ATC Group: A04AA Serotonin (5HT3) antagonists

The World Health Organization's ATC classification organizes medical drugs based on therapeutic properties, chemical composition, and anatomy. It helps make essential medicines readily available globally and is widely used in the pharmaceutical industry.

Position of A04AA in the ATC hierarchy

Level
Code
Title
1
Alimentary tract and metabolism
2
Antiemetics and antinauseants
3
Antiemetics and antinauseants
4
A04AA
Serotonin (5HT3) antagonists

Group A04AA contents

Code
Title
Ondansetron
Granisetron
Tropisetron
Dolasetron
Palonosetron

Active ingredients in A04AA

Active Ingredient
Description

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

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

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.

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