Granisetron: The second serotonin-receptor antagonist

OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of granisetron, focusing on critical analysis of published clinical trials and comparison with other antiemetic agents, including ondansetron. DATA SOURCES: MEDLINE (1966-1995) and CANCERLIT (1991- 1995) searches of English-language literature using the terms 'granisetron' and 'granisetron (m)' were performed. STUDY SELECTION AND DATA EXTRACTION: All articles were considered for possible inclusion in this review. Abstracts of clinical trials were included only when they were judged to add critical information not otherwise available in the medical literature. For studies published more than once, the most recent publication was cited. DATA SYNTHESIS: Nausea and vomiting are rated by patients as the most distressing chemotherapy-related adverse effects and may produce potentially life- threatening complications. The discovery of the role of serotonin in nausea and vomiting and the development of selective serotonin₃-receptor (5-HT₃) antagonists has significantly diminished the incidence and consequences of chemotherapy-related nausea and vomiting. Granisetron is the second 5-HT₃- receptor antagonist to be marketed in the US. Granisetron has been compared with other antiemetic agents, including ondansetron, against highly and moderately emetogenic chemotherapy. The results of these trials have shown granisetron to be superior to conventional antiemetics and as effective as ondansetron in the prevention of chemotherapy-induced nausea and vomiting. The optimal dose of granisetron has yet to be determined. Formulary decision should be based on a cost comparison among the 5-HT₃-receptor antagonists at individual institutions. CONCLUSIONS: Granisetron is a safe, effective antiemetic agent for the management of nausea and vomiting caused by cancer chemotherapy.