To measure the concentration of tacrolimus in the blood in order to establish the correct dose, maintain therapeutic levels and detect toxic levels
As soon as tacrolimus therapy begins, frequently at first then at regular intervals to monitor concentrations over time
A blood sample taken from a vein in your arm
Have the sample collected 12 hours after the last dose and/or immediately prior to the next dose or as directed by your doctor
This test measures the amount of tacrolimus in the blood. Tacrolimus is an immunosuppressive drug that is given orally or intravenously to patients who have had a kidney, liver, heart, or other organ transplant. It is a powerful drug that helps to prevent rejection of the transplanted organ by the body. Normally, a person’s immune system would recognise the new organ as foreign and begin to attack it. Tacrolimus limits this response and helps to prevent organ rejection by reducing the activity of certain immune cells called T-lymphocytes.
Tacrolimus levels in the blood must be kept within a narrow therapeutic range. If the concentration is too low organ rejection may occur, if it is too high then the person may have symptoms associated with toxicity. Dosages must be adjusted to an individual. Often people will begin with higher doses of tacrolimus at the start of therapy and then decrease the dose over the next few weeks. Tacrolimus is usually taken twice a day at set intervals before or after meals. When a person takes a dose, blood concentrations rise and peak within about 2 to 3 hours then begin to slowly fall. The blood test is usually measured as a “trough” level. It is timed so that the collection is 12 hours after the dose, and/or prior to the next dose – at the drug’s lowest concentration in the blood.
How is the sample collected for testing?
A blood sample is obtained by inserting a needle into a vein in the arm.
Is any test preparation needed to ensure the quality of the sample?
Have the blood sample collected 12 hours after the last dose and/or immediately prior to the next dose or as directed by your doctor
How is it used?
The tacrolimus test is requested to measure the amount of drug in the blood to find out whether concentrations have reached therapeutic levels and are below toxic levels. It is important to monitor levels of tacrolimus for several reasons:
- There is not a good relationship between the dose of tacrolimus given and level of drug in the blood.
- Absorption and metabolism of oral doses of tacrolimus can vary greatly between patients and even in the same patient depending on the time of the dose and what, if any food has been eaten.
- Tacrolimus can cause kidney damage, especially in high doses. Measuring levels in people who have had a kidney transplant may help to distinguish between kidney rejection (levels in the blood are low) and kidney damage due to tacrolimus toxicity (levels in the blood are high).
Tacrolimus monitoring helps ensure that each individual is receiving the right amount of drug needed to treat his or her particular case.
When is it requested?
Tacrolimus is requested frequently at the start of therapy, often daily when trying to establish an appropriate dosing regimen. Once dosages have been established and shown to be well tolerated then the frequency of tacrolimus testing may be decreased. The test is performed when dosages are changed and whenever patients have symptoms that suggest side effects, toxicity or organ rejection.
- Kidney damage (nephrotoxicity)
- Tremors, headache (neurotoxicity)
- High blood pressure
- Nausea and vomiting
- Electrolyte disturbances, such as high potassium concentrations (hyperkalaemia)
- Tinnitus -intermittent and/or persistent ringing or roaring in the ears
Monitoring at intervals is necessary as long as the patient is taking tacrolimus.
What does the test result mean?
Concentrations that are higher than the established therapeutic range may increase the risk of associated toxicity, including damage to the kidneys and nerves. Concentrations that are too low may lead to rejection of the transplanted organ. Side effects may be seen at any dosage but tend to be more severe with higher tacrolimus levels.
The therapeutic range established by a laboratory will depend on both the method used to measure the drug and the type of transplant. Results from different methods are not interchangeable. A doctor will usually have his patients samples sent consistently to the same laboratory and will be guided by that laboratory’s therapeutic ranges.
Is there anything else I should know?
A variety of drugs, such as calcium channel blockers, antifungal drugs, macrolide antibiotics (such as erythromycin), protease inhibitors, chloramphenicol, and another immunosuppressant such as ciclosporin can increase tacrolimus concentrations. Drugs such as anticonvulsants (carbamazepine, phenytoin), antimicrobials (rifampin), and the immunosuppressant sirolimus can decrease tacrolimus concentrations.
Grapefruit juice and herbal supplements such as St. John’s Wort should be avoided while taking tacrolimus.
Tacrolimus may be given for a period of time to patients who have had bone marrow transplant. Topical tacrolimus may be used to treat a variety of skin conditions, such as eczema, that have not responded well to other medications. This topical use of tacrolimus is intended to be local, not systemic, and is not usually monitored. In some countries, tacrolimus is also licensed for use as a treatment for myasthenia gravis.
Patients should not alter their dose or the time that they take their dose without consulting their doctor. Tacrolimus should be taken consistently with respect to meals. Food, especially high fat meals can significantly reduce the bioavailability (amount of the drug that reaches the circulation) compared with fasting. Women who are pregnant or planning to become pregnant should talk to their doctor about associated risks.
How long will I need to be on tacrolimus?
Transplant patients must take tacrolimus or a different immunosuppressant (or combination of drugs) throughout their life. Talk to your doctor about the best choice for your condition. This choice may change over time.
Who requests tacrolimus tests?
Tacrolimus will usually be monitored by the doctor and transplant team that performed your surgery, or by a doctor that has specific knowledge of the condition or disease for which the drug is prescribed.
Should I tell my other health care providers that I am taking tacrolimus?
Yes, this is important information for them, partially because of drug interactions and partially because of the immunosuppressive action of tacrolimus. It can affect your ability to heal, to tolerate vaccinations, and may increase the risk of developing certain cancers (such as skin cancers).