Azelastine, a phthalazinone compound, is a second generation histamine
H-1 receptor antagonist which has shown clinical efficacy in relievin
g the symptoms of allergic rhinitis when administered as either an ora
l or intranasal formulation. It is thought to improve both the early a
nd late phase symptoms of rhinitis through a combination of antihistam
inic, antiallergic and anti-inflammatory mechanisms. Symptom improveme
nts are evident as early as 30 minutes after intranasal administration
of azelastine [2 puffs per nostril (0.56 mg)] and are apparent for up
to 12 hours in patients with seasonal allergic rhinitis (SAR). The ef
fect on nasal blockage is variable: in some studies objective and/or s
ubjective assessment showed a reduction in blockage, whereas in other
studies there was no improvement. Intranasal azelastine 1 puff per nos
tril twice daily is generally as effective as standard doses of other
antihistamine agents including intranasal levocabastine and oral cetir
izine, ebastine, loratadine and terfenadine at reducing the overall sy
mptoms of rhinitis. The relative efficacies of azelostine and intranas
al corticosteroids (beclomethasone and budesonide) remain unclear. How
ever, overall, the corticosteroids tended to improve rhinitis symptoms
to a greater extent than the antihistamine. Azelastine was well toler
ated in clinical trials and postmarketing surveys. The most frequently
reported adverse events were bitter taste, application site irritatio
n and rhinitis. The incidence of sedation did not differ significantly
between azelastine and placebo recipients and a preliminary report sh
owed cardiovascular parameters were not significantly altered in patie
nts with perennial allergic rhinitis (PAR). Conclusion: Twice-daily in
tranasal azelastine offers on effective and well tolerated alternative
to other antihistamine agents currently recommended for the symptomat
ic relief of mild to severe SAR and PAR in adults and children (aged g
reater than or equal to 12 years in the US; aged greater than or equal
to 6 years in some European countries including the UK). The rapid on
set, confined topical activity and reduced sedation demonstrated by th
e intranasal formulation of azelastine may offer an advantage over oth
er antihistamine agents, although this has yet to be confirmed.