Rapamune

Sirolimus

Prophylaxis of organ rejection in patients receiving renal transplant.

De novo transplant combination therapy: Low to moderate immunologic risk Loading dose: 6 mg as soon as possible after transplant. Maintenance: 2 mg daily. High immunologic risk Loading dose: 15 mg on day 1 post-transplant. Maintenance: Initially 5 mg daily on day 2, adjust dose based on whole blood conc 10-15 ng/mL by obtaining trough levels on days 5-7. Cyclosporine w/drawal Discontinue use over 4-8 wk at 2-4 mth after transplantation. Adjust dose based on whole blood trough conc 16-24 ng/mL (chromatographic method) for 1st yr, thereafter 12-20 ng/mL.

May be taken with or without food: Take consistently either always w/ or always w/o meals. Avoid grapefruit juice.

Hypersensitivity.

Hypersensitivity eg, anaphylactic/anaphylactoid reactions, angioedema, exfoliative dermatitis & hypersensitivity vasculitis. Not recommended in liver or lung transplant patients. Lymphoma & other skin malignancies; ILD. Increased risk of opportunistic infections. Impaired or delayed wound healing; fluid accumulation. Administer Pneumocystis carinii pneumonia prophylaxis for 1 yr post-transplant & cytomegalovirus prophylaxis for 3 mth after transplant. Limit exposure to sun & UV light. Monitor for rhabdomyolysis development, serum cholesterol & triglycerides levels. Not recommended in co-administration w/ CYP3A4 &/or P-gp strong inhibitors & inducers. Co-administration w/ calcineurin & ACE inhibitors. Monitor renal function. Not recommended in high-risk renal transfer patients eg, Banff 93 grade III acute or vascular rejection, dialysis-dependent or w/ serum creatinine >4.5 mg/dL, Black patients, renal re-transplants, multi-organ transplants & patients w/ high reactive Ab panel. Hepatic impairment. Initiate effective contraception prior to, during & 12 wk after last dose. Pregnancy & lactation. Childn <13 yr.

Pneumonia, fungal, viral & bacterial infection, herpes simplex, UTI; thrombocytopenia, anemia, leukopenia; hypokalaemia, hypophosphataemia, hyperlipidaemia, hyperglycaemia, hypertriglyceridaemia, fluid retention, DM; headache; tachycardia; HTN, lymphocele; abdominal pain, constipation, diarrhoea, nausea; rash, acne; arthralgia; proteinuria; menstrual disorder (amenorrhoea & menorrhagia); impaired healing, oedema, peripheral oedema, pyrexia, pain; abnormal LFT (increased ALT & AST), increased blood creatinine & lactate dehydrogenase. Sepsis, pyelonephritis, cytomegalovirus infection, herpes zoster; squamous cell skin & basal cell carcinoma; haemolytic uraemic syndrome, neutropenia; hypersensitivity (eg, angioedema, anaphylactic & anaphylactoid reaction); pericardial effusion; venous thrombosis (DVT); pulmonary embolism, pneumonitis, pleural effusion, epitaxis; pancreatitis, stomatitis, ascites; osteonecrosis; ovarian cyst.

Increased levels w/ CYP3A4 & P-gp inhibitors eg, diltiazem, nicardipine, verapamil, clotrimazole, fluconazole, itraconazole, ketoconazole, voriconazole, clarithromycin, erythromycin, telithromycin, troleandomycin, cisapride, metoclopramide, bromocriptine, cimetidine, cyclosporine, danazol, ritonavir, indinavir, boceprevir, telaprevir, grapefruit juice. Decreased levels w/ CYP3A4 & P-gp inducers eg, carbamazepine, phenobarb, phenytoin, rifabutin, rifampicin, rifapentine, St. John's wort. Rhabdomyolysis w/ cyclosporine, HMG-CoA reductase inhibitors &/or fibrates. Calcineurin inhibitor-induced hemolytic uremic syndrome/TTP/thrombotic microangiopathy w/ calcineurin inhibitor. Avoid use of live vaccines.

Immunosuppressants

L04AA10 - sirolimus ; Belongs to the class of selective immunosuppressive agents. Used to induce immunosuppression.

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