Pharmacy World and Science

, Volume 15, Issue 5, pp 186–192 | Cite as

Terfenadine: A mixture of equipotent antihistamine enantiomers without a clear ‘isomeric ballast’

  • Ming-Qiang Zhang
  • Henk Timmerman


Terfenadine was the first non-sedating histamine H1 receptor antagonist and one of the most frequently prescribed H1 antihistamines. Terfenadine has one asymmetric centre in the molecule and is currently used as a racemate. Different methods and approaches for obtaining pure enantiomers of terfenadine are summarized and discussed in the present paper. Studies on antihistamine activity of the enantiomers, their side-effects on the central nervous system, calcium channel affinity and metabolism are also reviewed and analysed.


Adverse effects Calcium channels Histamine H1 receptor blockaders Metabolism Receptors, histamine H1 Resolution Stereoisomers Synthesis Terfenadine 


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Copyright information

© Periodicals Service Company 1993

Authors and Affiliations

  • Ming-Qiang Zhang
    • 1
  • Henk Timmerman
    • 1
  1. 1.Department of PharmacochemistryFree UniversityHV Amsterdamthe Netherlands

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