The role of second-generation 5-HT3 receptor antagonists in managing chemotherapy-induced nausea and vomiting in hematological malignancies.

Abstract

Compared with solid tumor patients, those with hematological malignancies are at particular risk of chemotherapy-induced nausea and vomiting (CINV) because of their young age, exposure to highly-emetogenic induction, consolidation and salvage regimens, the high-dose conditioning regimens used before stem cell transplantation (SCT), and the heavy psychological burden of such treatments. In the absence of prophylaxis, around 75% of patients undergoing SCT experience delayed CINV. With first-generation 5-HT(3) receptor antagonists, only about 20% are completely protected from nausea and vomiting, and this frequent and debilitating adverse event has not been fully addressed. In contrast to solid tumors, there are no internationally agreed guidelines for the prevention and treatment of CINV in hematological malignancies. Work on a consensus is urgently required. The second-generation 5-HT(3) antagonist palonosetron is highly effective in preventing CINV in patients with solid tumors. The extended half-life of this agent and its mechanisms of action including allosteric binding, positive cooperativity and 5-HT(3) receptor internalization, may make it particularly effective in controlling delayed CINV. Although controlled comparisons against first-generation 5HT(3) agents have not yet been conducted in the setting of SCT, available evidence suggests that palonosetron may prove beneficial in preventing CINV in high risk patients with hematological malignancies.

• Authors: Lee S Schwartzberg, Peter Jacobs, Panagiota Matsouka, Wellington Azevedo, Antonio Pinto
• Journal: Critical reviews in oncology/hematology (Crit Rev Oncol Hematol) Vol. 83 Issue 1 Pg. 59-70 (Jul 2012) ISSN: 1879-0461 [Electronic] Netherlands
• PMID: 22321726 (Publication Type: Journal Article, Review)
• Copyright: Copyright © 2012. Published by Elsevier Ireland Ltd.

Chemical References

• Antiemetics
• Antineoplastic Agents
• Isoquinolines
• Quinuclidines
• Receptors, Serotonin, 5-HT3
• Serotonin 5-HT3 Receptor Antagonists
• Palonosetron

Topics

• Antiemetics (administration & dosage, pharmacokinetics, therapeutic use)
• Antineoplastic Agents (administration & dosage, adverse effects)
• Clinical Trials, Phase III as Topic
• Half-Life
• Hematologic Neoplasms (therapy)
• Hematopoietic Stem Cell Transplantation
• Humans
• Isoquinolines (administration & dosage, pharmacokinetics, therapeutic use)
• Nausea (drug therapy, etiology, prevention & control)
• Palonosetron
• Quinuclidines (administration & dosage, pharmacokinetics, therapeutic use)
• Receptors, Serotonin, 5-HT3 (metabolism)
• Salvage Therapy
• Serotonin 5-HT3 Receptor Antagonists (administration & dosage, pharmacokinetics, therapeutic use)
• Stem Cell Transplantation
• Transplantation Conditioning (adverse effects)
• Vomiting (drug therapy, etiology, prevention & control)