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Ophthalmic Drugs for Patients with Allergic Conjunctivitis



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Am Fam Physician. 2000 Nov 1;62(9):2105-2110.

New ophthalmic formulations of ketotifen fumarate, pemirolast potassium and nedocromil sodium have recently received labeling approval from the U.S. Food and Drug Administration for the treatment of adults and children with itchy eyes resulting from allergic conjunctivitis. Pemirolast and nedocromil are mast-cell stabilizers; ketotifen, in addition to this property, also has H1-receptor antagonist activity. Inhaled nedocromil has been available in the United States since 1993. Consultants from the Medical Letter reviewed the effectiveness and safety of new ophthalmic formulations for the treatment of patients with allergic conjunctivitis.

Over-the-counter antihistamine-decongestant combinations for ophthalmic use have a short duration of effectiveness and can cause rebound vasodilation with sustained use. Ophthalmic mast-cell stabilizers (i.e., cromolyn and lodoxamide) and H1-receptor antagonists (i.e., levocabastine and emedastine) have been shown to be effective in the treatment of patients with seasonal allergic conjunctivitis. Like ketotifen, olopatadine is a mast-cell stabilizer and a selective H1-receptor antagonist and has been shown to be useful in the treatment of patients with allergic conjunctivitis. The ophthalmic formulation of ketorolac, a nonsteroidal anti-inflammatory drug, is marketed for the treatment of itching caused by seasonal allergic conjunctivitis, but it can produce irritation on instillation and may be less effective than mast-cell stabilizers or H1-receptor antagonists. Long-term use of ophthalmic corticosteroids may cause cataracts and increase intraocular pressure, and is indicated only in the treatment of patients with severe allergic reactions (see the accompanying table).

Ophthalmic Drugs For Allergic Conjunctivitis

Drug Concentration (%) Usual daily dosage Cost *

Mast-cell stabilizers

Cromolyn sodium†—generic

4

1 to 2 drops every four to six hours

$18.77

Crolom

20.79

Opticrom

26.46

Lodoxamide tromethamine

0.1

1 to 2 drops four times daily

19.00

Alomide†

Nedocromil sodium

2

1 to 2 drops twice daily

30.10

Alocril

Pemirolast potassium

0.1

1 to 2 drops four times daily

18.67‡

Alamast

H1-receptor antagonists

Emedastine

0.05

1 drop four times daily

28.92

Emadine

Levocabastine hydrochloride

0.05

1 drop four times daily

22.78

Livostin

Mast-cell stabilizers andH1-receptor antagonists

Ketotifen fumarate

0.025

1 drop every eight to 12 hours

15.05

Zaditor

Olopatadine hydrochloride

0.1

1 drop twice daily

18.53

Patanol

Nonsteroidal anti-inflammatory drugs

Ketorolac tromethamine

0.5

1 drop four times daily

43.88

Acular


*—Cost to the pharmacist for two weeks' treatment of both eyes, based on one drop per dose, according to the average wholesale price (AWP) listings in Drug Topics Red Book 2000, April Update, and First DataBank PriceAlert, April 15, 2000.

—Labeling approved by the U.S. Food and Drug Administration for the treatment of patients with vernal keratoconjunctivitis, vernal conjunctivitis and vernal keratitis.

—AWP according to the manufacturer.

Adapted with permission from the Medical Letter Consultants. New drugs for allergic conjunctivitis. Med Lett Drugs Ther 2000;42:39.

Ophthalmic Drugs For Allergic Conjunctivitis

View Table

Ophthalmic Drugs For Allergic Conjunctivitis

Drug Concentration (%) Usual daily dosage Cost *

Mast-cell stabilizers

Cromolyn sodium†—generic

4

1 to 2 drops every four to six hours

$18.77

Crolom

20.79

Opticrom

26.46

Lodoxamide tromethamine

0.1

1 to 2 drops four times daily

19.00

Alomide†

Nedocromil sodium

2

1 to 2 drops twice daily

30.10

Alocril

Pemirolast potassium

0.1

1 to 2 drops four times daily

18.67‡

Alamast

H1-receptor antagonists

Emedastine

0.05

1 drop four times daily

28.92

Emadine

Levocabastine hydrochloride

0.05

1 drop four times daily

22.78

Livostin

Mast-cell stabilizers andH1-receptor antagonists

Ketotifen fumarate

0.025

1 drop every eight to 12 hours

15.05

Zaditor

Olopatadine hydrochloride

0.1

1 drop twice daily

18.53

Patanol

Nonsteroidal anti-inflammatory drugs

Ketorolac tromethamine

0.5

1 drop four times daily

43.88

Acular


*—Cost to the pharmacist for two weeks' treatment of both eyes, based on one drop per dose, according to the average wholesale price (AWP) listings in Drug Topics Red Book 2000, April Update, and First DataBank PriceAlert, April 15, 2000.

—Labeling approved by the U.S. Food and Drug Administration for the treatment of patients with vernal keratoconjunctivitis, vernal conjunctivitis and vernal keratitis.

—AWP according to the manufacturer.

Adapted with permission from the Medical Letter Consultants. New drugs for allergic conjunctivitis. Med Lett Drugs Ther 2000;42:39.

Neither ketotifen, pemirolast or nedocromil result in significant absorption or accumulation of drug. Results of one four-week clinical trial revealed that ketotifen 0.05 percent was as effective as cromolyn 2 percent in decreasing the signs and symptoms associated with allergic conjunctivitis. Evidence from another clinical trial revealed that pemirolast 0.1 percent used four times daily was more effective (during the second 30 days of treatment) than placebo in preventing signs and symptoms of allergic conjunctivitis. Evidence from another trial involving patients with allergic conjunctivitis who took pemirolast 0.1 percent for four months revealed that pemirolast was more effective than placebo after six to eight weeks of treatment. Results from several double-blind studies showed that nedocromil 2 percent was more effective than placebo in the treatment of itching associated with allergic conjunctivitis. As with other mast-cell stabilizers, response to treatment with pemirolast or nedocromil may require weeks of treatment, although some patients detect a reduction of symptoms in a few days.

Ocular irritation, burning or stinging may occur with the use of these drugs. Conjunctival injection, headache and rhinitis were common side effects associated with the use of ketotifen, although allergic reactions, stinging, discharge, eye pain and photophobia occurred in less than 5 percent of patients. With pemirolast, the most common adverse side effects were headache, rhinitis and mild cold or flu symptoms. Headache was the most common adverse side effect associated with the use of nedocromil, but unpleasant taste and nasal congestion also occurred.

The consultants conclude that ketotifen, pemirolast and nedocromil appear to be effective in the treatment of itching caused by allergic conjunctivitis. Whether these drugs are more effective than the existing drugs in their class has not been determined.

Medical Letter Consultants. New drugs for allergic conjunctivitis. Med Lett Drugs Ther. May 1, 2000;42:39–40.



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