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Tofacitinib (Oral)

toe-fa-SYE-ti-nib

Oral route(Tablet;Tablet, Extended Release)

Serious infections leading to hospitalization or death, including tuberculosis and bacterial, invasive fungal, viral, and other opportunistic infections, have occurred in patients receiving tofacitinib. If a serious infection develops, interrupt tofacitinib until the infection is controlled. Prior to starting tofacitinib and during therapy, perform a test for latent tuberculosis; if it is positive, start treatment for tuberculosis prior to starting tofacitinib. Monitor all patients for the development of signs and symptoms of infection during and after treatment with tofacitinib, including active tuberculosis during treatment, even if the initial latent tuberculosis test is negative. Lymphoma and other malignancies have been observed in patients treated with tofacitinib. Epstein Barr virus-associated posttransplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with tofacitinib and concomitant immunosuppressive medications .

Medically reviewed on June 7, 2018

Commonly used brand name(s)

In the U.S.

  • Xeljanz
  • Xeljanz XR

Available Dosage Forms:

  • Tablet
  • Tablet, Extended Release

Therapeutic Class: Musculoskeletal Agent

Pharmacologic Class: Tyrosine Kinase Inhibitor

Uses For This Medicine

Tofacitinib is used alone or together with other medicines (eg, DMARDs) to treat moderate to severely active rheumatoid arthritis and active psoriatic arthritis in patients who have taken other medicines (eg, methotrexate) but did not work well. Tofacitinib is a Janus kinase (JAK) inhibitor that works on the immune system.

Tofacitinib is available only with your doctor's prescription.

Before Using This Medicine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For tofacitinib, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to tofacitinib or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of tofacitinib in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of tofacitinib in the elderly. However, elderly patients are more likely to have serious infections, which may require caution in patients receiving tofacitinib.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking tofacitinib, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using tofacitinib with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Adenovirus Vaccine
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Carbamazepine
  • Cholera Vaccine, Live
  • Enzalutamide
  • Fosphenytoin
  • Idelalisib
  • Infliximab
  • Influenza Virus Vaccine, Live
  • Measles Virus Vaccine, Live
  • Mitotane
  • Mumps Virus Vaccine, Live
  • Phenytoin
  • Poliovirus Vaccine, Live
  • Primidone
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Smallpox Vaccine
  • St John's Wort
  • Typhoid Vaccine
  • Varicella Virus Vaccine, Live
  • Yellow Fever Vaccine
  • Zoster Vaccine, Live

Using tofacitinib with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Fluconazole

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of tofacitinib. Make sure you tell your doctor if you have any other medical problems, especially:

  • Anemia (blood disease) or
  • Diabetes or
  • Hyperlipidemia (high cholesterol in the blood) or
  • Infection, history of or
  • Neutropenia (blood disease) or
  • Stomach or bowel problems (eg, blockage, diverticulitis, perforation, ulcers), history of—Use with caution. May make these conditions worse.
  • Hepatitis B, history of or
  • Hepatitis C, history of or
  • Herpes zoster infection or
  • Tuberculosis, active or history of or
  • Weakened immune system—May cause side effects to become worse.
  • Infection, active or
  • Liver disease, severe—Use is not recommended in patients with these conditions.
  • Kidney disease, moderate or severe or
  • Liver disease, moderate—Use with caution. The effects may be increased because of slower removal of the medicine from the body.
  • Lung disease (eg, interstitial lung disease), or history of or
  • Lymphopenia (blood disease)—Use with caution. May increase risk of developing infections.

Proper Use of This Medicine

Use tofacitinib exactly as directed by your doctor. Do not take more or less of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

Tofacitinib should come with a Medication Guide. Read and follow the instructions carefully. Ask your doctor if you have any questions.

You may take tofacitinib with or without food.

Swallow the extended-release tablet whole with water. Do not cut, crush, break, or chew it.

A part of the extended-release tablet may pass into your stools. This is normal and is nothing to worry about.

Dosing

The dose of tofacitinib will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of tofacitinib. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For psoriatic arthritis:
    • For oral dosage form (extended-release tablets):
      • Adults—11 milligrams (mg) once a day together with another medicine.
      • Children—Use and dose must be determined by your doctor.
    • For oral dosage form (tablets):
      • Adults—5 milligrams (mg) two times a day together with another medicine.
      • Children—Use and dose must be determined by your doctor.
  • For rheumatoid arthritis:
    • For oral dosage form (extended-release tablets):
      • Adults—11 milligrams (mg) once a day.
      • Children—Use and dose must be determined by your doctor.
    • For oral dosage form (tablets):
      • Adults—5 milligrams (mg) two times a day.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of tofacitinib, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if tofacitinib is working properly and to decide whether you should continue to use it. Blood tests are needed to check for unwanted effects.

Using tofacitinib while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant during treatment with tofacitinib and for at least 4 weeks after the last dose. If you think you have become pregnant while using tofacitinib, tell your doctor right away.

If you plan to have children, talk with your doctor before using tofacitinib. Some women using tofacitinib have become infertile (unable to have children).

You will need to have a skin test for tuberculosis before you start using tofacitinib. Tell your doctor if you or anyone in your home has ever had a positive reaction to a tuberculosis skin test.

Your body's ability to fight infection may be reduced while you are using tofacitinib. It is very important that you call your doctor at the first sign of an infection. Check with your doctor right away if you have a fever, chills, cough, flu-like symptoms, or unusual tiredness or weakness.

Using tofacitinib may increase your risk of getting skin cancer (eg, non-melanoma skin cancer) or cancer of the lymph system (lymphoma). Talk to your doctor if you have concerns about this risk.

Tofacitinib can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection:

  • If you can, avoid people with infections. Check with your doctor right away if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
  • Check with your doctor right away if you notice any unusual bleeding or bruising, black, tarry stools, blood in the urine or stools, or pinpoint red spots on your skin.
  • Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
  • Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
  • Be careful not to cut yourself when you are using sharp objects, such as a safety razor or fingernail or toenail cutters.
  • Avoid contact sports or other situations where bruising or injury could occur.

While you are being treated with tofacitinib, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval. Tofacitinib may lower your body's resistance and there is a chance you might get the infection the vaccine is meant to prevent. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

This Medicine Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common

  • Bladder pain
  • bloody or cloudy urine
  • blurred vision
  • body aches or pain
  • chills
  • cough
  • difficult, burning, or painful urination
  • difficulty breathing
  • dizziness
  • ear congestion
  • fever
  • frequent urge to urinate
  • headache
  • loss of voice
  • lower back or side pain
  • muscle aches
  • nervousness
  • pounding in the ears
  • slow or fast heartbeat
  • sneezing
  • sore throat
  • stuffy or runny nose
  • unusual tiredness or weakness

Incidence not known

  • Bloating or swelling of the face, arms, hands, lower legs, or feet
  • confusion
  • dark urine
  • decreased urination
  • difficult or labored breathing
  • dry mouth
  • fainting
  • increase in heart rate
  • light-colored stools
  • lightheadedness
  • nausea
  • pale skin
  • persistent non-healing sore
  • rapid breathing
  • rapid weight gain
  • reddish patch or irritated area
  • sunken eyes
  • thirst
  • tightness in the chest
  • tingling of the hands or feet
  • troubled breathing with exertion
  • unusual bleeding or bruising
  • unusual weight gain or loss
  • upper right abdominal or stomach pain
  • vomiting
  • wrinkled skin
  • yellow eyes and skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common

  • Diarrhea

Incidence not known

  • Belching
  • burning feeling in the chest or stomach
  • burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
  • difficulty with moving
  • flushing or redness of the skin
  • heartburn
  • indigestion
  • itching skin, rash
  • muscle pain or stiffness
  • pain in the joints
  • stomach discomfort, upset, or pain
  • tenderness in the stomach area
  • trouble sleeping
  • unusually warm skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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