Akynzeo (Netupitant and Palonosetron) – Oral

What Is Akynzeo?

Akynzeo (netupitant and palonosetron) is a prescription medication made up of two primary ingredients, netupitant and palonosetron hydrochloride. It is given along with the anti-inflammatory steroid dexamethasone to prevent acute and delayed nausea and vomiting caused by emetogenic chemotherapy—chemotherapy that is associated with a higher incidence of nausea—in adults ages 18 and older.

Both netupitant and palonosetron work by blocking natural chemicals in your body that can cause nausea and vomiting.

Akynzeo is available as a capsule, taken by mouth, and as a solution to be administered intravenously (IV).

What Is Akynzeo Used For?

Akynzeo has been approved by the Food and Drug Administration (FDA) to prevent nausea and vomiting associated with chemotherapy in adults. Akynzeo should be taken along with the drug dexamethasone.

Akynzeo capsules contain two different medications: netupitant and palonosetron. Netupitant is an antiemetic medication (a drug used to treat nausea) that belongs to a group of drugs called neurokinin 1 receptor (NK1R) antagonists. These NK1R medications are a class of antiemetic drugs that possess unique anxiolytic (antianxiety), antidepressant, and antiemetic properties.

Comparatively, palonosetron is an antiemetic used to prevent nausea and vomiting, and is categorized as a 5-HT3 receptor antagonist. These 5-HT3 medications are used to treat certain types of irritable bowel syndrome (IBS) and to relieve nausea and vomiting.

Chemotherapy-induced nausea and vomiting can be divided into different phases. Acute nausea and vomiting occur within 24 hours of chemotherapy. Delayed nausea and vomiting happen between two and five days after receiving chemotherapy. Akynzeo helps prevent both the acute and delayed phases.

How to Take Akynzeo

Akynzeo should be taken one hour before receiving your chemotherapy. One dose is enough to treat acute and delayed nausea and vomiting. You can take Akynzeo with or without food.

Your healthcare provider will also prescribe dexamethasone, a steroid medication that works with Akynzeo to prevent nausea and vomiting. Dexamethasone should be taken 30 minutes before receiving chemotherapy. Depending on your chemotherapy regimen, your healthcare provider may also prescribe dexamethasone for the three days after chemotherapy.

Take Akynzeo exactly as directed. Do not take more or less of it or take it more often than prescribed by your healthcare provider.

Storage

Store Akynzeo at room temperature (about 68–77 degrees Fahrenheit). Occasional short trips in temperatures between 59 and 86 degrees are permitted. Store Akynzeo away from direct heat, moisture, and light. Keep the medication out of reach and out of sight of children and pets.

What Are the Side Effects of Akynzeo?

This is not a complete list of side effects, and others may occur. A medical professional can advise you on side effects. If you experience other effects, contact your pharmacist or a medical professional. You may report side effects to the FDA at www.fda.gov/medwatch or 800-FDA-1088.

As with all medications, Akynzeo can cause side effects. Tell your healthcare provider about any side effects you experience while taking this medication.

Common Side Effects

Most people are able to take Akynzeo without any problems, but side effects can occur. Be sure to let your healthcare provider know if you experience any side effects worsen or continue.

The most common side effects of Akynzeo include:

• Constipation 
• Fatigue 
• Headache 
• Skin redness 
• Upset stomach 
• Muscle weakness
  

Severe Side Effects

Rarely, Akynzeo may cause severe reactions. Call your healthcare provider right away if you experience any severe side effects. Call 911 if your symptoms feel life-threatening or if you think you’re experiencing a medical emergency. 

Anaphylaxis is a severe, sudden allergic reaction to an allergen that can occur when taking this drug.

Seek emergency medical help right away if you develop:

• Chest pain 
• Urticaria (hives)
• Angioedema (swollen face)
• Dyspnea (trouble breathing)

Serotonin syndrome is a rare but potentially life-threatening condition that develops from too much serotonin building up in your body. Akynzeo can cause serotonin syndrome by itself, but it’s more likely to occur if you take other medicines like antidepressants or antimigraine drugs with Akynzeo.

Stop taking Akynzeo and go to the nearest emergency room if you develop any signs of serotonin syndrome, including:

• Agitation 
• Diarrhea 
• Dizziness 
• Tachycardia (fast heartbeat)
• Fever
• Hallucinations or other changes in mental status
• Muscle twitching
• Nausea and vomiting 
• Seizures 
• Tremors
• Sweating
• Dyskinesias (unsteady movements)

Dosage: How Much Akynzeo Should I Take?

Modifications

Users should be aware of the following before beginning Akynzeo:

Pregnancy: ​​Studies are limited on the effects of Akynzeo on the health of a fetus. Notify your healthcare provider if you are pregnant, become pregnant, or plan to become pregnant while taking this drug.

Breastfeeding: While there is no evidence that breastfeeding while taking Akynzeo poses any harm to a nursing baby, speak with your healthcare provider to fully weigh the risks and benefits of treatment before breastfeeding while on Akynzeo.

Adults over 65: For older individuals, a change in dosage may be necessary due to past clinical studies having showed that people in this age group experienced a variety of decreased hepatic (liver), renal (kidney), or cardiac (heart) function as a result of Akynzeo consumption.

Pediatric use: The safety and effectiveness of Akynzeo have not been established in people under 18 years of age. Therefore, only adults should be prescribed and take the medication.

People who smoke: Smoking can lower Akynzeo's effectiveness. Try to stop smoking before starting Akynzeo and avoid smoking while taking Akynzeo. Your healthcare provider can help you with this goal.

Missed Dose

Because Akynzeo is intended to be taken as needed, if you miss a dose, take it when you remember. If it is almost time for the next dose, skip the missed dose and resume your regular dosing schedule. Do not take an extra dose to try to make up for a missed dose.

Overdose: What Happens If I Take Too Much Akynzeo?

Do not take more Akynzeo than directed on the package label.

Akynzeo comes in a package containing one capsule, so an overdose is unlikely. During clinical trials, some participants received an Akynzeo dose about 12 times greater than the normal dose.

The side effects that occurred with this high dosing were similar to those seen with the normal dosing. In studies, high-dosage side effects included constipation, fatigue, headache, skin redness, upset stomach, and weakness.

Regardless, general signs of a potential medication-related drug overdose include:

• Nausea or vomiting
• Appetite loss
• Sweating
• Bleeding
• Bruising
• Upper stomach pain
• Jaundice (yellowing of the skin or whites of the eyes)
  

Precautions

What Are Reasons I Shouldn't Take Akynzeo?

Akynzeo is not appropriate for everyone. You should not take this medication if you are allergic to netupitant, palonosetron, or any of the inactive ingredients in Akynzeo.

Additionally, make your healthcare provider know about any and all allergies you may have, including any past reactions to:

• Lotronex (alosetron)
• Anzemet (dolasetron)
• Sancuso (granisetron)
• Zofran (ondansetron)
  

What Other Medications May Interact With Akynzeo?

Tell your healthcare provider about all of the medicines you take, including prescription and over-the-counter (OTC) medicines, and vitamins or supplements. 

Akynzeo may increase the levels of certain medications. Your healthcare provider may recommend avoiding or lowering the dose of the following medicines:

• Benzodiazepines, such as Nayzilam (midazolam), Xanax (alprazolam), and Halcion (triazolam)
• Rhinocort (budesonide)
• Certain cholesterol-lowering medications, such as Livalo (pitavastatin) and Zocor (simvastatin)
• Colcrys (colchicine)
• Erectile dysfunction (ED) medicines, such as Viagra (sildenafil), Cialis (tadalafil), or Levitra (vardenafil)
• Flonase (fluticasone) 
• Neoral (cyclosporine) 
• Norpace (disopyramide)
• Orap (pimozide)
• Uroxatral (alfuzosin)

Some drugs may prevent Akynzeo from working as well, including:

• Dilantin (phenytoin)
• Mysoline (primidone) 
• Donnatal (phenobarbital, hyoscyamine sulfate, atropine sulfate, and scopolamine hydrobromide)
• Rifadin (rifampin) 
• Tegretol (carbamazepine)

Taking certain medications with Akynzeo can increase your chance of developing serotonin syndrome. Let your healthcare provider know if you take:

• Antidepressant medications, such as Elavil (amitriptyline)
• Fentanyl 
• Lithium 
• Remeron (mirtazapine) 
• Selective serotonin reuptake inhibitors (SSRIs), such as Prozac (fluoxetine), Celexa (citalopram), and Paxil (paroxetine)) 
• Serotonin-norepinephrine reuptake inhibitors (SNRIs), such as Effexor XR (venlafaxine), Cymbalta (duloxetine), and Pristiq (desvenlafaxine)
• Ultram (tramadol)
• Zyvox (linezolid)

This is not a complete list of all the medicines that may interact with Akynzeo. Always keep an updated list of all the medicines you take and share this information with your healthcare provider anytime there are changes.

What Medications Are Similar?

Akynzeo is the only combination antiemetic that contains both an NK1R antagonist (netupitant) and a 5-HT3 receptor antagonist (palonosetron hydrochloride). Healthcare providers often prescribe both NK1R and 5-HT3 receptor antagonists to prevent nausea and vomiting associated with chemotherapy. Akynzeo helps cut down on the number of pills you need to take.

Other NK1R antagonists include:

• Emend (aprepitant)
• Varubi (rolapitant) 

Other 5-HT3 receptor antagonists include:

• Sancuso (granisetron)
• Zofran (ondansetron)

This is a list of drugs also prescribed to prevent nausea and vomiting from chemotherapy. It is not a list of drugs recommended to take with Akynzeo. Do not take these drugs together. Ask your healthcare provider if you have any questions about your medications.

How Can I Stay Healthy While Taking Akynzeo?

Nausea and vomiting are some of the most feared side effects of chemotherapy. Uncontrolled symptoms can have a significant impact on your quality of life and make it hard to get through the day. Fortunately, proper prevention can greatly reduce your chances of experiencing these side effects.

Akynzeo, when taken with dexamethasone, is a highly effective option. One study found that 99% of people who received Akynzeo had no vomiting on the day of chemo, and 90% did not experience vomiting for five days after chemo.

Discuss your nausea and vomiting prevention plan with your healthcare provider. Ask whether they will prescribe a medication that you can take as needed when you experience symptoms and how often you can take it. Having a clear plan can help ease your mind before you receive your chemotherapy treatment.