Antiemetic

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.
  • Amisulpride (Barhemsys), administered by intravenous injection.
  • Domperidone (Motilium)
  • Droperidol
  • Olanzapine (Zyprexa)
  • 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
• 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.
  • 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.
  • Cinnarizine (UK only)
  • Cyclizine
  • Diphenhydramine (Benadryl)
  • Dimenhydrinate (Gravol, Dramamine)
  • Doxylamine (Bonjesta, Unisom)
  • Mirtazapine (Remeron) is an antidepressant that also has antiemetic effects. It is a potent histamine H1 receptor antagonist, Ki=1.6 nM, and also exhibits notable 5-HT3 antagonism.
  • 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)
• 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.
  • Nabilone
  • Dronabinol (Marinol/Syndros) is a Schedule II drug in the U.S. when in an oral solution (Syndros), and Schedule III when in sesame oil and encapsulated in a soft gelatin capsule (Marinol).
  • Some synthetic cannabinoids such as Nabilone (Cesamet) or the JWH series.
  • Sativex is an oral spray containing THC and CBD. It is currently legal in Canada and a few countries in Europe and the US
• 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.
  • Lorazepam (Ativan) is said to be very good as an adjunct treatment for nausea along with first line medications such as Compazine.
• 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.
• Other
  • Trimethobenzamide is thought to work on the CTZ
  • Ginger contains 5-HT3 antagonists gingerols, shogaols, and galanolactone.{{Cite journal | doi-access = free
  • Emetrol is also claimed to be an effective antiemetic.
  • Propofol is given intravenously. It has been used in an acute care setting in hospital as a rescue therapy for emesis.
  • Muscimol is purported to have antiemetic activity.

References

References

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2. (2011-09-07). "Antiemetics for reducing vomiting related to acute gastroenteritis in children and adolescents". The Cochrane Database of Systematic Reviews.
3. (1 June 2003). "Nausea and Vomiting in Pregnancy - American Family Physician". American Family Physician.
4. (2001). "Drugs During Pregnancy and Lactation: Handbook of Prescription Drugs and Comparative Risk Assessment". Gulf Professional Publishing.
5. Karthaus, Meinolf. (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.
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.
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8. (1983-05-01). "Review of Cannabinoids and their Antiemetic Effectiveness". Drugs.
9. "Drug Scheduling".
10. "2017 - Final Rule: Placement of FDA-Approved Products of Oral Solutions Containing Dronabinol [(-)-delta-9-trans-tetrahydrocannabinol (delta-9-THC)] in Schedule II".
11. (1999-08-04). "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.".
12. (2011-05-11). "THC and CBD oromucosal spray (Sativex ® ) in the management of spasticity associated with multiple sclerosis". Expert Review of Neurotherapeutics.
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15. (January 2016). "Prophylactic antiemetic effects of Midazolam, Ondansetron, and their combination after middle ear surgery". Journal of Research in Pharmacy Practice.
16. (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.
17. (2017). "Effect of Lorazepam in Reducing Psychological Distress and Anticipatory Nausea and Vomiting in Patients Undergoing Chemotherapy". Journal of Pharmacology & Pharmacotherapeutics.
18. (1 February 2007). "Antiemetic activity of corticosteroids in patients receiving cancer chemotherapy: dosing, efficacy, and tolerability analysis". Annals of Oncology.
19. (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]].
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21. (March 2000). "Efficacy of ginger for nausea and vomiting: a systematic review of randomized clinical trials". British Journal of Anaesthesia.
22. O'Connor, Anahad. (August 21, 2007). "The Claim: Eating Ginger Can Cure Motion Sickness". [[The New York Times]].
23. (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.
24. Gov, Us. "MUSCIMOL - CAMEO Chemicals".