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:

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

Each mL of EMADINE contains: Active: 0.884 mg emedastine difumarate equivalent to 0.5 mg emedastine. Preservative: benzalkonium chloride 0.01%. Inactives: tromethamine; sodium chloride; hydroxypropyl methylcellulose; 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.

Last updated on RxList: 11/7/2008

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

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

EMADINE (emedastine difumarate ophthalmic solution) 0.05% is supplied as follows: 5 mL in opaque, plastic DROP-TAINER® dispensers.

5 mL: NDC 0065-2000-05

Storage

Store at 4°C - 30°C (39° - 86°F)

Revised: August 2002. Alcon Laboratories, Inc. Fort Worth, Texas 76134. FDA rev date: 5/12/2003

Last updated on RxList: 11/7/2008

In controlled clinical studies of EMADINE 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.

No information provided.

Last updated on RxList: 11/7/2008

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

Information for Patients: 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 ophthalmic solution) 0.05% should not be used to treat contact lens related irritation. The preservative in EMADINE ® (emedastine difumarate ophthalmic solution) 0.05%, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling EMADINE ® (emedastine difumarate ophthalmic solution) 0.05% before they insert their contact lenses.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Emedastine difumarate demonstrated no carcinogenicity effects in lifetime studies in mice and rats at dietary doses more than 80,000 times and more than 26,000 times the maximum recommended ocular human use level of 0.002 mg/kg/day for a 50 kg adult, respectively. Higher dose levels were not tested. Emedastine difumarate was determined to be nonmutagenic in an in vitro bacterial reverse mutation (Ames) test, an in vitro modification of the Ames test, an in vitro mammalian chromosome aberration test, an in vitro mammalian forward mutation test, an in vitro mammalian DNA repair synthesis test, an in vivo mammalian sister chromatid exchange test and an in vivo mouse micronucleus test. There was no evidence of impaired fertility or reproductive capacity in rats at 15,000 times the maximum recommended ocular human use level.

Pregnancy: Pregnancy Category B

Teratology and peri- and post-natal studies have been conducted with emedastine difumarate in rats and rabbits. At 15,000 times the maximum recommended ocular human use level, emedastine difumarate was shown not to be teratogenic in rats and rabbits and no effects on peri/post-natal development were observed in rats. There are, however, no adequate and well controlled studies in pregnant women. Because animal studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

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 is administered to a nursing mother.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 3 years have not been established.

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Last updated on RxList: 11/7/2008

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

EMADINE® is contraindicated in persons with a known hypersensitivity to emedastine difumarate or any of EMADINE's components.

Last updated on RxList: 11/7/2008

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 (<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'-oxo analogs 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

Last updated on RxList: 11/7/2008

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Last updated on RxList: 11/7/2008

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

EMEDASTINE SOLUTION - OPHTHALMIC

(eh-meh-DASS-teen)

COMMON BRAND NAME(S): Emadine

USES: Emedastine is used to relieve redness, itching, and swelling of the eyes from allergies (allergic conjunctivitis). This medication is an antihistamine. It works by blocking certain natural substances (histamines) that cause allergic symptoms.

Do not use this medication to treat redness and irritation from wearing contact lenses.

HOW TO USE: To apply eye drops, wash your hands first. To avoid contamination, do not touch the dropper tip or let it touch your eye or any other surface.

Remove contact lenses before using this medication because it contains a preservative that can be absorbed by them. Wait at least 10 minutes after using this medication before putting the lenses back in. Do not wear your contact lenses if your eyes are red.

Use this medication usually up to 4 times a day or as directed by your doctor. Tilt your head back, look upward and pull down the lower eyelid to make a pouch. Hold the dropper directly over your eye and place one drop into the eye. Look downward and gently close your eyes for 1 to 2 minutes. Place one finger at the corner of your eye (near the nose) and apply gentle pressure. This will prevent the medication from draining out. Try not to blink and do not rub your eye. Repeat these steps for your other eye if so directed.

Do not rinse the dropper. Replace the dropper cap after each use.

If you are using another kind of eye medication (e.g., drops or ointments), wait at least 5 minutes before applying other medications. Use eye drops before eye ointments to allow the eye drops to enter the eye.

Inform your doctor if your condition persists or worsens.

SIDE EFFECTS: This medication may temporarily sting or burn your eyes for a minute or two when applied. Temporary blurred vision, headache, dry eyes, feeling as if something is in your eye, eye discomfort, staining of the eyes, a bad taste in your mouth, weakness, or unusual dreams may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using emedastine, tell your doctor or pharmacist if you are allergic to it; or to preservatives (e.g., benzalkonium chloride); or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history.

Use caution engaging in activities requiring clear vision such as driving or using machinery because your vision may be temporarily blurred or unstable after applying this drug. Limit alcoholic beverages.

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

It is not known if this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop, or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.

Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. This medicine may be harmful if swallowed.

NOTES: Do not share this medication with others.

Consult your doctor for additional ways to minimize and relieve your symptoms (e.g., avoiding irritants that trigger allergies, using cold compresses and lubricating eye drops).

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store between 39-86 degrees F (4-30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets. Discard the solution if it changes color.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.