Peeters T L
Zentrum für gastroenterologische Forschung der katholischen Universität Leuven.
Z Gesamte Inn Med. 1991 Aug;46(10-11):349-54.
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.
小剂量时，红霉素可模拟胃动素对胃肠动力的作用。体外实验表明，红霉素是一种胃动素激动剂：它能取代与受体结合的胃动素；直接作用于平滑肌，且具有相同的动物和组织特异性。结构变化会导致结合亲和力和收缩活性发生相应改变。一些胃动素类药物，如具有促动力特性的红霉素衍生物，没有抗生素活性，但它们能显著增强促动力活性。胃动素类药物可被定义为一类新的促动力物质：胃动素模拟物。红霉素可使糖尿病性、特发性及迷走神经切断术后胃轻瘫患者胃内固体和液体食物排空延迟的情况恢复正常。对于治疗胃食管反流病、胃炎、小肠病理性过度生长、胆囊运动功能减退及慢性便秘，红霉素似乎是一种有前景的药物。作用更强的物质可能会成为更有效的药物。对胃动素与胃动素类药物之间关系的更好理解可能会带来有关胃肠动力调节的新知识。
