Merello M, Lees A J, Webster R, Bovingdon M, Gordin A
Department of Neurology, University College and Middlesex Hospitals School of Medicine, London, UK.
J Neurol Neurosurg Psychiatry. 1994 Feb;57(2):186-9. doi: 10.1136/jnnp.57.2.186.
Catechol-O-methyltransferase (COMT) inhibitors may be useful in the treatment of Parkinson's disease by improving the bioavailability of levodopa and by prolonging its effects. Entacapone (OR-611), a novel COMT inhibitor, which does not cross the blood brain barrier, was assessed in 12 patients with Parkinson's disease and motor fluctuations in a randomised, double-blind, cross-over, single dose study. The magnitude and duration of the therapeutic response to a single dose of 200 mg levodopa/50 mg carbidopa was evaluated after concomitant placebo, or 200 or 800 mg entacapone. A significant increase in the duration of the motor response to levodopa was seen when 200 mg entacapone was given with levodopa/carbidopa. Plasma levodopa concentrations were increased with both doses of the COMT inhibitor. The latency to onset of motor response did not differ significantly between active drug and placebo. Entacapone may prove useful in prolonging the duration of the benefit obtained from individual doses of levodopa.
儿茶酚-O-甲基转移酶（COMT）抑制剂可能通过提高左旋多巴的生物利用度及其作用持续时间，对帕金森病的治疗有益。恩他卡朋（OR - 611）是一种新型的COMT抑制剂，不能穿过血脑屏障，在一项随机、双盲、交叉、单剂量研究中，对12例患有帕金森病和运动波动的患者进行了评估。在给予安慰剂、200毫克或800毫克恩他卡朋后，评估单次服用200毫克左旋多巴/50毫克卡比多巴的治疗反应的幅度和持续时间。当200毫克恩他卡朋与左旋多巴/卡比多巴合用时，观察到左旋多巴运动反应的持续时间显著增加。两种剂量的COMT抑制剂均使血浆左旋多巴浓度升高。活性药物和安慰剂之间运动反应开始的潜伏期无显著差异。恩他卡朋可能有助于延长单次剂量左旋多巴所带来益处的持续时间。
