Palonosetron

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Drug Info:

Palonosetron

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Brand names: Aloxi™

Chemical formula:



Palonosetron Hydrochloride Solution for injection

What is this medicine?

PALONOSETRON is used to prevent nausea and vomiting caused by chemotherapy. It also helps prevent delayed nausea and vomiting that may occur a few days after your treatment.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•irregular heart rhythm
•an unusual or allergic reaction to palonosetron, dolasetron, granisetron, ondansetron, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for infusion into a vein. It is given by a health care professional in a hospital or clinic setting.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•cisapride
•droperidol
•ziprasidone

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Your condition will be monitored carefully while you are receiving this medicine.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•fast or irregular heartbeat
•fever and chills
•swelling of the hands and feet
•tightness in the chest

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation or diarrhea
•dizziness
•headache

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

This drug is given in a hospital or clinic and will not be stored at home.

Last updated: 7/30/2003 10:38:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.


An antiemetic used to prevent nausea and vomiting induced by chemotherapy drugs. It acts by inhibiting the action of the neurotransmitter serotonin at specific receptors in the central nervous system and gut. It is available in injectable form on prescription only.

Side effects:
include diarrhoea, constipation, headache, dizziness, indigestion, and abdominal pain.

Precautions:
palonosetron should be used with caution in people with a history of constipation or intestinal obstruction, those who are taking drugs known to cause arrhythmias, and in pregnant or breastfeeding women.

Proprietary preparation:
Aloxi.

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Palonosetron
Systematic (IUPAC) name
(3aS)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a,
4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
Clinical data
AHFS/Drugs.com monograph
MedlinePlus a610002
Licence data US FDA:link
Pregnancy cat. B1 (AU) B (US)
Legal status -only (US)
Routes Intravenous, oral
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%)
Identifiers
CAS number 135729-61-2 N
ATC code A04AA05
PubChem CID 148211
DrugBank DB00377
ChemSpider 4892289 YesY
UNII 5D06587D6R YesY
ChEMBL CHEMBL1189679 N
Chemical data
Formula C19H24N2O 
Mol. mass 296.407 g/mol
SMILES eMolecules & PubChem
 N (what is this?)  (verify)

Palonosetron (INN, trade name Aloxi)It is sold as EME OD 0.5MG in India (INTAS PHARMACEUTICALS LTD) 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]


See also

References

  1. ^ 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. PMC 1618755. PMID 17106506. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1618755. 
  2. ^ a b Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. http://www.medscape.com/viewarticle/580032. Retrieved 2008-09-04.  Freely available with registration.



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