Instructions for use Dexamethasone-Darnitsa eye drops 1 mg/ml bottle 10 ml
Composition
active ingredient: dexamethasone;
1 ml of solution contains dexamethasone sodium phosphate 1 mg;
Excipients: boric acid, sodium tetraborate, disodium edetate, benzalkonium chloride, water for injections.
Dosage form
Eye drops, solution.
Main physicochemical properties: clear, colorless liquid, odorless.
Pharmacotherapeutic group
Drugs used in ophthalmology. Anti-inflammatory drugs. Corticosteroids, simple drugs. Dexamethasone.
ATX code S01B A01.
Pharmacological properties
Pharmacodynamics
The drug belongs to synthetic fluorinated glucocorticosteroids. It has a pronounced anti-inflammatory effect with reduced mineralocorticoid effects compared to some other steroids and is one of the most potent anti-inflammatory drugs. The mechanism of action of the drug is similar to the pharmacological action of other fluorinated glucocorticosteroids and differs only in greater strength and duration of effect. It has an anti-inflammatory effect by inhibiting vascular adhesive molecules of endothelial cells, cyclooxygenase I or II, and the release of cytokines. As a result, the formation of inflammatory mediators is reduced and the adhesion of leukocytes to the vascular endothelium is inhibited, thus preventing their penetration into the inflamed tissues of the eye.
Pharmacokinetics
After instillation into the conjunctival sac, the maximum concentration of dexamethasone in the intraocular fluid is observed after 2 hours and is 30 ng/ml. Binding to blood plasma proteins (albumin) is 77–84%. The half-life is 3–4 hours. Clearance ranges from 0.111 to 0.225 l/h/kg and the volume of distribution is from 0.576 to 1.15 l/kg. Metabolized in the liver. Approximately 60% of the dose is excreted in the urine as 6-β-hydroxydexamethasone. The overall resorptive effect of dexamethasone is insignificant.
Indication
Treatment of steroid-responsive non-infectious inflammatory and allergic conditions of the conjunctiva, cornea and anterior segment of the eye, including inflammatory reactions in the postoperative period.
Contraindication
Hypersensitivity to the active substance or to any of the excipients; acute untreated bacterial eye infections; fungal eye infections; mycobacterial eye infections; viral infections of the cornea and conjunctiva (acute superficial keratitis caused by herpes simplex, vaccinia and chickenpox, except keratitis caused by herpes zoster).
Interaction with other medicinal products and other types of interactions
When using several topical eye medications at the same time, the interval between their applications should be at least 15 minutes. Eye ointments should be applied last.
With simultaneous use of the drug with atropine, other anticholinergics and mydriatics, an increase in intraocular pressure is possible.
Concomitant use of topical steroids and topical nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of corneal wound healing complications.
When used concomitantly with ophthalmic medications containing phosphates, the risk of corneal deposits or clouding increases, especially in patients with compromised corneas.
CYP3A4 inhibitors (including ritonavir and cobicistat) may reduce the clearance of dexamethasone, leading to increased systemic effects and the development of Cushing's syndrome and/or adrenal suppression. Such combinations should be avoided unless the benefit of treatment outweighs the increased risk of systemic corticosteroid side effects. In such cases, patients should be carefully monitored for systemic corticosteroid effects.
There is no information on the interaction of the drug with other medicines.
Application features
The medicinal product is intended for ophthalmic use only.
Side effects that occur when instilling the drug disappear after 5–15 seconds and are not an indication for its withdrawal.
To prevent possible systemic resorption, after instillation of the drug, the tear ducts should be held with fingers for 2–3 minutes.
When using the medicine, do not touch the dropper tip to prevent contamination of the medicine.
With prolonged topical use of corticosteroids, the development of ocular hypertension and/or glaucoma with subsequent damage to the optic nerve, deterioration of visual acuity and visual field disorders, as well as the formation of posterior subcapsular cataracts of the posterior chamber of the eye is possible. During prolonged use of the drug, intraocular pressure should be regularly monitored.
This is especially important in children, as the risk of corticosteroid-induced ocular hypertension may be higher in children and may occur earlier than in adults.
Topical corticosteroids may delay the healing of corneal wounds and, in the presence of diseases characterized by corneal or sclera thinning, may lead to perforation. Topical NSAIDs are also known to delay or delay wound healing. Concomitant use of topical NSAIDs and topical steroids may increase the risk of wound healing complications (see section 4.5). The cornea should be monitored (fluorescein staining) during treatment with the drug.
Corticosteroids may reduce resistance to bacterial, viral, or fungal infections, interfere with the detection of such infections, and mask their clinical signs, preventing the detection of antibiotic ineffectiveness.
In acute purulent eye diseases, corticosteroids may mask infections or spread existing infections. If treatment lasts more than 10 days, intraocular pressure should be monitored.
In patients who have been or are being treated with corticosteroids, the possibility of developing a fungal infection should be considered in cases of persistent corneal ulceration. If a fungal infection occurs, treatment with the drug should be discontinued.
The drug should be used with extreme caution and only in combination with antiviral therapy in the treatment of stromal keratitis or uveitis caused by herpes simplex. Slit-lamp biomicroscopy should be performed periodically.
The product contains phosphates, which may cause corneal deposits or clouding when used topically. It should be used with caution in patients with compromised corneas and in patients receiving concomitant treatment with other ophthalmic drugs containing phosphates.
It is not recommended to wear contact lenses during the treatment of eye inflammation. If necessary, soft contact lenses should be removed before using the drug and reinserted no earlier than 15 minutes after instillation of the drug.
This medicinal product contains benzalkonium chloride, which may cause eye irritation and is known to discolour soft contact lenses. Contact with soft contact lenses should be avoided.
Cushing's syndrome and/or adrenal suppression may occur following intensive or prolonged continuous therapy in susceptible patients, including children and patients receiving CYP3A4 inhibitors (including ritonavir and cobicistat), due to systemic absorption of dexamethasone. In these cases, treatment should be gradually discontinued.
Ability to influence reaction speed when driving vehicles or other mechanisms
The drug has no or negligible influence on the ability to drive or use machines. As with other eye drops, temporary blurred vision or other visual disturbances may occur. If blurred vision occurs during instillation, the patient should wait until the vision clears before driving or using machines.
Use during pregnancy or breastfeeding
Pregnancy
There are only limited data on the use of the drug in pregnant women. Reproductive toxicity has been demonstrated in animal studies - topical corticosteroids can be absorbed systemically and cause fetal abnormalities in pregnant animals. The potential risk to humans is unknown, therefore the drug is not recommended for use during pregnancy.
Breast-feeding
Glucocorticosteroids are excreted in breast milk in amounts that may affect breastfeeding when administered systemically. However, systemic exposure is low when administered topically. Since it is not known whether the drug is excreted in human milk, a risk to the child during breastfeeding cannot be excluded. Therefore, a decision should be made whether to temporarily discontinue breastfeeding for the duration of drug administration or to discontinue/abstain from drug therapy, taking into account the potential benefit of the drug for the mother and the benefit of breastfeeding for the child.
Fertility.
Fertility studies have not been conducted with intraconjunctival dexamethasone. There are limited clinical data on the effects of dexamethasone on male or female fertility.
Method of administration and doses
The bottle is protected by a tamper-evident seal. When using for the first time, the cap must be turned to separate it from the protective ring.
The bottle has a special configuration, thanks to which, when pressure is applied to the bottom, the solution is dosed according to the principle of “one press – one drop”. The hardness of the bottle walls significantly reduces the possibility of a jet release of the drug – a common cause of eye drop overdose.
Severe or acute eye inflammation:
As initial therapy, 1–2 drops of the drug should be instilled into the conjunctival sac(s) of the affected eye(s) every 30–60 minutes.
The dose can then be reduced to 1 drop 3–4 times daily if this dose is sufficient to control inflammation.
If the desired result is not achieved within 3–4 days, additional systemic or subconjunctival therapy may be prescribed.
Chronic eye inflammation:
1–2 drops of the drug should be instilled into the conjunctival sac(s) of the affected eye(s) every 3–6 hours, or more often if necessary.
Minor inflammation, allergy:
1–2 drops of the drug should be instilled into the conjunctival sac(s) of the affected eye(s) every 3–4 hours until the desired effect is achieved.
It is recommended to constantly monitor intraocular pressure.
After instillation, careful eyelid closure or nasolacrimal occlusion is recommended. This reduces systemic absorption of drugs administered into the eye, which reduces the likelihood of systemic side effects.
If several topical eye medications are used simultaneously, the interval between their applications should be at least 15 minutes. Eye ointments should be applied last.
Elderly patients
There is no need for dose adjustment.
Patients with impaired liver and kidney function
Due to the low systemic absorption of dexamethasone after topical application of this medicinal product, there is no need for dose adjustment.
Children
The safety and efficacy of the drug in children have not been established.
Overdose
The special configuration of the bottle makes accidental overdose of the drug unlikely. There is no information on cases of overdose.
In case of overdose with topical application, wash excess medication from the eye(s) with warm water.
Adverse reactions
On the part of the organs of vision:
keratitis, conjunctivitis, keratoconjunctivitis sicca, eyelid ptosis, corneal discoloration, photophobia, blurred vision, mydriasis, eye pain, eye irritation, foreign body sensation in the eyes, unusual sensations in the eyes, formation of scales at the edges of the eyelids; corneal calcification (due to the use of eye drops containing phosphates in some patients with severely damaged corneas); immediately after instillation, the following are possible: a short-term burning sensation, tingling, discomfort in the eyes, itching, eye hyperemia and increased tearing;
with prolonged use - increased intraocular pressure with subsequent damage to the optic nerve, decreased visual acuity, visual field disorders, formation of posterior subcapsular cataracts, glaucoma, corneal erosion, in the presence of diseases that lead to thinning of the cornea or sclera - increased risk of their perforation (see section "Peculiarities of use").
On the part of the endocrine system: after prolonged therapy, systemic adsorption may occur with suppression of the function of the adrenal cortex and the development of Cushing's syndrome.
Nervous system: dysgeusia (taste disorder), headache, dizziness.
Immune system: hypersensitivity reactions; patients with hypersensitivity to benzalkonium chloride may develop allergic blepharitis or conjunctivitis.
Glucocorticosteroids may reduce resistance to infections.
Expiration date
2 years.
After opening the bottle, store the medicine for no more than 28 days.
Storage conditions
Store in original packaging at a temperature not exceeding 15 ° C. Do not freeze.
Keep out of reach of children.
Packaging
10 ml in a bottle; 1 bottle in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
