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


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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  1. 1.
    Kinsolving, C.R., Munro, N.L., Carr, A.A.: Separation of the CNS and H1 Receptor effects of antihistamine agents. Pharmacologist15, 221 (1973)Google Scholar
  2. 2.
    Bain, W.A.: The quantitative comparison of histamine antagonists in man. Proc. Roy. Soc. Med.42, 615–623 (1949)Google Scholar
  3. 3.
    Green, A.M.: One year's experience with sustained release antihistamine medication. Ann. Allergy12, 273–283 (1954)Google Scholar
  4. 4.
    Dundas, E., Toogood, J.H., Wanklin, J.: Inhibition of experimental skin wheal by some ataractic and antihistaminic drugs. J. Allergy32, 1–7 (1961)Google Scholar
  5. 5.
    Kerp, L., Kasemir, H., Tie, P.N.: Prüfung des Antihistamins HS 592 (Tavegil) am Histamin-bezw. “48/80” — Erythem und bei Patienten mit allergischen Sofortreaktionen. Med. Welt1966, 2794–2798Google Scholar
  6. 6.
    Joubert, L., Gaut, Z., Abrams, W.B.: A new approach to the use of histamine skin tests in the study of antihistamine drugs. Clin. Pharmacol. Ther.10, 250–257 (1969)Google Scholar
  7. 7.
    Fowle, A.S.E., Hughes, D.T.D., Knight, G.J.: The evaluation of histamine antagonists in man. Europ. J. Clin. Pharmacol.3, 215–220 (1971)Google Scholar
  8. 8.
    Bilzer, W., Gundert-Remy, U., Weber, E.: Relationship between antihistaminic activity and plasma level of diphenhydramine. Europ. J. clin. Pharmacol.7, 393–395 (1974)Google Scholar
  9. 9.
    Petrin, A.: Experiment on healthy volunteers with the new antihistamine 22–914 (Sandoz) Int. J. clin. Pharmacol.12, 199–201 (1975)Google Scholar
  10. 10.
    Peck, A.W., Fowle, A.S.E., Bye, C.: A comparison of triprolidine and clemastine on histamine antagonism and performance tests in man: implications for the mechanism of drug induced drowsiness. Europ. J. clin. Pharmacol.8, 455–463 (1975)Google Scholar
  11. 11.
    Carruthers S.G., Shoeman, D.W., Azarnoff, D.L.: Effects of diphendydramine (D) in man after single oral (DO) and intravenous (DI) doses. Clin. Res.24, 4, 562 A (1976)Google Scholar

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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