European Journal of Clinical Pharmacology

, Volume 12, Issue 3, pp 195–199

Inhibitory activity of terfenadine on histamine-induced skin wheals in man

  • K. J. Hüther
  • G. Renftle
  • N. Barraud
  • J. T. Burke
  • J. Koch-Weser
Originals

Summary

The inhibitory effect of orally administered terfenadine on the area of histamine-induced skin wheals was studied by single dose and multiple dose trials in 12 normal male volunteers. Single doses of 20, 60 and 200 mg of terfenadine produced dose-dependent decreases in histamine wheal area that reached a maximum by the fourth hour after dosing. The 60 and 200 mg doses blocked almost 90% of histamine whealing, and significant reduction of the wheal area persisted for 8 h. During the multiple dose trial histamine whealing was markedly inhibited after the fifth and sixth dose of terfenadine 20, 40 or 60 mg every 8 h and of 60 mg every 12 h. On the last three dosage schedules inhibition persisted for at least 12 h after the final dose. Inhibition of histamine-induced skin whealing appears to be a quantitative index of the time course of histamine H1-receptor antagonist action.

Key words

Histamine antagonists terfenadine effective doses skin wheals subjective effects 

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Copyright information

© Springer-Verlag 1977

Authors and Affiliations

  • K. J. Hüther
    • 1
  • G. Renftle
    • 2
  • N. Barraud
    • 1
  • J. T. Burke
    • 1
  • J. Koch-Weser
    • 1
  1. 1.Centre de Recherche Merrell InternationalStrasbourg CedexFrance
  2. 2.Base Hospital, German Air Force BaseBremgartenFederal Republic of Germany

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