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What is Tofacitinib: Uses, Dosage, Side Effects and More

Created at:1/13/2025

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Tofacitinib is a prescription medication that helps calm down your immune system when it's overactive. This oral medication belongs to a class of drugs called JAK inhibitors, which work by blocking certain proteins that fuel inflammation in your body.

You might be prescribed tofacitinib if you have conditions like rheumatoid arthritis, psoriatic arthritis, or ulcerative colitis. It's designed to help reduce pain, swelling, and other symptoms when your immune system mistakenly attacks healthy tissue.

What is Tofacitinib Used For?

Tofacitinib treats several autoimmune conditions where your body's defense system works too hard. The medication is FDA-approved for rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis in adults.

For rheumatoid arthritis, tofacitinib helps reduce joint pain, stiffness, and swelling that can make daily activities challenging. Many people find their morning stiffness improves and they can move more comfortably throughout the day.

In psoriatic arthritis, this medication targets both joint inflammation and skin symptoms. It can help ease the painful, swollen joints while also improving the scaly skin patches that often accompany this condition.

For ulcerative colitis, tofacitinib works to reduce inflammation in your colon. This can help control symptoms like frequent bowel movements, abdominal pain, and bleeding that interfere with your quality of life.

How Does Tofacitinib Work?

Tofacitinib works by blocking specific enzymes called JAK proteins that send inflammation signals throughout your body. Think of these proteins as messengers that tell your immune system to create inflammation.

When these JAK proteins are overactive, they can cause your immune system to attack healthy tissues like your joints or digestive tract. By blocking these signals, tofacitinib helps reduce the inflammation that causes your symptoms.

This medication is considered a targeted therapy, meaning it focuses on specific parts of your immune system rather than suppressing everything. However, it's still a strong medication that requires careful monitoring by your healthcare provider.

You might start noticing improvements in your symptoms within a few weeks, though it can take up to three months to feel the full benefits. Everyone responds differently, so your doctor will work with you to find the right approach.

How Should I Take Tofacitinib?

Take tofacitinib exactly as your doctor prescribes, usually twice daily with or without food. You can take it with milk or water, and timing with meals isn't critical for absorption.

Swallow the tablets whole without crushing, breaking, or chewing them. The extended-release formulation is designed to release the medication slowly throughout the day, so altering the tablet can affect how it works.

Try to take your doses at the same times each day to maintain steady levels in your bloodstream. Setting phone reminders can help you establish a routine, especially when you're first starting the medication.

If you have trouble swallowing tablets, talk to your doctor about your options. They might suggest techniques to make swallowing easier or discuss whether this medication is the best choice for you.

How Long Should I Take Tofacitinib For?

Most people take tofacitinib as a long-term treatment to manage their chronic condition. Your doctor will regularly evaluate whether the medication continues to help you and remains safe.

You'll likely have blood tests every few months to monitor your immune system, liver function, and overall health. These check-ups help ensure the medication is working well without causing concerning side effects.

Some people may need to take breaks from tofacitinib if they develop infections or other health issues. Your doctor will guide you through any necessary adjustments to keep you as healthy as possible.

Never stop taking tofacitinib suddenly without talking to your healthcare provider first. Stopping abruptly could cause your symptoms to return quickly, and your doctor may want to gradually reduce your dose instead.

What Are the Side Effects of Tofacitinib?

Like all medications that affect your immune system, tofacitinib can cause side effects ranging from mild to serious. Most people tolerate it well, but being aware of potential reactions helps you know what to watch for.

Common side effects that many people experience include headaches, diarrhea, and cold-like symptoms. These often improve as your body adjusts to the medication over the first few weeks.

Here are the most frequent side effects you might notice:

  • Upper respiratory infections like colds or sinus infections
  • Headaches that are usually mild to moderate
  • Diarrhea or changes in bowel movements
  • High blood pressure
  • Nausea or stomach discomfort

These common effects are generally manageable and often lessen over time. However, let your doctor know if any of these symptoms become bothersome or don't improve.

More serious side effects require immediate medical attention, though they're less common. Because tofacitinib affects your immune system, you have a higher risk of developing infections.

Contact your doctor right away if you experience any of these concerning symptoms:

  • Fever, chills, or flu-like symptoms that don't improve
  • Unusual fatigue or weakness
  • Persistent cough or breathing difficulties
  • Unusual bruising or bleeding
  • Skin changes like new rashes or sores
  • Abdominal pain or changes in bowel habits

These symptoms could indicate serious infections or other complications that need prompt evaluation and treatment.

Rare but serious side effects include blood clots, particularly in the lungs or legs, and certain types of cancer. Your doctor will discuss these risks with you and monitor for any warning signs during your treatment.

Who Should Not Take Tofacitinib?

Certain people should avoid tofacitinib due to increased risks of serious complications. Your doctor will carefully review your medical history before prescribing this medication.

You shouldn't take tofacitinib if you have active, serious infections like tuberculosis or hepatitis B. The medication can make these infections worse by suppressing your immune system's ability to fight them.

People with a history of blood clots, heart problems, or certain cancers may not be good candidates for tofacitinib. Your doctor will weigh the benefits against these potential risks for your specific situation.

Here are conditions that typically prevent someone from taking tofacitinib:

  • Active tuberculosis or other serious infections
  • History of blood clots in lungs or legs
  • Severe liver problems
  • Low blood cell counts
  • Pregnancy or breastfeeding
  • Recent live vaccines

Your doctor will also consider your age, other medications, and overall health status when deciding if tofacitinib is right for you.

If you're planning to become pregnant or are breastfeeding, discuss this with your doctor. The effects of tofacitinib on pregnancy and nursing aren't fully understood, so alternative treatments might be safer.

Tofacitinib Brand Names

Tofacitinib is available under the brand name Xeljanz for immediate-release tablets and Xeljanz XR for extended-release tablets. Both formulations contain the same active ingredient but release it differently.

Xeljanz comes in 5mg tablets that you typically take twice daily. Xeljanz XR is an 11mg extended-release tablet usually taken once daily, which some people find more convenient.

Your doctor will choose the formulation that works best for your condition and lifestyle. Both versions are equally effective when taken as prescribed.

Tofacitinib Alternatives

Several other medications can treat the same conditions as tofacitinib, though they work through different mechanisms. Your doctor might consider these alternatives if tofacitinib isn't suitable for you.

Other JAK inhibitors include baricitinib (Olumiant) and upadacitinib (Rinvoq). These medications work similarly to tofacitinib but might have slightly different side effect profiles.

Biologic medications like adalimumab (Humira), etanercept (Enbrel), and infliximab (Remicade) are also effective for autoimmune conditions. These are given by injection or infusion rather than oral tablets.

Traditional disease-modifying drugs like methotrexate and sulfasalazine remain important treatment options. These medications have been used for decades and might be appropriate depending on your specific situation.

Is Tofacitinib Better Than Methotrexate?

Tofacitinib and methotrexate work differently and aren't necessarily better or worse than each other. The best choice depends on your specific condition, medical history, and personal preferences.

Methotrexate has been used for decades and is often the first medication doctors try for rheumatoid arthritis. It's generally well-tolerated and costs less than newer medications like tofacitinib.

Tofacitinib might be chosen if methotrexate doesn't work well enough or causes bothersome side effects. Some people prefer taking oral tablets over the injections that methotrexate sometimes requires.

Your doctor will consider factors like how severe your symptoms are, other health conditions you have, and your treatment goals when choosing between these medications.

Frequently asked questions about Tofacitinib (oral route)

Tofacitinib may increase the risk of heart problems and blood clots, especially in people who already have heart disease or risk factors. Your doctor will carefully evaluate your cardiovascular health before prescribing this medication.

If you have a history of heart attack, stroke, or blood clots, your doctor might recommend alternative treatments. They'll also monitor you closely if you do take tofacitinib, watching for any signs of cardiovascular complications.

Be sure to tell your doctor about any chest pain, shortness of breath, or leg swelling while taking tofacitinib. These could be signs of serious heart or circulation problems that need immediate attention.

If you accidentally take more tofacitinib than prescribed, contact your doctor or poison control center immediately. Taking too much can increase your risk of serious side effects, especially infections.

Don't wait to see if you feel okay, as some effects of an overdose might not appear right away. Your doctor may want to monitor you closely or adjust your treatment plan.

To prevent accidental overdoses, keep your medication in its original container with clear labeling. Consider using a pill organizer if you take multiple medications, but check with your pharmacist about the best way to store tofacitinib.

If you miss a dose, take it as soon as you remember, unless it's almost time for your next scheduled dose. In that case, skip the missed dose and continue with your regular schedule.

Never take two doses at once to make up for a missed dose, as this can increase your risk of side effects. Taking extra medication won't help you feel better faster and could be dangerous.

If you frequently forget doses, talk to your doctor about strategies to help you remember. Consistent dosing helps maintain steady levels of the medication in your system for the best results.

Only stop taking tofacitinib when your doctor tells you it's safe to do so. Most people with chronic autoimmune conditions need long-term treatment to keep their symptoms under control.

Your doctor will regularly evaluate whether tofacitinib is still helping you and monitor for any concerning side effects. They might adjust your dose or switch medications if needed, but these decisions should always be made together.

If you're concerned about side effects or feel the medication isn't working, schedule an appointment to discuss your options. There are often ways to address problems without stopping treatment entirely.

You can receive most routine vaccines while taking tofacitinib, but you should avoid live vaccines like the nasal flu vaccine or shingles vaccine. Your doctor will help you plan the safest vaccination schedule.

It's especially important to stay up to date with vaccines like the annual flu shot and pneumonia vaccine, as tofacitinib can make you more susceptible to infections. These vaccines can help protect you from serious illnesses.

Always tell healthcare providers that you're taking tofacitinib before receiving any vaccines. They can ensure you get the appropriate type and timing of immunizations for your situation.

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