The effect of premedication with terfenadine, an H-1 antagonist, on na
sal challenge with antigen, histamine and methacholine was evaluated.
A single dose of terfenadine had no effect on the response to a locali
zed challenge with methacholine but completely blocked the secretory r
esponse to histamine on both the ipsilateral and contralateral sides.
These results suggest that terfenadine has no anticholinergic activity
and that the direct and reflex secretory response to challenge with h
istamine is mediated by the H-1 receptor. A single dose of terfenadine
significantly reduced sneezing and nasal secretion after challenge wi
th antigen but had no effect on nasal congestion. A double-blind place
bo-controlled clinical trial was undertaken to compare the effects of
pretreatment with terfenadine for 1 week on the response to sequential
nasal challenge with antigen and histamine. Terfenadine significantly
reduced the number of sneezes and the levels of kinins, albumin and T
AME esterase activity following challenge with antigen. The levels of
histamine were also significantly reduced, suggesting inhibition of th
e degranulation of mast cells. The number of sneezes and the levels of
albumin were also significantly reduced by terfenadine following chal
lenge with histamine.