Palonosetron hydrochloride

What is Palonosetron hydrochloride?

• Palonosetron hydrochloride (Aloxi) is a serotonin-3 (5-HT3) receptor antagonist used for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV), postoperative nausea and vomiting (PONV).

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Palonosetron structure

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Palonosetron 3D

What are the uses of this medicine?

Palonosetron hydrochloride (Aloxi) is a prescription medicine called an “antiemetic.” Aloxi is used in adults to help prevent the nausea and vomiting that happens:

• right away or later with certain anti-cancer medicines (chemotherapy)
• up to 24 hours while recovering from anesthesia after surgery
• Aloxi is used in children 1 month old to less than 17 years of age to help prevent the nausea and vomiting that happens right away with certain anti-cancer medicines (chemotherapy).

How does this medicine work?

• Palonosetron is a 5-HT3 receptor antagonist.
• 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.
• Palonosetron hydrochloride blocks the action of the chemical serotonin, which binds to certain nerves and may trigger nausea and vomiting. Blocking serotonin may help lessen nausea and vomiting.
• Palonosetron hydrochloride is a type of serotonin receptor antagonist and a type of antiemetic.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• are allergic to palonosetron hydrochloride or any of the ingredients in Aloxi.

What drug interactions can this medicine cause?

Serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular symptoms) has been described following the concomitant use of 5-HT3 receptor antagonists and other serotonergic drugs (e.g., selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and intravenous methylene blue).

Is this medicine FDA approved?

• The oral formulation was approved on August 22, 2008, for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.

How should this medicine be used?

Recommended dosage: Postoperative Nausea and Vomiting:

• Dosage for Adults - a single 0.075 mg intravenous dose administered over 10 seconds immediately before the induction of anesthesia.

Chemotherapy-Induced Nausea and Vomiting:

Age	Dose	Infusion Time
Adults	0.25 mg x 1	Infuse over 30 seconds beginning approx. 30 min before the start of chemo
Pediatrics(1 month to less than 17 years)	20 micrograms per kilogram (max 1.5 mg) x 1	Infuse over 15 minutes beginning approx. 30 min before the start of chemo

Administration:

• Aloxi will be given to you in your vein by intravenous (I.V.) injection.
• Aloxi is usually given about 30 minutes before you receive your anti-cancer medicine (chemotherapy) or right before anesthesia for surgery.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 0.25 mg/5mL (free base) single-use vial
• 0.075 mg/1.5mL (free base) single-use vial

This medicine is available in fallowing brand namesː

• Aloxi

What side effects can this medication cause?

The most common side effects of Aloxi in adults are headache and constipation.

Aloxi can cause allergic reactions that can sometimes be serious which may include:

• hives
• swollen face
• breathing trouble
• chest pain

What special precautions should I follow?

• Hypersensitivity reactions, including anaphylaxis, have been reported with or without known hypersensitivity to other selective 5-HT3 receptor antagonists.
• The development of serotonin syndrome has been reported with 5-HT3 receptor antagonists. Most reports have been associated with concomitant use of serotonergic drugs (e.g., selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and intravenous methylene blue).If symptoms of serotonin syndrome occur, discontinue Aloxi and initiate supportive treatment. Patients should be informed of the increased risk of serotonin syndrome, especially if Aloxi is used concomitantly with other serotonergic drugs.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• convulsions
• gasping
• pallor
• cyanosis
• collapse

Management of overdosage:

• There is no known antidote to Aloxi.
• Overdose should be managed with supportive care.

Can this medicine be used in pregnancy?

• Adequate and well controlled studies with Aloxi have not been conducted in pregnant women.
• Aloxi should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• It is not known if Aloxi is safe and effective in children less than 1 month old to help prevent nausea and vomiting after chemotherapy.
• It is not known if Aloxi is safe and effective in children for the prevention of nausea and vomiting while recovering from anesthesia after surgery.

What are the active and inactive ingredients in this medicine?

• Active ingredient: palonosetron hydrochloride
• Inactive ingredients: mannitol, disodium edetate, and citrate buffer in water

Who manufactures and distributes this medicine?

Distributed by: Eisai Inc., Woodcliff Lake, NJ under license of Helsinn Healthcare SA, Switzerland.

• Marketed by Eisai Inc., Woodcliff Lake, NJ and Helsinn Therapeutics (U.S.), Inc. Iselin, NJ , under license of Helsinn Healthcare SA, Switzerland.
• Aloxi® is a registered trademark of Helsinn Healthcare, SA, Lugano, Switzerland.

What should I know about storage and disposal of this medication?

• Store at controlled temperature of 20–25°C (68°F–77°F). Excursions permitted to 15–30°C (59-86°F).
• Protect from freezing.
• Protect from light.

• Dailymed label info on Palonosetron hydrochloride
• FDA Palonosetron hydrochloride

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