The current risk assessment of human exposure to low-level pyrethroids (PYRs) is generally based on the estimation of residue intake from diets. Limited data are available on individual exposure levels in human studies, which is partly attributable to the difficulty in biological monitoring of PYR exposure. This obstacle has been overcome in recent years due to the evolution of analytical chemistry. Separation and sensitive identification and quantitation of urinary PYR metabolites are today reliably made with liquid chromatography-mass spectrometry and gas chromatography-mass spectrometry. This article gives an overview of the biological monitoring of urinary PYR metabolites, reviews PYR metabolite levels in general populations, and discusses future research perspectives in the field of environmental health.