Studies are described on the metabolism and the toxico-logic analysis of the nonopioid Cough suppressant dropropizine [R,S-3-(4-phenyl-1-piperazinyl) 1,2-propandiol, DRO] in human urine using gas chromatography-mass spectrometry (GC-MS). The metabolisin studies showed that DRO was metabolized in humans mainly by hydroxylation of the aromatic ring, by N-dealkytation of the parent drug and of the hydroxyl-metabolite to the corresponding N-phenylpiperazines, and by degradation of the piperazine moiety. The authors' systematic toxicologic analysis (STA) procedure using full-scan GC-MS after acid hydrolysis, liquid-liquid extraction, and microwave-assisted acetylation allowed the unambiguous detection of DRO and its above-mentioned metabolites in human urine up to about 32 hours after intake of a single common therapeutic dose. The target analytes were found to be the parent compound DRO (earlier phase of excretion) and the hydroxylated metabolite para-hydroxy-DRO (later phase of excretion). Both allowed unambiguous detection of an intake of DRO and also differentiation from other phenylpiperazine derivatives.