Kani F, Gayral P, Pfaff-Dessales M C, Mahuzier G, Jacquot C, Auget J L
Eur J Drug Metab Pharmacokinet. 1983 Oct-Dec;8(4):313-20. doi: 10.1007/BF03188763.
The pharmacokinetic parameters of diethylcarbamazine were compared in the plasma and peritoneal fluid of 5 non-infected rodents. In the filarial animals, the absorption rate constant and the elimination rate constant were significantly increased. The peak plasma concentration was twofold higher in the infested rodents than the control animals, and this may account for the rapid action of diethylcarbamazine on blood-circulating microfilariae. The area under the curve was unchanged. Total clearance is slightly increased in filarial rodents. These data are explained by an important reduction of renal clearance combined with a moderate increase of extra renal clearance. High levels of diethylcarbamazine in peritoneal fluid, resulting from the excellent diffusion of the drug in filarial animals explains the activity on adult worms. But the parasitism does not affect the mechanism of distribution of the drug between plasma and peritoneal liquid.
在5只未感染的啮齿动物中比较了乙胺嗪在血浆和腹膜液中的药代动力学参数。在感染丝虫的动物中，吸收速率常数和消除速率常数显著增加。受感染啮齿动物的血浆峰值浓度比对照动物高两倍，这可能解释了乙胺嗪对血液循环中的微丝蚴的快速作用。曲线下面积没有变化。丝虫感染的啮齿动物的总清除率略有增加。这些数据可以通过肾清除率的显著降低和肾外清除率的适度增加来解释。由于药物在感染丝虫的动物中具有良好的扩散性，腹膜液中乙胺嗪的高浓度解释了其对成虫的活性。但寄生虫感染并不影响药物在血浆和腹膜液之间的分布机制。
