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ATC Group: A04AA Serotonin (5HT3) antagonists

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
4
A04AA
Serotonin (5HT3) antagonists

Contents

Code
Title
A04AA01
Ondansetron
A04AA02
Granisetron
A04AA03
Tropisetron
A04AA04
Dolasetron
A04AA05
Palonosetron
A04AA55
Palonosetron, combinations

Active Ingredients

Chemical substance
Description
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.

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.

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.

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 capsules
MPI, EU: SmPC
ALOXI Solution for injection
MPI, EU: SmPC
GRANISETRON Concentrate for solution for injection or infusion
MPI, EU: SmPC
UK
GRANISETRON Film-coated tablets
MPI, EU: SmPC
UK
ONDANSETRON Solution for injection or infusion
MPI, EU: SmPC
UK
ONDANSETRON Syrup
MPI, EU: SmPC
UK
SANCUSO Transdermal patch
MPI, EU: SmPC
ZOFRAN Suppositories
MPI, EU: SmPC
UK