This paper reviews systematic toxicological analysis (STA) procedures for acidic drugs and/or metabolites relevant to clinical and forensic toxicology or doping control using gas chromatography, gas chromatography-mass spectrometry, liquid chromatography, thin-layer chromatography and capillary electrophoresis. Papers from 1992 to 1998 have been taken into consideration. Screening procedures in biosamples (whole blood, plasma, serum, urine, vitreous humor, brain, liver or hair) of humans or animals (horse, or rat) are included for the following drug classes: angiotensin-converting enzyme (ACE) inhibitors and angiotensin II (AT-II) blockers, anticoagulants of the 4-hydroxy coumarin type, barbiturates, dihydropyridine calcium channel blockers (calcium antagonists), diuretics, hypoglycemic sulfonylureas and non-steroidal anti-inflammatory drugs (NSAIDs). Methods for confirmation of preliminary results obtained by screening procedures using immunoassay or chromatographic techniques are also included. Furthermore, procedures for the simultaneous detection of several drug classes are reviewed. The toxicological question to be answered and the consequences for the choice of an adequate method, the sample preparation and the chromatography itself are discussed. The basic information about the biosample assayed, work-up, separation column, mobile phase or separation buffer, detection mode and validation data of each procedure is summarized in 16 tables. They are arranged according to the drug class and the analytical method. Examples of typical applications are presented. Finally, STA procedures are reviewed and described allowing simultaneous screening for different (acidic) drug classes.