Pharmacokinetics of pyrethroids in twospotted spider mites

The penetration and degradation of six pyrethroids were examined in the twospotted spider mite, Tetranychus urticae Koch, and the results were related to their toxicity as measured by inhibition of respiration using the Warburg technique and mortality using the slide-dip bioassay. FMC-54800 1,1′-biphenyl-3ylmethyl cis-3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropanecarboxylate] was the most toxic pyrethroid to the mites based on both respiration and mortality studies. It and flucythrinate had the highest pharmacokinetic efficiency as determined by delivery and maintenance of internal levels of parent compounds. Permethrin, fenvalerate, and fluvalinate were intermediate in pharmacokinetic efficiency, whereas cypermethrin was significantly lower. The highest intrinsic activity, as estimated by the percentage inhibition of respiration per microgram of internal parent, was possessed by cypermethrin and FMC-54800. Fenvalerate and fluvalinate had intermediate levels, while permethrin and flucythrinate had significantly lower capacities to inhibit respiration. The combination of relatively high pharmacokinetic efficiency and intrinsic activity of FMC-54800 appeared to be responsible for its high toxicity. In addition to these findings, differences in the kinetics for cis and trans isomers were observed for permethrin but not cypermethrin. This study has yielded evidence that acaricidal activity of pyrethroids can be enhanced by optimizing the structure for increased pharmacokinetic efficiency and increased intrinsic activity.