Pharmacology of the anticholinergic bronchospasmolytic agent flutropium bromide.
The anticholinergic agent (8r)-8-(2-fluoroethyl)-3 alpha-hydroxy-1 alpha H,tropanium bromide benzilic acid ester (flutropium bromide, Ba 598 BR) is a classic competitive antagonist of acetylcholine. In in vitro experiments it is more effective than atropine. In addition there are indications, that flutropium bromide may interfere with the anaphylactic reaction in a certain dose range in vitro. In in vivo experiments for the characterization of the anticholinergic properties flutropium bromide is also somewhat more effective than atropine after parenteral administration. Because of its quaternary structure no central anticholinergic effect is detectable. Furthermore, a poor enteral absorption is to be expected; this can be concluded from the low relative effectiveness after oral administration. After systemic administration, flutropium bromide is only slightly more effective than atropine. The duration of action is longer. After local administration as an aerosol it is superior to atropine with regard to both effectiveness and duration of action. Since in aerosol administration the ratio of the main effect to the most sensitive side effects, inhibition of salivary secretion, is 1:100, no side effects are to be expected even after high inhalational overdoses. Flutropium bromide can therefore be described as a preparation which is free of side effects. When used prophylactically it represents a therapeutic alternative to beta-mimetics and xanthine derivatives for most cases of obstructive airway diseases.
D000818:Animals; D001286:Atropine Derivatives / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D001993:Bronchodilator Agents / Q000494:pharmacology*; D004285:Dogs; D005260:Female; D005744:Gastric Acid / Q000378:metabolism; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D006636:Histamine Release / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009184:Mydriatics; D010095:Oxotremorine / Q000037:antagonists & inhibitors; D010276:Parasympatholytics / Q000494:pharmacology*; D051381:Rats; D012472:Salivation / Q000187:drug effects
D001286:Atropine Derivatives; D001993:Bronchodilator Agents; D009184:Mydriatics; D010276:Parasympatholytics; D010095:Oxotremorine; C039778:flutropium bromide