BMA Concise Guide to Medicine & Drugs


Brand names Adoport, Advagraf, Modigraf, Perixis, Prograf, Protopic

Used in the following combined preparations None


Drug group Immunosuppressant drug

Overdose danger rating Medium

Dependence rating Low

Prescription needed Yes

Available as generic No


Tacrolimus is an immunosuppressant used in many types of organ transplants to help prevent rejection. It is usually used in combination with other immunosuppressants. Tacrolimus may also be used topically to treat moderate to severe eczema when other drugs are inappropriate or have been unsuccessful. As tacrolimus suppresses the immune system when taken by mouth or injected, it increases susceptibility to infection and it can also cause kidney damage. Tacrolimus should not be taken by people who are allergic to any macrolide antibiotic. If you are taking oral tacrolimus, it is important to always use the same formulation as they are not all interchangeable.


Your drug prescription is tailored for you. Do not alter dosage without checking with your doctor.

How taken/used Capsules, SR capsules, granules, liquid, injection, ointment.

Frequency and timing of doses Oral and injected preparations 1–2 x daily. Oral preparations should be taken on an empty stomach or 2–3 hours after a meal. Topical preparation Initially 1–2 x daily; reduced to 2 x weekly when eczema improves.

Dosage range Oral and injected preparations Dosage is calculated on an individual basis. Topical preparation 0.1% or 0.03% ointment (adults); 0.03% ointment (children).

Onset of effect Within 12 hours (oral and injection). 1–2 weeks (ointment).

Duration of action 2–4 days.

Diet advice If taking tacrolimus orally, avoid high-potassium foods and grapefruit juice. No special restrictions for other preparations.

Storage Store at room temperature and protect from moisture. Keep out of the reach of children.

Missed dose Take as soon as you remember, unless your next dose is due within 12 hours, in which case omit the missed dose and take the next dose as scheduled. Do not double your next dose.

Stopping the drug Do not stop the drug without consulting your doctor. If it is being taken after a transplant, stopping may lead to organ rejection. If the drug is being used for eczema, stopping may lead to recurrence or worsening of symptoms.

Exceeding the dose An occasional unintentional dose is unlikely to cause major problems. Large oral overdoses may cause tremor, headache, vomiting, and kidney damage. Notify your doctor.


Used topically, tacrolimus may cause local irritation, rash, or pins and needles (paraesthesia); discuss with your doctor if these occur. Taken orally, common side effects include nausea, difficulty in sleeping or drowsiness, diarrhoea, headache, tremor, and generalized paraesthesia; discuss with your doctor if nausea, sleeping problems, or drowsiness are severe or if any of the other symptoms occur. If you experience spontaneous bruising or bleeding, fever, or a sore throat, seek immediate medical attention. Long-term use of the drug may cause other adverse effects (see Prolonged use).


General note Many drugs may affect the level of tacrolimus. Check with your doctor before taking any new medication.

Grapefruit juice and St John’s wort can affect blood levels of tacrolimus and should be avoided if taking the drug orally or by injection. If tacrolimus is being taken after a transplant, the interaction with St John’s wort can cause organ rejection.

Vaccines Tacrolimus may affect your response to vaccines. Discuss with your doctor before having a vaccine.


Tacrolimus is prescribed only under medical supervision, but be sure you tell your doctor if:

· You have long-term kidney or liver problems.

· You have lactose intolerance.

· You suffer from peanut or soya allergy.

· You are pregnant or planning a pregnancy.

· You are taking other medicines.

Pregnancy Safety not established. Discuss with your doctor.

Breast-feeding Safety not established. Discuss with your doctor.

Infants and children Used only by specialist children’s doctors.

Over 60 No special problems.

Driving and hazardous work If taking tacrolimus orally, avoid such activities until you know how the drug affects you. It may cause drowsiness. No known problems with topical use.

Alcohol Avoid. Alcohol may increase drowsiness (oral tacrolimus), or cause skin irritation (topical tacrolimus).

Sunlight and sunbeds Avoid prolonged, unprotected exposure as this can increase the risk of skin cancer.


Long-term oral or injected tacrolimus can affect kidney and/or liver function, increases susceptibility to infection, and is associated with an increased risk of some skin and lymphoid cancers. Prolonged use may also increase the chance of high blood pressure or diabetes. Topically, the drug is associated with herpes skin infections (e.g. cold sores); there may also be an increased risk of skin cancer.

Monitoring For oral or injected tacrolimus, regular blood tests, tests of kidney and liver function, and checks of blood presure and for diabetes should be carried out.