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New Anti-Nausea Medication Approved for Chemotherapy Patients

  • December 11, 2014
  • RPh on the Go

nausea-medication-chemotherapy-akynzeoThe Food and Drug Administration (FDA) recently approved a combination medication, netupitant-palonosetron, to prevent nausea and vomiting in patients receiving chemotherapy. Known as Akynzeo, the medication uses both the neurokinin-1 receptor antagonist netupitant and the serotonin type 3-receptor antagonist palonosetron. Each capsule has three 100-mg netupitant tablets, and one 0.56 mg palonosetron hydrochloride capsule. The medication can be taken with or without food.

The product’s labeling suggests adults should take one capsule by mouth approximately an hour prior to starting a chemotherapy treatment. Adults who receive high emetogenic chemotherapy should take 12 mg of dexamethasone by mouth once per day on days two through four of treatment.

Adults who are receiving either anthracyclines or cyclophosphamide based chemotherapy, or another other form of chemotherapy are not considered highly emetogenic. Those who are not using highly emetogenic chemotherapy should only take one dose of 12 mg dexamethasone before the start of chemotherapy on the first day.

The netupitant and is metabolite inhibits cytochrome P-450 (CYP) isoenzyme 3A4. It can increase CYP3A4 plasma concentration substrates for at least four days. When this medication is coadministered with rifampin, plasma concentration of netupitant can decrease by more than 50%.

This medication is not recommended for children who are undergoing any sort of chemotherapy. Clinical trials indicate the most common side effects of this treatment were: headache, indigestion, constipation, fatigue, and weakness.

Patients who are taking medications that are primarily metabolized by CYP3A4 should use this medication only when the benefit outweighs the risk, as the inhibitory effect of this medicine can last for several days. It’s important to reduce the dose of dexamethasone when given with Akynzeo.

All patients who are taking this medication should be monitored for signs of serotonin syndrome. Though rare, this condition may present as a side effect of using Akynzeo. Symptoms include: seizures, changes in mental status, autonomic instability, gastrointestinal symptoms, and neuromuscular symptoms. Hypersensitivity reactions have also been reported in rare cases.

This medicine should not be used in patients who have severe liver and/or kidney impairment, or end stage kidney disease.

Akynzeo will be supplied in cartons that contain a single capsule in a blister pack. The capsules will be hard gelatin featuring a white body and a caramel cap. “HE1” will be imprinted on the body. These cartons should be stored at 68 to 77 F, or 20 to 25 C. Eisai Inc and Helsinn Therapeutics US Inc. will co-promote the product.

Neither company has announced a date of availability for this medication.


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