Class: Calcineurin Inhibitor
Dosage Forms. Capsule: 0.5 mg, 1 mg, 5 mg
Common FDA Label Indication, Dosing, and Titration.
1. Cardiac transplant rejection, prophylaxis: 0.075 mg/kg/d po in 2 divided doses; titrate dose based on serum levels and tolerability
2. Liver transplant rejection, prophylaxis: Adults, 0.1-0.15 mg/kg/d po in 2 divided doses; titrate dose based on clinical response, serum levels and tolerability; Children: 0.15-0.2 mg/kg/d po in 2 divided doses; titrate dose based on serum levels and tolerability
3. Renal transplant rejection, prophylaxis: 0.2 mg/kg/d po in 2 divided doses; titrate dose based on serum levels and tolerability
1. Corneal graft rejection; prophylaxis: Use cardiac transplant dose above
MOA. Tacrolimus binds to cyclophylin, which inhibits the antigenic response of helper T lymphocytes, which in turn reduces the production of interleukin 2 and suppresses interferon-gamma. Inhibition of the immune response limits inflammation.
Drug Characteristics: Tacrolimus
Medication Safety Issues: Tacrolimus
Drug Interactions: Tacrolimus
Adverse Reactions: Tacrolimus
Efficacy Monitoring Parameters. Lack of signs of rejection (elevation in SCr for renal transplant, LFTs for liver transplant).
Toxicity Monitoring Parameters. Tacrolimus trough whole blood concentrations (target 5-20 ng/mL). Monitor electrolytes, FPG, BP and SCr, BUN, lipids, and CBC. Itching or hives, swelling of face, hands, mouth facial or throat, chest tightness, trouble breathing, blistering, peeling, or red skin rash, chest pain, change in urination, unusual bruising or bleeding, severe abdominal pain.
Key Patient Counseling Points. Take on an empty stomach. Avoid alcohol, grapefruit, and grapefruit juice. Many medications, over-the-counter medications, and foods interact with tacrolimus. Monitor carefully.
Clinical Pearls. Tacrolimus is more effective in preventing acute rejection than cyclosporine for patients with liver and kidney transplants. When changing between brand and generic forms, monitor tacrolimus levels. Topical formulation also available.