Tofacitinib belongs to the class of medications called immunomodulators or selective immunosuppressants. It is usually used in combination with methotrexate to decrease the inflammation and joint damage that is experienced with rheumatoid arthritis when methotrexate and at least one other disease modifying medication has not been effective or tolerated. Tofacitinib is used to treat active psoriatic arthritis in combination with methotrexate or other therapies when other treatments have not been effective. It may be used to treat moderate-to-severe active ulcerative colitis (UC) when other treatments for UC have failed or the effectiveness has decreased. Tofacitinib is also used by adults to treat ankylosing spondylitis when other disease-modifying medications have not been successful or should not be used.

Children weighing 40 kg or more may be given tofacitinib to treat active juvenile idiopathic arthritis (JIA) in multiple joints or juvenile psoriatic arthritis when other treatments have failed or are not an option.

Tofacitinib works by blocking the activity of an enzyme called Janus kinase. This enzyme is responsible for sending inflammatory signals in the body. Blocking this enzyme helps to decrease the immune reaction which causes rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

[for Xeljanz]

To treat rheumatoid arthritis, the recommended dose of tofacitinib is 5 mg taken 2 times daily in combination with methotrexate, where tolerated.

To treat psoriatic arthritis, the recommended dose of tofacitinib is 5 mg taken 2 times daily in combination with methotrexate or another medication for psoriatic arthritis.

When treating ankylosing spondylitis, the recommended dose of tofacitinib is 5 mg taken 2 times daily.

To treat ulcerative colitis, the recommended dose of tofacitinib is 10 mg taken 2 times daily for at least 8 weeks. Depending on how well it is working, your doctor may suggest decreasing the dose to continue treatment.

To treat juvenile idiopathic arthritis, the recommended dose for children weighing 40 kg or more is 5 mg taken 2 times daily. It may be taken alone or in addition to methotrexate. 

Tofacitinib may be taken with or without food. Swallow the tablet whole. Do not crush or chew the tablets.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important that this medication be taken exactly as prescribed by your doctor.

If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

[for Xeljanz XR]

The recommended dose of the long-acting formulation of tofacitinib for the treatment of rheumatoid arthritis is 11 mg taken once daily in combination with methotrexate.

It may be taken with or without food. Swallow the tablets whole. Do not split, crush, or chew the tablets.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important that this medication be taken exactly as prescribed by your doctor.

If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Xeljanz

5 mg
Chaque comprimé blanc, rond, pelliculé, portant l'inscription « Pfizer » sur une face et « JKI 5 » sur l'autre, contient 5 mg de tofacitinib sous forme de citrate de tofacitinib. Ingrédients non médicinaux : croscarmellose sodique, lactose monohydraté, stéarate de magnésium et cellulose microcristalline; pelliculage : HPMC 2910/hypromellose 6cP, lactose monohydraté, Macrogol/PEG 3350, dioxyde de titane et triacétine (triacétate de glycérol).

10 mg
Chaque comprimé bleu, rond, pelliculé, portant l'inscription « Pfizer » sur une face et « JKI 10 » sur l'autre, contient 10 mg de tofacitinib sous forme de citrate de tofacitinib. Ingrédients non médicinaux : croscarmellose sodique, lactose monohydraté, stéarate de magnésium et cellulose microcristalline; pelliculage : HPMC 2910/hypromellose 6cP, lactose monohydraté, Macrogol/PEG 3350, dioxyde de titane et triacétine (triacétate de glycérol), AD et C bleu nº 2/carmin d'indigo sur substrat d'aluminium, AD et C bleu nº 1/bleu brillant FCF sur substrat d'aluminium.

Xeljanz XR

11 mg
Chaque comprimé pelliculé rose, ovale, à libération prolongée, contient 11 mg de tofacitinib sous forme de citrate de tofacitinib. Ingrédients non médicinaux : sorbitol, hydroxyéthylcellulose, copovidone et stéarate de magnésium, acétate de cellulose, hydroxypropylcellulose, HPMC 2910/hypromellose, dioxyde de titane, triacétine et oxyde de fer rouge, gomme laque, hydroxyde d'ammonium, propylèneglycol et oxyde magnétique de fer/oxyde de fer noir.

Do not take this medication if you:

• are allergic to tofacitinib or any ingredients of the medication
• are pregnant or breast-feeding
• have severely decreased liver function

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

• acne
• back pain
• cough
• diarrhea
• headache
• heartburn
• joint pain
• loss of appetite
• nausea
• runny or stuffy nose
• skin rash
• vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

• abdominal pain
• broken bones
• dizziness
• flu-like symptoms (sudden lack of energy, fever, cough, sore throat)
• increased blood pressure
• muscle pain, weakness
• new skin lesions or changes to existing skin lesions
• shortness of breath (new or worsening)
• signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
• signs of heart problems (e.g., fast or irregular heartbeat or pulse, chest pain, sudden weight gain, difficulty breathing, leg swelling)
• signs of infection (symptoms may include fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness)
• signs of a skin infection (e.g., redness, inflammation, swelling, warmth)
• signs of kidney problems (e.g., decreased urination, nausea, vomiting, swelling of the feet and ankles)
• signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
• signs of pneumonia (e.g., fever, chills, shortness of breath, cough)
• swelling of legs and ankles or hands and arms
• symptoms of bronchitis (e.g., persistent cough, fatigue, shortness of breath)
• symptoms of shingles/herpes zoster infection (e.g., painful skin rash with blisters)
• symptoms of a urinary tract infection (e.g., pain when urinating, urinating more often than usual, low back or flank pain)

Stop taking the medication and seek immediate medical attention if any of the following occur:

• signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• signs of bleeding in the stomach (e.g., bloody, black, or tarry stools; spitting up of blood; vomiting blood or material that looks like coffee grounds)
• signs of a blood clot in the arm or leg (tenderness, pain, swelling, warmth, or redness in the arm or leg) or lungs (difficulty breathing, sharp chest pain that is worst when breathing in, coughing, coughing up blood, sweating, or passing out)
• signs of a heart attack (e.g., chest pain or pressure, pain extending through shoulder and arm, nausea and vomiting, sweating)
• symptoms of lung cancer (e.g., worsening cough, shortness of breath, loss of appetite, coughing up blood, fatigue, unexplained weight loss)
• symptoms of lymphoma (e.g., painless swollen lymph nodes, fever, chills, night sweats, unexplained weight loss, persistent cough, difficulty breathing, headache)
• vision changes

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Blood clots: This medication may increase the chance of blood clot formation, causing reduction of blood flow to organs or the extremities. If you have a history of clotting you may be at increased risk of experiencing blood clot-related problems such as heart attack, stroke, or clots in the deep veins of your leg. Blood clots have also been reported in the retinal veins of the eye. Discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

If you experience symptoms such as sharp pain and swelling in the leg, difficulty breathing, chest pain, blurred vision or difficulty speaking, get immediate medical attention.

Cancer: Although not common, tofacitinib has been associated with several different types of cancer including skin, lung, breast, prostate, and lymphoma. If you have risk factors for developing cancer, including a history of smoking, make sure your doctor is aware. Discuss any concerns that you may have with your doctor.

Cholesterol: Tofacitinib can cause increased blood cholesterol levels. This may happen to people with normal cholesterol levels or high cholesterol levels at the beginning of treatment.

If you are at risk of developing high cholesterol or you have high cholesterol levels before starting tofacitinib, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Your doctor will monitor your cholesterol levels regularly while you are taking this medication.

Diabetes: Decreased blood glucose levels have been reported by people with diabetes who take tofacitinib. If you have diabetes, your doctor may want you to monitor your blood glucose more frequently.

Gastrointestinal narrowing: People who have narrowing of the stomach should discuss this with their doctor before using the long-acting formulation of this medication. Because the shell around the medication does not break down, people with narrowing in the digestive system are at increased risk of experiencing a blockage.

Gastrointestinal perforation: People who take anti-inflammatory medications such as NSAIDs or corticosteroids while they are also taking tofacitinib may be more likely to experience a tear in the lining of the stomach, which can cause serious bleeding. This can occur without abdominal pain.

If you notice bloody or black and tarry stools, or vomit blood or material that looks like coffee grounds, seek medical help immediately.

Heart problems: Recent studies have shown that tofacitinib increases the likelihood of major heart problems including heart attack and changes to the normal rhythm of the heart. If you have risk factors for heart problems, including congestive heart failure, heart block, a history of irregular heartbeat, are a past or current smoker, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Heart rate: This medication may decrease your heart rate. If you have a history of decreased heart rate, irregular heart rhythms, or heart disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Infection: This medication reduces your body's response to infection. People taking tofacitinib are at an increased risk of developing serious infections that can be difficult to treat and may cause hospitalization or death. These infections include tuberculosis and fungal infections as well as infections caused by bacteria and viruses. These infections are more likely to occur if you are taking another medication that reduces the activity of the immune system.

If you have been exposed to tuberculosis, have a history of serious or recurrent infections, or have medical conditions that may increase the likelihood of developing infections, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

If possible, avoid contact with people with contagious infections. Tell your doctor immediately if you notice signs of an infection, such as fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness.

Kidney function: If you have reduced kidney function or kidney disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. A lower dose of this medication may be necessary.

Liver function: People taking tofacitinib may have changes in liver function that produce abnormal liver test results. Your doctor will recommend regular liver tests while you are taking this medication. If you have severe changes in liver function, your doctor may recommend that you take a lower dose of this medication or stop taking it altogether.

Lung inflammation: Lung inflammation (interstitial lung disease), causing difficulty breathing has occurred rarely for some people taking this medication. This complication can be serious and sometimes fatal. If you experience new or worsening shortness of breath or cough (with or without fever) at any time while you are taking tofacitinib, contact your doctor immediately.

Muscle effects: Muscle damage has been associated with the use of tofacitinib. Report any unexplained muscle pain, tenderness, weakness or cramps, or any brown or discoloured urine to your doctor immediately, particularly if you are also experiencing malaise (a general feeling of being unwell).

Vaccinations: People taking this medication should not receive certain vaccines. Talk to your doctor about whether any vaccines you are scheduled to have may be used with this medication.

Vision changes: This medication may cause blood clots in the eyes. If you develop blurry vision or any signs of vision loss, contact your doctor immediately.

Pregnancy: This medication should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

People who may become pregnant should use effective birth control during treatment with tofacitinib and for 4 to 6 weeks after the last dose.

Breast-feeding: It is not known if tofacitinib passes into breast milk. If you are breast-feeding and taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children weighing less than 40 kg. The extended-release form of tofacitinib should not be given to children under the age of 18.

Children who weigh 40 kg or more may be given tofacitinib to treat polyarticular juvenile idiopathic arthritis or juvenile psoriatic arthritis.

Seniors: People over the age of 65 have a higher risk of developing infections and serious side effects when taking tofacitinib. Talk to your doctor to determine whether the benefits outweigh the risks for your condition.

For a full list of interactions, use the Drug Interaction Checker available on the Drugs.com website.

If you are taking other medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.