title: Gastrointestinal motor-stimulating activity of macrolide antibiotics and analysis of their side effects on the canine gut.
abstract: For clarification of the nature of the side effects of macrolide antibiotics on the gastrointestinal tract, the motor-stimulating activity of these agents was studied in unanesthetized dogs. The results showed that erythromycin and oleandomycin, the 14-membered macrolides with two side chain sugars combined at C3 and C5 in a glycosidic linkage in parallel, strongly stimulate gastrointestinal motor activity, an action accompanied by vomiting at large doses. On the other hand, leucomycin, acetylspiramycin, and tylosin, belonging to a 16-membered macrolide with two side chain sugars in series combined at C5 of the lactone ring, did not induce contractions of the gastrointestinal tract. Motor-stimulating activity by erythromycin and oleandomycin was greatly inhibited by atropine sulfate. These results point to structure-physiological activity relationships.
mesh_terms: D000617:Aminoglycosides / Q000494:pharmacology*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000494:pharmacology*; D001285:Atropine / Q000494:pharmacology; D001667:Binding, Competitive; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004917:Erythromycin / Q000009:adverse effects / Q000494:pharmacology; D005260:Female; D005769:Gastrointestinal Motility / Q000187:drug effects*; D007933:Leucomycins / Q000009:adverse effects / Q000494:pharmacology; D008297:Male; D008837:Micrococcus / Q000187:drug effects; D009119:Muscle Contraction / Q000187:drug effects; D009827:Oleandomycin / Q000009:adverse effects / Q000494:pharmacology
chemical_list: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D007933:Leucomycins; D004917:Erythromycin; D001285:Atropine; D009827:Oleandomycin