Rm. Naclerio, THE EFFECT OF ANTIHISTAMINES ON THE IMMEDIATE ALLERGIC RESPONSE - A COMPARATIVE REVIEW, Otolaryngology and head and neck surgery, 108(6), 1993, pp. 723-730
Antihistamines are believed to reduce the sneezing and rhinorrhea asso
ciated with allergic rhinitis, primarily by competitive antagonism of
histamine for H-1 cellular receptors, but additional mechanisms of act
ion may contribute to their clinical efficacy. To improve our understa
nding of H-1 antihistamine action, we studied the effects of pretreatm
ent with terfenadine, cetirizine, ketotifen, azatadine, diphenhydramin
e, and azelastine on increases in vascular permeability, mast cell act
ivation, and sneezing induced by nasal challenge with antigen. All stu
died antihistamines reduced sneezing, indicating that they all effecti
vely antagonize histamine after its release. In addition, terfenadine
and topically administered azatadine blocked the release of histamine.
Studies with cetirizine and azelastine revealed that these antihistam
ines significantly reduced sulfidopeptide leukotriene levels. Terfenad
ine and azelastine also reduced kinin production. These results confir
m that antihistamines are effective in reducing sneezing and, in some
cases, vascular permeability. The findings of these studies also illus
trate that the various antihistamines have multiple and different mech
anisms of action that may hove implications for their clinical uses.