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 or diarrhea, dry mouth, and fatigue.
• *Dolasetron can be administered in tablet form or in an injection.
• * Granisetron can be administered in tablet, oral solution, injection D, or in a single transdermal patch to the upper arm.
• * Ondansetron is administered in an oral tablet form, orally dissolving tablet form, orally dissolving film, sublingual, or in an IV/IM injection.
• * Tropisetron can be administered in oral capsules or in injection form.
• * Palonosetron can be administered in an injection or in oral capsules.
• 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.
• *Amisulpride, administered by intravenous injection.
• *Domperidone
• * Olanzapine
• * Haloperidol
• * Alizapride
• * Prochlorperazine
• * Chlorpromazine
• *Metoclopramide
• NK1 receptor antagonist
• *Aprepitant is a commercially available NK1 Receptor antagonist
• *Casopitant is an investigational NK1 receptor antagonist
• *Rolapitant another recently approved drug from this class
• Antihistamines 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.
• * Cinnarizine
• * Cyclizine
• * Diphenhydramine
• * Dimenhydrinate
• * Doxylamine
• *Mirtazapine is an antidepressant that also has antiemetic effects it is also a potent histamine H1 receptor antagonist, K_i=1.6 nM.
• *Meclizine
• *Promethazine can be administered via a rectal suppository, intravenous injection, oral tablet or oral suspension for adults and children over 2 years of age.
• *Hydroxyzine
• 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.
• * Dronabinol is a Schedule II drug in the U.S.
• * Some synthetic cannabinoids such as Nabilone 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 & the US as of June 25, 2018.
• Benzodiazepines
• *Midazolam 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 is said to be very good as an adjunct treatment for nausea along with first line medications such as Compazine.
• Anticholinergics
• * Hyoscine
• * Atropine
• * Diphenhydramine
• Steroids
• * Dexamethasone 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. Preliminary clinical data suggests ginger may be effective for treatment of nausea and/or vomiting in a number of settings.
• * 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.
• * Peppermint is claimed to help nausea or stomach pain when added into a tea or peppermint candies.
• * Muscimol is purported to have antiemetic activity.
• * Ajwain is purported to be antiemetic. It is a popular spice in India, Ethiopia and Eritrea.