Etanercept – Drug Class, Mechanism of action, Uses, Dosage and Side effects,

Etanercept - Drug Class, Mechanism of action, Uses, Dosage and Side effects

What is Etanercept?

Contents

Etanercept decreases a protein that is produced by the immune system. Our immune system fight against infections. The people who are suffering from auto-immune disorders are treated with this medicine. The immune system attacks its own cells as an invader and causes auto-immune disorders. It is used to treat the symptoms of diseases like ankylosing spondylitis, rheumatoid arthritis, and joint damage caused by these conditions. It is also used in the treatment of plaque psoriasis. It is also given to the children of age 2 years or above suffering from polyarticular idiopathic arthritis.

Enbrel (Etanercept): Side Effects, Interactions, Warning, Dosage & Uses

Etanercept molecular formula, class, weight, chemical name and structure

Etanercept molecular formula– C2224H3472N618O701S36 (monomer)

Molecular weight– 150 kilo- daltons

Chemical name– 1-235-Tumor necrosis factor receptor (human) fusion protein with 236-467-immunoglobulin G1 (human γ1-chain Fc fragment) dimer

Molecular formula:

Etanercept molecular formula, class, weight, chemical name and structure

Why is etanercept prescribed?

This medicine is used to treat following conditions:

Rheumatoid Arthritis

Etanercept is used for treating the symptoms of rheumatoid arthritis. It is used to improve the physical function. It inhibits the progress of damage that is caused by this disease. This medicine is used in the adults having moderate to severe rheumatoid arthritis.

Juvenile Arthritis

It is used to manage the symptoms of severe to moderate polyarticular juvenile idiopathic arthritis. It is a very common arthritis in children.

Psoriatic Arthritis

This medicine improves the physical function and inhibits the progress of damage caused by this disease. It is used for the treatment of Psoriatic arthritis.

Ankylosing Spondylitis

It is used in the treatment of Ankylosing spondylitis.

Psoriasis

It helps to manage severe to moderate signs of chronic plaque psoriasis.

How does Etanercept works in the body?

There are two receptors for TNF. One is p55 of 55 -kilo dalton protein and other is p75 of 75 kilos Dalton. The TNF biological activity is hugely affected by binding with either of the receptors. Now, this drug Etanercept is a soluble dimeric form of p75. This drug binds to both the TNF molecules and removes them from circulation.

TNF is a cytokine that is responsible for immune and inflammatory responses. Increased level of TNFs are found in the condition of rheumatoid arthritis, plaque psoriasis, ankylosing spondylitis and psoriatic arthritis. It is found in the tissue and the fluid in these mentioned diseases.

etanercept mechanism of action PPT

Etanercept brand names– Enbrel injection

What is Etanercept used for?

FDA labeled indications for etanercept are:

  • Ankylosing Spondylitis (AS)
  • Graft Versus Host Disease (GVHD)
  • Hidradenitis Suppurativa (HS)
  • Plaque Psoriasis
  • Polyarticular Juvenile Idiopathic Arthritis
  • Psoriatic Arthritis
  • Pyoderma Gangrenosum
  • Rheumatoid Arthritis
  • Severe, active Rheumatoid arthritis

Etanercept dosage for different indications

For the reconstitution of 25-mg Multiple vialed dose

  • You must keep dose tray having Etanercept powder & diluent at room temperature. It must be kept for 15-30 minutes before administration.
  • You can reconstitute powder by mixing 1 ml of water for injection. This bacteriostatic water is provided by the company. It must be added to the 25-mg vial.
  • Add the diluent slowly to the vial. Then, swirl contents to reduce the formation of foam.
  • You must use vial adapter that comes along with the pack for the reconstitution and withdrawal of a dose from the vial.
  • You must use gauge needle to inject the dose. Avoid excess shaking to prevent the formation of foam.
  • The final volume is 1 ml in the vial. The process of dissolution gets completed in 10 minutes.
  • You must avoid the filtration of the solution.
  • Don’t ever mix the contents of two vials.

Considerations on preparations

  • 50-mg of dose as a single injection- Preferred preparations are prefilled injector or 50-mg prefilled syringe.
  • 50-mg of dose as two injections- preparation of prefilled syringe or 25-mg vial.
  • Special advice for children- You are not advised to use 25-mg prefilled syringe who has weight < 31 kg and 50 mg in weight< 63 kg.

Juvenile Arthritis Children of age 2-17 years- the maximum dose is 50 mg or 0.8 mg/kg every week.

Rheumatoid Arthritis Adults – the dose is 50 mg every week.

Psoriatic Arthritis Adults- the dose is 50 mg every week.

Ankylosing Spondylitis Adults – the dose is 50 mg every week.

Psoriasis Initially 25- 50 mg twice every week for 3 months.

Maintenance dosage: 50 mg once every week

Renal Impairment- Special Populations- there is limited data that indicate dosage adjustment is not required in the patients suffering from renal impairment.

Etanercept side effects

  • The various side effects of Etanercept are as follows-
  • Vomiting, Dizziness and Mild nausea
  • Stomach pain and Diarrhea
  • Headache and heartburn
  • Pain in joint and  swelling with fever
  • Redness at the injection site
  • Changes in weight and weakness
  • Cold symptoms
  • Numbness and tingling, burning pain and Seizures
  • Bleeding and bruising
  • Swelling and changes in skin like blisters
  • Difficulty in breathing and swallowing
  • Vision changes
  • Infection like sore throat, body aches, neck stiffness, flu, itching and redness
  • Chest pain and cough
  • Black or tarry stools
  • Changes in mood or personality

How to take Etanercept?

  • Before the treatment your doctor will perform tests to check whether you have an infection or not.
  • Etanercept is given along with other medicines like salicylates, analgesics, methotrexate and glucocorticoids. It is given in the people who are suffering from ankylosing spondylitis, rheumatoid arthritis and psoriatic arthritis.
  • In the children who are suffering from juvenile Idiopathic arthritis this medicine can be given with the analgesic, NSAIDs and glucocorticoids.
  • It is administered in the form of injection. In the children and adults who are receiving 50 mg dose must be given a single injection. Two injections can also be given on the same day as per the directions of the doctor.
  • It must be given in the thighs, upper arm or abdomen. The sites of injection must be changes. Don’t inject in the red, bruised or hard areas. Also avoid the areas where there are scars, stretch marks or lesions.
  • You can have warmth, pain, swelling and redness at the place of the injection. If the symptoms continued for five days contact your doctor immediately.
  • You must use disposable syringe or needle only once. Don’t shake it.
  • Prepare the dose just before the injection. You are advised not to use medicine if it looks cloudy.
  • You must allow the prefilled syringe to keep for room temperature for 15-30 minutes. Don’t remove the cover of the needle.
  • Store Etanercept in the refrigerator. Don’t use the medicine after the date of expiration. If you have missed this medicine with diluent and store in refrigerator in 14 days.
  • Keep it away from light, heat and cold temperature.
  • It must be taken under the supervision of health care provider. If you are required to take by self, then take the help of a skilled person.

Overdose of Etanercept

If the overdose has occurred then seek the doctor immediately.

Missed Dose of Etanercept

Seek the advice of the doctor if you have missed the dose.

Precautions and warnings during Etanercept use

Take the following precaution into consideration before taking this medicine.

Don’t use Etanercept if you are allergic and have an infection like sepsis. You must tell your doctor before taking this medicine.

  • Weak immunity
  • Have Hepatitis B, HIV or AIDS and tuberculosis or any kind of serious infection.
  • In the case of symptoms like fever, diarrhea, flu and painful urination
  • Skin sore and open cut
  • Congestive heart failure and diabetes
  • History of multiple sclerosis, myelitis, optic neuritis, and Guillain-Barré syndrome
  • Seizure and epilepsy
  • Breathing disorder or Asthma
  • If scheduled to receive vaccines, or recently vaccinated with BCG.
  • In the case, you are a pregnant or nursing mother. It passes into breast milk and can cause harm to baby

For how long Etanercept stay in the body?

The 25 mg of this drug was administered to 25 patients by single injection suffering from RA. It was observed that the half -life is 102 ± 30 hours and clearance of 160 ± 80 mL/hr. Maximum serum concentration was reported as 1.1 ± 0.6 mcg/mL. After six months these patients showed mean C max as 2.4 ± 1.0 mcg/mL.

Etanercept during pregnancy

There is not any controlled study for pregnant women. It is shown that this drug crosses the placenta in small amounts. The toxicity studies were performed in rabbits and rats at the doses of 60-100 higher than human dose. It has shown that they cross the placenta and is harmful to the fetus. As the animal reproduction studies are not always true for humans. This drug can be used in pregnancy if needed. Three cases were reported that showed the presence of this drug in the cord blood levels at the time of delivery.

Etanercept during breastfeeding

There is a limited data that this drug is present in low amount in human milk. The caution must be taken while administering this drug to the nursing mother. The adverse side effects on the breastfed child must be observed.

Etanercept in children

The physician must consider the benefits and risk before giving this drug to the children. Also, you must keep a check on other vaccines that are given to the children.

Etanercept in elderly patients

As there are higher incidences of infections in the elderly patients, so this drug must be given with caution.

Etanercept in diabetes

The incidence of hypoglycemia is reported with the therapy of Etanercept. So, it must be given with caution in the patient suffering from diabetes.

Can Etanercept cause serious infections?

Patients that are given Etanercept are at the risk of developing serious infections. The infection can occur on the sites and organ systems and can lead to death. The patients are reported to suffer from disseminated disease. They can have the infection caused by bacteria, fungi, parasite, viral or other pathogens. Treatment with this drug should be avoided in the patient suffering from an active infection.

The patients having an age greater than 65 years of age having the co-morbid condition, and taking immunosuppressant are at greater risk of developing an infection. The immunosuppressant are corticosteroids and methotrexate. You must take into consideration if you are suffering from recurrent infection and tuberculosis. Patients must be closely monitored for the symptoms of infection if treated with this drug. This drug must be discontinued if you have developed a sepsis. If you have developed an infection during the treatment, then close monitoring is essential.

Can Etanercept cause tuberculosis?

It has been observed that there are the cases of reactivation of tuberculosis in the patients that are receiving Etanercept. The risk of reactivation of tuberculosis is high with TNF blocking agents. In the clinical studies, the cases are reported that there is the development of tuberculosis. In these patients, they were tested negative prior to the treatment with this drug. Patients must be observed for the risk of tuberculosis before and during the therapy. Anti-tuberculosis treatment must be taken into consideration before starting the therapy of this drug. You must consult with the doctor.

Can Etanercept causes fungal infections?

There has been the history of serious fatal fungal infections. Infection like histoplasmosis, has been recorded with TNF blockers. The people who are travelling can develop mycoses, a kind of fungal infection. Anti-fungal therapy must be taken into consideration in the case of diagnosis. You must consult your physician. The correct diagnosis and treatment of anti-fungal infection is very important.

Can Etanercept causes Neurologic conditions?

Treatment of TNF blocking agents like Etanercept can cause onset or reactivation of CNS disorders. It can result in changes in mental status, permanent disability, demyelinating disorders, and peripheral nervous problems. The most marketing studies of the therapy of this drug have been reported to cause optic neuritis, transverse myelitis, and other demyelinating peripheral neuropathy.

Can Etanercept cause lymphomas?

Many clinical trials of TNF blocking agents, many cases of lymphoma has been reported. In a clinical trial, the lymphomas was observed in 3306 adults’ patients receiving the therapy of Etanercept. Therefore, you must consult your doctor in the case of risk of developing lymphomas during receiving the therapy of this drug.

Can Etanercept cause leukemia?

The cases of chronic and acute leukemia have been reported. If you are taking the therapy of Etanercept in the treatment of rheumatoid arthritis, then there can be the onset of leukemia. The patients suffering from rheumatoid arthritis are at higher risk of developing leukemia. During the controlled trials in 5445 patients, two cases of leukemia were reported.

Can Etanercept causes Melanoma and non-melanoma Skin Cancer?

This skin cancer has been reported in the patients that are treated with this drug. In the clinical trial where 15,401 patients were enrolled in a controlled and open clinical trial, 0.043 cases per 100 patients were reported. In different clinical studies where rheumatoid arthritis patients were treated with this drug has 0.41, 0.37 cases per 100 patients. Post marketing studies have also shown the development of skin cancer during the therapy of this drug. Periodic skin examinations are required. Consult your doctor immediately.

Can Etanercept causes disorders in pediatric patients?

There are reported fatal malignancies among children and young adults who are undergoing the therapy of this drug. The cases of lymphomas like Hodgkin’s and non-hodgkin’s lymphoma. There were other cases of different kinds of malignancies.

Can Etanercept be used in the patients suffering from heart problems?

The worsening of the congestive heart failure is reported in the patients receiving the treatment of this drug. This disease can develop without any history of cardiovascular disease. Doctors must advise the use of this drug with great caution. The patients must be observed carefully.

Can Etanercept causes hematological reactions

There are 0.1 % reports of aplastic anemia and pancytopenia in the patients treated with this drug. However the relation between the two is not clear. Caution must be taken while treating these patients with this drug who have a prior history of hematological reactions. If you develop any symptoms, contact your doctor immediately. You can develop the signs of fever, pallor, bleeding and bruising. If the patient is having serious condition, then discontinuation of the therapy is the only alternative.

Can Etanercept causes hepatitis B reactivation?

Very rare cases of hepatitis B reactivation has been reported in the patients who were given the therapy of this drug. These incidents were reported in the patients who are taking the drugs to suppress the immune system. The patients who have to receive the therapy must be observed for the symptoms of hepatitis B reactivation. The doctor must be very cautious in order to prescribe this drug. Regular check up with clinical and laboratory signs must be kept under observation. If the person has developed the Hepatitis B reactivation, then stop the therapy with this drug.

Can Etanercept cause allergic reactions?

2 % of the cases have been reported in the patients who are suffering from allergic reactions with the therapy of this drug. The therapy must be discontinued immediately if the serious allergic reaction occurs.

Can Etanercept can be given with other vaccines?

Other vaccines must not be given with this drug. You must tell your doctor all the immunizations that your kid is taking prior or at the time of Etanercept.

Can Etanercept causes autoimmune diseases?

The treatment of Etanercept can result in the formation of autoantibodies. If the patient develops symptoms of lupus then, this therapy must be discontinued. The symptoms of autoimmune diseases must be taken into consideration.

Can Etanercept causes immunosuppression?

TNF is responsible for mediating immune responses. TNF blocking agents like Etanercept affects defenses against infections. In a clinical study on 49 patients, there is no evidence of immunosuppression on the patients who are undergoing the therapy with this drug.

Can Etanercept can be used in Wegener’s Granulomatosis Patients?

The use of this drug is not recommended in the patients who are suffering from Wegener’s Granulomatosis. It was reported with the higher incidence of malignancies.

Can Etanercept are used in patients With Moderate to Severe Alcoholic Hepatitis?

Doctors must use this drug with caution in the people who are suffering from moderate to severe alcoholic hepatitis.

Can Etanercept be given with live Vaccines?

Patients who are receiving the treatment of this drug must avoid taking live vaccines. The data is not available on the secondary transmission of infection in the case of live vaccines in the patients undergoing the treatment with Etanercept. The patient exposing to varicella virus can be discontinued with the therapy of this drug for a short period of time.

Can Etanercept be given with Immune-Modulating Biologic Products?

A study has revealed 7 % rate of infection in the patients on the treatment of Etanercept and anakinra therapy for 24 weeks. The most common infection was cellulitis and pneumonia. Also, this combination was proved to be fatal in patients that were suffering from pulmonary fibrosis due to respiratory failure. Also, 2% of patients have developed neutropenia. The simultaneous administration of abatacept and Etanercept has resulted in serious effects.

Can Etanercept be given with Cyclophosphamide?

The simultaneous administration of both these drugs must be avoided. It can lead to serious side effects.

Can Etanercept be given with Sulfasalazine?

The patients who were treated with Etanercept and sulfasalazine in a clinical trial were found to have fewer neutrophils as compared with when treated with each drug alone.

Can Etanercept be given with Clonazepam?

Etanercept decreases the effect of clonazepam. The dose adjustment is required in the case of administration of both the drugs. Consult your doctor in the case of any side effects.

Can Etanercept be given with Adalimumab?

The administration of both these drugs can result in the development of life threatening infections. Consult your doctor for the appropriate dosing of both these drugs. You must inform your doctor in the case of symptoms like chills, fever, diarrhea, shortness of breath, weight loss, body sores or pain the urination.

Can Etanercept be given with Methotrexate?

It can increase the risk of fatal infections when both drugs are administered together. You must consult your doctor so that he can titrate the doses.

Can Etanercept be given with Hydroxychloroquine?

The simultaneous administration of both these drugs may increase the risk of nerve damage. Your doctor may be able to look out for any side effects. He is competitive enough to adjust the doses. If you encounter any side effects like weakness, pain, numbness, tingling in hands then consult him immediately.

Can Etanercept be given with Prednisone?

It increases the risk of life threatening infections. Contact your doctor for the right treatment.

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About Miljan Krcobic 257 Articles

My name is Miljan Krčobić. I was born on 14th of November 1989. in Negotin, Serbia, where I finished elementary and high school. In June 2015 I graduated from the Faculty of Pharmacy in Belgrade and thus acquired the title Master of Pharmacy. From the July of 2015 to January 2016 I worked in a pharmaceutical company Hemofarm a.d.(Member of STADA group) based in Vrsac, Serbia, as an expert associate for GMP compliance within the sector Quality Assurance. I am currently working in a pharmacy called Zivkovic in Negotin. As a freelancer I write medical articles on Elance and Upwork.