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Drugs, Supplies and Delivery
Certolizumab (Cimzia)
Certolizumab, marketed under the brand name Cimzia, is a biologic medication and a PEGylated tumor necrosis factor-alpha (TNF-α) inhibitor. Unlike other TNF inhibitors, certolizumab lacks an Fc region, minimizing placental transfer and making it a preferred option for certain patient populations. It is used to treat autoimmune conditions such as rheumatoid arthritis (RA), psoriatic arthritis (PsA), axial spondyloarthritis (axSpA), Crohn’s disease, and plaque psoriasis. This article synthesizes information from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to detail certolizumab’s mechanism, uses, dosing, side effects, precautions, and interactions.
Certolizumab is a monoclonal antibody fragment (Fab’) conjugated to polyethylene glycol (PEG). It binds to and neutralizes soluble and membrane-bound TNF-α, a pro-inflammatory cytokine. By inhibiting TNF-α, certolizumab:
- Reduces inflammation: Blocks TNF-α from activating immune cells and producing inflammatory mediators (e.g., IL-1, IL-6).
- Modulates immune response: Suppresses tissue damage in autoimmune diseases (Lippincott, Lange).
The PEGylation extends its half-life to ~14 days, allowing biweekly dosing. The absence of an Fc region prevents placental transfer, making it safer in pregnancy (BNF).
- Rheumatoid Arthritis (RA):
- Reduces joint inflammation and slows radiographic progression, often combined with methotrexate (BNF).
- Psoriatic Arthritis (PsA):
- Improves skin and joint symptoms (Lippincott).
- Axial Spondyloarthritis (axSpA):
- Includes ankylosing spondylitis and non-radiographic axSpA (Lange).
- Crohn’s Disease:
- Induces and maintains remission in moderate to severe cases (BNF).
- Plaque Psoriasis:
- Treats adults with moderate to severe psoriasis (Lippincott).
- RA, PsA, axSpA:
- Initial dose: 400 mg subcutaneously at weeks 0, 2, and 4.
- Maintenance: 200 mg every 2 weeks or 400 mg every 4 weeks (BNF).
- Crohn’s Disease:
- 400 mg subcutaneously at weeks 0, 2, and 4, then 400 mg every 4 weeks (Lippincott).
- Plaque Psoriasis:
- 400 mg every 2 weeks for two doses, then 200 mg every 2 weeks (Lange).
Administration:
- Administer subcutaneously into the thigh or abdomen.
- Rotate injection sites to avoid skin reactions (BNF).
- Common: Upper respiratory infections, injection-site reactions (pain, erythema), and headache (Lippincott).
- Serious:
- Infections: Tuberculosis (TB) reactivation, invasive fungal infections (e.g., histoplasmosis), and sepsis (Lange).
- Malignancies: Increased risk of lymphoma and skin cancer (BNF).
- Heart Failure: Exacerbation of pre-existing heart failure (Lippincott).
- Demyelinating Disorders: Rare cases of multiple sclerosis-like symptoms (Lange).
- Active Infections: Avoid use in active TB, sepsis, or opportunistic infections. Screen for latent TB and hepatitis B before initiation (BNF).
- Heart Failure: Avoid in moderate to severe heart failure (Lippincott).
- Pregnancy/Lactation: Preferred over other TNF inhibitors in pregnancy due to minimal placental transfer. Compatible with breastfeeding (Lange).
- Hypersensitivity: Contraindicated in patients with severe reactions to certolizumab or its components (BNF).
- Live Vaccines: Avoid concurrent use (e.g., MMR, varicella) due to immunosuppression (Lippincott).
- Other Immunosuppressants: Increased infection risk with methotrexate, corticosteroids, or JAK inhibitors (Lange).
- Abatacept/Anakinra: Avoid combination due to heightened infection risk (BNF).
Certolizumab pegol is the generic name. It is marketed under the brand name Cimzia®. Available as pre-filled syringes (200 mg/mL) or lyophilized powder for reconstitution. Biosimilars are not yet widely available as of 2023.
