Tacrolimus (FK 506)(tack row’ lim us)
Advagraf (CAN), Astagraf XLDNC, Hecoria, Prograf, Protopic
PREGNANCY CATEGORY C
Drug Classes
Immunomodulator
Immunosuppressant
Therapeutic Actions
Immunosuppressant; inhibits T-lymphocyte activation; exact mechanism of action not known but binds to intracellular protein, which may prevent the generation of nuclear factor of activated T cells and suppress the immune activation and response of T cells.
Indications
Prophylaxis for organ rejection in liver, kidney, and heart transplants in conjunction with adrenal corticosteroids
NEW INDICATION: Prophylaxis for organ rejection in kidney transplant patients with mycophenolate, corticosteroids, with or without basiliximab induction (ER capsule)
Topical: Short-term and intermittent long-term treatment of moderate to severe atopic dermatitis when other therapies are not effective or contraindicated
Unlabeled uses: Crohn’s disease, pyoderma gangrenosum, psoriasis, prevention and treatment of acute graft-versus-host disease following hematopoietic stem-cell transplantation, rheumatoid arthritis, uveitis, lupus nephritis
Contraindications and Cautions
Contraindicated with allergy to tacrolimus, hypersensitivity to HCO-60 polyoxyl 60 hydrogenated castor oil (IV form), pregnancy, lactation.
Use cautiously with impaired renal function, hyperkalemia, malabsorption, impaired hepatic function.
Available Forms
Capsules—0.5, 1, 5 mg; ER capsuleDNC—0.5, 1, 5 mg; injection—5 mg/mL; ointment—0.03%, 0.1%
Dosages
Adults
Oral
Kidney transplant: 0.2 mg/kg/day PO divided every 12 hr if given with azathioprine. Reduce dosage to 0.1 mg/kg/day PO in divided doses if given with mycophenolate, mofetil and/or interleukin-2 receptor antagonists.
Kidney transplant (ER form): 0.1 mg/kg/day PO ER capsule preoperatively, 0.2 mg/kg/day PO ER capsule postoperatively; if using basiliximab induction, 0.15 mg/kg/day PO ER capsule.
Liver transplant: 0.10–0.15 mg/kg/day PO divided every 12 hr; administer initial dose no sooner than 6 hr after transplant. If transferring from IV, give first dose 8–12 hr after discontinuing IV infusion.
Adjust dosage based on clinical assessment of rejection tolerance of drug.
Heart transplant: 0.075 mg/kg/day PO or IV in two divided doses given every 12 hr. Give first dose no sooner than 6 hr after transplant. If therapy starts with IV route, switch to oral route as soon as possible, 8–12 hr after discontinuing IV infusion.
Parenteral
For patients unable to take capsules, 0.03–0.05 mg/kg/day (liver or kidney transplant) or 0.01 mg/kg/day (heart transplant) as continuous IV infusion begun no sooner than 6 hr after transplant. Switch to oral drug as soon as possible.
Topical
Apply thin layer of 0.03% or 0.1% ointment to affected area bid. Rub in gently and completely. Stop drug when signs and symptoms resolve.
Pediatric patients
Children may require the larger dose; begin treatment at higher end of recommended adult dose.
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