Analytical methods have been developed for the detection of a variety of compounds that are found intact or as metabolites in biological samples from workers exposed to pesticides. Such tests are used primarily in research settings to describe patterns of absorption, metabolism, and excretion, to derive exposure limits for occupational exposure, to evaluate the adequacy of these limits and of work practices in field settings, and to confirm the etiology of poisonings for medicolegal purposes. We review here methods used in studies of occupational pesticide exposure, with particular attention to validation in terms of dose-response relationships, to technical complexity and cost, to the requirements for analytical quality control, and to the utility of these methods for field research purposes. Biological monitoring for intact pesticides or metabolites in agricultural workers is limited to a few chemicals, notably, pentachlorophenol, methyl bromide, and chlordimeform. These programs and their use in regulation and enforcement are described.