Oftan Dexamethasone, eye drops 1 mg/ml 5 ml

Pharmacological action Pharmacotherapeutic group: Glucocorticosteroids for topical use

ATC code S01BAO1

Pharmacological action

Pharmacodynamics

Synthetic fluorinated glucocorticosteroid. It has a strong anti-inflammatory and anti-allergic effect.

Interacting with specific protein receptor in the target tissues it regulates the expression of corticoid-dependent genes and thus affects protein synthesis. Stabilizes lysosomal membrane enzymes of leukocytes; inhibits kininin synthesis, mitosis and leukocyte migration; inhibits antibody synthesis and impairs antigen recognition. All these effects are involved in suppressing the inflammatory response in tissues in response to mechanical, chemical or immune damage. Duration of anti-inflammatory effect after 1 drop of the solution is from 4 to 8 hours.

Pharmacokinetics

When applied topically systemic absorption is low. After injection into the conjunctival sac penetrates well into the corneal epithelium and conjunctiva; therapeutic concentrations are achieved in the aqueous humor of the eye; in inflammation or mucosal damage penetration rate increases.

About 60-70% of dexamethasone entering the systemic bloodstream is bound to plasma proteins. It is metabolized in the liver under the action of cytochrome P450 containing enzymes (CYP3A4); metabolites are excreted through the intestine. Plasma half-life (t1/2) averages 3.6 ± 0.9 hours.

Indications

Acute and chronic inflammatory processes:

– non-purulent forms of conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium 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 epithelization of the cornea;

– inflammation of the posterior segment of the eye (choroiditis, chorioretinitis);

– sympathetic ophthalmia.

Allergic eye diseases: allergic conjunctivitis or keratoconjunctivitis.

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

Pharmacological effect

Pharmacological action
Pharmacotherapeutic group: Glucocorticoid for local use

ATX code S01BAO1

Pharmacological action

Pharmacodynamics

Synthetic fluorinated glucocorticosteroid. Has a pronounced anti-inflammatory and anti-allergic effect.

By interacting with a specific protein receptor in target tissues, it regulates the expression of corticoid-dependent genes and thus affects protein synthesis. Stabilizes lysosomal enzymes of leukocyte membranes; inhibits the synthesis of kinins, mitosis and migration of leukocytes; suppresses antibody synthesis and disrupts antigen recognition. All of these effects 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 solution is from 4 to 8 hours.

Pharmacokinetics

When applied topically, 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; when the mucous membrane is inflamed or damaged, the penetration rate increases.

About 60-70% of dexamethasone entering the systemic circulation is bound to plasma proteins. Metabolized in the liver under the influence of cytochrome P450 containing enzymes (CYP3A4); metabolites are excreted through the intestines. The plasma half-life (t1/2) averages 3.6 ± 0.9 hours.

Special instructions

If it is necessary to use contact lenses during treatment with Oftan Dexamethasone, they should be removed before using the drug and, if necessary, installed no earlier than 15 minutes after installation, because Oftan Dexamethasone contains the preservative benzalkonium chloride, which can be absorbed by soft contact lenses and cause discoloration and adverse effects on eye tissue.

If treatment is longer 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. If infection is present, the use of drops should be combined with appropriate antimicrobial therapy.

Impact on the ability to drive vehicles and operate machinery

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

Active ingredient

Dexamethasone

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 mcg,

boric acid 15.0 mg,

sodium tetraborate 600.0 mcg,

disodium edetate 500.0 mcg,

water for injections up to 1 ml.

Pregnancy

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 child.

Duration of therapy is no more than 7-10 days.

Contraindications

Keratitis associated with herpes simplex, chickenpox and other viral diseases of the cornea and conjunctiva.
Tuberculosis of the eye.
Mycobacterial eye infections.
Fungal eye infections.
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 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.

Side Effects

After instillation, a quickly passing burning sensation and allergic reactions are possible.

With long-term use it is possible

development of secondary glaucoma and steroid cataracts, as well as ulceration, opacification, thinning and/or perforation of the cornea;
rarely – the spread of bacterial or herpetic infections.

The drug contains the preservative benzalkonium chloride, which can cause eye irritation.

Interaction

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

Long-term use with iodoxuridine may increase destructive processes in the corneal epithelium.

Overdose

An overdose with topical use of Oftan Dexamethasone eye drops is unlikely.

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

Storage conditions

The drug should be stored out of the reach of children at a temperature of 2° to 8°C.

Shelf life

2 years

Manufacturer

Santen JSC, Finland