Cimetropium bromide: in vitro and in vivo evaluation of spasmolytic activity on human and dog colon.
The present study investigates the spasmolytic properties of cimetropium bromide, compared to atropine, on human and canine large bowel. The drug behaved as a competitive antagonist of muscarinic-mediated contractions in isolated colonic preparations from both species, with affinity values (pA2) ranging between 7.41 and 7.82. When administered intravenously to conscious dogs provided with a colonic Thiry fistula, cimetropium was a potent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. The compound (10-100 micrograms/kg) counteracted colonic motor response to neostigmine administration with an ID50 of 27.9 micrograms/kg; both tonic and phasic components of contractile response were affected. In a comparable range of doses (3-100 micrograms/kg), the drug inhibited motor activity elicited by intraluminal distension.
Department of Pharmacology, Istituto De Angeli, Milano, Italy.
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Sagrada
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Schiavone
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Cefalà
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R
Micheletti
D000818:Animals; D003108:Colonic Diseases / Q000503:physiopathology*; D004285:Dogs; D005769:Gastrointestinal Motility / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D009116:Muscarine / Q000037:antagonists & inhibitors; D009388:Neostigmine / Q000494:pharmacology; D010276:Parasympatholytics; D010812:Physical Stimulation; D012018:Reflex / Q000502:physiology; D012602:Scopolamine Derivatives / Q000494:pharmacology*; D013035:Spasm / Q000503:physiopathology*
D010276:Parasympatholytics; D012602:Scopolamine Derivatives; C016859:cimetropium; D009388:Neostigmine; D009116:Muscarine