Dosing and uses of Aloxi (palonosetron)
Adult dosage forms and strengths
injectable solution: single-use vials
- 0.05mg/mL
Prevention of Chemotherapy-induced Nausea & Vomiting
Indicated for prevention of acute N/V associated with moderately or highly emetogenic chemotherapeutic agents; also for delayed N/V associated moderately emetogenic chemotherapeutic agents
0.25 mg IV over 30 seconds x1, beginning 30 minutes before chemotherapy
Prevention of Postoperative Nausea & Vomiting
Indicated for prevention of PONV following surgery; efficacy beyond 24 hr has not been demonstrated
0.075 mg IV infused over 10 seconds immediately before anesthesia
Dosage modifications
Renal or hepatic impairment: Dose adjustment not necessary
Pediatric dosage forms and strengths
injectable solution: single-use vials
- 0.05mg/mL
Prevention of Chemotherapy-induced Nausea & Vomiting
Indicated for prevention of acute N/V associated with initial and repeat courses of emetogenic cancer chemotherapy, including highly emetogenic cancer chemotherapy
<1 month: Safety and efficacy not established
1 month to 17 years: 20 mcg/kg IV infused over 15 minutes x1, beginning 30 minutes before chemotherapy; not to exceed 1.5 mg/dose
Prevention of Postoperative Nausea & Vomiting
<18 years: Safety and efficacy not established
Aloxi (palonosetron) adverse (side) effects
1-10%
Prolonged QT interval (up to 5% )
Anxiety
Dizziness
Headache
Weakness
Constipation
Diarrhea
Prutitus
Hyperkalemia
LFT's increased
<1%
First degree atrioventricular block
Second degree atrioventricular block
Frequency not defined
Immune hypersensitivity reaction (very rare)
Seizure
Warnings
Contraindications
Hypersensitivity to drug, other selective 5-HT3 receptor antagonists (eg, granisetron), or any other component
Coadministration with apomorphine; combination reported to cause profound hypotension and loss of consciousness
Cautions
Use caution in patients with congenital long QT syndrome or other factors that may prolong QT intervaL
Serotonin syndrome reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs including SSRIs, SNRIs, MAO inhibitors, lithium, tramadol, methylene blue IV, and mirtazapine
Hypersensitivity reactions, including anaphylaxis, reported with or without known hypersensitivity to other 5-HT3 receptor antagonists
For chemotherapy, the drug should follow a specific schedule, and not be administered as needed
Drug is not recommended in PONV if expectation for nausea or vomiting is very small; use only if the expectation is low or it is essential to avoid nausea and vomiting in the postoperative period
Pregnancy and lactation
Pregnancy category: B
Lactation: unknown, discontinue drug or do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Aloxi (palonosetron)
Mechanism of action
Selective 5-HT3 receptor antagonist; palonosetron binds to 5-HT3 receptors both in peripheral and central nervous system with primary effects in GI tract
Pharmacokinetics
Half-life: 40 hr
Peak plasma: 5.6±5.5 ng/mL (dose-proportional)
AUC: 35.8±20.9 ng.hr/mL (dose-proportional)
Protein bound: 62%
Vd: 8.3±2.5 L/kg
Metabolism: CYP2D6, CYP3A and CYP1A2
Metabolites: N-oxide-palonosetron and 6-S-hydroxy-palonosetron (<1% parent activity)
Excretion: Urine (80-93%); feces (5-8%)
Clearance: 160±35 mL/hr/kg (total)
Administration
IV Incompatibilities
Do not mix with other drugs
IV Administration
Flush IV line with NS before and after administration
CINV: give IVP evenly over 30 sec (adults) or 15 min (children)
PONV: IVP over 10 sec
