Remicade
Remicade
Generic Name
Remicade
Mechanism
Remicade (infliximab) is a chimeric monoclonal antibody that binds both soluble and membrane‑bound TNF‑α (tumor necrosis factor‑α).
* Neutralization of TNF‑α → ↓ inflammatory cytokine signaling.
* Induction of apoptosis in TNF‑α‑expressing cells.
* Complement‑mediated cytotoxicity against TNF‑α–positive cells.
Result: attenuation of the inflammatory cascade central to autoimmune diseases such as Crohn’s disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, and plaque psoriasis.
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Pharmacokinetics
| Parameter | Typical Values | Notes |
| Absorption | Intravenous infusion (median 3.2 mg/kg). | No oral formulation. |
| Distribution | 11–14 L/kg; Vd ~15 L (∼3 % of plasma proteins). | Limited penetration into adipose tissue. |
| Metabolism | Proteolytic catabolism → amino acids. | No hepatic or renal metabolism. |
| Elimination | Half‑life 8–10 days (dose‑dependent). | Clearance 1–2 L/d. |
| Bioavailability | 100 % (IV). | • |
| Accumulation | Linear; steady‑state at week 14–16 (4–6 infusions). | • |
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Indications
* Rheumatoid arthritis (sufficiently active disease in adults, 6–15 mg/kg induction, then 3–5 mg/kg q8–12 weeks).
* Crohn’s disease (moderate‑to‑severe; 5 mg/kg induction, then 5 mg/kg q8 weeks).
* Ulcerative colitis (moderate‑to‑severe; 5 mg/kg induction, then 5 mg/kg q8 weeks).
* Ankylosing spondylitis (≥2 infliximab courses).
* Plaque psoriasis (severe disease; 5 mg/kg induction, then 5 mg/kg q8 weeks).
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Contraindications
* Contraindications:
• Active, uncontrolled infections (TB, endemic fungal).
• Known hypersensitivity to infliximab or murine proteins.
* Warnings:
• Infection risk: reactivation of latent TB, opportunistic infections (Pneumocystis jirovecii, CMV).
• Malignancy: increased risk of non‑melanoma skin cancers and lymphoma (especially if used with other immunosuppressants).
• Heart failure: exacerbation of congestive symptoms (Class III/IV HF).
• Infusion reactions: anaphylactic, anaphylactoid, or delayed reactions.
• Vaccinations: live vaccines contraindicated; inactivated vaccines may be used but efficacy can be reduced.
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Dosing
* Induction (Weeks 0, 2, 6)
• Adults: 5 mg/kg IV over 2 h (initial 90 min, subsequent 60 min).
• Pediatrics (≥ 27 kg): same dosing; < 27 kg → weight‑based 5 mg/kg.
* Maintenance
• 5 mg/kg IV every 8 weeks (common).
• Alternatively, 3–5 mg/kg q8–12 weeks for rheumatoid arthritis.
* Intravenous infusion schedule: patient monitored for ≥ 30 min post‑infusion.
* Premedication: antihistamine, acetaminophen ± corticosteroid (if prior infusion reaction).
* Tapering: discontinue after 24–36 months unless relapse occurs.
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Adverse Effects
| Category | Representative Adverse Effects |
| Common |
• Infusion reactions (fever, chills, rash, SOB). • Upper respiratory tract infections. • Headache. |
| Serious |
• Serious infections (TB, fungal, viral). • Neoplasm (non‑melanoma skin cancer, lymphoma). • Heart failure decompensation. • Hepatotoxicity (↑ALT/AST). • Progressive multifocal leukoencephalopathy (PML). |
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Monitoring
* Baseline
• TB screening (IGRA/PPD, chest X‑ray).
• CBC, CMP, ESR/CRP.
• Hepatitis B/C serology.
* During Therapy
• CBC and CMP at each infusion.
• Monitor for signs of infection or malignancy.
• Drug‑tolerability: pre‑infusion vitals, post‑infusion observation.
* After 24 months: reassess continued need; consider drug‑level testing if therapeutic failure.
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Clinical Pearls
* Steroid‑Boost – Initiating Remicade with a short taper of oral steroids reduces early infusion reactions (past 20 % reduction).
* Biologic Sequencing – Switching to Remicade after anti‑TNF‑α failure (e.g., adalimumab) is effective in ~40 % of patients; consider anti‑drug antibodies.
* Pediatric Care – In infants (< 27 kg), use 5 mg/kg dosing; weight‑based monitoring prevents over‑exposure in rapid growth.
* Infusion Time Optimization – Patients with ≤ 2 prior reactions can have infusion time shortened to 90 min after the first 2 h exposure.
* Vaccination Strategy – Inactivated vaccines can be administered 2–4 weeks before the first dose; avoid live vaccines until cessation of therapy.
* Drug Interactions – Remicade does not inhibit cytochrome P‑450 enzymes; however, co‑administration with biologics (e.g., abatacept) can increase infection risk.
* Storage – Reconstituted solution must be used within 24 h; store at 2–8 °C in a protected area.
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