Epinepta^® (Drops) Instructions for Use

Marketing Authorization Holder

Sun Pharmaceutical Industries, Ltd. (India)

ATC Code

S01GX10 (Epinastine)

Active Substance

Epinastine (Rec.INN registered by WHO)

Dosage Form

Epinepta®

Eye drops 0.05%: dropper bottle 5 ml

Dosage Form, Packaging, and Composition

Eye drops in the form of a colorless, transparent solution.

Excipients: benzalkonium chloride (50% solution), disodium edetate, sodium chloride, sodium dihydrogen phosphate monohydrate, sodium hydroxide, hydrochloric acid, purified water.

5 ml – dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

An antiallergic drug for topical use in ophthalmology

Pharmacotherapeutic Group

Agents used in ophthalmology; decongestants and antiallergic agents; other antiallergic agents

Pharmacological Action

It is a direct H₁-histamine receptor antagonist for topical use. It is characterized by a high degree of affinity for H₁-histamine receptors, while its binding to H₂-histamine receptors is 400 times weaker.

Epinastine can also bind to α₁ and α₂-adrenergic receptors and serotonin 5-HT₂ receptors. Furthermore, it binds weakly to cholinergic, dopaminergic, and other receptors.

Epinastine does not cross the blood-brain barrier and thus does not cause central nervous system side effects and does not have a sedative effect.

It has an antihistamine effect, exerts a modulating influence on the accumulation of inflammatory cells, and stabilizes mast cells.

In studies of allergen provocation tests in humans, the use of epinastine was accompanied by a weakening of allergic ocular reactions after sensitization of the eyes with an allergen. The duration of the effect was at least 8 hours.

Pharmacokinetics

With topical application, the mean C_max in plasma is 0.042 ng/ml and is reached after 2 hours.

The volume of distribution of epinastine is 417 L. Plasma protein binding is 64%. The clearance of epinastine is 928 ml/min, the terminal T_1/2 is about 8 hours.

Less than 10% of epinastine is metabolized. The majority is excreted by the kidneys unchanged, mainly as a result of active tubular secretion.

Indications

Treatment of the symptoms of seasonal allergic conjunctivitis.

ICD codes

Dosage Regimen

Instill one drop into the affected eye(s)twice daily, once in the morning and once in the evening.

Administer the drops while wearing contact lenses is not recommended; remove lenses prior to instillation and wait at least 10 minutes before reinserting.

Continue treatment for the entire duration of allergen exposure.

Use the medication until symptoms resolve; the maximum recommended treatment duration is 8 weeks.

Do not allow the dropper tip to contact any surface, including the eye, to prevent contamination of the solution.

If using other topical ophthalmic agents, administer them at least 10 minutes apart from Epinepta^® drops.

Adverse Reactions

Nervous system disorders: uncommon – headache.

Eye disorders: common – burning sensation, eye irritation; uncommon – conjunctival/eye hyperemia, eye discharge, dry eye, eye itching, visual impairment, increased lacrimation, eye pain.

Respiratory system disorders: uncommon – asthma, nasal mucosal irritation, rhinitis.

Gastrointestinal system disorders: uncommon – dysgeusia.

Contraindications

Hypersensitivity to epinastine, children under 12 years of age.

Use in Pregnancy and Lactation

Use during pregnancy and breastfeeding is indicated under medical supervision, only in cases where the intended benefit to the mother outweighs the potential risk to the fetus or child.

Pediatric Use

Contraindicated for use in children under 12 years of age.

Special Precautions

Effect on ability to drive vehicles and operate machinery

When using epinastine, short-term blurred vision (a feeling of a “veil” before the eyes) is possible, so until this effect disappears, it is necessary to refrain from driving vehicles and other potentially dangerous machinery.

Drug Interactions

When using several ophthalmic drugs for topical application, the intervals between their use should be at least 10 minutes.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.