Mr. Ibrahem/Palonosetron
Clinical data
Pronunciation/pæləˈnsətrɒn/ pal-ə-NOH-sə-tron
Trade namesAloxi
AHFS/Drugs.comMonograph
MedlinePlusa610002
License data
Pregnancy
category
  • AU: B1
Routes of
administration
Intravenous, by mouth
Drug class5-HT3 antagonist[1]
Legal status
Legal status
Pharmacokinetic data
Bioavailability97% (oral)
Protein binding62%
MetabolismLiver, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved)
Elimination half-lifeApproximately 40–50 hours
ExcretionKidney, 80% (of which 49% unchanged); fecal (5 to 8%)
Identifiers
  • (3aS)-2-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
Chemical and physical data
FormulaC19H24N2O
Molar mass296.414 g·mol−1
3D model (JSmol)
Specific rotation[α]D −136°
[α]D –94.1° (HCl)
Melting point87 to 88 °C (189 to 190 °F)
  • O=C5N([C@H]2C1CCN(CC1)C2)C[C@@H]4c3c5cccc3CCC4
  • InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1 checkY
  • Key:CPZBLNMUGSZIPR-NVXWUHKLSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Palonosetron, sold under the brand name Aloxi, is a medication used to prevent chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting.[2][3] In delayed CINV there is tentative data suggesting it may be more effective than granisetron.[4] It can be given by mouth or by injection into a vein.[1]

Common side effects include QT prolongation, slow heart rate, headache, constipation, and weakness.[3] Other side effects may include anaphylaxis and serotonin syndrome.[3] Use in pregnancy appears to be safe, but such use has not been well studied.[5] It is a 5-HT3 antagonist.[1]

Palonosetron was approved for medical use in the United States in 2003 and Europe in 2005.[3][2] It is on the World Health Organization's List of Essential Medicines as an alternative to ondansetron.[6] It is available as a generic medication.[1] In the United Kingdom it costs the NHS about £55 per dose as of 2021.[1] This amount in the United States costs about 50 USD.[7]

References

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  1. ^ a b c d e f BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 456. ISBN 978-0857114105.
  2. ^ a b c "Aloxi". Archived from the original on 14 April 2021. Retrieved 25 October 2021.
  3. ^ a b c d e f "Palonosetron Monograph for Professionals". Drugs.com. Archived from the original on 21 January 2021. Retrieved 25 October 2021.
  4. ^ Billio A, Morello E, Clarke MJ (January 2010). Billio A (ed.). "Serotonin receptor antagonists for highly emetogenic chemotherapy in adults". The Cochrane Database of Systematic Reviews (1): CD006272. doi:10.1002/14651858.CD006272.pub2. PMID 20091591. (Retracted, see doi:10.1002/14651858.cd006272.pub3)
  5. ^ "Palonosetron (Aloxi) Use During Pregnancy". Drugs.com. Archived from the original on 25 November 2020. Retrieved 25 October 2021.
  6. ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  7. ^ "Palonosetron Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 19 January 2021. Retrieved 25 October 2021.