Cimetropium bromide: in vitro and in vivo evaluation of spasmolytic activity on human and dog colon

Digestion. 1989;42(3):143-50. doi: 10.1159/000199839.

Abstract

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.

MeSH terms

  • Animals
  • Colonic Diseases / physiopathology*
  • Dogs
  • Gastrointestinal Motility / drug effects
  • Humans
  • In Vitro Techniques
  • Muscarine / antagonists & inhibitors
  • Neostigmine / pharmacology
  • Parasympatholytics
  • Physical Stimulation
  • Reflex / physiology
  • Scopolamine Derivatives / pharmacology*
  • Spasm / physiopathology*

Substances

  • Parasympatholytics
  • Scopolamine Derivatives
  • cimetropium
  • Neostigmine
  • Muscarine