Pharmacology I · Exam 2 · Class of 2028

Ocular Drug Reference

Every agent in the ophthalmology lecture, with indication, patient education, side effects, contraindications and mechanism. 30 entries, each citing its slide. Indication, education, side effects and contraindications come FIRST, because mechanism is the part already over-weighted.

★ The one he said he would ask

In the recording, on the topical vasoconstrictors: “Most of you will probably forget this and we’ll get it wrong on the test. But I will tell you, I will ask this question … there’s rebound hyperemia … star that, underline it, highlight it. A lot of people still get it wrong every test. I don’t know why because I tell you explicitly, that’s what I’m going to be asking about.”

So: no more than two weeks, because prolonged use causes rebound hyperemia on stopping; and if no improvement in 72 hours, stop and see a provider. He noted the same trap returns with nasal sprays in ENT.

What he took OFF the table

Indications for the individual antibiotics — “don’t worry so much about indications for use … a lot of them have a lot of crossover.” They are listed below for reference, not for memorizing.
Formulations — “I don’t care that you memorize that necessarily, with some exceptions.”
Which agent causes irritation or hypersensitivity — “don’t memorize which ones cause eye irritation or hypersensitivity. ANY of these can do that.” The effects worth attaching to one class are the aminoglycoside corneal ulceration, the ciprofloxacin white precipitate, and the fluoroquinolone taste.
The specific combination products — “I don’t care that you memorize, but just know if I was to say, hey, patient’s on this drug right now, what would be a helpful second line agent to add on?” So learn the principle: add a different mechanism, for synergy and fewer drops.

Antibacterial Antiviral Antifungal Allergy Inflammation Dry eye Glaucoma Diagnostic

Antibacterial

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Erythromycin (ointment)	Superficial conjunctival or corneal infection; prophylaxis of ophthalmia neonatorum	Soothing on an inflamed eye, so it may be used even when bacterial infection is not confirmed. Dirt cheap.	Ocular irritation, hypersensitivity — shared by essentially every ophthalmic antibiotic	None specific	Blocks transpeptidation at the 50S ribosome	slide 15
Azithromycin (AzaSite)	Bacterial conjunctivitis	Given twice daily rather than four or more times — but considerably more expensive, so not used as often clinically.	Ocular irritation, hypersensitivity	Cost is the practical barrier	Blocks transpeptidation at the 50S ribosome	slide 17
Ciprofloxacin (Ciloxan)	Conjunctivitis, keratitis, corneal ulcers, blepharitis, dacryocystitis	A WHITE PRECIPITATE appears in about 17% — specific to this agent, and worth warning about so it is not mistaken for worsening.	Ocular irritation, white precipitate, unpleasant taste after instillation	Emerging resistance; expensive	Inhibits DNA gyrase and topoisomerase IV	slide 21
Moxifloxacin (Vigamox), ofloxacin, levofloxacin, gatifloxacin	Conjunctivitis; corneal ulcers	PREFERRED for corneal ulcers or suspected Pseudomonas, and for conjunctivitis in CONTACT LENS WEARERS once keratitis is excluded.	Ocular irritation, unpleasant taste after instillation	Expensive; emerging resistance	Inhibits DNA gyrase and topoisomerase IV	slide 22
Gentamicin, tobramycin (Tobrex)	Conjunctivitis and external infections of the eye and adnexa	Watch for CORNEAL ULCERATION and reactive keratoconjunctivitis after several days of use — the one adverse effect specific enough to attach to a class.	Ocular irritation, CORNEAL ULCERATION, reactive keratoconjunctivitis	Prolonged use	Binds the 30S ribosomal subunit	slide 23
Sulfacetamide sodium	Bacterial conjunctivitis and other superficial ocular infection	Ask about sulfa allergy before prescribing.	Ocular irritation, allergic reactions	AVOID in sulfonamide allergy	Antagonizes PABA to block folic acid synthesis	slide 19
Bacitracin (ointment)	Bacterial conjunctivitis, blepharitis, keratitis, corneal ulcers, meibomianitis	Inexpensive ointment for lid and surface disease.	Ocular irritation	None specific	Blocks cell wall synthesis by preventing mucopeptide transfer	slide 20
Trimethoprim / polymyxin B (Polytrim)	Bacterial conjunctivitis	A combination of two different mechanisms in one drop.	Ocular irritation	None clinically	Trimethoprim blocks reduction of folic acid to tetrahydrofolate; polymyxin B binds membrane phospholipids and lets contents leak	slide 18

Antiviral

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Trifluridine (Viroptic)	Herpes simplex keratitis and keratoconjunctivitis	The topical antiviral. Adenoviral conjunctivitis has NO antiviral — it is self-limited and treated symptomatically.	Ocular irritation, PUNCTATE KERATOPATHY, hypersensitivity	None specific	Inhibits thymidylate synthetase and substitutes for thymidine in viral DNA	slide 27
Ganciclovir (Zirgan)	Herpetic keratitis; cytomegalovirus retinitis by intravitreal injection	The other ophthalmic preparation alongside trifluridine.	Ocular irritation, punctate keratitis	None specific	Competitively inhibits deoxyguanosine triphosphate binding to DNA polymerase	slide 28
Acyclovir, valacyclovir, famciclovir	Herpes zoster ophthalmicus; herpes simplex keratitis and iridocyclitis	Oral or intravenous rather than topical.	Systemic	Renal dosing considerations	Nucleoside analogs	slide 26
Foscarnet, ganciclovir, valganciclovir, cidofovir	Cytomegalovirus retinitis	Intravenous, oral or intravitreal — specialty use cases.	Systemic toxicity	Specialty use	Various antiviral mechanisms	slide 26

Antifungal

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Natamycin (Natacyn)	Conjunctivitis and keratitis from Aspergillus, Candida, Cephalosporium, Fusarium, Penicillium	THE ONLY commercially available ophthalmic antifungal. Everything else is compounded or systemic. Risk factors for ocular fungal infection: trauma, chronic ocular surface disease, contact lens wear, immunosuppression INCLUDING topical steroid use.	Ocular irritation	None specific	Binds sterol, increasing fungal cell membrane permeability	slide 32

Allergy

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Ketotifen (Zaditor, OTC), olopatadine, azelastine, alcaftadine, bepotastine, emedastine, epinastine	Ocular allergy	Onset within MINUTES; allow two weeks to judge full efficacy. Typically PREFERRED over mast cell stabilizers.	Ocular irritation, headache, INCREASED ocular dryness	No significant interactions	H1 INVERSE AGONISTS — they inactivate the receptor rather than simply blocking it, and remain competitive with histamine	slide 42
Cromolyn (Opticrom), lodoxamide (Alomide), nedocromil (Alocril)	Predictable seasonal allergy in patients who cannot tolerate other therapy	5 to 14 days for full efficacy and NOT useful for acute symptoms. Often four times daily, which is not ideal.	Ocular irritation, unpleasant taste, headache	None specific	Inhibit mast cell degranulation, limiting histamine, tryptase and prostaglandin D2	slide 45
Tetrahydrozoline (Opti-Clear), naphazoline (VasoClear), naphazoline with pheniramine (Visine-A)	Short-term relief of conjunctival redness and edema	★ NO MORE THAN TWO WEEKS — prolonged use causes REBOUND HYPEREMIA on stopping. If no improvement within 72 HOURS, stop and see a provider. The same trap appears with nasal sprays.	REBOUND HYPEREMIA after discontinuation	Prolonged use; accidental ingestion in children	Alpha-1 agonist LOCALLY; these imidazolines target alpha-2 SYSTEMICALLY, which is what makes an ingestion dangerous	slide 48

Inflammation

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Bromfenac, diclofenac, flurbiprofen, ketorolac, nepafenac	Postoperative inflammation and pain; allergic conjunctivitis	NOT routinely recommended for conjunctivitis.	Lacrimation, keratitis, RAISED intraocular pressure, ocular irritation	Caution where pressure matters	Block cyclooxygenase, stopping conversion of arachidonic acid to prostaglandins and thromboxanes	slide 51
Dexamethasone, prednisolone (Pred Forte), difluprednate	Severe ocular allergy, anterior uveitis, external eye inflammatory disease, inflammation after ocular surgery	Limited to a pulse of LESS THAN TWO WEEKS. Generally reserved for refractory symptoms.	CATARACT formation, raised pressure and glaucoma, infection from reduced immune function, delayed wound healing, corneal ulcers	Raised pressure is MORE LIKELY WITH A FAMILY HISTORY	Inhibit phospholipase A2, cutting off arachidonic acid derived mediators; also inhibit fibrin and collagen deposition, reducing scarring	slide 52
Fluorometholone (FML), loteprednol (Alrex), rimexolone (Vexol)	As for the other ocular steroids	The SOFT STEROIDS — lower risk of raising intraocular pressure.	Same class risks, but less pressure elevation	Same cautions, reduced	As for the glucocorticoids	slide 55

Dry eye

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Cyclosporine (Restasis)	Chronic dry eye with inflammation — keratoconjunctivitis sicca	Treat the underlying disease first. Systemic causes: Sjogren syndrome, rheumatoid arthritis, vitamin A deficiency, Stevens-Johnson syndrome.	OCULAR BURNING (17%), foreign body sensation, blurred vision	None specific	Inhibits production and release of interleukin 2, reducing T cell activation; raises tear production	slide 58

Glaucoma

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Latanoprost (Xalatan), travoprost, bimatoprost (Lumigan), tafluprost	Open-angle glaucoma — FIRST LINE and the most commonly used	ONCE DAILY and do not exceed it — more frequent dosing INHIBITS the pressure-lowering effect. Warn about lash and iris changes.	Conjunctival hyperemia, ocular irritation, CHANGES IN EYELASH LENGTH AND IRIS COLOR	Limited systemic side effects	Prostaglandin F2 alpha analogs; increase aqueous OUTFLOW	slide 65
Timolol (Timoptic), carteolol, levobunolol — nonselective	Open-angle glaucoma — second line	Nonselective is MORE efficacious in the eye because beta-2 receptors predominate there — but that is also why it is worse tolerated.	Worsening heart failure, BRADYCARDIA, heart block, INCREASED AIRWAY RESISTANCE	Asthma, heart failure, bradyarrhythmia	Block beta receptors in ciliary body epithelium; less cyclic AMP, less aqueous PRODUCTION	slide 67
Betaxolol (Betoptic-S) — beta-1 selective	Open-angle glaucoma	The selective option, so LESS risk of bronchoconstriction in a patient with asthma.	As for the class, reduced respiratory risk	Still cardiac caution	Selective beta-1 blockade; reduces aqueous production	slide 68
Brimonidine (Alphagan P), apraclonidine (Iopidine)	Open-angle glaucoma — the only class doing BOTH jobs	Brimonidine is more lipophilic; apraclonidine is highly ionized at physiological pH. Allergic conjunctivitis is LESS common with brimonidine.	Ocular irritation, hyperemia (rebound effect), pruritus, allergic conjunctivitis	CONTRAINDICATED IN CHILDREN UNDER TWO — central nervous system depression and apnea	Alpha-2 agonists; decrease production AND increase outflow	slide 69
Dorzolamide (Trusopt), brinzolamide (Azopt)	Open-angle glaucoma	Warn about the taste and the sting — both are common enough to cause people to stop.	BITTER TASTE (25%), burning or stinging (33%), allergic conjunctivitis	Sulfonamide-derived	Inhibit carbonic anhydrase in ciliary body epithelium; less bicarbonate, less fluid transport	slide 70
Pilocarpine (Pilopine HS), carbachol (Miostat), acetylcholine (Miochol-E)	Open-angle glaucoma; acetylcholine in surgical settings	Poor compliance from side effects and frequent dosing. YOUNGER patients are usually intolerant because of the visual blurring.	FIXED SMALL PUPILS, myopia, visual disturbance, headache	Younger patients tolerate miotics poorly	Activate muscarinic receptors; ciliary muscle contraction facilitates OUTFLOW	slide 72

Diagnostic

Agent	Indication	Patient education	Side effects	Contraindications & cautions	Mechanism	Slide
Proparacaine (Alcaine), tetracaine (Altacaine)	Tonometry, foreign body removal, superficial corneal surgery	★ DO NOT WRITE PRESCRIPTIONS FOR THESE. The eye stays numb 10 to 20 minutes with NO BLINK REFLEX.	Hypersensitivity, burning sensation	Never dispensed for home use	Inhibit sodium influx into the neuron, preventing signal propagation	slide 75
Tropicamide (Mydriacyl), cyclopentolate (Cyclogyl), atropine	Fundoscopic examination; uveitis, to prevent synechiae and relieve ciliary spasm	Mydriasis. The pupil is LESS reactive to light than with a sympathomimetic.	Photosensitivity, blurred vision	Caution where dilation is unsafe	Antimuscarinics — competitively block muscarinic acetylcholine receptors	slide 76
Phenylephrine (Neo-Synephrine)	Mydriasis for examination	The dilated pupil stays MORE REACTIVE TO LIGHT than with an antimuscarinic.	Photosensitivity, conjunctival hyperemia	Caution in cardiovascular disease	Adrenergic receptor agonist	slide 77
Fluorescein	Anterior segment staining; disclosing corneal injury	Reveals epithelial defects of the cornea and conjunctiva.	Hypersensitivity, burning sensation	None specific	Stains epithelial defects	slide 78