ATC Group: A04A Antiemetics and antinauseants

Anatomical Therapeutic Chemical Classification System

Translations

Language
Translation
  English
Antiemetics and antinauseants

Hierarchical Position

Level
Code
Title
3
A04A
Antiemetics and antinauseants

Contents

Active Ingredients

Chemical substance
Description

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

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 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 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 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 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.

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 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.

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

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.