GRANISETRON - THE 2ND SEROTONIN-RECEPTOR ANTAGONIST

OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical effi cacy, and adverse effects of granisetron, focusing on critical analysi s of published clinical trials and comparison with other antiemetic ag ents, including ondansetron. DATA SOURCES: MEDLINE (1966-1995) and CAN CERLIT (1991-1995) searches of English-language literature using the t erms ''granisetron'' and ''granisetron (m)'' were performed. STUDY SEL ECTION AND DATA EXTRACTION: All articles were considered for possible inclusion in this review. Abstracts of clinical trials were included o nly when they were judged to add critical information not otherwise av ailable in the medical literature. For studies published more than onc e, the most recent publication was cited. DATA SYNTHESIS: Nausea and v omiting are rated by patients as the most distressing chemotherapy-rel ated adverse effects and may produce potentially life-threatening comp lications. The discovery of the role of serotonin in nausea and vomiti ng and the development of selective serotonin(3)-receptor (5-HT3) anta gonists 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 bee n compared with other antiemetic agents, including ondansetron, agains t highly and moderately emetogenic chemotherapy. The results of these trials have shown granisetron to be superior to conventional antiemeti cs and as effective as ondansetron in the prevention of chemotherapy-i nduced nausea and vomiting. The optimal dose of granisetron has yet to be determined. Formulary decisions should be based on a cost comparis on among the 5-HT3-receptor antagonists at individual institutions. CO NCLUSIONS: Granisetron is a safe, effective antiemetic agent for the m anagement of nausea and vomiting caused by cancer chemotherapy.