Tacrolimus
Tacrolimus is a medicine used to treat systemic lupus erythematosus (SLE), also known as lupus. Lupus is an inflammatory disease that affects different parts of the body.
Tacrolimus belongs to a group of medicines called calcineurin inhibitors. It works by blocking calcineurin, which helps lower the amount of interleukin-2—a molecule that increases T-cells which form part of the immune system.
In lupus, T-cells can become too active and cause the immune system to attack healthy tissues. Tacrolimus helps reduce this overactivity, preventing damage to the body.
Important things to remember
• You must see your rheumatologist regularly to make sure the treatment is working and check for possible side effects.
• You should have regular blood tests as suggested by your rheumatologist.
• It is important to tell your rheumatologist if you have a new serious illness such as a serious infection, cancer or heart failure.
• If you are worried about any side effects, you should contact your rheumatologist as soon as possible.
• If you stop tacrolimus for any reason, you must contact your rheumatologist. Failure to do so may mean that your treatment may no longer be funded.
• If you plan to become pregnant, it is important to discuss the timing with your rheumatologist.
What benefit can you expect from your treatment?
It may take a number of weeks for you to notice a difference in your symptoms.
Tacrolimus can improve many different body systems that are affected by lupus and you may see improvement in your arthritis, with less joint swelling and pain, as well as improvement in your skin if you have a rash.
Tacrolimus may also improve how well your kidneys are working, as well as how well your bone marrow produces platelets (cell fragments that help bleeding to clot).
Stopping tacrolimus
If tacrolimus treatment is stopped or delayed there is a risk that your condition will get worse again. Continue with your treatment unless advised by your rheumatologist or unless side effects develop (see Side effects).
If you stop tacrolimus for any reason, you must contact your rheumatologist.
How will you be monitored while on tacrolimus?
• Tacrolimus will only be given if your disease is active and if other treatments have not worked. It is not often used as a first-line treatment in Australia, unless you have lupus nephritis (kidney disease).
• Treatment will only continue if it helps your condition. This must be checked between 12 and 16 weeks after the start of treatment.
• Blood tests are needed during your treatment to monitor for side effects and to check if the treatment is working. The amount of tacrolimus in the blood is important and will be checked regularly by your treating doctor to make sure it is in the therapeutic range.
• How often you have blood tests will depend on what other medicines you are taking and what other illnesses you have. Your rheumatologist will advise on this.
How is tacrolimus given?
Tacrolimus is taken as an oral tablet, usually twice a day (morning and evening). It should be taken either 1 hour before or 2-3 hours after a meal (i.e. on an empty stomach) to maximise the absorption of the medicine. Each tablet should be taken as soon as it is opened from the blister and it should be taken with water.
If your lupus primarily affects your skin, tacrolimus is also available as a cream. This may reduce the risk of side effects.
What is the dosage?
The dose of tacrolimus differs between people but can be up to 8mg daily, usually divided into two doses (morning and evening dose).
If you miss a dose of tacrolimus, just take your next dose as planned. Don’t double up the dose to make up for the missed dose.
Can other medicines be given while taking tacrolimus?
Tacrolimus can interact with a lot of other medicines. Your prescriber will need to know a full list of the medicines (including over-the-counter medicines and supplements) you are currently taking. Some antibiotics and antifungals can change the amount of tacrolimus in your blood, so these will need to be checked before they are used.
Are there any side effects?
It is not uncommon to experience side effects with tacrolimus. The risk of side effects will be weighed against the potential benefit by your treating doctor.
Tell your doctor if you notice side effects that you think are caused by this medicine. Many side effects go away when tacrolimus treatment is reduced or stopped.
Common mild side effects
- Diarrhoea, cough, headache, hunger, thirst, joint pain, nausea, runny nose.
Serious side effects
• Hypertension (high blood pressure) is common in people taking tacrolimus. Your doctor will check your blood pressure regularly and may recommend that you check it yourself at home as well. In some people, medicine to control the blood pressure may be required.
• Impaired kidney function can occur. Your treating doctor will test your blood and urine regularly to ensure that any reduction in your kidney function is detected early.
• High potassium or low magnesium in the blood. Your doctor will check for these regularly.
• Cardiomyopathy (enlarged heart) can occur in some people taking this medicine. If you notice increased tiredness, shortness of breath, or start coughing up clear mucus, see your family doctor or go to the emergency department right away.
• Tacrolimus may increase your risk of diabetes mellitus (high blood sugar) which can result in damage to many different organs including your kidneys and eyes. Your doctor will test your blood sugar levels.
• Tacrolimus may increase your risk of skin cancer and lymphoma (cancer of the lymph nodes). It is important to have your skin checked regularly by your family doctor and have any suspicious skin changes looked at. If you notice any change to moles or other skin lesions, they should be checked by a health care professional. Using sunscreen, wearing hats and avoiding direct sunlight between 10am and 3pm can reduce chances of skin cancers. Avoid using tanning beds.
• This medicine may increase your risk of infections, which may need treatment. Tacrolimus may need to be stopped for a while if you have an infection, so it is important to contact your doctor for advice.
• To lower your risk of infection, avoid close contact with sick people and wash your hands regularly.
• Tacrolimus can cause abnormalities in your blood count and the blood vessels. Symptoms such as tiredness, easily bruising, fever, sore throat, dark/bloody urine, stroke symptoms, yellowing to the skin/eyes should be reviewed urgently by your GP or the emergency department of your local hospital.
• PRES (posterior reversible encephalopathy syndrome) is a rare neurological event that may occur in people taking this medicine, due to damage to the brain or nerves. If you notice any change in your vision, thinking, mood, personality, drowsiness, weakness etc, it must be reviewed by a medical professional.
• Tell your doctor or go to the hospital immediately if you have an allergic reaction as you need urgent medical attention.
Other side effects not listed in this leaflet may also occur. Tell your doctor if you notice any other side effects that you think might be caused by tacrolimus.
What precautions are necessary?
Infections
- If you have an active infection of any kind, treatment with tacrolimus will not be started until the infection is treated successfully.
Use with other medicines
- Tacrolimus can interact with a lot of other medicines. Some of these medicines can be continued, usually at a different dose. Other medicines cannot be used together with tacrolimus. You should tell all your doctors about all medicines you are taking or plan to take, especially if your GP starts any new medicines. This includes over the counter or herbal/naturopathic medicines.
Vaccines
- While being treated with tacrolimus you should not be immunised with ‘live’ vaccines such as: MMR (measles, mumps and rubella), Varicella vaccines (Chicken pox), OPV (oral polio virus), BCG (Bacillus Calmette Guerin), Japanese Encephalitis or Yellow Fever.
- Talk with your rheumatologist before receiving any vaccines.
- Pneumococcal, COVID-19 and the yearly seasonal flu vaccinations are encouraged.
- For more information on vaccination including the COVID-19 vaccination go: here
Surgery
- Surgery If you require surgery for any reason, you should discuss this with your rheumatologist as some people need to stop taking tacrolimus before surgery.
Alcohol
- Alcohol can interact with tacrolimus, causing the levels in the blood to be unstable. Whilst alcohol can be used while taking tacrolimus, it is important to let your doctor know if your use is increasing. It is important to be honest with your doctor about your use of alcohol in case dosage adjustment is required.
Use in pregnancy and when breastfeeding
- If you are pregnant or plan to become pregnant it is extremely important to discuss this with your rheumatologist before beginning this medicine.
- Women who can become pregnant should use effective contraception while taking tacrolimus. Use of tacrolimus is not recommended in men who are trying to become fathers.
- Women who are breastfeeding should talk to their doctor about taking tacrolimus.
- More detailed information is available here.
How to store tacrolimus
- • Store tacrolimus at room temperature (avoid freezing), in a closed container, away from heat, moisture and direct sunlight.
- Keep all medicines out of reach of children.
- Return any out-of-date medicine to your pharmacy.
For more information see the Tacrolimus- printable information sheet
This Information Sheet has been prepared using materials obtained from various sources which have been reviewed by the Australian Rheumatology Association (ARA). It contains general information only and does not contain a complete or definitive statement of all possible uses, actions, precautions, side effects or interactions of the medicines referenced. This information is not intended as medical advice for individual conditions nor for making an individual assessment of the risks and benefits of taking a particular medicine. Decisions regarding the assessment and treatment of patients are the sole responsibility of the treating medical professional, exercising their own clinical judgment and taking into account all of the circumstances and the medical history of the individual patient.
ARA has used all reasonable endeavours to ensure the information on which this Information Sheet is based is accurate and up to date. However, the ARA accepts no responsibility or liability for the accuracy, currency, reliability and/or completeness of the information contained in this Information Sheet. To the maximum extent permitted by law, the ARA expressly disclaims any liability for any injury, loss, harm or damage arising from or in connection with use of and reliance on the information contained in this Information Sheet.
This information sheet is copyright and may be reproduced in its entirety but may not be altered without prior written permission from the ARA.
Page updated February 2025
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