Is there a pharmacological basis for differences in 5-HT3-receptor antagonist efficacy in refractory patients?
5-HT3-receptor antagonists are the current antiemetic 'gold standard' for chemotherapy- and radiotherapy-induced nausea and vomiting. Interestingly, studies have shown that patients experiencing poor control of acute chemotherapy-induced nausea and vomiting with one antiemetic therapy may respond well to another agent, including a drug of the same class. This review examines pharmacological differences between the 5-HT3-receptor antagonists in order to determine potential reasons for their differing efficacy, particularly in relation to refractory emesis. Differences in drug metabolism by the cytochrome P450 system, inadequate dosing of the respective agents, differences in onset and duration of action, and effects on serotonin release and reuptake are discussed.
de Wit
Ronald
R
Rotterdam Cancer Institute, Groene Hilledijk 301, 3075, Rotterdam, The Netherlands. r.dewit@erasmusmc.nl
Aapro
Matti
M
Blower
Peter R
PR
D000932:Antiemetics / Q000494:pharmacology / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000009:adverse effects; D006801:Humans; D009325:Nausea / Q000139:chemically induced / Q000188:drug therapy*; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism; D058831:Serotonin 5-HT3 Receptor Antagonists; D012702:Serotonin Antagonists / Q000494:pharmacology / Q000627:therapeutic use*; D014839:Vomiting / Q000139:chemically induced / Q000188:drug therapy*
D000932:Antiemetics; D000970:Antineoplastic Agents; D044406:Receptors, Serotonin, 5-HT3; D058831:Serotonin 5-HT3 Receptor Antagonists; D012702:Serotonin Antagonists