Tacrolimus FK506

Brand Name





• Macrolide antibiotic with immunosuppressant properties

Mechanism of Action

• Binds to a T-cell binding protein and prevents synthesis of interleukin-2 and other lymphokines essential to T-lymphocyte function


• Prophylaxis of graft rejection in liver and kidney allogeneic transplantation

• It is recommended that tacrolimus be used concomitantly with adrenal corticosteroids


• Hypersensitivity to tacrolimus

• Hypersensitivity to HCO-60 (polyoxyl 60 hydrogenated castor oil) with IV formulation


• Increased incidence of posttransplant diabetes mellitus and insulin use at 24 months in kidney transplant recipients

• Neurotoxicity

• Nephrotoxicity

• Hyperkalemia

• Increased risk of infection and lymphomas

• Patients should be monitored closely for at least the first 30 minutes of therapy for signs of anaphylactic reactions


• Hypertension is a common occurrence with tacrolimus and may require treatment with antihypertensive agents. Since tacrolimus may cause hyperkalemia, potassium-sparing diuretics should be avoided

• Hyperglycemia may occur and require treatment

• Lower doses should be used in patients with renal insufficiencies

• Patients with hepatic impairment may have a higher risk of developing renal insufficiency

• Patients should be informed of the need for regular laboratory monitoring

• Pregnancy Category C

Adverse Events

• Headache • Hypomagnesemia

• Hypertension

• Renal dysfunction

Drug Interactions

Drugs with Synergistic Nephrotoxicity

• Tobramycin • Ketoconazole

• Cimetidine • Azapropazon

• Ranitidine

Appendix I

Tacrolimus (FK-506) (cont'd)

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