Rasagiline is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinson’s disease. Rasagiline has been associated with a low rate of serum enzyme elevations during treatment, but has not been linked to instances of clinically apparent acute liver injury.
Rasagiline (ra sa' ji leen) is a specific inhibitor of monamine oxidase (MAO) type B which is a major enzyme in the pathway of dopamine and levodopa metabolism. As a result, rasagiline results in an increase in the bioavailability of levodopa enhancing and increasing the duration of its effects in Parkinson disease. Rasagiline was approved for use in the United States in 2007, the second MAO-B inhibitor approved for use in the therapy of Parkinson disease, and is currently approved for use monotherapy or as an adjunct to levodopa therapy. Rasagiline is available in tablets of 0.5 and 1 mg under the brand name of Azilect. Rasagiline is typically given in oral doses of 0.5 to 1 mg once daily alone or in combination with levodopa/carbidopa. Common side effects include headache, nausea, dizziness, agitation, delusions, insomnia, orthostatic hypotension, dry mouth, headache and gastrointestinal upset – most of which are attributable to enhanced dopaminergic effects.
Rasagiline has been reported to cause serum enzyme elevations in a small proportion of patients treated long term, although the abnormalities were usually mild and self-limiting. Rasagiline has not been implicated in cases of acute liver injury, but such instances have been reported with other less specific MAO inhibitors.
Likelihood score: E (unlikely cause of clinically apparent liver injury).
Mechanism of Injury
Rasagiline is extensively metabolized by the hepatic cytochrome P450 system (CYP 1A2) to inactive metabolites.
Outcome and Management
Instances of hepatotoxicity attributed to rasagiline have been mild and self-limiting elevations in serum enzymes. No instances of severe liver injury, acute liver failure, chronic hepatitis or vanishing bile duct syndrome have been linked to rasagiline use.
Other Drugs in the Subclass, Selective MAO Inhibitors: Selegiline
REPRESENTATIVE TRADE NAMES
Rasagiline – Generic, Azilect®
Product labeling at DailyMed, National Library of Medicine, NIH
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updated: 21 July 2017
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