Palonosetron

Palonosetron may be found in some form under the following brand names:

• Akynzeo

• Aloxi

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of palonosetron, there are no specific foods that you must exclude from your diet when receiving this medication.

• Tell all of your health care providers that you take palonosetron. This includes your doctors, nurses, pharmacists, and dentists.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Chest pain or pressure or passing out.
• Slow heartbeat.
• Chills.
• Sore throat.
• Trouble passing urine.
• Trouble controlling body movements.
• A very bad and sometimes deadly health problem called serotonin syndrome may happen. The risk may be greater if you take this medicine with drugs for depression, migraines, or certain other drugs. Call your doctor right away if you have agitation; change in balance; confusion; hallucinations; fever; fast or abnormal heartbeat; flushing; muscle twitching or stiffness; seizures; shivering or shaking; sweating a lot; very bad diarrhea, upset stomach, or throwing up; or very bad headache.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache.
• Hard stools (constipation).

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

• Antiemetic
• Selective 5-HT3 Receptor Antagonist

Palonosetron is a selective 5-HT3 receptor antagonist, blocking serotonin, both on vagal nerve terminals in the periphery and centrally in the chemoreceptor trigger zone

Absorption

Capsules [Canadian product]: Well absorbed

Distribution

Vd:Children 1 month to 17 years: Mean range: 5.3 to 6.3 L/kg; Adults: 8.3 ± 2.5 L/kg

Metabolism

~50% metabolized via CYP enzymes (and likely other pathways) to relatively inactive metabolites (N-oxide-palonosetron and 6-S-hydroxy-palonosetron); CYP1A2, 2D6, and 3A4 contribute to its metabolism

Excretion

Urine (80%; 40% as unchanged drug)

Clearance:

Infants and children <2 years: 0.31 L/hour/kg

Children 2 to <12 years: Mean range: 0.19 to 0.23 L/hour/kg

Children ≥12 years, Adolescents, and Adults: 0.160 L/hour/kg

Time to Peak

Plasma: Capsules [Canadian product]: 5.1 ± 5.9 hours

Half-Life Elimination

IV: Children 1 month to 17 years: Median: 29.5 hours (range: 20 to 30 hours); Adults: ~40 hours

Protein Binding

~62%

No dosage adjustment is necessary.

Store intact vials at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Do not freeze. Protect from light. Solutions of 5 mcg/mL and 30 mcg/mL in NS, D5W, D51/2NS, and D5LR injection are stable for 48 hours at room temperature and 14 days under refrigeration (Trissel 2004).

Capsules [Canadian product]: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).