[The potentials of erythromycin derivatives in the treatment of gastrointestinal motility disorders].
In low dosages erythromycin imitates the effect of motilin on the gastrointestinal motility. In vitro experiments show that erythromycin is a motilin agonist: it displaces motilin which is bound to its receptor; it directly acts on smooth musculature and it possesses the same animal and tissue specificity. Structural changes cause adequate changes in the binding affinity and in the contractile activity. Several motilides such as erythromycin derivatives with prokinetic properties have no antibiotic activity, but they cause a distinct increase of the prokinetic activity. Motilides may be defined as a new group of prokinetic substances: the motilinomimetics. Erythromycin normalises the delayed evacuation of the stomach of solid and fluid food in diabetic, idiopathic and postvagotomy gastroparesis. For the treatment of gastrooesophageal reflux disease, gastritis, pathological overgrowth of the small intestine, hypokinesia of the gallbladder and the chronic obstipation erythromycin appears as a promising medicament. The substances with a stronger effect may become even still more useful medicaments. A better understanding of the relation between motilin and motilides may lead to new knowledge about the regulation of the gastrointestinal motility.
Peeters
T L
TL
Zentrum für gastroenterologische Forschung der katholischen Universität Leuven.
D001659:Biliary Tract / Q000187:drug effects; D003106:Colon / Q000187:drug effects; D004917:Erythromycin / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D004943:Esophagogastric Junction / Q000187:drug effects; D005746:Gastric Emptying / Q000187:drug effects; D005767:Gastrointestinal Diseases / Q000188:drug therapy / Q000503:physiopathology; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006801:Humans; D007418:Intestinal Pseudo-Obstruction / Q000188:drug therapy; D009037:Motilin / Q000378:metabolism*
D009037:Motilin; D004917:Erythromycin
Die Möglichkeiten von Erythromycinderivaten in der Behandlung von gastrointestinalen Motilitätsstörungen.