• Clinical science
  • Clinician

Antiemetics

Summary

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

Antiemetic class Drug Mechanism of action Clinical use Side effects
Dopamine receptor antagonists
  • Prokinetic effect used to treat diabetic and postsurgery gastroparesis (delayed gastric emptying)
  • Hyperemesis gravidarum
  • Persistent GERD
  • D2 antagonist
  • Central antiemetic effect at the area postrema
  • Prokinetic effect

Serotonin receptor antagonists

(5-HT3 antagonists)

  • 5-HT3 antagonist
  • Strong central antiemetic effect at the area postrema
  • Peripheral antiemetic effect via inhibition of the vagus nerve
Anticholinergic agents
  • Motion sickness, vestibular-induced nausea, and vomiting

Antihistamines

Neurokinin receptor antagonists

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

Glucocorticoids

Benzodiazepines [3][4]

  • GABA agonist
  • Central antiemetic effect likely due to depression of the chemotrigger zone [4]

Atypical antipsychotics [3][4][5][6]

Cannabinoids [3][7][8]

  • Cannabinoid (CB1 and CB2) agonists
  • Central antiemetic effect: CB1 agonism in the brain stem suppresses the emetic reflex.
  • Peripheral antiemetic effect: CB2 agonism in the gastrointestinal tract inhibits gastrointestinal motility.
  • CINV treatment
  • Anorexia causing weight loss in patients with advanced HIV


References:[9][9][9][10][10][10][10][11][12][13][14][15][16][17]

Indications

References:[10][18][13]

Contraindications

References:[18][13][15]

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

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  • 12. U.S. Food and Drug Administration. 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.
  • 13. Drugs.com. Ondansetron. https://www.drugs.com/pro/ondansetron.html. Updated February 21, 2017. Accessed February 21, 2017.
  • 14. UpToDate. Prochlorperazine: Drug information. In: Post TW, ed. UpToDate. Waltham, MA: UpToDate. https://www.uptodate.com/contents/prochlorperazine-drug-information. Last updated January 1, 2017. Accessed March 22, 2017.
  • 15. UpToDate. Metoclopramide: Drug information. In: Post TW, ed. UpToDate. Waltham, MA: UpToDate. https://www.uptodate.com/contents/metoclopramide-drug-information. Last updated January 1, 2017. Accessed March 22, 2017.
  • 16. McInnis M, Mehta S, Lewis C, et al. Step-Up to USMLE Step 1 2015 . Lippincott Williams & Wilkins; 2014.
  • 17. Pedigo NW Jr, Brizzee KR. Muscarinic cholinergic receptors in area postrema and brainstem areas regulating emesis. Brain Res Bull. 1985; 14(2): pp. 169–77. pmid: 3995361.
  • 18. Katzung B,Trevor A. Basic and Clinical Pharmacology. McGraw-Hill Education; 2014.
last updated 03/27/2020
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