Jung H, Medina R, Castro N, Corona T, Sotelo J
Instituto Nacional de Neurologia y Neurocirugia and Universidad Nacional Autonoma de Mexico, Mexico City.
Antimicrob Agents Chemother. 1997 Jun;41(6):1256-9. doi: 10.1128/AAC.41.6.1256.
A brief therapeutic regimen of praziquantel, reduced to a single day, has been effective for treatment of neurocysticercosis. To study its pharmacokinetic characteristics, levels of praziquantel in plasma were determined for eight healthy volunteers after the administration of three oral doses of 25 mg/kg of body weight given at 2-h intervals, alone and with the simultaneous administration of cimetidine. Each volunteer received both regimens in a randomized crossover design. Blood samples were taken during a period of 12 h, and praziquantel concentration was measured by high-performance liquid chromatography. Levels of praziquantel in plasma remained above 300 ng/ml during a period of 12 h; they increased 100% when cimetidine was jointly administered. Compared with other regimens, the high levels obtained and the longer duration of action seem to be advantageous in prolonging the exposure of the parasites to the drug and support previous clinical experience showing that the treatment of neurocysticercosis with praziquantel can be reduced from 2 weeks to 1 day with the drug still retaining its cysticidal properties. Moreover, simultaneous administration of praziquantel and cimetidine could improve further the efficacy of the single-day therapy for cysticercosis and other parasitic diseases, such as schistosomiasis.
吡喹酮简化为单日给药的简短治疗方案已被证明对治疗神经囊尾蚴病有效。为研究其药代动力学特征，对8名健康志愿者进行了研究，他们分别单次口服给予3剂25mg/kg体重的吡喹酮（每2小时间隔给药），一次单独给药，一次同时给予西咪替丁。每位志愿者均按随机交叉设计接受这两种给药方案。在12小时内采集血样，采用高效液相色谱法测定吡喹酮浓度。血浆中吡喹酮水平在12小时内均保持在300ng/ml以上；同时给予西咪替丁时，其水平增加了100%。与其他给药方案相比，所获得的高血药浓度和更长的作用持续时间似乎有利于延长寄生虫与药物的接触时间，这也支持了先前的临床经验，即吡喹酮治疗神经囊尾蚴病的疗程可从2周缩短至1天，且该药仍保留其杀囊尾蚴特性。此外，同时给予吡喹酮和西咪替丁可进一步提高治疗囊尾蚴病及其他寄生虫病（如血吸虫病）的单日疗法的疗效。
