piperidines and ramosetron

To investigate the effect of combined prophylactic ramosetron and total intravenous anaesthesia (TIVA) on postoperative nausea and vomiting (PONV), compared with sevoflurane anaesthesia without prophylactic antiemetics, in female patients undergoing thyroidectomy.. Female patients were randomized between the sevoflurane group (anaesthesia maintained with sevoflurane) or TIVA + ramosetron group (TIVAR; 0.3 mg ramosetron just before anaesthesia induction, remifentanil and propofol anaesthesia). Incidence and severity of PONV and use of rescue antiemetics were recorded during the first 24 h after surgery.. In the early postoperative period (0-6 h), the incidence of PONV, severe emesis and rescue antiemetic use were significantly lower in the TIVAR group (n = 36) than in the sevoflurane group (n = 36). In the late postoperative period (6-24 h), the incidence of severe emesis was significantly lower in the TIVAR group than in the sevoflurane group.. A combination of TIVA and prophylactic ramosetron decreases early PONV and late postoperative severe emesis compared with sevoflurane anaesthesia.

Topics: Adult; Anesthesia, Intravenous; Benzimidazoles; Demography; Female; Humans; Piperidines; Postoperative Nausea and Vomiting; Propofol; Prospective Studies; Remifentanil; Thyroidectomy

The role of 5-hydroxytryptamine (5-HT)3 and 5-HT4 receptors in the regulation of gut motility in the ferret was investigated. The selective 5-HT3 receptor antagonist ramosetron (1 - 10 microg/kg s.c.) prolonged the interval of gastric antral migrating motor complex, but had only slight effect on small intestinal and colonic motility in unfed animals. The selective 5-HT4 receptor antagonist SB 204070 did not affect motility throughout gut in unfed animals. Neither ramosetron nor SB 204070 affected the motility throughout gut in fed animals. In conclusion, neither 5-HT3 nor 5-HT4 receptors tonically regulate ferret gut motility except that 5-HT3 receptors have a key role in the occurrence of migrating motor complex specifically in the stomach. The role of 5-HT3 and 5-HT4 receptor system in the regulation of gut motility in ferrets is similar to that in other mammalian species studied, including humans. This similarity suggests that the ferret is a suitable model animal to study gut motor functions in humans.

Topics: Animals; Benzimidazoles; Dioxanes; Ferrets; Gastrointestinal Motility; Male; Piperidines; Receptors, Serotonin; Receptors, Serotonin, 5-HT3; Receptors, Serotonin, 5-HT4; Serotonin Antagonists

The influence of diabetic hyperglycemia on solid gastric emptying in rats was examined. Diabetes was produced by streptozotocin (STZ, 40 mg/kg i.v.), and diabetic hyperglycemia was observed from 1 day after the STZ injection. The gastric emptying of glass beads in the diabetic rats was significantly delayed compared with that in age-matched control rats at 1, 3 and 7 days after diabetes induction. A slight decrease in gastric emptying was observed in the diabetic rats from 2 to 52 weeks after the diabetes induction. We also investigated the influence of gastroprokinetic agents on STZ-induced diabetic gastroparesis and subdiaphragmatic vagotomy-induced gastroparesis in rats. The selective 5-HT3 receptor antagonists ramosetron (YM060), YM114 (KAE-393), granisetron and ondansetron, and the substituted benzamides (5-HT4 receptor agonist/5-HT3 receptor antagonists) cisapride mosapride and SC-53116 dose-dependently enhanced gastric emptying in normal rats. These compounds also reversed the impairment of diabetic gastroparesis rats at 7 days after the STZ injection, but higher doses were required. The solid gastric emptying in subdiaphragmatic vagotomized rats was also delayed. Ramosetron and the substituted benzamides cisapride and zacopride partially reversed the gastroparesis in the vagotomized rats. These results suggest that acute hyperglycemia is important mechanism for the delay of solid gastric emptying in diabetic rats. It is also suggested that selective 5-HT3 receptor antagonists and substituted benzamides enhance gastric emptying not only in normal rats but also in diabetic and vagotomized rats.

Topics: Animals; Benzamides; Benzimidazoles; Blood Glucose; Cisapride; Diabetes Mellitus, Experimental; Gastric Emptying; Gastrointestinal Motility; Gastroparesis; Granisetron; Male; Morpholines; Ondansetron; Piperidines; Pyrroles; Rats; Rats, Wistar; Serotonin Antagonists; Serotonin Receptor Agonists; Vagotomy

The role of 5-HT3 receptors in the control of intestinal propulsive activity was investigated in mice by a simple method in which the time taken for excretion of the head of an orally administered non-absorbable marker (whole gut transit time) was measured. Selective 5-HT3 receptor antagonists ramosetron (YM060) at 0.01-0.3 mg/kg s. c. and ondansetron at 0.1-1 mg/kg s.c. dose-dependently prolonged the whole gut transit time. Prokinetic benzamides, such as renzapride (0.3-10 mg/kg s.c.), zacopride (0.01-0.3 mg/kg s.c.) and cisapride (0.1-3 mg/kg s.c.), which have been reported to possess 5-HT3 receptor blocking properties, also dose-dependently prolonged it. These results indicate that activation of 5-HT3 receptors seems to be one factor that underlies the physiological control of intestinal propulsive activity in mice. In contrast to their beneficial therapeutic effects on gastroduodenal dysmotility, prokinetic benzamides, at least those which have 5-HT3 receptor antagonistic activity, may be unsuitable in the treatment of impaired lower intestinal propulsive activity.

Topics: Adrenergic alpha-Agonists; Animals; Benzamides; Benzimidazoles; Bridged Bicyclo Compounds, Heterocyclic; Cholinesterase Inhibitors; Cisapride; Clonidine; Gastrointestinal Transit; Intestines; Male; Mice; Mice, Inbred C57BL; Neostigmine; Ondansetron; Piperidines; Receptors, Serotonin; Serotonin Antagonists