Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action unclear. Tacrolimus bind to cytosolic receptors known as immunophilins (i.e., cyclophilin and FK binding protein-12 [FKBP-12], respectively), forming complexes that inhibit the production of cytokines via the calcineurin pathway. Inhibition of calcineurin activity inhibits early activation of T-cells (ie.immunosuppresion results).
Tacrolim 0.1% Ointment
Prophylaxis of rejection in kidney graft transplant:
Adult: Initially, 0.2-0.3 mg/kg/day in 2 divided doses every 12 hr. Begin oral dose within 24 hr of transplant.
Prophylaxis of rejection in liver graft transplant:
Adult: Initially, 0.1-0.2 mg/kg/day in 2 divided doses every 12 hr. Start treatment 12 hr after transplantation.
Child: Initially, 0.15-0.20 mg/kg/day in 2 divided doses every 12 hr. Begin no sooner than 6 hr after transplant.
Prophylaxis of cardiac graft rejection:
Adult: With or without antibody induction: Starting within 5 days of transplantation but no earlier than 6 hr after transplantation. 75 mcg/kg daily in 2 divided doses.
Fistulising Crohn’s disease:
Adult: 200 mcg/kg/day in 2 divided doses for 10 wk.
Adult: >15 yr: Apply thinly 0.03% or 0.1% ointment to affected area bid. Rub in gently and completely. For short-term and intermittent use only. If no improvement after 6 wk, re-confirm diagnosis.
Child: 2-15 yr: Apply thinly 0.03% oint to affected area bid. Rub in gently and completely. For short-term and intermittent use only.