Emadine Information
Emadine (Emedastine difumarate) Description
Emadine (Emedastine difumarate) ® (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:
1H-benzimidazole,1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl),(E)-2-butenedioate (1:2)
Emadine (Emedastine difumarate) Clinical Pharmacology
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 (
Emadine (Emedastine difumarate) Indications And Usage
Emadine (Emedastine difumarate) ® (emedastine difumarate ophthalmic solution) 0.05% is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis.
Emadine (Emedastine difumarate) Contraindications
Emadine (Emedastine difumarate) ® (emedastine difumarate ophthalmic solution) is contraindicated in persons with a known hypersensitivity to emedastine difumarate or any of its components.
Emadine (Emedastine difumarate) Warnings
FOR TOPICAL OPHTHALMIC USE ONLY - NOT FOR INJECTION OR ORAL USE.
Emadine (Emedastine difumarate) Precautions
To prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep the bottle tightly closed when not in use. Do not use if the solution has become discolored.
Patients should be advised not to wear a contact lens if their eye is red. Emadine (Emedastine difumarate) ® (emedastine difumarate ophthalmic solution) 0.05% should not be used to treat contact lens related irritation. The preservative in Emadine (Emedastine difumarate) ® (emedastine difumarate ophthalmic solution) 0.05%, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and , should be instructed to wait at least ten minutes after instilling Emadine (Emedastine difumarate) ® (emedastine difumarate ophthalmic solution) 0.05% before they insert their contact lenses.
Emadine (Emedastine difumarate) Nursing Mothers:
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) ® (emedastine difumarate ophthalmic solution) 0.05% is administered to a nursing mother.
Emadine (Emedastine difumarate) Adverse Reactions
In controlled clinical studies of Emadine (Emedastine difumarate) ® (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.
Emadine (Emedastine difumarate) Overdosage
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.
Emadine (Emedastine difumarate) Dosage And Administration
The recommended dose is one drop in the affected eye up to four times daily.
Emadine (Emedastine difumarate) How Supplied
Emadine (Emedastine difumarate) ® (emedastine difumarate ophthalmic solution) 0.05% is supplied as follows:
5 mL in opaque, plastic DROP-TAINER® dispenser.
5 mL: NDC 0065-0325-05
U.S. Patents Nos. 5,441,958.
Revised: May 2009
ALCON LABORATORIES, INC.
6201 South Freeway
Fort Worth, Texas 76134 USA
1-800-757-9195
[email protected]
Printed in USA
©2002, 2003, 2009 Alcon, Inc.
Emadine (Emedastine difumarate) Principle Display Panel
NDC 0065-0325-05
Alcon®
Emadine (Emedastine difumarate) ®
(emedastine
Difumarate
Ophthalmic
solution) 0.05%
5 mL Sterile
