Valencia C I, Catto B A, Webster L T, Barcelon E, Ofendo-Reyes R
Department of Pharmacology, College of Medicine, University of the Philippines, Manila.
Southeast Asian J Trop Med Public Health. 1994 Jun;25(2):409-14.
Despite extensive use of praziquantel, the current drug of choice for the treatment of schistosomiasis and other helminthic infections, little information is available about its pharmacokinetics in individuals living in geographic areas where such infections are endemic. We investigated the pharmacokinetics of praziquantel by determining its serum concentration-time course in four selected Filipino volunteers with mild Schistosoma japonicum infection who lived in an endemic area in the Southern Philippines. At specified intervals during a 24-hour time period after a single oral dose of praziquantel (25 mg/kg BW), intravenous samples of blood were drawn, processed and analyzed for praziquantel using reverse phase high pressure liquid chromatography. The same study was repeated one week later to assess pharmacokinetic reproducibility. A third study, simulating current field practice, consisted of dosing the patient four hours apart and analyzing for praziquantel in serial blood samples drawn at specified time intervals after the first and second dose. The following results were obtained: 1) Serum concentration-time course of praziquantel was reproducible for each patient but varied from patient to patient. 2) Praziquantel was rapidly absorbed in the gastrointestinal tract as measurable amounts appeared in the blood as early as 15 minutes after dosing. Time to peak serum concentration ranged from 1.50 to 6.00 hours with almost complete elimination from blood by 24 hours whether it was administered as a single dose (1 x 25 mg/kg BW) or as a twice a day dose (2 x 25 mg/kg BW) 4 hours apart. Half-life values ranged from 1.00 to 2.50 hours.(ABSTRACT TRUNCATED AT 250 WORDS)
尽管吡喹酮是目前治疗血吸虫病和其他蠕虫感染的首选药物且应用广泛,但关于其在这些感染流行地区居民体内的药代动力学信息却很少。我们通过测定4名轻度日本血吸虫感染的菲律宾志愿者(居住在菲律宾南部的一个流行地区)的血清浓度-时间过程,研究了吡喹酮的药代动力学。在单次口服吡喹酮(25mg/kg体重)后的24小时内,在特定时间间隔采集静脉血样,处理后用反相高压液相色谱法分析吡喹酮。一周后重复相同研究以评估药代动力学的可重复性。第三个研究模拟当前现场实践,即每隔4小时给患者给药一次,并在第一剂和第二剂后的特定时间间隔采集系列血样分析吡喹酮。得到以下结果:1)吡喹酮的血清浓度-时间过程对每位患者是可重复的,但患者之间存在差异。2)吡喹酮在胃肠道迅速吸收,给药后15分钟血液中就出现可测量的量。血清浓度达峰时间为1.50至6.00小时,无论单次给药(1×25mg/kg体重)还是间隔4小时每日两次给药(2×25mg/kg体重),24小时时血液中几乎完全消除。半衰期值为1.00至2.50小时。(摘要截短于250字)