The focus of this chapter is on pesticides, which play a significant role in controlling pests in agriculture, crop production, and crop protection. Nevertheless, it is important to keep in mind that pesticides can lead to contamination of environmental media, bioaccumulate in the food chain, and pose potential health risks to nontarget organisms, as well as to humans. Therefore, this chapter provides a brief description of the chemical and physical characteristics and usage patterns of various pesticides, their primary health risks, and toxicokinetic properties, along with references to further scientific literature. The primary objective is to present a detailed overview of their occurrence in human matrices, such as blood, urine, and breast milk. In this context, detailed information is provided on organophosphate pesticides, carbamates and dithiocarbamates, glyphosate and glufosinate, pyrethroids and pyrethrins, neonicotinoids, toxaphenes, and the insect repellent N,N-diethyl-meta-toluamide (DEET).