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[吡喹酮治疗中枢神经系统囊尾蚴病患者脑脊液和血浆中吡喹酮水平的测定]

[Determination of praziquantel levels in cerebrospinal fluid and plasma in patients with cysticercosis of the central nervous system treated with praziquantel].

作者信息

Jia J Y

机构信息

Dept of Internal Medicine, 268th Hospital of PLA.

出版信息

Zhonghua Shen Jing Jing Shen Ke Za Zhi. 1991 Jun;24(3):174-6, 189-90.

PMID:1889331
Abstract

The CSF and plasma concentrations of praziquantel (PZQ) were determined with high pressure liquid chromatography in 37 patients with cysticercosis of the central nervous system during a dosing regimen of PZQ 20 mg/kg p o q 8h for 3 days. The pharmacokinetic parameters were estimated using the nonlinear least squares method. The results showed that PZQ could pass through the blood-brain barrier. The absorption and elimination rates in CSF were slower than those in plasma, the corresponding mean levels being 0.1 and 0.27 micrograms/ml, which were lower than those in plasma. There was a linear correlation between CSF and plasma concentrations (r = 0.87, P less than 0.01). The neurological complications during the period of therapy were not related to the CSF level of PZQ. The cure rates of muscular and cerebral cysticerci were 14/14 and 5/37 respectively. The difference in susceptibility was considered to be caused by the pharmacokinetic behavior of PZQ and CSF and plasma. It was suggested that in general favorable regimens had better be adjusted with adequate increase of the dosage of PZQ, shortening the dosing interval, and prolong the period of PZQ treatment, but individualization of the PZQ dosing regiment would be necessary in accordance with the plasma concentration of the PZQ.

摘要

采用高压液相色谱法测定了37例中枢神经系统囊尾蚴病患者在口服吡喹酮(PZQ)20mg/kg、每8小时1次、共3天的给药方案期间脑脊液和血浆中PZQ的浓度。使用非线性最小二乘法估算药代动力学参数。结果显示PZQ能够透过血脑屏障。脑脊液中的吸收和消除速率比血浆中的慢,相应的平均水平分别为0.1和0.27微克/毫升,低于血浆中的水平。脑脊液和血浆浓度之间存在线性相关性(r = 0.87,P<0.01)。治疗期间的神经并发症与脑脊液中PZQ水平无关。肌肉和脑囊尾蚴的治愈率分别为14/14和5/37。易感性差异被认为是由PZQ以及脑脊液和血浆的药代动力学行为所致。建议一般而言,较好的治疗方案最好通过适当增加PZQ剂量、缩短给药间隔以及延长PZQ治疗时间来调整,但根据PZQ的血浆浓度对PZQ给药方案进行个体化调整是必要的。

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