Anti-inflammatory Drugs

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Ocular Steroids - Powerhouse Potions

  • Potent anti-inflammatory & immunosuppressive agents, crucial in ophthalmology.
  • Mechanism:
    • Inhibit phospholipase A2 (PLA2) via lipocortin → ↓ arachidonic acid synthesis → ↓ prostaglandins & leukotrienes.
    • Stabilize mast cells, reduce capillary permeability & cellular exudation.
  • Types (Potency & Penetration):
    • Strong (High Potency): Prednisolone acetate (1% susp.), Dexamethasone (0.1%), Difluprednate (0.05% emulsion - very potent).
      • Excellent penetration: Prednisolone acetate, Difluprednate.
    • Moderate Potency: Fluorometholone (FML) (0.1%), Loteprednol etabonate (0.2%, 0.5%).
      • 📌 "Soft steroids" (Loteprednol, FML): Ester-based, rapidly metabolized locally; lower risk of ↑ IOP.
    • Weak Potency: Medrysone, Hydrocortisone (rarely used topically for significant inflammation).
  • Key Indications: Uveitis (all forms), severe allergic conjunctivitis/keratoconjunctivitis, post-operative inflammation, non-necrotizing scleritis, interstitial keratitis (non-infectious).
  • Major Side Effects:
    • ↑ Intraocular Pressure (IOP) → Steroid-induced glaucoma (monitor closely!).
    • ⭐ > Most common type of cataract induced by steroids is Posterior Subcapsular Cataract (PSC).
    • Delayed corneal epithelial wound healing.
    • ↑ Susceptibility to secondary infections (e.g., fungal keratitis, HSV reactivation).
    • Corneal thinning/perforation (prolonged use).
  • ⚠️ Cautions: Active infections (esp. dendritic HSV keratitis, fungal). Always taper dose gradually to prevent rebound inflammation.

Posterior subcapsular cataract

Ocular NSAIDs - Soothing Cyclo-Stoppers

  • Mechanism: Inhibit cyclooxygenase (COX-1 & COX-2) enzymes $ ightarrow$ ↓ prostaglandin synthesis.
  • Key Drugs & Properties:
    • Ketorolac 0.4% / 0.5%: Potent analgesic; widely used post-op.
    • Diclofenac 0.1%: Good anti-inflammatory; stings on instillation.
    • Flurbiprofen 0.03%: Intraoperative miosis inhibition.
    • Nepafenac 0.1% / 0.3%: Prodrug, better penetration; used for CME prevention post-cataract surgery.
    • Bromfenac 0.09%: Long half-life, once/twice daily dosing.
  • Primary Uses:
    • Post-operative inflammation & pain (cataract, refractive surgery).
    • Cystoid Macular Edema (CME) prophylaxis & treatment.
    • Allergic conjunctivitis (mild cases).
    • Episcleritis/Scleritis (adjunct or alternative to steroids).
    • Corneal abrasion pain relief.
  • Side Effects:
    • Stinging/burning on instillation (common).
    • Delayed corneal epithelial healing.
    • Rare: Corneal thinning/melt (especially with prolonged use or in compromised corneas).

⭐ Topical NSAIDs, especially ketorolac and diclofenac, can be associated with corneal melt in predisposed eyes (e.g., dry eye, rheumatoid arthritis).

COX pathway and NSAID inhibition

  • Advantages over Steroids:
    • No risk of ↑ Intraocular Pressure (IOP).
    • No risk of cataract formation.
    • Less immunosuppression. 📌 No Sight-threatening Adverse Incidents Daily (usually safe, but watch cornea!)

Other Immunomodulators - Specialized Shields

  • For chronic/severe immune ocular conditions; steroid-sparing.
  • Cyclosporine A (CsA): Calcineurin inhibitor; ↓ T-cell activation.
    • Topical (0.05%, 0.09%): ↑ tear production in KCS; VKC, AKC.

    ⭐ Topical Cyclosporine A (e.g., 0.05%) works by inhibiting T-cell activation and cytokine production, approved for increasing tear production in keratoconjunctivitis sicca (KCS).

    • Systemic: Severe uveitis (e.g., Behçet's). Key SE: Nephrotoxicity.
  • Tacrolimus (FK506): Calcineurin inhibitor (potent).
    • Topical (0.03%): VKC, AKC.
    • Systemic: Severe uveitis.
  • Sirolimus (Rapamycin): mTOR inhibitor. Uveitis.
  • Other Systemic Agents: For refractory uveitis.
    • Antimetabolites: Methotrexate, Azathioprine, Mycophenolate Mofetil (MMF).
    • Biologics: TNF-α inhibitors (e.g., Adalimumab for JIA-uveitis).

High‑Yield Points - ⚡ Biggest Takeaways

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Practice Questions: Anti-inflammatory Drugs

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Flashcards: Anti-inflammatory Drugs

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_____ toxicity can cause bull s eye maculopathy.

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_____ toxicity can cause bull s eye maculopathy.

Hydroxychloroquine

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