Dexametasonlong^® (Drops) Instructions for Use

Marketing Authorization Holder

Firn M, LLC (Russia)

ATC Code

S01BA01 (Dexamethasone)

Active Substance

Dexamethasone (Rec.INN registered by WHO)

Dosage Form

Dexametasonlong®

Eye drops 0.1%: 5 ml or 10 ml bottle with dropper dispenser

Dosage Form, Packaging, and Composition

Eye drops as a transparent, colorless or slightly yellowish liquid.

Excipients: benzalkonium chloride – 0.1 mg, potassium chloride – 1.4 mg, sodium chloride – 3.6 mg, disodium edetate dihydrate – 0.5 mg, hypromellose 3 mg, potassium dihydrogen phosphate 3.63 mg, sodium hydrogen phosphate dodecahydrate 7.13 mg, macrogol 4000 30 mg, purified water to 1 ml.

5 ml – plastic bottles (1) with dropper dispenser – cardboard packs.
10 ml – plastic bottles (1) with dropper dispenser – cardboard packs.

Clinical-Pharmacological Group

Topical corticosteroids for ophthalmology

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Impairs the ability of macrophages to phagocytose and to form interleukin-1. Promotes stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability caused by the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A₂, which leads to suppression of prostaglandin and leukotriene synthesis. Suppresses the release of COX (mainly COX-2), which also contributes to the reduction of prostaglandin production.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses antibody formation.

Dexamethasone suppresses the release of ACTH and β-lipotropin by the pituitary gland, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly to blood vessels, it has a vasoconstrictor effect.

Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, increases the activity of gluconeogenesis enzymes. In the liver, Dexamethasone enhances glycogen storage by stimulating the activity of glycogen synthase and the synthesis of glucose from protein metabolism products. An increase in blood glucose levels activates insulin secretion.

Dexamethasone suppresses glucose uptake by fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, leading to fat accumulation.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, and bone tissue. Osteoporosis and Cushing’s syndrome are the main factors limiting long-term glucocorticosteroid therapy. As a result of the catabolic effect, growth suppression in children is possible.

In high doses, Dexamethasone may increase the excitability of brain tissue and contribute to a decrease in the seizure threshold. Stimulates excessive production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.

When applied topically, the therapeutic activity of dexamethasone is due to its anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect) action.

Pharmacokinetics

When used topically in ophthalmology, it is absorbed through the cornea with intact epithelium into the aqueous humor of the anterior chamber of the eye. In case of inflammation of the eye tissues or damage to the mucous membrane and cornea, the absorption rate of dexamethasone significantly increases.

Indications

Allergic and inflammatory eye diseases: non-purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharoconjunctivitis, blepharitis, episcleritis, scleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia; macular edema due to occlusion of the central retinal vein or its branches, visual impairment due to diabetic macular edema in patients with aphakia, in patients with an insufficient response to therapy, or those for whom therapy with drugs other than glucocorticosteroids is not suitable, inflammation of the posterior segment uvea, which is non-infectious uveitis.

ICD codes

Dosage Regimen

Instill one to two drops into the conjunctival sac of the affected eye(s).

For severe inflammation, apply drops every 1-2 hours initially.

As inflammation subsides, reduce frequency to three to four times daily.

For mild to moderate inflammation, apply drops four to six times daily.

For allergic conjunctivitis, use four times daily until symptoms resolve.

Do not use for more than 14 days without ophthalmological re-evaluation.

For post-operative inflammation, begin application 24 hours after surgery.

Apply one drop four times daily for two weeks, then taper as directed.

To minimize systemic absorption, apply gentle pressure on the lacrimal sac for 1-2 minutes after instillation.

Avoid direct contact of the dropper tip with the eye or any surface.

If using other topical ophthalmic agents, maintain an interval of at least 10 minutes between applications.

Apply eye ointments after instilling eye drops.

Do not wear contact lenses during treatment.

Adverse Reactions

Nervous system disorders uncommon – dysgeusia.

Eye disorders common – eye discomfort; uncommon – keratitis, conjunctivitis, dry eye syndrome, corneal staining with medical dye, photophobia, blurred vision, eye itching, foreign body sensation in eyes, increased lacrimation, unusual sensation in eye, crusting on eyelid margins, eye irritation, eye hyperemia.

Immune system disorders hypersensitivity.

Endocrine disorders Cushing’s syndrome, adrenal insufficiency.

Nervous system disorders dizziness, headache.

Eye disorders glaucoma, ulcerative keratitis, increased intraocular pressure, decreased visual acuity, corneal erosion, eyelid ptosis, eye pain, mydriasis.

Contraindications

For short-term use for vital indications – hypersensitivity to dexamethasone.

Bacterial, viral, fungal eye diseases, tuberculous eye lesions, violation of the integrity of the ocular epithelium, acute form of purulent eye infection in the absence of specific therapy, corneal diseases combined with epithelial defects, trachoma, glaucoma with decompensated increase in intraocular pressure not controlled by medications, aphakia with rupture of the posterior lens capsule; age under 18 years (for some dosage forms).

Use in Pregnancy and Lactation

During pregnancy (especially in the first trimester), as well as during lactation, Dexamethasone is used taking into account the expected therapeutic effect and the negative impact on the fetus. With long-term therapy during pregnancy, the possibility of fetal growth disorders cannot be excluded. If used at the end of pregnancy, there is a risk of adrenal cortex atrophy in the fetus, which may require replacement therapy in the newborn.

Use in Hepatic Impairment

Should be used with caution in severe chronic liver failure.

Use in Renal Impairment

Should be used with caution in severe chronic renal failure.

Pediatric Use

Not recommended for use in children.

Contraindication: age under 18 years (for some dosage forms).

Geriatric Use

Use with caution in elderly patients to avoid the risk of exacerbation of chronic diseases.

Special Precautions

Long-term use of topical glucocorticosteroids may lead to increased intraocular pressure and/or glaucoma with optic nerve damage, decreased visual acuity and visual field defects, and the formation of posterior subcapsular cataracts. Therefore, in patients using glucocorticosteroid-containing drugs for a long time (more than 10 days), intraocular pressure should be measured regularly.

The risk of increased intraocular pressure and/or cataract formation due to corticosteroid use is higher in predisposed patients (e.g., with diabetes mellitus). The risk of increased intraocular pressure is increased in patients with concomitant ocular hypertension and/or glaucoma, as well as in patients with a family history of glaucoma. Weekly monitoring of intraocular pressure is necessary in such patients.

Caution should be exercised and periodic biomicroscopy should be performed when using the drug for the treatment of deep keratitis caused by Herpes simplex.

If there is no improvement within 7-8 days, the choice of therapy should be reconsidered.

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

In case of concomitant bacterial infections, appropriate antibacterial therapy should be prescribed.

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

Topical glucocorticosteroids may slow down the process of corneal healing.

It is known that in diseases that cause thinning of the cornea or sclera, perforations may occur as a result of using topical glucocorticosteroids.

If therapy lasts more than 2 weeks, the condition of the cornea should be monitored. The use of dexamethasone in the complex therapy of Sjögren’s syndrome is possible only for moderate to severe keratoconjunctivitis, the duration of the course of therapy should not exceed 2 weeks due to the possibility of adverse reactions.

After application, it is recommended to perform nasolacrimal occlusion or gently close the eye. This may reduce the systemic absorption of the drug when applied topically, and thereby reduce the likelihood of systemic adverse reactions.

It is not recommended to wear contact lenses when treating eye inflammation.

Topical and systemic use of glucocorticosteroids may lead to visual disturbances. If a patient develops symptoms such as blurred vision or other visual disturbances, they should be referred to an ophthalmologist to identify possible causes of their development, which may include cataracts, glaucoma, or rare conditions such as central serous chorioretinopathy, which have been reported after the use of systemic and topical glucocorticosteroids.

Topical glucocorticosteroids should not be used until the etiology of the eye lesion has been established.

Effect on the ability to drive vehicles and mechanisms

Temporary decrease in visual clarity or other visual disturbances may affect the ability to drive a car or operate machinery. If a patient experiences temporary blurred vision after using the drug, they should wait until their vision is restored before driving a car or operating machinery.

Drug Interactions

When used concomitantly with antipsychotic agents, bucarban, azathioprine, there is a risk of cataract development; with agents that have anticholinergic action – a risk of glaucoma development.

Concomitant use of topical steroids and topical NSAIDs may increase the likelihood of impaired corneal healing.

There are data on the occurrence of hemorrhagic complications, including subconjunctival hemorrhage, with the use of dexamethasone in ophthalmology in some dosage forms in patients receiving antiplatelet agents and anticoagulants. Caution is required if concomitant use is necessary.

The risk of additional increase in intraocular pressure cannot be excluded if Dexamethasone is used together with anticholinergic agents, which can also cause an increase in intraocular pressure in predisposed patients. In case of concomitant use with antiglaucoma drugs, a decrease in the hypotensive effect of the latter is possible.

CYP3A4 inhibitors, including ritonavir and cobicistat, can increase the level of systemic exposure, leading to an increased risk of adrenal function suppression/Cushing’s syndrome. Combination of these drugs should be avoided, except in cases where the beneficial effect outweighs the increased risk of systemic side effects of glucocorticosteroids, but in this case the patient should be closely monitored for the occurrence of systemic effects of corticosteroids.

In case of use with other topical ophthalmic drugs, the interval between their applications should be at least 10 minutes.

Eye ointments should be applied last.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.