picumast and Asthma

A double-masked study was performed to investigate a possible side effect of the antiallergic substance Picumast dihydrochloride on lens transparency. 372 patients with Picumast dihydrochloride- or Ketotifen-treatment regularly underwent ophthalmologic examinations and Scheimpflug photography of the anterior eye segment. Results of slitlamp examinations as well as microdensitometric analyzes of the film negatives after one year treatment did not reveal any evidence that Picumast dihydrochloride compromised lens transparency in humans.

Topics: Asthma; Cataract; Coumarins; Densitometry; Double-Blind Method; Histamine H1 Antagonists; Humans; Ketotifen; Lens, Crystalline; Photography

In a randomized double-blind study, 107 patients with extrinisic, intrinsic or mixed bronchial asthma and impaired lung function received either picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarin dihydrochloride) 1 mg or placebo twice daily for 6 weeks after a 2-week placebo phase. Patients given picumast dihydrochloride demonstrated significant improvements compared with baseline in morning and evening peak flow and asthmatic symptoms like morning tightness, cough, dyspnoea, obstruction, number of asthma attacks during night and day, sum of asthmatic symptom scores, in vital capacity and Tiffeneau index, and a significant reduction of inhaled adjuvant medications. In contrast, placebo recipients improved significantly only in daytime asthma attacks, obstruction, sum of symptom scores, and Tiffeneau index. The differences between the picumast dihydrochloride and placebo groups significantly favoured picumast dihydrochloride for improvements in mean number of daytime asthma attacks, morning tightness, aerosol use and sum of symptom scores. Adverse reactions were minor and infrequent; no tiredness occurred with picumast dihydrochloride. Tolerability of both picumast dihydrochloride and placebo was rated as "good" to "very good" by patients and physicians.

Topics: Adult; Asthma; Coumarins; Double-Blind Method; Female; Forced Expiratory Volume; Histamine H1 Antagonists; Humans; Male; Middle Aged; Randomized Controlled Trials as Topic

The efficacy and tolerability of picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarin dihydrochloride) (2 mg twice daily orally) in comparison with ketotifen (1 mg twice daily orally) was investigated in 400 patients with bronchial asthma (picumast dihydrochloride n = 202, ketotifen n = 198) in a double-blind, controlled, parallel group study. Assessment of therapeutic and preventative efficacy was by means of symptom scores, quantitative measurements (accumulatory threshold dose) of the bronchial hyperreactivity by means of inhalatory acetylcholine provocation, measurements of peak expiratory flow, vital capacity (VC) and 1-s capacity (FEV1) as well as global assessment of efficacy by the doctor and patient. Tolerability was assessed by recording side effects and global assessment of tolerance on a rank scale at the end of the treatment as well as by means of clinico-chemical parameters. Picumast dihydrochloride and to a lesser extent ketotifen both led to a clinically relevant and statistically significant increase in the inhalatory provocation dose (PD50) for acetylcholine. There was a moderate improvement in the symptom scores and a rise in peak flow values in both treatment groups. The mean total score of asthmatic symptoms of both drugs showed a clear but quantitatively low improvement after 12 months' treatment. The differences in efficacy between picumast dihydrochloride and ketotifen were not statistically significant. During the course of the study, adverse reactions were recorded on 117 occasions (picumast dihydrochloride n = 41, ketotifen n = 76).(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Adult; Asthma; Coumarins; Double-Blind Method; Female; Forced Expiratory Volume; Histamine H1 Antagonists; Humans; Ketotifen; Male; Middle Aged; Peak Expiratory Flow Rate; Randomized Controlled Trials as Topic; Vital Capacity

In a pilot study 8 patients with allergic obstructive airway disease were treated with the new compound picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarine++ + dihydrochloride) 2 x 2 mg daily orally during a period of 8 days additionally to a usual therapy of bronchodilators and corticoids in a steady state. It was demonstrated that the compound inhibited the allergen induced histamine liberation of patients basophils significantly. Compared with a collective of patients without an additional picumast dihydrochloride treatment the effect of the substance was shown more clearly. From reasons of these experimental data picumast dihydrochloride may be of a considerable value as a prophylactic agent in allergic bronchial asthma when given orally.

Topics: Asthma; Chromatography, High Pressure Liquid; Coumarins; Female; Histamine H1 Antagonists; Histamine Release; Humans; Hypersensitivity; Leukocytes; Male; Middle Aged

104 adult patients with predominantly extrinsic perennial asthma who were maintained on bronchodilator or glucocorticoid therapy, were entered into a one-year open study designed to evaluate the efficacy, safety and acceptability of picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarin dihydrochloride) (2 mg twice daily). 74 patients completed the 12-month treatment period and a further 18 (total 92) were followed up for at least 2 months. Adverse drug reactions were reported in 14 patients and 5 of them were withdrawn from the trial for only non serious reactions. 12 patients were excluded from the analysis of efficacy because they dropped out early and no sufficient data were available for a judgement. Although this was an open study, analysis of diary card measurements and clinical assessments indicate that picumast dihydrochloride could represent a new and effective prophylactic therapy in the long-term management of bronchial asthma. Picumast dihydrochloride improved forced expiratory volume in 1 s (FEV1), peak flow and subjective asthmatic symptoms in 51%, 64% and 70% of the patients, respectively. 92% of those who participated in this study were willing to take the study drug again.

Topics: Adult; Asthma; Coumarins; Female; Forced Expiratory Volume; Histamine H1 Antagonists; Humans; Male; Vital Capacity