Generic Name and Formulations:
Tacrolimus 0.5mg, 1mg, 5mg; ext-rel caps.
Astellas Pharma US, Inc.
Organ rejection prophylaxis in kidney transplant patients, in combination with mycophenolate mofetil (MMF) and corticosteroids, with or without basiliximab induction.
Not interchangeable or substitutable with tacrolimus extended-release or immediate-release products.
Swallow whole. Take once daily in the morning, preferably on an empty stomach. If previously on Prograf IV infusion, initial oral dose may be given 8–12hrs after discontinuing infusion. ≥16yrs: with basiliximab induction: initially 0.15mg/kg/day; give first dose prior to or within 48hrs after transplantation; but may be delayed until renal function has recovered; without induction (pre-op): 0.1mg/kg/day; give dose within 12hrs prior to reperfusion when used with MMF and corticosteroids; without induction (post-op): 0.2mg/kg/day; give first dose within 12hrs after reperfusion but not less than 4hrs after pre-op dose when used with MMF and corticosteroids. Black patients may require higher doses. Renal or hepatic impairment: use lowest effective dose. Post-op oliguria: give initial dose no sooner than 6hrs and within 48hrs of transplantation, but may delay therapy until renal function recovers. See full labeling.
<16yrs: not established.
Not indicated for use in liver transplantation. Increased risk of lymphomas and other malignancies (eg, skin). Avoid sun, UV light. Epstein Barr Virus seronegative. Increased risk of infections (eg, bacterial, viral, fungal, protozoal, cytomegalovirus), opportunistic infections including polyoma virus. Avoid in congenital long QT syndrome. CHF, bradyarrhythmias, concomitant antiarrhythmic drugs, or electrolyte disturbances; consider obtaining ECGs and monitor electrolytes periodically. New-onset diabetes: monitor for hyperglycemia. Hepatic or renal impairment; monitor and consider dose reduction. Obtain tacrolimus whole blood concentrations (see full labeling), serum creatinine, potassium, and fasting glucose periodically. Pregnancy (Cat.C), nursing mothers: not recommended.
Concomitant sirolimus, live vaccines, cyclosporine: not recommended. Concomitant mycophenolic acid (MPA) products; monitor. Concomitant strong CYP3A4 inhibitors/inducers or substrates: must adjust dosing regimen, closely monitor tacrolimus blood concentrations and for QT prolongation. Caution with potassium-sparing diuretics, ACEIs, ARBs. Avoid grapefruit/grapefruit juice, alcohol. Additive nephrotoxicity with aminoglycosides, ganciclovir, amphotericin B, cisplatin, ritonavir. May be potentiated by calcium channel blockers (eg, verapamil, diltiazem, nifedipine, nicardipine), antifungals (eg, voriconazole, posaconazole, itraconazole, fluconazole, ketoconazole), macrolides (eg, troleandomycin, clarithromycin, erythromycin), metoclopramide, lansoprazole, omeprazole, chloramphenicol, cimetidine, danazol, ethinyl estradiol, amiodarone, protease inhibitors (eg, telaprevir, boceprevir, nelfinavir, ritonavir), nefazodone, schisandra sphenanthera extracts, clotrimazole, magnesium-aluminum-hydroxide. May be antagonized by carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, caspofungin, St. Johns wort, methylprednisolone, prednisone.
Diarrhea, constipation, nausea, peripheral edema, tremor, anemia, headache, abdominal pain, insomnia, hypertension, renal dysfunction, infections (viral, cytomegalovirus, polyoma virus), hypophosphatemia, hyperkalemia, hypomagnesemia, hyperglycemia, nephrotoxicity or neurotoxicity (esp. in high doses), JC virus-associated progressive multifocal leukoencephalopathy, post-transplant diabetes mellitus, posterior reversible encephalopathy syndrome (consider reduced dose or discontinue), malignancies (lymphomas, skin), post-transplant lymphoproliferative disorder, pure red cell aplasia (consider discontinuation), Torsade de Pointes.
Ext-rel caps—30, 50
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