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Explore chapters and articles related to this topic
Serotonin and the Afferent Innervation of the Gastrointestinal Tract
Published in T.S. Gaginella, J.J. Galligan, SEROTONIN and GASTROINTESTINAL FUNCTION, 2020
Helen E. Raybould, David Grundy, Paul L. R. Andrews
In man, the effects of 5-HT3 receptor antagonists are more varied. Ondansetron had no effect on gastric emptying of a mixed nutrient meal,30 but did significantly increase whole gut transit time. Talley, et al.31 showed ondansetron had no effect on mouth-to-cecal transit time. Tropisetron (ICS 205-930) had no effect on solid emptying, although at higher doses it may have a moderate effect.32,33 Renzapride increased gastric emptying in healthy volunteers.34 Tropisetron had little effect on fat-induced delayed gastric emptying in healthy man.35
Postirradiation Emesis
Published in John Kucharczyk, David J. Stewart, Alan D. Miller, Nausea and Vomiting: Recent Research and Clinical Advances, 2017
Gregory L. King, Milan T. Makale
As has been pointed out by Gershon and co-workers,185 it is impossible to accurately relate the electrophysiological actions of these compounds with their action on GI motility either in vitro or in vivo. Given the complexity of the enteric nervous system, such compounds could act as specific receptor agonists or antagonists, nonspecifically, or not at all under certain conditions. In support of this notion, several in vivo studies failed to find a strict correlation between the 5-HT3 receptor antagonist activity of some compounds and their ability to act as prokinetic or antiemetic agents.208–212 For example, renzapride enhances GI myoelectric activity and abolishes a delayed gastric emptying at a dose near that needed to act at 5-HT3 receptors.212 ICS 205-930, however, does not change myoelectric activity, but it abolishes delayed gastric emptying at a dose much greater than that needed to act at 5-HT3 receptors.
Current and future treatment management strategies for gastroparesis
Published in Expert Opinion on Orphan Drugs, 2019
Priyadarshini Loganathan, Mahesh Gajendran, Richard McCallum
Prucalpride approved in Europe and Canada, improves small bowel transit and GE in constipated patients [40]. FDA has recently approved this medication in December 2018 for chronic idiopathic constipation. Based on the mechanism of action relating to being a 5-HT4 agonist, and in view of the track record of cisapride and Tegaserod it is predicted that Prucalpride will also be investigated and utilized in GP. Velusetrag another 5-HT4 agonist was shown in a double-blinded placebo-controlled trial to accelerate GE and has no cardiac toxicity. Two multicenter Phase 2 clinical trials are being conducted. Other 5-HT4 agents currently under investigation are Naronapride, Renzapride, Mosapride [41], and YKP 10,811, which has been shown to improve gastric transit, colonic transit, and colonic motility [42,43].