What is palonosetron used for?

Palonosetron is a prescription medicine that is used to prevent upset stomach and throwing up.

Description

ALOXI (palonosetron hydrochloride) is an antiemetic and antinauseant agent. It is a serotonin subtype 3 (5-HT3) receptor antagonist with a strong binding affinity for this receptor. Chemically, palonosetron hydrochloride is: (3aS)-2-[(S)-1-Azabicyclo [2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1-oxo-1Hbenz[de]isoquinoline hydrochloride. The empirical formula is C19H24N2O.HCl, with a molecular weight of 332.87. Palonosetron hydrochloride exists as a single isomer and has the following structural formula:

Palonosetron hydrochloride is a white to off-white crystalline powder. It is freely soluble in water, soluble in propylene glycol, and slightly soluble in ethanol and 2-propanol.

ALOXI injection is a sterile, clear, colorless, non pyrogenic, isotonic, buffered solution for intravenous administration. ALOXI injection is available as 5-mL single use vial or 1.5-mL single use vial. Each 5-mL vial contains 0.25 mg palonosetron base as 0.28 mg palonosetron hydrochloride, 207.5 mg mannitol, disodium edetate and citrate buffer in water for intravenous administration.

Each 1.5-mL vial contains 0.075 mg palonosetron base as 0.084 mg palonosetron hydrochloride, 83 mg mannitol, disodium edetate and citrate buffer in water for intravenous administration.

The pH of the solution in the 5-mL and 1.5-mL vials is 4.5 to 5.5.

 Mechanism of Action

Palonosetron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors.

Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex

Postoperative nausea and vomiting is influenced by multiple patient, surgical and anesthesia related factors and is triggered by release of 5-HT in a cascade of neuronal events involving both the central nervous system and the gastrointestinal tract. The 5-HT3 receptor has been demonstrated to selectively participate in the emetic response.

Before taking palonosetron, tell your doctor:

• If you are allergic to palonosetron; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take palonosetron with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take palonosetron?

• 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, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is palonosetron best taken?

Use palonosetron as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given as a shot into a vein.

What do I do if I miss a dose?

• Call your doctor to find out what to do.

What are the side effects of palonosetron that I need to call my doctor about immediately?

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, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Chest pain.
• Pain and irritation where palonosetron goes into the body.
• A type of abnormal heartbeat (prolonged QT interval) can happen with palonosetron. Call your doctor right away if you have a fast heartbeat, a heartbeat that does not feel normal, or if you pass out.
• A severe and sometimes deadly problem called serotonin syndrome may happen. The risk may be greater if you also take 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; severe diarrhea, upset stomach, or throwing up; or very bad headache.

What are some other side effects of palonosetron?

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.
• 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 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

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.

How do I store and/or throw out palonosetron?

• If you need to store palonosetron at home, talk with your doctor, nurse, or pharmacist about how to store it.

Label

PRINCIPAL DISPLAY PANEL-Label

NDC 16729- 365-66
Palonosetron HCl injection
0.25 mg/5 mL (0.05 mg/mL)
For intravenous injection only.
5 mL single-use sterile vial.

 

PRINCIPAL DISPLAY PANEL-Carton

NDC 16729- 365-66
Palonosetron HCl injection
0.25 mg/5 mL (0.05 mg/mL)
For intravenous injection only.
5 mL single-use sterile vial.
Discard unused portion

SRC: NLM .