HUMAN DOSE-EXCRETION STUDIES WITH PYRETHROID INSECTICIDES CYPERMETHRIN AND ALPHACYPERMETHRIN - RELEVANCE FOR BIOLOGICAL MONITORING
HUMAN DOSE-EXCRETION STUDIES WITH PYRETHROID INSECTICIDES CYPERMETHRIN AND ALPHACYPERMETHRIN - RELEVANCE FOR BIOLOGICAL MONITORING
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DOI：
10.3109/00498258809041697
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发表时间：
1988-05-01
期刊：
影响因子：
1.8
通讯作者：
VANSITTERT, NJ
中科院分区：
文献类型：
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作者：
EADSFORTH, CV;BRAGT, PC;VANSITTERT, NJ
对氯氰菊酯（顺式/反式混合物1：1）和α-氯氰菊酯（构成顺式氯氰菊酯的两种灾难性对映异构体之一）进行了剂量排泄研究，每种情况下，每个剂量水平有两名志愿者。这些研究包括：（a）单次口服0.25毫克和0.75毫克的氯氰菊酯，然后每天重复口服相同剂量的氯氰菊酯，持续5天;（B）每天重复口服0.25毫克、0.75毫克和1.5毫克的氯氰菊酯，持续5天;（c）前臂皮肤单次施用25毫克的氯氰菊酯。在给药前后监测尿液中游离和结合的3-（2，2-二氯乙烯基）-2，2-二甲基环丙烷羧酸。单次口服氯氰菊酯的代谢和排泄率与顺式氯氰菊酯相似，平均43%的剂量在前24 h尿液中以环丙烷羧酸形式排泄。当氯氰菊酯重复口服给药时，尿代谢物排泄量没有增加。受试者在给药后24小时内平均排泄49%的环丙烷羧酸。当氯氰菊酯作为重复口服剂量给药时，尿环丙烷羧酸排泄量没有增加。给药后24小时内，受试者平均分别排泄72%的反式异构体剂量和顺式异构体剂量的45%。约0.1%的应用皮肤剂量的25毫克氯氰菊酯在72小时内排泄的尿环丙烷羧酸。从尿排泄数据中无法得出关于氯氰菊酯及其代谢物在皮肤或其他器官中的浓度或其他代谢或排泄途径的可能性的结论。
Dose-excretion studies with cypermethrin (as a 1:1 cis/trans mixture) and alpha-cypermethrin (one of the two disastereoisomer pairs which constitute cis cypermethrin) were carried out with, in each case, two volunteers per dose level. The studies included (a) single oral alphacypermethrin doses of 0.25 mg and 0.75 mg followed by repeated alphacypermethrin doses at the same levels, daily for five days, (b) repeated oral cypermethrin doses of 0.25 mg, 0.75 mg and 1.5 mg daily for five days, and (c) a single dermal application of 25 mg cypermethrin to the forearm. Urine was monitored for the free and conjugated 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylic acid before and after dosing. Metabolism and rate of excretion of a single oral dose of alphacypermethrin was similar to that of cis cypermethrin, on average, 43% of the dose was excreted as the cyclopropanecarboxylic acid in the first 24 h urine. There was no increase in urinary metabolite excretion when alphacypermethrin was administered as a repeated oral dose. Subjects excreted, on average, 49% of the dose as the cyclopropanecarboxylic acid in the subsequent 24 h periods after dosing. There was no increase in the urinary cyclopropanecarboxylic acid excretion when cypermethrin was administered as a repeated oral dose. Subjects excreted, on average, 72% of the trans isomer dose and 45% of the cis isomer dose respectively in the subsequent 24 h periods after dosing. Approximately 0.1% of the applied dermal dose of 25 mg cypermethrin was excreted within 72 h as the urinary cyclopropanecarboxylic acid. No conclusions can be drawn from such urinary excretion data as to the concentration of cypermethrin and its metabolites in the skin or other organs, or the possibility of other routes of metabolism or excretion.