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everolimus

Pronunciation

Generic Name: everolimus (Zortress) (E ver OH li mus (ZOR tress))
Brand Name: Zortress

What is everolimus (Zortress)?

Everolimus lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader.

The Zortress brand of everolimus is used to prevent organ rejection after a kidney or liver transplant. Zortress is used together with cyclosporine, steroids, and other medications.

This medication guide provides information about the Zortress brand of everolimus. Afinitor is another brand of everolimus used to treat certain types of cancer.

Everolimus may also be used for purposes not listed in this medication guide.

What is the most important information I should know about Zortress?

Zortress may increase your risk of infection or certain cancer by changing the way your immune system works.

Serious and sometimes fatal infections may occur during treatment with Zortress. Stop using this medicine and call your doctor right away if you have signs of infection such as: fever, chills, body aches, or flu symptoms.

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Zortress can cause a blood clot in the blood vessels of your transplanted organ, especially within 30 days after transplant. Tell your doctor right away if you have: shortness of breath, fever with nausea or vomiting, blood in your urine, dark colored urine, little or no urinating, jaundice (yellowing of your skin or eyes), or pain in your stomach, groin, lower back, or side.

What should I discuss with my health care provider before taking Zortress?

You should not use this medication if you are allergic to everolimus or sirolimus (Rapamune), or if you have problems digesting lactose or galactose (sugar).

Zortress can lower blood cells that help fight infection, and may cause you to produce too much of a certain type of white blood cell. This can lead to serious conditions including cancer, severe brain infection causing disability or death, or a viral infection causing kidney transplant failure. Ask your doctor about your specific risk.

To make sure you can safely take everolimus, tell your doctor if you have any of these other conditions:

  • high cholesterol or triglycerides;

  • diabetes or high blood sugar;

  • a breathing disorder, such as asthma or COPD (chronic obstructive pulmonary disease);

  • a personal or family history of skin cancer (melanoma); or

  • if you have ever had a heart transplant.

FDA pregnancy category C. It is not known whether Zortress will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. Use effective birth control while you are using this medication and for at least 8 weeks after your treatment ends.

Zortress can lower sperm count in men, which may affect fertility (your ability to have children).

It is not known whether everolimus passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are taking Zortress.

How should I take Zortress?

Zortress is usually taken twice daily (every 12 hours). Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.

You may take the medicine with or without food, but take it the same way each time. If you also take cyclosporine or tacrolimus, take both medications at the same time.

Do not stop taking Zortress or change your dose without first talking to your doctor.

Take this medication with a full glass (8 ounces) of water.

Do not crush or chew an everolimus tablet. Swallow the pill whole.

While using Zortress, you will need frequent blood and urine tests at your doctor's office.

Store at room temperature in the original container, away from moisture, heat, and light. Keep each tablet in its blister pack until you are ready to take it.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking Zortress?

This medicine can pass into body fluids (including urine, feces, vomit, semen, vaginal fluid). For at least 48 hours after you receive a dose, avoid allowing your body fluids to come into contact with your hands or other surfaces. Patients and caregivers should wear rubber gloves while cleaning up body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

Body fluids should not be handled by a woman who is pregnant or who may become pregnant. Use condoms during sexual activity to avoid exposure to body fluids.

Do not receive a "live" vaccine while using Zortress, or you could develop a serious infection. Live vaccines include measles, mumps, rubella (MMR), rotavirus, typhoid, yellow fever, varicella (chickenpox), zoster (shingles), and nasal flu (influenza) vaccine.

Zortress may increase your risk of developing skin cancer. Avoid exposure to sunlight or tanning beds. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.

Grapefruit and grapefruit juice may interact with Zortress and lead to unwanted side effects. Avoid the use of grapefruit products while taking Zortress.

Zortress side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; chest pain, difficult breathing; swelling of your face, lips, tongue, or throat.

Serious and sometimes fatal infections may occur during treatment with Zortress. Stop using this medicine and call your doctor right away if you have signs of infection such as: fever, chills, body aches, or flu symptoms.

Zortress can cause a blood clot in the blood vessels of your transplanted organ, especially within 30 days after transplant. Tell your doctor right away if you have: shortness of breath, fever with nausea or vomiting, blood in your urine, dark colored urine, little or no urinating, jaundice (yellowing of your skin or eyes), or pain in your stomach, groin, lower back, or side.

Call your doctor at once if you have:

  • pain or burning when you urinate;

  • redness, warmth, swelling, oozing, or slow healing of a wound or surgical incision;

  • new or worsening cough, wheezing, breathing problems;

  • stabbing chest pain, cough with yellow or green mucus;

  • pale skin, feeling light-headed, rapid heart rate, easy bruising, unusual bleeding (nose, mouth, vagina, or rectum);

  • white patches or sores inside your mouth or on your lips;

  • high potassium (slow heart rate, weak pulse, muscle weakness, tingly feeling);

  • high blood sugar (increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss); or

  • dangerously high blood pressure (severe headache, blurred vision, buzzing in your ears, anxiety, confusion, uneven heartbeats, seizure).

Common side effects may include:

  • swelling in your legs, ankles, or feet;

  • diarrhea, constipation; or

  • mild stomach discomfort.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

Everolimus Dosing Information

Usual Adult Dose for Organ Transplant -- Rejection Prophylaxis:

Kidney Transplant (Zortress):

Initial dose: 0.75 mg orally twice daily in combination with reduced dose cyclosporine, administered as soon as possible after transplantation.

Maintenance dose: Adjust maintenance dose to achieve trough concentrations within the 3 to 8 ng/mL target range.

Comments: Dose adjustments may be required based on everolimus blood levels, tolerability, individual response, change in concomitant medications and the clinical situation. Dose adjustments can be made at 4 to 5 day intervals. Administer consistently with or without food at the same time as cyclosporine.

Oral prednisone should be initiated once oral medication is tolerated. Steroid doses may be further tapered on an individualized basis depending on the clinical status of patient and function of graft.

Both cyclosporine doses and the cyclosporine target range for whole blood trough concentrations should be reduced, when given with everolimus, in order to minimize the risk of nephrotoxicity.

The recommended cyclosporine therapeutic ranges when administered with everolimus are 100 to 200 ng/mL through Month 1 post-transplant, 75 to 150 ng/mL at Months 2 and 3, 50 to 100 ng/mL at Month 4, and 25 to 50 ng/mL from Month 6 through Month 12 post-transplant. In renal transplantation, there are limited data regarding dosing everolimus with reduced cyclosporine trough concentrations of 25 to 50 ng/mL after 12 months.

Cyclosporine, USP Modified is to be administered as oral capsules twice daily unless cyclosporine oral solution or intravenous administration of cyclosporine cannot be avoided. Cyclosporine, USP Modified should be initiated as soon as possible - and no later than 48 hours - after reperfusion of the graft and dose adjusted to target concentrations from Day 5 onwards. Everolimus has not been evaluated in clinical trials with other formulations of cyclosporine.
If impairment of renal function is progressive the treatment regimen should be adjusted. In renal transplant patients, the cyclosporine dose should be based on cyclosporine whole blood trough concentrations.
Prior to dose reduction of cyclosporine, it should be ascertained that the everolimus whole blood trough concentration is at least 3 ng/mL. There is an interaction of cyclosporine on everolimus, and consequently, everolimus concentrations may decrease if the cyclosporine dose is reduced.

Liver Transplant (Zortress):

Initial dose: 1 mg orally twice daily in combination with reduced dose tacrolimus. Start everolimus at least 30 days post-transplant.

Maintenance dose: Adjust maintenance dose to achieve trough concentrations within the 3 to 8 ng/mL target range.

Comments: Dose adjustments may be required based on everolimus blood levels, tolerability, individual response, change in concomitant medications and the clinical situation. Dose adjustments can be made at 4 to 5 day intervals. Administer consistently with or without food at the same time as tacrolimus.

Steroid doses may be further tapered on an individualized basis depending on the clinical status of patient and function of graft.

Both tacrolimus doses and the target range for whole blood trough concentrations should be reduced, when given in a regimen with everolimus, in order to minimize the potential risk of nephrotoxicity.

The recommended tacrolimus therapeutic range when administered with everolimus are whole blood trough concentrations of 3 to 5 ng/mL by three weeks after the first dose of everolimus (approximately Month 2) and through Month 12 post transplant. In liver transplantation, there are limited data regarding dosing everolimus with reduced tacrolimus trough concentrations of 3 to 5 ng/mL after 12 months.

Tacrolimus is to be administered as oral capsules twice daily unless intravenous administration of tacrolimus cannot be avoided.

In liver transplant patients, the tacrolimus dose should be based on tacrolimus whole blood trough concentrations. Prior to dose reduction of tacrolimus it should be ascertained that the steady-state everolimus whole blood trough concentration is at least 3 ng/mL. However, tacrolimus does not affect everolimus trough concentrations, and everolimus concentrations do not decrease if the tacrolimus dose is reduced.

Usual Adult Dose for Breast Cancer:

Advanced hormone receptor positive, HER2 negative breast cancer, advanced renal cell carcinoma, advanced pancreatic neuroendocrine tumors, and renal angiomyolipoma with TSC:

Recommended dose (Afinitor): 10 mg orally once daily to be taken at the same time every day.

Treatment should be continued as long as clinical benefit is observed or until unacceptable toxicity occurs.

Usual Adult Dose for Renal Cell Carcinoma:

Advanced hormone receptor positive, HER2 negative breast cancer, advanced renal cell carcinoma, advanced pancreatic neuroendocrine tumors, and renal angiomyolipoma with TSC:

Recommended dose (Afinitor): 10 mg orally once daily to be taken at the same time every day.

Treatment should be continued as long as clinical benefit is observed or until unacceptable toxicity occurs.

Usual Adult Dose for Pancreatic Cancer:

Advanced hormone receptor positive, HER2 negative breast cancer, advanced renal cell carcinoma, advanced pancreatic neuroendocrine tumors, and renal angiomyolipoma with TSC:

Recommended dose (Afinitor): 10 mg orally once daily to be taken at the same time every day.

Treatment should be continued as long as clinical benefit is observed or until unacceptable toxicity occurs.

Usual Adult Dose for Renal Angiomyolipoma:

Advanced hormone receptor positive, HER2 negative breast cancer, advanced renal cell carcinoma, advanced pancreatic neuroendocrine tumors, and renal angiomyolipoma with TSC:

Recommended dose (Afinitor): 10 mg orally once daily to be taken at the same time every day.

Treatment should be continued as long as clinical benefit is observed or until unacceptable toxicity occurs.

Usual Adult Dose for Brain/Intracranial Tumor:

Subependymal giant cell astrocytoma (SEGA) with TSC (Afinitor):

Initial dose: 4.5 mg/m2 orally once daily

Maintenance dose: A dose adjustment may be required based on everolimus trough blood levels, tolerability, individual response, change in concomitant medications, and change in SEGA volume. Dose adjustments can be made at 2 week intervals as needed to maintain trough levels of 5 to 15 ng/ml.

Duration of therapy: Continue treatment until disease progression or unacceptable toxicity occurs. The optimal duration of therapy is unknown.

Comments: Management of severe and/or intolerable adverse reactions may require a temporary dose reduction and/or interruption of therapy.

Usual Pediatric Dose for Brain/Intracranial Tumor:

Subependymal giant cell astrocytoma (SEGA):
3 years or younger: Not recommended

3 years or older:
Initial dose (Afinitor):
Body surface area less than 0.58 m2: Not recommended

Body surface area 0.58 to 1.2 m2: 2.5 mg orally once daily

Body surface area 1.3 to 2.1 m2: 5 mg orally once daily

Body surface area 2.2 m2 or greater: 7.5 mg orally once daily

A dose adjustment may be required based on everolimus trough blood levels, tolerability, individual response, change in concomitant medications, and change in SEGA volume. Dose adjustments can be made at 2 week intervals. The optimal duration of therapy has not been determined.

Management of severe and/or intolerable adverse reactions may require a temporary dose reduction and/or interruption of therapy.

What other drugs will affect Zortress?

Many drugs can interact with Zortress. Not all possible interactions are listed here. Tell your doctor about all your medications and any you start or stop using during treatment with Zortress, especially:

  • aprepitant, conivaptan, cyclosporine, deferiprone, imatinib, natalizumab; or

  • an antibiotic--clarithromycin, dalfopristin, erythromycin, telithromycin; an antidepressant--fluvoxamine, nefazodone; antifungal medication--fluconazole, itraconazole, ketoconazole; heart or blood pressure medication--diltiazem, verapamil; HIV/AIDS medication--atazanavir, delavirdine, fosamprenavir, indinavir, nelfinavir, ritonavir, saquinavir.

This list is not complete and many other drugs can interact with Zortress. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Give a list of all your medicines to any healthcare provider who treats you.

Where can I get more information?

  • Your pharmacist can provide more information about everolimus (Zortress).
  • Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
  • Disclaimer: Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 4.03. Revision Date: 2013-07-12, 1:25:47 PM.

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