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.