oxitropium and Bronchial-Spasm

Oxytropium bromide, a new synthetic anticholinergic agent, delivered by a dose inhaler, was compared to a placebo in a cross-over double-blind trial. The drop in FEV1 after administration of increasing doses of acetylcholine aerosol spray was measured 45 min after administration of the test drug, and the dose-response curve was determined. The placebo modified neither acetylcholine threshold dose (bronchial sensitivity) nor the slope of the curve (bronchial reactivity). Oxytropium bromide elevated the response threshold and decreased bronchial reactivity to vagal stimuli.

Topics: Acetylcholine; Adolescent; Adult; Bronchial Spasm; Clinical Trials as Topic; Double-Blind Method; Female; Forced Expiratory Volume; Humans; Male; Middle Aged; Parasympatholytics; Respiratory Therapy; Scopolamine Derivatives

Oxitropium bromide (Ba 253, Boehringer, Ingelheim) is a scopolamine-like atropine derivate with a mode of action approximating to that of ipratropium bromide (Atrovent, Sch 1000). The peak effect and duration of bronchodilatation with oxitropium bromide appears to be better than that of ipratropium bromide. Fifteen patients with a stable chronic bronchial obstruction were investigated in a double blind cross-over study. The obstruction was partially reversible by beta-stimulation. The patients inhaled 0.2 mg oxitropium bromide or placebo at 9.30 p.m. after two controls of FEV1 at 9 p.m. and 9.15 p.m. We re-examined the patients at 7 a.m. and 7.15 a.m. the following day and observed a significant parasympathetic additional obstruction under placebo, whereas, under the medication with oxitropium bromide overnight, significant bronchodilation was observable. When 0.2 mg oxitropium bromide was given at 7.30 a.m. to all patients, those pretreated with placebo showed significantly better bronchodilation than those pretreated with oxitropium bromide. It is concluded that oxitropium bromide is a long-acting (10 hours) overnight bronchodilator. The bronchodilation is probably due to prolonged parasympathicolysis in the airways.

Topics: Adult; Aged; Bronchial Spasm; Bronchodilator Agents; Female; Humans; Male; Middle Aged; Parasympatholytics; Respiratory Therapy; Scopolamine Derivatives

12 patients with obstructive airway diseases took part in a double-blind study in which 0.02 and 0.2 mg of Ba 253 as metered aerosols were compared with a placebo. Both doses of Ba 253 elicited a significant fall of mean total airway resistance compared to the placebo, and this fall was still discernible even 8 h after inhalation. Under the higher dose, the maximum response was significantly greater and it occurred about 2 h after inhalation; the response was still significantly more pronounced 8 h after inhalation. There was no objective evidence of local or systemic side effects attributable to a vagus-blocking effect. In the light of published reports and our own experience, when Ba 253 is inhaled in the stated doses it appears to be equivalent to ipratropium bromide as regards potency, duration of action, tolerance and therapeutic safety margin.

Topics: Aerosols; Airway Resistance; Bronchial Spasm; Dose-Response Relationship, Drug; Drug Evaluation; Female; Humans; Lung Diseases, Obstructive; Male; Scopolamine Derivatives; Time Factors

The recently developed anticholinergic agent Oxitropium bromide (OTB) by metered dose inhaler is compared in a double-blind crossover study with the beta-adrenergic agent Fenoterol (FEN). Total airway resistance and forced expiratory volume served as evaluation criteria for the bronchodilating effect. The maximum effect is reached more quickly with FEN, but the effect of OTB lasts longer. On the whole the results show that the intensity of action of the anticholinergic agent coincides to a large extent with that of the beta-adrenergic agent.

Topics: Adult; Aerosols; Aged; Airway Resistance; Atropine Derivatives; Bronchial Spasm; Clinical Trials as Topic; Dose-Response Relationship, Drug; Double-Blind Method; Ethanolamines; Fenoterol; Forced Expiratory Volume; Humans; Lung; Middle Aged; Parasympatholytics; Scopolamine Derivatives

A marked and long-lasting bronchospasmolytic effect without any cardiovascular side effects has been demonstrated in anaesthetized dogs following inhalation of 0.1 mg oxitropium bromide, with glucose as vehicle, administered as powder in powder inhaler capsules.

Topics: Aerosols; Animals; Blood Pressure; Bronchial Spasm; Dogs; Heart Rate; Myocardial Contraction; Parasympatholytics; Powders; Scopolamine Derivatives

The anticholinergic substance (8r)-6 beta, 7 beta-epoxy-8-ethyl-3 alpha-[(-)-tropoyloxyl]-1 alpha H, 5 alpha H-tropanium bromide (oxitropium bromide, Ba 253 BR, Ventilat) is a competitive antagonist of acetylcholine. In vitro, it is many times as effective as atropine. In vivo, oxitropium bromide, following i.v. administration, is also more effective than atropine. Due to its quaternary structure, a central anticholinergic effect cannot be demonstrated. Furthermore, poor enteral resorption is to be expected. Locally administered, as an aqueous aerosol, the effect of the substance is distinctly greater than that of atropine, both in potency and duration of action. This is also true when administered by metered-dose inhaler compared with ipratropium bromide. As, following aerosol administration, the margin between major effect and the most sensitive side-effect is in the ratio 1 : 100, side-effects are unlikely even with marked inhalational overdosage. Oxitropium bromide can be described, therefore, as a preparation free of side-effects which represents in prophylactic use in many cases of obstructive airway disease, an alternative to beta-mimetics and xanthine derivatives.

Topics: Acetylcholine; Animals; Blood Pressure; Bronchial Spasm; Dogs; Electrocardiography; Female; Gastric Mucosa; Guinea Pigs; Heart Rate; In Vitro Techniques; Male; Mice; Muscle Contraction; Muscle, Smooth; Mydriatics; Oxotremorine; Parasympatholytics; Rats; Salivation; Scopolamine Derivatives; Species Specificity