Composition, form of production and packaging
Eye drops 0.1% in the form of a suspension of white color; possibly the presence of a precipitate, which is rapidly resuspended with slight agitation.
1 ml
dexamethasone 1 mg
Excipients: polysorbate 80, hypromellose (hydroxypropylmethylcellulose 4000), disodium phosphate dodecahydrate, citric acid monohydrate, sodium chloride, disodium edetate dihydrate, benzalkonium chloride, purified water.
10 ml - a bottle-droppers polymer (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
GCS for topical application in ophthalmology. Has a pronounced anti-inflammatory, anti-allergic and anti-exsudative action.
Interacting with specific protein receptors in target tissues, regulates the expression of corticoid-dependent genes and thus affects protein synthesis. Reduces the formation, release and activity of inflammatory mediators (including histamine, kinin, prostaglandins, lysosomal enzymes).
Suppresses the migration of cells to the site of inflammation. Reduces vasodilation and increased vascular permeability in the focus of inflammation. Stabilizes lysosomal enzymes of leukocyte membranes. Suppresses the synthesis of antibodies and disrupts the recognition of the antigen. It inhibits the release of interleukin 1 and interleukin 2,? -terferon from lymphocytes and macrophages. It induces the formation of lipocortin, inhibits the release of eosinophils by inflammatory mediators and stabilizes the membranes of mast cells. All these effects are involved in suppressing the inflammatory response in tissues in response to mechanical, chemical or immune damage.
The duration of anti-inflammatory action of the drug after instillation of 1 drop of solution is from 4 to 8 hours.
PHARMACOKINETICS
Suction and distribution
After instillation into the conjunctival sac, dexamethasone penetrates well into the corneal epithelium and conjunctiva, and therapeutic concentrations are achieved in the aqueous humor of the eye. With inflammation or damage to the mucous membrane, the penetration rate increases.
Systemic absorption of the drug is minimal. About 60-70% of dexamethasone entering the systemic circulation communicates with plasma proteins.
Metabolism and excretion
Dexamethasone is metabolized in the liver by the action of cytochrome-containing enzymes. Metabolites are excreted with feces. T 1/2 is an average of 3 hours.
INDICATIONS
- conjunctivitis (non-inflammatory and allergic);
- keratitis;
- keratoconjunctivitis (without epithelial damage);
- blepharitis;
- sclerite;
- episcleritis;
- chorioretinitis;
- uveitis;
- Blepharoconjunctivitis;
- optic neuritis;
- sympathetic ophthalmia;
- prevention and treatment of inflammation after surgical interventions and injuries;
- restoration of the transparency of the cornea and reduction of neovascularization after keratitis, burns.
DOSING MODE
Adults with acute inflammatory processes, the drug is instilled into the conjunctival sac by 1-2 drops 4-5 times / day for 2 days; In the future, the drug is used 1-2 drops 3-4 times / day for 4-6 days.
In chronic inflammatory processes, the drug is instilled 2 times / day for 3-6 weeks.
The maximum duration of the drug is 6 weeks.
With allergic eye diseases , the drug is buried in the conjunctival sac 1-2 drops 4-5 times / day for 2 days with a gradual withdrawal within 1-2 weeks.
If the eyeball is damaged as a result of injuries or during surgical interventions after an antiglaucoma filtering operation, the drug is used on the day of the operation or the next day.
After the operation of cataract extraction, surgery for strabismus, retinal detachment, as well as after the injury, the drug is used starting from the 8th day. Depending on the degree of symptoms of inflammation, the drug should be instilled 1-2 drops 2-4 times / day for 2-4 weeks.
Children aged 6 to 12 years in the treatment of allergic and inflammatory conditions are instilled 1 drop 2-3 times / day for 7-10 days. If necessary, the treatment is continued after a fluorescein test is performed on the 10th day (to check the integrity of the corneal epithelium).
SIDE EFFECT
Basically, the drug has good tolerability.
Local reactions: immediately after instillation of the drug, a rapid burning sensation, lacrimation, blurring of vision is possible.
With prolonged use of the drug (more than 2 weeks), it is possible to increase intraocular pressure, glaucoma development with optic nerve damage, decreased visual acuity and loss of visual fields, as well as the formation of posterior subcapsular cataract, thinning and perforation of the cornea; very rarely - the spread of herpetic and bacterial infection.
In patients with hypersensitivity to dexamethasone or benzalkonium, chloride may develop allergic conjunctivitis and blepharitis.
Possible development of pruritus, palpebral or conjunctival erythema.
When corneal ulcers or sclera appear, the drug can slow the healing and promote the development of re-infection.
With prolonged use, an increased risk of developing systemic side effects , characteristic of GCS .
On the part of the endocrine system: a decrease in glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, oppression of adrenal function, Isenko-Cushing syndrome.
On the part of the digestive system: nausea, vomiting, increased or decreased appetite, exacerbation of chronic gastrointestinal diseases.
From the cardiovascular system: arrhythmia, bradycardia, increased blood pressure.
From the side of the central nervous system: increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, headache.
CONTRAINDICATIONS
- viral diseases of the eyes;
- fungal diseases of the eyes;
- Purulent eye diseases (without concomitant antimicrobial therapy);
- trachoma;
- increased intraocular pressure;
- damage to the integrity of the corneal epithelium;
- tuberculosis of the eye;
- children's age till 6 years;
- Pregnancy;
- the period of lactation (breastfeeding);
- Hypersensitivity to the components of the drug.
PREGNANCY AND LACTATION
The use of the drug during pregnancy during lactation (breastfeeding) is contraindicated.
APPLICATION FOR CHILDREN
Contraindication: children under 6 years.
In the treatment of allergic and inflammatory conditions, children older than 6 years are instilled 1 drop 2-3 times / day for 7-10 days. If necessary, the treatment is continued after a fluorescein test is performed on the 10th day (to check the integrity of the corneal epithelium).
SPECIAL INSTRUCTIONS
The drug is intended for topical use only. Do not use for intraocular injection.
Before use, the preparation should be shaken.
If there is no improvement after 3-4 days of treatment, additional local or systemic therapy should be prescribed.
The preparation contains antimicrobial preservative benzalkonium chloride, which can be adsorbed by soft contact lenses. Therefore, you should not use the drug while wearing soft contact lenses. It is necessary to remove the lenses before using the drug and to establish not earlier than 15 minutes after instillation.
When using the drug in combination with other ophthalmic drops, it is necessary to keep the interval between instillations for at least 15 minutes.
Treatment with the drug can mask the picture of a bacterial or fungal infection, so when treating infectious eye diseases the drug should be combined with adequate antimicrobial therapy.
Dexamethasone can lead to a false positive test result for doping.
Impact on the ability to drive vehicles and manage mechanisms
Taking into account the possibility of lacrimation after instillation of the drug, do not apply it directly before driving vehicles or working with mechanisms. Within 30 minutes after the instillation of the drug should refrain from occupations that require increased attention.
OVERDOSE
Overdose when used in ophthalmology is unlikely.
Symptoms: local manifestations are possible. There is no specific antidote. The drug should be withdrawn and symptomatic therapy prescribed.
Prolonged use of the drug or use in large doses can increase systemic absorption of dexamethasone, and it is also possible to develop ocular hypertension and certain diseases of the cornea or lens.
DRUG INTERACTION
With prolonged use of dexamethasone with idoxuridine, destructive processes in the epithelium of the cornea may increase.
Dexamethasone can enhance the action of barbiturates.
The combined use of phenytoin with dexamethasone leads to a decrease in the concentration of the latter.
Warfarin combined with dexamethasone increases the risk of bleeding.
In normal local administration, the dose is not sufficient to induce the induction or saturation of liver enzymes.
With simultaneous use of dexamethasone with diuretics (especially thiazide and inhibitors of carbonic anhydrase) and amphotericin B, it is possible to increase the excretion of potassium from the body and increase the risk of developing heart failure.
With the simultaneous use of dexamethasone with cardiac glycosides, their tolerability worsens and the likelihood of developing ventricular extrasystole (due to induced hypokalemia) increases.
With simultaneous use of dexamethasone with ethanol and NSAIDs, the risk of erosive and ulcerative gastrointestinal lesions increases.
Estrogens and oral estrogen-containing contraceptives reduce the clearance of dexamethasone, which may be accompanied by an increase in the severity of its action.
The combined use of antiarrhythmic drugs with dexamethasone may lead to a decrease in the effect of the latter.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 3 years.
After opening the vial, the drug should be stored for no more than 4 weeks.
