Concise Prescribing Info
Prophylaxis of organ rejection in patients receiving renal transplant including patients at low to moderate & high immunological risk.
Dosage/Direction for Use
Patient at low to moderate immunologic risk Cyclosporine (CsA) combination therapy Loading dose: 6 mg post-transplantation for de novo transplant recipients. Maintenance: 2 mg daily. Dose should be increased to obtain whole blood trough conc (w/in the range of 16-24 ng/mL) at 2-4 mth after renal transplantation while CsA should be w/drawn. Target conc: 12-20 ng/mL (chromatographic method). Patient at high immunologic risk Combination w/ tacrolimus therapy Loading dose: Up to 10 mg on days 1 & 2 post-transplantation. Initial maintenance dose of 5 mg/day starting on day 3. Starting dose of tacrolimus: Up to 0.2 mg/kg/day in divided doses & should be adjusted to achieve whole blood trough conc of 10-15 ng/mL for 14 days, 5-10 ng/mL from day 15 to end of wk 26, & 3-5 ng/mL from wk 27 to the end of wk 52. Administer prednisone at min of 5 mg/day. Combination w/ CsA therapy Loading dose: Up to 15 mg on day 1 post-transplantation. Initial maintenance: 5 mg/day starting on day 2. Starting dose of CsA: Up to 7 mg/kg/day in divided doses & should be subsequently adjusted to achieve whole blood trough conc of 200-300 ng/mL for 14 days, 150-200 ng/mL from day 15 to the end of wk 26 & 100-150 ng/mL from wk 27 to end of wk 52. Administer prednisone at min of 5 mg/day. Renal allograft recipient Max: Not exceeding 40 mg daily. Ped patient ≥13 yr weighing <40 kg Initial loading dose: 3 mg/m2. Maintenance: May be adjusted based on BSA to 1 mg/m2/day. Patient w/ hepatic impairment Maintenance dose be reduced by approx ⅓ to ½.
May be taken with or without food: Take consistently either always w/ or always w/o meals. Do not crush/chew/split tab. Avoid grapefruit juice.
Special Precautions
Increased susceptibility to opportunistic infection including activation of latent viral infections, sepsis & fatal infections, & development of lymphoma & other malignancies, particularly of the skin. Hypersensitivity reactions eg, anaphylactic/anaphylactoid reactions, angioedema, exfoliative dermatitis & hypersensitivity vasculitis. Excess mortality, graft loss & hepatic artery thrombosis in liver transplant patients. Bronchial anastomotic dehiscence in lung transplant patients. Impaired or delayed wound healing including lymphocele & wound dehiscence. Limit exposure to sunlight & UV light. Monitor for hyperlipidemia; elevated lipids, & possible development of rhabdomyolysis & other adverse effects in patients administered w/ HMG-CoA reductase inhibitor &/or fibrate; renal function during co-administration w/ tacrolimus or cyclosporine. Consider discontinuation of immunosuppressive regimen in patients w/ elevated serum creatinine levels. Continuation of combination therapy w/ CsA >4 mth after transplantation in patients at low to moderate immunologic risk. May delay recovery of renal function in patients w/ delayed graft function. Periodic quantitative monitoring of urinary protein excretion. Conversion to sirolimus in patients w/ GFR <40 mL/min. De novo use w/o calcineurin inhibitor. Interstitial lung disease. Continue prophylaxis for Pneumocystis carinii pneumonia (1 yr after transplantation) & cytomegalovirus (3 mth after transplantation). Concomitant use w/ calcineurin inhibitor may increase risk of calcineurin inhibitor-induced HUS/TTP/TMA & w/ ACE inhibitors may result in angioneurotic edema-type reactions. Initiate effective contraception before, during & 12 wk after therapy. W/drawal of CsA in high-risk renal transplant patients. Avoid use of live vaccines during treatment. Patients w/ Banff 93 grade III acute rejection or vascular rejection prior to CsA w/drawal, those who are dialysis-dependent or w/ serum creatinine >4.5 mg/dL, Black patients, renal re-transplants, multi-organ transplants & w/ a high panel of reactive antibodies. Hepatic impairment. Contraception must be initiated before therapy & maintained during therapy & for 12 wk after therapy has been stopped. Pregnancy & lactation. Childn <13 yr. Elderly.
Adverse Reactions
Sepsis, pneumonia, mycobacterial infection (including TB), pyelonephritis, fungal & cytomegalovirus infection, herpes zoster, Epstein-Barr virus, viral & bacterial infection, herpes simplex, UTI; lymphoma, neuroendocrine carcinoma of the skin, malignant melanoma, post-transplant lymphoproliferative disorder, squamous cell carcinoma of skin, basal cell carcinoma; pancytopenia, thrombotic thrombocytopenic purpura, hemolytic uremic syndrome, neutropenia, thrombocytopenia, anemia, leukopenia; hypersensitivity (including angioedema, anaphylactic & anaphylactoid reactions); hypokalemia, hypophosphatemia, hyperlipidemia (including hypercholesterolemia), hyperglycemia, hypertriglyceridemia, fluid retention, DM; posterior reversible encephalopathy syndrome, headache; pericardial effusion, tachycardia; venous thrombosis (including DVT), HTN, lymphoedema, lymphocele; pulmonary hemorrhage & embolism, alveolar proteinosis, pneumonitis, pleural effusion, epistaxis; pancreatitis, stomatitis, ascites, abdominal pain, constipation, diarrhea, nausea; exfoliative dermatitis, hypersensitivity vasculitis, rash, acne; osteonecrosis, arthralgia; nephrotic syndrome, focal segmental glomerulosclerosis, proteinuria; menstrual disorder (including amenorrhea & menorrhagia), ovarian cyst; impaired healing, edema, peripheral edema, pyrexia, pain; abnormal liver function test (including increased ALT & AST), increased blood creatinine & blood lactate dehydrogenase.
Drug Interactions
Not recommended w/ strong CYP3A4 inhibitors (eg, ketoconazole, voriconazole, itraconazole, telithromycin, clarithromycin) or CYP3A4 inducers (eg, rifampin, rifabutin). May increase sirolimus levels w/ CYP3A4 & P-glycoprotein (P-gp) inhibitors. May decrease sirolimus levels w/ CYP3A4 & P-gp inducers. Decreased sirolimus levels w/ CYP3A4 & P-gp inducers. Increased bioavailability w/ diltiazem. Significantly affected/increased rate & extent of absorption of both drugs w/ verapamil, erythromycin & ketoconazole. Monitor for the development of rhabdomyolysis w/ CsA, HMG-CoA reductase inhibitors &/or fibrates. May affect response to vaccination & drug metabolism w/ grapefruit juice.
MIMS Class
ATC Classification
L04AA10 - sirolimus ; Belongs to the class of selective immunosuppressive agents. Used to induce immunosuppression.
Rapamune sugar-coated tab 0.5 mg
100's (P19,351.85/box)
Rapamune sugar-coated tab 1 mg
100's (P34,158.99/box)
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