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ATC Group: A04A Antiemetics and antinauseants

Anatomical Therapeutic Chemical Classification System

Hierarchical Position

Level
Code
Title
1
A
Alimentary tract and metabolism
2
A04
Antiemetics and antinauseants
3
A04A
Antiemetics and antinauseants

Contents

Code
Title
A04AA
Serotonin (5HT3) antagonists
A04AD
Other antiemetics

Active Ingredients

Chemical substance
Description
Aprepitant

Aprepitant is a selective high-affinity antagonist at human substance P neurokinin 1 (NK1) receptors.

Chlorobutanol
Dimenhydrinate

Dimenhydrinate is a theoclate salt of the ethanolamine derivative diphenhydramine. It exhibits reversible competitive antagonism with histamine for the capture of H1 receptors. It has anticholinergic (antimuscarinic) properties that explain the anti-emetic action of the drug in cases of labyrinthial irritation (nausea, vertigo), and the central suppression it causes.

Dolasetron

Dolasetron and its active metabolite, hydrodolasetron (MDL 74,156), are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema.

Dronabinol

Dronabinol is an active ingredient of cannabis, which has complex effects on the CNS, including central sympathomimetic activity. Dronabinol exerts its action by activating CB1 and CB2 recepors which makes it a CNS active medicine.

Fosaprepitant

Fosaprepitant is the prodrug of aprepitant and when administered intravenously is converted rapidly to aprepitant. The contribution of fosaprepitant to the overall antiemetic effect has not fully been characterised, but a transient contribution during the initial phase cannot be ruled out.

Granisetron

Granisetron is a potent anti-emetic and highly selective antagonist of 5-hydroxytryptamine (5HT3 receptors). Pharmacological studies have demonstrated that granisetron is effective against nausea and vomiting as a result of cytostatic therapy.

Metopimazine
Nabilone

Nabilone is a synthetic cannabinoid and dibenzopyrane derivative, an analog of dronabinol (also known as tetrahydrocannabinol or THC), the psychoactive ingredient in cannabis with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It has been suggested that nabilone is a highly selective and strong agonist for the cannabinoid receptors CB1 and CB2, both of which are coupled to Gi/o proteins. The CB1 receptors are expressed predominantly in central and peripheral neurons and receptor stimulation has been implicated in the reduction of chemotherapy-induced nausea.

Netupitant

Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK1) receptors. Delayed emesis has been associated with the activation of tachykinin family neurokinin 1 (NK1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses.

Ondansetron

Ondansetron is a potent, highly selective 5HT3 receptor-antagonist. Its precise mode of action in the control of nausea and vomiting is not known.

Palonosetron

Palonosetron is a selective high-affinity receptor antagonist of the 5HT3 receptor.

Rolapitant

Rolapitant is a selective antagonist of human substance P/neurokinin 1 (NK1) receptors.

Scopolamine

Scopolamine is a naturally occurring belladonna alkaloid and has anticholinergic properties. It acts as a competitive antagonist to acetylchloline and other parasympathomimetic agents. Its mechanism of action in the central nervous system in preventing motion sickness has yet to be elucidated. Scopolamine produces classical symptoms of parasympathetic blockade.

Tropisetron

Tropisetron is a highly potent and selective competitive antagonist of the 5-HT3 receptor. Tropisetron selectively blocks the excitation of the presynaptic 5-HT3 receptors of the peripheral neurons in this reflex, and may exert additional direct actions within the CNS on 5-HT3 receptors mediating the actions of vagal input to the area postrema.

Monographs

Monograph
Type
Country
ALOXI Soft capsule
MPI, EU: SmPC
ALOXI Solution for injection
MPI, EU: SmPC
CESAMET Capsule
MPI, US: SPL/Old
US
EMEND Hard capsule
MPI, EU: SmPC
GRANISETRON Concentrate for solution for injection or infusion
MPI, EU: SmPC
UK
GRANISETRON Film-coated tablet
MPI, EU: SmPC
UK
IVEMEND Powder for solution for infusion
MPI, EU: SmPC
ONDANSETRON Solution for injection or infusion
MPI, EU: SmPC
UK
ONDANSETRON Syrup
MPI, EU: SmPC
UK
SANCUSO Transdermal patch
MPI, EU: SmPC
SCOPODERM Transdermal patch
MPI, EU: SmPC
UK
ZOFRAN Suppositories
MPI, EU: SmPC
UK