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Namespace Prefixes

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Statements

Subject Item
n2:DB00377
rdf:type
n5:Drug
n5:description
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. As of 2008, it is the most recent 5-HT3 antagonist to enter clinical use. [wikipedia]
n5:dosage
n10:271B6419-363D-11E5-9242-09173F13E4C5 n10:271B641A-363D-11E5-9242-09173F13E4C5 n10:271B6416-363D-11E5-9242-09173F13E4C5 n10:271B6417-363D-11E5-9242-09173F13E4C5 n10:271B6418-363D-11E5-9242-09173F13E4C5
n5:generalReferences
# De Leon A: Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent). 2006 Oct;19(4):413-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17106506 # Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15102873 # Rubenstein EB: Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16163194 # Yang LP, Scott LJ: Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19852528 # Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15139789 # Eisenberg P, MacKintosh FR, Ritch P, Cornett PA, Macciocchi A: Efficacy, safety and pharmacokinetics of palonosetron in patients receiving highly emetogenic cisplatin-based chemotherapy: a dose-ranging clinical study. Ann Oncol. 2004 Feb;15(2):330-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14760130 # Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15378559
n5:group
approved investigational
n5:halfLife
Approximately 40 hours
n5:indication
For the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy, as well as prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy. Also used for the prevention of postoperative nausea and vomiting for up to 24 hours post operation.
n5:manufacturer
n22:271B6414-363D-11E5-9242-09173F13E4C5
owl:sameAs
n4:DB00377 n23:DB00377
dcterms:title
Palonosetron
adms:identifier
n12:PA10352 n13:148211 n14:DB00377 n15:58063-797-25 n16:Palonosetron n17:46508530 n25:130656
n5:mechanismOfAction
Palonosetron is a selective serotonin 5-HT<sub>3</sub> receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT<sub>3</sub> receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT<sub>3</sub> receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT<sub>3</sub> receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron's potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy.
n5:packager
n22:271B6410-363D-11E5-9242-09173F13E4C5 n22:271B6411-363D-11E5-9242-09173F13E4C5 n22:271B640E-363D-11E5-9242-09173F13E4C5 n22:271B640F-363D-11E5-9242-09173F13E4C5 n22:271B640D-363D-11E5-9242-09173F13E4C5 n22:271B6412-363D-11E5-9242-09173F13E4C5 n22:271B6413-363D-11E5-9242-09173F13E4C5
n5:patent
n18:5202333
n5:routeOfElimination
After a single intravenous dose of 10 mcg/kg [14C]-palonosetron, approximately 80% of the dose was recovered within 144 hours in the urine
n5:synonym
Palonosetrón Palonosetronum Palonosetron Palonosétron (3aS)-2,3,3a,4,5,6-hexahydro-2-[(3S)-3-quinuclidinyl]-1H-benz[de]isoquinolin-1-one SID50111798 (3aS)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a, 4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
n5:toxicity
A single intravenous dose of palonosetron at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse.
n5:volumeOfDistribution
* 8.3 ± 2.5 L/kg
n5:proteinBinding
62%
n5:salt
n5:synthesisReference
Pierluigi Rossetto, Peter MacDonald, Ettore Bigatti, Gaia Banfi, Dario Tentorio, "Processes for preparing palonosetron salts." U.S. Patent US20080200681, issued August 21, 2008.
foaf:page
n8:aloxi.htm n24:palonosetron.html
n5:IUPAC-Name
n6:271B641F-363D-11E5-9242-09173F13E4C5
n5:InChI
n6:271B6425-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n6:271B6424-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n6:271B6421-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n6:271B6422-363D-11E5-9242-09173F13E4C5
n5:SMILES
n6:271B6423-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n6:271B641D-363D-11E5-9242-09173F13E4C5
n5:logP
n6:271B641B-363D-11E5-9242-09173F13E4C5 n6:271B6434-363D-11E5-9242-09173F13E4C5 n6:271B641E-363D-11E5-9242-09173F13E4C5
n5:logS
n6:271B641C-363D-11E5-9242-09173F13E4C5
n19:hasATCCode
n20:A04AA05
n5:H-Bond-Acceptor-Count
n6:271B642B-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n6:271B642C-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n6:271B6426-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n6:271B6427-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n6:271B6429-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n6:271B6428-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n6:271B642A-363D-11E5-9242-09173F13E4C5
n5:absorption
Low oral bioavailability.
n5:affectedOrganism
Humans and other mammals
n5:casRegistryNumber
119904-90-4
n5:clearance
* 160 +/- 35 mL/h/kg
n5:containedIn
n9:271B6415-363D-11E5-9242-09173F13E4C5
n5:Bioavailability
n6:271B6430-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n6:271B6432-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n6:271B6433-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n6:271B642F-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n6:271B642E-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n6:271B6431-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n6:271B6420-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-basic-
n6:271B642D-363D-11E5-9242-09173F13E4C5