Rheumatoid Arthritis Medications

There are a variety of rheumatoid arthritis medications your physician or dermatologists may prescribe. These medications will work differently for each individual. We hope that with this information you will feel comfortable asking your physicians the right questions to help find the right treatment for you:

This information is part of CreakyJoints’ comprehensive guide for patients living with rheumatoid arthritis. Learn more or download Raising the Voice of Patients: A Patient’s Guide to Living with Rheumatoid Arthritis.

DMARD (Disease-Modifying Anti-Rheumatic Drug)

DMARDs are the most widely used and studied drugs used as therapy for RA. A DMARD is an RA medication that slows down the progression of your disease. DMARD stands for disease-modifying antirheumatic drug. Other than glucocorticoids (steroids), DMARDs have been on the market the longest and have the most evidence to support their use. The most commonly used DMARD is methotrexate (Rheumatrex®, Trexall®). Another commonly used DMARD is leflunomide (Arava®). Other DMARDs include hydroxychloroquine (Plaquenil®) and sulfasalazine (Azulfidine®). Hydroxychloroquine (Plaquenil) and sulfasalazine (Azulfidine) are often used for milder RA. They are thought to have fewer possible side effects.

Methotrexate (Trexall®, Rheumatrex®, Otrexup®, Resuvo®)

Methotrexate for RA: What do we already know?

Methotrexate is considered the gold standard in terms of monotherapy treatment of RA with a DMARD, and is generally the first choice.

Methotrexate works by blocking enzymes that help DNA (genetic material in the cells of your body) form or repair. This prevents some cells in your body from reproducing themselves. Experts believe that methotrexate also interacts with your immune system. Although it is not entirely clear how methotrexate works in RA, it’s been proven to be effective in reducing swelling, pain, and long-term damage to joints.

Methotrexate is given once a week as either a pill or shot. Some people have better results with the shot, as the medicine is absorbed differently this way and is better tolerated by people who may have experienced an upset stomach when taking the pill form.

What are the possible side effects of methotrexate?

It’s important to remember that most patients do not experience serious side effects from methotrexate, and for those who do have them, they may improve with time. Side effects are more likely to occur at higher doses and you should always consult your doctor if you think you’re experiencing any of these side effects.

  • Gastrointestinal problems, such as nausea, stomach upset, and loose stool
  • Mouth ulcers
  • Hair loss
  • Abnormal liver function blood tests
  • Abnormal blood counts

Rare side effects of methotrexate include liver cirrhosis or scarring. This usually happens with patients who already have liver problems or are taking more drugs that impact the liver. Lung problems also occur rarely, and typically only with patients who already have lung issues. Report any difficulty breathing or a cough that won’t go away to your doctor. Take these side effects very seriously.

People with liver disease may not be able to take methotrexate or require closer monitoring or lower dosing.

Increased skin sensitivity to the sun can also occur, but may stop when the medication is stopped. Supplements like folic acid may help you manage these side effects. If regular folic acid doesn’t help, you may try another type called methylated folic acid. Talk to your doctor about getting methylated folic acid if you still get mouth ulcers, hair loss, or just a “yucky feeling” from your methotrexate. Vitamin A and dextromethorphan (the DM in Robitussin DM) can also be used to help with those side effects.

Do not get pregnant while taking methotrexate. For women, recommendations vary from 1 month to 3 months as to how long you should be off methotrexate before getting pregnant. The package insert recommends male patients be off methotrexate for 3 months.

Certain antibiotics such as “sulfa” drugs (i.e. Bactrim) should not be taken with methotrexate. Check with your physician before taking an antibiotic with your methotrexate.

Hydroxychloroquine (Plaquenil®)

Hydroxychloroquine (Plaquenil)is often used alone in mild RA or in combination with other medications in people with more severe RA.

Hydroxychloroquine for RA: What do we already know?

Hydroxychloroquine (Plaquenil) is an antibiotic used to treat malaria, but it also works to treat symptoms of RA, lupus, and other rheumatic diseases. It can reduce your joint pain and swelling. In the long term, it may help prevent joint damage or lower your risk of joint disability.

We don’t really know why this drug works to control RA symptoms or complications. One theory is that hydroxychloroquine (Plaquenil) interferes with communications between the cells of your immune system.

Your hydroxychloroquine (Plaquenil) dose will be based on your weight. Usually, adults with RA will take either 200 or 400 mg of hydroxychloroquine (Plaquenil) per day in pill form.

What are the possible side effects of hydroxychloroquine (Plaquenil)?

Most people tolerate hydroxychloroquine (Plaquenil) well. Some side effects include nausea and diarrhea, but they may lessen over time or if you take your pills with food. Less common side effects are rashes, changes in your skin’s pigment (like dark spots), changes to your hair (like thinning), or muscle weakness.

Although rare, hydroxychloroquine (Plaquenil) use could lead to damage of the cells in the back of your eye that detect light and color. You’ll receive a specialized baseline eye exam when you start the drug. Later, you’ll follow up with your ophthalmologist as directed. The most recent recommendations say you don’t need a follow-up eye exam for five years, but you may need one sooner depending on your other medical conditions or if you have changes in your vision while taking hydroxychloroquine.

Hydroxychloroquine seems to be safe during pregnancy, but any time you are considering pregnancy you should discuss all medications with your doctor.

Other rare side effects of hydroxychloroquine (Plaquenil) are:

  • Anemia, especially in people with porphyria
  • Muscle weakness

Leflunomide (Arava®)

Leflunomide (Arava) is used to treat moderate to severe RA. It can lower joint damage and disability that RA can cause. It can also help ease your symptoms. It may be used alone or in combination with other DMARDs.

Leflunomide for RA: What do we already know?

Leflunomide (Arava) blocks the development of certain cells in your immune system. By doing this, leflunomide (Arava) works to suppress your immune system and reduce inflammation that causes pain, swelling, and other symptoms.

The typical dose of leflunomide (Arava) is one 20 mg pill a day. Some people may take 10 mg a day, especially if the higher dose causes side effects. You should take your leflunomide (Arava) with food.

Your doctor may prescribe a “loading dose” of leflunomide (Arava) for you, which means you’ll be prescribed extra drug in the beginning to give the medication a chance to build up in your body and become effective. Because of the possibility of increased side effects with a loading dose, most rheumatologists do not use loading doses of leflunomide (Arava). Without the loading dose it may take a little longer (six to twelve weeks) to notice a benefit from leflunomide (Arava).

One of the side effects of leflunomide (Arava), like methotrexate, is the potential for liver toxicity. So you shouldn’t drink alcohol or take certain medications while you take leflunomide (Arava). If you’ve had significant liver disease in the past, leflunomide (Arava) may not be right for you. You’ll need regular liver function blood tests to make sure your liver is healthy.

Leflunomide (Arava) can also be harmful to an unborn fetus. It can cause serious birth defects, so you should take extra precautions not to get pregnant while taking this drug. Because leflunomide (Arava) can stay in your system anywhere from 10 weeks to 2 years, it is important to get a blood test to see if the drug is still in your blood before even trying to get pregnant. Breastfeeding should be avoided as well, unless leflunomide (Arava) is completely out of your system. Men who take leflunomide (Arava) should also use birth control to avoid getting their partner pregnant because of the birth defect risk.

What are the possible side effects of leflunomide (Arava)?

The most common side effect of leflunomide (Arava) is diarrhea. It often gets better over time. You can take anti-diarrheal medicines to ease this side effect, or even lower your leflunomide (Arava) dose.

Other side effects include nausea, indigestion, hair loss, stomach pain, liver toxicity, or skin rashes. More rarely, this drug may lower your amount of blood cells or platelets, or cause lung problems like cough or shortness of breath.

Leflunomide (Arava) may also raise your risk of getting infections. Let your doctor know if you have signs of an infection, like fever or chills.

Sulfasalazine (Azulfidine®)

Sulfasalazine (Azulfidine) is used to treat RA symptoms like pain or swelling. Over time, it can help slow down the progression of your disease. It may be used alone or in combination with other DMARDs.

Sulfasalazine for RA: What do we already know?

Sulfasalazine (Azulfidine) is part of a class of medicines called sulfa drugs. It’s a mix of salicylate, which is the main ingredient in aspirin, and an antibiotic. Some people are allergic to all sulfa drugs, so they can’t take sulfasalazine (Azulfidine).

We don’t know exactly why sulfasalazine (Azulfidine) eases RA symptoms like pain, swelling, or joint stiffness. It may prevent joint damage and over the long term, loss of your joint function.

Most people take two 500 mg tablets of sulfasalazine (Azulfidine) twice per day. Some people may start with a lower dose, such as one or two tablets per day, then build up to the normal dose. Some people may need six 500 mg tablets per day.

You should take your sulfasalazine (Azulfidine) with food and a full glass of water to help ease stomach side effects. You shouldn’t crush or chew up your sulfasalazine (Azulfidine) tablets.

Sulfasalazine (Azulfidine) should be safe to take during pregnancy but, as always, you should check with your physician if you are planning a pregnancy. It may be necessary to take extra folic acid if you continue on sulfasalazine during pregnancy. However, using it during breastfeeding may cause a serious type of jaundice in babies.

If you have an infection, your doctor may have you stop taking sulfasalazine (Azulfidine).

What are the side effects of sulfasalazine (Azulfidine)?

Most people have few side effects with sulfasalazine (Azulfidine). The most common ones are nausea, stomach upset, and headache. Usually, this gets better over time. You can take a coated sulfasalazine (Azulfidine) pill that may be easier to digest.

Rarer side effects of sulfasalazine include headache, skin rashes, itching, mouth sores, or liver or lung problems. If you get a severe rash, tell your doctor.

Sulfasalazine (Azulfidine) may make your skin more sensitive to sunburns, so wear a high SPF sunblock lotion or avoid getting too much sun. Some people who take sulfasalazine (Azulfidine) have orange-colored urine or skin. While this seems alarming, it’s actually harmless. It will go away when you stop taking this drug.

Sulfasalazine (Azulfidine) can make it harder for you to fight off infections because it can lower the amount of white blood cells your body makes. Your doctor can test your blood to make sure your blood cell levels are healthy.

Treatment Changes

What if the monotherapy doesn’t work? What next? If your RA disease activity remains moderate or high despite DMARD monotherapy, another DMARD agent, biologic agent, or JAK inhibitor may be added to your DMARD.

Combination Therapy

Everyone is different. In some cases, methotrexate or hydroxychloroquine (Plaquenil) might not work by itself or at all. In those cases, a doctor will discuss the following with you:

  • Double therapy: Double therapy is the use of two different medications, usually methotrexate and another DMARD, such as leflunomide, sulfasalazine, or hydroxychloroquine.
  • Triple therapy: Triple therapy uses three medications instead of two. Monitoring for both triple and double therapy is similar to monitoring for DMARD monotherapy. Closer monitoring, initially, may be warranted depending on the combination of medications.

Sometimes, combination therapy will include the use of a biologic. Evidence shows that more aggressive treatments are associated with better control of the disease, slower radiological progression (meaning that your X-rays or imaging scans show that your joint damage is slowing down), and improved functional outcomes. There are many combinations of medications, although there is uncertainty around which is the most effective.

It’s up to your doctor to decide which medication combination is best for you. In general, combination therapy is well tolerated, but needs to be monitored closely for any increased side effects. As always, there is a risk for infection in people who are using DMARD and biologic therapy. Alert your doctor if you notice any sign of infection, such as fever, chills, or flu-like symptoms.

Biologics

Biologics are a newer type of medication produced by living cells. They’re designed to act like the proteins that are already in your body. They target specific areas of your immune system. Because they’re so specific, they can cause fewer side effects than DMARDs. Infection is one possible side effect of biologics. Your rheumatologist will watch you closely for any signs that you have an infection. Biologics can be used alone or in combination with methotrexate or another DMARD. Due to their specificity, if one biologic fails, another may work for you. Keep the dialogue open with your doctor in the case that you may need to switch.

TNFi biologics

These biologics work by targeting something called tumor necrosis factor proteins, or TNF. TNF is a protein that sends signals to your body, eventually leading to inflammation that causes swelling, pain, and stiffness. By inhibiting, or stopping, TNF, these medications can reduce inflammation. That’s why they’re often called TNF inhibitors (or TNFi).

Some common TNFi biologics are adalimumab (Humira®), certolizumab pegol (Cimzia®), etanercept (Enbrel®), golimumab (Simponi®, Simponi Aria®), and infliximab (Remicade®).

These biologics are molecules that are specially designed to target TNF and block it at the source. They can cool down your immune response that’s out of control in RA.

Your doctor may prescribe TNFi biologics if previous DMARD monotherapy was ineffective. Personal considerations such as out-of-pocket cost, comorbidities, and side effects may make TNFi therapy (often with the addition of methotrexate) the best option.

For individuals with established RA, TNFi biologics could be an addition to your DMARD monotherapy or double therapy, or used alone. Your rheumatologist will determine which option is best for you based on your personal medical history.

Make sure you have a talk with your physician about why a certain treatment option is best for you. Treatments like TNFi are very case-specific.

How do I take my TNFi biologic?

You may be able to give yourself this medication, via injections, at home (known as “self-injection”), or via an infusion in the doctor’s office or other infusion site. A healthcare professional will indicate where on your body it is safe to administer these injections (usually the upper leg or stomach). Make sure to rotate the injection sites. If you have psoriasis, do not inject in affected areas. If you’re afraid to inject yourself, talk to your nurse, clinic staff, or pharmacy about having someone there give you these shots.

Be sure you are confident on how to do this procedure before you administer the medication on your own. Don’t be afraid to ask for help!

You may also get your biologic as an infusion instead of a shot. A healthcare professional gives you the drug through an IV. You’ll get your treatment in your doctor’s office, at a special infusion center, or at your local hospital. You and your doctor can decide if an infusion is the right option for you. The infusions can last as little as 30 minutes, or could take up to several hours — depending on the drug, dose, and individual.

Adalimumab (Humira) is given as a 40 mg self-administered subcutaneous (under the skin) injection every other week.

Certolizumab pegol (Cimzia) is given as a subcutaneous injection of 400 mg on weeks 0, 2, and 4, followed by 200 mg every two weeks or 400 mg every four weeks. Cimzia can also be given in a lyophilized (dehydrated and freeze-dried) formula that is given in the doctor’s office.

Etanercept (Enbrel) is given as a 50 mg self-administered subcutaneous injection every week or 25 mg self-administered injection twice weekly.

Golimumab (Simponi) is given as a 50 mg self-administered subcutaneous injection once monthly.

Golimumab (Simponi Aria) is given via IV infusion in the clinic or infusion center on weeks 0 and 4, followed by IV infusion every eight weeks. Dose is based on weight.

Infliximab (Remicade) is given via IV infusion in the clinic or infusion center at weeks 0, 2, and 6, then by infusion every four to eight weeks. Dose is based on weight.

The benefits of TNFi inhibitors are usually seen within a few weeks (but can take up to four to six weeks), unlike DMARDs, which can take up to a few months to have their effects.

Side Effects of TNFi Biologics

Side effects of TNFi’s might include injection site reactions, upper respiratory infections, laboratory abnormalities, and headache. The likelihood of experiencing these and any side effects vary from individual to individual, and should always be discussed with your doctor before beginning treatment.

Infliximab has been associated with the development of antinuclear and anti-double stranded DNA antibodies, nausea, abdominal pain, and infusion reactions. Serious side effects include increased risk of infection, especially tuberculosis and fungal infections. Untreated hepatitis B may worsen while taking TNFi’s. You should be tested for TB and hepatitis before starting one of these medications. Less common side effects include allergic reaction and development of other immune system disorders. If you have had cancer of any type, or have an increased risk, you will need to discuss the various options with your rheumatologist regarding the use of any biologics.

If you think that you might have an infection, check with your doctor before taking your drug. Biologic drugs make it harder for your body’s immune system to fight off infections. They may even make it harder for you to spot the early signs of infection, so talk to your doctor about what to look for.

For more information, go here.

If you’re planning to have surgery, talk to your rheumatologist first. You may need to go off your biologic for some time before you have the surgery.

TNFi Biologics Contraindications

Live and attenuated live vaccines, such as the shingles vaccine, yellow fever vaccine, and Flumist® (intranasal flu vaccine), should not be given when taking a TNFi biologic. These medications can interact with vaccines and certain foods and medications. Make sure you talk to your doctor about current medications, planned vaccinations, and any diet changes you make (use of vitamins, herbal products).

Adalimumab (Humira) specifically interacts with blood thinners (i.e. warfarin (Coumadin®)).

Existing Conditions and TNFI biologics

  • Congestive Heart Failure (CHF): TNFi biologic therapy is not recommended for patients living with uncontrolled CHF, as it can lead to a worsening of this condition.
  • Previous Serious Infection: TNFi drugs have been found to increase the incidence of pneumonia, tuberculosis (TB), certain fungal diseases, and skin/soft tissue infection. You will be required to be tested for TB before starting any biologic drug.
  • Hepatitis C without Receiving Antiviral Therapy: The ACR recommends that your physician speak with a gastroenterologist and hepatologist to consider the management of these two disease states. TNFi can be carefully administered while managing treatment of hepatitis C.
  • Previously Treated Lymphoproliferative Disorder: TNFis can increase your chances of lymphoma. As an increased risk of lymphoma in RA patients taking TNFis compared to a non-RA population has been shown in studies, these biologics are not recommended for patients with a previous history of lymphoproliferative disorders.

People who have or have had multiple sclerosis should not take TNFi drugs.

Be sure to tell your doctor if you are: pregnant or breastfeeding and/or have kidney or liver disease, cancer, CHF, blood or bone marrow problems, or any type of infection. Also mention any nervous-system problems such as Guillain-Barré syndrome or multiple sclerosis. They may indicate that you should not be on TNFis.

When starting most biologics, you’ll need to take frequent blood tests to monitor the drug’s effects. Once you’re established on a biologic, however, your tests will become less frequent. Specifically, for TNFi biologics, blood tests will be done to check for bone marrow suppression, a low white blood cell count, or effects on the liver.

Other Biologics

Biologics for RA: What do we already know?

There are other biologics that target the immune system in different ways from TNFi drugs. They interact with different kinds of white blood cells, such as T cells or B cells, in your immune system. They can also block chemicals called cytokines that cause inflammation.

White blood cells and cytokines are made by your immune system to fight off infection. But in RA, they may be out of control and cause inflammation. So these drugs can suppress your immune system, ease inflammation, stop RA’s progress, and ease your symptoms.

What do the recommendations say?

If disease activity remains moderate or high despite use of DMARD therapy, biologics that target the immune system in different ways from TNFi drugs or a JAK inhibitor may be added to the DMARD or used alone without a DMARD, depending on the drug.

Why am I prescribed a biologic?

Your doctor may prescribe a biologic if previous DMARD monotherapy was ineffective. Personal considerations such as out-of-pocket cost, comorbidities, and side effects may make a biologic (often with the addition of methotrexate) the best option.

How will I take my biologic?

You may be able to give yourself this medication, via injections, at home (known as “self-injection”), or via an infusion in the doctor’s office or other infusion site. A healthcare professional will indicate where on your body it is safe to administer these injections (usually the upper leg or stomach). Make sure to rotate the injection sites. If you have psoriasis, do not inject in affected areas. If you’re afraid to inject yourself, talk to your nurse, clinic staff, or pharmacy about having someone there give you these shots.

Be sure you are confident on how to do this procedure before you administer the medication on your own. Don’t be afraid to ask for help!

You may also get your biologic as an infusion instead of a shot. A healthcare professional gives you the drug through an IV. You’ll get your treatment at a special infusion center, in your doctor’s office, or at your local hospital. You and your doctor can decide if an infusion is the right option for you. The infusions can last as little as 30 minutes or could take up to several hours — depending on the drug, dose, and individual.

Some common biologics that work differently than TNFi biologics:
Abatacept (Orencia®), rituximab (Rituxan®), or tocilizumab (Actemra®)

Potential Side Effects of Biologics

As with all biologics, the greatest risk while taking these drugs is infection. Notify your doctor immediately if you experience the signs of infection: fever, chills, or nausea.

Side effects of Abatacept (Orencia)

Abatacept works by blocking signaling to a special kind of white blood cell called a T cell. The most common side effects of abatacept (Orencia®) are headaches, colds, sore throats, nausea and in children, diarrhea, cough, fever, and abdominal pain. In rare cases, allergic reactions, hives, shortness of breath, or low blood pressure may occur. Serious side effects such as infections may occur. You should not receive a live vaccine while on abatacept (Orencia®). Abatacept can be given by IV infusion or self injected

Side Effects of Tocilizumab (Actemra)

Tocilizumab works by blocking a cytokine known as Il-6 that can cause inflammation. Rare reactions include fever and chills and increased risk of infection. Increased cholesterol levels and/or an increase in liver enzymes may also occur. A very rare complication that may occur is bowel perforation, or a hole in the bowel wall. Notify your doctor immediately if you have a history of diverticulitis, develop abdominal pain, or have bloody bowel movements while taking tocilizumab (Actembra®). Tocilizumab can be given by IV infusion or self-injected.

Side Effects of Rituximab (Rituxan)

Rituximab works by blocking a special kind of white blood cell known as B cells. Some patients can feel side effects during or up to 24 hours after receiving rituximab (Rituxan®). They can include mild throat tightening, flu-like symptoms, rash, itchiness, dizziness, and back pain. In rare cases, patients may experience wheezing, mouth or throat swelling, trouble breathing, or chest pain. Other side effects may include headache, cough, nausea, upset stomach, sweating, nervousness, muscle stiffness, and numbness. In very rare cases, a severe skin reaction, mouth sores, vision changes, loss of balance, difficulty walking, or confusion may occur. Contact your doctor immediately if you experience these. Rituximab is given by IV infusion.

Some side effects can be reduced by taking a steroid injection before your rituximab (Rituxan®) infusion, or by taking acetaminophen (Tylenol®) or diphenhydramine (Benadryl®). Sometimes an infusion may be stopped and then restarted at a slower rate to ease the frequency of side effects.

How to Monitor

You may have to undergo regular blood testing while on a biologic. Blood tests are also used to measure liver and kidney function, as these are the organs that process what goes through your body. Complete blood counts (CBCs) are tests that measure your bone marrow health and immune cells. This is checked when you get your blood drawn while you’re taking these drugs. By monitoring your blood, your medical team is able to ensure that your body can fight infection without causing the pain, stiffness, and swelling of arthritis.

Again, it’s important for you to watch for any signs of infections, like coughs, discomfort when you urinate, or if you have cuts that aren’t healing. If you have any of these signs in between your doctor’s visits, let your doctor know before you take your next biologic dose.

Biologics Contraindications

With all of the biologics there are times when these medications should not be used. Some of these situations include a history of recurrent life-threatening infection, untreated tuberculosis or other active infection, history of lymphoma (except for rituximab), active demyelinating disease (MS), or active hepatitis B.

Existing Conditions and Biologics

Previously Treated or Untreated Skin Cancer (Non-Melanoma or Melanoma): These biologics are not contraindicated in this condition, but it’s very important to have careful monitoring by a dermatologist.

Comorbidities

Chronic respiratory conditions, diabetes, heart disease, and stroke. Talk with your doctor if you have any of these comorbidities. In some cases, medications to treat these conditions may interact with your biologics. It is important that your doctor is giving you the proper treatments for your health concerns.

For more information on biologic drugs, go here.

Janus Kinase (JAK) Inhibitors

JAK inhibitors are a new class of arthritis drugs that treat RA. They’re not biologics. They are known as small molecule medications.

JAK inhibitors come in pill form. They decrease your immune system’s ability to make certain enzymes that can lead to RA symptoms. The first JAK inhibitor is tofacitinib (Xeljanz®). Many others are being developed now, and may be approved soon.

JAK inhibitors can be used with or without methotrexate. Your rheumatologist may even prescribe this drug before you try a biologic if he or she thinks it’s the right option for you.

Tofacitinib (Xeljanz®)

What is Tofacitinib?

Tofacitinib (Xeljanz) is used to treat RA in patients who cannot tolerate methotrexate. It’s one of a newer class of arthritis drugs called janus kinase (JAK) inhibitors.

Tofacitinib for RA: What do we already know?

Tofacitinib (Xeljanz) works by decreasing the effectiveness of the immune system to reduce pain, swelling, and inflammation.

What do the recommendations say?

According to the ACR’s RA treatment guidelines, “the voting panel strongly recommended the use of tofacitinib (Xeljanz) for patients with established RA with moderate or high disease activity despite DMARD monotherapy.”

Why am I taking tofacitinib?

Your doctor may prescribe tofacitinib (Xeljanz) if you are not able to tolerate methotrexate, or if you have taken methotrexate without any result. You may be taking tofacitinib (Xeljanz) alone or in combination with another drug.

How do I take tofacitinib?

Tofacitinib (Xeljanz) comes in tablet form. It can be taken once or twice a day, usually without food. You should take tofacitinib (Xeljanz) at the same time every day. It is a good idea to read the label carefully and talk with your doctor to make sure you fully understand how to take your medication.

There are two forms of tofacitinib (Xeljanz), although both are tablets. Extended-release tablets typically have 11 mg of medication and are taken once a day. They are broken down differently by your body, and release the product at a slower rate. Rapid release tablets typically have 5 mg of medication and are taken twice a day. They are broken down quickly and release the product much faster.

How long will it take for tofacitinib to work?

With tofacitinib (Xeljanz), you may start to see an improvement in your symptoms in as little as two weeks. However, it typically takes up to three to six months to reach full effectiveness.

When to Talk to Your Doctor While Taking Tofacitinib

Talk to your doctor if you experience any of the following:

  • Negative reactions or side effects
  • Concerns about why you have been prescribed this drug
  • Your symptoms do not improve within six months
  • Questions or confusion about your medication usage
  • If you are planning surgery
  • If you are planning on missing your dose for any reason
  • Possible signs of an infection like chills or nausea
  • Fever
  • If you may be pregnant

Side Effects of Tofacitinib

Many patients do not experience side effects, and those who do rarely experience serious side effects. Many side effects become less serious and frequent over time. Some less serious side effects include:

  • Nausea
  • Indigestion
  • Diarrhea
  • Headaches
  • Upper respiratory tract infection
  • Increased cholesterol levels

In rare cases, more serious side effects can occur, such as:

  • Infection
  • Abnormal blood counts
  • Abnormal liver function tests
  • Increased risk of bowel perforation
  • Decrease in kidney function

Taking your medication as prescribed by your doctor, getting your blood regularly monitored, and attending all your medical appointments will reduce the occurrence and seriousness of any side effects.

How to Monitor

While you are taking tofacitinib (Xeljanz), you will need to get periodic blood tests so your doctor can monitor different values. This is to ensure that the medication is working effectively and to keep track of whether or not there are any negative side effects.

Lymphocyte count: You’ll need this test once before you begin taking tofacitinib (Xeljanz) to note your “baseline,” and then every three months after. Lymphocyte counts are used to measure your white blood cells. White blood cells are an important part of your immune system. Lymphocyte counts are used to determine whether or not the medication is working, and to make sure that your immune system can still prevent you from getting an infection. If your lymphocyte count is too low, your doctor may change your dosage or medication.

Neutrophil/platelet counts: You’ll need this test once to note your baseline, once after four to eight weeks, and every three months after. Neutrophil counts measure another type of white blood cells, and so they are monitored as another way to ensure your medication is working and not causing harm. Platelets are also a part of your immune system, but control your blood’s ability to clot. If you have too few, there is a risk for unusual bleeding. If your blood work shows too few platelets or neutrophils, your doctor may adjust your dosage or medication.

Hemoglobin: You’ll need this test once to note your baseline, once after four to eight weeks, and every three months after. Hemoglobin is a part of your red blood cells, and helps carry oxygen in your bloodstream. Too little hemoglobin can lead to increased abnormal bleeding. Monitoring can reveal whether or not you are at risk for bleeding, and if your hemoglobin is too low, your doctor may adjust your medication.

Lipids: You’ll need this test four to eight weeks after you begin taking the medication and periodically afterward. Lipid levels are measured to ensure that tofacitinib (Xeljanz®) is not having a negative effect on your cholesterol levels.

LFTs: LFTs, or Liver Function Tests, should be done periodically to ensure that liver damage does not occur.

Viral Hepatitis: Prior to starting your medication, you should be tested for viral hepatitis. You should not take this drug if you are positive for viral hepatitis.

You will also need to have your heart rate and blood pressure periodically monitored, as well as skin tests, and signs and symptoms of any potential infections. This is to ensure that you’re not having any negative side effects. If you have any potential harmful impacts from taking this drug, your doctor may adjust your dosage or medication.

Tofacitinib Contraindications

Contraindications for tofacitinib (Xeljanz) are: having a history of a reaction to tofacitinib, pregnancy, some liver disease, some kidney disease, blood disorders, some cancers, active infections, or a history of active tuberculosis.

Tofacitinib Comorbidities

Talk with your doctor if you have any of these comorbidities: chronic respiratory conditions, diabetes, heart disease, or stroke. In some cases, medications to treat them may interact with tofacitinib (Xeljanz), and it is important your doctor is giving you the proper treatments.

Glucocorticoids

What are Glucocorticoids?

Glucocorticoids are medicines used to reduce inflammation. They may also be called corticosteroids or even “steroids” for short. The most commonly prescribed glucocorticoids are prednisone and methylprednisolone (Medrol®).

Glucocorticoids for RA: What do we already know?

These medications can reduce RA symptoms very quickly. They’re often used as a “bridge therapy” while you’re waiting for your DMARD or biologics to kick in. They can also be used if you have a flare and need quick symptom relief.

Glucocorticoids are designed to act the same way as the hormones (natural steroids) made by your adrenal glands that sit on top of your kidneys. They can suppress inflammation and make your immune system less active. Increasing the dosage to more than 6 mg per day can also raise the likelihood of side effects.

Why am I taking a glucocorticoid?

More than likely, you are taking glucocorticoids short term to help treat joint pain and swelling during a flare or while you’re waiting for your DMARD or biologic drug to take effect. Sometimes, none of your other medications reduce your symptoms enough, so you add a low dose of steroids. Because steroids have side effects, it’s best to take the lowest possible dose you need to ease your symptoms. You should never suddenly stop your steroids if you have been taking them for longer than two weeks, unless you have tapered to a low enough dose as directed by your doctor.

What are the possible side effects of glucocorticoids?

  • Increased infection risk
  • Diabetes
  • Hypertension
  • High blood pressure
  • Weight gain
  • Osteopenia and osteoporosis (thinning or weakened bones)
  • Glaucoma or cataracts in your eyes
  • Acne
  • Roundness of the face or “moon face”
  • Nervousness and inability to sleep (particularly if you take it at night)

Your chances of having these side effects depend on your dose, how long you take glucocorticoids, or if you have other medical conditions.

How to Monitor

You and your doctor should be on the lookout for any of the above side effects. If you have these, you may need to adjust your steroid dose. If you have diabetes you will need to check your blood sugar more often and may have to adjust your medication, as steroids can increase your blood sugar. Your doctor will review your use of glucocorticoids often. You probably won’t need to keep taking these drugs for very long.

How can I reduce the side effects of glucocorticoids?

Here are some steps you can take to lower your risk of side effects from glucocorticoids:

  • Increase your calcium and vitamin D intake, and do weight-bearing exercises to protect your bones. You may need to take a medicine to protect your bones if you remain on steroids for a long time.
  • Eat plenty of green, leafy veggies, and lower your intake of sugar and salt to prevent weight gain, diabetes risk, and high blood pressure.
  • Cut back on or quit smoking and drinking alcohol to boost your bone and heart health.

Biosimilars

There’s another new option that will soon be available to treat RA: biosimilar drugs. These are very similar copies of the various biologics that are already on the market. You may have seen this term in the news, or even heard your doctor or nurses mention it. Biosimilars are drugs that are made to be very similar to existing biologic drugs like TNF inhibitors.

The difference between biosimilars and generic drugs

Biosimilars are not exactly like generic drugs, which are exactly the same as the original, brand-name drug, but usually cheaper. But because they use already-completed research to be developed, biosimilars are designed to take less time and clinical trial data to approve, and should be cheaper than the original biologic drug. Biosimilars’ names include the original drug’s generic name and a four-letter suffix to distinguish it. Once approved, biosimilars should have registered (®) brand names of their own.

Approved Biosimilars

In 2016, three biosimilars to biologics used to treat RA have been approved by the FDA so far:

  • Infliximab-dyyb (Inflectra®)
  • Etanercept-szzs (Erelzi®)
  • Adilimumab-atto (Amjevita)

Biosimilar development & approval process

More biosimilars to biologics used to treat RA are in development now. Due to patent exclusivity held by the innovator drug manufacturers, biosimilars may not be immediately available. There are ongoing challenges to patent rights that are currently in the court system to determine when the particular biosimilar will be permitted to be sold.

The Interchangeability of Biosimilars

Biosimilars will be taken in the same way as their reference drug, and have the same possible side effects, contraindications, and monitoring tests. All biosimilars have to meet the same standards of safety and efficacy as any other prescription drug approved by the FDA. But because they cost less to develop and test, they may not be quite as expensive as other biologics. However, biosimilars are not identical to the original drug — they’re just highly similar.

Each state has different laws about how biosimilars may be substituted for their reference biologic when a prescription comes to the pharmacy. If you have any concerns, talk to your doctor about your state’s rules. More than 35 states have passed laws so far that require pharmacies, including mail-order specialty pharmacies, to notify doctors if they plan to substitute a biosimilar for the reference biologic. Physician associations, pharmacists’ groups, the FDA, pharmaceutical companies, and others are still debating these issues.

In the future, there are expected to be biosimilars that are so close to their reference biologics that the FDA will designate them as interchangeable. There are no interchangeable drugs in development yet, and the FDA has not even established the criteria for designating a drug as “interchangeable.”

When and if a drug is given the interchangeable tag in the future, pharmacists may be able to substitute that drug for the original reference biologic when they fill a prescription from a rheumatologist.

RAISE YOUR VOICE: Biosimilars for RA are being approved by the FDA now, and more are on the way soon. These drugs will offer you more options to treat your RA, control inflammation, and ease symptoms. The first step to take is to ask your rheumatologist if there’s a biosimilar available that’s right for you. Start a conversation with your doctor about biosimilars to your current RA biologic drug, and what potential risks, benefits, or savings you may have if you switch. Call your insurance company to find out if a biosimilar to your current RA biologic is on their formulary, and how much the biosimilar may cost for you. Information is power. You deserve clear, simple information — including side effects, risks, benefits, and out-of-pocket costs — for all your treatment options. Once approved by the FDA, biosimilars’ manufacturers will also have websites that tell you more about these treatments and patient assistance programs, which may offer you discounts and savings.