Bauer V R
Arzneimittelforschung. 1985;35(1A):435-40.
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.
抗胆碱能物质（8R）-6β，7β-环氧-8-乙基-3α-[（-）-托品酰氧基]-1αH，5αH-托烷溴化物（氧托溴铵，Ba 253 BR，Ventilat）是乙酰胆碱的竞争性拮抗剂。在体外，其效力是阿托品的许多倍。在体内，静脉注射后，氧托溴铵也比阿托品更有效。由于其季铵结构，无法证明其中枢抗胆碱能作用。此外，预计其肠道吸收较差。局部以水性气雾剂给药时，该物质的效力和作用持续时间明显大于阿托品。与异丙托溴铵相比，通过定量吸入器给药时也是如此。由于气雾剂给药后，主要作用与最敏感副作用之间的差距为1：100，因此即使吸入剂量明显过量也不太可能出现副作用。因此，氧托溴铵可被描述为一种无副作用的制剂，在许多阻塞性气道疾病的预防使用中，它是β-拟交感神经药和黄嘌呤衍生物的替代品。
