This MedLibrary.org supplementary page on Palonosetron is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:
Related Sponsors
 |
|
 |
|
|
Palonosetron
|
|
| Systematic (IUPAC) name | |
| (3aR)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a, 4,5,6-hexahydro-1H-benzdeisoquinolin-1-one |
|
| Identifiers | |
| CAS number | |
| ATC code | A04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C19H24N2O |
| Mol. mass | 296.407 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 97% (oral) |
| Protein binding | 62% |
| Metabolism | Hepatic, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved) |
| Half life | Approximately 40 hours |
| Excretion | Renal, 80% (of which 49% unchanged); fecal (5 to 8%) |
| Therapeutic considerations | |
| Licence data |
|
| Pregnancy cat. | |
| Legal status | |
| Routes | Intravenous, oral |
Palonosetron (INN, trade name Aloxi) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV—nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy—and is the only drug of its class approved for this use by the U.S. Food and Drug Administration.[1] As of 2008, it is the most recent 5-HT3 antagonist to enter clinical use.
Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy,[1] or as a single oral capsule one hour before chemotherapy.[2] The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.[2]
References
- ^ a b De Leon A (2006). "Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting". Proceedings (Baylor University. Medical Center) 19 (4): 413–6. PMID 17106506. Full text at PMC: 1618755.
- ^ a b Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. Retrieved on 2008-09-04. Freely available with registration.
|
|||||||||||
|
|||||||||||||||||||||||||||||
 |
This pharmacology-related article is a stub. You can help Wikipedia by expanding it. |
Wikipedia content modification information:
- This page was last modified on 5 September 2008, at 01:24.
Wikipedia Authorship and Review
Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.
Wikipedia Usage Guidelines
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Palonosetron".
The URL for this specific entry is:
All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.