Drugs Used in Rheumatoid Arthritis

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RA & DMARDs Intro - Joint Warfare Kickoff

  • Rheumatoid Arthritis (RA): Chronic, autoimmune, systemic inflammatory disease targeting synovial joints.
  • Pathogenesis: Immune attack (T/B cells, Mφ) + cytokines (TNF-α, IL-1, IL-6) → synovitis, pannus, joint destruction.
  • Goals: Remission/low activity, ↓inflammation/pain, prevent damage, ↑QoL.
  • DMARDs (Disease-Modifying Antirheumatic Drugs):
    • csDMARDs (Conventional Synthetic)
    • tsDMARDs (Targeted Synthetic)
    • bDMARDs (Biologic) Radiograph of hands with rheumatoid arthritis

⭐ Early aggressive treatment with DMARDs is crucial to prevent irreversible joint damage and disability in RA.

csDMARDs - Classic Joint Defenders

⭐ Methotrexate is the anchor csDMARD for RA; co-administration of folic acid (e.g., 5 mg/week) is essential to mitigate its hematologic, GI, and hepatic side effects.

DrugMoAKey ADRs (📌 MTX: Myelosuppression, Stomatitis, Liver fibrosis, Pneumonitis)ContraindicationsMonitoring
Methotrexate (MTX)DHFR inhibitorMyelosuppression, Stomatitis, Liver fibrosis, PneumonitisPregnancy, liver/renal diseaseCBC, LFTs, Scr
Sulfasalazine (SSZ)Anti-inflam., immunomod.GI upset, rash, oligospermia, yellow-orange urineSulfa allergy, G6PD def.CBC, LFTs
Leflunomide (LEF)DHODH inhibitorDiarrhea, hepatotoxicity, alopecia, HTNPregnancy, liver diseaseCBC, LFTs, BP
Hydroxychloroquine (HCQ)TLR inhib., ↑lysosomal pHRetinopathy, GI upset, rashPre-existing maculopathyEye exam (baseline, annual >5yrs)

bDMARDs (TNF & IL-6) - Cytokine Storm Tamers

Biological DMARDs (bDMARDs) targeting Tumor Necrosis Factor-alpha (TNF-α) and Interleukin-6 (IL-6) are pivotal in Rheumatoid Arthritis (RA) management by downregulating inflammatory cytokine pathways.

FeatureTNF-α InhibitorsIL-6R Antagonists
ExamplesEtanercept, Infliximab, Adalimumab, Golimumab, CertolizumabTocilizumab, Sarilumab
MechanismNeutralize TNF-α, reducing inflammation.Block IL-6 receptor, inhibiting IL-6 signaling.
Key ADRs↑ Infections (esp. TB reactivation), demyelination, injection site reactions.↑ Infections, dyslipidemia, ↑ LFTs, GI perforation (rare).
Pre-screeningLatent TB, Hepatitis B/C.Latent TB, Hepatitis B/C, LFTs, lipid profile.

More Biologics & JAKinibs - Precision Joint Ops

  • Other bDMARDs:
    • Abatacept: T-cell co-stimulation modulator. For moderate-severe RA.
    • Rituximab: Anti-CD20 B-cell depleter. For TNF-inhibitor refractory RA. ADR: ⚠️ PML.
  • JAK Inhibitors (tsDMARDs - Oral):
    • Tofacitinib, Baricitinib, Upadacitinib.
    • MOA: Inhibit Janus Kinase (JAK) enzymes.
    • ADRs: Infections (herpes zoster), cytopenias, ↑ lipids.

    ⭐ JAK inhibitors (e.g., Tofacitinib) are oral targeted DMARDs but carry FDA boxed warnings for increased risk of serious infections, malignancy, major adverse cardiovascular events (MACE), and thrombosis. Biologic agents mechanisms in rheumatoid arthritisoka

Adjuncts & Strategy - Relief Crew & Tactics

  • NSAIDs: Symptomatic relief (pain, inflammation). No disease modification. Key ADRs: GI, renal.
  • Glucocorticoids: Rapid symptom control (bridging/flares). Bridging: <10mg/day prednisone. ADRs: osteoporosis. Taper ASAP.

    ⭐ Glucocorticoids are used for rapid symptom control in RA (bridging therapy or flare management) but should be tapered to the lowest effective dose or discontinued as soon as possible due to long-term side effects.

  • Strategy:
    • Treat-to-Target (T2T): Aim remission/Low Disease Activity (LDA).
    • Combination DMARDs.
    • Monitor disease activity (DAS28).

High‑Yield Points - ⚡ Biggest Takeaways

  • Methotrexate (MTX) is the anchor DMARD for RA, typically first-line.
  • Leflunomide inhibits dihydroorotate dehydrogenase; an alternative to MTX.
  • Sulfasalazine is used for mild RA and IBD; may cause oligospermia.
  • Hydroxychloroquine (HCQ) is safest DMARD in pregnancy; requires retinal screening.
  • TNF-α inhibitors (e.g., Infliximab, Adalimumab) increase risk of TB reactivation.
  • Rituximab, a CD20 inhibitor, depletes B-cells.
  • Tofacitinib is an oral JAK inhibitor, a newer targeted DMARD.

Practice Questions: Drugs Used in Rheumatoid Arthritis

Test your understanding with these related questions

Which of the following drugs is not used in Rheumatoid arthritis?

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Flashcards: Drugs Used in Rheumatoid Arthritis

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IL-4 is an _____inflammatory cytokine.

TAP TO REVEAL ANSWER

IL-4 is an _____inflammatory cytokine.

anti-

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