Antiemetic

An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. They may be used for severe cases of gastroenteritis, especially if the patient is dehydrated.

Types

5-HT3 antagonist
  • 5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they can be used to treat post-operative and cytotoxic drug nausea & vomiting. However, they can also cause constipation or diarrhea, dry mouth, and fatigue.[1]
    • Dolasetron (Anzemet) can be administered in tablet form or in an injection.
    • Granisetron (Kytril, Sancuso) can be administered in tablet (Kytril), oral solution (Kytril), injection D(Kytril), or in a single transdermal patch to the upper arm (SANCUSO).
    • Ondansetron (Zofran) is administered in an oral tablet form, orally dissolving tablet form, orally dissolving film, sublingual, or in an IV/IM injection.
    • Tropisetron (Setrovel, Navoban) can be administered in oral capsules or in injection form.
    • Palonosetron (Aloxi) can be administered in an injection or in oral capsules.

Dopamine antagonist
  • Dopamine antagonists act on the brainstem and are used to treat nausea and vomiting associated with cancer, radiation sickness, opioids, cytotoxic drugs and general anaesthetics. Side effects include muscle spasms and restlessness.[1]
    • Amisulpride (Barhemsys), administered by intravenous injection.
    • Domperidone (Motilium)
    • Olanzapine (Zyprexa)
    • Trimethobenzamide
    • Haloperidol (limited in usefulness by extra-pyramidal and sedative side-effects)
    • Alizapride
    • Prochlorperazine (Compazine, Stemzine, Buccastem, Stemetil, Phenotil)
    • Chlorpromazine (Use limited by sedating properties)
    • Metoclopramide
    • Promethazine (Pentazine, Phenergan, Promacot) can be administered via a rectal suppository, intravenous injection, oral tablet or oral suspension for adults and children over 2 years of age.

NK1 receptor antagonist
  • NK1 receptor antagonist
    • Aprepitant (Emend) is a commercially available NK1 Receptor antagonist
    • Casopitant is an investigational NK1 receptor antagonist
    • Rolapitant (Varubi) another recently approved drug from this class

Antihistamine
  • Antihistamines (H1 histamine receptor antagonists) are effective in many conditions, including motion sickness, morning sickness in pregnancy, and to combat opioid nausea. H1 receptors in central areas include area postrema and vomiting center in the vestibular nucleus. Also, many of the antihistamines have anticholinergic properties that block muscarinic receptors at the same sites. The American Gastroenterological Association (AGA) recommends the use of antihistamines and anti-cholinergics in the treatment of nausea secondary to vertigo and motion sickness. [2]
    • Cinnarizine (UK only)
    • Cyclizine
    • Diphenhydramine (Benadryl)
    • Dimenhydrinate (Gravol, Dramamine)
    • Doxylamine, it is used in the combination drug pyridoxine/doxylamine to treat nausea and vomiting of pregnancy.[3][4]
    • Mirtazapine (Remeron) is an antidepressant that also has antiemetic effects[5][6] it is also a potent histamine H1 receptor antagonist, Ki=1.6 nM.[7]
    • Meclizine (Bonine, Antivert)
    • Promethazine (Pentazine, Phenergan, Promacot) can be administered via a rectal suppository, intravenous injection, oral tablet or oral suspension for adults and children over 2 years of age.
    • Hydroxyzine (Vistaril) is used in the treatment of nausea due to motion sickness.[8]

Cannabinoid
  • Cannabinoids are used in patients with cachexia, cytotoxic nausea, and vomiting, or who are unresponsive to other agents. These may cause changes in perception, dizziness, and loss of coordination.[1]

Benzodiazepines

Anticholinergic
  • Anticholinergics. The American Gastroenterological Association (AGA) recommends the use of antihistamines and anti-cholinergics in the treatment of nausea secondary to vertigo and motion sickness. [14]
    • Hyoscine (also known as scopolamine)
    • Diphenhydramine
    • Promethazine (Pentazine, Phenergan, Promacot) can be administered via a rectal suppository, intravenous injection, oral tablet or oral suspension for adults and children over 2 years of age.

Steroid
  • Steroids
    • Dexamethasone (Decadron) is given in low dose at the onset of a general anesthetic as an effective antiemetic. It is also used in chemotherapy as a single drug as well as with other antiemetics such as 5-HT3 receptor antagonists and NK1 receptor antagonist, but the specific mechanism of action is not fully understood.[15]

Angiosperms
    • Ginger contains 5-HT3 antagonists gingerols, shogaols,[16] and galanolactone.[17] Preliminary clinical data suggests ginger may be effective for treatment of nausea and/or vomiting in a number of settings.[18][19]

Other
    • Muscimol is purported to have antiemetic activity.[20]
    • Gabapentin [21]
    • Pyridoxine/doxylamine for pregnancy associated nausea

See also
  • Cancer and nausea
  • Emetic – substances that induce nausea and vomiting

References
  1. http://www.mesotheliomaweb.org/mesothelioma/treatment/chemotherapy/anti-Enausea-treatment/%5B%5D
  2. Flake ZA, Scalley RD, Bailey AG (March 2004). "Practical selection of antiemetics". American Family Physician. 69 (5): 1169–74. PMID 15023018. Archived from the original on 24 March 2016. Retrieved 10 March 2016.
  3. Madjunkova, S; Maltepe, C; Koren, G (June 2014). "The delayed-release combination of doxylamine and pyridoxine (Diclegis®/Diclectin®) for the treatment of nausea and vomiting of pregnancy". Paediatric Drugs. 16 (3): 199–211. doi:10.1007/s40272-014-0065-5. PMC 4030125. PMID 24574047.
  4. Cada, DJ; Demaris, K; Levien, TL; Baker, DE (October 2013). "Doxylamine succinate/pyridoxine hydrochloride". Hospital Pharmacy. 48 (9): 762–6. doi:10.1310/hpj4809-762. PMC 3857125. PMID 24421551.
  5. Pae C-U (2006). "Low-dose mirtazapine may be successful treatment option for severe nausea and vomiting". Progress in Neuro-Psychopharmacology and Biological Psychiatry. 30 (6): 1143–5. doi:10.1016/j.pnpbp.2006.03.015. PMID 16632163.
  6. Kast RE, Foley KF (July 2007). "Cancer chemotherapy and cachexia: mirtazapine and olanzapine are 5-HT3 antagonists with good antinausea effects". European Journal of Cancer Care. 16 (4): 351–4. doi:10.1111/j.1365-2354.2006.00760.x. PMID 17587360.
  7. National Institute of Mental Health. PDSD Ki Database (Internet) [cited 2013 Sep 27]. Chapel Hill (NC): University of North Carolina. 1998-2013. Available from: "Archived copy". Archived from the original on 2013-11-08. Retrieved 2013-12-01.CS1 maint: archived copy as title (link)
  8. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  9. Vincent, Beverly J.; McQuiston, Debra J.; Einhorn, Lawrence H.; Nagy, Catherine M.; Brames, Mary J. (1983-05-01). "Review of Cannabinoids and their Antiemetic Effectiveness". Drugs. 25 (1): 52–62. doi:10.2165/00003495-198300251-00006. ISSN 1179-1950. PMID 6301800.
  10. "Drug Scheduling". www.dea.gov. Retrieved 2019-02-21.
  11. "2017 - Final Rule: Placement of FDA-Approved Products of Oral Solutions Containing Dronabinol [(-)-delta-9-trans-tetrahydrocannabinol (delta-9-THC)] in Schedule II". www.deadiversion.usdoj.gov. Retrieved 2019-02-21.
  12. Honarmand, Azim; Safavi, Mohammadreza; Chegeni, Mansoureh; Hirmanpour, Anahita; Nazem, Masoud; Sarizdi, Seyyad Hamid (January 2016). "Prophylactic antiemetic effects of Midazolam, Ondansetron, and their combination after middle ear surgery". Journal of Research in Pharmacy Practice. 5 (1): 16–21. doi:10.4103/2279-042X.176556. ISSN 2319-9644. PMC 4776542. PMID 26985431.
  13. Herrstedt J, Aapro MS, Roila F, Kataja VV (2005). "ESMO Minimum Clinical Recommendations for prophylaxis of chemotherapy-induced nausea and vomiting (NV)" (PDF). Annals of Oncology. 16 (Suppl 1): i77–i79. doi:10.1093/annonc/mdi805. PMID 15888767. Archived (PDF) from the original on 2008-03-07.
  14. Flake ZA, Scalley RD, Bailey AG (March 2004). "Practical selection of antiemetics". American Family Physician. 69 (5): 1169–74. PMID 15023018. Archived from the original on 24 March 2016. Retrieved 10 March 2016.
  15. Grunberg, S. M. (1 February 2007). "Antiemetic activity of corticosteroids in patients receiving cancer chemotherapy: dosing, efficacy, and tolerability analysis". Annals of Oncology. 18 (2): 233–240. doi:10.1093/annonc/mdl347. ISSN 0923-7534. PMID 17108149.
  16. Abdel-Aziz H, Windeck T, Ploch M, Verspohl EJ (2006-01-13), "Mode of action of gingerols and shogaols on 5-HT3 receptors: binding studies, cation uptake by the receptor channel and contraction of isolated guinea-pig ileum", Eur J Pharmacol, 530 (1–2): 136–43, doi:10.1016/j.ejphar.2005.10.049, PMID 16364290
  17. Huang, Q.; Iwamoto, Y.; Aoki, S.; Tanaka, N.; Tajima, K.; Yamahara, J.; Takaishi, Y.; Yoshida, M.; Tomimatsu, T.; Tamai, Y. (1991). "Anti-5-hydroxytryptamine3 effect of galanolactone, diterpenoid isolated from ginger". Chemical & Pharmaceutical Bulletin. 39 (2): 397–399. doi:10.1248/cpb.39.397. PMID 2054863.
  18. Marx, WM; Teleni L; McCarthy AL; Vitetta L; McKavanagh D; Thomson D; Isenring E. (2013). "Ginger (Zingiber officinale) and chemotherapy-induced nausea and vomiting: a systematic literature review" (PDF). Nutr Rev. 71 (4): 245–54. doi:10.1111/nure.12016. PMID 23550785.
  19. Ernst, E.; Pittler, M.H. (1 March 2000). "Efficacy of ginger for nausea and vomiting: a systematic review of randomized clinical trials" (PDF). British Journal of Anaesthesia. 84 (3): 367–371. doi:10.1093/oxfordjournals.bja.a013442. PMID 10793599. Retrieved 6 September 2006.
  20. hoe 2#section1 Muscimol. Chemical Data Sheet, Database of Hazardous Materials, CAMEO chemicals
  21. Guttuso T Jr (2014). "Gabapentin's anti-nausea and anti-emetic effects: a review". Exp Brain Res. PMID 24668130.CS1 maint: uses authors parameter (link)
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