Tacrolimus

Category: pharmacological

Aliases: FK-506, Prograf, Advagraf

Pharmacological Mechanism

Binds FKBP-12 → inhibits calcineurin → same T-cell IL-2 suppression mechanism as cyclosporine but ~100× more potent per mg. CYP3A4 + P-gp substrate — interaction list as severe as cyclosporine. Displaced cyclosporine as preferred transplant immunosuppressant.

Half-Life (t½)

PO: 12h, IV: 12h

Dosing Guidelines

• PO: Typical 0.167mg (Range: 0.1 - 0.3 mg)
• IV: Typical 0.167mg (Range: 0.1 - 0.3 mg)
• TD: Typical 0.167mg (Range: 0.1 - 0.3 mg)

Target Organ Systems

• digestive
• immune-hematologic

Interactions

• Schisandra
• St. John's Wort