Zortress 0.75mg Tablet
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Indications & Clinical Uses
- Zortress 0.75 mg (everolimus) is an mTOR-inhibitor immunosuppressant used to help prevent rejection of a transplanted organ.
- In the US it is approved for adults at low-to-moderate immunologic risk who have had a kidney transplant, used with basiliximab induction, reduced-dose cyclosporine and corticosteroids, and for adults who have had a liver transplant, started at least 30 days after the transplant together with reduced-dose tacrolimus and corticosteroids.
- It is not recommended for kidney transplant patients at high immunologic risk, for recipients of other organs, for heart transplant recipients (increased mortality was seen), or for people under 18.
- The 0.75 mg tablet is one of four strengths (0.25, 0.5, 0.75 and 1 mg).
- Zortress is a transplant medicine and must not be confused with other everolimus products used for different conditions.
- It is prescribed and monitored by transplant specialists.
Side Effects
- Boxed warning: Zortress carries a boxed warning for malignancies and serious infections, kidney graft thrombosis, nephrotoxicity (when used with standard-dose cyclosporine) and increased mortality in heart transplantation.
- In kidney transplant, the most common reactions (20% or more) were peripheral oedema (45%), constipation (38%), high blood pressure (30%), nausea (29%), anaemia (26%), urinary tract infection (22%) and high blood fats (21%).
- In liver transplant, reactions in more than 10% included diarrhoea, headache, peripheral oedema, high blood pressure, nausea, fever, abdominal pain and low white blood cell counts.
- Other serious effects include lung inflammation (pneumonitis), delayed wound healing, protein in the urine, new-onset diabetes, small-vessel clotting problems (TMA/TTP/HUS), BK and JC virus infections and angioedema.
- Report fever, signs of infection, new cough or breathlessness, swelling or passing less urine promptly.
Precautions & Warnings
- Only physicians experienced in immunosuppressive therapy and transplant care should prescribe Zortress.
- Blood levels must be monitored: the target everolimus trough is 3 to 8 ng/mL, and cyclosporine doses must be reduced and monitored to protect the kidneys; levels also need checking in liver impairment.
- Zortress is contraindicated in anyone hypersensitive to everolimus, sirolimus or any ingredient.
- Kidney function, urine protein, blood fats, blood sugar and blood counts need regular checks.
- Kidney graft thrombosis mostly occurs within the first 30 days.
- Women who could become pregnant must use effective contraception during treatment and for 8 weeks after stopping, breastfeeding is not recommended, and fertility may be reduced in women (amenorrhoea) and men (lower sperm counts).
- Avoid live vaccines.
- Follow the prescribed product and dose exactly, and do not switch to another everolimus product unless your transplant team tells you to.
Avoid Interactions
- Medicines and foods that increase everolimus levels or toxicity: cyclosporine (its dose must be reduced and levels monitored), strong CYP3A4/P-gp inhibitors such as ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, ritonavir, boceprevir and telaprevir (not recommended), moderate inhibitors such as erythromycin, verapamil and fluconazole, cannabidiol, and grapefruit or grapefruit juice (avoid).
- ACE inhibitors raise the risk of angioedema, and simvastatin or lovastatin given with cyclosporine raise the risk of muscle breakdown (rhabdomyolysis).
- Medicines that reduce efficacy: strong inducers rifampin and rifabutin (not recommended), and moderate inducers carbamazepine, phenobarbital, phenytoin and St John's wort.
- Avoid live vaccines such as intranasal influenza, MMR, polio, BCG, yellow fever, varicella and typhoid.
- Tacrolimus has minimal interaction.
- Tell your transplant team about all medicines and supplements.
References
Frequently Asked Questions
Zortress (everolimus) helps prevent organ rejection in adults who have had a kidney or liver transplant. For kidney transplants it is combined with basiliximab, reduced-dose cyclosporine and steroids. For liver transplants it starts at least 30 days after surgery with reduced-dose tacrolimus.
Zortress (everolimus) tablets are taken by mouth at the dose set by your transplant team. Doses are adjusted using blood tests to keep the everolimus trough level between 3 and 8 ng/mL. Do not change the dose yourself or switch to another everolimus product.
Common Zortress (everolimus) side effects include swelling of the legs, constipation, high blood pressure, nausea, anaemia, urinary infections, high blood fats, diarrhoea and headache. Serious effects include infections, lung inflammation, poor wound healing and kidney problems. Report fever, cough, breathlessness or reduced urine promptly.
Avoid grapefruit and grapefruit juice, live vaccines and St John's wort while taking Zortress (everolimus). Strong CYP3A4 inhibitors such as ketoconazole or clarithromycin, and inducers such as rifampin, are not recommended. Tell your transplant team about every medicine and supplement you use.
Zortress (everolimus) needs regular blood tests. Your team checks everolimus trough levels, usually 4 to 5 days after any dose change, plus cyclosporine levels, kidney function, urine protein, blood fats, blood sugar and blood counts. The target everolimus level is 3 to 8 ng/mL.
Zortress (everolimus) has a boxed warning for cancers and serious infections from immunosuppression, kidney graft thrombosis (mostly within 30 days), kidney damage with standard-dose cyclosporine, and higher death rates in heart transplant recipients. It is not recommended after heart transplantation.

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