Review Article





P Simon, M Jayachandran, R Vijendra, S Rao, MS Baliga, PL Palatty


ABSTRACT: In the treatment of cancer, nausea and vomiting are two of the most important and common toxiceffects of chemotherapy and adversely affects the patient’s quality of life and worse withdrawal from treatment. Physiologically, emesis is controlled by the vomiting centre in the medulla, that integrates afferent input from the vestibular system, the chemoreceptor trigger zone (CTZ), the cortex and the gut. Mechanistically, antiemetic mediate their action by blocking various type of receptors involved in inducing emesis and  located in different regions and various organ of the body. Some of the most important anti-emetics used in prevention of nausea and vomiting are ondansetron, granisetron, metochlopramide, aprepitant and palonosetron. In addition to this, aprepitantis also combined with dexamethasone and the 5-HT3 antagonists toenhance prevention of acute emesis. In this comprehensive review an attempt is made at summarizing on the various antiemetic agents and their usefulness in the treatment of cancer. Also emphasis is placed on the recent research on combination of antiemetic and elucidating the role of various agents used in the combinations of to mediate optimal effects.


KEY WORDS: chemotherapy-induced nausea and vomiting (CINV), anti-emetics, olanzapine


  1. Frame DG. Best practice management of CINV in oncology patients: I. Physiology and treatment of CINV. Multiple neurotransmitters and receptors and the need for combination therapeutic approaches. J Support Oncol 2010; 8(2 Suppl 1):5-9.

  2. Kris MG, Gralla RJ, Clark RA. Incidence, course and severity of delayed nausea and vomiting following the administration of high dose cisplatin. J ClinOncol 1985; 3:1379-1384.

  3. de Jongh FE, van Veen RN, Veltman SJ, de Wit R, van der Burg ME, van den Bent MJ et al. Weekly high-dose cisplatin is a feasible treatment option: analysis on prognostic factors for toxicity in 400 patients. Br J Cancer 2003; 88(8):1199- 1206.

  4. Kloth OD. New development and current challenges for antiemetic therapy for chemotherapy induced emesis. In:Weiner LM, ed. The cancer protocol guide, Philadelphia:Lipincott Williams and Witkins Healthcare; 2000: 6-11.

  5. Aapro MS, Grunberg SM, Manikhas GM, Olivares G, Suarez T, Tjulandin SA et al. A phase III, double-blind, randomized trial of palonosetron compared with ondansetron in preventing chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy. Annals of Oncology 2006; 17:1441–1449.

  6. Abhay R. Shelke, Mustian KM, Morrow GR. The Pathophysiology Of Treatment- Related NauseaAnd Vomiting In Cancer Patients: Current Models. Indian J PhysiolPharmacol 2004; 48:256–268.

  7. Washabau RJ, Elie S. Antiemetic therapy. In: Kirk RW, BonaguraJD,eds. Kirk’s Current Veterinary Therapy XII Small Animal Practice. Philadelphia: WB Saunders;1995:679-684.

  8. Burrows CF. Vomiting and regurgitation: a clinical perspective. Lehigh, Pennsylvania. ALPO Centre;1990:18-38.

  9. Adams HR. Pharmacology and Therapeutics. 8thedition.2001

  10. Willard MD. Some new approaches to the treatment of vomiting. JAVMA 1984; 184:590.

  11. Miller AD, Leslie RA. The area postrema and vomiting. Front Neuroendocrinol 1994;15(4):301-320.

  12. Complications of vomiting-The Boerhaave and the Mallory-Weiss syndromes- Medical Staff Conference, University of California, San Francisco. West J Med 1974;121:50-54

  13. Shelke AR, Mustian KM, Morrow GR. The pathophysiology of treatment-related nausea and vomiting in cancer patients: current models. Indian J PhysiolPharmacol. 2004 Jul; 48(3):256-268.

  14. Aapro MS, Molassiotis A, Olver I. Anticipatory nausea and vomiting. Support Care Cancer 2005; 13:117–121.

  15. American Society of Clinical Oncology guideline for antiemetics in oncology: update 2006.J ClinOncol. 2006 Jun20;24(18):2932- 2947.

  16. Girish C, Manikandan S. Aprepitant: A substance P antagonist for chemotherapy induced nausea and vomiting. Indian J Cancer 2007;44:25-30.

  17. Herrstedt J, Dombernowsky P. Anti-emetic therapy in cancer chemotherapy: current status. Basic ClinPharmacolToxicol. 2007;101:143–150.

  18. HerrstedtJ.Nauseaandemesis:Stillanunsolvedproblemincancerpatients? Support Care Cancer 2002;10:85-87.

  19. Berger M, Gray JA, Roth BL. The expanded biology of serotonin. Annu Rev Med. 2009;60:355-366. 

  20. Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. p.187.

  21. de Wit R, Aapro M, Blower PR (2005). "Is there a pharmacological basis for differences in 5-HT3-receptor antagonist efficacy in refractory patients?”. Cancer ChemotherPharmacol 56 (3):231–238.

  22. Gholipour T, Ghasemi M, Riazi K, Ghaffarpour M, Dehpour AR. Seizure susceptibility alteration through 5-HT(3) receptor: modulation by nitric oxide. Seizure. 2010 Jan; 19(1):17-22.

  23. Blower P. A pharmacologic profile of oral granisetron (Kytril tablets). SeminOncol1995; 22(suppl 10):3–5.

  24. Boccia RV, Gordan LN, Clark G, Howell JD, Grunberg SM. Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III study. Support Care Cancer. 2011;19(10): 1609.

  25. FDA Drug Safety Communication: Abnormal Heart Rhythms Associated with Use of Anzemet (DolasetronMesylate).Available at: http://www Accessed December 17, 2012.

  26. Wong EH, Clark R, Leung E, Loury D, Bonhaus DW, JakemanL, Parnes H, Whiting RL, Eglen RM. The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br J Pharmacol.1995;114(4):851–859.

  27. 27. MGI Pharma. Aloxi (PalonosetronHCl Injection). Bloomington, MN:MGI Pharma,204.

  28., accessed August 2, 2012

  29. Tanihata S, Oda S, Nakai S, Uchiyama T. Antiemetic effect of dexamethasone on cisplatin-induced early and delayed emesis in the pigeon. Eur J Pharmacol 2004;484:311–321.

  30. Ho CM, Ho ST, Wang JJ, et al. Dexamethasone has a central antiemetic mechanism in decerebrated cats. AnesthAnalg2004;99:734–739.

  31. Suzuki T, Sugimoto M, Koyama H, et al. Inhibitory effect of glucocorticoids on human-cloned 5-hydroxytryptamine3A receptor expressed in xenopus oocytes. Anesthesiology2004;101:660–665.

  32. Herrstedt J, Aapro MS, Smyth JF, Del Favero A. Corticosteroids, dopamine antagonists and other drugs. Support Care Cancer 1998;6:204–214.

  33. MARZENA ET AL 2007.

  34. Patel L, Lindley C. Aprepitant—a novel NK1-receptor antagonist. Expert OpinPharmacother.2003; 4:2279–2796.

  35. Massaro AM, Lenz KL. Aprepitant: A novel antiemetic for chemotherapy-induced nausea and vomiting. Ann Pharmacother2005; 39:77-85.

  36. Kufe DW, Pollock RE, Weichselbaum RR, et al., editors. Holland-Frei Cancer Medicine. 6th edition. Hamilton (ON): BC Decker; 2003. Physiology and pharmacology in                controlling emesis.                                 

  37. Majumdar AK, Howard L, Goldberg MR, Hickey L, Constanzer M, Rothenberg PL, Crumley TM, Panebianco D, Bradstreet TE, Bergman AJ, Waldman SA, Greenberg HE, Butler K, Knops A, De Lepeleire I, Michiels N, Petty KJ. Pharmacokinetics of aprepitant after single and multiple oral doses in healthy volunteers. J ClinPharmacol. 2006;46:291–300.

  38. Product information. Emend (Aprepitant). Merck: Whitehouse station, NJ; May 2003.

  39. Hesketh PJ, Grunberg SM, Gralla RJ, Warr DG, Roila F, de Wit R, et al. The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: A multinational, randomized, double-blind, placebo- controlled trial in patients receiving high-dose cisplatin-the Aprepitant Protocol 052 Study Group. J ClinOncol2003;21:4112-4119.

  40. ID=402, accessed June 4,2012

  41. Patrick Langford, Paul Chrisp.Fosaprepitant and aprepitant: an update of the evidence for their place in the prevention of chemotherapy-induced nausea and vomiting 2010 Volume 2010:5; 77 –90.

  42. Billy R. Martin, Jenny L. Wiley. Mechanism of Action of Cannabinoids: How It May Lead to Treatment of Cachexia, Emesis, and Pain. J Support Oncol 2004;2:305–316.

  43. M. Ben Amar. Cannabinoids in medicine: A review of their therapeutic potential Journal of Ethnopharmacology 105 (2006)1–25.

  44. Mark A Ware1,Paul Daeninck,VincentMaidaA review of nabilone in the treatment of chemotherapy-induced nausea and vomiting TherClin Risk Manag. 2008 February; 4(1):99–107

  45. Hutcheon, A.W et al. A randomisedmulticentre single blind comparison of a cannabinoid antiemetic (levonantradol) with chlorpromazine in patients receiving their first cytotoxic chemotherapy. European Journal of Cancer and Clinical Oncology,1983; 19:1087–1090.

  46. Justin-Besancon, L.; Laville, C. (1964). "Antiemetic Action of Metoclopramide with Respect to Apomorphine and Hydergine" (in French). ComptesRendus des Séances de la Société de Biologieet de sesFiliales 158:723–727.

  47. K.D Tripathi. Essentials of medical pharmacology. 6thedition

 To cite this article:

Simon P, Jaichandran M, Vijendra R, Rao S, Baliga MS, Palatty PL. Usefulness of anti-emetics in the treatment of cancer: a review. Int. J. Med. Lab. Res. 2021; 6,2:33-45.