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Aloxi

Aloxi - General Information

Aloxi (INN, trade name Aloxi) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy and is the only drug of its class approved for this use by the U.S. Food and Drug Administration. As of 2007, it is the most recent 5-HT3 antagonist to enter clinical use. [Wikipedia]

 

Pharmacology of Aloxi

Aloxi is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Aloxi is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors.

 

Aloxi for patients

ALOXI™
(Ah-lock-see)
Palonosetron HCI injection

PATIENT COUNSELING INFORMATION

Instructions for Patients

  • Patients should be advised to report to their physician all of their medical conditions, especially if they have heart problems including a problem called “congenital QT syndrome” or they are taking medicines that have caused or may cause severe heart beat changes such as diuretics, anti-arrhythmics or anthracycline. [see WARNINGS and PRECAUTIONS].
  • Patients should be advised to report to their physician any pain, redness, or swelling in and around the infusion site [see ADVERSE REACTIONS].
  • Patients should be instructed to read the patient insert.

FDA-Approved Patient Labeling

Read the Patient Information that comes with ALOXI before your treatment with ALOXI and each time you get ALOXI. There may be new information. This information does not take the place of talking with your doctor about your medical condition or your treatment. If you have questions about ALOXI, ask your doctor or pharmacist.

What is ALOXI?

ALOXI is a medicine called an “antiemetic.” ALOXI is used in adults to help prevent the nausea and vomiting that happens:

  • right away with certain anti-cancer medicines (chemotherapy)
  • or later with certain anti-cancer medicines

What is ALOXI used for?

ALOXI is used to prevent nausea and vomiting that may happen: soon after taking certain anti-cancer medicines later after taking certain anti-cancer medicines

Who should not take ALOXI?

Do not take ALOXI if you are allergic to any of the ingredients in ALOXI. The active ingredient is palonosetron hydrochloride. See the end of this leaflet for a complete list of ingredients in ALOXI.

ALOXI has not been studied in children under 18 years of age.

What should I tell my doctor before using ALOXI?

Tell your doctor about all of your medical conditions, including if you:

  • have heart problems including a problem called “congenital QT syndrome”
  • have low potassium in your blood have low magnesium in your blood
  • are pregnant. It is not known if ALOXI may harm your unborn baby. You and your doctor should decide if ALOXI is right for you.
  • are breastfeeding. It is not known if ALOXI passes into your milk and if it can harm your baby. You should choose to either take ALOXI or breastfeed, but not both.

Tell your doctor about all of the medicines you take including prescription and nonprescription medicines, vitamins and herbal supplements. ALOXI should be given with caution in patients who may be taking other medicines that have caused, or may cause, severe heart beat changes.

Especially, tell your doctor if you take:

  • “water pills” (diuretics)
  • medicine to control your heartbeat (anti-arrhythmics)
  • anthracycline (an anti-cancer medicine)

How should I use ALOXI?

ALOXI is given in your vein by IV (intravenous) injection. It is only given to you by a healthcare provider in a hospital or clinic. ALOXI is usually injected into your vein about 30 minutes before you get your anti-cancer medicine (chemotherapy).

What are the possible side effects of ALOXI?

ALOXI should be given with caution in patients who have or may develop severe heart beat changes from QT prolongation. This can happen in people who have certain heart or other medical problems or who take certain medicines.

The most common side effects of ALOXI are headache and constipation. Diarrhea and dizziness have also been observed.

These are not all the side effects from ALOXI. For more information ask your doctor or pharmacist.

General information about ALOXI

Medicines are sometimes prescribed for conditions other than those listed in patient information leaflets. ALOXI was prescribed for your medical condition.

This leaflet summarizes the most important information about ALOXI. If you would like more information, talk with your doctor. You can ask your doctor or pharmacist for information about ALOXI that is written for health professionals. You can also visit the ALOXI web site at www.ALOXI.com. Or visit www.ManageCINV.com. This is a web site for patients with nausea and vomiting from anti-cancer medicines.

What are the ingredients in ALOXI?

Active ingredient: palonosetron hydrochloride

Inactive ingredients: mannitol, disodium edetate, and citrate buffer in water

 

Aloxi Interactions

Palonosetron is eliminated from the body through both renal excretion and metabolic pathways with the latter mediated via multiple CYP enzymes. In vitro studies indicated that palonosetron is not an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP2E1 and CYP3A4/5 (CYP2C19 was not investigated) nor does it induce the activity of CYP1A2, CYP2D6, or CYP3A4/5. Therefore, the potential for clinically significant drug interactions with palonosetron appears to be low.

A study in healthy volunteers involving single-dose IV palonosetron (0.75 mg) and steady state oral metoclopramide (10 mg four times daily) demonstrated no significant pharmacokinetic interaction.

In controlled clinical trials, ALOXI injection has been safely administered with corticosteroids, analgesics, antiemetics/antinauseants, antispasmodics and anticholinergic agents.

Palonosetron did not inhibit the antitumor activity of the five chemotherapeutic agents tested (cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin C) in murine tumor models.

 

Aloxi Contraindications

ALOXI is contraindicated in patients known to have hypersensitivity to the drug or any of its components.

 

Additional information about Aloxi

Aloxi Indication: For the treatment of nausea and vomiting associated with cancer chemotherapy.
Mechanism Of Action: Aloxi is a selective serotonin 5-HT3 receptor antagonist. The serotonin 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 efferents to initiate the vomiting reflex. Therefore Aloxi works by blocking the reception of serotonin at these 5-HT3 receptors.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Palonosetron
Synonyms: Not Available
Drug Category: Antiemetics; Serotonin Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Palonosetron: Aloxi; Onicit;
Absorption: Low oral bioavailability.
Toxicity (Overdose): A single intravenous dose of palonosetron at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse.
Protein Binding: 62%
Biotransformation: Hepatic (50%), primarily CYP2D6-mediated, although CYP3A4 and CYP1A2 are also involved.
Half Life: Approximately 40 hours
Dosage Forms of Aloxi: Solution Intravenous
Chemical IUPAC Name: Not Available
Chemical Formula: C19H24N2O
Palonosetron on Wikipedia: http://en.wikipedia.org/wiki/Palonosetron
Organisms Affected: Humans and other mammals