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

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Abstract
Selective histamine‐H1 receptor antagonists inhibit adenosine 5′‐monophosphate (AMP)‐induced bronchoconstriction by > 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 (P20 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 (P1 receptor antagonist emphasizes the central role of histamine in the airways response to this nucleotide.