Tofacitinib

What is tofacitinib?

Tofacitinib (brand name: Xeljanz®) is a tablet that belongs to a class of medicines called Janus Kinase (JAK) inhibitors. JAK inhibitors work by blocking signals in the body that cause inflammation. In rheumatoid arthritis and other inflammatory conditions, reducing these signals helps reduce inflammation and pain, and helps protect the joints from further damage.

What benefit can you expect from your treatment?

Tofacitinib can help people with inflammatory arthritis live longer with a better quality of life.
You may notice some relief of joint swelling, pain and stiffness within the first 2 to 4 weeks of treatment, though it can take up to 3 months to improve.
The benefits of continuing tofacitinib will be reviewed at each clinic appointment and it is important you advise your rheumatologist of any new medical conditions at each visit.

Stopping tofacitinib

If you stop or delay your tofacitinib treatment, your disease may get worse. Keep taking your treatment, unless advised by your rheumatologist to stop or unless serious side effects occur (see Side effects).
If you stop tofacitinib for any reason you must contact your rheumatologist. Failure to do so may mean that your treatment may no longer be funded.

How will you be checked while on tofacitinib?

• Tofacitinib will only be given if your disease is active and if standard treatments have not worked.
• Tofacitinib will only be continued if it helps your condition. This will be checked around 12-16 weeks after the start of treatment.
• You will need regular blood tests to check for side effects and to see if the treatment is helping. 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 tofacitinib taken?

Tofacitinib is taken by mouth in tablet form. The tablet should be swallowed whole do not crush, break or chew the tablet.

When should it be taken?

Take this medicine with a full glass of water at the same time each day. It can be taken with or without food.
If you miss a dose: Take a dose as soon as you remember. If it is almost time for your next dose, wait until then and take a regular dose. Do not take extra medicine to make up for a missed dose.

What is the dosage?

The usual dose for adults with rheumatoid arthritis and other inflammatory conditions is 5mg taken twice daily.

Can other medicines be taken with tofacitinib?

This medicine may be used alone or with other arthritis medicines including:
• Other disease modifying anti rheumatic drugs (DMARDs) such as methotrexate.
• Steroid medications such as prednisolone or cortisone injections into the joint.
• Anti-inflammatory medicines (NSAIDs) such as naproxen (Naprosyn®) or ibuprofen (Brufen®, Nurofen®).
• Simple pain medicines such as paracetamol.
• There may be some instances where these medicines may not be right for you, always check with your doctor prior to taking any of these medicines.

Tofacitinib cannot be used with other biologic DMARDs or targeted synthetic DMARDs (such as baricitinib, upadacitinib, etanercept and adalimumab).

Are there any side effects?

You might experience side effects with your treatment. Tell your doctor if you notice side effects that you think are caused by this medicine. Many side effects disappear when tofacitinib treatment is stopped.

Most common side effects

• The most common side effects reported are mild upper respiratory tract infections (common cold, sinus infections), nausea, cough, and fever. Infections may need treatment and tofacitinib may need to be stopped for a while if you develop infection, so it is important to contact your doctor for advice.

Less common or rare side effects

• Blood clots in the veins of the legs, lungs and arteries are possible in some people taking tofacitinib. This can happen more often in patients with an inflammatory condition. Other risk factors including heart disease will be assessed by your doctor.
• Serious infections such as tuberculosis (TB) are seen rarely, and screening for TB is needed before treatment begins.
• Increases in cholesterol levels occur in some patients when taking tofacitinib. This can be monitored using blood tests.
• Changes in liver function can occur, it is recommended to have regular blood tests to monitor this.
• Tofacitinib increases the risk of getting shingles. If you get a painful skin rash with blisters, inform your doctor immediately. Vaccination for shingles should be discussed with your rheumatologist before starting treatment, and is available for free in Australia for people on tofacitinib.
• Tofacitinib may increase the chance of bowel perforation, although this is rare.
• People with rheumatoid arthritis and other inflammatory conditions are at increased risk of lymphoma and some other cancers. Medicines that change your immune system like tofacitinib may further increase this risk.
• Skin cancers have been reported in people taking tofacitinib. Yearly skin checks are recommended.
• It is recommended that people on tofacitinib remain up to date with their age appropriate cancer screening such as mammogram, bowel cancer screening, and lung cancer screening for smokers.
• If you experience any side effects, please inform your doctor or pharmacist promptly.

What precautions are necessary

Infections

If you have an active infection of any kind, treatment with tofacitinib will not be started until the infection is treated successfully. If you have a serious infection for example requiring antibiotics or antivirals, generally you should pause tofacitinib until you are getting better.

Cardiovascular risk

People with rheumatoid arthritis and other inflammatory conditions have an increased risk of cardiovascular disorders. Recent reports have associated this medicine and other JAK inhibitors with an increased risk of heart related events. Ensure your doctor is aware of any pre-existing risk factors (e.g. high blood pressure, high cholesterol, smoking status).

Use with other medicines

Some medicines may not be used with tofacitinib as it may change their effectiveness and how well tofacitinib may work for you.
Some medicines that may change how tofacitinib works include:

• Antifungals & antibiotics including ketoconazole, itraconazole, posaconazole or voriconazole, clarithromycin, rifampicin and phenytoin.
• Some medicines may increase your risk of infection including those used to suppress your immune system including phenytoin, azathioprine, ciclosporin and tacrolimus.
• Other medicines may require additional review and monitoring as they may increase the risk of side effects when taking tofacitinib including: NSAIDs, opioids and corticosteroids.

There may be other medicines that can affect tofacitinib. You should inform your doctor and pharmacist of all of the medicines you are taking or plan to take. This includes over the counter or herbal/naturopathic medicines to see if these affect tofacitinib.

Use with alcohol

You may drink alcohol while taking tofacitinib. However, if you are also taking methotrexate, you should be cautious about how much alcohol you drink.

Vaccines

If you are taking tofacitinib you should not be immunised with ‘live’ vaccines such as:
• MMR (measles, mumps and rubella)
• Varicella (chicken pox)
• OPV (oral polio virus)
• BCG (bacillus calmette guerin)
• Japanese Encephalitis or Yellow Fever

Talk with your rheumatologist before receiving any vaccines.
Pneumococcal, Shingrix – Inactivated Vaccine (not live) vaccines and the yearly seasonal flu vaccinations are encouraged.

For more information on vaccination including the COVID-19 vaccination go to https://rheumatology.org.au/For-Patients/Adult-Medication-Information/Vaccinations-in-Rheumatology

Surgery

If you require surgery for any reason, treatment with tofacitinib should be stopped one week before surgery. It will be restarted again after the operation at a time agreed by your surgeon and rheumatologist.

Use in pregnancy and when breastfeeding

• Tell your doctor if you are planning on getting pregnant when taking tofacitinib.
• Tofacitinib should not be used during pregnancy. Women of childbearing potential should use effective birth control both during treatment and for at least 4 weeks after final dose of tofacitinib.
• Do not breastfeed if you are taking tofacitinib as it is uncertain how much of the drug might be excreted in breastmilk.More detailed information is available at https://rheumatology.org.au/For-Patients/Medicine-Safety-in-Pregnancy-and-Breastfeeding

How to store tofacitinib

Store tofacitinib in a cool, dry place, away from direct heat and light (e.g. not in the bathroom).
Keep all medicines out of reach of children.

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, heart failure or stroke, so that your arthritis treatment can be reviewed.
• If you are worried about any side effects, you should contact your rheumatologist as soon as possible.
• If you stop tofacitinib for any reason, you must contact your rheumatologist. Failure to do so may mean that your treatment may no longer be funded.
• Patients commencing tofacitinib should ensure they have close monitoring of their cardiovascular risk factors, including blood pressure and cholesterol with their local doctor.
• If you are taking tofacitinib and plan to become pregnant you must discuss the timing with your rheumatologist.

For more information see the Tofacitinib – printable information sheet.