Everolimus
Cytostatic · Protein kinase inhibitor
Indications
Tab 0.25 mg/0.75 mg: Prophylaxis of organ rejection in adult patients at low to moderate immunological risk receiving an allogenic renal or cardiac transplant, in combination with cyclosporin for microemulsion and corticosteroids. Tab 5 mg/10 mg: Advanced renal cell carcinoma that has progressed during or after VEGF- targeted therapy.
Dosage
Prophylaxis of organ rejection: Adults: 0.75 mg twice daily. Advanced renal cell carcinoma: Adults: 10 mg once daily. Children: Not recommended.
Adverse Effects
Leucopenia and hyperlipidaemia while used concomitantly with cyclosporin for microemulsion and corticosteroids. Infections, thrombocytopenia, anaemia, venous thromboembolism, pneumonia, diarrhoea, nausea, vomiting, abdominal pain, general pain, oedema, hypertension, acne, wound complication, myalgia, hepatitis, blood dyscrasias, anorexia, insomnia, headache, epistaxis, dry mouth, fatigue, chest pain, fever, weight loss. Less commonly congestive heart failure and impaired wound healing; hepatitis B reactivation and haemorrhage. Dehydration, anxiety, somnolence, convulsions, dysgeusia, ocular hyperaemia, conjunctivitis, proteinuria, blood glucose disturbances, respiratory disorder, epistaxis, cough, dyspnoea, pulmonary embolism, pneumonitis, mucosal inflammation, GI upset, stomatitis, dysphagia, skin and nail disorders, hand-foot syndrome, joint pain, asthenia, pyrexia, irritability,…
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Hypersensitivity to everolimus, sirolimus or to any of the ingredients in the preparation. Patients with rare hereditary problems of lactase deficiency or glucose-galactose malabsorption should not take this medicine. Severe hepatic impairment. Ensure adequate contraception for women of childbearing age. SEGA and refractory seizures, hepatic impairment in children <18 years. Precautions: Increased risk of developing lymphomas and other malignancies, particularly of the skin. Over suppression of the immune system with increased susceptibility to infection. Patients should be closely monitored. Use effective contraception. Moderate hepatic impairment. Ensure any infection is resolved before starting treatment. Discontinue if invasive systemic fungal infection develops. Advise patient…
Interactions
Rifampicin, rifabutin, ketoconazole, itraconazole, voriconazole, live vaccines, clarithromycin, telithromycin, ritonavir, erythromycin, fluconazole, phenytoin, carbamazepine, phenobarbital, calcium channel blockers, protease inhibitors and anti-HIV drugs. Inhibitors or inducers of CYP3A4 or P-glycoprotein inhibitors (e.g. antifungal, macrolide, protease inhibitor, calcium channel blocker, cyclosporin), inducers (e.g., rifampicin, anticonvulsants, NNRTIs, St John's wort, dexamethasone) or substrates (e.g., midazolam, pimozide, ergot alkaloids). ACE inhibitors. Drugs that affect platelet function or increase haemorrhage risk.
Advice to Patient
Take consistently either with meals or without meals. Do not chew or crush tablets. Swallow whole with a glass of water. Contact prescriber if there is severe persistent cough, difficulty in breathing, wheezing, chest pain, nausea, fever, chills, skin rash, tiredness, weakness, joint pain and inflammation, loss of appetite, yellowing of the skin or eyes, pale stool, dark coloured urine, pain in the upper right side of the stomach. Avoid grapefruit juice and products during therapy.
Pharmacokinetics
Absorption: Rapid. Metabolism: Extensively metabolized in the liver. Bioavailability: Tablets: Approx 30% (Afinitor). Half-life elimination: Approx 30 hours (Afinitor and Zortress); in pediatric renal transplant patients (3 to 16 years), half-life similar to adult data. Time to peak, plasma: 1 to 2 hours (Afinitor and Zortress). Excretion: Feces (80%); Urine (Approx 5%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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