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Gastrointestinal Aspects of Eating Disorders
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Bruce D. Waldholtz, Arnold E. Andersen
In addition, erythromycin has been shown to improve gastric emptying in diabetic gastroparesis, but has not been studied in gastroparesis associated with anorexia nervosa. It improves gastric emptying for solids and liquids by acting as a motilin-receptor agonist, a hormone responsible for phase III contractions during the intradigestive motor complex (38). While studies demonstrate that these agents can improve gastric emptying in patients with gastroparesis from diabetes or possibly in anorexia nervosa, the routine use of these agents cannot be recommended in anorexia nervosa until studies demonstrate them to be effective. On a case-by-case basis, cisapride may be usefully employed.
Postulated Physiological and Pathophysiological Roles on Motility
Published in Edwin E. Daniel, Neuropeptide Function in the Gastrointestinal Tract, 2019
Hans-Dieter Allescher, Sultan Ahmad
Recent studies, however, demonstrated that EM and more potent synthesized analogues, which were called motilides, act directly on the motilin receptor, as demonstrated by receptor binding studies.628,629 Changes of the chemical structure produced potent nonpeptide agonists for the motilin receptor, some more than 2000 times more potent than EM; e.g., the compound EM-536 (8,9-anhydroerythromycin A 6,9-hemiketal-propagyl-bromide) showed an EC50 of 5.3 nM in exciting the isolated rabbit duodenum and displaced [125I]motilin binding with an IC50 of 3 to 40 nM.628 Erythromycin was shown previously to be a potent stimulant of gastric motility630,631 which would induce phase III activity in normal subjects and in patients suffering from diabetic gastroparesis.630 In these patients, erythromycin (200 mg i.v.) accelerated gastric emptying of liquids and solids to normal levels, suggesting that erythromycin and especially its more potent analogues might have therapeutic value in patients with impaired gastric emptying.632
Palliative Care of Gastroparesis
Published in Victor R. Preedy, Handbook of Nutrition and Diet in Palliative Care, 2019
Erythromycin, a macrolide antibiotic, has been used with mixed results in GP. It is a motilin receptor agonist that mimics the action of motilin on GI tract smooth muscles (Acosta and Camilleri 2015). Erythromycin has been demonstrated to be effective in improving gastric emptying in GP patients. Erythromycin is more effective when given intravenously rather than orally. It is effective at low doses of 75–250 mg daily. Two main concerns with erythromycin use are loss of effectiveness over time because of downregulation of the motilin receptors, and potential for antimicrobial resistance. Adverse effects of erythromycin include abdominal pain, ototoxicity and QT interval prolongation. In refractory cases of GP, erythromycin can be combined with metoclopramide. Cisapride, increased gastric emptying of both solids and liquids, has been shown to have significant drug-drug interactions. It was withdrawn from markets in the United States and other countries due to the risk of serious cardiac events.
Gastroparesis syndromes: emerging drug targets and potential therapeutic opportunities
Published in Expert Opinion on Investigational Drugs, 2023
Le Yu Naing, Matthew Heckroth, Prateek Mathur, Thomas L Abell
Motilin receptor agonists increase gastric emptying due to stimulation of enteric cholinergic activity. Camicinal is a small molecule selective motilin receptor agonist given via the enteral route. It has been shown to accelerate gastric emptying and increase glucose absorption in mechanically ventilated, feed-intolerant patients when given a single dose[49]. Hobson et al. showed that a single dose of 125 mg of carmicinal decreased gastric emptying time and was well tolerated in healthy males but had no effect on esophageal function or small bowel and colonic transit time[49]. Another study demonstrated that a single 50 mg dose of carmicinal had no significant impact on gastroduodenal manometry or pH parameters. Still, a 150 mg dose increased the occurrence of gastric phase III contractions compared to placebo but did not affect small bowel manometry parameters or esophageal and gastric pH[50]. The effect of carmicinal on gastric emptying was maintained with a 14-day repeat-dose trial and was found to have an effect in type I diabetes associated gastroparesis [51,52].
Motilin Receptor Expression Found in the Human Main and Accessory Lacrimal Glands
Published in Ocular Immunology and Inflammation, 2022
Richard R. Sadig, Alexandra Allende, Geoffrey Hall, Dinh Tran, Michele C Madigan, Stephanie L. Watson, Kenneth G. -J. Ooi
The motilin receptor is an important prokinetic receptor traditionally found in the antrum of the stomach as well as the duodenum.5 Motilin is a 22 amino acid ligand hormone secreted mainly by specialized enterochromaffin mucosal cells of the upper GIT system including the stomach antrum and the duodenum. Its secretion is usually in response to changes in the pH of the stomach, alkalinization of the duodenum and distention of the stomach.6–8 The actions of motilin also affect the cholinergic pathway to stimulate contractions of the gall bladder and the sphincter of Oddi.7 The motilin receptor is a guanine-coupled receptor of class 1 type 1. The motilin receptor has two main bindings site identified, an extracellular portion and a transcellular portion. The extracellular portion involves the docking of peptide-like structures (such as motilin) onto the extramembranous loop portion of the motilin receptor.9 Motilin is released with cholinergic vagal stimulation of local antral nerve plexuses.10 This suggests that motilin can be released both in local response and via central neuronal control – predominantly under cholinergic control.8,10 Motilin receptors have also been found in rabbit brains– with the highest densities found in the hippocampus, hypothalamus and amygdala, as well as in the cerebellum.4,11 Its role in the central nervous system is not entirely clear but it is postulated to be involved with neurotransmission via synaptosomes, as well as stimulating appetite, mood and memory6,11,12,13
Safety considerations when managing gastro-esophageal reflux disease in infants
Published in Expert Opinion on Drug Safety, 2021
Melina Simon, Elvira Ingrid Levy, Yvan Vandenplas
Erythromycin is a motilin receptor agonist that contributes to gastric emptying and induces phase III activity of the interdigestive migratory motor complex. Phase III, which is the most characteristic phase of the migrating motor complex, is the phase when the smooth muscle of the gastrointestinal tract rapidly contracts. In phase III, the pylorus remains open, allowing food to move into the small intestine [159].