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Autonomic dysfunction
Published in Jeremy Playfer, John Hindle, Andrew Lees, Parkinson's Disease in the Older Patient, 2018
Cisapride, a prokinetic agent, was effective for constipation in PD,78 but is currently unavailable because of an associated risk of cardiac conduction defects. Alternative prokinetic agents include domperidone and the new 5-HT4 receptor agonists, tegaserod and mosapride citrate. Domperidone is an effective prokinetic agent in the upper gastrointestinal tract,79 but has been shown to have little effect on the lower gastro intestinal slow transit times in PD. The 5-HT4 receptor agonists facilitate intestinal motility by facilitating release of acetylcholine from enteric cholinergic neurons. A small study in patients with MSA and PD has suggested a beneficial effect of mosapride on constipation.80
The Conception Vessel (CV)
Published in Narda G. Robinson, Interactive Medical Acupuncture Anatomy, 2016
Acupuncture at CV 12, ST 36, SP 6, and PC 6 once daily for one week for multiple courses over a six week period experienced significant alleviation of symptoms and less intraesophageal acid and bile reflux. Results were not significantly different from patients who received omeprazole and mosapride.22
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
Mosapride is a selective 5-hydroxytryptamine type 4 (5-HT4) receptor agonist and 5-HT3 receptor antagonist. It is a prokinetic agent mostly used for gastroparesis, functional dyspepsia, gastroesophageal reflux, and it improves delayed gastric emptying. It is mostly used in Asian countries and South America for functional dyspepsia and is not currently available in the US. The Japan Mosapride Mega-Study (JMMS) in 2012 showed that a two-week treatment of mosapride significantly improved gastric stasis and epigastric pain[44]. A recent meta-analysis showed that mosapride was superior to placebo in improving gastric emptying time in patients with diabetic gastroparesis, but there was no statistically significant difference between mosapride and domperidone. The efficacy of mosapride combined with domperidone or mecobalamin was higher than mosapride alone[45]. However, another meta-analysis showed no statistically significant effect of mosapride on functional dyspepsia compared to placebo[46]. A randomized controlled trial of mosapride added to chronic hepatitis C treatment with pegylated interferon α-2b and ribavirin showed that the mosapride added group had total and distal gastric motility improvement in solid phase gastric emptying half-times within four weeks after the therapy compared to the control group.
Drugs under development for the treatment of functional dyspepsia and related disorders
Published in Expert Opinion on Investigational Drugs, 2019
Jan Tack, Imke Masuy, Karen Van Den Houte, Lucas Wauters, Jolien Schol, Tim Vanuytsel, Alain Vandenberghe, Florencia Carbone
Another class of prokinetic agents are the serotonin-4 (5-HT4) receptor agonists. The first 5-HT4-receptor agonist used for treating gastric motility disorders was metoclopramide, which is also a D2-receptor antagonist, but which received a black box warning for its risk of inducing extrapyramidal symptoms [15]. Cisapride, a 5-HT4-receptor agonist developed in the 1990s, became the leading prokinetic drug for the treatment of upper gastrointestinal hypomotility disorders but was withdrawn from the market for its arrhythmogenic potential, due to its affinity for the human ether-a-gogo (HERG) channel [20]. Several other, more selective, 5-HT4 receptor agonists have been developed, including mosapride, tegaserod, prucalopride and velusetrag [8,15,20,21]. Mosapride is used as a prokinetic agent in many Asian countries, but a controlled trial in Europe failed to show efficacy in FD [15]. Both for itopride (see above) and mosapride, differences were observed between Western and Asian studies. While these may reflect differences in patient selection and choice of endpoints, a review of the recent literature indicated that PDS is a more prevalent subtype in Asia, and that GERD co-morbidity is significantly higher in the West [22]. The latter may, in theory, contribute to a lesser efficacy signal of prokinetic therapies focusing on the stomach in Western FD studies.
The tissue distribution and excretion study of mosapride and its active des-p-fluorobenzyl and 4′-N-oxide metabolites in rats by ultra-high performance liquid chromatography-tandem mass spectrometry method
Published in Xenobiotica, 2020
Kunjie Li, Xu Jiang, Zhili Xiong, Feng Qin, Longshan Zhao
The highest concentration of mosapride in male rat tissues was detected in the duodenum (3255 ± 1170 ng/g, 0.5 h), followed by the cecum (2754 ± 1316 ng/g, 0.5 h), the liver (2218 ± 27.0 ng/g, 0.5 h) and the stomach (1955 ± 1426 ng/g, 0.5 h). The highest concentration of mosapride in female rats was detected in the stomach (3039 ± 2247 ng/g, 0.5 h), followed by the cecum (2863 ± 1788 ng/g, 8 h), the liver (2381 ± 1678 ng/g, 0.5 h) and the duodenum (1973 ± 1327 ng/g, 0.5 h). It can be seen from the above results that the major distribution tissues of mosapride in male rats were similar to that in female rats, with the highest concentrations detected at 0.5 h after drug administration. However, an interesting finding was that the concentration of mosapride in the cecum was higher at 8 h than at 0.5 h. The high concentration of mosapride in the tissues of stomach and intestinal can be attributed to several reasons. First, it may be due to the selective distribution of mosapride in the stomach and intestinal. Second, it may be attributed to the poor absorption of mosapride after an oral dose, which resulted in the remains of mosapride in the lumens. Finally, we speculate that it may be because mosapride has a strong ability to form hydrogen bonds with the phospholipid polar end of the membrane on the gastric wall and intestinal wall, which makes the compound more likely to stick to the stomach and intestinal walls. This may be also one of the reasons why mosapride can bind to the 5-HT4 receptors distributed in the gastrointestinal tract (Sakurai-Yamashita et al., 1999; Yoshikawa et al., 1998), and thus generating the gastrointestinal motility promoting activity.