Terfenadine: a mixture of equipotent antihistamine enantiomers without a clear 'isomeric ballast'.
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.
Zhang
M Q
MQ
Department of Pharmacochemistry, Free University, Amsterdam, The Netherlands.
Timmerman
H
H
D000818:Animals; D002490:Central Nervous System / Q000187:drug effects; D006801:Humans; D013237:Stereoisomerism; D016593:Terfenadine / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*
D016593:Terfenadine