REMICADE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REMICADE (REMICADE).
Infliximab is a chimeric monoclonal IgG1 antibody that binds with high affinity to tumor necrosis factor alpha (TNFα), neutralizing its pro-inflammatory cytokine activity by preventing its interaction with p55 and p75 cell surface TNF receptors.
| Metabolism | Infliximab is a monoclonal antibody eliminated by target-mediated clearance and nonspecific proteolytic catabolism; no specific metabolic pathway or cytochrome P450 enzymes involved. |
| Excretion | Infliximab is eliminated primarily via the reticuloendothelial system. No significant renal or biliary excretion; less than 0.1% of dose excreted unchanged in urine. Clearance is mainly through proteolytic catabolism. |
| Half-life | Terminal elimination half-life is approximately 7.7 to 9.5 days (range 7-12 days). The prolonged half-life supports every-8-week dosing; may be shorter in patients with high tumor burden or immunogenicity. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution at steady state (Vd_ss) is approximately 3.0 to 4.0 L, indicating limited extravascular distribution (mainly in the vascular compartment). Not reported per kg; absolute Vd ~3-4 L. |
| Bioavailability | Bioavailability is 100% when administered intravenously (the only approved route). Not applicable for subcutaneous or oral routes. |
| Onset of Action | Intravenous administration: Clinical effect may be observed within 2 weeks after the first infusion for rheumatoid arthritis and Crohn's disease; maximal response typically by 6 weeks. |
| Duration of Action | Duration of action is approximately 8 weeks (consistent with dosing interval). Some patients may sustain response for up to 12 weeks; loss of response may occur due to antibody formation or subtherapeutic concentrations. |
| Action Class | Disease Modifying Anti-Rheumatoid Drugs (DMARDs)- Biologics |
| Brand Substitutes | Infimab Injection |
5 mg/kg IV at weeks 0, 2, and 6, then every 8 weeks thereafter; for rheumatoid arthritis, may increase to 10 mg/kg every 8 weeks if needed.
| Dosage form | VIAL |
| Renal impairment | No dose adjustment required for renal impairment; not removed by hemodialysis. |
| Liver impairment | No specific Child-Pugh based guidelines; use with caution in moderate to severe hepatic impairment due to potential increased risk of infections. |
| Pediatric use | For Crohn's disease: 5 mg/kg IV at weeks 0, 2, and 6, then every 8 weeks; for ulcerative colitis: 5 mg/kg IV at weeks 0, 2, and 6, then every 8 weeks. |
| Geriatric use | No specific dose adjustment; monitor closely for infections and infusion reactions due to increased age-related risks. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REMICADE (REMICADE).
| Breastfeeding | Infliximab is excreted in breast milk in low concentrations. The milk-to-plasma ratio is approximately 0.01–0.04, indicating minimal transfer. Limited data suggest no adverse effects in breastfed infants. However, because infliximab is a large protein, oral bioavailability is likely low due to digestion in the infant's gastrointestinal tract. Caution is advised; consider benefits of breastfeeding and potential infant exposure. |
| Teratogenic Risk | Infliximab (REMICADE) is a monoclonal IgG1 antibody that crosses the placenta predominantly during the third trimester. First trimester exposure is not associated with major malformations. Second and third trimester exposure may result in detectable serum levels in the infant for up to 6 months, potentially increasing risk of infections. No increased risk of congenital anomalies has been consistently demonstrated. |
■ FDA Black Box Warning
Increased risk of serious infections, including tuberculosis (TB), bacterial sepsis, invasive fungal infections (such as histoplasmosis), and infections due to other opportunistic pathogens. Also has been associated with reactivation of hepatitis B virus (HBV) in patients who are chronic carriers of this virus. Lymphoma and other malignancies, some fatal, have been reported in children and adolescent patients treated with TNF blockers, including infliximab.
| Serious Effects |
["Severe infection (such as abscess, TB, opportunistic infections)","Moderate to severe heart failure (NYHA Class III/IV)","History of hypersensitivity to infliximab or any murine proteins"]
| Precautions | ["Serious infections (including TB, invasive fungal, and other opportunistic infections)","Hepatitis B reactivation","Hepatotoxicity (severe hepatic reactions, including acute liver failure)","Heart failure (worsening or new onset)","Hematologic cytopenias (including pancytopenia)","Hypersensitivity reactions (including anaphylaxis and serum sickness-like reactions)","Demyelinating disease exacerbation or new onset","Lupus-like syndrome","Malignancies (including lymphoma)"] |
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| Fetal Monitoring | Monitor maternal disease activity (e.g., Crohn's disease, rheumatoid arthritis) throughout pregnancy. Assess fetal growth via serial ultrasound. Monitor for intrauterine growth restriction (IUGR) as disease activity may affect fetal growth. Evaluate newborn for infections; avoid live vaccines in infants exposed in utero for at least 6 months. Consider checking infant serum infliximab levels if clinically indicated. |
| Fertility Effects | Infliximab does not appear to impair fertility in men or women. Animal studies show no adverse effects on fertility. In humans, infliximab may improve fertility in women with inflammatory bowel disease or rheumatoid arthritis by reducing disease activity that can impair reproductive function. |