Antiemetic effects of Lerisetron in radiation-induced emesis in the dog.
The 5-HT3 receptor antagonists are the most potent antiemetics known at present. 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 60Co was used, and 8 Gy were administered over the total body surface. An irradiated control group was established and received no medication, and two irradiated groups received treatment with either Ondansetron or Lerisetron. The 'up-down' technique was employed to determine the effective dose (ED50). A logarithmic-scale was used to increase or decrease the doses in each case. The initial doses were 300 microg/kg for Ondansetron and 100 microg/kg for Lerisetron. All animals in the control group vomited. The ED50 of Ondansetron was 178+/-151 microg/kg body wt and that of Lerisetron was 63+/-18 microg/kg. Lerisetron is more potent and presented less individual variability than Ondansetron, but its antiemetic effects were equally effective.
Department of Experimental Surgery, La Paz Hospital, Madrid, Spain.
I A
IA
Gomez-de-Segura
A G
AG
Grande
E
E
De Miguel
D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage*; D001562:Benzimidazoles / Q000008:administration & dosage*; D003037:Cobalt Radioisotopes / Q000009:adverse effects; D004285:Dogs; D004334:Drug Administration Schedule; D017294:Ondansetron / Q000008:administration & dosage*; D010880:Piperidines / Q000008:administration & dosage*; D011878:Radiotherapy / Q000009:adverse effects*; D012702:Serotonin Antagonists / Q000008:administration & dosage*; D014839:Vomiting / Q000188:drug therapy* / Q000209:etiology
D000932:Antiemetics; D001562:Benzimidazoles; D003037:Cobalt Radioisotopes; D010880:Piperidines; D012702:Serotonin Antagonists; D017294:Ondansetron; C115094:lerisetron