EMADINE ® (emedastine difumarate ophthalmic solution) 0.05%

EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% is a sterile ophthalmic solution containing emedastine, a relatively selective, H1-receptor antagonist for topical administration to the eyes. Emedastine difumarate is a white, crystalline, water-soluble fine powder with a molecular weight of 534.57. The chemical structure is presented below:

Structural Formula:

Chemical Name:

1H-benzimidazole,1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl),(E)-2-butenedioate (1:2)

Each mL of EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% contains: Active: 0.884 mg emedastine difumarate equivalent to 0.5 mg emedastine. Preservative: benzalkonium chloride 0.01%. Inactives: tromethamine; sodium chloride; hypromellose; hydrochloric acid/sodium hydroxide (adjust pH); and purified water. It has a pH of approximately 7.4 and an osmolality of approximately 300 mOsm/kg.

Emedastine is a relatively selective, histamine H1 antagonist. In vitro examinations of emedastine's affinity for histamine receptors (H1: Ki = 1.3 nM, H2: Ki = 49,067 nM, and H3: Ki = 12,430 nM) demonstrate relative selectivity for the H1-histamine receptor. In vivo studies have shown concentration-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva following topical ocular administration.

Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. Following topical administration in man, emedastine was shown to have low systemic exposure. In a study involving 10 normal volunteers dosed bilaterally twice daily for 15 days with emedastine ophthalmic solution 0.05%, plasma concentrations of the parent compound were generally below the quantitation limit of the assay (less than 0.3 ng/mL).

Samples in which emedastine was quantifiable, ranged from 0.30 to 0.49 ng/mL. The elimination half-life of oral emedastine in plasma is 3-4 hours. Approximately 44% of the oral dose is recovered in the urine over 24 hours with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5’-oxoanalogs of 5- and 6-hydroxyemedastine and the N-oxide are also formed as minor metabolites.

In an environmental study, patients with allergic conjunctivitis were treated with EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% for six weeks. The results demonstrated that EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% provides relief of the signs and symptoms of allergic conjunctivitis. In conjunctival antigen challenge studies, in which subjects were challenged with antigen both initially and up to four hours after dosing, EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% was demonstrated to be significantly more effective than placebo in preventing ocular itching associated with allergic conjunctivitis.

EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis.

EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% is contraindicated in persons with a known hypersensitivity to emedastine difumarate or any of its components.

FOR TOPICAL OPHTHALMIC USE ONLY - NOT FOR INJECTION OR ORAL USE.

Emedastine has been identified in breast milk in rats following oral administration. It is not known whether topical ocular administration could result in sufficient systemic absorption to produce detectable quantities in breast milk. Nevertheless, caution should be exercised when EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% is administered to a nursing mother.

In controlled clinical studies of EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% lasting for 42 days, the most frequent adverse reaction was headache 11%. The following adverse experiences were reported in less than 5% of patients: Abnormal dreams, asthenia, bad taste, blurred vision, burning or stinging, corneal infiltrates, corneal staining, dermatitis, discomfort, dry eye, foreign body sensation, hyperemia, keratitis, pruritus, rhinitis, sinusitis and tearing. Some of these events were similar to the underlying disease being studied.

Somnolence and malaise have been reported following daily oral administration. Oral ingestion of the contents of a 15 mL DROP-TAINER^® dispenser would be equivalent to 7.5 mg. In case of overdosage, treatment is symptomatic and supportive.

The recommended dose is one drop in the affected eye up to four times daily.

EMADINE^® (emedastine difumarate ophthalmic solution) 0.05% is supplied as follows:

5 mL in opaque, plastic DROP-TAINER^® dispenser.

5 mL: NDC 0065-0325-05

STORAGE: Store at 4°C to 30°C (39°F-86°F).

Rx Only

©2002, 2003, 2009, 2018 Novartis

Distributed by:

ALCON LABORATORIES, INC.

Fort Worth, Texas 76134 USA

Alcon^®

a Novartis company

Revised: April 2018

T2018-34

NDC 0065-0325-05

Alcon^®

Emadine^®
(emedastine difumarate ophthalmic solution) 0.05%
 
5 mL

Sterile