Everolimus (oral)

An immunosuppressant, Everolimus is a mTOR inhibitor prescribed to lower the body's immune resistance.

Overview

Everolimus is a mTOR inhibitor which is used as an immunosuppressant for patients with recently transplanted organs and an antineoplastic for patients with certain tumors. It is available as a tablet for oral administration or a tablet for oral suspension.

In patients with recent kidney or liver transplants, Everolimus is prescribed to lower the body's immune resistance. In organ transplant patients, the body may try to reject the new organ and send white blood cells to attack it. Everolimus stops the body's white blood cells from attacking the new organ, which also reduces the body's natural immune defenses.

In patients with advanced or late-stage cancers or noncancerous tumors, Everolimus works by preventing cancer cells from growing. Everolimus also affects the normal cells of the body, which is why it is only prescribed to patients who have not had satisfactory responses to other medications or who are not able to undergo surgery.

Conditions Treated

  • Kidney cancer
  • Breast cancer
  • Renal angiomyolipoma or kidney tumors
  • Subependymal giant cell astrocytoma or SEGA brain tumors
  • Neuroendocrine pancreatic tumors
  • Neuroendocrine lung tumors
  • Neuroendocrine intestinal tumors
  • Tuberous sclerosis complex

Type Of Medicine

  • Immunosuppressant
  • MTOR inhibitor
  • Antineoplastic

Side Effects

Mild Side Effects

Some patients who take Everolimus may experience some mild side effects that do not normally require medical treatment. These side effects are a result of your body adjusting to the new medication, and usually subside or go away during the course of treatment. If these side effects persist, worsen, or become bothersome, tell your doctor. Your doctor may be able to suggest some courses of treatment or ways to help you reduce the side effects.

Some patients who take Everolimus may experience gastrointestinal side effects such as:

  • Pain in the abdomen or in the stomach area
  • A full or bloated feeling
  • Excessive gas or increased flatulence
  • A change in the sensation of taste or a loss of taste

Some patients who take Everolimus may experience dermatological side effects such as:

  • Dry skin
  • Skin that itches
  • A rash on the skin
  • Bumps on the skin
  • Redness or flushing of the skin
  • Discoloration or unusual coloring on or around the fingernails or toenails
  • Redness, swelling, peeling skin, or blistering on the hands and palms or the soles of the feet
  • Tingling, numbness, pain, or other unusual sensations on the soles of the feet or the palms of the hands

Some patients who take Everolimus may experience muscular side effects such as:

  • Pain in the back
  • Pain in the legs or arms
  • Pain in the jaw
  • A loss of strength or lack of strength

Some patients who take Everolimus may experience side effects that disrupt sleep such as:

  • Insomnia or an inability to sleep
  • Unusual drowsiness or sleepiness
  • Eyes that itch, burn, or are dry
  • Pain, swelling, or redness of the eye and area around the eye, including the eyelid

Serious Side Effects

Some patients who take Everolimus may experience more serious side effects. These side effects can be indicative of health problems that have been triggered by the Everolimus, and may require medical attention. If you experience any of these side effects while taking Everolimus, contact your doctor as soon as possible.

Some patients who take Everolimus may experience respiratory side effects such as:

  • Pain in the chest
  • Tightness in the chest
  • Hoarseness or a cough
  • Breathing that is labored or difficult
  • Difficulty when swallowing

Some patients who take Everolimus may experience gastrointestinal side effects such as:

  • Diarrhea
  • A decrease in body weight
  • Rapid or sudden weight gain
  • A loss of appetite
  • Nausea
  • Vomiting
  • Pain in the stomach or unusual stomach aches

Some patients who take Everolimus may experience side effects that involve unusual bleeding such as:

  • Bloody noses or bleeding of the nose
  • Bleeding gums or blood inside the mouth
  • Coughing up of blood or vomiting blood
  • Blood in the urine
  • Urine that is red or dark brown
  • Blood in the stool
  • Stools that are red or black and have a tarry consistency
  • Prolonged bleeding from cuts

Some patients who take Everolimus may experience eliminatory side effects such as:

  • Urination that is difficult or painful
  • Increased urination or increased thirst
  • Bloody urine or blood in the urine
  • Urine that is red or dark brown
  • Stools that include blood
  • Stools that are red or black and have a tarry look
  • Pain in the lower back or side

Some patients who take Everolimus may experience neurological side effects such as:

  • Blurred vision
  • Nervousness
  • Unusual weakness or tiredness
  • Dizziness
  • Confusion
  • Ongoing lethargy
  • Irritability, hostility, or a feeling of agitation
  • Depression
  • Seizures
  • Twitches in the muscle
  • Stupor
  • Extreme fatigue
  • Tingling in the feet or the hands
  • A feeling of tingling, itching, numbness, prickling, crawling, burning, pins and needles, or other strange feeling
  • A general feeling of illness or discomfort

Some patients who take Everolimus may experience other side effects such as:

  • Sores, white spots, or ulcers inside the mouth, on the tongue, or on the lips
  • Swelling or bloating of the face or extremities such as the hands, arms, feet, or lower legs
  • A fever or chills
  • Irregular breathing
  • A fast, slow, pounding, or otherwise irregular pulse or heartbeat
  • Unusual sweating

Dosage

The dosage and schedule for Everolimus provided here are standard measures based on guidelines by the manufacturer. The dose and scheduling of Everolimus prescribed to you will be different depending on the condition it is meant to treat. Your doctor may order you to take a different dosage or use Everolimus on a different schedule than indicated here. Always follow your doctor's directions first. Do not take more of this medicine than your doctor has prescribed for you, do not take this medicine more frequently than your doctor has prescribed for you, and do not take this medicine for longer than your doctor has told you to. Do not stop taking this medicine or change your dose of Everolimus without checking with your doctor first. Before you start taking Everolimus, read the patient information leaflet that comes with the medication. Consult your doctor with any questions about the patient information leaflet or how to take the medicine.

The standard dose of Everolimus for adults with different medical conditions is as follows:

  • Patients taking Everolimus for advanced breast cancer, advanced kidney cancer, advanced neuroendocrine tumors, or angiomyolipomas (a benign tumor of the kidney) should take 10 milligrams of Everolimus per day. This dose will be given in a tablet form.
  • Patients taking Everolimus to prevent rejection of a kidney transplant will begin taking 0.75 milligrams of Everolimus twice per day, 12 hours apart. This dose may be adjusted.
  • Patients taking Everolimus to prevent rejection of a liver transplant will begin taking 1 milligram of Everolimus twice per day, 12 hours apart. This dose may be adjusted.
  • Patients taking Everolimus for a subependymal giant cell astrocytoma or SEGA brain tumor will take a dose that is based on their body size. The base calculation for this dosage is 4.5 milligrams of Everolimus per square meter of body size, to be taken once per day. This dose may be adjusted. This dose may be given in a tablet form or in a tablet used in a suspension.

Everolimus may be taken with or without food. Patients who take the medication with food should take it with food every time it is taken, and patients who take the medication without food should take it without food every time it is taken. Everolimus should be taken at the same time each day. If you need to change the time you take Everolimus or change the way you take Everolimus, contact your doctor.

Everolimus may be given in an oral tablet for swallowing, or a tablet for oral suspension - only one one of these at a time. If you take a regular tablet of Everolimus, you will need to swallow the tablet whole with a full glass of water. Do not break, chew, or crush the tablet. If you touch a tablet that has been broken or crushed, wash your hands immediately.

If you have been prescribed a suspension of Everolimus, you will receive a tablet that is meant to be dissolved in water. Do not swallow this tablet whole. If people other than the patient taking Everolimus touch or prepare the oral tablet, they will need to wear disposable gloves to avoid coming into direct contact with the Everolimus. Everolimus tablets for oral suspension may be dissolved in a glass or an oral syringe.

In order to dissolve the oral tablet in a glass, measure 25 milliliters of water into a glass. Place a whole tablet of Everolimus into the glass. After 3 minutes have passed, give the water and Everolimus a gentle stir. Drink the suspension as soon as the tablet is dissolved. After you have ingested the suspension, pour the same amount of water into the glass and drink the liquid in order to ingest the residue.

If you are using an oral syringe for the Everolimus, you will need a syringe that is able to measure 10 milliliters. Use a fresh syringe for each dose. Remove the plunger and place the tablet in the syringe's barrel, then put the plunger back and push it down until it is touching the tablet. Fill a cup with 30 milliliters of water, and use the syringe tip to suck enough water into the syringe to fill it halfway. With the tip facing up, draw in 4 milliliters of air. Put the syringe in an empty cup, tip still facing up. After 3 minutes of time, turn the syringe up and down gently 5 times. With the tip facing up, push the plunger until most of the air has been removed. The suspension may now be administered by mouth. Draw 5 milliliters of water into the syringe, followed by 4 milliliters of air with the tip up. Gently swirl the liquid around the sides of the syringe, push out the air with the tip up, and then administer the rest of the liquid.

Interactions

Drug interactions can increase your risk of side effects or change the way a drug works in your body. Keep a list of all the drugs, medications, and supplements you take regularly, whether they have been prescribed to you by a doctor or other medical professional or whether you are taking them over the counter. Your doctor, pharmacist, or other medical professional will be able to identify potentially harmful interactions.

Everolimus may weaken the immune system and increase your risk of infection. This may be dangerous when taken with other drugs that weaken the immune system, such as:

  • Rituximab
  • Natalizumab
  • ACE inhibitors i.e. captopril or lisinopril

Some medications may change the way Everolimus is removed from your body, which can have negative effects on the way the medication works or increase your risk of side effects. These medications include:

  • Cobicistat
  • Nefazodone
  • Telithromycin
  • St. John's Wort
  • Macrolide antibiotics like erythromycin or clarithromycin
  • Azole antifungals like ketoconazole or itraconazole
  • HIV and HCV protease inhibitors like ritonavir, indinavir, or atazanavir

Some patients may take Everolimus for organ transplants. Patients with kidney transplants may take Everolimus with cyclosporine, and patients with liver transplants may take Everolimus with tacrolimus. If you are taking Everolimus for an organ transplant and are prescribed either of these drugs, take them at the same time to ensure efficiency.

Warnings

Progress Checks

Patients taking Everolimus will need to keep regular appointments with their doctor while taking Everolimus. Your doctor can examine you to make sure that the medication is working correctly and your condition is progressing as it should. You may also need blood tests and urine tests in order to screen for unwanted side effects before more physical symptoms occur.

Medical History

Before starting to take Everolimus, tell your prescribing doctor or your pharmacist your medical history to ensure that it is safe for you to take Everolimus. Conditions that may require special treatment or attention when taking Everolimus include:

  • Any liver problems or liver disease
  • A history of diabetes, whether it is under control or not
  • High triglyceride levels
  • High cholesterol levels
  • Any current, recent, or recurrent infections you have or have had

Dizziness

Everolimus may cause dizziness in some patients. When you begin to take Everolimus, do not drive a car, use heavy machinery, or perform any activity that requires coordination or alertness until you know how you react to the Everolimus. If the dizziness from Everolimus becomes bothersome or prevents you from performing necessary activities, contact your doctor. While taking Everolimus, limit the use of alcohol or other substances that may contribute to dizziness or drowsiness.

Pregnancy

Everolimus may decrease fertility. Patients who are planning to have children should discuss the possibility with their doctor before beginning an Everolimus regimen. Inform your doctor if you are pregnant or intend to become pregnant or conceive children while using Everolimus.

Using Everolimus while pregnant may cause harm to the fetus. Because of the risk of fetal harm, patients who are using Everolimus should not attempt to become pregnant or conceive children while using the drug. Sexually active patients should make sure they are using an effective form of birth control while taking Everolimus and for a minimum of eight weeks after stopping the Everolimus regimen. If you become pregnant or think you have become pregnant while taking Everolimus, inform your doctor as soon as possible.

Everolimus can be absorbed into the bloodstream through the lungs and the skin. This should not cause unwanted effects in adults who handle the substance. However, people who are pregnant or who may become pregnant should not handle Everolimus tablets or be exposed to the dust from the tablets, as exposure to Everolimus can harm a fetus. If you are pregnant or think you may become pregnant and are exposed to Everolimus, contact your doctor for assistance.

Everolimus may pass into breast milk in a nursing parent who is taking the drug. This may harm the infant who ingests the Everolimus in the breast milk. Patients who take Everolimus should not breast-feed infants while using this medication, and should not breast-feed infants for at least 2 weeks after stopping the use of Everolimus. Consult your doctor for further guidance regarding breastfeeding while using Everolimus.

Noninfectious Pneumonitis

Some patients using Everolimus may contact noninfectious pneumonitis, which is a serious lung condition that needs medical attention. Contact your doctor immediately if you experience any of the following symptoms of noninfectious pneumonitis while using Everolimus:

  • Chills
  • A fever
  • Shortness of breath
  • A cough or a persistent cough
  • Difficulty breathing
  • Chest pain

Kidney Problems

Some patients using Everolimus may experience a malfunction of the kidneys. Check with your doctor immediately if you experience any of the symptoms of a serious kidney problem such as:

  • Unusual tiredness or weakness
  • Confusion
  • Dizziness
  • Irritability
  • Agitation
  • A decreased amount of urine produced
  • Headaches
  • Nausea
  • Twitching of the muscles
  • Swelling of the face, hands, or ankles
  • Rapid weight gain

Kidney Transplants

Patients who have kidney transplants are at a heightened risk for complications when taking Everolimus. If you have recently had a kidney transplant, consult your doctor about precautions you can take to reduce the risk of these complications.

Patients with recent kidney transplants who have received their kidneys in the last 30 days have an increased risk of experiencing a blood clot in the new kidney. If you are taking Everolimus in the month after you have received a new kidney, call your doctor immediately if you experience symptoms such as:

  • A decreased amount of urine or decreased frequency in urinating
  • Urine that is unusually dark
  • Pain in your lower back, side, stomach, or groin
  • Nausea
  • Vomiting
  • A fever or chills

Taking Everolimus after receiving a transplanted kidney can increase your risk for developing certain viral infections which can be serious and even fatal. Viral infections you may be more susceptible to while taking Everolimus include polyoma virus-associated nephropathy or PVAN, BK virus-associated nephropathy or BKVAN, and progressive multiple leukoencephalopathy or PML. These viruses attack your kidneys and change the way they work, which may cause the failure of a transplanted kidney. Contact your doctor immediately if you experience any of the symptoms of these viral infections, such as:

  • A loss of appetite
  • Nausea
  • Vomiting
  • Weight gain
  • Increased thirst
  • A decrease in amount of urine produced or frequency of urination
  • Bloody urine
  • Pain in the lower back or the side
  • Unusual weakness or tiredness
  • Difficulty in breathing
  • Swelling in the face, the fingers, or the lower legs

Risk of Infections and Bleeding

In some patients, Everolimus may temporarily decrease the number of white blood cells present in your bloodstream. Everolimus may also temporarily decrease the number of platelets present in your bloodstream. The lack of white blood cells and platelets may lower your body's resistance to infection and prevent your blood from clotting properly as usual. Patients may need regular blood tests to determine the number of white blood cells and platelets present in the bloodstream.

There are precautions you can take while using Everolimus to reduce the incidence of uncontrolled bleeding or infection. Remember to:

  • Avoid people who have infections or illnesses, and contact your doctor if you think you may be getting sick. Signs of an infection include painful or difficult urination, pain in the lower back or side, a fever or chills, and a cough or hoarseness. If you experience these symptoms, check with your doctor as soon as possible.
  • Watch out for signs of unusual or excess bleeding. You may notice blood in your urine, stools that are black and tarry or have blood in them, unusual bleeding or bruising on the body, or red spots on your skin that look like pinpoints. If you experience any of these symptoms, check with your doctor immediately.
  • Reduce the potential of injury when grooming. Be cautious when you are using nail clippers, a razor, or any other sharp grooming or hygiene implements. When taking care of your oral hygiene, be careful when you use a toothpick, dental floss, or a regular toothbrush. Your dentist, doctor, or nurse may be able to suggest some alternative ways to clean your mouth while you are at risk for bleeding.
  • If you are having dental work done or any other medical procedure performed, let the medical professionals in charge of the procedure know that you are taking Everolimus and at risk for bleeding. Check with your doctor before you undergo any medical or dental procedures.
  • Avoid any situations in which injury or bruising is likely to occur, such as contact sports.
  • Your mucuous membranes are particularly susceptible to infection. Wash your hands throughly before you touch the inside of your nose or your eyes, and do not touch anything else before you touch these areas. Keep your hands clean and wash frequently.
  • If you do sustain a cut or injury, keep a careful eye on the abrasion or injury site. Everolimus can prevent your body from healing properly after you sustain an injury. Contact your doctor immediately if you see pus, blood, or other fluid in your incision or injury, if an incision or cut opens up, or if the area around an incision or injury becomes warm, red, swollen, or painful.
  • Corticosteroids and other medications that weaken the immune system increase your risk for infection while you are taking Everolimus. Do not take other medications, drugs, or supplements, whether they are prescribed to you or over the counter, while taking Everolimus unless you discuss them with your doctor first and make sure it is safe for you.

Immunizations

Everolimus may lower your body's resistance to infection. Because of this tendency, patients who are using Everolimus or who have recently stopped using Everolimus will need to check with their doctor before having any vaccines or immunizations. While affected by an Everolimus regimen, patients who receive immunizations or vaccinations may have unwanted effects. This may lead to the vaccination not working as well as necessary in order to protect the patient, or to the patient actually contracting what the immunization is meant to prevent.

Patients taking Everolimus should avoid being around individuals who have recently had live virus vaccines, as the presence of a live vaccine in the body of a healthy individual may transmit it to an immunocompromized individual. If you have any questions about safe conduct around individuals who have recently had live virus vaccines, contact your doctor. Live virus vaccines include immunizations for:

Skin Cancer

Patients taking Everolimus are at an increased risk for skin cancer. There are some precautions you can take in order to reduce your risk of skin cancer while taking Everolimus. Remember to:

  • Avoid tanning booths, tanning beds, sun lamps, or other artificial sources of light that mimic the sun
  • Avoid direct sunlight if at all possible, especially between the hours of 10 AM and 3 PM
  • If you go outside during the day, wear protective clothing such as a hat, sunglasses, or long sleeves
  • If you go outside during the day, make sure to apply sunscreen or another sunblock product that is at least 15 SPF and higher if possible
  • Use a sunblock product for your lips that is at least 15 SPF or higher, such as special chapstick

Angioedema

Everolimus can cause allergic reactions in some patients. The most common allergic reaction triggered by Everolimus comes in the form of an attack of angioedema, a reaction similar to hives that produces swelling or large lumps in layers of the skin. The risk of encountering this reaction is heightened when Everolimus is taken alongside with ACE inhibitors, a type of heart and blood pressure medication that dilates the blood vessels and dilutes blood pressure.

ACE inhibitors include medications such as captopril or Capoten, enalapril or Vasotec, fosinopril or Monopril, quinapril or Accupril, and ramipril or Altace. Exercise caution when taking these medications along with Everolimus.

If you experience the symptoms of angioedema when taking Everolimus, get help and contact your doctor immediately. You may need medical assistance. Symptoms of angioedema include:

  • A rash on the skin
  • Itching on the skin
  • Difficulty breathing
  • Tightness in the chest
  • Large and hive-like swellings on the face, eyelids, tongue, and throat, or on the extremities such as hands, legs, and feet, or the genital organs

Mouth Sores

Some patients taking Everolimus may develop sores or ulcers in the mouth. If you develop sores or ulcers in the mouth or experience pain or discomfort because of open mouth sores while taking Everolimus, contact your doctor right away. You may need to use a special mouth gel, mouthwash, or other medicated dental formulas to treat your sores and prevent more ulcers from forming in your mouth. Ask your doctor for recommendations for products that are safe or suitable to use for mouth sores while taking Everolimus.

Blood Sugar Levels in Diabetics

Everolimus can affect blood sugar levels in some patients. Patients with diabetes are particularly susceptible to these side effects. If you have diabetes and are taking Everolimus, make sure to monitor your blood sugar or urine sugar tests very closely. Tell your doctor immediately if you notice a change in these tests while taking Everolimus.

Storage

Everolimus comes in a blister pack. Keep your Everolimus in the blister pack for best storage, and keep the container tightly closed. Everolimus should be kept at room temperature and not exposed to direct light, moisture, or excess heat. Do not store Everolimus in the bathroom in order to avoid degradation of the medication. Keep your medication away from children and pets.

Do not keep medication that you no longer need. Do not keep medication that is past its expiration date. If you need to dispose of Everolimus that is past its expiration date or that you are no longer taking, do not dispose of it in the trash or toilet. Ask your doctor or pharmacist about safe ways to dispose of Everolimus. Your pharmacy or other medical facility may have a safe disposal program.

Summary

Everolimus is prescribed to prevent organ rejection to patients who have recently had kidney or liver transplants. It works by suppressing the body's natural immune system, ensuring that the body's white blood cells do not attack the new organ.

Everolimus is also prescribed to patients who have had certain cancers or noncancerous tumors in cases where other medicines did not work and surgery will not be performed. It suppresses the growth of cancerous cells and gives the body a chance to destroy the cancer, but also can have negative effects on normal cells.

Everolimus is taken as an oral tablet or a tablet for suspension. Patients taking Everolimus for cancer of the breast or kidney, a benign kidney tumor, or neuroendocrine tumors will take 10 mg of Everolimus per day as a tablet. Patients taking Everolimus for a SEGA brain tumor will take 4.5 mg of Everolimus per day per square meter of body size, and may take this in tablet form or suspension form. Patients taking Everolimus for kidney transplants will begin by taking 0.75 mg of Everolimus twice per day, 12 hours apart. Patients taking Everolimus for liver transplants will begin by taking 1 mg of Everolimus twice per day, 12 hours apart.

Everolimus can cause mild side effects that do not usually need medical attention. These side effects include a bloated or painful feeling in the abdomen or stomach, flatulence, a change in the sensation of taste, dry or itchy skin, discolored or red skin, tingling or numbness on the soles and palms, rashes, pain in the back, jaw, legs, or arms, a feeling of weakness, insomnia or drowsiness, and painful or itchy eyes.

Everolimus can cause more serious side effects that may be symptoms of a serious health problem and may need medical attention. Check with your doctor if you experience pain or tightness in the chest, labored or difficult breathing or a cough, diarrhea, nausea, vomiting, a loss of appetite, sudden weight loss or gain, unusual bleeding, blood in the stool or urine, vomiting up blood, difficult urination or increased urination, blurred vision, mood changes, seizures, fatigue, sores or white spots in the mouth, swelling or bloating of the extremities, an irregular pulse, or unusual sweating.

Everolimus can be ingested through the skin. Individuals who handle Everolimus and are not taking it for medical reasons should wear disposable gloves.

Everolimus can increase your risk of bleeding and reduce your immune response. Patients taking Everolimus should be careful to avoid injury or cuts, even small ones. Patients taking Everolimus should not receive live immunizations, be around people who have recently had live immunizations, or be around people who have infections.

Everolimus can increase your risk of skin cancer. Take precautions to avoid the sun while taking Everolimus.

Everolimus can affect blood sugar levels in diabetics. If you are diabetic and taking Everolimus, tell your doctor if you see any change in your blood sugar or urine sugar levels.