Granisetron. A review of its pharmacological properties and therapeutic use as an antiemetic

Drugs. 1991 Nov;42(5):805-24. doi: 10.2165/00003495-199142050-00007.


Granisetron (BRL 43694) is a highly selective 5-HT3 receptor antagonist which possesses significant antiemetic activity, likely mediated through antagonism of 5-HT3 receptors on abdominal vagal afferents and possibly in or near the chemoreceptor trigger zone. Clinical trials in cancer patients demonstrate that, compared with placebo, granisetron significantly reduces the incidence of nausea and vomiting for 24 hours after administration of high-dose cisplatin. In large comparative trials, 70% of patients who received granisetron prior to cisplatin or other chemotherapy experienced complete inhibition of vomiting with little or no nausea for 24 hours after antineoplastic administration; these results were similar to those obtained with high-dose metoclopramide plus dexamethasone, and superior to a combination of chlorpromazine plus dexamethasone, or prochlorperazine plus dexamethasone, or methylprednisolone monotherapy. The most frequently reported adverse event associated with granisetron administration is headache which occurs in about 10 to 15% of patients while constipation, somnolence, diarrhoea and minor transient changes in blood pressure have been reported less frequently. Extrapyramidal effects, which can occur with high-dose metoclopramide and may be a limiting factor in its use, have not been noted with granisetron administration. Thus, granisetron is an effective, well tolerated and easily administered agent for the prophylaxis of nausea and vomiting induced by cancer chemotherapy which appears to be devoid of extrapyramidal side effects associated with metoclopramide. As a member of a new class of drugs, the selective 5-HT3 receptor antagonists, granisetron provides the medical oncologist with a new, potentially more acceptable antiemetic therapy.

Publication types

  • Clinical Trial
  • Multicenter Study
  • Review

MeSH terms

  • Animals
  • Antiemetics / administration & dosage
  • Antiemetics / pharmacokinetics
  • Antiemetics / pharmacology
  • Antiemetics / therapeutic use*
  • Antineoplastic Agents / adverse effects
  • Female
  • Granisetron
  • Humans
  • Indazoles / administration & dosage
  • Indazoles / pharmacokinetics
  • Indazoles / pharmacology
  • Indazoles / therapeutic use*
  • Male
  • Nausea / chemically induced
  • Nausea / prevention & control
  • Neoplasms / drug therapy
  • Serotonin Antagonists
  • Vomiting / chemically induced
  • Vomiting / prevention & control


  • Antiemetics
  • Antineoplastic Agents
  • Indazoles
  • Serotonin Antagonists
  • Granisetron