Systemic Therapy Program
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Disease Group



Cancer Type

Document Type

Drug Monographs
Treatment Regimens
Scientific Name:
PALONOSETRON
Brand Name(s):
Aloxi

Drug Monograph

Pharmacology

Mechanism of Action

Selective serotonin receptor (5-HT3) antagonist, blocking serotonin both peripherally (primary site of action) and centrally in the chemoreceptor trigger zone. Palonosetron has a high affinity for this receptor, and no other receptors.

Pharmacokinetics

Distribution
Excretion in breast-milk unknown
cross blood brain barrier? unknown
Vd:  8.3 +/- 2.5 L/kg
PPB: 62%
Metabolism
multiple routes of metabolism, including CYP2D6, CYP3A, CYP1A2
Inactive Metabolites: N-oxide-palonosetron, 6-5-hydroxy-palonosetron
Excretion
80% of a dose is recovered in the urine within 144 hrs, about half as metabolites and half as unchanged drug).
Cl  160 +/- 35 mL/h/kg (total body)
  66.5 +/- 18.2 mL/h/kg (renal)
t½  Terminal: 40 hours

Side Effects

IMMEDIATE ONSET (hours to days)
   headache (9%)
EARLY ONSET  (days to weeks)
   constipation (5%)
   sedation, diarrhea, fatigue (all <1%)

Therapeutics

Approved Indications

Prevention of acute and delayed nausea & vomiting from highly or moderately emetogenic chemotherapy

Routes

I.V. bolus

Administration

• Injected into free-flowing IV over 30 seconds, flush line with Normal Saline

IV Compatibility

Normal Saline

Dosing

Standard dosing:
• 0.25mg IV (inject as IV bolus over 30 seconds), starting 30 minutes before chemotherapy
• It is not recommended to administer a second dose within 7 days
• Palonosetron may be administered with dexamethasone, but this has not been assessed for improvement of effectiveness
See ‘Guidelines For The Management Of Nausea & Vomiting In Cancer Patients’ for further dosing details
Pediatric:
No pediatric dosing has been established

Contraindications

Sensitivity to palonosetron, or product components

Monitoring

Clinical Monitoring

NO RECOMMENDED TOXICITY RATINGS

Extravasation Hazard

No

Significant Interactions

None Known Palonosetron is not an inhibitor of CYP450 isoenzymes, and is metabolized by multiple mechanism; therefore interactions through this mechanism are unlikely

Product Information

Commercial Product Description

Brand Name: AloxiTM Vials with 0.25mg/5mL

Pharmaceutical Considerations

Injection:  Ampoules of 0.25mg/5mL single-use clear solution without preservative.
Store at 20-25oC; Do not freeze, protect from light

Availability & Funding

Administrative Information (Nova Scotia)

CCNS Provincial Formulary Status- Basic Level Pharmacare Formulary Status- Non-Formulary