Etanercept; Uses, Dosage, Side Effects, Drug Interactions

Etanercept belongs to the class of medications called biological response modifiers (“biologics”) or tumor necrosis factor inhibitors (TNF blockers). It works by decreasing TNF, a protein produced by the immune system to helps the body fight infections. It is a biopharmaceutical that treats autoimmune diseases by interfering with tumor necrosis factor (TNF, a soluble inflammatory cytokine) by acting as a TNF inhibitor. TNF-alpha is the “master regulator” of the inflammatory (immune) response in many organ systems. Autoimmune diseases are caused by an overactive immune response. Etanercept has the potential to treat these diseases by inhibiting TNF-alpha.

It has U.S. F.D.A. approval to treat rheumatoid arthritis, juvenile rheumatoid arthritis and psoriatic arthritis, plaque psoriasis and ankylosing spondylitis. 

Mechanism of Action of Etanercept

Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF. Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinase-3, also known as stromelysin. There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (p75 or p55). Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation.TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Increased levels of TNF are found in tissues and fluids of those with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis (AS), and plaque psoriasis.

Indications of Etanercept

• Rheumatoid arthritis
• Severe, active rheumatoid arthritis
• Ankylosing spondylitis 
• Psoriatic arthritis
• Graft versus host disease
• Juvenile idiopathic arthritis
• Juvenile rheumatoid arthritis
• Macrophage activation syndrome
• Plaque Psoriasis
• Psoriasis
• Spondyloarthritis
• Uveitis
• Polyarticular juvenile idiopathic arthritis
• Pyoderma gangrenosum

Contra-Indications of Etanercept

• Tuberculosis
• Infection caused by Blastomyces dermatitidis Fungus
• Opportunistic fungal infection
• Pneumonia 
• Severe infection
• Infection that Lasts a Long Time
• Malignant melanoma
• Leukemia
• Diabetes that is not under control
• Reduction in the body’s resistance to infection
• Acquired Decrease of all cells in the blood
• Low blood counts due to bone marrow failure
• Decreased neutrophils a type of white blood cell
• Multiple sclerosis
• Demyelinating Disease
• Sudden blindness and pain Upon moving the eye
• Heart failure
• Pneumonia caused by Legionella pneumophila bacteria
• Hardening of the liver caused by alcohol
• Liver inflammation caused by the body’s own immune response
• Seizures
• Reactivated tuberculosis
• Sepsis syndrome
• Malignant lymphoma
• Relapse of hepatitis B infection symptoms
• Hepatitis B
• Hepatosplenic T-cell lymphoma
• Opportunistic viral infection

Dosage of Etanercept

Strengths: 25 mg; 50 mg/mL; 25 mg/0.5 mL

Rheumatoid Arthritis

• 50 mg subcutaneously once a week
• Doses higher than 50 mg per week are not recommended.

Psoriatic Arthritis

• 50 mg subcutaneously once a week
• Doses higher than 50 mg per week are not recommended.

Ankylosing Spondylitis

• 50 mg subcutaneously once a week
• Doses higher than 50 mg per week are not recommended.

Pediatric Juvenile Idiopathic Arthritis

2 years and older

• Less than 63 kg: 0.8 mg/kg subcutaneously once a week
• Greater than or equal to 63 kg: 50 mg subcutaneously once a week
• Maximum dose: 50 mg subcutaneously once a week.

Side Effects of Etanercept

The most common

• Nausea and vomiting
• Severe stomach ache
• multiple sclerosis,
• Severe diarrhea
• Vaginal thrush
• Skin rash redness or itching, pain, or swelling at the injection site
• A headache
• chest pain
• constipation
• a cough
• diarrhea or loose stools
• difficulty with breathing
• dizziness
• heartburn
• muscle pain

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• difficulty with moving
• a headache, severe and throbbing
• joint or back pain
• Loss of energy or weakness
• pain or burning in the throat
• runny or stuffy nose
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in the chest
• discomfort in arms, shoulders, neck or upper back
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• rust colored urine
• decreased amount of urine

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• tremors
• weight loss
• chest pain or tightness
• confusion
• a cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• a headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities

Drug Interactions of Etanercept

Etanercept may interact with the following drugs, supplements, & may change the efficacy of the drug

• abatacept
• anakinra
• bacillus Calmette-Guérin (BCG)
• belimumab
• canakinumab
• certolizumab pegol
• cyclophosphamide
• denosumab
• fingolimod
• infliximab
• leflunomide
• nivolumab
• natalizumab
• pimecrolimus
• roflumilast
• sulfasalazine
• tacrolimus
• tocilizumab
• tofacitinib
• trastuzumab
• vaccines (e.g., yellow fever, BCG, cholera, typhoid, varicella, meningococcal, diphtheria)
• vedolizumab

Pregnancy Catagory of Etanercept

FDA Pregnancy Category B

Pregnancy

There have been no studies on the use of etanercept by pregnant women. Etanercept crosses the placenta and may affect the developing baby if it is used by the mother during pregnancy. For this reason, this medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

This medication passes into breast milk. If you are a breastfeeding mother and are taking etanercept, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children younger than 4 years old. It can be used to treat children aged 4 to 17 years who have moderate-to-severe juvenile idiopathic arthritis or chronic severe psoriatic arthritis.

References

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