Infliximab

Trade Names:
Remicade
- Injection, lyophilized powder for solution 100 mg (contains sucrose 500 mg)

Pharmacology

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Neutralizes the biological activity of tumor necrosis factor alpha (TNFα) by binding to its soluble and transmembrane forms, and inhibits TNFα receptor binding.

Pharmacokinetics

Absorption

Single IV infusions show a linear relationship between the dose administered and the C _max .

Distribution

Distributed primarily within the vascular compartment.

Elimination

The half-life is 8 to 9.5 days.

Indications and Usage

Reduce signs and symptoms and induce and maintain clinical remission of moderate to severe Crohn disease in patients who have had inadequate response to conventional therapy; reduce number of draining enterocutaneous and rectovaginal fistulas and maintain fistula closure in fistulizing Crohn disease; in combination with methotrexate to reduce signs and symptoms, inhibit progression of structural damage, and improve physical function in patients with moderately to severely active rheumatoid arthritis; reduce signs and symptoms of active ankylosing spondylitis; reduce signs and symptoms of and inhibit progression of structural damage and improve physical function of patients with active psoriatic arthritis; treatment of chronic severe plaque psoriasis in patients who are candidates for systemic therapy; reduce signs and symptoms, achieve clinical remission and mucosal healing, and eliminate corticosteroid use in patients with moderately to severely active ulcerative colitis.

Unlabeled Uses

Management of Behçet syndrome uveitis; treatment of erythrodermic psoriasis; treatment of pustular psoriasis; treatment of pyoderma gangrenosum.

Contraindications

Hypersensitivity to murine proteins or other components of product; administration of more than 5 mg/kg to patients with moderate or severe CHF.

Dosage and Administration

IV 5 mg/kg infusion followed by additional 5 mg/kg at 2 and 6 wk after the first infusion, then every 6 wk thereafter.

IV 5 mg/kg as an induction regimen at 0, 2, and 6 wk, followed by a maintenance regimen of 5 mg/kg every 8 wk. In adult patients who respond and then lose response, consider treatment with 10 mg/kg.

IV 5 mg/kg as an induction regimen at 0, 2, and 6 wk, followed by a maintenance regimen of 5 mg/kg every 8 wk. In adult patients who respond and then lose response, consider treatment with 10 mg/kg.

IV 5 mg/kg infusion followed by additional 5 mg/kg at 2 and 6 wk after the first infusion, then every 8 wk.

IV 3 mg/kg infusion followed by additional 3 mg/kg doses at 2 and 6 wk after the first infusion, then every 8 wk thereafter in combination with methotrexate. For patients with incomplete response, may give up to 10 mg/kg or treat as often as every 4 wk.

IV 5 mg/kg as an induction regimen at 0, 2, and 6 wk followed by a maintenance regimen of 5 mg/kg every 8 wk thereafter.

General Advice

• For administration by IV infusion only. Not for intradermal, subcutaneous, IM, IV bolus, or intra-arterial administration.
• Begin infusion of diluted solution within 3 h of preparation.
• Administer by IV infusion over a period of not less than 2 h through an infusion set with an in-line, sterile, nonpyrogenic, low-protein-binding filter with pore size of 1.2 mcm or less.
• Do not infuse infliximab concomitantly in the same IV line with any other agent.
• Discard any unused infusion solution. Do not save unused solution for later administration.

Storage/Stability

Store vials of powder for injection in refrigerator (36° to 46°F). Do not freeze.

Drug Interactions

Risk of serious infection and neutropenia may be increased.

Do not coadminister live vaccines.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (7%); chest pain, hypotension (1%); arrhythmia, bradycardia, cardiac arrest, circulatory failure, MI, new and worsening heart failure, pulmonary embolism, syncope, tachycardia, thrombophlebitis; pericardial effusion, systemic and cutaneous vasculitis (postmarketing).

CNS

Headache (18%); fatigue (9%); confusion, dizziness, meningitis, neuritis, peripheral neuropathy, suicide attempt (at least 0.2%); convulsions (less than 1%); neuropathies; peripheral demyelinating disorders, including Guillain-Barré syndrome, chronic inflammatory demyelinating polyneuropathy, and multifocal motor neuropathy (postmarketing).

Dermatologic

Rash (10%); flushing (9%); pruritus (7%); sweating, ulceration, urticaria; erythema multiforme, psoriasis, Stevens-Johnson syndrome, toxic epidermal necrosis (postmarketing).

GI

Nausea (21%); abdominal pain, diarrhea (12%); dyspepsia, blood in stool (10%); constipation, GI hemorrhage, ileus, intestinal obstruction, pancreatitis, perforation and stenosis, peritonitis, proctalgia.

Genitourinary

UTI (8%); menstrual irregularity, renal calculus, renal failure.

Hematologic

Anemia (11%); leukopenia (9%); neutropenia (7%); hemolytic anemia, lymphadenopathy, lymphoma, pancytopenia, thrombocytopenia; idiopathic thrombocytopenic purpura, thrombotic thrombocytopenic purpura (postmarketing).

Hepatic

Elevated ALT and AST (51%); acute liver failure, biliary pain, cholecystitis, cholelithiasis, cholestasis, hepatitis, jaundice (postmarketing).

Hypersensitivity

Antibodies to infliximab (36%); respiratory tract allergic reaction (6%); delayed hypersensitivity reported as serum sickness or a combination of arthralgia and/or myalgia with fever and or rash (1%); allergic reactions including laryngeal/pharyngeal edema and severe bronchospasm (postmarketing).

Local

Infusion reactions (20%).

Metabolic

Dehydration, edema.

Musculoskeletal

Arthralgia, back pain (8%); bone fracture (7%); myalgia, transverse myelitis (postmarketing).

Respiratory

Upper respiratory tract infection (32%); sinusitis (14%); coughing, pharyngitis (12%); bronchitis (10%); rhinitis (8%); dyspnea (1%); lower respiratory tract infection (including pneumonia), pleural effusion; adult respiratory distress syndrome, bronchitis, pleurisy, pulmonary edema, respiratory insufficiency; interstitial pneumonitis/fibrosis (postmarketing).

Miscellaneous

Infections (56%); pain, viral infections (8%); fever (7%); bacterial infection (6%); moniliasis (5%); chills (3%); abscess, cellulitis, diaphragmatic hernia, intervertebral disk herniation, lupus-like syndrome, malignancies including non-Hodgkin lymphoma and Hodgkin disease, neoplasms (eg, blood cell, basal cell breast), sepsis, serum sickness, surgical/procedural sequela, tendon disorder (postmarketing).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 6 yr of age.

Safety and efficacy not established.

Elderly

Use with caution because of higher incidence of infection in elderly patients.

Hypersensitivity

Reactions vary in their time of onset. Urticaria, dyspnea, and hypotension have occurred during or within 2 h of infliximab infusion; however, serum sickness–like reactions have been observed in Crohn disease patients 3 to 12 days after infliximab treatment.

Autoimmunity

May result in autoantibody formation and, rarely, development of a lupus-like syndrome.

Heart failure

Treatment has been associated with adverse outcomes in patients with heart failure, and should be used in patients with heart failure only after other treatment options have been considered. Worsening heart failure and new-onset heart failure have been reported during postmarketing experience.

Hematologic

Leukopenia, neutropenia, pancytopenia, and thrombocytopenia, sometimes fatal, have been reported.

Hepatitis B virus reactivation

Has occurred in patients who are chronic carriers of this virus.

Hepatotoxicity

Autoimmune hepatitis and severe hepatic reactions, including acute liver failure, jaundice, hepatitis, and cholestasis, have been reported.

Immunogenicity

Treatment can be associated with development of antibodies to infliximab. The incidence in patients given a 3-dose induction regimen followed by maintenance dosing is about 10%.

Malignancy

Patients with long duration of Crohn disease or rheumatoid arthritis and chronic exposure to immunosuppressant therapies are more prone to develop lymphomas.

Neurologic events

Rarely, optic neuritis, seizure, and new-onset or exacerbation of clinical symptoms and/or radiographic evidence of CNS demyelinating disorders, including multiple sclerosis, may occur.

Vaccinations

Bring children with Crohn disease up to date with all vaccinations prior to starting infliximab therapy. It is recommended that live vaccines not be given concurrently.

Overdosage

Symptoms

Single doses of up to 20 mg/kg have been administered without toxic effects.

Patient Information

• Advise patient or caregiver that medication will be prepared and administered by health care provider in a medical setting.
• Advise patient or caregiver to review the Medication Guide before each treatment infusion session.
• Review treatment infusion schedule with patient or caregiver (eg, 2 and 6 wk after initial infusion, then every 6 wk thereafter when treating ankylosing spondylitis, or every 8 wk thereafter when treating rheumatoid arthritis or Crohn disease).
• Advise patient to notify health care provider immediately of any of the following: bleeding or unusual bruising; change in vision; dark, brown-colored urine; difficulty breathing or unexplained shortness of breath; difficulty swallowing; fever or other signs of infection; flu-like symptoms; new or worsening headache; new or worsening joint or muscle pain; numbness or tingling in any part of the body; paleness; rash, hives, or itching; right upper stomach pain; sore throat; swelling of hands or face; unexplained cough; unexplained tiredness; weakness in arms or legs; or yellowing of the skin or eyes.
• 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 infliximab therapy.

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