5-HT3-receptor antagonists: a review of pharmacology and clinical efficacy.
OBJECTIVE
To review the role of serotonin in chemotherapy-induced emesis and the mechanism by which 5-hydroxytryptamine3 (5-HT3)-receptor antagonists block the action of serotonin; to review the pharmacology and clinical efficacy of the 5-HT3-receptor antagonists in controlling nausea and vomiting induced by highly emetogenic chemotherapy regimens, including a comparison of agents in this class.


METHODS
Journal articles and proceedings of clinical oncology conferences.


RESULTS
Prior to the availability of 5-HT3-receptor antagonists, metoclopramide was the therapy of choice for prevention of cisplatin-associated emesis. Several randomized, double-blind, comparative trials have established that a 5-HT3-receptor antagonist used alone is more effective than metoclopramide and equal to or better than the combination of metoclopramide and dexamethasone.


CONCLUSIONS
5-HT3-receptor antagonists contribute significantly to the current armamentarium of antiemetic agents. Clinical trials consistently have demonstrated a benefit with these agents that exceeds the previously established antiemetic standards.


CONCLUSIONS
5-HT3-receptor antagonists have had a profound impact on the clinical management of acute chemotherapy-induced nausea and vomiting. Based on their unique mechanism of action and low toxicity profile, the 5-HT3-receptor antagonists offer a relatively new approach to controlling nausea and vomiting associated with highly emetogenic chemotherapy.
Cunningham
R S
RS
Cancer Institute of New Jersey, New Brunswick.
D000932:Antiemetics / Q000494:pharmacology / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000009:adverse effects; D017829:Granisetron / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D009325:Nausea / Q000139:chemically induced / Q000188:drug therapy* / Q000503:physiopathology; D017294:Ondansetron / Q000494:pharmacology / Q000627:therapeutic use; D012702:Serotonin Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D014839:Vomiting / Q000139:chemically induced / Q000188:drug therapy* / Q000503:physiopathology
D000932:Antiemetics; D000970:Antineoplastic Agents; D017829:Granisetron; D017294:Ondansetron; D012702:Serotonin Antagonists