Pharmacology

Published on 10/03/2015 by admin

Filed under Opthalmology

Last modified 22/04/2025

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2 Pharmacology

Routes of Administration

Topical

absorption related to corneal penetration

Anesthetics

Autonomic System

Cholinergic Drugs

Ocular Hypotensive (Glaucoma) Medications

Miotics

Anti-Inflammatory Drugs

Steroids

Potency

increased by 1–2 double bond(s), 9 fluorination, 6 methylation, O at C11; IOP elevation from deoxygenation at C21 (Table 2-2)

Table 2-2 Relative potencies of steroids

Steroid Relative potency
Hydrocortisone 1 (the standard)
Cortisone 0.8
Triamcinolone 4
Prednisone 4
Prednisolone 5
Dexamethasone 25–30
Betamethasone 25–30
Fluorometholone 40–50
Fluocinolone 240

Subconjunctival / sub-Tenon’s injection (Table 2-3)

produces higher ocular concentration and longer duration; beware in IOP responder

Table 2-3 Common ophthalmic steroids

Generic name Trade name
Topical  
Prednisolone acetate 1% Pred Forte, Omni Pred
Fluorometholone acetate 0.1% Flarex
Dexamethasone alcohol 0.1% Maxidex
Fluorometholone alcohol 0.1% FML
Prednisolone phosphate 1% Inflamase
Dexamethasone phosphate 1% Decadron
Difluprednate 0.05% Durezol
Loteprednol etabonate 0.5% Lotemax
Loteprednol etabonate 0.2% Alrex
Subconjunctival  
Dexamethasone phosphate Decadron
Methylprednisolone acetate Solumedrol, Depomedrol
Prednisolone acetate Durapred
Triamcinolone acetonide Kenalog
Betamethasone Celestone
Intravitreal  
Triamcinolone acetonide Kenalog, Triesence

Immunosuppressive Agents

Anti-Infective Drugs

Antibiotics

Inhibitors of Cell Wall Synthesis

β-Lactams (cidal)

Inhibitors of Protein Synthesis

Antifungals

Ocular Toxicology (Table 2-4)

Anticholinergics (atropine, scopolamine, Donnatal)

toxicity causes flushing, agitation, tachycardia, somnolence, dry mouth, dry eye, mydriasis, cycloplegia, blurry vision, angle closure; increased sensitivity in albinism, Down syndrome, and neonates

Table 2-4 Ocular toxicology

Ocular structure Effect Drug
Extraocular muscles Nystagmus, diplopia Anesthetics, sedatives, anticonvulsants, propranolol, antibiotics, phenothiazines, pentobarbital, carbamazepine, MAO inhibitors
Lid Edema Chloral hydrate
  Discoloration Phenothiazines
  Ptosis Guanethidine, propranolol, barbiturates
Conjunctiva Hyperemia Reserpine, methyldopa
  Allergy Antibiotics, sulfonamides, atropine, antivirals, glaucoma medications
  Discoloration Phenothiazines, chlorambucil, phenylbutazone
Cornea Keratitis Antibiotics, phenylbutazone, barbiturates, chlorambucil, steroids
  Deposits Chloroquine, amiodarone, tamoxifen, indomethacin, gold
  Pigmentation Vitamin D
Increased IOP Open angle Anticholinergics, caffeine, steroids
  Narrow angle Anticholinergics, antihistamines, phenothiazines, tricyclic antidepressants, haloperidol, sulfonamides (Topamax)
Lens Opacities / cataract Steroids, phenothiazines, ibuprofen, allopurinol, long-acting miotics
  Myopia Sulfonamides, tetracycline, prochlorperazine, autonomic antagonists, duloxetine (Cymbalta)
Retina Edema Chloramphenicol, indomethacin, tamoxifen, carmustine
  Hemorrhage Anticoagulants, ethambutol
  Vascular damage Oral contraceptives, oxygen, aminoglycosides, talc, carmustine, interferon
  Pigmentary degeneration Phenothiazines, indomethacin, nalidixic acid, ethambutol, isotretinoin, chloroquine, hydroxychloroquine
Optic nerve Neuropathy Ethambutol, isoniazid, sulfonamides, digitalis, imipramine, streptomycin, busulfan, cisplatin, vincristine, chloramphenicol, disulfiram
  Papilledema Steroids, vitamin A, tetracycline, phenylbutazone, amiodarone, nalidixic acid, isotretinoin

Review Questions (Answers start on page 357)