Wiseman L R, Brogden R N
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1998 Mar;12(3):243-8; discussion 249-50. doi: 10.2165/00002512-199812030-00006.
Propionyl-L-carnitine stimulates energy production in ischaemic muscles by increasing citric acid cycle flux and stimulating pyruvate dehydrogenase activity. The free radical scavenging activity of the drug may also be beneficial. Propionyl-L-carnitine improves coagulative fibrinolytic homeostasis in vasal endothelium and positively affects blood viscosity. Improvements in maximum walking distance (MWD) correlated positively with increased mitochondrial oxidative adenosine triphosphate (ATP) synthesis in a study in patients with peripheral arterial disease. Oral propionyl-L-carnitine 1 to 3 g/day significantly improved mean MWD compared with placebo in patients with peripheral arterial obstructive disease (Fontaine Leriche stage II) in double-blind multicentre phase III studies (mean improvements ranged from 21 to 50% with placebo and from 33 to 73% with propionyl-L-carnitine). In one phase III study, propionyl-L-carnitine 1 to 3 g/day significantly improved mean MWD (measured by treadmill) compared with placebo (by 73 vs 46% after 24 weeks) in patients with intermittent claudication. Oral propionyl-L-carnitine therapy was associated with significant improvements in quality of life compared with placebo in patients with a baseline MWD < 250m. Propionyl-L-carnitine appears to be well tolerated, showing a similar incidence of adverse events to that reported in placebo recipients.
丙酰-L-肉碱通过增加柠檬酸循环通量和刺激丙酮酸脱氢酶活性来刺激缺血肌肉中的能量产生。该药物的自由基清除活性可能也有益处。丙酰-L-肉碱可改善血管内皮中的凝血纤溶稳态，并对血液粘度产生积极影响。在一项针对外周动脉疾病患者的研究中，最大步行距离（MWD）的改善与线粒体氧化三磷酸腺苷（ATP）合成增加呈正相关。在双盲多中心III期研究中，对于外周动脉阻塞性疾病（Fontaine Leriche II期）患者，口服丙酰-L-肉碱1至3克/天与安慰剂相比，显著改善了平均MWD（安慰剂组平均改善幅度为21%至50%，丙酰-L-肉碱组为33%至73%）。在一项III期研究中，对于间歇性跛行患者，丙酰-L-肉碱1至3克/天与安慰剂相比，显著改善了平均MWD（通过跑步机测量）（24周后分别为73%和46%）。对于基线MWD < 250m的患者，与安慰剂相比，口服丙酰-L-肉碱治疗可显著改善生活质量。丙酰-L-肉碱似乎耐受性良好，不良事件发生率与安慰剂组报告的相似。
