First-Generation 5-HT3 Receptor Antagonists

  • Roy Chen
  • Kathy Deng
  • Harry RaftopoulosEmail author


Chemotherapy-induced nausea and vomiting (CINV) is a significant side effect of cancer therapy and can lead to poor compliance with therapy, treatment delays, dehydration, hospitalization, and a marked decrement in patient quality of life. With appropriate CINV control, safe outpatient administration of chemotherapy can be accomplished with no change in patients’ pre-therapy quality of life. Over the last 30 years, developments have improved in the control of CINV, including the advent of 5-hydroxytryptamine-3 (5HT-3) receptor antagonists which are an integral ingredient in regimens used today. With the variety of chemotherapy regimens today and the ongoing development of new combinations in addition to targeted therapy, there have been corresponding dynamic goals for control of not only CINV in general but in differentiating control of nausea over and above that of vomiting. In fact, current antiemetic therapy conceptually fulfills the true definition of “targeted therapy” as there is significant understanding of pathways involved in emesis as well as specific targeted antagonists to these pathways. This chapter will focus on the 5HT-3 pathway and the specific receptor antagonists to this pathway.


Emetogenic Chemotherapy Antiemetic Efficacy Oral Ondansetron Oral Granisetron Dorsal Vagal Nucleus 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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© Springer International Publishing Switzerland 2016

Authors and Affiliations

  1. 1.Hematology-OncologyNorth Shore Hematology Oncology AssociatesEast SetauketUSA
  2. 2.Hematology-OncologyNorth Shore LIJ School of MedicineHempsteadUSA
  3. 3.Merck & Co.RahwayUSA

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