Tacrolimus FK506
Brand Name |
Prograf® |
Company |
Fujisawa |
Class |
• 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 |
Indications |
• Prophylaxis of graft rejection in liver and kidney allogeneic transplantation • It is recommended that tacrolimus be used concomitantly with adrenal corticosteroids |
Contraindications |
• Hypersensitivity to tacrolimus • Hypersensitivity to HCO-60 (polyoxyl 60 hydrogenated castor oil) with IV formulation |
Warnings |
• 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 |
Precautions |
• 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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