Tacrolimus

Question 1

What is tacrolimus

Answer 1

Calcineurin inhibitor with a similar profile to ciclosporin

Question 2

What are the warning signs of tacrolimus

Answer 2

Neurotoxicity- tremor and headache

Nephrotoxicity- elevated serum creatinine concentrations

Eye disorders- blurred vision, photophobia

Skin disorders- rash, toxic epidermal necrolysis

Blood disorders- signs of infection like fever, sore throat, mouth ulcers, also unexplained bruising or bleeding

Hyperglycaemia- diabetes mellitus, increased thirst or urination

Cardiovascular disorders- cardiomyopathy, arrhythmias, hypertension

Liver toxicity- jaundice, nausea, vomiting, abdominal discomfort, dark urine

Question 3

What should you monitor for in tacrolimus

Answer 3

Blood pressure

ECG- cardiomyopathy (discontinue if occurs)

Fasting blood glucose concentration

Renal function

Liver function

Serum electrolytes (particularly K+)

Haematological, neurological (including visual) and coagulation parameters

Question 4

What is the advice for tacrolimus in pregnancy

Answer 4

Avoid risk of premature delivery

Question 5

What are the other points you should be aware of in tacrolimus

Answer 5

Avoid excess exposure to UV light (use a wide spectrum sunscreen)

Ensure the patient understands the importance of taking immunosuppressants daily

It may affect the performance of skilled tasks like driving

Should not receive immunisation with live vaccines

Avoid a high potassium diet and grape fruit juice

Switching between oral tacrolimus products has been associated with toxicity and graft rejection- should only be prescribed by brand name

Question 6

What are the main interactions involved with tacrolimus

Answer 6

Increased plasma concentration with clarithromycin, diltiazem, erythromycin, fluconazole, grape fruit juice, itraconazole, nifedipine, omeprazole, ranolazine

Reduced plasma concentration with phenobarbital, st john’s wort, rifampicin, phenytoin

Increased nephrotoxicity when given with aminoglycosides, amphotericin and NSAIDS (ibuprofen), certain antivirals (aciclovir)

Plasma concentration of ciclosporin increased

Increased hyperkalaemia risk when given with potassium-sparing diuretics (amiloride, spironolactone), K+ salts, angiotensin II receptor antagonist