INSTRUCTION

(Information for specialists)

on application of medicinal agent

GENTADEX

Registration number:

Trade name: Gentadex

International nonproprietary name: None

Appearance:clear transparent or yellowish fluid

Composition: 1 ml of solution contains: active ingredients: dexamethasone sodium phosphate (calculated on anhydrous and alcohol-free substance) – 1.0 mg, gentamycin sulphate – 3.0 mg;

excipients: disodium hydrogen phosphate, sodium dihydrophosphate, sodium tetraborate, trisodium citrate, sodium chloride, disodium EDTA dihydrate, benzalkonium chloride, water for injection.

Pharmaceutical form: solution (eye drops)

Pharmacotherapeutic group: Corticosteroids in combination with antimicrobial preparations.

ATC-code: S01CA01

Pharmacological action

Pharmacodynamics

 Combined preparation for local administration in ophthalmology. Its effect is stipulated by the ingredients entering into the composition: dexamethasone sodium phosphate, glucocorticosteroid and gentamycin sulphate, antibiotic of the aminoglycoside group.

Gentamycin sulphate is a broad spectrum antimicrobial (bactericidal) agent. It is active against the majority of gram-negative and gram-positive organisms: Pseudomonas aeruginosa, Escherichia coli, Proteus spp., Klebsiella spp., Serratia spp., Salmonella spp., Shigella spp., including multiple stable strains. It is less active against various streptococci and gram-negative cocci. The agent is not active against anaerobe bacteria, fungi, viruses. The agent penetrates actively the cell membrane of bacteria and binds to 30S bacterial ribosome subunit and inhibits activator protein synthesis.

Dexamethasone is a synthetic fluorated glucocorticosteroid, exhibits anti-inflammatory, antiallergic, immunodepressive effect, possesses antiexudative and antifibroblastogenic properties. It does not virtually have a mineral corticosteroidal effect, interacts with specific cytoplasmic receptors and forms a complex penetrating the nucleus and promoting mRNA synthesis; the latter induces protein formation mediating cell effects including lipocortin, which inhibits A2 phospholipase, suppresses arachidonic acid liberation contributing to inflammatory processes and allergy. Dexamethasone inhibits protein genes expression contributing to inflammatory reactions. It prevents from inflammatory mediators release from eosinophils and mast cells, inhibits the activity of hyaluronidase, collagenase and proteases, suppresses the activity of fibroblasts and collagen formation, reduces capillary permeability, stabilizes cell membranes including lysosomal, inhibits cytokine release from lymphocytes and macrophages.

Pharmacokinetics

If applied locally systemic absorption of the preparation’s ingredients is low. Dexamethasone has been reported to penetrate through the intact corneal epithelium the ocular anterior chamber fluid. In case of inflammation and conjunctiva damage the rate of penetration accelerates.

Indications for administration

Bacterial diseases of the anterior segment caused by organisms susceptible to gentamycin:

• blepharitis; conjunctivitis; keratitis (without epithelium lesions); iridocyclitis; scleritis and episcleritis.

Infected eczema of lid skin.

Allergic processes of the anterior segment in addition to bacterial infection. Prevention and treatment of inflammatory processes in the postoperative period.

Contraindications

hypersensitivity to any ingredient of the preparation;

viral (including herpetic) or fungal infections, tuberculosis, purulent ophthalmia, trachoma;

corneal epithelium disintegration and sclera thinning;

Mode of administration and dosage

In mild infectious process the preparation is administered as intraconjunctival instillations by 1-2 drops every 4 hours. In case of severe infectious process the preparation is instilled q.h. As far as inflammatory processes attenuate the frequency of instillations decreases. Duration of treatment should not exceed 7 days, except for the cases of obvious disease improvement (dexamethasone can mask underlying infections, and continuous administration of gentamycin can contribute to stable flora development).

Side effect

Allergic reactions: irritation, burning, pain, pruritus, dermatitis.

In case of continuous administration of the preparation ocular hypertension with glaucoma symptom complex (if administer for more than 7 days regular intraocular tension measurement is recommended); posterior capsular cataract; cornea thinning and perforation; addiction of secondary (fungal) infection are likely.

Transient burning, lacrimation, conjunctiva hyperemia are likely immediately upon instillation.

Overdose

If administered locally overdose is negligible. Herewith, continuous administration can cause a systemic effect.

Symptoms: if administered locally side effect aggravation of the preparation’s ingredients are likely.

Treatment: withdraw the preparation and prescribe symptomatic therapy. There is no specific antidote.

Clinical particulars

Pregnancy and lactation: the preparation should be used in pregnancy and breastfeeding for 7-10 days (not more) only if the potential benefit justifies the possible risk to the fetus and mother.

Soft contact lens should be removed prior to the preparation administration, and worn not earlier than 15 minutes later.

Effect on ability to drive and use machines: the preparation is not recommended immediately prior to driving or using machines as lacrimation may occur.

During instillation the pipette tip should not touch the eye.

Interaction with other drug products

Gentamycin sulphate is an antibiotic of the aminoglycoside group which is characterized by nephro- and ototoxicity, in particular at high doses and in patients with renal and hepatic impairment. Concomitant administration with other antibiotics with by nephro- and ototoxical (streptomycin, monomycin, kanamycin, framycetin) should be avoided. Continuous concomitant administration with idoxuridine may accelerate destructive processes in the cornea epithelium.

Storage conditions

Store in protected from light place at temperature not above 25°C.

Keep away from children.

Shelf life

2 years.

Do not use after the expiration date specified on the package.

Store once-opened vial in the refrigerator at temperature from 2 to 8°C for 14 days.

Package

1 ml per dropping tube.

5 ml per bottle.

Each bottle or two dropping tubes with inserts are put in a package.

Pharmacy purchasing terms

Apply on doctor’s prescription.