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PMID: 10051176: New, selective COMT inhibitors for PD
New, selective catechol-O-methyltransferase inhibitors as therapeutic agents Levodopa remains the most effective drug for Parkinson's disease (PD). However, its benefits are limited owing to extensive metabolism by catechol-O-methyltransferase (COMT), especially if levodopa is used in combination with peripheral dopa-decarboxylase inhibitors. A new generation of potent, orally active, selective, and reversible COMT inhibitors has become available recently. Among these, tolcapone and entacapone have been best characterised. Preclinical and clinical studies have shown that COMT inhibitors markedly enhance levodopa availability and prolong its plasma half-life. In recent large clinical trials they proved to be able to ameliorate motor fluctuations, reduce disability, and decrease levodopa requirements in PD patients. The tolerability profiles of entacapone and tolcapone are good. COMT inhibition promises to become an important means of extending the benefits of levodopa therapy in PD. Pharmacol Ther 1999 Jan;81(1):1-36 in Parkinson's disease. Bonifati V, Meco G Department of Neurosciences, University La Sapienza, Rome, Italy. PMID: 10051176, UI: 99158485 <> janet paterson 52 now / 41 dx / 37 onset 613 256 8340 po box 171 almonte ontario canada K0A 1A0 a new voice: <> <janet313@xxxxxxxxxxx>
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