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NEUROLOGY 2004;62:S39-S46
© 2004 American Academy of Neurology

Neurology supplements are not peer-reviewed. Information contained in Neurology supplements represent the opinions of the authors and are not endorsed by nor do they reflect the views of the American Academy of Neurology, Editor-in-Chief, or Associate Editors of Neurology.

Safety and tolerability of COMT inhibitors

David J. Brooks, MD DSc, FRCP, FMedSci

From the Faculty of Medicine, Imperial College London, United Kingdom.

Address correspondence and reprint requests to Prof. David J. Brooks, Cyclotron Building, MRC Clinical Sciences Centre, Imperial College School of Medicine, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.

Combining levodopa with the catechol-O-methyltransferase (COMT) inhibitor entacapone has been shown to be an effective strategy in the management of Parkinson’s disease (PD) patients experiencing motor fluctuations. Safety and tolerability information has come from postmarketing surveillance studies as well as several randomized, placebo-controlled trials with long-term open-label extension phases specifically investigating the safety and tolerability of levodopa plus entacapone. Results show the most common dopaminergic side effects to be dyskinesia and nausea, which result from the increased bioavailability of levodopa and can be readily managed. Non-dopaminergic side effects include diarrhea and harmless urine discoloration. There is no convincing evidence of hepatic injury with entacapone use, and therefore monitoring of liver enzymes is unnecessary. With over 300,000 patient-years of exposure, levodopa combined with entacapone can be considered safe and well tolerated.




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Drug Metab. Dispos.Home page
E. Elovaara, J. Mikkola, L. Luukkanen, L. Antonio, S. Fournel-Gigleux, B. Burchell, J. Magdalou, and J. Taskinen
ASSESSMENT OF CATECHOL INDUCTION AND GLUCURONIDATION IN RAT LIVER MICROSOMES
Drug Metab. Dispos., December 1, 2004; 32(12): 1426 - 1433.
[Abstract] [Full Text] [PDF]




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