Tocilizumab

Belonging to a class of medication called interleukin-6 (IL-6) receptor inhibitors, tocilizumab injection works by blocking the activity of interleukin-6, the substance that causes inflammation.

Overview

Tocilizumab (brand name Actemra) is a biologic medication approved for the treatment of patients with moderate to severe cases of Polyarticular Juvenile Idiopathic Arthritis (PJIA), active rheumatoid arthritis (RA), giant cell arteritis and Systemic Juvenile Idiopathic Arthritis (SJIA). The drug works by blocking inflammatory protein IL-16 to improve swelling and joint pain caused by arthritis as well as other symptoms caused by inflammation.

For adults with rheumatoid arthritis or giant cell arteritis, tocilizumab can either be administered as a monthly intravenous infusion or as a subcutaneous injection on a weekly or bi-weekly basis. For people with Polyarticular Juvenile Idiopathic Arthritis and Systemic Juvenile Idiopathic Arthritis, the medication is administered intravenously on a monthly basis. When administered as a subcutaneous injection, tocilizumab can be injected either into the abdomen or thigh. The spot of injection should be rotated to avoid injecting the medication into the same spot multiple times. Some patients will begin experiencing improvements within weeks after the first tocilizumab treatment.

Tocilizumab may be taken along or in combination with methotrexate or other non-biologic medications. However, the drug should never be used alongside another biologic medication. During medication, blood tests should be conducted to monitor rise in cholesterol and liver enzymes as well as a reduction in blood cell count.

How tocilizumab works

Besides other physiological functions, interleukin 6 (IL-6) is involved in the development of inflammatory and immunological reactions. Autoimmune diseases like rheumatoid arthritis are associated with abnormally high levels of IL-6. Tocilizumab works by binding soluble as well as membrane-bound interleukin-6 receptors to prevent IL-6 from exerting its pro-inflammatory effects. Studies have found that the soluble form and membrane bound form of the IL-6 receptors may have different effects on the pathogenesis of RA, with the soluble form being more implicated in the progression of the disease.

Before taking tocilizumab…

Tell your healthcare provider if you have ever suffered from tuberculosis, if anyone in your household is currently treating tuberculosis or if you have recently traveled to a location where certain infections are prevalent (Mississippi River Valley, Ohio River Valley, and Southwest).

Tell your healthcare provider if you are experiencing any signs of infection like chills, fever, cough, fatigue, body aches, skin wounds and open sores, stomach pain, diarrhea, weight loss, coughing up blood and painful urination.

Tell your doctor if you have any allergies. You should never use this medication if you are allergic to tocilizumab or any of its ingredients.

To be sure that tocilizumab is right for you, tell your healthcare provider if you have ever had the following:

  • An infection such as pneumonia, herpes, or yeast infection
  • HIV/AIDS
  • Liver disease
  • Stomach ulcer, diverticulitis, or any form of stomach or intestinal bleeding
  • A weak immune system
  • Diabetes
  • Hepatitis B or if you are a carrier of the virus
  • Cancer
  • Nerve-muscle disease like multiple sclerosis; or
  • If you have recently received or are scheduled to receive any vaccination

Conditions treated by tocilizumab

  • Rheumatoid arthritis
  • Systemic juvenile idiopathic arthritis
  • Castleman's disease
  • Neuromyelitis optica
  • Giant cell arteritis
  • Cytokine release syndrome

Type of medicine

  • monoclonal antibody

Tocilizumab side effects

Tocilizumab can lower the ability of the patient’s immune system to fight other infections. Thus, if you develop symptoms of another infection while using tocilizumab, consider stopping the medication and talking to your doctor immediately.

Allergic reactions to intravenous tocilizumab infusions have been reported. These can come with symptoms such as fever and chills. Also, tocilizumab has been associated with an increase in cholesterol levels in some patients, thus close cholesterol monitoring is strongly recommended during medication. If your cholesterol levels become too high, you may consider taking medication to lower it.

Bowel perforation, a hole in the bowel wall, is a rare complication that occurs as a result of tocilizumab use. Notify your doctor if you have a history of diverticulitis or if you develop abdominal pain or spot blood in your stool while using this medication.

Severe, and sometimes fatal infections may develop during tocilizumab treatment. Inform your doctor immediately if you develop the following signs of infection:

  • Fever, muscle pain, chills, night sweats, white patches on the throat, sores on the mouth, persistent fatigue and sudden weight loss.
  • Rapid and inconsistent heartbeats, chest pain, rapid breathing, coughing up blood, wheezing, shortness of breath.
  • Painful skin sores, severe skin rashes, redness or swelling under your skin, blistering skin rash with tingly or burning sensation.
  • Watery diarrhea, burning or pain while urinating.
  • Bone pain, blurred vision, swollen glands, headache, confusion and nausea.
  • Black, bloody or tarry stool.
  • Severe constipation or diarrhea, stomach cramps and bloating.

Some of the common tocilizumab side effects include:

  • Mild headache
  • Runny or stuffy nose, sore throat, and sinus pain
  • Increased blood pressure (buzzing in the ears, high blood pressure, confusion, anxiety, uneven heartbeats and shortness of breath)
  • Swelling, burning effect, pain around the spot of injection.

Call your healthcare provider for medical advice about these side effects. You may also report tocilizumab side effects to the FDA through this hotline number: 1-800-FDA-1088.

Tocilizumab dosage

  • Adult dose for rheumatoid arthritis

Tocilizumab may be used as monotherapy or concomitantly with methotrexate or other non-biologic medications. The recommended adult dosage for rheumatoid arthritis is 4mg/kg weight once every four weeks as a 60-minute single drip infusion. Based on the patient’s response the dosage can be increased to 8mg/kg weight once every four weeks as a 60-minute single drip infusion. The maximum adult dose is 800 mg per infusion in rheumatoid arthritis patients.

  • Pediatric dose for Juvenile Idiopathic Arthritis

Tocilizumab may be used as monotherapy or in combination with methotrexate in juveniles 2 years and older.

Weight less than 30 kg: 10mg/kg weight should be given once every four weeks as a 60-minute single drip infusion.

Weight 30kg or more: 8 mg/kg weight should be given once every four weeks as a 60-minute single drip infusion.

Important note

The amount of medication that you take depends on a number of factors including the strength of the medicine as well as your health condition. In addition, the frequency of doses, time recommendable in between doses, and the duration you take the medication depend on the medical problem for which you are using the medication.

Tocilizumab dosage will vary from patient to patient. It is important that you follow your healthcare provider’s instruction or directions on the medication’s label. The dosage described above are only the average doses of this medicine. If your dose is different, do not change it unless your healthcare provider advises you to do so.

Missed dose

If you miss your tocilizumab dose, take it as soon as possible. However, if your next dose is just days away, you may skip the missed dose and resume your regular dosing. Do NOT double dose tocilizumab.

Overdose

Tocilizumab overdose is unlikely. However, call your healthcare provider or 911 as soon as you suspect a drug overdose. You may also report tocilizumab over to the drugs and poisons department in your area.

Proper use of tocilizumab

A nurse or a trained healthcare provider will administer this medication in a hospital setting. Tocilizumab is administered using a needle placed in one of the patient’s veins to treat PJIA, SJIA or rheumatoid arthritis. The drug must be infused slowly, so the needle will remain in place for at least 60 minutes.

Tocilizumab injection can also be administered as a shot under the patient’s skin to treat giant cell arteritis or rheumatoid arthritis. It may sometimes be administered at home to patients who do not wish to be in the clinic or hospital. If this medication is used at home, your nurse or healthcare provider should teach you how to prepare and inject the medicine. Be sure to understand exactly how this is done.

Tocilizumab comes with a Medication Guide and patient instructions. Carefully read and follow these instructions and ask your pharmacist or healthcare provider if you have any questions.

Tocilizumab is available in two forms. You may use the vial (glass container) or prefilled syringe. If you are using tocilizumab at home, your doctor will show you areas where the injection can be given. It is recommended that you use different body areas each time you inject. Keep track of where you give each injection to help you rotate body areas. This will help you avoid developing skin problems.

Allow the medication to warm to room temperature for about 30 minutes before injecting yourself with it.

If the medicine in the prefilled syringe has particles, or has changed color, do not use it. Tocilizumab should be clear and colorless or slightly yellow at the time of use.

Each tocilizumab prefilled syringe should only be used once. Appropriately dispose of used syringes in a hard, closed container that the needles cannot prick through. This container should be kept out of children and pet’s reach.

Tocilizumab interactions

In deciding to use tocilizumab, the risk of taking the medication must be weighed against the benefits it will bring to the patient. This is a decision you and your healthcare provider will need to make. For tocilizumab, the following should be considered:

Allergies

Inform your healthcare provider if you have ever had any allergic reactions to this medication, any of its ingredients, or any other medicine. Also, be sure to mention if you have any other types of allergies such as dyes, animals, preservatives, and food.

Children

Studies have not revealed any pediatric-specific complications that would limit the usefulness of tocilizumab therapy in children with SJIA and PJIA. That said, the medication’s safety and efficacy have not been established in toddlers younger than 2 years of age.

Aging adults

All studies performed to date have not indicated geriatric-specific complication that would limit the usefulness of this medication in elderly patients. However, use of tocilizumab in elderly patients is likely to trigger serious infections. As such, caution is required when administering tocilizumab to elderly patients.

Breastfeeding

There are no sufficient studies in women for determining the risk to infants when administering tocilizumab to breastfeeding mothers. However, the potential benefits of the medication against risks ought to be weighted before administration.

Other medications

Talk to your doctor before using tocilizumab together with the following medications:

  • Cholera vaccine
  • Adenovirus vaccine
  • Bacillus of Calmette and Guerin vaccine
  • Measles virus vaccine, live
  • Influenza virus vaccine, live
  • Poliovirus vaccine, live
  • Mumps virus vaccine, live
  • Rotavirus vaccine, live
  • Smallpox vaccine
  • Rubella virus vaccine
  • Typhoid vaccine
  • Yellow fever vaccine
  • Varicella vaccine
  • Using tocilizumab alongside Infliximab is not recommended. However, if both medicines are prescribed together, your healthcare provider may choose to change the dose or the frequency of using one or both medications.
  • Tocilizumab should not be used in combination with biological DMARDs like selective co-stimulation modulators, anti-CD20 monoclonal antibodies, IL-1R, and TNF antagonists due to the likelihood of immunosuppression as well as increased risk of infection.
  • Doctors recommend that tocilizumab should not be administered to patients whose Absolute Neutrophil Count (ANC) is less than 2000/m3, platelet count less than 100,000/m3, or patients whose AST or ALT levels are greater than 1.5 times the upper limit of normal ULN.

Other interactions

Using alcohol and tobacco and certain foods when on tocilizumab medication may cause interactions to occur. Discuss with your healthcare provider the use of tocilizumab with alcohol, tobacco, and food.

Other medical problems associated with tocilizumab

Certain pre-existing medical conditions may affect the use of tocilizumab. Inform your doctor if you have any of the following medical conditions:

  • Hyperlipidemia (high fats in the blood)
  • Chronic inflammatory demyelinating polyneurotherapy (nerve problem)
  • Multiple sclerosis
  • Liver disease
  • Neutropenia
  • Bowel or stomach problems
  • Thrombocytopenia
  • A weak immune system
  • Active or recurring infection
  • Tuberculosis

Other drugs that may affect tocilizumab

Tell your healthcare provider of all medicines you are currently on, or recently used, especially:

  • Any other rheumatoid arthritis medications such as adalimumab, abatacept, anakinra, etanercept, certolizumab, infliximab, golimumab, or rituximab.

Tocilizumab warnings

  • Treatment with tocilizumab may increase your risk of developing certain infections. Talk to your doctor if you develop symptoms discussed above
  • Notify your doctor if you are pregnant or breastfeeding before starting tocilizumab medication
  • Avoid live vaccinations when on this medication. These include the nasal spray vaccine, shingles vaccine, and others such as mumps, measles and yellow fever vaccines
  • Treatment with tocilizumab may predispose you to certain types of cancers. Talk to your healthcare provider about your specific risks
  • Tocilizumab treatment can lower blood cells that help keep your immune system strong. Thus, your blood needs to be monitored on a regular basis. Your infusion may be rescheduled or delayed on the result of your blood test.
  • Some infections are more likely in certain parts of the world. Tell your doctor where you have recently traveled to, or your immediate travel plans, during treatment.
  • If you have ever suffered from Hepatitis B, tocilizumab treatment can cause this condition to come back or worsen. Again, you will need regular blood tests to check your liver function during tocilizumab treatment, and for several months after stopping the medication.
  • If you need surgery, inform your doctor ahead of time that you are on tocilizumab treatment. You may need to withdraw from the medication for some time in order to prepare for the surgery.
  • Tocilizumab has long-term effects on the body. You will need to take certain medical tests every six months after you stop this therapy.
  • You may be treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice

Tocilizumab storage

Like with any medication, keep tocilizumab in the package it came in, tightly closed, and out of reach of children and pets. Keep the medication away from direct sunlight. Tocilizumab may be kept in the refrigerator; however, do not freeze it. Keep all prefilled syringes dry. Appropriately dispose of all outdated and unneeded medication. Talk to your pharmacist about proper drug disposal mechanism.

Summary

Tocilizumab injection is a monoclonal antibody that is used alone or in combination with other medications to manage the signs and symptoms of moderate to severe active rheumatoid arthritis. The medication helps keep the joint damage from worsening as a result of other medications like etanercept, adalimumab and infliximab.

Tocilizumab is also used to treat Systemic Juvenile Idiopathic Arthritis (SJIA) and Polyarticular Juvenile Idiopathic Arthritis (PJIA) in children 2 years and older. This medication should only be administered under strict supervision of a healthcare provider.

Patients treated with tocilizumab tend to be at increased risk of developing other infections, with some progressing to serious and, at times, fatal outcomes. These infections include tuberculosis, bacterium infection, fungal invasion as well as other opportunistic infections. Patients should be evaluated for latent tuberculosis and treated if necessary prior to initiation of tocilizumab therapy. Patients on this therapy should be closely monitored for symptoms of infection even if the initial latent tuberculosis test returned negative results. Also, patients on tocilizumab should be closely monitored for changes in cholesterol levels.

Tocilizumab may be administered alone or together with steroid medicine (glucocorticoids) to treat inflammation of the arteries (commonly known as giant cell arteritis). It may be used alone after ending glucocorticoid treatment.

Before starting tocilizumab treatment, your doctor should carry out tests to ensure that you do not suffer from tuberculosis or any other infection. Tocilizumab is administered through an IV. Your healthcare provider will give you this type of injection. The injection is given every one to four weeks. Call your healthcare provider, or the ER, in an event of severe tocilizumab side effects.

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Last Reviewed:
December 24, 2017
Last Updated:
December 22, 2017
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