Akynzeo
Akynzeo
Netupitant, Palonosetron Hydrochloride
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Akynzeo (Netupitant, Palonosetron Hydrochloride)

What is Akynzeo?

Akynzeo is a prescription-only drug in a capsule form, used to prevent nausea and vomiting in adults receiving highly to moderately emetogenic chemotherapy treatment. The most common side-effects of chemotherapy are nausea and vomiting; without the proper prophylactic treatment, cancer patients will experience these symptoms. Preventing and managing these side effects of chemotherapy is an integral part of the care plan for cancer patients. These side effects are distressing for the patient and their family members. If left untreated, cancer patients can become nonadherent to treatment and discontinue their therapy early on. Unresolved nausea and vomiting can cause nutritional deficiencies, appetite, and eating disorders. Chemotherapy-induced nausea and vomiting can impair patients’ daily function and cause them to have more frequent doctor visits or emergency department visits. Nausea and vomiting brought about by chemotherapy can vary and depend on the chemotherapy drug, its regimen, route of administration, and dosage. Gender and age are also related factors. Cisplatin-containing chemotherapy is considered highly emetogenic, although Akynzeo is also used with moderately emetogenic chemotherapy.

Akynzeo contains two active ingredients; 300mg of netupitant and 0.5mg of palonosetron hydrochloride. The combination of these anti-nausea and antiemetic drugs help to treat and prevent acute or delayed nausea and vomiting. Chemotherapy is used to treat cancer. This commonly causes severe nausea and vomiting when receiving initial or repeated doses. In addition, highly emetogenic or moderately emetogenic chemotherapy is known to induce vomiting.

How does it work?

The active ingredients in Akynzeo are responsible for blocking two mechanisms involved in inducing nausea and vomiting, initiated during chemotherapy.

Netupitant blocks neurokinin-1 receptors found broadly in the central and peripheral nervous systems. These receptors are responsible for the delayed phase of nausea and vomiting, usually occurring after the first 24 hours after receiving chemotherapy.

Palonosetron blocks 5HT3 receptors acting as an antagonist. These receptors can be found in the gut and are responsible for the immediate phase of nausea, happening within the first 24 hours of receiving chemotherapy, and are highly dependent on serotonin and 5HT3 receptors. Chemotherapy induces vomiting and sickness by stimulating the production of serotonin in the small intestine. Serotonin activates 5HT3 receptors in the vagal afferents and starts the vomiting reflex. Combining these drugs helps control both phases of nausea and vomiting induced by chemotherapy.

Dosage

Akynzeo comes in capsule form with 300mg of netupitant and 0.5mg of palonosetron.

How to take Akynzeo?

Take Akynzeo precisely as prescribed.

Those undergoing highly emetogenic chemotherapy, usually cisplatin-based, are recommended to have a capsule 1 hour before the administration of chemotherapy. This is generally accompanied by the administration of dexamethasone 30 minutes before the administration of chemotherapy. Dexamethasone can also be given for a few days after the chemotherapy has been administered.

For moderately emetogenic chemotherapy, one capsule of Akynzeo is recommended an hour before the start of chemotherapy and accompanied by dexamethasone 30 minutes before. Usually, in these cases, follow-up dexamethasone doses are not required.

You can take Akynzeo either with or without food. However, the capsule should not be opened and should be swallowed whole.

Akynzeo is given in advance to prevent nausea and vomiting.

How to store Akynzeo?

Store the capsules in their original container, away from moisture or heat. Keep at room temperatures and away from children and pets. Avoid storing it in the bathroom.

Overdose

Acute symptoms of overdose with Akynzeo are:

  • Headache
  • Dizziness
  • Constipation
  • Anxiety and palpitations
  • Euphoria
  • Leg pain

Because of the antiemetic properties of this medication, drug-induced emesis may not be successful.

If you suspect overdosing on Akynzeo, discontinue taking it and seek immediate medical attention. Seek immediate medical attention by contacting the poison control center or calling 911 if you feel like passing out or have difficulty breathing.

Side Effects

Contact your healthcare professional if you notice any of the following symptoms.

Common side effects of this medication include:

  • Headache
  • Tiredness and weakness
  • Upset stomach
  • Constipation
  • Dyspepsia
  • Erythema
  • Serotonin syndrome. Signs of this condition include agitation, fever, sweating, hallucinations, increased heart rate, muscle stiffness, twitching, diarrhea, loss of coordination, dilated pupils, confusion, headache, unconsciousness, and shivering. When Akynzeo is used concomitantly with serotonergic drugs like SSRIs, SNRIs, mirtazapine, fentanyl, lithium, tramadol, and monoamine oxidase inhibitors, serotonin levels can accumulate in the body. Seratonin syndrome can be fatal if left untreated. If you start experiencing any of these symptoms, you are to discontinue Akynzeo and seek immediate medical attention. Mild serotonin syndrome can go away within a couple of days once you seize to take the medications that have caused it. You may be given medication that blocks serotonin to counteract serotonin syndrome.

You may experience signs of anaphylaxis after taking Akynzeo. Signs and symptoms include hives, itchiness, hypotension, throat swelling and tightness, chest pain, difficulty breathing, and loss of consciousness.

Precautions

Do not take Akynzeo if you are allergic or have a hypersensitivity to its active ingredients or excipients.

All women should do a pregnancy test before starting this medication, including premenopausal women. Women of child-bearing potential should not become pregnant while on this medication. Instead, effective contraceptive methods should be used.

It is not known whether Akynzeo passes through breastmilk. Akynzeo should not be used while breastfeeding. It should be discontinued during the treatment, and no breastfeeding should be done for one month after treatment is stopped.

Since Aknyzeo can cause dizziness and fatigue, it may moderately affect driving or operating machinery. Therefore, driving or operating machinery should be done with caution.

Palonosetron can increase bowel transit time; therefore, patients with a history of constipation should be monitored closely following the administration of Akynzeo.

Warnings

Akynzeo should not be given to children under the age of 18 years.

Inform your doctor if you have severe hepatic or renal impairment or end-stage renal disease. You may need to be prescribed a slightly adjusted dose of Akynzeo or given a different treatment if this is the case.

If you are allergic to dolasetron, ondansetron, or other medication used for nausea and vomiting, let your doctor know before they prescribe Aknyzeo.

Inform your doctor if you take medication for depression, Parkinson’s disease, migraine, or headaches. This medication can be a stimulant or opioid medication. Any medication can interact with Akynzeo and cause a condition called Serotonin Syndrome.

Illicit drugs and Akynzeo may cause serotonin syndrome; therefore, be sure to inform your doctor if you use such substances and have been prescribed Akynzeo.

If you take any other over-the-counter medication, prescription, or herbal remedy, be sure to inform your doctor.

Drug interactions

The following are drugs that can interact with Aknyzeo:

  • Ivabradine- Used to treat chronic heart failure
  • SNRIs such as duloxetine, atomoxetine, and venlafaxine- Used to treat depression
  • SSRIs such as citalopram, escitalopram, fluoxetine, sertraline, and paroxetine- Used to treat depression
  • Sumatriptan- Used to treat migraines and cluster headaches
  • Oxycodone- Used to treat moderate to severe pain
  • Olanzapine- Used to treat schizophrenia, mania, and bipolar disorder
  • Hydromorphone- Used to treat moderate to severe chronic pain
  • Teriparatide- Used to strengthen bones and reduce their risk of breaking
  • Famotidine- Used to prevent and treat heartburn, stomach ulcers, esophagitis, and GERD
  • St John’s Wort- Used to treat depression
  • Rifampin- Used to treat Tuberculosis
  •  Ketoconazole- Used to treat skin infections caused by fungi
  • Granisetron, ondansetron- Used to treat nausea and vomiting

Patients who are already on tacrolimus, imatinib, anastrozole, or paclitaxel can have increased plasma concentration of these medications when taken with Aknyzeo.

Akynzeo with rifampin, carbamazepine, phenobarbital, or pioglitazone should be avoided.

Inform your doctor of any prescription, over-the-counter or herbal medicines you take before starting on Akynzeo.

Contraindications

Akynzeo is contraindicated in:

  • Patients with an allergy or hypersensitivity to its active ingredients or any of its excipients
  • Pregnant women

Frequently Asked Questions

Speak to your doctor if you have missed a dose of Akynzeo before your chemotherapy session. They may prescribe alternative medication to help prevent nausea and vomiting brought about by chemotherapy.

Akynzeo should be taken precisely as suggested by your doctor. This is usually taken 1 hour before the administration of chemotherapy.

This medication is given before chemotherapy administration to help prevent its side effects. However, taking it if you are already nauseated or have vomited may yield minimal benefits.

Akynzeo and dexamethasone are given in combination to help prevent acute and delayed nausea caused by chemotherapy. Certain chemotherapy induces nausea and vomiting more than other types; therefore, you may be given dexamethasone with Akynzeo because the chemotherapy you are being given is highly emetogenic, like cisplatin-based chemotherapy.

Akynzeo helps prevent chemotherapy-induced nausea and vomiting, while dexamethasone will help with the delayed nausea and vomiting phase. The use of dexamethasone after every chemotherapy session depends on the type of chemotherapy agent you are being given and its chances of causing delayed nausea and vomiting.

Your doctor will guide you on your eating habits and physical activity while on Akynzeo.

Akynzeo is also available in powder form to be reconstituted in a vial and administered intravenously.

Akynzeo and dexamethasone can be given together when a patient is on highly emetogenic chemotherapy. If you are being given moderately emetogenic chemotherapy, you may not need to take dexamethasone for days following your chemotherapy session. Akynzeo and dexamethasone on the day of your chemotherapy session can be enough.

Akynzeo is a prescription-only medication and needs to be ordered by your doctor.

Using these two medications together can cause various side effects. Follow your doctor’s instructions, inform them of any other medicines you could be on, and take medication as prescribed.

The excipients found in the capsule are 7mg of sorbitol, 20mg of sucrose, and less than 23mg of sodium. The capsule may also contain traces of lecithin derived from soy. Therefore, patients with known sensitivity to peanuts or soya may need to be monitored for signs of an allergic reaction during administration. In addition, the sorbitol present in the capsule can affect the bioavailability of other medicines when taken concomitantly.

Akynzeo is taken before every chemotherapy cycle for as long as your doctor prescribes.

Akynzeo is a combination of two active ingredients: anti-nausea and antiemetic. Akynzeo is not classified as a chemotherapy drug but helps with chemotherapy-induced nausea and vomiting.

You should swallow the capsule whole and not deconstruct it. This is because it contains different active ingredients that are intended to be taken at once.

Based on studies carried out, Akynzeo does not seem to have a significant effect on hormonal contraceptive pills.

In conducted studies, it was found that netupitant could be measured in the plasma within 15 minutes to 3 hours after ingesting. Concentrations in the plasma were thought to be at their maximum approximately within 5 hours after consuming.