10/16/2020 Antiemetics - AMBOSS

Antiemetics
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Summary

Antiemetics are a heterogeneous group of drugs used to treat various causes of nausea and vomiting. Different
antiemetics act on different receptors, and they may have a peripheral effect, a central effect, or both. Whereas
serotonin antagonists, for example, bind 5-HT3 receptors and effectively combat cytotoxic drug nausea, certain
anticholinergic drugs target M1 receptors and specifically treat motion sickness (kinetosis). Hospitals and clinics
commonly use the dopamine D2 antagonist metoclopramide. However, because of its strong central effect and
possible extrapyramidal side effects, metoclopramide must be used with caution.

Overview

Antiemetic
class Drug Mechanism of action Clinical use Side effects

Dopamine Prochlorperazine D2 antagonist Antipsychotic Gastrointestinal

receptor Central agent Diarrhea
antagonists antiemetic effect Hyperemesis Pain
at the area gravidarum Hyperprolactinema
postrema Neurological
Depression
Fatigue
Drowsiness
Restlessness
Lowering of
seizure
threshold
Overdose leads
to reversible
extrapyramidal
syndrome (e.g.,
dystonia,
parkinsonism,
tardive
dyskinesia, and
akathisia) and
neuroleptic
malignant
syndrome

Do not combine
metoclopramide
with
antipsychotics
because this
increases the
risk of
dyskinesia!
Antidote:
biperiden
(anticholinergic
agent)
Avoid combination
with digoxin and
antidiabetic drugs.

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Antiemetic
class Drug Mechanism of action Clinical use Side effects
Contraindicated in
Metoclopramide D2 antagonist, Prokinetic
patients with
serotonin effect used to
suspected small
receptor treat diabetic
bowel obstruction
antagonist and
postsurgery
Central gastroparesis
antiemetic effect (delayed
at the area gastric
postrema emptying)
Peripheral Hyperemesis
antiemetic effect gravidarum
in the Persistent
gastrointestinal GERD
tract (prokinetic
effect); causes
increase in

:
Gastric
contractions
Duodenal
and jejunal
motility
Resting
tone of the
lower
esophageal
sphincter
Together with
decreased
pylorus sphincter
activity allows
food to pass
more quickly
through the
stomach and the
small intestine
No influence on
colon motility

Domperidone D2 antagonist Nausea and Gastrointestinal

Central vomiting Diarrhea
antiemetic effect Gastrointestinal Pain
at the area motility Hyperprolactinema
postrema disorders Domperidone, in
Prokinetic effect contrast to
metoclopramide and
prochlorperazine,
crosses the blood-
brain-barrier only
minimally, hence
neurological side
effects are limited
May cause cardiac
arrhythmias

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10/16/2020 Antiemetics - AMBOSS

Antiemetic
class Drug Mechanism of action Clinical use Side effects

Serotonin Ondansetron 5-HT3 antagonist Ondansetron is Headaches

receptor Granisetron Strong central commonly Constipation or
antagonists Dolasetron antiemetic effect used for diarrhea
Palonosetron at the area generalized QT interval
(5-HT3 postrema nausea. prolongation
antagonists) Peripheral Chemotherapy- (torsades de pointes)
antiemetic effect induced Increase in liver
via inhibition of vomiting, enzymes
the vagus nerve radiation- Serotonin syndrome
induced
vomiting, and
postoperative
nausea and
vomiting
(PONV)

Anticholinergic Scopolamine Nonspecific Motion Anticholinergic side

agents muscarinic sickness, effects: dry mouth,
antagonist vestibular- mydriasis,
Central induced tachycardia, urinary
antiemetic effect nausea, and retention
at the area vomiting Antidote:
postrema and on physostigmine
the vestibular (cholinesterase
system inhibitor)
Peripheral
antiemetic effect
via inhibition of
the vagus nerve

Antihistamines Meclizine H1 antagonist Strong sedative Antihistamine effects:

Dimenhydrinate Central Nausea and drowsiness and
Diphenhydramine antiemetic effect vomiting due to confusion
Doxylamine at the area vestibular Anticholinergic side
Promethazine postrema and causes [1] effects: dry mouth,
vestibular system Hyperemesis dilated pupils, blurred
gravidarum vision, reduced bowel
(also see sounds, and urinary
antiemetics retention (antidote:
during physostigmine)
pregnancy)

Neurokinin Aprepitant NK1 antagonist CINV Hypersensitivity

receptor Fosaprepitant Inhibition of NK1 prophylaxis reactions
antagonists receptors in the Infusion site
solitary nucleus reactions
→ central Increased levels of
antiemetic effect other drugs
via
due to weak CYP3A4
Additional enzyme inhibition
inhibition of
substance P-
induced vomiting
due to
antagonism

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10/16/2020 Antiemetics - AMBOSS

References:[9][9][9][10][10][10][10][11][12][13][14][15][16][17]

Indications

Nonspecific nausea and vomiting

Chemotherapy-induced nausea and vomiting
Vertigo (e.g., vestibular neuritis, Ménière's disease)
Motion sickness
Gastrointestinal motility disorder (e.g., due to diabetic gastroparesis)
Postoperative nausea and vomiting

References:[10][18][13]

Contraindications

Dopamine receptor antagonists

Intestinal obstruction (ileus)
Prolactin-dependent tumors

Parkinson disease: unlike domperidone, metoclopramide can cross the blood-brain barrier and
exacerbate the pre-existing dopamine deficiency that causes parkinsonism.
Serotonin receptor antagonists: severe liver disease, prolonged QT interval
Anticholinergic agents and antihistamines
Tachyarrhythmias, heart failure
Urinary retention, BPH
Glaucoma
Pyloric stenosis

References:[18][13][15]

We list the most important contraindications. The selection is not exhaustive.

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