Aprepitant
From Proteopedia
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Aprepitant, sold under the brand name Emend among others, is a medication used to prevent chemotherapy-induced nausea and vomiting (CINV) and to prevent postoperative nausea and vomiting (PONV).<ref name="a4">[https://www.drugs.com/monograph/aprepitant-fosaprepitant.html "Aprepitant/Fosaprepitant Dimeglumine Monograph for Professionals".] Drugs.com. Archived from the original on 13 August 2020. Retrieved 13 October 2019.</ref> See also [https://en.wikipedia.org/wiki/Aprepitant Aprepitant]. | Aprepitant, sold under the brand name Emend among others, is a medication used to prevent chemotherapy-induced nausea and vomiting (CINV) and to prevent postoperative nausea and vomiting (PONV).<ref name="a4">[https://www.drugs.com/monograph/aprepitant-fosaprepitant.html "Aprepitant/Fosaprepitant Dimeglumine Monograph for Professionals".] Drugs.com. Archived from the original on 13 August 2020. Retrieved 13 October 2019.</ref> See also [https://en.wikipedia.org/wiki/Aprepitant Aprepitant]. | ||
| - | Aprepitant is classified as an NK1 antagonist because it blocks signals given off by | + | Aprepitant is classified as an NK1 antagonist because it blocks signals given off by Neurokinin 1 receptors. This, therefore, decreases the likelihood of vomiting in patients. |
NK1 is a [[G protein-coupled receptor]] located in the central and peripheral nervous system. This receptor has a dominant ligand known as Substance P (SP). SP is a neuropeptide, composed of 11 amino acids, which sends impulses and messages from the brain. It is found in high concentrations in the vomiting center of the brain, and, when activated, it results in a vomiting reflex. In addition to this it also plays a key part in the transmission of pain impulses from the peripheral receptors to the central nervous system. | NK1 is a [[G protein-coupled receptor]] located in the central and peripheral nervous system. This receptor has a dominant ligand known as Substance P (SP). SP is a neuropeptide, composed of 11 amino acids, which sends impulses and messages from the brain. It is found in high concentrations in the vomiting center of the brain, and, when activated, it results in a vomiting reflex. In addition to this it also plays a key part in the transmission of pain impulses from the peripheral receptors to the central nervous system. | ||
Revision as of 10:33, 26 December 2023
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References
- ↑ "Aprepitant/Fosaprepitant Dimeglumine Monograph for Professionals". Drugs.com. Archived from the original on 13 August 2020. Retrieved 13 October 2019.
- ↑ Bergström M, Hargreaves RJ, Burns HD, Goldberg MR, Sciberras D, Reines SA, Petty KJ, Ogren M, Antoni G, Långström B, Eskola O, Scheinin M, Solin O, Majumdar AK, Constanzer ML, Battisti WP, Bradstreet TE, Gargano C, Hietala J. Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant. Biol Psychiatry. 2004 May 15;55(10):1007-12. PMID:15121485 doi:10.1016/j.biopsych.2004.02.007
- ↑ Gralla RJ, de Wit R, Herrstedt J, Carides AD, Ianus J, Guoguang-Ma J, Evans JK, Horgan KJ. Antiemetic efficacy of the neurokinin-1 antagonist, aprepitant, plus a 5HT3 antagonist and a corticosteroid in patients receiving anthracyclines or cyclophosphamide in addition to high-dose cisplatin: analysis of combined data from two Phase III randomized clinical trials. Cancer. 2005 Aug 15;104(4):864-8. PMID:15973669 doi:10.1002/cncr.21222
