic dose in clinical studies was 3 mg per day given in 3 divided doses. Common side effects include profound hypotension (with the first dose), somnolence, fatigue, vivid dreams, insomnia, anxiety, confusion, depression, dizziness, headache, nausea and gastrointestinal upset.
Pergolide has been reported to cause serum aminotransferase elevations in a small proportion of patients, but these abnormalities are usually mild, asymptomatic and self-limiting even without dose adjustment. In addition, pergolide has been implicated in a small number of cases of clinically apparent, acute liver injury, but the frequency, severity, clinical characteristics and typical pattern of enzyme elevations have not been characterized. Thus, pergolide is may be a rare cause of clinically apparent liver injury.
Likelihood score: E* (unproven but suspected cause of clinically apparent liver injury).
Mechanism of Injury
Pergolide is metabolized extensively by the liver and metabolic byproducts excreted rapidly in the urine.
Outcome and Management
Most instances of suspected hepatotoxicity of pergolide have been mild and self-limited. There have been no published reports of acute liver failure or chronic hepatitis due to pergolide. There is likely cross sensitivity to hypersensitivity reactions among the different ergot alkaloids, such as bromocriptine.
REPRESENTATIVE TRADE NAMES
Pergolide – Generic, Permax®
Product labeling at DailyMed, National Library of Medicine, NIH
||CAS REGISTRY NUMBER
updated: 20 July 2017
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