TNF Inhibitors

medicine injections

Fast Facts

  • TNF inhibitors target an inflammation-causing substance called Tumor Necrosis Factor (TNF).
  • They can alter a disease’s effect on the body by controlling inflammation in the joints, gastrointestinal tract and skin.
  • Patients should talk to their doctor before getting any vaccinations while using an anti-TNF drug. Some vaccinations are safe, but live vaccines should be avoided.

TNF inhibitors are a type of drug used worldwide to treat inflammatory conditions such as rheumatoid arthritis (RA), psoriatic arthritis, juvenile arthritis, inflammatory bowel disease (Crohn’s and ulcerative colitis), ankylosing spondylitis and psoriasis. They reduce inflammation and stop disease progression.

How it works

TNF is a chemical produced by the immune system that causes inflammation in the body. In healthy individuals, excess TNF in the blood is blocked naturally, but in those who have rheumatic conditions, higher levels of TNF in the blood lead to more inflammation and persistent symptoms.

Uses

There are five different TNF inhibitors that have been approved by the U.S. Food and Drug Administration for the treatment of rheumatic diseases. To decrease side effects and costs, most patients with mild or moderate disease may be treated with methotrexate before adding or switching to an TNF inhibitor. These agents can be used by themselves or in combination with other medications such as prednisone, methotrexate, hydroxychloroquine, leflunomide, or sulfasalazine.

Dosing

The starting doses for RA are shown in Table 1. Similar doses are used for other rheumatic conditions. TNF inhibitors may be given by injection under the skin or by infusion into the vein. There are pamphlets and videos that can teach you how to give yourself an injection under the skin. Physicians, nurses, and pharmacists can also teach you how to give the injection.

The medicine can be injected into the thigh or abdomen. The site of injection should be rotated so the same site is not used multiple times. Infliximab and golimumab infusions are administered at a doctor’s office or an infusion center. These treatments take up to 4 hours.

TABLE 1: Comparison of anti-TNF drugs in RA
Drug Usual Dosing Regimen
Infliximab (Remicade ®)

Initially: Given at the clinic or at an infusion center as an intravenous infusion (IV) at a dose of 3-5 mg/kg (according to body weight) at weeks 0, 2, and 6.

Maintenance: IV infusions every 4-8 weeks. Dose may be increased to 5-10 mg/kg and frequency may be increased to every 4 weeks..

Etanercept (Enbrel ®)

Initially: 50 mg once a week or 25 mg twice a week as a self-administered subcutaneous injection.

Maintenance: Same

Adalimumab (Humira ®)

Initially: 40 mg every other week as a self-administered subcutaneous injection.

Maintenance: Same

Golimumab (Simponi ®)

Initially: 50 mg once per month as a self-administered subcutaneous injection.

Maintenance: Same

Certolizumab pegol (Cimzia) 

Initially: 400 mg (given as 2 x 200 mg injections) self-administered every 2 weeks at weeks 0, 2 and 4.

Maintenance: 200 mg every 2 weeks or 400 mg (2 x200 mg injections) every 4 weeks as a self administered injection. 

Time to effect

The time that it takes for the medication to have an effect may vary by patient. Most patients have reported a change in their symptoms after 2 or 3 doses but it usually takes 3 months to see the full benefit.

Side effects

The most common side effect seen with the injectable drugs are skin reactions, commonly referred to as “injection site reactions.” The patients usually complain of a localized rash with burning or itching. These reactions can last up to a week. Infliximab has been associated with a severe allergic reaction with swelling of the lips, difficulty breathing and low blood pressure. Your doctor will usually order a pre-medication to decrease the chances of an infusion reaction.

The most significant side effect is an increased risk for all types of infections, including tuberculosis (TB) and fungal infections. Some of these infections may be severe. Patients should be tested for TB before starting therapy because a hepatitis B infection can worsen during treatment. The usual way of testing is with a skin test, but a blood test is also available.

TNF inhibitors should be stopped if the patient has high fever or is being treated with antibiotics for an infection. Once the medication is stopped, it should not be restarted until the infection goes away.

Long-term use of TNF inhibitors may increase the risk of cancers such as lymphoma and skin cancer. There are rare neurologic complications as well. People who have a history of multiple sclerosis should not use them. People with significant heart failure should not use a TNF inhibitor because their heart disease could worsen.

Information to discuss with health care providers

These medications are expensive (more than $10,000 per year), but they are covered by most health care insurance plans. Copay amounts vary widely. Ask your doctor about prescription assistance plans that can help you to get the medication at a lower price or free of charge.Refer to the package insert for more information.

Updated February 2017 by Kelly Weselman, MD, and reviewed by the American College of Rheumatology Committee on Communications and Marketing.

This information is provided for general education only. Individuals should consult a qualified health care provider for professional medical advice, diagnosis and treatment of a medical or health condition.

© 2017 American College of Rheumatology