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.
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.Elderly
No dosage adjustments or special monitoring are needed in elderly patients.Race
Has not been adequately characterized.Gender
Dosage adjustments are not necessary based on gender.
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.Oral
Prevention of acute nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy.
IV 0.25 mg administered over 30 sec approximately 30 min before the start of chemotherapy.Adults
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.
Store at 59° to 86°F. Protect from light and protect injectable from freezing.
None well documented.
None well documented.
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%).
Burning, discomfort, induration, pain (postmarketing).
Category B .
Safety and efficacy not established.
May occur in patients who have exhibited hypersensitivity to other selective 5-HT 3 receptor antagonists.
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.
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