The 5-HT3 receptor antagonists are the most potent antiemetics known at pre
sent. Lerisetron is a new 5-HT3 receptor antagonist chemically unrelated to
other antagonists like Ondansetron. An emesis model in the dog induced by
irradiation with Co-60 was used, and 8 Gy were administered over the total
body surface. An irradiated control group was established and received no m
edication, and two irradiated groups received treatment with either Ondanse
tron or Lerisetron. The 'up-down' technique was employed to determine the e
ffective dose (ED50). A logarithmic scale was used to increase or decrease
the doses in each case. The initial doses were 300 mu g/kg for Ondansetron
and 100 mu g/kg for Lerisetron. All animals in the control group vomited. T
he ED50 of Ondansetron was 178 +/- 151 mu g/kg body wt and that of Lerisetr
on was 63 +/- 18 mu g/kg. Lerisetron is more potent and presented less indi
vidual variability than Ondansetron, but its antiemetic effects were equall
y effective.