tacrolimus at a glance
Medicine class
Calcineurin-inhibitor immunosuppressant
Main role
Preventing or treating rejection after organ transplantation
Administration
The selected concentrate is diluted and given by intravenous infusion by healthcare professionals
Monitoring
Blood tacrolimus concentration, kidney and liver function, potassium, glucose, blood pressure and blood count
What is tacrolimus used for?
The selected product is licensed for specialist transplant care.
Preventing rejection of a transplanted liver, kidney or heart.
Treating transplanted-organ rejection that has not responded to other immunosuppressants.
How does tacrolimus work?
Tacrolimus binds to FKBP12 inside cells. The resulting complex inhibits calcineurin, reducing T-cell activation and immune-signalling proteins involved in attacking a transplanted organ.
tacrolimus preparations and strengths
Solution for infusion
Route: Intravenous
Strengths: 5 mg/mL
How to take tacrolimus
The selected concentrate is prepared and administered in hospital. It must be diluted before intravenous infusion and must not be given as a bolus. Do not stop systemic tacrolimus without the transplant team's direction, as inadequate immunosuppression can allow organ rejection.
Healthcare professionals prepare and administer this formulation using compatible non-PVC equipment.
Avoid grapefruit and grapefruit juice while receiving tacrolimus.
Tell the transplant team before starting any prescription, non-prescription or herbal product.
tacrolimus side effects
Common or expected effects
- Tremor or headache
- Kidney-function impairment
- Raised blood glucose or diabetes
- Raised potassium
- Infections
- High blood pressure
- Difficulty sleeping
Get urgent medical advice
- Severe infection
- Serious allergic or infusion reaction
- Seizures, marked confusion or sudden visual disturbance
- Severe kidney impairment or greatly reduced urine
- Thrombotic microangiopathy, which may cause fever, unusual bruising, tiredness, jaundice, confusion or reduced urine
- Heart-rhythm disturbance
tacrolimus in pregnancy
Tacrolimus can be considered during pregnancy when a specialist judges it necessary; stopping effective anti-rejection treatment can be dangerous. Evidence remains limited. People planning pregnancy or who become pregnant should contact their transplant and maternity teams rather than stopping tacrolimus themselves. Maternal, pregnancy and newborn monitoring may be needed.
tacrolimus while breastfeeding
Tacrolimus passes into breast milk. The selected product information advises against breastfeeding during treatment, so feeding options should be discussed with transplant and maternity teams.
tacrolimus interactions
Tacrolimus has many clinically important interactions. Check new or discontinued medicines with the transplant team because blood concentrations can change quickly.
Strong CYP3A4 inhibitors, including clarithromycin, azole antifungals, ritonavir and cobicistat
They can sharply increase tacrolimus exposure and the risks of kidney, neurological and heart-rhythm toxicity.
CYP3A4 inducers, including rifampicin, carbamazepine and phenytoin
They can lower tacrolimus concentrations and increase the risk of transplant rejection.
Ciclosporin
Combined use should be avoided because tacrolimus exposure and kidney toxicity may increase.
Common questions about tacrolimus
Answers are fully visible for fast scanning and source review.
What is tacrolimus used for after an organ transplant?
It suppresses immune responses that would otherwise attack the transplanted organ. It can prevent rejection or treat rejection that has not responded to other immunosuppressants.
Is tacrolimus a steroid?
No. It is a calcineurin-inhibitor immunosuppressant, although it may be used alongside corticosteroids and other anti-rejection medicines.
Why are tacrolimus blood tests needed?
Exposure varies between people and can change with illness, formulation changes and interacting medicines. Monitoring helps balance rejection prevention against toxicity.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.