Oftan^® Dexamethason (Drops) Instructions for Use

Marketing Authorization Holder

Santen, Oy (Finland)

Manufactured By

Nextpharma, Oy (Finland)

Labeled By

Manufacturing Packaging Farmaca, MPF B.V. (Netherlands)

Quality Control Release

SANTEN, OY (Finland)

Contact Information

SANTEN LLC (Russia)

ATC Code

S01BA01 (Dexamethasone)

Active Substance

Dexamethasone (Rec.INN WHO registered)

Dosage Form

Oftan® Dexamethasone

Eye drops 1 mg/1 ml: dropper bottle 5 ml

Dosage Form, Packaging, and Composition

Eye drops as a transparent, colorless solution.

Excipients : benzalkonium chloride – 40 mg, boric acid – 15 mg, sodium tetraborate – 0.6 mg, disodium edetate – 0.5 mg, purified water – up to 1 ml.

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

Clinical-Pharmacological Group

Topical corticosteroids for ophthalmology

Pharmacotherapeutic Group

Agents used in ophthalmology; anti-inflammatory agents; corticosteroids

Pharmacological Action

Synthetic fluorinated glucocorticosteroid for topical use in ophthalmology. The drug has a pronounced anti-inflammatory and anti-allergic effect.

Dexamethasone interacts with specific protein receptors in target tissues, thereby regulating the expression of corticosteroid-dependent genes and subsequently affecting protein synthesis. It stabilizes the lysosomal membranes of leukocytes. It inhibits the synthesis of kinins, mitosis, and leukocyte migration. It inhibits antibody synthesis and disrupts antigen recognition. All these mechanisms are involved in suppressing the inflammatory response in tissues in response to mechanical, chemical, or immune damage.

The duration of the anti-inflammatory effect after instillation of 1 drop of the drug is 4-8 hours.

Pharmacokinetics

Absorption

With topical application, systemic absorption is low. After instillation into the conjunctival sac, it penetrates well into the corneal epithelium and conjunctiva. At the same time, therapeutic concentrations are achieved in the aqueous humor of the eye; with inflammation or damage to the mucous membrane, the penetration rate increases.

Distribution and Metabolism

About 60-70% of dexamethasone entering the systemic circulation binds to plasma proteins. It is metabolized in the liver by the action of the CYP3A4 isoenzyme.

Excretion

Metabolites are excreted through the intestines. T_1/2 averages 3.6±0.9 hours.

Indications

Acute and chronic inflammatory processes

• Non-purulent forms of conjunctivitis, keratitis, keratoconjunctivitis, and blepharitis;
• Scleritis and episcleritis;
• Iritis, iridocyclitis, and other uveitis of various origins;
• Superficial corneal lesions of various etiologies (chemical, physical, or immune mechanisms) after complete corneal epithelialization;
• Inflammation of the posterior segment of the eye (chorioretinitis);
• Sympathetic ophthalmia.

Allergic eye diseases

• Allergic conjunctivitis or keratoconjunctivitis.

Prevention and treatment of inflammatory phenomena in the postoperative and post-traumatic period.

ICD codes

Dosage Regimen

For acute conditions, 1-2 drops are instilled into the conjunctival sac every 1-2 hours.

After the inflammation subsides, the drug is instilled 1-2 drops into the conjunctival sac 3-5 times/day.

The duration of treatment should not exceed 2-3 weeks.

The decision on the duration of treatment is based on objective data, including the effectiveness of the drug, the severity of clinical symptoms, and the possible risk of side effects.

Adverse Reactions

From the organ of vision, a transient burning sensation and allergic reactions are possible after instillation. With prolonged use of dexamethasone (more than 3 weeks), the development of secondary glaucoma and steroid cataract, as well as ulceration, clouding, thinning, and/or perforation of the cornea, is possible; rarely – the spread of bacterial or herpetic infections. The drug contains the preservative benzalkonium chloride, which can cause eye irritation.

If side effects occur, the patient should contact the attending physician as soon as possible.

Contraindications

• Keratitis associated with herpes simplex, chickenpox, and other viral diseases of the cornea and conjunctiva;
• Ocular tuberculosis;
• Mycobacterial eye infections;
• Fungal eye diseases;
• Acute purulent eye diseases;
• Damage to the corneal epithelium (including the condition after removal of a corneal foreign body);
• Corneal epitheliopathy;
• Increased intraocular pressure;
• Glaucoma;
• Age under 18 years (due to the lack of data on the efficacy and safety of the drug in children and adolescents under 18 years of age);
• Hypersensitivity to the components of the drug.

Use in Pregnancy and Lactation

To date, there are no clinical trial data regarding the use of Oftan^® Dexamethasone during pregnancy and lactation. Oftan^® Dexamethasone can be used during pregnancy and breastfeeding only as prescribed by the attending physician, if the expected therapeutic effect justifies the potential risk to the fetus and the child. The duration of therapy is no more than 7-10 days.

Pediatric Use

Contraindicated under the age of 18 years (due to the lack of data on the efficacy and safety of the drug in children and adolescents under 18 years of age).

Special Precautions

Oftan^® Dexamethasone contains the preservative benzalkonium chloride, which can be absorbed by soft contact lenses and cause discoloration and have an adverse effect on eye tissues. If it is necessary to use contact lenses during treatment with Oftan^® Dexamethasone, they should be removed before using the drug and, if necessary, inserted no earlier than 15 minutes after instillation.

If treatment with the drug continues for more than 2 weeks, it is necessary to regularly monitor intraocular pressure and the condition of the cornea.

Corticosteroid therapy may mask an ongoing bacterial or fungal infection. In the presence of an infection, the use of drops should be combined with appropriate antimicrobial therapy.

Effect on the ability to drive vehicles and operate machinery

Due to possible lacrimation after instillation, the drug is not recommended to be used immediately before driving vehicles or operating mechanical equipment.

Overdose

Overdose with topical application of Oftan^® Dexamethasone eye drops is unlikely.

Symptoms: local irritation is possible.

Treatment: there is no specific antidote. The drug should be discontinued and symptomatic therapy prescribed.

Drug Interactions

Interaction with other drugs is mainly due to the participation of the CYP3A4 isoenzyme in the elimination of dexamethasone. Dexamethasone induces the CYP3A4 isoenzyme, thus reducing the effectiveness of calcium channel blockers, quinidine, and erythromycin. With the usual regimen of topical application, the dose of the drug is insufficient to cause induction or saturation of liver enzymes.

With prolonged use with idoxuridine, an increase in destructive processes in the corneal epithelium is possible.

Storage Conditions

The drug should be stored out of the reach of children at a temperature from 2°C (35.6°F) to 8°C (46.4°F).

Shelf Life

The shelf life is 2 years.

After opening the dropper bottle, the shelf life is 1 month.

Dispensing Status

The drug is dispensed by prescription.

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.