Safety profile of enantiomers vs. racemic mixtures: it's the same?

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT The physicochemical properties of racemates and stereoisomers of medicines can differ significantly, and this may affect the side-effect profile in addition to the pharmacokinetics and intended pharmacology. WHAT THIS STUDY ADDS This is a study to investigate the profile of adverse drug reactions of racemic and enantiomeric forms of drugs. Our data suggest differences in the safety profile for ofloxacin and omeprazole. This area requires more work to investigate this for other compounds. AIMS The objective was to investigate the safety profile of four drugs marketed as racemic and enantiomeric forms in France. METHODS Data from the French PharmacoVigilance Data Base (January 2005 to June 2010) were analysed for four pairs of racemic/isomeric drugs. A casenoncase approach was used to measure the disproportionality of combination between adverse drug reaction (ADR) and exposure to drug. RESULTS No significant difference in the number of ADRs was observed between Rac-cetirizine/(R)-cetirizine or Rac-citalopram/(S)-citalopram pairs. (S)-Omeprazole induced more haematological effects than Rac-omeprazole. Rac-Ofloxacin induced more haematological, renal and neuropsychiatric ADRs than (S)-ofloxacin, whereas levofloxacin was associated with more reports of musculoskeletal ADRs. CONCLUSIONS The profile of ADRs could differ for some drugs marketed as racemic and enantiomeric forms. Further studies would be necessary to confirm these data.