Tacrolimus

Indications
 Oral
Prophylaxis of rejection in kidney graft transplant
Adult: Initially, 0.2-0.3 mg/kg/day in 2 divided doses every 12 hr. Begin oral dose within 24 hr of transplant.
Renal impairment: Dose reduction needed.
Hepatic impairment: Severe impairment (Child-Pugh score of ≥10): Use lower dosages and close monitoring of blood concentrations needed.
Oral
Prophylaxis of rejection in liver graft transplant
Adult: Initially, 0.1-0.2 mg/kg/day in 2 divided doses every 12 hr. Start treatment 12 hr after transplantation.
Child: Initially, 0.15-0.20 mg/kg/day in 2 divided doses every 12 hr. Begin no sooner than 6 hr after transplant.
Renal impairment: Dose reduction needed.
Hepatic impairment: Severe impairment (Child-Pugh score of ≥10): Use lower dosages and close monitoring of blood concentrations needed.
Oral
Fistulising Crohn's disease
Adult: 200 mcg/kg/day in 2 divided doses for 10 wk.
Renal impairment: Dose reduction needed.
Hepatic impairment: Severe impairment (Child-Pugh score of ≥10): Use lower dosages and close monitoring of blood concentrations needed.
Oral
Prophylaxis of cardiac graft rejection
Adult: With or without antibody induction: Starting within 5 days of transplantation but no earlier than 6 hr after transplantation. 75 mcg/kg daily in 2 divided doses.
Intravenous
Prophylaxis of rejection in kidney graft transplant
Adult: Initially, 0.05-0.1 mg/kg/day as a continuous infusion over 24 hr. Start within 24 hr of transplantation for up to a max of 7 days, then transfer to oral treatment.
Renal impairment: Dose reduction needed.
Hepatic impairment: Severe impairment (Child-Pugh score of ≥10): Use lower dosages and close monitoring of blood concentrations needed.
Intravenous
Prophylaxis of rejection in liver graft transplant
Adult: Initially, 10-50 mcg/kg/day as a continuous infusion over 24 hr. Start treatment 12 hr after transplantation and continue for up to a max of 7 days. Transfer to oral therapy as soon as patient is able to tolerate; 1st oral dose should be given 8-12 hr after stopping infusion.
Child: Initially, 0.03-0.05 mg/kg/day as a continuous infusion over 24hr. Begin no sooner than 6 hr post-transplant, starting at the lower end of the dosage range. Continue until the oral medication can be tolerated. Oral therapy should start 8-12hr after IV infusion discontinued.
Renal impairment: Dose reduction needed.
Hepatic impairment: Severe impairment (Child-Pugh score of ≥10): Use lower dosages and close monitoring of blood concentrations needed.
Intravenous
Prophylaxis of cardiac graft rejection
Adult: With or without antibody induction: Starting within 5 days of transplantation but no earlier than 6 hr after transplantation. 10-20 mcg/kg daily via infusion over 24 hr, for up to a max of 7 days. Transfer to oral therapy as soon as patient is able to tolerate; 1st oral dose to be given 8-12 hr after stopping infusion.
Topical/Cutaneous
Atopic dermatitis
Adult: >15 yr: Apply thinly 0.03% or 0.1% ointment to affected area bid. Rub in gently and completely. For short-term and intermittent use only. If no improvement after 6 wk, re-confirm diagnosis.
Child: 2-15 yr: Apply thinly 0.03% oint to affected area bid. Rub in gently and completely. For short-term and intermittent use only.

Special Populations: In renal impairment, patients should receive the lowest value of the recommended IV and oral dosing ranges. Further reductions in dose < these ranges may be required. For patients with postoperative oliguria, therapy should be delayed up to 48 hrs or longer. In hepatic impairment, patients should be monitored closely and dosing adjustments considered.

Reconstitution: Dilute concentrate with 0.9% sodium chloride or 5% dextrose injection to a concentration of 4-20 mcg/ml . Diluted solution may be stored in polyethylene or glass containers for up to 24 hr. Diluted infusion solution must not be stored in a PVC container due to reduced stability and potential for extraction of phthalates.
Incompatibility: Do not use plasticized polyvinyl chloride (PVC) container as stability of the solution is decreased and polyoxyl 60 hydrogenated castor oil contained in the formulation may leach phthalates from PVC containers. Tacrolimus injection should not be mixed or co-infused with solutions of pH 9 or greater due to chemical instability in alkaline media.
Contraindications
 Hypersensitivity, lactation.
Warnings / Precautions
 Monitoring of blood trough serum concentrations to prevent organ rejection and to reduce drug-related toxicity. Topical: Used with caution on the face or neck, large areas of the body (not >50% of the total BSA), or areas of broken skin. Infections at the treatment site should be cleared prior to therapy. Delay use in patients with unknown cause of lymphadenopathy or acute infectious mononucleosis till resolution. Use in patients with Netherton's syndrome is not recommended. Pregnancy.
Adverse Reactions
 Systemic: Tremor, headache, paraesthesias, nausea and diarrhoea, hypertension, blood dyscrasias, leucocytosis, impaired renal function, serum electrolyte disturbances, infectious complications. Mood changes, sleep disturbances, confusion, dizziness, tinnitus, visual disturbances convulsions, alterations in glucose metabolism, ECG changes, tachycardia, myocardial hypertrophy, constipation, dyspepsia and GI haemorrhage; dyspnoea, asthma, pleural effusions; alopoecia, hirsutism, skin rash and pruritus; myalgia, spasm, leg cramps, peripheral oedema, liver dysfunction and coagulation disorders. Topical: Burning, stinging, soreness, pruritus, skin disorders, headache and flu-like symptoms. Increased incidence of malignancy.
Potentially Fatal: Nephrotoxicity, neurotoxicity and anaphylactic reaction.
Drug Interactions
 Increased nephrotoxicity with ciclosporin, aminoglycosides, amphotericin B, cisplatin, NSAIDs, vancomycin, co-trimoxazole, aciclovir, ganciclovir. Increased risk of hyperkalemia with potassium-sparing diuretics. Increased plasma concentrations and toxicity with azole antifungals, calcium-channel blockers, cimetidine, danazol, HIV-protease inhibitors, macrolide antibacterials and metoclopramide. Antacids, rifampin, rifabutin, casofungin, phenytoin, phenobarbital and carbamazepine decrease tacrolimus plasma concentrations. Concurrent admin of sirolimus and tacrolimus decrease levels of both.
See Below for More tacrolimus Drug Interactions
Food Interactions
 Food decreases rate and extent of absorption. Grapefruit and pomelo juice may increase the serum levels. St John's wort may decrease serum levels.
Mechanism of Actions
 Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action unclear. Tacrolimus bind to cytosolic receptors known as immunophilins (i.e., cyclophilin and FK binding protein-12 [FKBP-12], respectively), forming complexes that inhibit the production of cytokines via the calcineurin pathway. Inhibition of calcineurin activity inhibits early activation of T-cells (ie.immunosuppresion results).
Absorption: Incomplete and variable. Food decreased rate and extent of tacrolimus absorption.
Distribution: 99% bound to plasma protein, mainly to albumin and alpha-1-acid glycoprotein, and has a high level of association with erythrocytes.
Metabolism: Extensively metabolized by cytochrome P-450 system (CYP3A).
Administration
 Should be taken on an empty stomach. (Take on an empty stomach at least 1 hr before or 2-3 hr after meals. Avoid grapefruit & grapefruit juice.)
Storage Conditions
 Topical/Cutaneous: Store at 15-30°C.
ATC Classification
 L04AD02 - tacrolimus ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.
D11AX14 - 他克莫司 ;
Storage
 Topical/Cutaneous: Store at 15-30°C.
Available As
  • Tacrolimus 0.03%
  • Tacrolimus 0.03% w/w
  • Tacrolimus 0.1%
  • Tacrolimus 0.1% w/w
  • Tacrolimus 0.3 mg
  • Tacrolimus 0.3% w/w
  • Tacrolimus 0.5 mg
  • Tacrolimus 1 mg
  • Tacrolimus 2 mg
  • Tacrolimus 5 mg

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