Tofacitinib | Side Effects, Dosage, Uses & More
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Generic Name:

tofacitinib, Oral tablet

Generic Name:
Xeljanz,Zeljanz XR

tofacitinib, Oral tablet

All Brands

  • Xeljanz
  • Zeljanz XR
SECTION 1 of 5

Highlights for tofacitinib

Oral tablet
1

Tofacitinib is an oral medication used to treat rheumatoid arthritis. It’s used by adults who can’t tolerate taking methotrexate. It’s also used by adults whose arthritis didn’t improve while taking methotrexate.

2

The usual dose is one 5-mg tablet taken twice per day. Your dose may depend on your health and other conditions you have.

3

The most common side effects of this drug include headache, cold or sinus infections, congested nose, runny nose, sore throat, and diarrhea.

4

Tofacitinib can decrease your body’s ability to fight infection because it lowers your immunity. You may be at risk for developing serious infections or cancer while taking it.

5

Your doctor may check your blood, lung, and liver function before you begin taking tofacitinib to make sure it’s safe for you.

IMPORTANT INFORMATION

FDA warning

This drug has a Black Box Warning. This is the most serious warning from the Food and Drug Administration (FDA). A black box warning alerts doctors and patients to potentially dangerous effects.

Serious infections that can be fatal. Tofacitinib can decrease your body’s ability to fight infections. Some people taking tofacitinib have had serious infections, such as tuberculosis and diverticulitis (infection in the small pouches of the digestive tract). Some of these infections have caused death.

Before starting tofacitinib, tell your doctor if you think you’re sick or if you’re being treated for an infection. Symptoms of an infection include:

  • fever, sweating, or chills
  • cough
  • shortness of breath
  • blood in your mucus
  • muscle aches
  • feeling tired
  • weight loss
  • red, warm, or painful sores on your body
  • stomach pain or diarrhea
  • burning when urinating or urinating more often than normal

Also tell your doctor if you have conditions that increase your risk of infection, including:

  • human immunodeficiency virus (HIV) infection
  • diabetes
  • a weakened immune system
  • tuberculosis (TB) or have been in close contact with someone with TB
  • current or past hepatitis B or C virus infection

You shouldn’t start taking tofacitinib if you have any kind of infection unless your doctor says it’s okay. Your doctor may test you for TB before starting tofacitinib and monitor you for TB during treatment. If you develop any symptoms of an infection, call your doctor right away. Tofacitinib may make you more likely to get infections and make any infections you get worse. If you get an infection while taking tofacitinib, your doctor may decide to take you off the drug until your infection is under control.

Cancer and immune system problems. Tofacitinib may increase your risk of blood cancer (lymphoma) or other types of cancers. This is because it changes the way your immune system works. Tell your doctor if you’ve ever had any kind of cancer.

Taking tofacitinib with certain medications to prevent kidney transplant rejection comes with risks. Some people who have done this have had a problem with certain white blood cells called lymphocytes rapidly increasing in number. This can lead to infections that may develop into cancer. Tell your doctor if you’ve had a kidney transplant and are taking medications to prevent your body from rejecting the transplant.

May cause stomach tearing

This drug may cause tears in your stomach or intestines. Tell your doctor if you’ve had inflammation in your intestines (diverticulitis) or ulcers in your stomach or intestines. You’re at higher risk of stomach tearing if you’re also taking methotrexate, nonsteroidal anti-inflammatory drugs, or corticosteroids. Call your doctor right way if you have a change in bowel habits and stomach pain or fever that won’t go away.

May reduce liver function

This drug may reduce liver function. Your doctor may take blood tests to check your liver function before and during treatment. You shouldn’t take this drug if your liver tests results are too high. If these tests are abnormal, your doctor may choose to stop this drug temporarily. 

May reduce blood cell counts

This drug may reduce the number of blood cells your body makes. Your doctor may take blood tests to check your blood cell counts before and during treatment. White blood cells are important because they help your body fight off infections. Red blood cells help carry oxygen to your body. If blood cell counts are too low, you may feel tired and weak. You shouldn’t take this drug if your blood cell counts are too low.

What is tofacitinib?

This drug is a prescription drug. It’s available as an oral tablet and extended-release oral tablet.

This drug is available as the brand-name drugs Xeljanz and Xeljanz XR. It isn’t available as a generic drug.

This drug may be used as part of a combination therapy. That means you need to take it with other drugs.

Why it's used

This drug is used to treat moderate to severe rheumatoid arthritis (RA) in adults who didn’t do well with methotrexate alone.

More Details

How it works

This drug works to block enzymes and signals in your body to prevent your immune system from attacking your joints. This may improve your RA pain and prevent further joint damage.

Why it's used

This drug is used to treat moderate to severe rheumatoid arthritis (RA) in adults who didn’t do well with methotrexate alone.

It can be used alone or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs). This drug shouldn’t be used with other biologic DMARDs or drugs that weaken your immune system. Examples are cyclosporine and azathioprine.

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tofacitinib Side Effects

Oral tablet

Most Common Side Effects

The most common side effects that occur with tofacitinib include:

  • headache

  • upper respiratory infections (like sinus infections or the common cold)

  • congested nose, runny nose, or sore throat

  • diarrhea

Serious Side Effects

If you experience any of these serious side effects, call your doctor right away. If your symptoms are potentially life threatening or if you think you’re experiencing a medical emergency, call 9-1-1.

  • serious infections, such as pneumonia, tuberculosis, diverticulitis (infection in the small pouches of the digestive tract), or others. Symptoms of infection may include:

    • fever, sweating, or chills
    • cough
    • shortness of breath
    • blood in your mucus
    • muscle aches
    • feeling tired
    • weight loss
    • red, warm, or painful sores on your body
    • stomach pain or diarrhea
    • burning when urinating or urinating more often than normal
  • liver damage or reactivated hepatitis B or hepatitis C virus infection. If your hepatitis B or C is inactive, this medication could reactivate it. Symptoms of these problems may include:

    • tiredness
    • yellowing of your skin or whites of your eyes
    • little or no appetite
    • vomiting
    • clay or pale-colored stools
    • fevers
    • chills
    • stomach pain
    • muscle aches
    • dark-colored urine
    • skin rash
  • stomach or intestine tears. Symptoms may include:

    • stomach pain that doesn’t go away
    • fever that doesn’t go away
    • change in your bowel habits
Pharmacist's Advice
Clinical Associate Professor, University of Illinois at Chicago College of Pharmacy

This drug is not sedating.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.
SECTION 3 of 5

tofacitinib May Interact with Other Medications

Oral tablet

This drug can interact with other medications, herbs, or vitamins you might be taking. That’s why your doctor should manage all of your medications carefully. If you’re curious about how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Note: You can reduce your chances of drug interactions by having all of your prescriptions filled at the same pharmacy. That way, a pharmacist can check for possible drug interactions.

Medications that might interact with this drug

Antifungal drugs

These include:

  • ketoconazole
  • fluconazole

This drug can interact with these drugs, which interfere with certain enzymes in your body. When you take these drugs together, the amount of this drug in your body is increased, putting you at risk for side effects. If you’re taking drugs like ketoconazole, your dose of this drug may be reduced.

Antibiotics
  • rifampin

This drug can interact with this drug, which interfere with certain enzymes in your body. Taking these drugs together decreases the amount of this drug in your body. This will cause it not to work as well. 

Immunity-lowering drugs

These include:

  • azathioprine
  • tacrolimus
  • cyclosporine
  • other biologic disease-modifying antirheumatic drugs (DMARDs)

Taking these drugs together can put you at an even greater risk for infection and other side effects.

Live vaccines

You shouldn’t receive live vaccines if you’re taking this drug. Examples are the live flu vaccine and measles, mumps, and rubella vaccine. Your body might not be able to respond to the vaccine properly. This puts you at risk for infection. Tell your doctor if you’ve recently received or are scheduled to receive a vaccination.

It’s okay to receive vaccines that aren’t live.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions. This information is not a substitute for medical advice. Always speak with your healthcare provider about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.
Drug warnings
liver
People with liver problems

Your body might not be able to process this drug correctly. This causes increased levels of the drug to stay in your body, putting you at risk for side effects. This drug can also cause additional damage to your liver.

kidney problems
People with kidney problems

You might not be able to clear this drug out of your body as well. This causes increased levels of the drug to stay in your body, putting you at risk for side effects.

digestive system
People with diverticulitis or ulcers

Tell your doctor if you’ve ever been diagnosed with diverticulitis or ulcers in your stomach or intestine. This drug can cause tears in your stomach and intestines. Your risk is increased if you’re also taking methotrexate, nonsteroidal anti-inflammatory drugs, or corticosteroids.

pregnant women
Pregnant women

This drug is a category C pregnancy drug. That means two things:

  1. Research in animals has shown adverse effects to the fetus when the mother takes the drug.
  2. There haven’t been enough studies done in humans to be certain how the drug might affect the fetus.

Speak with your doctor if you’re pregnant or plan to become pregnant. Tofacitinib should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus.

breastfeeding
Women who are breast-feeding

It isn’t known if this drug passes into breast milk. If it does, it may cause side effects in your baby if you breastfeed while taking this drug.

You and your doctor should decide whether you’ll take this drug or breastfeed.

seniors
For seniors

If you’re older than 65 years, your liver and kidneys may not work as well. These organs might not be able to clear this drug from your body as well. This causes increased levels of the drug to stay in your body, putting you at risk for side effects, including infections.

children
For children

The effectiveness and safety of this drug haven’t been established in people younger than 18 years.

allergies
Allergies

Tell your doctor if you’ve had an allergic reaction to this drug. Symptoms may include:

  • trouble breathing
  • swelling of your throat or tongue
  • hives
SECTION 4 of 5

How to Take tofacitinib (Dosage)

Oral tablet

All possible dosages and forms may not be included here. Your dose, form, and how often you take it will depend on:

  • your age
  • the condition being treated
  • how severe your condition is
  • other medical conditions you have
  • how you react to the first dose

What Are You Taking This Medication For?

Rheumatoid arthritis

Brand: Xeljanz

Form: Oral tablet
Strength: 5 mg

Brand: Xeljanz XR

Form: Extended-release oral tablet
Strength: 5 mg
Adult Dosage (ages 18 years and older)
  • 5 mg taken twice per day in evenly spaced doses for the immediate-release tablet.
  • 11 mg taken once per day for the extended-release tablet.
Child Dosage (ages 0-17 years)

Dosage for people younger than 18 years hasn’t been established.

Special considerations

Kidney Disease: For people with moderate to severe kidney disease, the recommended dose is 5 mg per day.

Liver Disease: For people with moderate liver disease, the recommended dose is 5 mg per day.

Use With Antifungal Drugs: For people also taking antifungal drugs like ketoconazole and fluconazole, the dose of tofacitinib may be decreased to 5 mg per day.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always to speak with your doctor or pharmacist about dosages that are right for you.
Pharmacist's Advice
Clinical Associate Professor, University of Illinois at Chicago College of Pharmacy

This drug comes with risks if you don’t take it as prescribed by your doctor.

If you don't take it at all

RA is a chronic, progressive condition. This means it can get worse over time, especially it’s left untreated. This drug may help improve how you feel and slow or stop the disease from worsening. RA can damage your joints and sometimes other organs even if you’re not experiencing symptoms. Take your medication as directed by your doctor, even when you’re feeling well. Doing so will give you the best chance of managing your arthritis and improving your quality of life.

If you stop taking it or miss a dose

If you stop taking this medication, miss doses, or don’t take it on schedule, your joint pain, swelling, and stiffness may get worse.

If you take too much

If you take too much of this drug, call your doctor or go to the nearest emergency room right away. The specific symptoms you may experience if you overdose aren’t known, but you’ll be monitored for any severe side effects.

What to do if you miss a dose

If you miss a dose, take it as soon as you remember. Skip the missed dose if it’s almost time for your next scheduled dose. Don’t take extra medicine to make up for the missed dose.

How can I tell if the drug is working?

You may be able to tell this drug is working if:

  • your joint pain, swelling, and stiffness decrease
  • you’re able to perform daily tasks better, such as getting in and out of bed, gripping objects, opening a jar, or buttoning a shirt

Your doctor may perform lab tests and X-rays to look for changes in your joints to see if the drug is working.

According to this drug’s prescribing information, studies showed that some people saw their joint pain and swelling decrease in 2 weeks after starting this drug. Others saw benefits in 3–6 months. Everybody is different, so the time it takes for this drug to work for you may be different.

This is long-term treatment.

Important considerations for taking this drug
take with or without food
You can take this drug with or without food
do not crush
Don’t cut or crush the oral tablet
storage
Store this medication at room temperature: 68–77°F (20–25°C)
See Details
refillable prescription
Prescription is refillable
luggage
Travel
See Details
clinical monitoring
Clinical monitoring
See Details
not usually stocked
Not every pharmacy stocks this drug, so call ahead
prior authorization needed
Insurance
See Details

Store this medication at room temperature: 68–77°F (20–25°C)

Safely throw away medicine that’s out of date or no longer needed.

Note: Keep your medications away from areas where they could get wet, such as bathrooms. Store them away from moisture and damp locations.

Travel

When traveling with your medication:

  • Always carry it with you or in your carry-on bag.
  • Don’t worry about airport X-ray machines. They can’t hurt this medication.
  • You may need to show your pharmacy’s preprinted label to identify the medication. Keep the original prescription-labeled bottle with you when traveling.

Clinical Monitoring

This drug can lower your ability to fight infections. Your doctor may monitor you for serious infections, including tuberculosis and infections caused by bacteria, fungi, or viruses.

Your doctor may order a blood test to measure cholesterol. They may test your blood and liver to check for side effects from the drug.

This drug may cause tears in your stomach or intestines. You’re at a higher risk if you’re also taking methotrexate, nonsteroidal anti-inflammatory drugs, or corticosteroids. Your doctor may check if you’re having fever and stomach-area pain that doesn’t go away, or a change in your bowel habits.

Insurance

Many insurance companies will require a prior authorization before they approve the prescription and pay for this drug.

Are there any alternatives?

There are other drugs available to treat your condition. Some may be more suitable for you than others. Talk to your doctor about possible alternatives.

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How Much Does tofacitinib Cost?

Oral tablet

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Content developed in collaboration with University of Illinois-Chicago, Drug Information Group

Medically reviewed by Creighton University, Center for Drug Information and Evidence-Based Practice on March 24, 2016

Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.
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