Oral formulations of the selective serotonin3 antagonists ramosetron (intraoral disintegrator formulation) and granisetron hydrochloride (standard tablet) in treating acute chemotherapy-induced emesis, nausea, and anorexia: a multicenter, randomized, single-blind, crossover, comparison study.

Background: Chemotherapeutic drugs used to treat cancer may cause nausea and emesis by inducing the release of 5-hydroxytryptamine (5-HT) in the small intestine. Blockage of 5-HT[3] receptors in the small intestine by 5-HT[3]-receptor antagonists might prevent the nausea and vomiting associated with chemotherapy for cancer.Objective: The aim of this study was to compare the efficacy and tolerability of the selective 5-HT[3] antagonists ramosetron (0.1-mg intraoral disintegrator preparation) and granisetron hydrochloride (2-mg standard tablet) in the treatment of acute chemotherapy-induced digestive disturbances.Methods: Male and female Chinese cancer patients aged 16 to 74 years were eligible for this multicenter, randomized, single-blind, crossover, comparison study. Patients were randomized to 1 of 2 treatment groups. Group 1 received 1-time administration of ramosetron 0.1 mg orally without water, followed by a 2-week washout period after which they received granisetron 2 mg orally with water. Group 2 received granisetron 2 mg orally with water, followed by a 2-week washout period after which they received ramosetron 0.1 mg orally without water. Each study drug was administered 1 time, 1 hour before infusion of the chemotherapeutic agent. For the efficacy assessment, response data were recorded every 6 hours for a total of 24 hours after the start of chemorecorded continuously over 24 hours.Results: A total of 73 patients (46 males, 27 females; mean age, 49.6 years [range, 17-70 years]) were enrolled. Group 1 comprised 37 patients; group 2, 36 patients. Data from 62 (84.9%) patients were used in the efficacy assessment; data from 70 (95.9%) patients were used in the tolerability assessment. The ability of ramosetron to prevent emesis, nausea, and anorexia was similar to that of granisetron during the 0-to-6-hour and 0-to-24-hour periods following administration of cisplatin or doxorubicin chemotherapy. The tolerability of ramosetron was similar to that of granisetron; AEs were generally mild and transient.Conclusions: In this study, both the intraoral disintegrator formulation of ramosetron and the standard tablet formulation of granisetron were clinically useful for preventing chemotherapy-induced digestive disturbances in cancer patients. [ABSTRACT FROM AUTHOR]