Antiemetic effects of Lerisetron in radiation-induced emesis in the dog.

Abstract

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.

• Authors: I A Gomez-de-Segura, A G Grande, E De Miguel
• Journal: Acta oncologica (Stockholm, Sweden) (Acta Oncol) Vol. 37 Issue 7-8 Pg. 759-63 ( 1998) ISSN: 0284-186X [Print] England
• PMID: 10050999 (Publication Type: Journal Article)

Chemical References

• Antiemetics
• Benzimidazoles
• Cobalt Radioisotopes
• Piperidines
• Serotonin Antagonists
• Ondansetron
• lerisetron

Topics

• Animals
• Antiemetics (administration & dosage)
• Benzimidazoles (administration & dosage)
• Cobalt Radioisotopes (adverse effects)
• Dogs
• Drug Administration Schedule
• Ondansetron (administration & dosage)
• Piperidines (administration & dosage)
• Radiotherapy (adverse effects)
• Serotonin Antagonists (administration & dosage)
• Vomiting (drug therapy, etiology)