Jh. Day et al., ONSET OF ACTION AND EFFICACY OF TERFENADINE, ASTEMIZOLE, CETIRIZINE, AND LORATADINE FOR THE RELIEF OF SYMPTOMS OF ALLERGIC RHINITIS, Annals of allergy, asthma, & immunology, 79(2), 1997, pp. 163-172
Background: Terfenadine, astemizole, cetirizine, and loratadine are co
mpared in their abilities to produce relief of symptoms of allergic rh
initis. Objective: 111 ragweed-sensitive subjects were primed with pol
len in the Environmental Exposure Unit. Study entry required adequate
symptoms over a 3 hour exposure to 5000 +/- 300 grains/m(3) of ragweed
pollen. On the test day, subjects were given a single dose of either
terfenadine 60 mg (22), astemizole 10 mg (22), cetirizine 10 mg (23),
loratadine 10 mg (22), or placebo (22) when sufficiently symptomatic a
fter a 60-minute exposure. Allergen levels were maintained and symptom
s recorded every 30 minutes. Results: Proportions of subjects with cli
nically important relief were cetirizine, 69.6%; terfenadine, 54.5%; l
oratadine, 50.0%; astemizole, 40.9%; and placebo, 31.8% but difference
s weren't significant between treatment groups (P = .119). Survival cu
rves for times to onset of clinically important relief for the four tr
eatment groups were not different (P = .119). Subjects realizing defin
itive relief were cetirizine, 65.2%; terfenadine, 45.5%; loratadine, 3
1.8%; placebo, 27.3%; and astemizole, 22.7% (P = .023). Survival analy
sis of onset time for definitive relief found significant differences
(P = .010). The ranking was cetirizine --> terfenadine --> loratadine
--> astemizole (quickest to slowest). Global evaluation based on subje
ct willingness to take the medication again yielded percentages: cetir
izine, 82.6%; terfenadine, 66.7%; astemizole, 63.6%; loratadine, 40.9%
; and placebo, 36.4% (P = .036). Conclusion: Cetirizine and terfenadin
e continuously ranked higher in terms of onset of action and efficacy,
while loratadine and astemizole ranked lower. Significance was detect
ed in definitive relief and relative efficacy.