Atopic Keratoconjunctivitis Medication

The goals of pharmacotherapy in the treatment of atopic keratoconjunctivitis are to reduce morbidity and to prevent complications, such as significant keratopathy, conjunctival fornix foreshortening, and corneal scarring or thinning requiring penetrating keratoplasty.

Mast cell stabilizers and antihistamines are the mainstays of prophylactic therapy. Antihistamines, steroids, and other immunosuppressives are used for immediate control of symptoms.

When medically treating patients with steroids or cyclosporine, a regular interval survey for drug-related adverse effects and complications is indicated.

For additional information, see PDR.net.

Class Summary

Topical mast cell stabilizers inhibit degranulation of sensitized mast cells upon exposure to specific antigens.

Cromolyn sodium 4%

Cromolyn inhibits the release of histamine and SRS-A (slow-releasing substance of anaphylaxis) from mast cells but has no intrinsic anti-inflammatory, antihistamine, or vasoconstrictive effects.

Lodoxamide tromethamine 0.1% (Alomide)

Lodoxamide stabilizes mast cells and inhibits increased vascular permeability, which is associated with immunoglobulin E (IgE) and antigen-mediated reactions. Alomide has been reported to prevent calcium influx into mast cells upon antigen stimulation without intrinsic anti-inflammatory, antihistamine, or vasoconstrictive effects.

Nedocromil sodium 2% (Alocril)

Nedocromil interferes with mast cell degranulation, specifically with the release of leukotrienes and platelet activating factor.

Class Summary

Topical antihistamine agents act by competitive inhibition of histamine at the H1 receptor. These medications are used for prophylaxis and symptomatic relief.

Olopatadine hydrochloride 0.1% (Patanol, Pataday)

Olopatadine inhibits histamine release through both selective H1 histamine receptor antagonism and less specific mast cell stabilization.

Ketotifen fumarate 0.025% (Zaditor, Alaway, Claritin Eye, Zyrtec Itchy Eye)

Ketotifen is a selective H1 histamine receptor antagonist and mast cell stabilizer that acts by inhibiting the release of mediators from cells involved in hypersensitivity reactions.

Azelastine hydrochloride 0.05% (Optivar)

Azelastine is both an antihistamine and mast cell stabilizer. The usual dose is 1 drop in the affected eye(s) twice daily.

Epinastine hydrochloride 0.05% (Elestat)

Epinastine is another H1 antihistamine and mast cell stabilizer. As with azelastine, the usual dose is 1 drop in the affected eye(s) twice daily.

Class Summary

Corticosteroids have anti-inflammatory properties and cause profound and varied metabolic effects. These agents modify the body's immune response to diverse stimuli.

Prednisolone acetate 1%, 0.12% (Pred Forte, Pred Mild)

On the basis of weight, prednisolone has 3-5 times the anti-inflammatory potency of hydrocortisone. Glucocorticoids inhibit edema, fibrin deposition, capillary dilatation and proliferation, phagocytic migration of the acute inflammatory response, deposition of collagen, and scar formation.

Fluorometholone 0.1%, 0.25% (FML, FML Forte)

Fluorometholone inhibits edema, fibrin deposition, capillary dilatation, and phagocytic migration of acute inflammatory response and capillary proliferation, collagen deposition, and scar formation. Used topically, this agent can elevate intraocular pressure (IOP) and cause steroid-response glaucoma. However, in clinical studies of documented steroid responders, fluorometholone demonstrated a significantly longer average time to produce a rise in IOP than dexamethasone phosphate. In a small percentage of individuals, a significant rise in IOP occurred within 1 week. The ultimate magnitude of the rise was equivalent.

Loteprednol etabonate 0.5%, 0.2% (Lotemax, Alrex)

Loteprednol is structurally similar to other corticosteroids, but the number 20 position ketone group is absent. This agent is a highly lipid soluble, which enhances cell penetration, and undergoes a predictable transformation to an inactive carboxylic acid metabolite.

Loteprednol was shown to be less effective than prednisolone acetate 1% in two 28-day controlled clinical studies in acute anterior uveitis; 72% of patients treated with Lotemax experienced resolution of anterior chamber cells compared with 87% of patients treated with prednisolone acetate 1%. The incidence of patients with clinically significant increases in IOP (>10 mm Hg) was 1% with Lotemax and 6% with prednisolone acetate 1%.

Class Summary

Immunosuppressant agents are used as adjunctive or alternative treatment in situations in which steroid use is ineffective or requires minimization.

Cyclosporine (Restasis)

The exact mechanism of the immunosuppressive activity of cyclosporine is unknown, but preferential and reversible inhibition of T lymphocytes in the G0 or G1 phase of the cell cycle has been suggested.