Prograf®
GoodRxTacrolimus · oral capsule
Misc.
Approved uses
Prophylaxis of organ rejection in liver, kidney or heart transplantation
Dosed by body weight and adjusted to whole-blood trough concentration, given consistently with or without food
PRES is the ocular emergency to know: visual disturbance up to cortical blindness
OFF-LABELNot in the FDA label for this product
Non-infectious uveitis, as a corticosteroid-sparing agent
Oral, titrated to effect and to renal tolerance
Cohort · n=62 · steroid taper
A retrospective series of 62 consecutive patients with non-infectious uveitis treated with tacrolimus found they tapered oral prednisone to 10 mg daily at a rate of 1.62 per patient-year, with an 85% probability of reaching 10 mg or less after about 14 months. Tacrolimus was stopped for intolerance at 0.13 per patient-year, and the cardiovascular measures that limit other agents stayed low: new or increased treatment for hypertension, cholesterol or diabetes each ran below 0.05 per patient-year, and creatinine rises of 30% or more were uncommon at 0.05 per patient-year.
Contraindications
Tacrolimus capsules are contraindicated in patients with a hypersensitivity to tacrolimus. Tacrolimus injection is contraindicated in patients with a hypersensitivity to HCO-60 (polyoxyl 60 hydrogenated castor oil). Hypersensitivity symptoms reported include dyspnea, rash, pruritus, and acute respiratory distress syndrome [seeAdverse Reactions ].
Available FormsTacrolimus capsules 0.5 mg, 1 mg and 5 mg, plus granules and an intravenous form.
Mechanism of ActionTacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed, after which the phosphatase activity of calcineurin is inhibited. Such inhibition prevents the dephosphorylation and translocation of various factors such as the nuclear factor of activated T-cells (NF-AT), and nuclear factor kappa-light-chain enhancer of activated B-cells (NF-κB).
Warnings & Precautions
- Increased risk of serious infection and of lymphoma and other malignancies resulting from immunosuppression. This carries a boxed warning.
- Nephrotoxicity is dose-related and common; monitor renal function and trough levels.
- Neurotoxicity, including tremor, headache, seizure and posterior reversible encephalopathy syndrome with visual disturbance and cortical blindness, has been reported.
- Hyperkalaemia, hypertension and new-onset diabetes after transplant are common.
- QT prolongation has been reported; avoid in congenital long QT syndrome.
- Therapeutic drug monitoring is required.
Common Side Effects
The most common adverse reactions (≥ 15%) were abnormal renal function, hypertension, diabetes mellitus, fever, CMV infection, tremor, hyperglycemia, leukopenia, infection, anemia, bronchitis, pericardial effusion, urinary tract infection, constipation, diarrhea, headache, abdominal pain, insomnia, paresthesia, peripheral edema, nausea, hyperkalemia, hypomagnesemia, and hyperlipemia.
Pregnancy & LactationPregnancy: Tacrolimus crosses the placenta and is associated with preterm delivery, neonatal hyperkalaemia and renal dysfunction.
Lactation: Tacrolimus is present in human milk; consider the mother's clinical need alongside any potential effect on the infant.
Pediatric UseSafety and effectiveness have been established in pediatric liver transplant patients. Liver Transplantation Safety and efficacy in pediatric de novo liver transplant patients less than 16 years of age are based on evidence from active controlled studies that included 56 pediatric patients, 31 of which received tacrolimus.