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Last updated: Acute Kidney Injury…
on 10 Apr 2017

Tacrolimus



Indication
  • Prophylaxis of transplant rejection in liver, kidney or heart allograft recipients
  • Treatment of allograft rejection. Also used for some auto-immune diseases e.g. minimal change disease
Preparations
  • Immunosuppressive agent. Calcineurin Inhibitor
  • Prograf® - a twice daily preparation; capsules 0.5 mg, 1 mg, 5 mg; IV infusion 5 mg/ml
  • Advagraf® - a slow release once daily preparation
  • Also available as Vivadex®, Adoport®, Tacni® - all twice daily preparations. Modigraf® granules for oral suspension - twice daily
  • Prescribe by brand. Do not switch between brands
Contraindications
  • Hypersensitivity to tacrolimus or other macrolides or to any of the excipients
Cautions
  • Monitor creatinine. Nephrotoxic, use with caution with other nephrotoxic agents
  • Monitor tacrolimus levels (trough): initially 8-15 ng/ml, maintenance 5-10 ng/ml. Second dose conventionally given at 6pm to allow to dose adjustment after levels are known. Twice daily preparations should ideally be given 12 hours apart
  • Monitor LFTs
     
  • Monitor FBC; microangiopathic haemolytic anaemia (MAHA)/haemolytic uraemic syndrome (HUS)
  • Use of live vaccines should be avoided
Side-effects
  • Increased risk of infection and malignancies (esp lymphoma, skin and cervical cancer)
  • Bone marrow suppression. Tremor, headache, peripheral neuropathy, neuro-psychiatric syndromes, tinnitus, cough, diarrhoea, acne, hepatic dysfunction, alopecia (vs hirsutism with ciclosporin), hypertension
  • Diabetes mellitus (occurs in up to 30% of patients; early switch to ciclosporin may prevent further pancreatic damage), hyperkalaemia, hyponatraemia and nephrotoxicity

Note: microangiopathic haemolytic anaemia (MAHA)/haemolytic uraemic syndrome (HUS) is well recognised; this can be atypical, eg thrombocytopenia or anaemia mild or absent

Dose
  • Kidney transplant – 0.15-0.3 mg/kg/day. Take the bigger dose in the morning if using a BD preparation
  • Intravenous – give one fifth of the total daily dose as a continuous infusion over 24 hours – monitor levels, interpretation is difficult
  • Prescribe by brand, do not switch between brands unless done in a controlled way
Dose in renal impairment
  • As in normal renal function. Not dialysed by PD, HD, CVVH
Interactions
  • Levels ↑ by macrolides, fluconazole, theophylline, diltiazem, verapamil and caspofungin
  • Levels ↓ by isoniazid, rifampicin, St Johns Wort, carbamazepine, phenytoin
  • Care with other nephrotoxic drugs
  • Increase risk of hyperkalaemia with other potassium sparing diuretics and potassium salts
How to Prescribe View Details
Patient comment
  • Always take the same brand, do NOT swap brands without your doctor asking you to
  • Take tacrolimus consistently either on an empty stomach (one hour before or two hours after food), or with meals
  • Avoid grapefruit juice
  • When coming to clinic do not take your morning dose until after you have had your bloods taken – bring a dose to clinic with you
  • If you suffer from an episode of diarrhoea it is advisable to get your creatinine and tacrolimus levels checked
  • There is an increased risk of infection and certain cancers (including skin and cervical)
  • Avoid sunbathing, use high factor sun cream and women should attend for yearly cervical smears
  • Avoid live vaccines – ask your pharmacist

    Note: Warn women re hair loss
     

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