5-HT(3)-receptor antagonists for the treatment of nausea and vomiting: a reappraisal of their side-effect profile

Abstract

Nausea and vomiting can cause considerable distress and discomfort to patients undergoing chemotherapy, radiotherapy, or surgery. Several classes of antiemetic agents exist to combat these side effects, though the 5-HT(3)-receptor antagonists have become the first-line treatment choice for many cancer patients and are considered the "gold standard" in antiemetic therapy. Compared with the older generation antiemetic drugs, 5-HT(3)-receptor antagonists are effective, well tolerated, and associated with few side effects. However, emerging differences among these agents suggest that the incidence and/or intensity of adverse events should not be regarded as a class effect. The side-effect profile of any supportive care therapy is particularly important in certain subgroups of patients, including pediatric patients and the elderly, as well as those suffering comorbid conditions, such as cardiovascular disease and renal or hepatic impairment. Indeed, dolasetron is associated with cardiovascular effects, and thus, should be used with extreme caution in patients who suffer from or may develop prolongation of cardiac conduction intervals. Ondansetron, on the other hand, is associated with a greater incidence of central nervous system side effects than either dolasetron or ondansetron, and pharmacokinetic parameters are affected in patients with hepatic impairment, thereby requiring dose adjustments. Clinicians are encouraged to evaluate patients on an individual basis when choosing which 5-HT(3)-receptor antagonist to prescribe.