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Palonosetron, sold under the brand name Aloxi, is a medication used for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). [2] [4] [5] It is a 5-HT 3 antagonist. [2] [4] [5] Palonosetron is administered intravenously, [6] or as a single oral capsule. [7] It has a longer duration of action than other 5-HT 3 antagonists.
The 5-HT 3 receptor antagonists suppress vomiting and nausea by inhibiting serotonin binding to the 5-HT 3 receptors. The highest concentration of 5-HT 3 receptors in the central nervous system are found in the STN and chemoreceptor trigger zone (CTZ), and 5-HT 3 antagonists may also suppress vomiting and nausea by acting at these sites. [29]
Dopamine receptor flow chart. Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. [1] The D 1-like class of dopamine receptors is coupled to Gα s/olf and stimulates adenylate cyclase production, whereas the D 2-like class is coupled to Gα i/o and thus inhibits adenylate cyclase production.
They are efficacious in treating chemotherapy-induced emesis and postoperative nausea and vomiting. [1] They include, but are not limited to: Dolasetron; Granisetron; Ondansetron; Palonosetron; Tropisetron; Other 5-HT 3 antagonists have been considered for use in the treatment of irritable bowel syndrome: Alosetron; Cilansetron
An antiemetic is a drug that is effective against vomiting and nausea.Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer.
It was developed up to phase II clinical trials for the treatment of postoperative nausea and vomiting, migraine and motion sickness. It showed good results in emesis, but development was discontinued. [12] LY-303870, or lanepitant (figure 5), is an N-acetylated reduced amide of L-tryptophan that was discovered by Eli Lilly. It underwent phase ...
A prokinetic agent (also prokineticin, gastroprokinetic agent, gastrokinetic agent or propulsive) is a type of drug which enhances gastrointestinal motility by increasing the frequency or strength of contractions, but without disrupting their rhythm. [1]
The vomiting center of the brain refers to the groups of loosely organized neurons in the medulla that include the CTZ within the area postrema and the nucleus tractus solitarii. [2] One of the ways the chemoreceptor trigger zone implements its effects on the vomiting center is by activation of the opioid mu receptors and delta receptors. [6]