5-HT3-receptor antagonists: a review of pharmacology and clinical efficacy.

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.Journal articles and proceedings of clinical oncology conferences.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.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.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.