Afinitor Disperz (Everolimus) 5mg

Everolimus, Afinitor (US/CDN)/Zortress (US)
Description: Antineoplastic Agent; mTOR Kinase Inhibitor; Immunosuppressant Agent
 

“ALERT: US Boxed Warning

Immunosuppression (Zortress):
Increased susceptibility to infection and the possible development of malignancies, such as lymphoma and skin cancer, may result from immunosuppression.

Only health care providers experienced in immunosuppressive therapy and management of transplant patients should use everolimus. Manage patients receiving the drug in facilities equipped and staffed with adequate laboratory and supportive medical resources. The health care provider responsible for maintenance therapy should have complete information requisite for the follow-up.

Renal graft thrombosis (Zortress):
An increased risk of kidney arterial and venous thrombosis, resulting in graft loss, was reported, mostly within the first 30 days post-transplantation.

Nephrotoxicity (Zortress):
Increased nephrotoxicity can occur with use of standard doses of cyclosporine in combination with everolimus. Therefore, use reduced doses of cyclosporine in combination with everolimus in order to reduce renal dysfunction. It is important to monitor the cyclosporine and everolimus whole blood trough concentrations.

Mortality in heart transplant (Zortress):
Increased mortality, often associated with serious infection, within the first 3 months of post-transplantation was observed in a clinical trial of de novo heart transplant patients receiving immunosuppressive regimens with or without induction therapy. Use in heart transplantation is not recommended.”

CSA NA – FDA Approved – REMS (N) – Can Ship

Everolimus, Afinitor/Zortress Everolimus is a macrolide immunosuppressant and a mechanistic target of rapamycin (mTOR) inhibitor which has antiproliferative and antiangiogenic properties.

Breast cancer; Neuroendocrine tumors; Renal cell carcinoma; Tuberous sclerosis complex-associated renal angiomyolipoma (Afinitor only)
Tuberous sclerosis complex-associated partial-onset seizures (Afinitor Disperz only)
Tuberous sclerosis complex-associated subependymal giant cell astrocytoma (Afinitor or Afinitor Disperz only)
Liver transplantation; Renal transplantation (Zortress only)

Before starting Everolimus, Afinitor/Zortress make sure your physician is aware of any allergies or medications you currently take, if you have had a heart transplant, if you have hepatic impairment, hereditary galactose intolerance, renal impairment, a solid organ transplant (aside from liver/kidney), are pregnant, or breastfeeding. Everolimus, Afinitor/Zortress use has been associated with rare but serious adverse events such as angioedema, bone marrow suppression, edema, graft thrombosis, hepatic artery thrombosis, hypersensitivity reactions, increased risk of infection, malignancy, metabolic effects, mucositis, stomatitis, nephrotoxicity, pulmonary toxicity, and wound healing impairment.

Afinitor: Oral: 10 mg once daily until disease progression or unacceptable toxicity; Initial: 4.5 mg/m2 and adjust based on serum concentrations, tolerability, and response.
Zortress: Oral: Initial: 0.75-1 mg twice daily in combination with other agents and adjust based on serum concentrations, tolerability, and response.
Afinitor Disperz: Oral: Initial: 4.5 or 5 mg/m2 once daily until disease progression or unacceptable toxicity.

How to Take: Swallow whole with a glass of water. May be taken with or without food, but to reduce variability take consistently with regard to food. Administer at the same time(s) each day. Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and moisture. Store Afinitor and Afinitor Disperz in the original container.

You Need to Avoid:  Significant drug interactions exist, requiring dose/frequency adjustment or avoidance so avoid starting any new medications without consulting prescriber.      Avoid grapefruit and grapefruit juice.   Patients should not be immunized with live viral vaccines during or shortly after treatment and should avoid close contact with recently vaccinated (live vaccine) individuals.

Transplantation: Hypertension, peripheral edema, diabetes mellitus, hypercholesterolemia, hyperglycemia, hyperkalemia, hypokalemia, hypomagnesemia, hypophosphatemia, abdominal pain, constipation, diarrhea, nausea, vomiting, dysuria, hematuria, urinary tract infection, anemia, leukopenia, bacterial infection, hepatitis C, infection, viral infection, fatigue, headache, insomnia, back pain, limb pain, increased serum creatinine, upper respiratory tract infection, fever, wound healing impairment

Antineoplastic: Edema, hypertension, peripheral edema, acne vulgaris, nail disease, pruritus, skin rash, xeroderma, amenorrhea, decreased serum bicarbonate, decreased serum fibrinogen, hypercholesterolemia, hyperglycemia, hypertriglyceridemia, hypoalbuminemia, hypocalcemia, hypokalemia, hypophosphatemia, abdominal pain, anorexia, constipation, decreased appetite, diarrhea, dysgeusia, gastroenteritis, nausea, stomatitis, vomiting, weight loss, xerostomia, irregular menses, proteinuria, urinary tract infection, anemia, leukopenia, lymphocytopenia, neutropenia, prolonged partial thromboplastin time, prolonged prothrombin time, thrombocytopenia, increased serum alanine aminotransaminase, increased serum alkaline phosphatase, increased serum aspartate aminotransferase, infection, aggressive behavior, anxiety, behavioral problems, dizziness, fatigue, headache, insomnia, malaise, migraine, arthralgia, asthenia, back pain, limb pain, myalgia, increased serum creatinine, cough, dyspnea, epistaxis, nasopharyngitis, oropharyngeal pain, pneumonia, pneumonitis, respiratory tract infection, rhinitis , upper respiratory tract infection, fever

Note this is not a complete list of side effects, only the most common

1. What do I do if side effects are intolerable?
   If side effects are causing a lot of distress speak to your physician as soon as possible to discuss options.
2. Why would my physician prescribe a medication with such serious side effects?
   Your physician takes the most recent clinical guidelines to make evidence-based decisions on what medication is appropriate in which situations.  Your current medications, your allergies, age, cost of medication, comorbid conditions and many other factors will further complicate or limit which medications are appropriate.  This medication is used for certain forms of cancer and your physician has determined the benefits outweigh the risks.  Furthermore, they will be monitoring your bloodwork and symptoms closely to avoid many of the serious side effects and will keep you on the lowest effective dosage for the shortest amount of time possible.