Tacrolimus (Oral)
Brand Name: Astagraf, Prograf
Generic Available*
Common Dosage Forms:
Capsules (Prograf)*: 0.5 mg, 1 mg, 5 mg
Capsules, extended release (Astragraf XL): 0.5 mg, 1 mg, 5 mg
Granules (Prograf): 0.2 mg, 1 mg/packet
*Tacrolimus is also available in a topical ointment which is not covered on this card.
FDA Indications/Dosages:
For the prophylaxis of organ rejection in kidney and liver transplants: Start with 0.075-0.2 mg/kg/day given in two divided doses (Prograf) or 0.15-0.2 mg/kg/day in one dose (Astagraf XL). Whole blood concentrations should be in the range of 5-20 ng/mL. Dosages must be individualized and titrated based on clinical assessments of rejection and tolerability.
Monitor: Blood glucose, Drug trough levels
Pharmacology/Pharmacokinetics: Tacrolimus causes immunosuppression by inhibiting T-lymphocyte activation. It is postulated that it works by binding to an intracellular protein, FKBP-12, which forms a complex with calcium, calmodulin, and calcineurin. This complex inhibits the phosphatase activity of calcineurin which inhibits the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT). Oral bioavailability is variable and is decreased when taken with food. Tacrolimus is 99% bound to plasma proteins. Metabolism occurs in the liver via CYP3A to activate and inactive metabolites.
Drug Interactions: Avoid the use of live vaccines during treatment. CYP3A inhibitors or substrates (ketoconazole, itraconazole, voriconazole, ritonavir, nelfinavir, verapamil, diltiazem, nifedipine, nicardipine, erythromycin, clarithromycin, troleandomycin, chloramphenicol, lansoprazole, omeprazole, bromocriptine, nefazodone, metoclopramide, danazol, ethinyl estradiol, cimetidine, and methyl prednisone) may increase plasma levels of tacrolimus. CYP3A inducers (phenytoin, phenobarbital, carbamazepine, St. John’s Wort, and rifampin) may decrease plasma levels of tacrolimus. Magnesium and aluminum hydroxide antacids may increase tacrolimus whole blood concentrations. Caution with use of other agents associated with hyperkalemia (potassium-sparing diuretics, ACEIs, and ARBs).
Contraindications/Precautions: Patients taking immunosuppressants are at an increased risk of developing lymphomas and malignancies, especially of the skin. Patients should protect themselves from sunlight and UV light. There is also an increased risk of bacterial, viral, protozoal, and fungal infections, sometimes serious in nature. Some cases of new onset diabetes mellitus have occurred in lever, heart, and kidney transplant patients taking tacrolimus. Use with caution in patients with hepatic impairment. Pregnancy Category C.
Adverse Effects: Most common adverse effects include infection, tremor, hypertension, constipation, diarrhea, headache, abdominal pain, insomnia, nausea, hypomagnesemia, UTI, hypophosphatemia, peripheral edema, asthenia, pain, hyperlipidemia, hyperkalemia, and anemia. Less common but serious adverse effects include nephrotoxicity, neurotoxicity, lymphomas, skin cancer, pure red cell aplasia, diabetes, and myocardial hypertrophy.
Patient Consultation:
Take each dose on an empty stomach – one hour before or two hours after a meal – unless otherwise directed.
It is important to be consistent with your doses. If a dose is missed, take it as soon as possible.
XL capsules must be taken whole.
Do not discontinue therapy without first consulting physician.
Avoid grapefruit or drinking grapefruit during treatment.
Avoid antacids containing magnesium, aluminum, cimetidine, lansoprazole, or omeprazole during treatment.
Avoid exposure to sunlight and UV light.
Contact a physician right away if you experience fever, sweat or chills, cough, muscle aches, or red and painful area of your skin, confusion, muscle tremors, numbness, seizures, vision changes, shortness of breath, chest pain, or felling lightheadedness or faint.