Liu Y H, Qian M X, Wang X G, Quan Y Z, Yan S H, Chen B Y, Li J S, Qiu Z Y
Institute of Infections and Parasitic Diseases, Chong-qing University of Medical Sciences.
Chin Med J (Engl). 1993 Aug;106(8):593-6.
Levo-praziquantel is the left isomer of racemic praziquantel. Animal experiments showed that it is an active component of schistosomicidal activity, while dextro-praziquantel is almost ineffective. Clinical trials in three endemic areas of Schistosomiasis japonica indicated that the therapeutic efficacy of levo-praziquantel is superior to racemic praziquantel. Pharmacokinetic and pharmacodynamic activities of the stereoselectivity of praziquantel isomers (enantiomers) are discussed.
左旋吡喹酮是消旋吡喹酮的左旋异构体。动物实验表明,它是具有杀血吸虫活性的有效成分,而右旋吡喹酮几乎无效。在日本血吸虫病三个流行地区进行的临床试验表明,左旋吡喹酮的治疗效果优于消旋吡喹酮。文中讨论了吡喹酮异构体(对映体)立体选择性的药代动力学和药效学活性。