Dexamethasone, eye drops 0.1% 10 ml

Dexamethasone is a glucocorticoid drug for topical use in ophthalmology. It has anti-inflammatory, anti-allergic and anti-exudative effects.

In the target tissues it interacts with specific protein receptors, regulates the expression of corticoid-dependent genes and thus affects protein synthesis. It decreases formation, release and activity of inflammatory mediators (including histamine, kininin, prostaglandins, lysosomal enzymes).

Inhibits cell migration to the site of inflammation. It reduces vasodilatation and increased vascular permeability in the inflammation area. It stabilizes the lysosomal enzymes of the leukocyte membranes. Inhibits antibody synthesis and disrupts antigen recognition.

Inhibits the release of interleukin 1 and interleukin 2, γ-interferon from lymphocytes and macrophages. Induces the formation of lipocortin, inhibits the release of inflammatory mediators by eosinophils and stabilizes the membranes of mast cells. All these effects are involved in suppressing the inflammatory reaction in tissues in response to mechanical, chemical or immune damage.

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

Pharmacokinetics

After injection into the conjunctival sac, dexamethasone penetrates well into the corneal epithelium and conjunctiva, with therapeutic concentrations achieved in the aqueous humor of the eye. When the mucous membrane is inflamed or damaged, the rate of penetration increases.

The systemic absorption of the drug is minimal. About 60-70% of dexamethasone entering the systemic bloodstream is bound to plasma proteins.

Dexamethasone is metabolized in the liver under the action of cytochrome-containing enzymes. Metabolites are excreted with the feces. T_1/2 averages 3 h.

Indications

Acute and chronic allergic and inflammatory eye diseases (incl. Conjunctivitis, scleritis, deep keratitis without epithelium damage, iritis, iridocyclitis, choriocytitis, chorioretinitis, optic neuritis), uveitis, episcleritis, blepharitis, scleritis, prevention and treatment of inflammatory processes in postoperative and post-traumatic period, restoration of corneal transparency and decrease of neovascularization after keratitis and burns.

Active ingredient

Composition

The active ingredient:

dexamethasone sodium phosphate 1 mg;

Excipients:

polysorbate 80,

hypromellose (hydroxypropyl methylcellulose 4000),

dodecahydrate phosphate dodecahydrate,

p> citric acid monohydrate,

sodium chloride,

dietate dihydrate,

benzalkonium chloride,

purified water.

How to take, the dosage

In the conjunctival sac.
In acute inflammatory processes

In case of chronic inflammatory processes

The maximum duration of the drug is 6 weeks.

In case of allergic eye disease

In case of damage to the eyeball due to trauma or during surgical interventions after anti-glaucoma filtering surgery, the drug is used on the day of surgery or the next day.

After cataract extraction surgery, strabismus surgery, retinal detachment, and after trauma, the drug is used from day 8. Depending on the degree of inflammatory symptoms the drug should be applied in 1-2 drops 2-4 times a day for 2-4 weeks.

When treating allergic and inflammatory conditions for children aged 6 to 12 years old 1 drop 2-3 times daily for 7-10 days. If necessary, the treatment is continued after a fluorescein test on the 10th day (to check the integrity of the corneal epithelium).

Interaction

Long-term use of dexamethasone with idoxuridine may increase destructive processes in the corneal epithelium.

Dexamethasone may increase the effect of barbiturates.

The co-administration of phenytoin with dexamethasone decreases the concentration of the latter.

Warfarin in combination with dexamethasone increases the risk of bleeding.

In the usual regimen of topical administration, the dose is insufficient to cause induction or saturation of hepatic enzymes.

Concomitant use of dexamethasone with diuretics (especially thiazide and carboanhydrase inhibitors) and amphotericin B may increase potassium excretion and increase the risk of heart failure.

The concomitant use of dexamethasone with cardiac glycosides impairs their tolerability and increases the risk of ventricular extrasystole (due to hypokalemia).

The simultaneous use of dexamethasone with ethanol and NSAIDs increases the risk of gastrointestinal erosive ulcers.

Estrogens and oral estrogen-containing contraceptives decrease clearance of dexamethasone, which may be accompanied by increased potency.

The co-administration of antiarrhythmic drugs with dexamethasone may decrease the effect of the latter.

Special Instructions

It is intended for topical use only.

The drug should be shaken before direct use.

If no improvement is seen after 3 to 4 days of treatment, additional local or systemic treatment should be prescribed.

The drug should not be used while wearing soft contact lenses. The drug contains an antimicrobial preservative benzalkonium chloride which may be adsorbed by soft contact lenses. The lenses should be removed before the drug is applied and inserted not earlier than 15 min after dosing.

If the drug is used in combination with other ophthalmic drops, it is necessary to maintain an interval of at least 15 min between injections.

The treatment with the drug may mask the picture of bacterial or fungal infection, therefore when treating infectious eye disease the drug should be combined with adequate antimicrobial therapy.

Dexamethasone can cause false positive doping tests.

Impact on driving and operating machinery

With regard to the possibility of tear production after injection, the drug should not be used immediately before driving or operating machinery. Within 30 minutes after instillation of the drug it is necessary to refrain from activities requiring increased attention.

Contraindications

Side effects

In short-term therapy: nausea, vomiting, bradycardia, arrhythmias, ulceration of gastrointestinal mucosa, reduced immunity.
In long-term use: Icenko-Cushing’s syndrome, hyperglycemia, pancreatitis, myocardial dystrophy, headache, seizures, psychosis.

Local reactions: a burning sensation that quickly disappears immediately after injection of the drug is possible. If the drug is used for a long time the intraocular pressure may increase (therefore if the drugs containing corticosteriods are used for more than 10 days the intraocular pressure should be measured regularly).
In case of use for more than 3 months a posterior capsular cataract may develop. Slow regeneration processes may occur.

Overdose

Symptoms: local manifestations are possible. There is no specific antidote. The drug should be discontinued and symptomatic therapy should be prescribed.

Long-term use of the drug or use in high doses may increase systemic absorption of dexamethasone, and ocular hypertension and some corneal or lens disorders may develop.

Pregnancy use

The use of the drug is contraindicated in pregnancy during lactation (breastfeeding).

Pediatric use

Contraindication: children under 6 years of age.

Similarities