Certican

Everolimus

In combination w/ ciclosporin for microemulsion & corticosteroids for the prophylaxis of organ rejection in adult patients at low to moderate immunological risk receiving allogeneic renal or cardiac transplant. In combination w/ tacrolimus & corticosteroids for the prophylaxis of organ rejection in adult patients receiving hepatic transplant.

Adult General kidney & heart transplant population Initially 0.75 mg bd administered as soon as possible after transplantation. Liver transplantantion 1 mg bd w/ initial dose starting approx 4 wk after transplantation.

May be taken with or without food: Take consistently either always w/ or always w/o meals. Swallow whole, do not crush. Avoid grapefruit products.

Hypersensitivity to everolimus or sirolimus.

Discontinue use if ILD occurs. Increased risk of acute rejection, developing infections, lymphomas & other malignancies particularly in skin, kidney arterial & venous thrombosis, calcineurin inhibitor-induced hemolytic uremic syndrome/TTP/thrombotic microangiopathy & new onset DM. Angioedema; proteinuria; hyperlipidemia; patients under HMG-CoA reductase inhibitor &/or fibrate. Impaired wound healing. Not recommended in concomitant use w/ strong CYP3A4 inhibitors & inducers. Concomitant use w/ thymoglobulin induction. Monitor blood trough levels, blood glucose conc, renal function, skin neoplasm. Minimize exposure to UV light & sunlight. Reversible azoospermia & oligospermia in patients treated w/ mTOR inhibitors. Not to be taken by patients w/ galactose intolerance, severe lactase deficiency, glucose-galactose malabsorption. Women of childbearing potential should use effective contraception during & up to 8 wk after therapy. Risk for male infertility in prolonged use. Not to be used during pregnancy & lactation.

Viral, bacterial & fungal infections, upper & lower resp tract infection, UTI, anaemia/erythropenia, leukopenia, thrombocytopenia, hyperlipidaemia, new onset DM, hypokalaemia, insomnia, anxiety, headache, venous thromboembolic events, HTN, cough, dyspnoea, diarrhoea, nausea, vomiting, abdominal pain, pericardial & pleural effusion, peripheral oedema, healing impairment, pain, pyrexia. Sepsis, wound infection; malignant &/or unspecified tumours, skin neoplasms; pancytopenia, TTP/hemolytic uraemic syndrome; tachycardia; epistaxis, lymphocele, renal graft thrombosis; oropharyngeal pain, pancreatitis, stomatitis/mouth ulceration; acne, angioedema, rash; myalgia, arthralgia; proteinuria, renal tubular necrosis; erectile dysfunction; incisional hernia; abnormal hepatic enzyme.

Increased clearance, decreased C_max & AUC w/ rifampicin. Increased bioavailability w/ ciclosporin. Increased C_max & AUC w/ ketoconazole, erythromycin, verapamil. Increased C_min w/ octreotide. Increased C_max & AUC_inf w/ midazolam. Increased metabolism & decreased blood levels by CYP3A4 inducers eg, St. John's wort, anticonvulsants, anti-HIV drugs. Increased blood levels by antifungals, Ca-channel blockers & PIs. Decreased efflux & increased blood conc w/ P-gp inhibitors. May affect response w/ live vaccines. Increased conc of CYP3A4 & CYP2D6 substrates w/ narrow therapeutic index. Avoid grapefruit & grapefruit juice.

Immunosuppressants

L04AH02 - everolimus ; Belongs to the class of mammalian target of rapamycin (mTOR) kinase inhibitors. Used as immunosuppressants.

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