Prograf

Tacrolimus

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 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. Lupus nephritis Adult 3 mg once daily. IV infusion Initially 0.03-0.05 mg/kg daily as continuous 24-hr IV infusion 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: Take at least 1 hr before or 2-3 hr after meals. Avoid grapefruit juice.

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

Stop infusion if signs or symptoms of anaphylaxis occur. Discontinue use of treatment or cyclosporine at least 24 hr prior to initiation of other drugs; pure red cell aplasia & myocardial hypertrophy is diagnosed. Maintain BP control & immediate reduction of immunosuppression if posterior reversible encephalopathy syndrome (PRES) is suspected or diagnosed. Increased risk of developing lymphomas & other malignancies, particularly of the skin; for opportunistic infections, including latent viral infection in immunosuppressed patients. Increased susceptibility to infection in combination w/ immunosuppressant therapy. Risk of thrombotic microangiopathy. Patients w/ risk factors for QT prolongation; lupus nephritis. Mild or moderate HTN; GI perforation; DM; neurotoxicity in high doses. May cause visual & neurological disturbances. Continuous observation 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, & monitor for renal function, QT prolongation w/ ECG, & for other side effects in co-administration w/ St. John's wort (Hypericum perforatum). Monitor serum K levels. Regularly assess serum creatinine, K, & fasting glucose. Perform routine monitoring of metabolic & hematologic system. Regularly monitor maternal blood glucose levels. Monitor & control BP during pregnancy. Limit sun & UV light exposure. Not recommended in co-administration w/ strong CYP3A4 inhibitors (eg, telaprevir, boceprevir, ritonavir, ketoconazole, itraconazole, voriconazole, clarithromycin) & inducers (eg, rifampin, rifabutin) w/o dose adjustment & subsequent close monitoring whole blood trough conc & tacrolimus-associated adverse reactions. Not to be used concomitantly w/ K-sparing diuretics during treatment. Avoid use of live attenuated vaccines; in combination w/ cyclosporine. Acute & chronic renal impairment. Increased risk of developing renal insufficiency related to high whole-blood levels. Transiently reduce dose or discontinue treatment in patients w/ impaired renal function. Hepatic impairment. Females & males of reproductive potential should use appropriate contraception prior to starting treatment. Increased hyperglycemia in pregnant women w/ diabetes including gestational diabetes. Exacerbated HTN in pregnant women & increased pre-eclampsia. Not to be used during lactation. Risk of prematurity, birth defects/congenital anomalies, low birth wt, & fetal distress in infants exposed to treatment in utero. Ped patients.

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/ aminoglycosides, amphotericin B, ibuprofen, & cisplatin. Additive/synergistic nephrotoxicity w/ cyclosporine. Increased blood levels w/ Ca channel blocker (eg, diltiazem, nicardipine, nifedipine, verapamil), antifungal agents (eg, clotrimazole, fluconazole, itraconazole, ketoconazole, voriconazole), macrolide antibiotics (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 & Schisandra sphenanthera extr. Decreased blood levels w/ 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 metabolized by CYP3A (eg, nelfinavir, ritonavir). Increased blood conc w/ nelfinavir. Increased C_max & AUC w/ telaprevir & boceprevir. Increased conc of phenytoin. Affected CYP3A-mediated metabolism by grapefruit juice. Not recommended in combination w/ sirolimus. Avoid use w/ live vaccines. Potential increased exposure of mycophenolic acid. Direct-acting antiviral therapy.

Immunosuppressants

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

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