Tacrolimus
Indications
Tacrolimus is used for:
Prophylaxis of transplant rejection in liver, kidney or heart allograft recipients.
Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products
Adult Dose
Consult specialist literature
Child Dose
Renal Dose
Administration
Contra Indications
Hypersensitivity to tacrolimus or other macrolides;
Lactation
Precautions
Routinely monitor the following during the initial post-transplant period: blood pressure, ECG, neurological and visual status, fasting blood glucose levels, electrolytes (particularly potassium), liver and renal function tests, haematology parameters, coagulation values, and plasma protein determinations.
Herbal preparations e.g. St. John’s wort (Hypericum perforatum) may reduce blood concentrations of tacrolimus.
Diarrhoea episodes (monitor for changes in plasma concn of tacrolimus).
Avoid co-administration of ciclosporin and tacrolimus.
QT interval elongation.
Monitor for increased risk of opportunistic infections (bacterial, fungal, viral and protozoal).
Limit exposure to sunlight and UV light (wearing protective clothing and using a sunscreen with a high SPF).
May cause visual disturbances.
Pregnancy
Pregnancy-Lactation
Interactions
CYP3A4 inhibitors (e.g. ketoconazole, fluconazole, erythromycin, ritonavir may increase while the inducers (e.g. rifampicin, phenytoin or St. John’s Wort) may decrease plasma levels of tacrolimus.
Corticosteroids may reduce tacrolimus blood levels.
Tacrolimus is a CYP3A4 inhibitor may affect the metabolism of the substrates of this enzyme e.g. Ciclosporin, phenytoin, statins. May increase the nephrotoxic or neurotoxic effects of aminoglycosides, gyrase inhibitors, vancomycin, sulfamethoxazole+trimethoprim, NSAIDs, ganciclovir or aciclovir. May increase hyperkalaemia due to high potassium intake, or potassium-sparing diuretics (e.g., amiloride, triamterene, or spironolactone).
Avoid concomitant use of live attenuated vaccines.
May displace drugs with high affinity for plasma proteins (e.g., NSAIDs, oral anticoagulants, or oral antidiabetics).
Adverse Effects
Side effects of Tacrolimus :
Diarrhoea, nausea, abdominal pains, dyspepsia, constipation, flatulence, bloating and distension;
Tremor, headache, insomnia, anxiety, mood disorders, seizures, neuropathies, dizziness, other CNS disorders;
Renal & hepatic impairment;
Vision blurred, photophobia, eye disorders; Tinnitus;
Dyspnoea, pharyngitis, cough, nasal congestion;
Hyperglycaemia, diabetes mellitus, hyperkalaemia, electrolyte & lipid abnormalities, hyperuricaemia, appetite decreased, anorexia, metabolic acidoses;
Hypertension, tachycardia, blood disorders;
Pruritus, rash, alopecias, acne, sweating increased;
Arthralgia, muscle cramps, pain in limb, back pain;
Increased risk for infections;
Primary graft dysfunction;
Asthenia, febrile disorders, oedema, pain and discomfort, blood alkaline phosphatase increased, weight increased;
Allergic and anaphylactoid reactions