Tacrolimus (Advagraf | Prograf)
Tacrolimus is a medication that treats rheumatic diseases by suppressing the immune system.
Tacrolimus is used to treat rheumatoid arthritis, as well as immune disorders of the eyes, lungs, muscles, skin, nerves, and blood vessels. Tacrolimus is also used to help prevent organ rejection in transplant patients.
Tacrolimus works by reducing the activity of T-cells, a type of white blood cell that plays an important part in the body’s immune system.
Taking Tacrolimus
Tacrolimus is available as Prograf which comes as immediate release 0.5, 1, and 5 mg oral capsules taken twice per day. Tacrolimus is also available as Advagraf which comes as extended release 0.5, 1, 3, and 5 mg oral capsules taken once per day.
The normal dose of tacrolimus to treat rheumatoid arthritis is 3 mg once a day. Otherwise the normal dose of tacrolimus is based on your body weight and blood levels of the medication.
It can take 3 to 4 months for the tacrolimus to work. It is important for people starting this medication to be patient and to keep taking it as prescribed.
Important Tests and Risks
Patients taking tacrolimus should get their blood and urine tested regularly (every two weeks to every month).
It is important for doctors to make sure that tacrolimus is not affecting blood counts or harming the kidneys or liver.
Patients starting tacrolimus should have their blood pressure checked every week for the first month of therapy, and then every month after that, for as long as they are taking the medicine.
Tacrolimus can make it a bit harder for people to fight off infections.
People taking this medicine should call their doctor they have a fever, think they have an infection, or have been prescribed antibiotics to treat an infection.
It’s important for patients to coordinate with their doctors and stop treatment before any surgery. Treatment can be re-started once things have healed and there’s no sign of infection.
Patients should discuss all vaccinations with their doctor because some are not advisable to get while taking tacrolimus.
Several prescription medications which can interact with tacrolimus.
Patients should make sure that their doctor knows every medicine and supplement that they are taking.
Common over-the-counter medications including cold remedies, pain medication, cough syrup, and laxatives are not known to interact with tacrolimus.
It is not known how tacrolimus could interact with most herbal medications.
Tacrolimus should not be taken with grapefruit juice because it interferes with the absorption of the medication.
It is recommended that patients taking tacrolimus drink 8 to 10 glasses of water per day (1.5 liters) to help their kidney function.
Science
Tacrolimus works by reducing the activity of T-cells, a type of white blood cell that plays an important part in the body’s immune system.
Tacrolimus binds to a protein cyclophilin (immunophilin) found on the surface of white blood cells, especially T-cells. This triggers a chain of reactions that reduces the function of these cells.
In preventing T-cells from working normally, tacrolimus suppresses a part of the body’s immune system. Although this suppression may make it slightly harder for patients to fight off infections, it also helps to stabilize an overactive immune system.
Safety
Tacrolimus can irritate the kidneys. Regular blood tests are important for doctors to monitor blood counts and make sure that the kidneys are not being harmed. Patients should drink 8-10 glasses of water per day to flush the kidneys.
MINOR side-effects include:
- Nausea, bloating, abdominal cramps, and diarrhea.
- Fatigue, weakness, muscle cramps, tremors, and flushing
- Headaches
- Tingling in the fingers, toes, tip of the nose, tongue, or lips.
- Swelling of the ankles – Patients should tell their doctor if they experience this side effect
RARE side-effects include:
- Kidneys – Tacrolimus may affect kidney function. Kidney function is monitored closely with blood tests while you are taking tacrolimus. When monitored closely, any change in kidney function is usually reversible by reducing the dose or stopping the tacrolimus.
- High Blood Pressure –Tacrolimus may cause an increase in blood pressure. If this should happen, the dose of your tacrolimus may be adjusted or a medication to control your blood pressure may be prescribed.
- Infection – Any infections or fevers should be taken seriously and reviewed by your doctor.
- Blood Sugars - Tacrolimus can increase blood sugars.
- Heart – Tacrolimus can rarely affect the heart rhythm. Let your doctor know if you have any heart problems. This can be made worse if combined with certain medications.
- Brain and Nerves - Tacrolimus can rarely be harmful to the brain and nerves. Let your doctor know if you develop a headache, a change in your vision, tremors, tingling in the fingers, toes, tip of the nose, tongue, or lips, or any confusion.
- Malignancy – When used for long periods of time, tacrolimus may be associated with a small increased risk of lymphoma and skin cancers. These cancers may be reversible when the medication is stopped.
How to minimize the side-effects of Tacrolimus:
- Regular monitoring is important. Patients should take tacrolimus as prescribed, get regular blood tests, and attend all appointments with their doctor.
- Patients should drink 8 to 10 glasses of water per day (1.5 liters) to help kidney function.
- Patients should report any infections to their doctor.
Patients should talk to their doctor if they are concerned about any side effects when taking tacrolimus.
Tacrolimus has been used safely in pregnancy. However, anyone who becomes pregnant while taking tacrolimus should let their doctor know.
People who should NOT take tacrolimus include:
- Patients who have had a previous serious reaction to tacrolimus
- Some patients with diseases of the kidney
- Patients with uncontrolled high blood pressure
- Patients with active uncontrolled infections
- Possibly patients with a past history of cancer
- Patients with other diseases which affect the immune system (e.g. HIV)
People taking Tacrolimus should call a doctor if they feel sick and want to stop, or if they are concerned about any side effects.
Other reasons to call a doctor while taking Tacrolimus include:
- New high blood pressure
- Fever or possible infection
- Pregnant or planning pregnancy
- Severe new headache, change in vision, or confusion
- Upcoming surgery
Anyone who becomes pregnant while taking tacrolimus should notify their doctor immediately.
Pregnancy and medications