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Drugs reference index «Etanercept»

Etanercept


Etanercept

Pronunciation: (ee-TAN-er-sept)Class: Immunomodulator

Trade Names:Enbrel- Injection, solution 25 mg per 0.5 mL- Injection, solution 50 mg per mL- Injection, lyophilized powder for solution 25 mg

Pharmacology

Binds specifically to tumor necrosis factor (TNF), blocking its interaction with cell surface TNF receptors, and modulating biological responses induced or regulated by TNF.

Pharmacokinetics

Absorption

C max is approximately 1.1 mcg/mL. T max is approximately 69 h (single dose). C max increases 2- to 7-fold, while AUC increases approximately 4-fold with repeated dosing.

Elimination

The half-life is approximately 102 h. Cl is approximately 160 mL/h.

Special Populations

Renal Function Impairment

No studies conducted.

Hepatic Function Impairment

No studies conducted.

Children

Cl is slightly reduced in patients 4 to 8 yr of age.

Age/Gender

Pharmacokinetic parameters are not different.

Indications and Usage

Reducing signs and symptoms and inhibiting the progression of structural damage in moderately to severely active rheumatoid arthritis (RA); reducing signs and symptoms of moderately to severely active polyarticular-course juvenile idiopathic arthritis in children 2 years of age and older; reducing signs and symptoms in patients with active ankylosing spondylitis; treatment of adult patients with chronic, moderate to severe plaque psoriasis who are candidates for systemic therapy or phototherapy; reducing signs and symptoms, inhibiting the progression of structural damage of active arthritis, and improving physical function in patients with psoriatic arthritis.

Unlabeled Uses

Crohn disease; CHF; pyoderma gangrenosum.

Contraindications

Sepsis; hypersensitivity to etanercept or to any of its components.

Dosage and Administration

Ankylosing Spondylitis, Psoriatic Arthritis, RAAdults

Subcutaneous 50 mg/wk, given as 1 injection.

For RA, dosages higher than 50 mg/wk are not recommended.

Juvenile Idiopathic ArthritisChildren 2 to 17 yr of age

Subcutaneous 0.8 mg/kg/wk (max, 50 mg/wk).

Plaque PsoriasisAdults

Subcutaneous 50 mg 2 times/wk (administered 3 or 4 days apart) for 3 mo followed by reduction to a maintenance dosage of 50 mg/wk.

Starting dosages of 25 or 50 mg/wk were also shown to be efficacious.

General Advice

  • For subcutaneous administration only. Not for intradermal, IM, IV, or intra-arterial administration.
  • Administer prescribed dose once or twice a week as ordered. For twice-weekly dose, separate doses by 72 to 96 h.
  • Do not administer if particulate matter, cloudiness, or discoloration is noted.
  • For a 50 mg dose as 1 subcutaneous injection, use a 50 mg/mL prefilled syringe. For a 50 mg dose administered as two 25 mg subcutaneous injections, use the multiple-use vial or two 25 mg prefilled syringes. Give the two 25 mg injections either on the same day or as single injections 3 or 4 days apart.
  • Rotate injection sites (thigh, abdomen, upper arm). Give new injections at least 1 inch or more from old site and never into areas where the skin is tender, bruised, red, or hard. In psoriasis patients, try not to inject directly into any raised, thick, red, or scaly patches (psoriasis skin lesions).
  • In adults, methotrexate, glucocorticoids, salicylates, NSAIDs, and analgesics may be continued during treatment with etanercept. In children, glucocorticoids, NSAIDs, or analgesics may be continued during treatment with etanercept.
  • Single-use prefilled syringe
  • Allow syringe to reach room temperature (approximately 15 to 30 min) before administering. Do not remove the needle shield while allowing the prefilled syringe to reach room temperature.
  • Do not shake prefilled syringe.
  • There may be small white particles of protein in the solution; this is not unusual for proteinaceous solutions.
  • The 25 mg prefilled syringe is not recommended for children weighing less than 31 kg (68 lbs).
  • The 50 mg prefilled syringe may be used for children weighing 63 kg (138 lbs) or more.
  • Multiple-use vial
  • Reconstitute powder using only supplied diluent (sterile bacteriostatic water for injection). Follow manufacturer's instructions.
  • Use vial adapter if reconstituted solution will be administered as a single dose. If the vial will be used for multiple doses, use a 25-gauge needle for reconstituting and withdrawing etanercept.
  • To prevent excessive foaming, inject diluent very slowly into medication vial and swirl gently to dissolve. Do not shake or vigorously agitate medication vial. Complete dissolution may take up to 10 min.
  • Reconstituted solution should be clear and colorless and administered within 14 days of reconstitution.
  • Withdraw prescribed dose into syringe for injection. Do not filter reconstituted solution. Do not mix contents with or transfer to another vial of etanercept.
  • Do not add other medications to etanercept or reconstitute with other diluents.

Storage/Stability

Single-use prefilled syringe

Refrigerate single-use prefilled syringe at 36° to 46°F. Do not freeze. Keep prefilled syringes in the original carton to protect from light until time of use. Do not use multiple-use vial or prefilled syringe beyond expiration date.

Multiple-use vial

Refrigerate multiple-use vial dose tray at 36° to 46°F. Do not freeze. Use reconstituted solution immediately or refrigerate at 36° to 46°F for up to 14 days. Discard solution if not used within 14 days.

Drug Interactions

Anakinra

A 7% rate of serious infections was observed in a 24-wk study with patients receiving etanercept and anakinra therapy. Concurrent therapy is not recommended.

Cyclophosphamide

Risk of noncutaneous solid malignancies may be increased. Concurrent use is not recommended.

Immunosuppressive agents

Use of etanercept in patients with Wegener granulomatosis receiving immunosuppressive agents is not recommended.

Sulfasalazine

The incidence of decreased neutrophil counts may be greater than with either drug alone.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Deep vein thrombosis, heart failure, hypertension, hypotension, MI, myocardial ischemia, stroke, thrombophlebitis (5%); chest pain, new-onset CHF, vasodilation (postmarketing).

CNS

Headache (24%); asthenia (11%); dizziness (8%); cerebral ischemia, depression, hydrocephalus, multiple sclerosis, seizure (5%); aseptic meningitis, fatigue, isolated demyelinating conditions (eg, transverse myelitis), paresthesias, personality disorder (postmarketing).

Dermatologic

Rash (14%); alopecia (6%); worsening psoriasis (5%); cutaneous ulcer, cutaneous vasculitis, erythema multiforme, nonmelanoma skin cancer, pruritus, Stevens-Johnson syndrome, subcutaneous nodules, TEN, urticaria (postmarketing).

EENT

Rhinitis (16%); pharyngitis (7%); sinusitis (5%); dry eyes, ocular inflammation, optic neuritis (postmarketing).

GI

Abdominal pain (19%); nausea (15%); vomiting (13%); dyspepsia (11%); mouth ulcer (6%); appendicitis, cholecystitis, GI bleeding, GI hemorrhage, pancreatitis (5%); esophagitis/gastritis; gastroenteritis; altered sense of taste, anorexia, diarrhea, dry mouth, intestinal perforation (postmarketing).

Genitourinary

Kidney calculus, membranous glomerulonephropathy (5%); UTI (postmarketing).

Hematologic-Lymphatic

Lymphadenopathy (5%); lymphoma; adenopathy, anemia, aplastic anemia, coagulopathy, leukopenia, neutropenia, pancytopenia, thrombocytopenia (postmarketing).

Hepatic

Autoimmune hepatitis (postmarketing).

Lab Tests

Transaminase elevations (postmarketing).

Local

Injection-site reactions (37%).

Metabolic-Nutritional

Type 1 diabetes mellitus, weight gain (postmarketing).

Musculoskeletal

Bursitis, polymyositis (5%); joint pain, lupus-like syndrome (postmarketing).

Respiratory

Upper respiratory tract infections (31%); cough (6%); dyspnea, pulmonary embolism, respiratory disorder, sarcoidosis (5%); interstitial lung disease, pulmonary disease, worsening of prior lung disorder (postmarketing).

Miscellaneous

Non-upper respiratory tract infections (51%); positive anti–double-stranded DNA antibodies (15%); antinuclear antibodies (11%); peripheral edema (8%); nonneutralizing antibodies (6%); group A streptococcal septic shock; malignancy; noncutaneous solid tumors; non-Hodgkin lymphoma; soft tissue and postoperative wound infection; varicella infection; abscess with bacteremia, angioedema, death, fever, flu-like symptoms, generalized pain, infections (including bacteria, fungal, protozoal and viral), sepsis, tuberculous arthritis (postmarketing).

Precautions

Warnings

Infections, including serious infections leading to hospitalization or death, have occurred. Infections have included active tuberculosis (TB), including reactivation of latent TB and bacterial sepsis. Patients should be evaluated for TB risk factors and should be tested for latent TB infection prior to starting and during treatment. Start treatment of latent TB prior to etanercept therapy. Monitor patients for signs and symptoms of infection, including patients who tested negative for latent TB infection.

Monitor

Document baseline disease-state activity. Reassess periodically to document response to therapy. Monitor patient for signs and symptoms of blood dyscrasias. Monitor patient for signs and symptoms of infection while on or after treatment with etanercept. Closely monitor new infections and be prepared to discontinue etanercept if patient develops a serious infection during therapy. Closely monitor patients who are carriers of hepatitis B virus (HBV) throughout therapy and for several months following termination of therapy. Monitor heart failure patients carefully.

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 2 yr of age with juvenile idiopathic arthritis. Safety and efficacy in children with plaque psoriasis have not been established.

Elderly

Because there is a higher incidence of infection in elderly patients, use with caution.

Special Risk Patients

Exercise caution when considering the use of etanercept in patients with a history of recurring infections or with underlying conditions that may predispose them to infections such as advanced or poorly controlled diabetes.

Allergic reactions

Allergic reactions, including anaphylaxis, may occur.

Autoimmunity

Formation of autoantibodies and, rarely, development of lupus-like syndrome may occur.

Benzyl alcohol

The diluent preservative contains benzyl alcohol, which has been associated with fatal gasping syndrome in premature infants.

Heart failure

Worsening of CHF, with and without identifiable precipitating factors, has been reported.

Hematologic

Rare and sometimes fatal cases of pancytopenia, including aplastic anemia, have been reported.

Hepatitis B reactivation

Etanercept has been associated with reactivation of HBV in chronic carriers of the virus.

Immunizations

Do not coadminister with live virus vaccines. If possible, bring juvenile idiopathic arthritis patients up to date with all immunizations in agreement with current guidelines prior to initiating therapy. Temporarily discontinue therapy in patients with significant exposure to varicella virus and consider prophylactic treatment with varicella zoster immune globulin.

Immunosuppression

Anti-TNF therapy affects host defenses against infections and malignancies. Safety and efficacy in patients with immunosuppression or chronic infections have not been evaluated.

Injection-site reactions

Mild to moderate injection-site reactions (eg, erythema, itching, swelling) may occur.

Latex allergy

Needle cover of the prefilled syringe contains natural rubber (latex).

Malignancies

Lymphoma has been reported in patients receiving TNF-blocking agents.

Neurologic events

Agents that inhibit TNF have been associated with rare cases of new-onset or exacerbation of CNS demyelinating disorders, some presenting with mental status changes and some associated with permanent disability. Transverse myelitis, optic neuritis, multiple sclerosis, and new onset or exacerbation of seizure disorders have been observed.

Overdosage

Symptoms

Maximum tolerated dosage has not been established.

Patient Information

  • Advise patient, family, or caregiver to read the Medication Guide before starting therapy and with each refill.
  • If patient or caregiver will be administering at home, review How to Use Enbrel, Instructions for Preparing and Giving an Injection insert with the patient or caregiver. Ensure the patient or caregiver understands how to store, prepare, and administer the dose, and how to dispose of used equipment and supplies. The first injection should be performed under the supervision of a qualified health provider.
  • Advise patient to continue other arthritis medications as recommended by health care provider.
  • Advise patient to immediately report any of the following to health care provider: bleeding or unusual bruising, fever or other signs of infection, paleness, sore throat.
  • Advise patient to report intolerable injection-site reactions or unusual symptoms to health care provider.
  • Advise patient with heart failure to notify health care provider immediately if new or worsening symptoms of heart failure (eg, shortness of breath, swelling of ankles or feet) develop.
  • Warn patient not to receive live vaccines while undergoing etanercept therapy.
  • Advise latex-sensitive patient that the needle cover on the prefilled syringe contains dry natural rubber (latex).

Copyright © 2009 Wolters Kluwer Health.

  • Etanercept MedFacts Consumer Leaflet (Wolters Kluwer)
  • Etanercept Detailed Consumer Information (PDR)
  • etanercept Subcutaneous Advanced Consumer (Micromedex) - Includes Dosage Information
  • Enbrel Prescribing Information (FDA)
  • Enbrel Consumer Overview

See Also...

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