Disease relevance of Ramosetron

• Ramosetron is effective for the long-term prevention of PONV [1].
• The treatment groups were comparable with regard to demographic characteristics and type of surgery After the second 24 hour postanesthesia period, significantly more patients in the ramosetron 0.3-mg and 0.6-mg groups were emesis free than in the placebo group (both P<0.001) [2].
• No relationship between body weight and the efficacy of ramosetron was observed [2].
• Antiemetic effect of ramosetron during hyperthermo-chemo-radiotherapy for esophageal cancer [3].
• A double-blind, crossover, randomized comparison of granisetron and ramosetron for the prevention of acute and delayed cisplatin-induced emesis in patients with gastrointestinal cancer: is patient preference a better primary endpoint [4]?

High impact information on Ramosetron

• When administered together with the 5-HT3 receptor antagonists, ramosetron or metoclopramide, both glucocorticoids showed an additive effect on 5-HT3 receptor [5].
• The selective 5-HT3 receptor antagonists GK-128, granisetron, ramosetron, azasetron and ondansetron depressed the increase in fecal pellet output caused by 2-methyl-5-HT and by wrap-restraint stress [6].
• A randomized clinical trial of a single dose of ramosetron for the prevention of vomiting after strabismus surgery in children: a dose-ranging study [7].
• OBJECTIVE: The aim of this study was to determine the effective dose of ramosetron, a 5-hydroxytryptamine type 3 receptor antagonist, for prophylaxis of severe POV (> or =2 episodes) in children undergoing general anesthesia for tonsillectomy [8].
• Randomized, double-blind, placebo-controlled, dosed-finding study of the antiemetic effects and tolerability of ramosetron in adults undergoing middle ear surgery [2].

Chemical compound and disease context of Ramosetron

• The incidence of a complete response, defined as no PONV and no need for another rescue medication, 0-3 h after anesthesia was 87% with granisetron and 90% with ramosetron; the corresponding incidence 3-24 h after anesthesia was 85% and 90%; the corresponding incidence 24-48 h after anesthesia was 70% and 92% (P < 0.05) [9].
• Both drugs showed similar results in regard to chemotherapy-induced gastrointestinal side effects, emesis and appetite loss on day 1, but by day 5, ramosetron was significantly better than ondansetron in terms of controlling appetite loss [10].
• Multicenter, randomized trial of ramosetron plus dexamethasone versus ramosetron alone in controlling cisplatin-induced emesis [11].
• Acute, subacute and chronic oral toxicity studies of the new serotonin (5-HT)3-receptor antagonist ramosetron in beagle dogs [12].
• Comparative clinical study of the anti-emetic effects of oral ramosetron and injected granisetron in patients with malignant glioma undergoing ACNU chemotherapy [13].

Biological context of Ramosetron

• Both GMC-like contraction and defecation were inhibited with the selective 5-HT(3) receptor antagonist ramosetron [14].
• 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 [15].
• The selective 5-HT3 receptor antagonists ramosetron (YM060, 0.1-10 micrograms/kg i.v.) and ondansetron (1-100 micrograms/kg i.v.) dose-dependently enhanced the gastric emptying of glass beads in rats [16].

Anatomical context of Ramosetron

• Effect of ramosetron on short-circuit current response in rat colonic mucosa [17].
• We conclude that the limited distribution of ramosetron to the brain is due, at least in part, to efflux mediated by the P-glycoprotein at the blood-brain barrier [18].
• We hypothesized the involvement of an efflux system(s) and investigated the contribution of P-glycoprotein to efflux transport of ramosetron across the blood-brain barrier by means of an in-vitro uptake study in cell lines that over-express P-glycoprotein [18].
• The potential of ramosetron ((R)-5-[(1-methyl-3-indolyl)carbonyl]-4,5,6,7-tetrahydro-1 H-benzimidazole hydrochloride, CAS 132907-72-3, YM060) orally disintegrating tablets to cause irritation to the oral mucosa was assessed in a group of six male and six female Syrian hamsters [19].
• Effects of various 5-HT3 receptor antagonists, granisetron, ondansetron, ramosetron and azasetron on serotonin (5-HT) release from the ferret isolated ileum [20].

Associations of Ramosetron with other chemical compounds

• Although the specific 5-hydroxytriptamine3 (5-HT3) receptor antagonists such as ondansetron and ramosetron are used as antiemetics, reports show that the use of 5-HT3 receptor antagonists with some glucocorticoids brings additional effects [5].
• METHODS: In this randomized, double-blind study, patients received granisetron 3 mg or ramosetron 0.3 mg intravenously at the end of surgery [21].
• OBJECTIVE: This prospective, randomized, double-blind, placebo-controlled, dose-ranging study was undertaken to assess the efficacy and safety of ramosetron, a selective 5-hydroxytryptamine type 3-receptor antagonist, in preventing nausea and vomiting after thyroidectomy [22].
• Background: This study observed and compared the preventive effects of ramosetron and ondansetron on gastrointestinal side effects caused by cisplatin-containing chemotherapy [10].
• SB203186 (1 microM), a 5-HT4-receptor antagonist, enhanced the 5-HTP-evoked 5-HT outflow, while ramosetron (1 microM), a 5-HT3-receptor antagonist reduced the stimulating effect of 5-HTP by 66% [23].

Gene context of Ramosetron

• METHOD: In a prospective, randomized, double-masked, placebo-controlled study, 80 children (38 boys and 42 girls), aged 4 to 10 years, scheduled for strabismus surgery, received intravenously either placebo or ramosetron at 1 of 3 different doses (3 microg/kg, 6 microg/kg, or 12 microg/kg) (n = 20 each) at the end of the surgical procedure [7].
• These results suggest that 5-HT increases Isc through the 5-HT3 and 5-HT4 receptors, and that ramosetron is a potent and selective 5-HT3 receptor antagonist in rat colonic mucosa [17].
• Contribution of P-glycoprotein to efflux of ramosetron, a 5-HT3 receptor antagonist, across the blood-brain barrier [18].
• KB-R6933 and ramosetron (0.03-1 mg/kg, p.o.) inhibited the diarrhea induced by 5-HT, but not that by castor oil or prostaglandin E2 (PGE2), in mice [24].
• In contrast, ramosetron and azasetron injected i.c.v. had no effect on CRH-induced defecation. alpha-Helical CRH-(9-41), ramosetron, and azasetron reduced defecation caused by restraint stress with ED50 values of 0.32, 3.6, and 19.7 micrograms/kg i.v., respectively [25].

Analytical, diagnostic and therapeutic context of Ramosetron

• Patients undergoing thyroidectomy were randomized to receive IV ramosetron 0.15, 0.3, or 0.6 mg or placebo at completion of the procedure [22].
• IMPLICATIONS: This randomized, double-blinded, placebo-controlled trial in 120 women found the effective dose of ramosetron for preventing postoperative nausea and vomiting after gynecological surgery to be 0.3 mg [26].
• Results of a prospective, randomized, double-blind, placebo-controlled, dose-ranging trial to determine the effective dose of ramosetron for the prevention of vomiting after tonsillectomy in children [8].
• CONCLUSIONS: In this population of patients receiving general anesthesia while undergoing thyroidectomy, ramosetron 0.3 mg was effective in preventing postoperative nausea and vomiting 0 to 48 hours after anesthesia [22].
• Methods: Fifty patients with malignant tumors undergoing their first chemotherapy were randomly divided into two groups, and each group received 0.3 mg of ramosetron and 16 mg of ondansetron in a prospective crossover comparison study [10].

References