Composition:
1 ml of the drug contains: active substance:
dexamethasone sodium phosphate 1.32 mg (equivalent to dexamethasone 1.0 mg);
excipients: benzalkonium chloride 40.0 μg,
boric acid 15.0 mg, sodium tetraborate 0.6 mg,
disodium edetate 0.5 mg,
water for injection up to 1 ml.
Pharmacodynamics:
Synthetic fluorinated corticosteroids for local 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. Stabilizes lysosomal enzymes of leukocyte membranes and inhibits the release of enzymes.
It inhibits the synthesis of kinins, mitosis and the migration of leukocytes. 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 When applied topically, systemic absorption is low. After instillation into the conjunctival sac, it penetrates well into the corneal epithelium and the 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. T1 / 2 is on average 3.6 ± 0.9 hours.
Side effects:
After instillation of eye drops of Oftan® Dexamethasone, a rapidly passing burning sensation, allergic reactions can occur.
Long-term use (more than 3 weeks) of dexamethasone can cause secondary glaucoma and steroid cataracts, as well as ulceration, turbidity, thinning or perforation of the cornea; in rare cases, dexamethasone can contribute to the spread of herpetic and bacterial infections. Oftan® Dexamethasone contains a preservative benzalkonium chloride, which can cause eye irritation. In case of side effects, contact your doctor as soon as possible.
Special conditions:
Oftan® Dexamethasone contains a preservative benzalkonium chloride, which can be absorbed by soft contact lenses and cause a change in their color and have an adverse effect on eye tissue. If you need to use contact lenses during treatment with Oftan®
Dexamethasone, they should be removed before using the drug and, if necessary, should be installed no earlier than 15 minutes after instillation. If treatment with the drug lasts more than 2 weeks, it is necessary to regularly monitor intraocular pressure and the condition of the cornea. Corticosteroid therapy may mask ongoing bacterial or fungal infections. In the presence of infection, the use of drops should be combined with appropriate antimicrobial therapy.
Influence on the ability to drive vehicles and control mechanisms. Due to possible lacrimation after instillation, the drug is not recommended to be used immediately before driving vehicles or operating mechanical equipment.
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 damage to the cornea of various etiologies (chemical, physical or immune mechanisms) after complete epithelialization of the cornea; - inflammation of the posterior segment of the eye (choroiditis, chorioretinitis); - edema, inflammation (including in the postoperative period); - sympathetic ophthalmia.
Allergic eye diseases: - allergic conjunctivitis or keratoconjunctivitis. Prevention and treatment of inflammatory phenomena in the postoperative and post-traumatic period.
Contraindications:
keratitis associated with herpes simplex, chickenpox and other viral diseases of the cornea and conjunctiva; - eye tuberculosis;
- mycobacterial infections of the eyes;
- fungal diseases of the eyes;
- acute purulent eye diseases;
- damage to the corneal epithelium (including the condition after removal of a foreign body of the cornea);
- corneal epithelialopathy; - increased intraocular pressure; - glaucoma; - age up to 18 years (due to the lack of data on the effectiveness and safety of the drug in children and adolescents under 18 years of age);
- Hypersensitivity to the components of the drug. Pregnancy and lactation:
To date, clinical trials regarding the use of Oftan® Dexamethasone during pregnancy, no lactation. Oftan® Dexamethasone can be used during pregnancy and during breastfeeding only as prescribed by the attending physician, unless the expected therapeutic effect justifies the potential risk to the fetus and to the baby.
Duration of therapy: no more than 7-10 days.
Drug Interactions:
Interaction with other drugs is mainly due to the participation of CYP3A4 isoenzyme in the excretion of dexamethasone. Dexamethasone induces the CYP3A4 isoenzyme, thus reducing the effectiveness of calcium channel blockers, quinidine and erythromycin. In the usual regimen of topical administration, the dose of the drug is insufficient to induce or saturate the liver enzymes. With prolonged use with iodoxuridine, intensification of destructive processes in the corneal epithelium is possible.
Dosage:
In acute conditions, 1-2 drops are prescribed in the conjunctival sac every 1-2 hours. After reducing inflammation, the drug is instilled 1-2 drops in the conjunctival sac 3-5 times / 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.
Overdose:
An overdose with topical administration of Oftan® Dexamethasone eye drops is unlikely. Symptoms: local irritation is possible. There is no specific antidote. The drug should be discontinued and symptomatic therapy prescribed.
