Mitemcinal fumarate  (Synonyms: GM 611 fumarate)

Mitemcinal fumarate is an orally active motilium agonist whose effects on defecation have been studied in rabbits and dogs. In normal rabbits, oral administration of mitemcinal (2.5-10 mg/kg) increased fecal weight in a dose-dependent manner within 0-3 hours without causing loose stools. Sennoside (12-48 mg/kg) also promoted defecation within 2-9 hours of oral administration, but the feces were significantly looser. In the morphine-induced constipation model, fecal weight in morphine-treated rabbits (1 mg/kg) was only 37.5% of that in untreated animals. Mitemcinal fumarate (0.5-20 mg/kg) increased fecal weight in a dose-dependent manner without increasing fecal water content. At the highest mitemcinal dose, fecal weight was restored to 83.9% of that in untreated animals. In normal dogs, mitemcinal fumarate (0.3-3 mg/kg) decreased the time to first defecation after oral administration without causing diarrhea at any dose. These results suggest that mitemcinal fumarate promotes defecation without causing severe diarrhea, suggesting that mitemcinal fumarate may be a new agent for the treatment of constipation because it has an earlier onset of action and a shorter duration of action, facilitating control of defecation time, compared with sennoside.

1628.03

C₄₀H₆₉NO₁₂.1/2C₄H₄O₄

154802-96-7

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• [1]. Mitemcinal (GM-611), an orally active motilin agonist, facilitates defecation in rabbits and dogs without causing loose stools