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Drugs reference index «Palonosetron Hydrochloride»

Palonosetron Hydrochloride

Pronunciation: (PAL-oh-NOE-se-tron HYE-droe-KLOR-ide)Class: 5-HT 3 receptor antagonist

Trade Names:Aloxi- Capsules 0.5 mg- Injection, solution 0.05 mg/mL


Selective antagonist for the 5-HT 3 receptor with a strong binding affinity for this receptor.



Following oral and IV administration, the C max and AUC are generally dose-proportional. After a single IV dose at 3 mcg/kg, mean C max was approximately 5.6 ng/mL and AUC was 35.8 ng•h/mL.

Following oral administration, bioavailability reaches 97%.


Vd is approximately 8.3 L/kg, and protein binding is about 62%.


Approximately 50% is metabolized to 2 metabolites that have less than 1% of the activity of palonosetron. The major isozyme responsible for metabolism appears to be CYP2D6 and, to a lesser degree, CYP1A2 and CYP3A are involved.


Following IV administration, approximately 80% of the dose is recovered in the urine. The terminal half-life is approximately 40 h.

Following oral administration, 85% to 93% is recovered in the urine and 5% to 8% in the feces.

Special Populations

Renal Function Impairment

No dosage adjustments are needed with any degree of renal function impairment. However, pharmacokinetics have not been studied in patients with end-stage renal disease.

Hepatic Function Impairment

No dosage adjustments are needed with any degree of hepatic function impairment.


No dosage adjustments or special monitoring are needed in elderly patients.


Has not been adequately characterized.


Dosage adjustments are not necessary based on gender.

Indications and Usage


Prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy; prevention of acute nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy; prevention of postoperative nausea and vomiting for up to 24 h following surgery.


Prevention of acute nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy.


Standard considerations.

Dosage and Administration

Chemotherapy-Induced Nausea and VomitingAdults

IV 0.25 mg administered over 30 sec approximately 30 min before the start of chemotherapy.


PO 0.5 mg administered approximately 1 h prior to the start of chemotherapy.

Postoperative Nausea and VomitingAdults

IV 0.075 mg administered over 10 sec immediately before the induction of anesthesia.

General Advice

  • For IV administration only. Not for intradermal, subcutaneous, or IM administration.
  • Do not administer if particulate matter, cloudiness, or discoloration is noted.
  • Administer prescribed dose via 30-sec IV infusion.
  • Discard any unused solution. Do not save unused solution for later administration.
  • Do not mix with other medications.
  • May be taken orally with or without food.


Store at 59° to 86°F. Protect from light and protect injectable from freezing.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions


ECG QT prolongation (5%); bradycardia (4%); hypotension, sinus bradycardia, tachycardia (1%).


Headache (9%); anxiety, dizziness, weakness (1%).


Constipation (5%); diarrhea (1%).


Urinary retention (1%).


Increased ALT, increased AST (1%).


Hypersensitivity (postmarketing).


Burning, discomfort, induration, pain (postmarketing).


Hyperkalemia (1%).



Category B .




Safety and efficacy not established.


May occur in patients who have exhibited hypersensitivity to other selective 5-HT 3 receptor antagonists.

CV effects

Although palonosetron has been safely administered to patients with preexisting cardiac impairment, administer with caution in patients who have or may develop prolongation of cardiac conduction intervals, particularly QTc.



No data available.

Patient Information

  • Advise patient, family, or caregiver that IV formulation will be prepared and administered by health care provider in a medical facility.
  • Advise patient, family, or caregiver that medication will greatly reduce likelihood of nausea or vomiting, but that these are still possible.
  • Instruct patient to inform health care provider if medication does not prevent nausea or vomiting.
  • Advise patient to report any of the following to health care provider: intolerable headache, persistent or intolerable constipation or diarrhea.

Copyright © 2009 Wolters Kluwer Health.

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