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Antiemetics

Last updated: June 30, 2021

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Antiemetics are a heterogeneous group of drugs used to treat various causes of nausea and vomiting. Different antiemetics act on different receptors, and they may have a peripheral effect, a central effect, or both. Whereas serotonin antagonists, for example, bind 5-HT3 receptors and effectively combat cytotoxic drug nausea, certain anticholinergic drugs target M1 receptors and specifically treat motion sickness (kinetosis). Hospitals and clinics commonly use the dopamine D2 antagonist metoclopramide. However, because of its strong central effect and possible extrapyramidal side effects, metoclopramide must be used with caution.

Overview of antiemetics
Antiemetic class Drug Mechanism of action Clinical use Side effects
Dopamine receptor antagonists
  • Prochlorperazine [1]
  • Metoclopramide [2]
  • Domperidone

Serotonin receptor antagonists

(5-HT3 antagonists)

  • Ondansetron [3]
  • Granisetron
  • Dolasetron
  • Palonosetron
Anticholinergic agents [4]
  • Scopolamine

Antihistamines

  • Meclizine
  • Dimenhydrinate
  • Diphenhydramine
  • Doxylamine
  • Promethazine

Neurokinin receptor antagonists

  • Aprepitant
  • Fosaprepitant
  • NK1 antagonist
  • Inhibition of NK1 receptors in the solitary nucleus central antiemetic effect
  • Additional inhibition of substance P-induced vomiting due to antagonism

Glucocorticoids

Benzodiazepines [7][8]

  • GABA agonist
  • Central antiemetic effect likely due to depression of the chemotrigger zone [8]

Atypical antipsychotics [7][8][9][10]

Cannabinoids [7][11][12]

References:[13]

References:[13]

We list the most important contraindications. The selection is not exhaustive.

  1. Prochlorperazine. https://www.drugbank.ca/drugs/DB00433. Updated: December 8, 2016. Accessed: February 21, 2017.
  2. FDA Requires Boxed Warning and Risk Mitigation Strategy for Metoclopramide-Containing Drugs Agency warns against chronic use of these products to treat gastrointestinal disorders. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2009/ucm149533.htm. Updated: April 18, 2013. Accessed: February 21, 2017.
  3. Ondansetron. https://www.drugs.com/pro/ondansetron.html. Updated: February 21, 2017. Accessed: February 21, 2017.
  4. Pedigo NW Jr, Brizzee KR. Muscarinic cholinergic receptors in area postrema and brainstem areas regulating emesis.. Brain Res Bull. 1985; 14 (2): p.169-77.
  5. Flake Z, Linn B, Hornecker J. Practical Selection of Antiemetics in the Ambulatory Setting. Am Fam Physician. 2015 .
  6. James E. Tisdale. Drug-induced Diseases: Prevention, Detection, and Management. American society of health-system phramacists : p. 834
  7. NCCN clinical Practice Guidelines in Oncology: Antiemesis, Version 1.2019. https://www.nccn.org/professionals/physician_gls/pdf/antiemesis.pdf. Updated: February 28, 2019. Accessed: September 16, 2019.
  8. Perwitasari DA, Gelderblom H, Atthobari J, et al. Anti-emetic drugs in oncology: pharmacology and individualization by pharmacogenetics. International Journal of Clinical Pharmacy. 2011; 33 (1): p.33-43. doi: 10.1007/s11096-010-9454-1 . | Open in Read by QxMD
  9. Tan L, Liu J, Liu X, et al. Clinical research of Olanzapine for prevention of chemotherapy-induced nausea and vomiting. Journal of Experimental & Clinical Cancer Research. 2009; 28 (1): p.131. doi: 10.1186/1756-9966-28-131 . | Open in Read by QxMD
  10. Brafford MV, Glode A. Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting.. Journal of the advanced practitioner in oncology. 2014; 5 (1): p.24-9.
  11. Sharkey KA, Wiley JW. The Role of the Endocannabinoid System in the Brain–Gut Axis. Gastroenterology. 2016; 151 (2): p.252-266. doi: 10.1053/j.gastro.2016.04.015 . | Open in Read by QxMD
  12. Darmani NA. Mechanisms of Broad-Spectrum Antiemetic Efficacy of Cannabinoids against Chemotherapy-Induced Acute and Delayed Vomiting. Pharmaceuticals. 2010; 3 (9): p.2930-2955. doi: 10.3390/ph3092930 . | Open in Read by QxMD
  13. Katzung B,Trevor A. Basic and Clinical Pharmacology. McGraw-Hill Education ; 2014