Prograf

Lupus nephritis when the effect of steroids is insufficient or administration of steroids is difficult. Prophylaxis of organ rejection in patients receiving allogenic liver or kidney transplants concomitantly w/ adrenal corticosteroids, or azathioprine or mycophenolate mofetil in kidney transplant recipients.

Cap Lupus nephritis Adult 3 mg once daily. Adult kidney transplant patient Administer initial dose w/in 24 hr of transplantation but delay until renal function recovers. In combination w/ azathioprine: Initially 0.2 mg/kg daily in 2 divided doses every 12 hr. In combination w/ mycophenolate mofetil/interleukin-2 receptor antagonist: Initially 0.1 mg/kg daily in 2 divided doses every 12 hr. Adult liver transplant patient Initially 0.1-0.15 mg/kg daily in 2 divided doses every 12 hr. Administer no sooner than 6 hr after transplantation. Patient receiving IV infusion: May give 1st oral dose 8-12 hr after discontinuing IV infusion. Ped liver transplant patient Initially 0.15-0.2 mg/kg daily in 2 divided doses every 12 hr. IV infusion Initially 0.03-0.05 mg/kg daily as continuous 24-hr IV infusion to be administered no sooner than 6 hr after transplantation. Ped liver transplant patient w/o pre-existing renal/hepatic dysfunction Initially 0.03-0.05 mg/kg daily.

Should be taken on an empty stomach: Cap: Take at least 1 hr before or 2-3 hr after meals.

Hypersensitivity to tacrolimus & HCO-60 (polyoxyl 60 hydrogenated castor oil).

Discontinue treatment if signs or symptoms of anaphylaxis occur; pure red cell aplasia; myocardial hypertrophy is diagnosed. Discontinue treatment or cyclosporine at least 24 hr prior to initiation of other drugs. Maintain BP control & immediate reduction of immunosuppression if posterior reversible encephalopathy syndrome (PRES) is suspected or diagnosed. Insulin-dependent post-transplant DM. Neurotoxicity in high doses. Increased risk of developing lymphomas & other malignancies, particularly of the skin; opportunistic infections, including latent viral infection in immunosuppressed patients. Lymphoproliferative disorder (LPD) related to Epstein-Barr Virus (EBV) infection; increased susceptibility to infection in combination w/ immunosuppressant therapy. Pure red cell aplasia. Mild or moderate HTN. GI perforation. Risk of thrombotic microangiopathy. May cause visual & neurological disturbances. Patients w/ risk factors for QT prolongation; lupus nephritis. Monitor renal function & blood conc; serum K levels. Continuously observe for at least 1st 30 min following start of infusion & at frequent intervals thereafter. Early & frequent continued monitoring of blood levels w/in 1st few days of co-administration, QT prolongation w/ ECG, & for other side effects in co-administration w/ CYP3A4 inhibitors. Consider echocardiographic evaluation In patients who develop renal failure or ventricular dysfunction while on therapy. Regularly assess serum creatinine, K, & fasting glucose. Perform routine monitoring of metabolic & hematologic system. Limit sun & UV light exposure. Concomitant use w/ other nephrotoxic drugs; amiodarone; St. John's wort (Hypericum perforatum); Ca channel blockers. Not to be used simultaneously w/ cyclosporine. Not to be used concomitantly w/ K-sparing diuretics during therapy. Avoid use of live attenuated vaccines. Not recommended in co-administration w/ strong CYP3A4 inhibitors (eg, telaprevir, boceprevir, ritonavir, ketoconazole, itraconazole, voriconazole, clarithromycin) & inducers (eg, rifampin, rifabutin). Acute & chronic renal impairment in transplant patients. May reduce dose or discontinue treatment in patients w/ renal impairment. Increased risk of developing renal insufficiency related to high whole-blood levels in liver transplant recipients experiencing post-transplant hepatic impairment. Females & males of reproductive potential should use appropriate contraception prior to starting treatment. Preterm delivery, neonatal hyperkalemia & renal dysfunction during pregnancy. Increased hyperglycemia in pregnant women w/ diabetes including gestational diabetes. Regularly monitor maternal blood glucose levels. May exacerbate HTN in pregnant women & increase pre-eclampsia; monitor & control BP during pregnancy. Not to breastfeed during therapy. Risk of prematurity, birth defects/congenital anomalies, low birth wt, & fetal distress in infants exposed to treatment in utero. Ped patients in lupus nephritis.

Headache, tremor, insomnia, paresthesia, dizziness; diarrhea, nausea, constipation, abnormal LFT, anorexia, vomiting, dyspepsia; HTN, chest pain; abnormal kidney function, increased creatinine & BUN, UTI, oliguria; hyperkalemia, hypokalemia, hyperglycemia, hypomagnesemia, hypophosphatemia, hyperlipidemia, DM, edema; anemia, leukocytosis, thrombocytopenia, leukopenia; abdominal & back pain, pain, fever, asthenia, ascites, peripheral edema, infection; pleural effusion, atelectasis, dyspnea, increased cough; pruritus, rash; arthralgia; post procedural pain, incision site complication, graft dysfunction. SJS, TEN.

Potential additive of synergistic renal function impairment w/ drugs associated w/ renal dysfunction eg, aminoglycosides, amphotericin B, ibuprofen, cisplatin. Additive/synergistic nephrotoxicity w/ cyclosporine. Increased whole blood & plasma levels w/ CYP3A4 inhibitors including Ca channel blocker (eg, diltiazem, nicardipine, nifedipine, verapamil), antifungal agents (eg, clotrimazole, fluconazole, itraconazole, ketoconazole, voriconazole), macrolides (eg, clarithromycin, erythromycin, troleandomycin), GI prokinetic agents (eg, cisapride, metoclopramide), bromocriptine, chloramphenicol, cimetidine, cyclosporine, danazol, ethinyl estradiol, amiodarone, methylprednisolone, lansoprazole, omeprazole, PIs, nefazodone, Mg-/Al- hydroxide, letermovir & cannabidiol. Increased metabolism & decreased whole blood or plasma levels w/ CYP3A4 inducers including anticonvulsants (eg, carbamazepine, phenobarb, phenytoin), antimicrobials (eg, rifabutin, caspofungin, rifampin), St. John's wort, sirolimus. Increased mean AUC & decreased mean C_max w/ Mg-/Al- hydroxide. Decreased oral bioavailability & increased clearance w/ rifampin. Concomitant use w/ nephrotoxic drugs (eg, ganciclovir) or drugs metabolized by CYP3A (eg, nelfinavir, ritonavir); direct-acting antiviral therapy. Increased blood conc w/ nelfinavir. Increased C_max & AUC w/ telaprevir & boceprevir. Increased conc of phenytoin. Avoid concomitant use w/ grapefruit juice. Decreased mean AUC & C_min w/ sirolimus. Avoid use w/ live vaccines. Potential increased exposure of mycophenolic acid.

Immunosuppressants

L04AD02 - tacrolimus ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.

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