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

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Abstract

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.

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Authors and Affiliations

  1. Department of Pharmacochemistry, Free University, De Boelelaan 1083, 1081, HV Amsterdam, the Netherlands

    Ming-Qiang Zhang &  Henk Timmerman

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  1. Ming-Qiang Zhang
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  2. Henk Timmerman
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Zhang, MQ., Timmerman, H. Terfenadine: A mixture of equipotent antihistamine enantiomers without a clear ‘isomeric ballast’. Pharm World Sci 15, 186–192 (1993). https://doi.org/10.1007/BF01880624

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