The effect of histamine-H1 receptor antagonism with terfenadine on concentration-related AMP-induced bronchoconstriction in asthma

Clin Exp Allergy. 1989 Jul;19(4):405-9. doi: 10.1111/j.1365-2222.1989.tb02406.x.


Selective histamine-H1 receptor antagonists inhibit adenosine 5'-monophosphate (AMP)-induced bronchoconstriction by greater than 80% when expressed as a percentage inhibition of the FEV1 time-response curve following inhalation of the provocation concentration of AMP required to produce a 20% decrease in FEV1 from baseline (PC20). To investigate this further we have determined that, in eight mild atopic asthmatic subjects, terfenadine (180 mg), administered 3 hr pre-challenge, increases the geometric mean PC20 for histamine from 0.4 (range 0.03-3) mg/ml after placebo, to 20.2 (range 0.6-64) mg/ml following active treatment (P less than 0.0001). For AMP, the PC20 increased from 9.3 (range 1.0-113.3) mg/ml after placebo, to 150.2 (range 32.1-1177.7) mg/ml with terfenadine (P less than 0.0001). This 16.2-fold (range, 5.5-47.9) displacement to the right of the AMP concentration-response curve by a selective histamine-H1 receptor antagonist emphasizes the central role of histamine in the airways response to this nucleotide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Asthma / immunology*
  • Benzhydryl Compounds / administration & dosage
  • Benzhydryl Compounds / pharmacology*
  • Bronchial Spasm / chemically induced
  • Bronchial Spasm / immunology*
  • Cyclic AMP / antagonists & inhibitors*
  • Double-Blind Method
  • Female
  • Forced Expiratory Volume
  • Histamine H1 Antagonists / administration & dosage
  • Histamine H1 Antagonists / pharmacology*
  • Humans
  • Male
  • Mast Cells / immunology
  • Random Allocation
  • Receptors, Histamine H1 / drug effects*
  • Receptors, Histamine H1 / immunology
  • Terfenadine


  • Benzhydryl Compounds
  • Histamine H1 Antagonists
  • Receptors, Histamine H1
  • Terfenadine
  • Cyclic AMP