Chemistry:Antiemetic

From HandWiki

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.[1][2]

Some antiemetics previously thought to cause birth defects appear safe for use by pregnant women in the treatment of morning sickness and the more serious hyperemesis gravidarum.[3][4]

Types

  • 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, dry mouth, and fatigue.
    • 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 (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 antagonists block dopamine receptors on the brainstem and gastrointestinal tract. They are used to treat nausea and vomiting associated with cancer, radiation sickness, opioids, cytotoxic drugs and general anaesthetics. Side effects include restlessness and tardive dyskinesia.
  • NK1 receptor antagonist which block NK1, also known as substance P. They are typically only used in the context of chemotherapy induced nausea and vomiting.[5]
    • 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
  • 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 listed here also block muscarinic acetylcholine receptors. They are known to cause significant sedation.
  • 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.
    • Cannabis, also known as medical marijuana in the United States, is a Schedule I drug.[9][10]
    • Nabilone
    • Dronabinol (Marinol/Syndros) is a Schedule II drug in the U.S. when in an oral solution (Syndros),[11] and Schedule III when in sesame oil and encapsulated in a soft gelatin capsule (Marinol).[12]
    • Some synthetic cannabinoids such as Nabilone (Cesamet) or the JWH series.
    • Sativex is an oral spray containing THC and CBD.[13] It is currently legal in Canada and a few countries in Europe and the US as of June 25, 2018 [14][15]
  • Benzodiazepines (GABA receptor positive allosteric modulators)
    • Midazolam (Versed) is given at the onset of anesthesia and has been shown in recent trials to be as effective as ondansetron, but most effective when used in combination with ondansetron.[16]
    • Lorazepam (Ativan) is said to be very good as an adjunct treatment for nausea along with first line medications such as Compazine.[17][18]
  • Anticholinergics
    • Hyoscine (also known as scopolamine)
    • Atropine
  • 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.[19]
  • Other

See also

References

  1. ↑ Manteuffel, Jacob (2009). "Use of antiemetics in children with acute gastroenteritis: Are they safe and effective?". Journal of Emergencies, Trauma, and Shock 2 (1): 3–5. doi:10.4103/0974-2700.44674. ISSN 0974-2700. PMID 19561947. 
  2. ↑ Fedorowicz, Zbys; Jagannath, Vanitha A; Carter, Ben (2011-09-07). "Antiemetics for reducing vomiting related to acute gastroenteritis in children and adolescents". The Cochrane Database of Systematic Reviews 2011 (9). doi:10.1002/14651858.CD005506.pub5. ISSN 1469-493X. PMID 21901699. 
  3. ↑ Quinlan, Jeffrey D.; Hill, D. Ashley (1 June 2003). "Nausea and Vomiting in Pregnancy - American Family Physician". American Family Physician 68 (1): 121–128. http://www.aafp.org/afp/2003/0701/p121.html. Retrieved 2015-10-09. 
  4. ↑ Schaefer, Christof; Scialli, Anthony; Rost van Tonningen, Margreet (2001). "Antiemetics and hyperemesis gravidarum". Drugs During Pregnancy and Lactation: Handbook of Prescription Drugs and Comparative Risk Assessment. Gulf Professional Publishing. ISBN 978-0-444-50763-1. https://books.google.com/books?id=CE569saGK70C&pg=PA40. 
  5. ↑ Karthaus, Meinolf; Schiel, Xaver; Ruhlmann, Christina H.; Celio, Luigi (2019-07-03). "Neurokinin-1 receptor antagonists: review of their role for the prevention of chemotherapy-induced nausea and vomiting in adults". Expert Review of Clinical Pharmacology 12 (7): 661–680. doi:10.1080/17512433.2019.1621162. ISSN 1751-2433. PMID 31194593. https://www.tandfonline.com/doi/full/10.1080/17512433.2019.1621162. 
  6. ↑ 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. 
  7. ↑ 7.0 7.1 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. 
  8. ↑ National Institute of Mental Health. PDSD Ki Database (Internet) [cited 2013 Sep 27]. Chapel Hill (NC): University of North Carolina. 1998-2013. Available from: "PDSP Database - UNC". http://pdsp.med.unc.edu/pdsp.php. 
  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". https://www.dea.gov/drug-scheduling. 
  11. ↑ "2017 - Final Rule: Placement of FDA-Approved Products of Oral Solutions Containing Dronabinol [(-)-delta-9-trans-tetrahydrocannabinol (delta-9-THC) in Schedule II"]. https://www.deadiversion.usdoj.gov/fed_regs/rules/2017/fr1122_6.htm. 
  12. ↑ "Schedules of Controlled Substances: Rescheduling of the Food and Drug Administration Approved Product Containing Synthetic Dronabinol [(-)-greek-DSUP9/SUP -(trans)-Tetrahydrocannabinol in Sesame Oil and Encapsulated in Soft Gelatin Capsules From Schedule II to Schedule III."] (in en). 1999-08-04. https://www.federalregister.gov/documents/1999/08/04/C9-16833/schedules-of-controlled-substances-rescheduling-of-the-food-and-drug-administration-approved-product. 
  13. ↑ Sastre-Garriga, Jaume; Vila, Carlos; Clissold, Stephen; Montalban, Xavier (2011-05-11). "THC and CBD oromucosal spray (Sativex ® ) in the management of spasticity associated with multiple sclerosis" (in en). Expert Review of Neurotherapeutics 11 (5): 627–637. doi:10.1586/ern.11.47. ISSN 1473-7175. PMID 21456949. http://www.tandfonline.com/doi/full/10.1586/ern.11.47. 
  14. ↑ Wadsworth, E; Hammond, D (2019-03-04). "International differences in patterns of cannabis use among youth: Prevalence, perceptions of harm, and driving under the influence in Canada, England & United States". Addictive Behaviors 90: 171–175. doi:10.1016/j.addbeh.2018.10.050. ISSN 0306-4603. PMID 30412908. 
  15. ↑ Rahman, Lu (2021-02-03). "Medical cannabis and regulatory framework in Europe" (in en-US). https://www.ddw-online.com/medical-cannabis-and-regulatory-framework-in-europe-what-you-need-to-know-9601-202102/. 
  16. ↑ 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. PMID 26985431. 
  17. ↑ Bishop, J. F.; Olver, I. N.; Wolf, M. M.; Matthews, J. P.; Long, M.; Bingham, J.; Hillcoat, B. L.; Cooper, I. A. (1984). "Lorazepam: A randomized, double-blind, crossover study of a new antiemetic in patients receiving cytotoxic chemotherapy and prochlorperazine". Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology 2 (6): 691–695. doi:10.1200/JCO.1984.2.6.691. PMID 6374058. 
  18. ↑ James, A.; Nair, M. M.; Abraham, D. S.; Kovoor, J. S.; Jose, W. M.; Reghu, R. (2017). "Effect of Lorazepam in Reducing Psychological Distress and Anticipatory Nausea and Vomiting in Patients Undergoing Chemotherapy". Journal of Pharmacology & Pharmacotherapeutics 8 (3): 112–115. doi:10.4103/jpp.JPP_54_17. PMID 29081618. 
  19. ↑ Grunberg, S. M. (1 February 2007). "Antiemetic activity of corticosteroids in patients receiving cancer chemotherapy: dosing, efficacy, and tolerability analysis" (in en). Annals of Oncology 18 (2): 233–240. doi:10.1093/annonc/mdl347. ISSN 0923-7534. PMID 17108149. 
  20. ↑ "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, 2006-01-13, doi:10.1016/j.ejphar.2005.10.049, PMID 16364290 
  21. ↑ Huang, Q.; Iwamoto, Y.; Aoki, S.; Tanaka, N.; Tajima, K.; Yamahara, J.; Takaishi, Y.; Yoshida, M. et al. (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. 
  22. ↑ 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". Nutr Rev 71 (4): 245–54. doi:10.1111/nure.12016. PMID 23550785. https://eprints.qut.edu.au/59091/2/Ginger_Article_Nutrition_Reviews_Accepted_Version_%28Recovered%29.pdf. Retrieved 2019-12-16. 
  23. ↑ Ernst, E.; Pittler, M. H. (March 2000). "Efficacy of ginger for nausea and vomiting: a systematic review of randomized clinical trials". British Journal of Anaesthesia 84 (3): 367–371. doi:10.1093/oxfordjournals.bja.a013442. ISSN 0007-0912. PMID 10793599. 
  24. ↑ O'Connor, Anahad (August 21, 2007). "The Claim: Eating Ginger Can Cure Motion Sickness". The New York Times. https://www.nytimes.com/2007/08/21/health/21real.html. 
  25. ↑ Kampo, Sylvanus; Afful, Alfred Parker; Mohammed, Shiraj; Ntim, Michael; Buunaaim, Alexis D. B.; Anabah, Thomas Winsum (2019-09-14). "Sub-hypnotic dose of propofol as antiemetic prophylaxis attenuates intrathecal morphine-induced postoperative nausea and vomiting, and pruritus in parturient undergoing cesarean section — a randomized control trial". BMC Anesthesiology 19 (1): 177. doi:10.1186/s12871-019-0847-y. ISSN 1471-2253. PMID 31521119. 
  26. ↑ Gov, Us. "MUSCIMOL - CAMEO Chemicals". https://cameochemicals.noaa.gov/chemical/5082. 



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