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January 1, 1988Xenobiotica

Human dose-excretion studies with pyrethroid insecticides cypermethrin and alphacypermethrin: Relevance for biological monitoring

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Authors

CEC. V. EadsforthShell (United States)PBPeter C. BragtMinistry of Health Welfare and SportNSN J van SittertLeiden University

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Implication

Experimental dose-excretion study reveals rapid oral metabolite elimination but minimal dermal absorption of cypermethrin in human volunteers, highlighting constraints for biological monitoring.

Key Points

  • Determine the excretion kinetics of cypermethrin and alphacypermethrin metabolites in human urine following oral and dermal exposures to assess their suitability for biomonitoring.
  • Administered single oral doses (0.25 mg, 0.50 mg, 0.75 mg) and 5-day repeated oral doses of alphacypermethrin to healthy volunteers (n=2 per dose level).
  • Tested 5-day repeated oral cypermethrin doses (0.25 mg, 0.75 mg, 1.5 mg) and a single dermal forearm dose of 25 mg cypermethrin in volunteers (n=2 per dose level).
  • Collected and analyzed urine samples for free and conjugated 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylic acid metabolites before and across 24 to 72 hours after dosing.
  • Following a single oral dose of alphacypermethrin, an average of 43% of the dose was excreted as cyclopropanecarboxylic acid within 24 hours, with 49% excreted in subsequent 24-hour windows during repeated dosing without accumulation.
  • Repeated oral cypermethrin resulted in no metabolite accumulation, clearing an average of 72% of the trans isomer and 45% of the cis isomer in urine across subsequent 24-hour periods.
  • Only approximately 0.1% of the 25 mg dermal cypermethrin application appeared in urine as cyclopropanecarboxylic acid over 72 hours.

Cite This Study

Eadsforth et al. (1988) studied this question.

synapsesocial.com/papers/6a9bad730b0288a0688fec2dhttps://doi.org/10.3109/00498258809041697
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Also Consider

Synapse has enriched 4 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Drug Metabolism and Disposition2014 · 2,519 citations
  2. 2In vivo percutaneous absorption and decontamination of pesticides in humans1985 · 117 citations
  3. 3Human dose-excretion studies with the pyrethroid insecticide, cypermethrin1983 · 86 citations
  4. 4The metabolism of the pyrethroid insecticide cypermethrin in rats; excreted metabolites1981 · 58 citations