ATC Group: A04AD Other antiemetics
Anatomical Therapeutic Chemical Classification System
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.
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.
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.
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.