ANTI-INFLAMMATORY: ALLERGY

IMIDAZOLES Inhibit ergosterol in fungal cell membranes, but activity is limited by metabolism. Clotrimazole, miconazole, econazole, ketoconazole, and thiabendazole all may be made into topical preparations.

NATAMYCIN (Natacyn, Pimaricin) 5% solution every 1 hour (50 mg/mL). Only commercially available topical antifungal. Polyene binds to sterols, damaging cell membranes of Þlamentous fungi, with activity similar to AMB; especially active against Fusarium and Aspergillus. Local hypersensitivity reaction is common, but it is the least toxic of the polyenes.

TRIAZOLES Action similar to imidazoles but less vulnerable to host metabolic degradation. Fluconazole (most active against Candida) and itraconazole may be made into a topical preparation.

Anti-inflammatory: Allergy

ANTAZOLINE, PHENIRAMINE, PYRILAMINE Traditional antihistamines.

AZELASTINE (Optivar) 1 gtt bid. Dual-mechanism antihistamine and mast cell stabilizer.

COMBINATION ANTIHISTAMINE PLUS OCULAR DECONGESTANT Naph- con-A, AK-Con-A, Opcon-A (pheniramine þ naphazoline), Vasocon-A (antazoline þ naphazoline).

CROMOLYN SODIUM (Crolom, Opticrom) 1 drop 4 to 6 times per day (solution 4%). Inhibits mast cell degranulation and thus blocks histamine release; used for prevention of allergic effects, not acute treatment.

EMEDASTINE (Emadine) 1 gtt qid (solution 0.05%). Potent, selective H1- antagonist.

KETOTIFEN (Zaditor) 1 gtt every 8 to 12 hours (solution 0.025%). Mast cell stabilizer.

LEVOCABASTINE (Livostin) 1 gtt qid (suspension 0.05%). Long-acting, highly potent, and selective H1-antagonist.

LODOXAMIDE (Alomide) 1 drop qid (solution 0.1%). Mechanism similar to cromolyn.

NAPHAZOLINE (Albalon, AK-Con, Vasocon, Naphcon) 1 gtt every 3 to 4 hours prn up to qid (solution 0.012, 0.02, 0.03, 0.1%). Vasoconstrictor that provides symptomatic relief by decreasing conjunctival edema and hyperemia.

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378 MEDICATIONS

OLOPATADINE (Patanol) 1 drop bid (solution 0.1%). Dual action as a mast cell stabilizer and highly selective H1-antagonist antihistamine.

PEMIROLAST (Alamast) 1 gtt qid (solution 0.1%). Mast cell stabilizer.

Anti-inflammatory: Antifibrotic

5-FLUOROURACIL (5FU): 50 mg/mL, 0.1 mL in 5Ð10 subconjunctival injections post-trabeculectomy, or 50 mg/mL on sponge for 3 to 5 minutes intraoperative. Pyrimidine analogue, inhibits thymidylate synthesis and DNA synthesis, incorporated during and aborts S phase, inhibits Þbroblast proliferation; application effective for about 3 weeks. Epithelial toxic. Also used in breast, gastrointestinal, and skin CA.

MITOMYCIN C (MMC) 0.2Ð0.5 mg/mL, 2 mL administered intraoperatively. Alkylating agent that cross-links DNA, not cell cycle speciÞc; dose is effective for about 5 hours. Has 100 > potency than 5FU. May cause avascular blebs, wound leak, hypotony, and intraocular toxicity.

Anti-inflammatory: Corticosteroids

PROPERTIES Binds to cytoplasmic glucocorticoid receptor that binds to DNA to increase or decrease gene transcription (over 100 steroidresponsive genes). Clinical effects include decreased capillary permeability, chemotaxis inhibition, and suppression of Þbrin deposition.

Also decreases eicosanoids (lipids derived from arachidonic acid in the cell membrane phospholipids):

Inhibits cyclooxygenase-created prostaglandins: vasodilation, increased permeability of bloodÐocular barrier, corneal neovascularization, decreased IOP via prostaglandin E2, prostaglandin D2, and prostaglandin F2-alpha.

Inhibits lipoxygenase-created leukotrienes: chemotactic for PMNs and eosinophils, conjunctival and uveal edema, immune modulation.

Also decreases platelet-activating factor, cytokines, tumor necrosis factor, nitrous oxide, and adhesion molecules. Downregulates ICAM-1, which is responsible for white blood cell (WBC) migration, and decreases growth factors and beta-adrenergic receptors.

May suppress endogenous steroids from adrenal cortex; created from cholesterol into corticosteroids (21 carbons) or androgens (19 carbons).

DEXAMETHASONE (Decadron, Maxidex, AK-Dex) 1 drop every l to 8 hours or ½Ð1 inch ribbon of ointment qdÐqid (suspension 0.1%, solution 0.1%,

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ointment 0.05%). Has >48 hours half-life; 30Ð40 more potent than hydrocortisone. Alcohol derivative is more effective than dexamethasone sodium phosphate.

FLUOROMETHOLONE (FML, FML Forte, Flarex) 1 drop every 1 to 12 hours or ½ inch ribbon of ointment every 4 to 24 hours (suspension 0.1, 0.25%, solution 0. l%, ointment 0.1%). Fluorinated structural analogue of progesterone that is less effective than dexamethasone or prednisolone but with a lower potential for elevating IOP. Acetate derivative (Flarex) is more effective than alcohol derivative (FML).

LOTEPREDNOL (Alrex, Lotemax) 1 drop qid (suspension 0.2, 0.5%).

MEDRYSONE (HMS) 1 gtt up to every 6 hours (suspension 1%). Least potent topical steroid.

PREDNISOLONE (AK-Pred, Pred Forte, Pred Mild) 1 gtt every l to 12 hours (suspension 0.12, 0.125, 1%, solution 0.125, 1%]. Has 12to 36-hour halflife and is 4 more potent than hydrocortisone.

RIMEXOLONE (Vexol) 1 drop every l to 6 hours (suspension 1%). Synthetic steroid that has same anti-inßammatory efÞcacy of 1% prednisolone but no greater risk of elevated IOP than ßuorometholone.

Anti-inflammatory: Nonsteroidals

PROPERTIES Blocks prostaglandin synthesis by inhibiting cyclooxygenase (and some affect lipoxygenase).

DICLOFENAC (Voltaren) 1 gtt qid (solution 0.1%) or 75 mg PO bid. Inhibition of postsurgical inßammation. Oral preparation has less bleeding than other nonspeciÞc NSAIDs.

FLURBIPROFEN (Ocufen) Used for allergy or inhibition of intraoperative miosis (solution 0.03%).

KETOROLAC (Acular) 1 gtt qid (solution 0.5%). Relief of allergic conjunctivitis itch and inhibition of postsurgical inßammation.

ORAL AGENTS Aspirin, ibuprofen, indomethacin, etc. Celecoxib (Celebrex) and others selectively inhibit COX-2 enzyme and thus have decreased systemic side effects.

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380 MEDICATIONS

SUPROFEN (Profenal) 1 gtt qid (solution 1.0%).

Antiseptics

BENZALKONIUM CHLORIDE (aqueous zephiran)

CHLORHEXIDINE GLUCONATE (Hibiclens) 4% solution

POVIDONE-ETHYL ALCOHOL SOLUTION

POVIDONE-IODINE SOLUTION Lowers conjunctival bacterial counts preoperatively and is effective for ophthalmia neonatorum prophylaxis. Lowest risk of conjunctival and corneal toxicity of all the antiseptics.

SILVER NITRATE 1% solution used for ophthalmia neonatorum prophylaxis (however, it is not active against Chlamydia). May cause local argyrosis (black deposits in the conjunctiva).

Antiviral Agents

ACYCLOVIR (Zovirax) For HSV, use 200Ð400 mg PO 5x/day for 7 to 10 days, or HZV 600Ð800 mg 5x/day for 10 days; use IV if immunosuppressed. All current antivirals are virostatic.

Synthetic guanosine analogue that is tri-phosphorylated by thymidine kinase (TK) to acyclovir triphosphate. The triphosphate accumulates in infected cells and competes with doxyguanosine triphosphate for viral DNA polymerase and terminates replication after incorporated into DNA.

200 greater afÞnity for viral thymidine kinase (TK) than mammalian

cell TK, thus low toxicity. Activity greatest for HSV-1 > HSV- 2 > HZV > EBV > CMV.

Most viral resistance is from alteration of TK gene.

CIDOFOVIR Nucleotide analogue inhibits viral DNA polymerase, used for CMV infection; does not require viral activation; long intracellular half-life. May cause profound hypotony (CB destruction) and severe uveitis (14% of intravitreal usage).

FAMICICLOVIR (Famvir) 500 mg PO every 8 hours to treat HZV and genital herpes, typically treated for 7 days.

FOMIVIRSEN (Vitravene) Exonuclease used as intravitreal injection for CMV retinitis.

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