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The Clinical Application of 5-HT Agonists and Antagonists in Gastrointestinal Disease
Published in T.S. Gaginella, J.J. Galligan, SEROTONIN and GASTROINTESTINAL FUNCTION, 2020
Timothy P. Roarty, Richard W. McCallum
Recently, Herrstedt and colleagues reported an added benefit with the combination of ondansetron and metopimazine, a dopamine D2 antagonist that is a piperidine derivative of phenothiazine, compared to ondansetron alone in 30 patients who had previously received chemotherapy and were currently receiving a moderately emetogenic regimen.122 The addition of metopimazine significantly reduced the number of acute episodes (day 1), delayed episodes (days 2 through 5), and overall episodes of emesis. The combination therapy was particularly effective in the control of delayed emesis, with no patients having more than two emetic episodes a day in contrast to seven patients (23%) given ondansetron alone who had three or more episodes a day.
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
These compounds are neuroleptics with sedative properties and include chlor-promazine, thiethlyperazine, thioperazine, perphenazine, trifluoperazine, metopi-mazine, and prochlorperazine. Early reports supported the notion that all these agents suppress radiation-induced emesis in humans.15,129–132 Later studies, however, found metopimazine and prochlorperazine to be no better than a placebo in alleviating the incidence or duration of emesis.133–135 Although the phenothiazines remain popular as clinically used antiemetics,136 and were even used at Chernobyl,3 the newer, more potent antiemetics will probably replace them.
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
Newer dopamine receptor antagonists, with potentially improved safety profiles, are currently being investigated. Trazpiroben (TAK-906) is a novel, potent D2/D3 receptor antagonist in which preclinical studies have demonstrated minimal blood-brain barrier penetration and low affinity for hERG channel inhibition[40]. Metopimazine is a peripherally restricted dopamine antagonist that has been used in Europe for years for the treatment of acute nausea and vomiting. Preclinical animal trials have shown increased antral contractions and improved gastric emptying of solid foods. As with trazpiroben, it does not readily cross the blood-brain barrier or antagonize hERG channels and thus may not carry the neurological and cardiovascular side effects of current DRAs. Repurposed metopimazine (NG101) is currently being studied for the treatment of gastroparesis[41]. Another novel dopamine receptor antagonist, CIN-102, is undergoing phase 2 clinical trials. CIN-102 is structurally like domperidone except for the substitution of specific hydrogen atoms with deuterium atoms, making it more structurally stable. This structural alteration is suggested to improve efficacy, safety, and tolerability, although early studies have shown a similar side-effect profile to domperidone.