picumast and Rhinitis--Allergic--Seasonal

The efficacy of picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarine++ + dihydrochloride) in a dosage of 2 mg o.d. (loading dose = 2 b.i.d. over the first three days) vs. placebo after nasal challenge was investigated in 20 patients with allergic rhinitis in a double-blind, controlled crossover study. The primary objective was the decrease in determinable nasal flow as a result of obstruction caused by swelling of the mucous membrane of the nose following nasal challenge with grass pollen. In addition, picumast dihydrochloride's effect on subjective symptoms elicited by nasal challenge, such as "runny nose" and "irritation", was also assessed. Picumast dihydrochloride's ability to inhibit nasal obstruction after challenge was significantly better than that of placebo in statistical terms. Nasal secretion after challenge with grass pollen was far less pronounced with picumast dihydrochloride than placebo. A positive effect on irritation was not seen after nasal challenge. The results of this study show that picumast dihydrochloride inhibits nasal obstruction and secretion in patients allergic to grass pollens following allergen challenge. It is also expected that picumast dihydrochloride will be able to clearly reduce allergic nasal reactions during times of natural, seasonally-high pollen counts.

Topics: Adult; Coumarins; Double-Blind Method; Histamine H1 Antagonists; Humans; Manometry; Middle Aged; Mucus; Nasal Mucosa; Regional Blood Flow; Rhinitis, Allergic, Seasonal; Sneezing

Of 99 evaluable patients with seasonal allergic rhinitis, 33, 35, and 31 were treated with picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorbenzyl)piperazine-1-yl]propoxycoumar in dihydrochloride) 1 mg, terfenadine 60 mg, and placebo, respectively, twice daily for 3 weeks. After 7 days' treatment physicians' assessments of symptomatic improvement showed that the effects of the two active drugs were similar and significantly superior to those of placebo. Some further improvement occurred over the remainder of the study, with no significant differences in efficacy appearing between picumast dihydrochloride and terfenadine. After 2 and 3 weeks of treatment the efficacies of both picumast dihydrochloride and terfenadine were "very good/good" in over 90% of patients. The tolerability of all three treatments was classified as "very good" in 60% to 70% of patients. Physicians were prepared to represcribe the study medication in about 90% of patients given picumast dihydrochloride or terfenadine compared with 52% administered placebo. Similar assessments performed by the patients generally agreed with these results. Withdrawal due to lack of efficacy occurred in 13, 2 and 0 patients treated, respectively, with placebo, terfenadine, or picumast dihydrochloride. Few adverse effects were reported. It is concluded that picumast dihydrochloride offers a comparable alternative to terfenadine in the treatment of seasonal allergic rhinitis.

Topics: Adult; Aged; Benzhydryl Compounds; Coumarins; Drug Tolerance; Histamine H1 Antagonists; Humans; Middle Aged; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Seasonal; Terfenadine

The efficacy of picumast dihydrochloride (3,4-dimethyl-7-[ 4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarine dihydrochloride) in a dosage of 2 mg o.d. vs. astemizole (10 mg o.d.) and placebo was investigated in a double-blind, controlled multicenter study. During the first 3 days of treatment, the patients were administered double their assigned dose as loading dose. A total of 119 patients were enrolled in the study, of whom 103 were evaluable for efficacy (picumast dihydrochloride n = 35, astemizole n = 35 and placebo n = 33). The primary objective was the number of patients for whom the investigator scored the effectiveness of study medication as adequate or better over a treatment period lasting at least 4 days. A statistically significantly improved efficacy over placebo was demonstrated by picumast dihydrochloride in terms of the primary objective as was a trend to improved efficacy over astemizole. Observation of the length of participation of the patients in the study up to the point of premature stopping due to inadequate efficacy, adverse events or non-compliance demonstrated that clearly more patients in both active drug groups remained in the study over the planned duration of 28 days compared with patients in the placebo group. In this respect, more patients on astemizole dropped out of the study prematurely compared with patients on picumast dihydrochloride. Serious adverse events did not occur.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Adult; Aged; Astemizole; Benzimidazoles; Coumarins; Double-Blind Method; Histamine H1 Antagonists; Humans; Middle Aged; Multicenter Studies as Topic; Patient Compliance; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Seasonal