Afinitor

1 What is Afinitor?

Brand: Afinitor, Afinitor Disperz, Zortress

Generic: Everolimus

Afinitor is used to treat late-stage kidney cancer in patients who have already received other medications that did not work well. It is also used to treat subependymal giant cell atrocytoma (SEGA; brain tumors), renal angiomyolipoma (non-cancerous kidney tumor), and late-stage pancreatic neuroendocrine tumors (PNET; a pancreas tumor that spreads to the nervous system).

This medication is used with Exemestane to treat late-stage hormone receptor-positive, HER-2 negative breast cancer in post-menopausal women who have already received other medications that did not work well.

This medication belongs to a group of medications called antineoplastics. It works by interrupting the growth of cancer cells, which are eventually destroyed by the body. Because the growth of normal body cells may also be affected, other unwanted side effects will also occur.

This medication is also used with other medications to lower the body’s natural immunity in patients who receive kidney or liver transplants. When a patient receives an organ transplant, the body’s white blood cells (WBCs) try to reject the transplanted organ. Everolimus works to suppress the immune system and prevents the WBCs from rejecting the transplanted organ.

Before you begin treatment with this medication, you should talk with your doctor about the risks and benefits of this medication.

This medication is only available with your doctor’s prescription.

This product is available in the following forms:

  • Tablet for suspension
  • Tablet
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2 What To Know Before Using

As with all medicines, the risks of using Afinitor must be compared to how much a medication will help you. This is a decision that you and your doctor will make together.

For this medication, there are many things that need to be considered:

  • AllergiesInform your doctor if you have ever had an allergic reaction to Doxorubicin or to any other medications. It is also important to inform your doctor of any non-medicine allergies such as foods, dyes, preservatives or animals.
  • Pediatric Usage: Up-to-date pediatric appropriate studies have not indicated that the use of this medication causes any problems that would limit the use of Everolimus in children when used for SEGA brain tumors. Up-to-date studies have no been performed on the relationship to age with the effects of everolimus when used for kidney cancer, pancreatic cancer (PNET), and kidney or liver transplants in the pediatric population. Safety and efficacy have not been established.
  • Geriatric Usage: Up-to-date studies have not shown any problems specific to the elderly that would limit the use of this medication in the elderly population. However, elderly patients are more likely to have unwanted side effects, which may require caution and a dose adjustment for elderly patients receiving this medication.
  • Pregnancy: This medication is listed as Pregnancy Category D. This means that studies in pregnant women have demonstrated a risk to the unborn child. However, the benefits of this medication in a life-threatening situation or serious disease may outweigh the potential risk.
  • BreastfeedingThere are no up-to-date studies in women for determining infant risk when using this medication while breastfeeding. Weigh the potential risks with the benefits before taking this medication while breastfeeding.
  • Drug Interactions: Certain medications should not be used together. However, in certain cases, two medications may be used together, even if an interaction might occur. In these cases, your doctor may want to change your dose or take other precautions. When taking this medication, it is important that you inform your doctor if you are taking any of the medications listed below. The following interactions were selected on the basis of potential significance and are not all-inclusive.Using this medication with any of the following medication is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medications you take:
    • Amprenavir
    • Atazanavir
    • Boceprevir
    • Delavirdine
    • Fosamprenavir
    • Lopinavir
    • Nelfinavir
    • Ritonavir
    • Saquinavir
    • TelaprevirUsing this medication with any of the following medication is not recommended, but may be unavoidable in some cases. Your doctor may make the decision not to treat you with this medication or change some of the other medications you take:
    • Abiraterone
    • Adenovirus Vaccine Type 4, Live
    • Adenovirus Vaccine Type 7, Live
    • Amiodarone
    • Aprepitant
    • Bacillus of Calmette and Guerin Vaccine, Live
    • Benazepril
    • Captopril
    • Carbamazepine
    • Ceritinib
    • Ciprofloxacin
    • Clarithromycin
    • Cobicistat
    • Conivaptan
    • Crizotinib
    • Dabrafenib
    • Darunavir
    • Diltiazem
    • Dronedarone
    • Eliglustat
    • Enalapril
    • Enalaprilat
    • Enzalutamide
    • Erythromycin
    • Fluconazole
    • Fosaprepitant
    • Fosinopril
    • FosphenytoinIdelalisib
    • Imatinib
    • Indinavir
    • Influenza Virus Vaccine, Live
    • Itraconazole
    • Ketoconazole
    • Lisinopril
    • Lumacaftor
    • Measles Virus Vaccine, Live
    • Mitotane
    • Moexipril
    • Mumps Virus Vaccine, Live
    • Nefazodone
    • Nilotinib
    • Perindopril
    • Phenobarbital
    • Phenytoin
    • Piperaquine
    • Poliovirus Vaccine, Live
    • Posaconazole
    • Primidone
    • Quinapril
    • Ramipril
    • Ranolazine
    • Rifabutin
    • Rifampin
    • Rifapentine
    • Rotavirus Vaccine, Live
    • Rubella Virus Vaccine, Live
    • Smallpox Vaccine
    • St. John’s Wort
    • Telithromycin
    • Tipranavir
    • Trandolapril
    • Typhoid Vaccine
    • Varicella Virus Vaccine
    • Verapamil
    • Voriconazole
    • Yellow Fever Vaccine
    • SofenoprilUsing this medication with any of the following medications may increase your risk of certain side effects. However, using both medications together may be the best treatment for you. If both medications are prescribed together, your doctor may change the dose or how often you use one or both of these medications:
    • Cyclosporine
  • Other Interactions: Certain medications should not be used while eating, or while eating certain foods in case of negative interactions. Using alcohol or tobacco with certain medications may also cause negative interactions. Talk with your doctor about the use of your medication with food, alcohol or tobacco.Using this medication with any of the following is not recommended, but may be unavoidable. If used together, your doctor may change the dose or how often you receive this medication, or give you special instructions about the use of food, alcohol or tobacco:
    • Grapefruit juice
  • Other Medical Problems: Pre-existing medical problems may affect the use of this medication. Be sure to tell your doctor if you have any other medical problems, especially:
    • Blood clotting problems
    • Diabetes
    • Current or history of Hepatites B infection
    • Hyperglycemia (high blood sugar)
    • Hyperlipidemia (high cholesterol)
    • Hypertriglyceridemia (high fat in the blood)
    • Hypoxia (low blood oxygen)
    • Infection (bacterial, fungal, viral)
    • Lung or breathing problems
    • Lymphoma (Lymph gland cancer)
    • Proteinuria (protein in the urine)
    • Skin Cancer - Use with caution. May make these conditions worse.
    • Glucose-galactase malabsorption
    • Current or history of heart transplant
    • Lapp lactase deficiency - Use of Zortress is not recommended in patients with these conditions
    • Liver disease - Use with caution. The effects may be increased because of slower removal of the medication from the body.

3 Proper Usage

Only take Afinitor as directed by your doctor. Do not take more, less or for a longer or shorter period of time than your doctor tells you.

This medication comes with a patient information brochure. It is very important that your read this information. Ask your doctor if you have any questions.

If you have a kidney or liver transplant, you may need to take this medication for the rest of your life to prevent rejection of the organ. Do not change your dose or stop taking this medication without first checking with your doctor.

Take this medication the same way every day. This means take it at the same time, consistently, either with or without food.

Swallow the regular tablet whole with a glass of water. Do not crush, break or chew the tablet. If you accidentally break or crush the tablet, wash your hands with water immediately.

Do not swallow the tablet for suspension. It must be dissolved in water before you take the medication. If you are preparing the oral suspension for another person, wear disposable gloves.

To dissolve the tablet in a small glass:

Measure 25ml of water into a small glass and put the tablet in the water without breaking or crushing it. Wait 3 minutes, then stir the mixture to break up the tablets. Drink the mixture immediately. After you drink the mixture, rinse the glass with another 25mL of water and drink the liquid.

To dissolve the tablet in an oral syringe:

  • Use a syringe that measures 10ml. Pull out the plunger and put the tablet in the barrel of the syringe. Replace the plunger and push it in until it touches the tablet.
  • Fill a small glass with 30ml (2 tbsp) of water. Place the syringe tip into the water and draw up enough water to cover the tablet and fill half of the syringe.
  • Hold the syringe with the tip up and draw in 4mL of air.
  • Place the syringe in an empty glass with the tip up and wait 3 minutes.
  • Turn the syringe up and push the plunger until most of the air is removed. Slowly turn the syringe up and down 5 times, but do not shake.
  • Hold the syringe with the tip up and push the plunger to remove most of the air.
  • Place the syringe in the mouth and slowly give the dose.
  • Fill the syringe with 5mL of water from a small glass.
  • Hold the tip up and add 4mL of air.
  • Swirl the water in the syringe to rinse any extra medication from the sides.
  • Hold the syringe with the tip up and push the plunger to remove most of the air.
  • Place the syringe in the mouth and slowly give the liquid.
  • Use a new syringe for each dose.

Do not use the regular tablet and the tablet for suspension together. Only use one form of this medication.

Do not eat grapefruit or drink grapefruit juice while taking this medication. Grapefruit and grapefruit juice may cause higher levels of Everolimus in the body, which may result in more unwanted effects.

If you have a kidney transplant, Everolimus will be given with another medication called Cyclosporine. These two medications should be taken at the same time.

If you have a liver transplant, Everolimus will be given with another medication called Tacrolimus. These two medications should be taken at the same time. Everolimus should not be started until at least 30 days after your liver transplant.

Dosing

Different patients will be given a different dose of this medication based on the strength of the medication. The number of doses you take each day, the time between doses and the length of time you take this medication depends on the reason you are taking this medication.

The following information only includes the average dose of this medication. If your dose is different, do not change it without first speaking to your doctor.

For tablet dosage forms:

  • For advanced breast cancer:
    • Adults - 10 mg once a day. Your doctor may adjust the dose as needed
    • Children - Use and dose must be determined by your doctor
  • For advanced kidney cancer:
    • Adults - 10 mg once a day. Your doctor may adjust the dose as needed
    • Children - Use and dose must be determined by your doctor
  • For advanced pancreatic neuroendocrine tumors (PNET):
    • Adults - 10mg once a day. Your doctor may adjust the dose as needed
    • Children - Use and dose must be determined by your doctor
  • For angiomyolipomas (kidney tumors):
    • Adults - 10mg once a day. Your doctor may adjust the dose as needed
    • Children - Use and dose must be determined by your doctor
  • For brain tumors (SEGA):
    • Adults and children 1 year of age or older - Dose is based on body size and must be determined by your doctor. Start at 4.5 mg per square meter (mg/m(2)) of body size once a day. Your doctor may adjust your dose as needed.
    • Children younger than 1 year of age - Use is not recommended
  • For kidney transplant rejection:
    • Adults - Start at 0.75 mg twice a day, taken 12 hours apart. Your doctor may adjust the dose as needed.
    • Children - Use and dose must be determined by your doctor

For tablets for suspension:

  • For brain tumors (SEGA):
    • Adults and children 1 year of age or older - Dose is based on body size and must be determined by your doctor. Start at 4.5 mg per square meter (mg/m(2)) of body size once a day. Your doctor may adjust your dose as needed.
    • Children younger than 1 year of age - Use is not recommended

Missed Dose

If you miss a dose of this medication, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and resume your normal dosing schedule. Do not double dose.

If you miss a dose of Afinitor or Afinitor Disperz, you may still take it up to 6 hours after the time you normally take the dose. If more than 6 hours have passed, skip the missed dose and resume your normal dosing schedule.

Storage

Store this medication in a closed container at room temperature. Keep it away form heat, moisture and direct light. Do not freeze.

Keep out of the reach of children. Keep in the original package until you are ready to use it. The oral suspension must be used within 60 minutes after mixing. If it is not used within this time frame, throw it away and prepare another dose.

Do not keep expired medication or medication you no longer need. Ask your doctor how to dispose of any medication you do not use.

4 Precautions To Take

It is very important that your doctor checks in with you often while you are receiving Afinitor to make sure that it is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medication while pregnant may harm your unborn child. Use an effective form of birth control while you use this medication and for at least 8 weeks after stopping treatment. If you think you have become pregnant while on this medication, inform your doctor immediately.

If you plan to have children, talk with your doctor before starting this medication. This medication may decrease fertility in men and women.

This medication may cause a serious lung problem called noninfectious pneumonitis. Inform your doctor immediately if you have chest pain, chills, cough, fever, shortness of breath or difficulty breathing.

Inform your doctor immediately if you have more than one of these symptoms while using this medication:

Agitation, confusion, decreased urination, dizziness, headache, irritability, muscle twitching, nausea, rapid weight gain, swelling in the face, ankles or hands, or unusual fatigue or weakness. These may be symptoms of a serious kidney problem.

While being treated with this medication, and after you stop treatment, do not have any vaccinations without your doctor’s approval. Everolimus may lower your body’s resistance and the vaccine may not work as well, or you may get the infection the vaccine is meant to prevent.

You should not be around other people living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza, polio virus, rotavirus and rubella. Do not get close to them and do not stay in the same room with them for very long. Ask your doctor about any questions.

This medication may temporarily lower the number of WBCs in your blood, which increases your risk of infection. It can also lower the number of platelets, which are necessary for proper blood clotting.

If this occurs, there are precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

  • Avoid people with infections, if you are able to. Tell your doctor immediately if you think you are getting an infection, or if you get a fever or chills, cough or hoarseness, lower back or side pain, or difficult or painful urination.
  • Tell your doctor immediately if you notice unusual bleeding or bruising, black stool, blood in the urine or stool, or red spots on the skin.
  • Be careful when using a toothbrush, dental floss or toothpick. Your doctor or dentist can recommend other ways to clean your teeth or gums. Talk with your doctor before having any dental work done.
  • Do not touch your eyes or the inside of your nose unless you have washed your hands and have not touched anything else in the meantime.
  • Take care not to cut yourself when using sharp objects, such as a razor, knife or nail clippers.
  • Avoid contact sports or situations where injury and bruising could occur.

This medication may increase your risk of getting skin cancer.

When you begin taking this medication:

  • Stay out of direct sunlight, especially between the hours of 10 AM and 3 PM, if you are able.
  • Wear protective clothing, including hat and sunglasses.
  • Apply a sunscreen product that has a high SPF of 15 or more.
  • Apply sunscreen lipstick that has an SPF of 15 or more.
  • Do not use sunlamps, tanning beds or tanning booths.

Zortress may cause a serious allergic reaction called angioedema. This may occur more often when used with certain heart and blood pressure medications called ACE inhibitors (Ex. captopril, enalapril, fosinopril, quinapril, ramipril). Tell your doctor immediately if you have a rash, itching, large hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or genital area, difficulty breathing or chest tightness while using this medication.

If you have a kidney transplant, this medication may increase your risk for blood clots in the new kidney. This usually occurs within the first 30 days after the transplant. Tell your doctor immediately if you have reduced urination, pain in your groin, lower back, side or stomach, dark-colored urine, nausea or vomiting.

This medication may prevent you from healing properly after an injury. Call your doctor immediately if you have any of these symptoms: blood, fluid, or pus in your incision, your incision opens and it is red, warm, painful or swollen.

If you are taking this medication after a kidney transplant, it may increase your risk of developing rare and serious viral infections such as polyoma virus-associated nephropathy (PVAN), progressive multiple leukoencephalopathy (PML) and BK virus-associated nephropathy (BKVAN). The BK virus may affect how your kidneys work and cause a transplanted kidney to fail.

Tell your doctor immediately if you experience more than one of these symptoms: blood in the urine, decreased urination, increased thirst (polydipsia), loss of appetite, lower back or side pain, nausea, swelling of the face, fingers or lower legs, difficulty breathing, unusual fatigue or weakness, vomiting or weight gain.

Everolimus may cause mouth ulcers and sores in some patients. Tell your doctor immediately if you have pain, discomfort or open sores in your mouth while using this medication. Your doctor may give you a special mouthwash or oral gel to treat the ulcers.

This medication may affect your blood sugar levels. Tell your doctor if you notice a change in your blood or urine sugar tests.

Tell your doctor if you are taking a corticosteroid or other medication that may weaken the immune system. This may increase your risk for developing a serious infection.

Do not take other prescription or over-the-counter medications without asking your doctor.

5 Potential Side Effects

Afinitor may produce unwanted affects along with the intended effects. Although not all of these side-effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if you experience any of the following side-effects:

More Common

  • Bloating or swelling in the face, arms, hands, lower legs, or feet
  • Bloody nose
  • Chest pain or tightness
  • Cough or hoarseness
  • Diarrhea
  • Difficult or labored breathing
  • Difficulty swallowing
  • Fever or chills
  • General feeling of discomfort or illness (malaise)
  • Lower back or side pain
  • Painful or difficult urination
  • Rapid weight gain
  • Sores, ulcers, or white spots on the lips, tongue, or inside the mouth
  • Tingling of the hands or feet
  • Weight loss

Less Common

  • Bleeding gums
  • Bloody urine
  • Blurred vision
  • Burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
  • Coughing up blood
  • Extreme fatigue
  • Fast, pounding, or irregular heartbeat or pulse (tachycardia, palpitations)
  • Increased thirst or urination (polydipsia, polyuria)
  • Irregular breathing
  • Loss of appetite
  • Nausea or vomiting
  • Nervousness
  • Nosebleeds
  • Prolonged bleeding from cuts
  • Red or black stool
  • Red or dark brown urine
  • Slow heartbeat (bradycardia)
  • Stomachache
  • Sweating
  • Unusual fatigue or weakness

Some side effects that may occur do not normally need medical attention. These may leave as your body becomes accustomed to treatment. Ask your doctor about ways to prevent or reduce some of these side effects.

Talk to your doctor if any of the following side effects continue or are bothersome, or if you have questions:

More Common

  • Abdominal or stomach pain
  • Change in taste
  • Dry skin
  • Itching skin
  • Lack or loss of strength
  • Loss of taste
  • Pain in the arms or legs
  • Rash
  • Unable to sleep (insomnia)

Less Common

  • Back pain
  • Blistering, peeling, redness, or swelling of the palms, hands, or bottoms of the feet
  • Bumps on the skin
  • Burning, dry, or itching eyes
  • Discoloration of the fingernails or toenails
  • Flushing or redness of the skin
  • Full feeling
  • Jaw pain
  • Numbness, pain, tingling, or unusual sensations in the palms of the hands or bottoms of the feet
  • Passing gas
  • Redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid
  • Sleepiness or unusual drowsiness

Some patients may experience other side effects that are not listed. Check with your doctor if you notice any other side effects.

Ask your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

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