•
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. •
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. 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. •
Muscimol is purported to have antiemetic activity. ==See also==