The emergence of ever new drugs of abuse on the illicit drug market is an ongoing challenge for analytical toxicologists. Because most of these new drugs or drug classes are not detected by established analytical methods targeting classic drugs of abuse, analytical procedures must be adapted or new procedures must be developed to cover these new compounds. This review summarizes the analytical toxicology of the following classes of emerging drugs of abuse: piperazines, phenethylamines (2Cs and FLYs), 4-substituted amphetamines, β-keto-amphetamines, 2,5-dimethoxy-amphetamines, pyrrolidinophenones, and synthetic cannabinoids.