Tacrolimus Sandoz

Tacrolimus

Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants. Treatment of refractory rejection in patients receiving allogeneic liver or kidney transplants. Monotherapy or in combination w/ NSAIDs &/or steroids for the treatment of active RA in adult patients for whom DMARD therapy is ineffective or inappropriate.

Kidney transplantation Initially 0.2-0.3 mg/kg/day every 12 hr in 2 divided doses administered w/in 24 hr of transplantation or until renal function has recovered. Liver transplantation 1st oral dose should be given 8-12 hr after discontinuing IV infusion. Adult Initially 0.1-0.15 mg/kg/day every 12 hr in 2 divided daily doses. Ped patient Initially 0.15-0.2 mg/kg/day. Heart transplantation Initially 0.075 mg/kg/day every 12 hr in 2 divided doses administered no sooner than 6 hr after transplantation. RA Adult 3 mg once daily.

May be taken with or without food: Swallow whole, do not cut/crush/chew. Do not use w/ grapefruit products.

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

Increased susceptibility to infection; possible development of lymphoma & other malignancies. Risk of HTN, hyperkalemia, heart failure, myocardial hypertrophy, arrhythmia, QTc prolongation, Torsade de Pointes; GI perforation; pure red cell aplasia; new onset DM, hyperglycemia, elevations in HbA1c, overt diabetes; anaphylactic reaction; neurotoxicity, particularly in high doses; nephrotoxicity; visual & neurological disturbance. Increased risk of developing renal insufficiency in liver transplant recipients experiencing post-transplant hepatic impairment. Reports of lymphoproliferative disorder related to EBV in immunosuppressed organ transplant recipients. Perform routine monitoring of metabolic & hematologic systems. Regularly assess serum creatinine, K & fasting glucose. Monitor blood levels & appropriate dosage adjustment in transplant patients when used concomitantly w/ CYP3A4 inducer/inhibitor. Not recommended for patients w/ rare hereditary disease of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Should be used during pregnancy only if potential benefit to mother justifies potential risk to fetus. Breast feeding should be avoided. Not indicated for RA in childn <18 yr. Safety & efficacy in elderly >65 yr have not been established.

Kidney transplantation: Infection, tremor, HTN, decreased renal function, constipation, diarrhea, headache, abdominal pain, insomnia. Liver transplantation: Tremor, headache, diarrhea, HTN, nausea & abnormal renal function; hyperkalemia & hypomagnesemia, hyperglycemia. Heart transplantation: Abnormal kidney function, HTN, DM, CMV infection, hyperglycemia, leukopenia, infection, hyperlipemia. RA: Flu syndrome, diarrhea, nausea, abdominal pain, dyspepsia, tremor.

Potential additive or synergistic impairment of renal function w/ aminoglycosides, amphotericin B, ganciclovir, acyclovir, cisplatin, NSAIDs, cyclosporine. Increased conc w/ antacid (Mg-/Al-hydroxide), anti-arrhythmic agent (amiodarone), azole antifungals (ketoconazole, clotrimazole, fluconazole, itraconazole, voriconazole), Ca-channel blockers (diltiazem, nicardipine, nifedipine, verapamil), GI prokinetic agents (cisapride, metoclopramide), macrolide antibiotics (erythromycin, clarithromycin, troleandomycin), PPIs (lansoprazole, omeprazole), bro­mocriptine, cimetidine, chloramphenicol, danazol, ethinyl estradiol, methylprednisolone, nefazodone, PIs (boceprevir, nelfinavir, ritonavir, saquinavir, telaprevir); grapefruit/grapefruit juice. Decreased conc w/ anticonvulsants (carbamazepine, phenobarb, phenytoin), anti-infectives (rifampicin, caspofungin, rifabutin), calcineurin inhibitor (sirolimus), St. John's wort. Vaccination may be less effective.

Immunosuppressants

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

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