Palonosetron

Trade Names:
Aloxi
- Injection 0.25 mg

Pharmacology

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

Pharmacokinetics

Absorption

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

Distribution

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

Metabolism

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.

Elimination

Approximately 80% of the dose is recovered in the urine. The terminal t _½ is approximately 40 h.

Indications and Usage

Prevention of acute nausea and vomiting associated with moderately and highly emetogenic cancer chemotherapy; prevention of delayed nausea and vomiting associated with moderately emetogenic cancer chemotherapy.

Contraindications

Standard considerations.

Dosage and Administration

IV 0.25 mg as a single dose approximately 30 min before the start of chemotherapy. Repeated dosing within a 7 day interval is not recommended.

General Advice

• For IV administration only. Not for intradermal, subcutaneous, or IM administration.
• Do not administer if particulate matter, cloudiness, or discoloration 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.

Storage/Stability

Store vials at controlled room temperature (59° to 86°F). Protect from light and freezing.

Drug Interactions

None well documented.

Do not mix with other drugs.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Nonsustained tachycardia, bradycardia, hypotension (1%).

CNS

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

GI

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

Metabolic

Hyperkalemia (1%).

Miscellaneous

Weakness (1%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

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 pre-existing cardiac impairment, administer with caution in patients who have or may develop prolongation of cardiac conduction intervals, particularly QTc.

Patient Information

• Advise patient, family, or caregiver that medication 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 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.

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