Ocular Pharmacology

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Ocular Pharmacokinetics & Routes - Eye Drug Journey

  • Key Barriers: Cornea (Lipophilic-Hydrophilic-Lipophilic layers), Blood-Aqueous Barrier (BAB), Blood-Retinal Barrier (BRB).
  • Topical Route: Commonest. Bioavailability ~5%. Governed by $pH = pKa + log([A-]/[HA])$. Systemic absorption via nasolacrimal duct.
  • Periocular Routes: Subconjunctival, Sub-Tenon's. Bypasses cornea, achieving higher local drug levels.
  • Intraocular Routes: Intravitreal, Intracameral. Offer 100% bioavailability; direct to target.
  • Systemic Route: Limited by BAB/BRB, especially for posterior segment delivery.

⭐ Topical drug absorption: Un-ionized, lipid-soluble forms penetrate the cornea more effectively. Ocular Drug Delivery Routes and Barriersoka

Autonomic Agents - Pupil & Pressure Puppeteers

  • Cholinergics (Miotics): Miosis, ciliary spasm, ↑outflow.
    • Direct: Pilocarpine (glaucoma), Carbachol.
      • Pilocarpine: 📌 Pilo-pin pupil.
    • Indirect: Physostigmine, Echothiophate.
    • Action: Miosis, accommodation, ↑trabecular outflow.

    ⭐ Pilocarpine 2% helps differentiate 3rd nerve palsy from pharmacological mydriasis.

  • Anticholinergics (Mydriatics/Cycloplegics): Mydriasis, cycloplegia (for refraction).
    • Atropine (long), Tropicamide (short).
    • Uses: Refraction (esp. children), uveitis (pain relief, prevent synechiae).
    • ⚠️ Risk: Angle-closure glaucoma.
  • Adrenergics:
    • α1 Agonist: Phenylephrine (mydriasis only, no cycloplegia).
    • α2 Agonists: Brimonidine, Apraclonidine (↓aqueous, ↑uveoscleral outflow).
    • β-Blockers: Timolol, Betaxolol (β1 selective) (↓aqueous production).
      • SEs: Bradycardia, bronchospasm.

Aqueous humor flow and drug targets in the eyeoka

Glaucoma Guardians - IOP Busters

Primary goal: Lower Intraocular Pressure (IOP). Medications target aqueous humor (AH) dynamics by decreasing production or increasing outflow.

  • Prostaglandin Analogs (PGAs): E.g., Latanoprost. ↑ Uveoscleral outflow. SE: iris pigmentation, lash growth. 📌 "Prosts" for outflow.
  • Beta-blockers: E.g., Timolol. ↓ AH production (ciliary body). Caution: systemic effects.
  • Alpha-2 Agonists: E.g., Brimonidine. Dual: ↓ AH production & ↑ uveoscleral outflow.
  • Carbonic Anhydrase Inhibitors (CAIs): E.g., Dorzolamide (topical), Acetazolamide (systemic). ↓ AH production (inhibits $HCO_3^-$ formation).
  • Miotics (Cholinergics): E.g., Pilocarpine. ↑ Trabecular outflow (ciliary muscle contraction).

⭐ Latanoprost is often first-line for open-angle glaucoma due to potent IOP reduction and once-daily dosing.

Glaucoma drug sites of action on aqueous humor pathways

Anti-Inflammatory & Anti-Infective Arsenal - Soothers & Slayers

  • Corticosteroids (Steroids):
    • Mechanism: Inhibit $PLA_2$ → ↓$PGs$, $LTs$.
    • Potent: Dexamethasone, Prednisolone. Soft: Fluorometholone (FML), Loteprednol (less IOP↑).
    • Uses: Uveitis, post-op, severe allergy.
    • SE: ↑IOP, PSC, infection risk.
  • NSAIDs (Non-Steroidal Anti-Inflammatory Drugs):
    • Mechanism: Inhibit $COX$ → ↓$PGs$.
    • Examples: Ketorolac, Nepafenac, Diclofenac.
    • Uses: Post-op pain/CME, allergy.
  • Anti-Infectives:
    • Antibacterial:
      • Fluoroquinolones (Moxifloxacin): Broad spectrum. 📌 "Floxacins Flock Everywhere" (penetration).
      • Aminoglycosides (Tobramycin): Gram -ve.
      • Macrolides (Azithromycin): Chlamydia.
    • Antifungal: Natamycin (filamentous), Amphotericin B/Voriconazole (Candida/Aspergillus).
    • Antiviral: Acyclovir (HSV), Ganciclovir (CMV).
    • Antiprotozoal: PHMB, Brolene (Acanthamoeba).

⭐ Steroid-induced glaucoma: common with Dexamethasone; less with FML, Loteprednol etabonate (soft steroids).

Miscellaneous Meds - Special Ops Agents

  • Anesthetics: Topical (Proparacaine); Injectable (Lignocaine).
  • Diagnostic Dyes:
    • Fluorescein: Stains corneal defects; Seidel's. (📌 FADES)

    ⭐ IV Fluorescein for Fundus Angiography (FFA) visualizes retinal circulation.

    • Rose Bengal/Lissamine Green: Stains devitalized cells (dry eye).
  • Anti-VEGF: Ranibizumab, Bevacizumab, Aflibercept (neovascularization).
  • Lubricants: Artificial tears (CMC, HPMC) for dry eye.

High‑Yield Points - ⚡ Biggest Takeaways

  • Autonomic drugs: pilocarpine (miotic), atropine (mydriatic/cycloplegic), timolol (↓IOP).
  • Prostaglandin analogs (e.g., latanoprost): first-line for glaucoma, ↑ uveoscleral outflow.
  • Topical steroids: potent anti-inflammatory; risk ↑IOP, cataracts.
  • Antivirals (e.g., acyclovir) treat herpes simplex keratitis.
  • Anti-VEGF agents (e.g., ranibizumab) for wet AMD, diabetic macular edema.
  • Fluorescein dye stains corneal abrasions; used in applanation tonometry.
  • Benzalkonium chloride (BAK), a common preservative, can cause ocular surface toxicity.

Practice Questions: Ocular Pharmacology

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Anti-glaucoma drug that acts by increasing uveoscleral outflow is

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Flashcards: Ocular Pharmacology

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Uveal tissue consists of _____

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Uveal tissue consists of _____

iris, ciliary body, and choroid.

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