Organ rejection prophylaxis:
Indications for ASTAGRAF XL:
Organ rejection prophylaxis in kidney transplant patients, in combination with mycophenolate mofetil (MMF) and corticosteroids, with or without basiliximab induction.
Limitations of Use:
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. With basiliximab induction: initially 0.15-0.2mg/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. See full labeling.
<4yrs: not established. ≥4yrs: with basiliximab induction: initially 0.3mg/kg/day; give dose within 24hrs after reperfusion.
Malignancies and serious infections in transplant patients. Increased mortality in female liver transplant patients.
Not indicated for use in liver transplantation. Increased risk of lymphomas and other malignancies (eg, skin). Avoid sun, UV light. Increased risk of infections (eg, bacterial, viral, fungal, protozoal, cytomegalovirus), opportunistic infections including polyoma virus. Monitor Epstein-Barr virus serology, development of infections during therapy. Risk of new onset diabetes after transplant (esp. Hispanic and black patients); monitor blood glucose. Avoid in congenital long QT syndrome. CHF, bradyarrhythmias, concomitant antiarrhythmic drugs, or electrolyte disturbances; consider obtaining ECGs and monitor electrolytes periodically. Hepatic or renal impairment; monitor and consider dose reduction. Obtain tacrolimus whole blood concentrations (see full labeling), serum creatinine, serum potassium, and fasting glucose periodically. Complete required immunizations prior to transplantation and treatment. Elderly. Labor & delivery. Advise females and males of reproductive potential to use appropriate conception prior to initiation. Pregnancy. Nursing mothers.
Concomitant live vaccines and 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, letermovir, schisandra sphenanthera extracts, clotrimazole, magnesium-aluminum-hydroxide. May be antagonized by carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, 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.