Drug Index

Mechanism :

Tacrolimus prolongs the survival of the host and transplanted graft in transplant models of liver, kidney, heart, bone marrow, small bowel and pancreas, lung and trachea, skin, cornea, and limb.

Indication :

  • Liver transplant
  • Renal transplant
  • Heart transplant
  • Atopic dermatitis

Contraindications :

Contraindicated in patients with a hypersensitivity to tacrolimus, to macrolides or any excipient, particularly polyoxymethylene hydrogenated castor oil, and in pregnancy. Patients with known sensitivity to similar compounds, or who are atopic should be monitored closely on commencing treatment. Particular care required in children <2 years of age who are initially EBV-seronegative‚ÄĒtherefore monitor EBV serology before starting and during treatment with tacrolimus. Routine monitoring of cardiovascular, visual, endocrine, renal, hematological and hepatic function is mandatory on commencement of treatment. Dose should be adjusted where clinically relevant changes are identified.

Dosing :

Heart transplant:
0.01 mg/kg/day IV continuous infusion. Subsequently 0.3 mg/kg/day oral, in 2 divided doses.
Liver transplant:
0.03-0.05 mg/kg/day by continuous IV infusion, then oral 0.15-0.2 mg/kg/day in 2 divided doses.
Renal transplant:
0.01 mg/kg/day by continuous IV infusion, then, oral 0.3 mg/kg/day in 2 divided doses.
Atopic dermatitis:
0.03% ointment: Thin layer to be applied to affected area every 12 hours. Discontinue when symptoms have cleared.

Adverse Effect :

Tremors, headache, infection, paresthesia, impaired renal function, constipation, asthenia, abdominal pain, hyperlipemia, dyspepsia, fever, arthralgia, back pain, diabetes, paresthesia, hypertension and hyperglycemia. Dyspnoea, dizziness, increased cough, rash, pruritus can occur. Susceptibility to bacterial, viral, fungal and/or protozoal infection is increased. EBV-associated lympho-proliferative disorders may occur. Impaired renal function, renal failure, hemolytic uremic syndrome (HUS) and tubular necrosis have been reported. In renal transplant recipients it is important to distinguish tacrolimus toxicity from signs of acute rejection. Anemia, coagulation disorders, thrombocytopenia, leucocytosis, leukopenia, pancytopenia, acidosis, hyper-and hypokalemia, hyperuricemia, hypocalcemia, hypomagnesemia, hypophosphatemia and hyponatremia.

Topical: Skin irritation, burning sensation, erythema, acne, herpes simplex, increased sensitivity to hot and cold, alcohol intolerance.

Interaction :

Cyclosporin: Half-life is increased in patients also receiving tacrolimus. Risk of nephrotoxicity is increased; concurrent use is not recommended.
Clotrimazole, Danazol, Dexamethasone, and Methylprednisolone: Interactions resulting in changes to blood/plasma levels of tacrolimus or the following have been reported.
Aminoglycosides, Amphotericin B, Co-Trimoxazole, Gyrase Inhibitors, NSAIDs and Vancomycin: Nephrotoxicity may be enhanced by concurrent administration.
Potassium-Sparing Diuretics: Risk of hyperkalemia.
Vaccinations: May be less effective. Live attenuated vaccines should be avoided.
Amphotericin B, Barbiturates, Bromocriptine, Carbamazepine, Corticosteroids, Cortisone, Cyclosporin, Diltiazem, Ergotamine, Erythromycin, Ethinylestradiol, Fluconazole, Isoniazid, Ketoconazole, Miconazole, Midazolam, Nifedipine, Phenytoin, Prednisolone, Rifampicin, Tamoxifen and Verapamil: Influence tacrolimus metabolism.
Warfarin and Phenytoin: Interactions with other drugs with a similarly high level of binding to plasma protein, such as warfarin and phenytoin should be considered likely.

Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-50Dose as in normal renal function
10-20Dose as in normal renal function
<10Dose as in normal renal function

Dose in Patients undergoing Renal Replacement Therapies
CAPDNot dialysed. Dose as in normal renal function
HDNot dialysed. Dose as in normal renal function
HDF/High fluxUnknown dialysability. Dose as in normal renal function
CAV/VVHDNot dialysed. Dose as in normal renal function

Hepatic Dose :

Metabolism of the drug is affected and plasma levels are increased, with prolongation of half-life. All of this can contribute to renal toxicity.
Severe hepatic impairment: Start with a dose lower than normal and monitor serum trough levels.
09/26/2020 21:52:34 Tacrolimus
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