Tacrolimus

Administration

  • Type: immunosuppressant
  • Dosage Forms: 0.5,1,5
  • Routes of Administration: PO, topical, IV
  • Common Trade Names:Prograf

Adult Dosing

Heart transplant rejection prophylaxis

  • 0.075mg/kg/day PO divided q12h
  • Start: >6h post-transplant; Info: adjust dose based on serum levels

Liver transplant rejection prophylaxis

  • 0.1-0.15mg/kg/day PO divided q12h
  • Start: >6h post-transplant; Info: adjust dose based on serum levels

Kidney transplant rejection prophylaxis

  • 0.1-0.2mg/kg/day PO divided q12h
  • Start: within 24h post-transplant; delay if renal function not adequate; Info: adjust dose based on serum levels

Pediatric Dosing

Liver transplant rejection prophylaxis

  • 0.15-0.2mg/kg/day PO divided q12h
  • Start: >6h post-transplant; Info: adjust dose based on serum levels

Special Populations

  • Pregnancy Rating: Pregnancy Category C
  • Lactation risk: possibly unsafe

Renal Dosing

  • Adult:
    • kidney transplant: give lowest recommended dose, may consider further dose decrease; postop oliguria: start 6-24h post-transplant; may delay until renal function adequate; HD: not defined
    • all other transplants: give lowest recommended dose, may consider further dose decrease; HD: not defined
  • Pediatric: give lowest recommended dose, may consider further dose decrease; HD: not defined

Hepatic Dosing

  • Adult: give lowest recommended dose, may consider further dose decrease; Child-Pugh Score >10: decrease dose, amount not defined
  • Pediatric: give lowest recommended dose, may consider further dose decrease; Child-Pugh Score >10: decrease dose, amount not defined

Contraindications

  • Allergy to class/drug
  • hypersensitivity to castor oil derivatives (IV form)
  • liver transplant use (ER cap form)
  • electrolyte abnormalities, uncorrected
  • congenital long QT syndrome
  • caution if QT prolongation
  • caution if QT prolongation family history
  • caution if torsades de pointes history
  • caution if ventricular arrhythmias
  • caution if bradycardia
  • caution if recent MI
  • caution if CHF
  • caution in female patients
  • caution in Black patients
  • caution in Hispanic patients
  • caution if renal impairment
  • caution if hepatic impairment

Adverse Reactions

Serious

  • immunosuppression
  • malignancy
  • lymphoma
  • post-transplant lymphoproliferative disorder
  • infection, severe
  • CMV
  • PML
  • BK virus-assoc. nephropathy
  • Stevens-Johnson syndrome
  • toxic epidermal necrolysis
  • anaphylaxis
  • nephrotoxicity
  • neurotoxicity
  • posterior reversible encephalopathy syndrome
  • seizures
  • myocardial hypertrophy
  • pericardial effusion
  • QT prolongation
  • torsades de pointes
  • hyperkalemia, severe
  • hypertension, severe
  • diabetes mellitus
  • myelosuppression
  • DIC
  • thrombocytopenic purpura
  • hemolytic anemia
  • pure red cell aplasia

Common

  • tremor
  • diarrhea
  • headache
  • hypertension
  • Creatinine increase
  • infection
  • nausea/vomiting
  • insomnia
  • pain
  • hypophosphatemia
  • constipation
  • asthenia
  • edema, peripheral
  • hypomagnesemia
  • fever
  • anemia
  • diabetes mellitus/hyperglycemia
  • paresthesia
  • LFTs elevated
  • hyperlipidemia
  • hyperkalemia
  • anorexia
  • dyspepsia
  • arthralgia
  • dyspnea
  • pruritus/rash
  • hypokalemia
  • dizziness
  • cough
  • leukopenia
  • photosensitivity
  • bronchitis

Pharmacology

  • Half-life: 3.5-40.6h; 23.6h (heart transplant patients), 18.8h (kidney transplant patients), 11.7h (liver transplant patients); Info: prolonged half-life in hepatic impairment
  • Metabolism: liver extensively; CYP450: 3A4 substrate
  • Excretion:feces 92.4%, urine 2.3% (<1% unchanged)

Mechanism of Action

Macrolide calcineurin inhibitor, inhibits T-lymphocyte activation

References

    epocrates

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