Safety profile of enantiomers vs. racemic mixtures: it's the same?
Version of Record online: 9 OCT 2012
© 2012 The Authors. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society
British Journal of Clinical Pharmacology
Volume 74, Issue 5, pages 886–889, November 2012
How to Cite
Caillet, C., Chauvelot-Moachon, L., Montastruc, J.-L., Bagheri, H. and French Association of Regional Pharmacovigilance Centers (2012), Safety profile of enantiomers vs. racemic mixtures: it's the same?. British Journal of Clinical Pharmacology, 74: 886–889. doi: 10.1111/j.1365-2125.2012.04262.x
- Issue online: 9 OCT 2012
- Version of Record online: 9 OCT 2012
- Accepted manuscript online: 7 MAR 2012 10:43AM EST
- Received; 14 October 2011; Accepted; 26 February 2012; Accepted Article Published Online; 7 March 2012
- adverse drug reaction;
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 case–noncase 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.