Indication

Tacrograt (Tacrolimus) is a calcineurin inhibitor immunosuppressant indicated for the prevention of organ rejection in adult and pediatric patients undergoing:

Liver transplantation
Kidney transplantation
Heart transplantation
Lung transplantation

It is used in combination with other immunosuppressive agents.

Pharmacology

Tacrolimus binds with the intracellular protein FKBP-12 and inhibits calcineurin activity. This results in:

Suppression of T-lymphocyte activation and proliferation
Reduced cytokine production (IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8, IL-10, TNF-α, IFN-γ, etc.)
Inhibition of T-cell dependent B-cell responses
Overall immunosuppressive effect that helps prevent organ rejection

Dosage & Administration

Oral therapy should be started when the patient can tolerate oral medication.
Liver, heart, and lung transplant patients: First dose should be given no earlier than 6 hours after transplantation.
Kidney transplant patients: First dose may be given within 24 hours after transplantation, but administration should be delayed until renal function recovers.

Adult Initial Oral Dose

Kidney Transplant

With Azathioprine: 0.2 mg/kg/day
With MMF/IL-2 receptor antagonist: 0.1 mg/kg/day

Liver Transplant

With corticosteroids only: 0.10-0.15 mg/kg/day

Heart Transplant

With Azathioprine or MMF: 0.075 mg/kg/day

Lung Transplant

With Azathioprine or MMF: 0.075 mg/kg/day

Daily doses should be administered every 12 hours.

Pediatric Initial Oral Dose

Kidney Transplant

0.3 mg/kg/day

Liver Transplant

0.15-0.2 mg/kg/day

Heart Transplant

0.3 mg/kg/day

Lung Transplant

0.3 mg/kg/day

Daily doses should be administered every 12 hours.

Important Note

In lung transplant patients with cystic fibrosis, oral tacrolimus bioavailability may be reduced. Higher doses may be required to achieve target trough concentrations. Therapeutic drug monitoring is recommended.