Infliximab Data - Uses, Dosage, Drug class, Brand name, Warnings, etc

Pharmacology	Infliximab is a chimeric monoclonal antibody that binds to soluble and transmembrane forms of TNF-α, neutralizing its activity and inhibiting TNF-α binding to its receptor sites. It has no effect on lymphotoxin (TNF-β). Infliximab induces pro-inflammatory cytokines including interleukins 1 and 6 and increases endothelial cell permeability by enhancing leukocyte migration.
Administration and Adult Dosage	- IV infusion for rheumatoid arthritis: 3 mg/kg, with repeat infusions at weeks 2 and 6, then every 8 weeks thereafter. Must be used with methotrexate - IV for moderately to severely active Crohn’s disease: 5 mg/kg as a single IV infusion; some patients may benefit from treatment every 8 weeks after the single infusion - IV for fistulizing Crohn’s disease: 5 mg/kg at weeks 0, 2, and 6
Special Populations - Pediatric Dosage	Safety and efficacy not established.
Special Populations - Geriatric Dosage	Same as adult dosage.
Dosage Forms	- Injection: 100 mg
Patient Instructions	- Infliximab is administered intravenously by a healthcare professional - Notify your physician if chest pain, fever, chills, facial flushing, itching, hives, or difficult breathing occurs within a few hours of administration
Pharmacokinetics - Fate	- Distributed primarily within the vascular compartment - Direct and linear relationship between dose, maximum serum concentration, and AUC - Age and weight do not affect clearance or volume of distribution - No systemic accumulation occurs
Pharmacokinetics - t¹⁄₂	- Elimination half-life: 8–9.5 days
Adverse Reactions & Side Effects	Frequent (≥5% of patients): - Headache, nausea, abdominal pain, fatigue, fever, pharyngitis, vomiting, pain, dizziness, bronchitis, rash, rhinitis, chest pain, coughing, pruritus, sinusitis, myalgia, back pain Infusion-related reactions: - Fever, chills, pruritus, urticaria, chest pain, hypotension, hypertension, dyspnea during or within 2 hr post-infusion Other: - Serious infections - Hypersensitivity reactions; antibodies to infliximab develop in ~13% of patients, increasing risk of infusion-related reactions Rare: - Lupus-like syndrome (1 in 340 patients) - Lymphoproliferative disorders
Contraindications	- Hypersensitivity to murine proteins - Presence of serious infection
Precautions & Warnings	- Women should use adequate contraception during and for at least 6 months after therapy - Use caution with immunosuppressive therapy or in patients with a history of infections - Avoid use in patients with known GI luminal strictures
Parameters to Monitor	- Monitor closely for infusion-related reactions during or within 2 hr post-infusion and for infection during therapy - For Crohn’s disease: Observe for improvement in abdominal cramping, bowel consistency, and rectal bleeding
Drug Interactions	- None known
Class and Drug Brand Name	- Class: Antirheumatic Drugs - Brand Name: Remicade
Notes	- Dilute the total volume of the reconstituted infliximab solution dose to 250 mL with 0.9% NaCl; gently mix - Administer over at least 2 hr through a nonpyrogenic, low protein-binding filter with a pore size of ≤1.2 µm - Effective in the treatment of severe esophageal Crohn’s disease and refractory perineal cutaneous Crohn’s disease - Have medications (e.g., acetaminophen, antihistamine, corticosteroid, epinephrine) available for immediate use in case of hypersensitivity reactions

References

Hand of Clinical Drug Data