Dexatobropt eye drops, 5 ml

Inflammatory diseases of the eye and its appendages caused by pathogens sensitive to the drug:

• blepharitis;

• conjunctivitis;

• blepharoconjunctivitis;

• keratitis;

• keratoconjunctivitis;

• iridocyclitis.

• Prevention and treatment of inflammation in the postoperative period after cataract extraction.

Locally. Shake the bottle before use.

For children over 12 years old and adults, including elderly patients, the drug is instilled in 1-2 drops into the conjunctival sac of the affected eye (or eyes) every 4-6 hours.

In the first 24-48 hours, the dose can be increased to 1-2 drops into the conjunctival sac every 2 hours, followed by a decrease in the frequency of instillations of the drug as the inflammatory phenomena decrease.

Care should be taken not to discontinue therapy prematurely.

In acute severe infectious process - 1-2 drops into the conjunctival sac every 60 minutes until the severity of the condition decreases. Then it is necessary to reduce the frequency of instillations of the drug to 1-2 drops into the conjunctival sac every 2 hours for 3 days. Then 1-2 drops into the conjunctival sac every 4 hours for 5-8 days. If necessary, continue instillation: 1-2 drops into the conjunctival sac for 5-8 days.

Prevention of inflammation in the postoperative period after cataract extraction - 1 drop into the conjunctival sac 4 times / day, starting from the day of surgery up to 24 days.

Therapy can be started before surgery: 1 drop into the conjunctival sac 4 times / day 1 day before surgery, 1 drop into the conjunctival sac on the day of surgery, then 1 drop into the conjunctival sac 4 times / day for 23 days. If necessary, the frequency of instillation of the drug can be increased to 1-2 drops into the conjunctival sac every 2 hours during the first 2 days after surgery.

After instillation of the drug, to reduce the risk of developing systemic side effects, it is recommended to lightly press with a finger on the projection area of ??the lacrimal sacs at the inner corner of the eye for 1-2 minutes after instillation of the drug - this reduces the systemic absorption of the drug.

In the case of use with other local ophthalmic drugs, the interval between their use should be at least 5 minutes.

The bottle must be closed after each use.

Do not touch the tip of the dropper bottle to any surface to maintain the sterility of the solution.

Eye drops in the form of a suspension of white or almost white color, the presence of a precipitate is possible, which quickly dissipates with gentle shaking.

1 ml

dexamethasone 1 mg

tobramycin 3 mg

Excipients: tyloxapol - 0.5 mg, hypromellose (HPMC 4000 cP) - 5 mg, sodium sulfate - 12 mg, sodium chloride - 3.3 mg, disodium edetate dihydrate - 0.1 mg, benzalkonium chloride - 0.1 mg, sodium hydroxide solution 1M or sulfuric acid 1M solution - up to pH 5.0-6.0, purified water - up to 1 ml.

• Hypersensitivity to any component of the drug;

• superficial forms of keratitis caused by Herpes simplex, in particular, treelike keratitis;

• vaccination, chickenpox and other viral diseases of the cornea and conjunctiva;

• mycobacterial eye infections;

• fungal diseases of the eyes;

• previously untreated parasitic eye infections;

• acute purulent diseases of the organ of vision without concomitant antimicrobial therapy;

• conditions after removal of a foreign body of the cornea or with defects in the corneal epithelium of another etiology;

• children under 12 years of age;

• period of breastfeeding.

With care: deep stromal keratitis caused by Herpes simplex; pregnancy.

pharmachologic effect

Combined preparation with antibacterial and anti-inflammatory action for topical use in ophthalmology.

Tobramycin is a broad-spectrum antibiotic from the aminoglycoside group. Violates protein synthesis and the permeability of the cytoplasmic membrane of the microbial cell. Active against gram-positive and gram-negative microorganisms: Staphylococcus spp. (including Staphylococcus aureus, Staphylococcus epidermidis, including strains resistant to penicillin); Streptococcus spp. (including some beta-hemolytic species of group A, some non-hemolytic species and some strains of Streptococcus pneumoniae), Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus mirabilis, Morganella morganii, Citrobacter influenza, Haemella influenza spp., Acinetobacter spp., Serratia marcescens.

Dexamethasone is a synthetic fluorinated GCS. It has a pronounced anti-inflammatory, anti-allergic and desensitizing effect. Dexamethasone actively suppresses inflammatory processes, inhibiting the release of inflammatory mediators by eosinophils, migration of mast cells and reducing capillary permeability. Does not possess mineralocorticoid activity.

Pharmacokinetics

Dexamethasone

After topical application of the drug, systemic absorption of dexamethasone is low. Cmax of dexamethasone in blood plasma is from 220 to 888 pg / ml (about 555 ± 217 pg / ml) after the drug is administered, 1 drop in each eye 4 times / day for 2 days.

About 77-84% of dexamethasone entering the systemic circulation binds to plasma proteins.

It is excreted by metabolism, about 60% in the form of 6 -? - hydroxydexamethasone by the kidneys. T1 / 2 averages 3-4 hours.

Tobramycin

After topical application of the drug, the systemic absorption of tobramycin is low. The concentration of tobramycin in blood plasma after administration of the drug, 1 drop in each eye 4 times / day for 2 days, was below the detection threshold in 9 of 12 patients. Cmax of tobramycin in blood plasma is 247 pg / ml, which is 8 times lower than the concentration threshold associated with nephrotoxicity.

Tobramycin is excreted by the kidneys, mainly unchanged.

Side effect

From the immune system: rarely - allergic manifestations of the eyes; frequency unknown - anaphylactic reactions, hypersensitivity reactions.

From the nervous system: infrequently - headache; frequency unknown - dizziness.

From the side of the organ of vision: infrequently - pain in the eye, itching in the eye, discomfort in the eye, increased intraocular pressure, edema of the conjunctiva, eye irritation; rarely - keratitis, blurred vision, dry eye syndrome, conjunctival hyperemia; the frequency is unknown - edema of the eyelids, erythema of the eyelids, mydriasis, lacrimation.

From the respiratory system: infrequently - rhinorrhea, laryngospasm.

From the digestive system: rarely - dysgeusia, nausea, discomfort in the epigastric region.

On the part of the skin and subcutaneous tissues: the frequency is unknown - erythema multiforme exudative, rash, facial edema, itching.

Application during pregnancy and lactation

Pregnancy

Systemic use of high doses of aminoglycosides has been associated with the development of ototoxicity. However, after topical application in ophthalmology, the systemic concentration of tobramycin is very low, and it will not cause direct or indirect adverse effects on reproductive function. Local use of corticosteroids in pregnant animals can cause fetal development disorders, incl. cleft palate. The clinical significance is unknown. Animal studies have shown that the introduction of GCS in recommended doses during pregnancy can increase the risk of impaired intrauterine development of the fetus, the development of diseases of the cardiovascular system and / or metabolic disorders and / or disorders of psychophysiological development.Currently, there is no data on the embryotoxic effect of the drug when used during pregnancy in humans. However, the danger to the fetus cannot be ruled out. The use of GCS in the last trimester of pregnancy can cause inhibition of the production of its own GCS in a fetus requiring treatment after birth.

Thus, the drug DexaTobropt during pregnancy should be used only when the potential benefit of therapy to the mother outweighs the potential risk to the fetus.

Breastfeeding period

There are no data on the penetration of dexamethasone into breast milk. Tobramycin passes into breast milk with systemic use. There are no data on the penetration of dexamethasone and tobramycin into breast milk after topical application in ophthalmic dosage forms. It is unlikely that dexamethasone and tobramycin, when applied topically in the form of eye drops, are likely to cause clinical effects in the newborn. However, the potential risk to the child cannot be completely excluded. The decision to discontinue breastfeeding or to suspend or discontinue drug therapy should be made taking into account the benefits of breastfeeding for the baby and the benefits of therapy for the mother.

Application in children

Contraindicated in children and adolescents under the age of 12 years.

special instructions

Some patients may experience hypersensitivity reactions to topical aminoglycosides. Hypersensitivity reactions (allergic reactions) can be of varying severity and range from local to generalized reactions, including erythema, pruritus, urticaria, rash, anaphylaxis, anaphylactoid reactions, or bullous reactions.

With the development of hypersensitivity during the use of the drug, treatment should be discontinued.

The development of cross-hypersensitivity to other aminoglycosides is possible. Patients who are hypersensitive to topical tobramycin may also be sensitive to other topical or systemic aminoglycosides.

Serious adverse reactions have occurred in patients receiving systemic aminoglycoside therapy, including neurotoxicity, ototoxicity, and nephrotoxicity. Caution should be exercised with the simultaneous local and systemic use of aminoglycosides.

Care is required when using the drug in the treatment of deep stromal keratitis caused by Herpes simplex; also with this herpetic lesion of the eye organ, frequent biomicroscopy is necessary.

Long-term use of GCS for local use in ophthalmology, exceeding the maximum recommended duration of therapy - 24 days, can lead to an increase in intraocular pressure and the development of a symptom complex of glaucoma, including damage to the optic nerve, decreased visual acuity and narrowing of the boundaries of visual fields; to the formation of a posterior subcapsular cataract. Therefore, in patients who have been using drugs containing GCS for a long time, intraocular pressure should be measured regularly and often.

The risk of increased intraocular pressure and / or the formation of cataracts due to the use of GCS is higher in patients with a predisposition (for example, with diabetes mellitus).

In predisposed patients, including children and patients receiving ritonavir, after intensive therapy or continuous long-term therapy, Itsenko-Cushing's syndrome and / or suppression of adrenal function may occur due to systemic absorption of dexamethasone with local ophthalmic use. In these cases, the drug should not be canceled immediately, but gradually.

GCS can reduce resistance to bacterial, viral or fungal infections and promote their development, as well as mask the clinical signs of infection.

The appearance of non-healing ulcers on the cornea may indicate the development of fungal invasion. If a fungal invasion occurs, GCS therapy should be discontinued.

Long-term use of antibiotics such as tobramycin can lead to increased growth of resistant organisms, incl. mushrooms. With the development of superinfection, the use of the drug should be discontinued and appropriate therapy initiated.

The use of a fixed combination of dexamethasone and tobramycin in the treatment of acute purulent infections of the organ of vision is possible only in the case of previously conducted local antibiotic therapy, because the use of dexamethasone during this period can aggravate the course of the infectious process. Abrupt cessation of therapy due to the possibility of resumption of symptoms of an infectious or inflammatory lesion of the organ of vision is undesirable.

When applied topically, GCS can slow down the healing process of the cornea. Topical NSAIDs also slow healing. The simultaneous use of topical NSAIDs and topical corticosteroids may increase the likelihood of impaired healing.

In diseases that cause thinning of the cornea or sclera, perforations may occur as a result of the use of corticosteroids for topical use. If the duration of therapy is more than 2 weeks, the condition of the cornea should be monitored.

In the case of topical application of tobramycin simultaneously with antibiotics of the aminoglycoside group for systemic use, the general blood picture should be monitored.

When treating inflammatory eye diseases, it is not recommended to wear contact lenses. This product contains benzalkonium chloride, which may irritate the eyes and discolor soft contact lenses. Avoid contact of the drug with soft contact lenses. If patients are allowed to wear contact lenses, then they must be instructed to remove soft contact lenses before using the drug and reinstall them no earlier than 15 minutes after instillation of the drug.

Impact on fertility

Studies of the effect of the drug on the fertility of animals or humans have not been conducted. Clinical data for assessing the effect on fertility in men or women are limited.

Influence on the ability to drive vehicles and use mechanisms

Temporary blurred vision or other visual impairments after using the drug may affect the ability to drive vehicles and mechanisms. If blurred vision occurs after instillation of the drug, then before starting to drive vehicles and mechanisms, the patient must wait until the clarity of vision is restored.

Overdose

The development of toxic effects with local application of the drug or if it is accidentally swallowed is unlikely.

Treatment: if an excess amount of the drug enters the conjunctival cavity, it is necessary to rinse the eyes with warm water. If accidentally swallowed - symptomatic treatment.

Drug interactions

With the combined use of NSAIDs for local use in ophthalmology and GCS for local use in ophthalmology, it is possible to potentiate the negative effect of drugs on the healing processes of the cornea.

Plasma concentrations of dexamethasone may increase in patients receiving ritonavir.