[Pharmacology of the bronchospasmolytic oxitropium bromide].
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.
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001986:Bronchial Spasm / Q000139:chemically induced / Q000503:physiopathology; D004285:Dogs; D004562:Electrocardiography; D005260:Female; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009184:Mydriatics; D010095:Oxotremorine / Q000037:antagonists & inhibitors; D010276:Parasympatholytics / Q000494:pharmacology*; D051381:Rats; D012472:Salivation / Q000187:drug effects; D012602:Scopolamine Derivatives / Q000494:pharmacology*; D013045:Species Specificity
D009184:Mydriatics; D010276:Parasympatholytics; D012602:Scopolamine Derivatives; D010095:Oxotremorine; C017590:oxitropium; D000109:Acetylcholine
Zur Pharmakologie des Bronchospasmolytikums Oxitropiumbromid.