Oftacortal

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT OFTACORTAL (oftacortal)

Composition:

active substance: dexamethasone sodium phosphate;

1 single-dose container contains:

active substance: dexamethasone sodium phosphate 0.45 mg, equivalent to 0.342 mg of dexamethasone;

excipients: sodium citrate, monobasic monohydrate sodium phosphate, dodecahydrate sodium hydrogen phosphate, 1 M solution of sodium hydroxide or 1 M solution of hydrochloric acid, water for injections.

Pharmaceutical form. Eye drops, solution.

Main physico-chemical properties: clear, colorless solution.

Pharmacotherapeutic group. Anti-inflammatory agents used in ophthalmology. Simple corticosteroid preparations. ATC code S01B A01.

Pharmacological Properties

Pharmacodynamics

Dexamethasone sodium phosphate is a corticosteroid with potent anti-inflammatory activity, which is 25 times greater than that of hydrocortisone. As with all corticosteroids, the anti-inflammatory activity of the drug is primarily manifested through inhibition of the release of arachidonic acid, a precursor of the major inflammatory mediators, prostaglandins and leukotrienes. The steroid acts by inducing the synthesis of the protein lipocortin, which in turn inhibits the activity of the enzyme phospholipase A2 that releases arachidonic acid.

Pharmacokinetics

Corticosteroids generally achieve therapeutic intraocular concentrations after instillation into the conjunctival sac. The extent of penetration in any case depends on the molecular characteristics and chemical form of the steroid.

Preclinical safety data

In animal studies, dexamethasone was well tolerated by rabbits and rats following topical administration for periods up to 6 months. The main signs of toxicity observed in all animal species after oral administration were related to adrenocorticosteroid effects of the drug and included changes in pituitary-adrenal glands and mild anemia. Primary signs of toxicity were observed in the stomach, liver, adrenal glands, pituitary gland, lungs, and spleen.

In studies conducted after topical application of the drug, most of these findings were absent or very low in severity.

Clinical characteristics

Indications

The medicinal product OFTACORTAL is indicated for the treatment of vernal and allergic conjunctivitis, blepharitis and blepharoconjunctivitis, allergic keratoconjunctivitis, scleritis, episcleritis, and uveitis.

Contraindications

• Hypersensitivity to the active substance or to any of the excipients of the medicinal product.
• Intraocular hypertension.
• Herpes simplex.
• Acute ulcerative phase of viral infections of the cornea.
• Conjunctivitis with ulcerative keratitis, including early stage (positive fluorescein test).
• Tuberculosis and fungal ocular infections.
• Acute purulent ophthalmia.
• Purulent conjunctivitis.
• Purulent and herpetic blepharitis.
• Hordeolum (stye).
• Corneal injury or abrasions.
• Children under 3 years of age.
• Contraindicated during pregnancy and breastfeeding.

Interaction with other medicinal products and other forms of interaction

Inhibitors of CYP3A4 (including ritonavir and cobicistat) may reduce the clearance of dexamethasone, leading to enhanced effects and adrenal suppression/Cushing's syndrome. Such combinations should be avoided, except when the benefit outweighs the risk of increased systemic side effects of corticosteroids; in such cases, careful monitoring of systemic corticosteroid effects is required.

Special precautions for use

Increased intraocular pressure and glaucoma

Prolonged treatment with corticosteroids for local ophthalmic use may lead to elevated intraocular pressure in predisposed patients, resulting in glaucoma with subsequent optic nerve damage, decreased visual acuity, and visual field defects.

In patients with glaucoma, corticosteroids should be used with caution, and intraocular pressure should be monitored frequently.

Prolonged use of corticosteroid medications may lead to the formation of posterior subcapsular cataracts.

During prolonged treatment with the medicinal product, intraocular pressure should be continuously monitored.

Masking of acute untreated infections

An acute untreated ocular infection may be masked or its activity may be intensified by the presence of corticosteroid medications.

Secondary ocular infections

Prolonged use of corticosteroid medications may suppress the immune response and thereby increase the risk of secondary ocular infections caused by pathogenic microorganisms isolated from ocular tissue.

In cases of persistent corneal ulceration, fungal infection should be considered in patients who are or have been treated with corticosteroids. In appropriate cases, fungal cultures should be performed.

Topical application of corticosteroids may prolong the course and exacerbate the severity of many viral eye infections (including herpes simplex).

The medicinal product should be used with particular caution in the treatment of stromal keratitis; periodic slit-lamp microscopy should also be performed.

The medicinal product is not recommended in the presence of herpetic keratitis; however, it may be permitted for use only under the supervision of an ophthalmologist, particularly regarding possible immune consequences of infection.

Thinning of the cornea and sclera

Particular attention should be paid to conditions associated with corneal thinning.

It is known that in conditions leading to thinning of the cornea or sclera, topical application of corticosteroids may result in the development of perforations.

Delayed healing

The use of steroids after cataract surgery may delay wound healing.

Potential for eye injury and contamination

To prevent injury or contamination of the eyes, care must be taken to ensure that the tip of the single-dose container does not touch the eyes or any other surface.

Cushing's syndrome and/or adrenal suppression related to systemic absorption of ophthalmic dexamethasone preparations may occur after intensive or prolonged continuous therapy in predisposed patients, including children and patients receiving CYP3A4 inhibitors (including ritonavir and cobicistat). In such cases, treatment should be discontinued gradually.

In the presence of viral infections, corticosteroids may promote disease progression leading to irreversible corneal clouding (see section "Contraindications").

Systemic absorption can be reduced by pressing on the lacrimal sac in the medial canthus for one minute during and after instillation of drops (this blocks the passage of drops through the nasolacrimal duct to the large absorptive surface of the nasal and pharyngeal mucosa, which is particularly advisable in children).

Visual disturbances

Visual disturbances may occur during treatment with systemic and topical corticosteroids. If a patient experiences symptoms such as blurred vision or other visual disorders, referral to an ophthalmologist should be considered to determine possible causes, which may include cataract, glaucoma, or rare conditions such as central serous chorioretinopathy (CSC), which has been reported after use of systemic and topical corticosteroids.

Pediatric population

The medicinal product should be used in children aged 3 to 12 years only when absolutely necessary and under direct medical supervision.

Use during pregnancy or breastfeeding

Pregnancy

The medicinal product may be used during pregnancy only when strictly necessary and under direct medical supervision.

Breastfeeding

The medicinal product OFTACORTAL is contraindicated during lactation.

Ability to affect reaction speed when driving or operating machinery

The medicinal product OFTACORTAL does not affect the ability to drive or operate machinery.

As with any other eye medication, if transient blurred vision occurs during use, the patient should wait for vision to clear before driving or operating machinery.

Method of Administration and Dosage

One drop of the solution into the conjunctival sac 3–4 times daily or as prescribed by a physician.

Instructions for Use

The medication is intended for ophthalmic use only.

The solution from a single-dose container must be used immediately after opening for the affected eye(s).

Patients should be informed about proper handling of the single-dose container.

1. Wash hands thoroughly before using the eye drops.
2. Ensure the single-dose container is undamaged.
3. Detach one single-dose container from the strip.
4. Open by twisting off the top part without pulling.
5. Sit or lie down, tilt the head backward and look upward. Gently and carefully pull the lower eyelid downward with the thumb and index finger.
6. To avoid possible contamination, do not allow the tip of the single-dose container to touch the eyes, eyelids, or any other surface.

Since sterility cannot be maintained after opening the single-dose container, any remaining solution should be discarded after administration.

Nasolacrimal occlusion by pressing on the tear ducts may reduce systemic absorption (see section "Special Warnings and Precautions for Use").

Children

The efficacy and safety of the medication for treatment in children aged 3 to 12 years have not been established.

In children aged 3 to 12 years, the medication should be used only after careful benefit-risk assessment and under strict medical supervision.

Overdose

Any overdose requires immediate discontinuation of the medication to prevent irritation, ulceration, or acute glaucoma.

In case of accidental ingestion, it is recommended to drink plenty of fluids.

Side effects

The following reactions have been reported after dexamethasone use:

Immune system disorders

Hypersensitivity reactions.

Eye disorders

Subcapsular cataract, ocular infection (including bacterial, fungal, and viral infections), eye irritation, ocular perforation (perforation of sclera or cornea), glaucoma, increased intraocular pressure, burning sensation in eyes, blurred vision (frequency unknown, see also section "Special precautions").

Endocrine disorders

Cushing's syndrome, adrenal suppression (see section "Special precautions").

In all these cases, it is advisable to discontinue treatment and initiate appropriate therapy.

Very rare cases of corneal calcification associated with the use of ophthalmic solutions containing phosphate have been reported in patients with significant corneal damage.

Reporting suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

Shelf life: 2 years.

After first opening of the sachet, use single-dose containers within 28 days.

After first opening of the single-dose container, its contents should be used immediately and the container discarded.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep closed containers in the sachet and in the carton.

Keep out of reach of children.

Packaging

0.3 mL in a single-dose container; 5 containers connected in a strip, in a sachet; 4 sachets in a cardboard box.

Prescription status

Prescription only.

Manufacturer

Farmigea S.p.A.

Manufacturer's address and place of business

Via Giovan Battista Oliva 6-8, Pisa, 56121, Italy