Oftaquix^® (Drops) Instructions for Use

Marketing Authorization Holder

Santen, Oy (Finland)

Manufactured By

Nextpharma, Oy (Finland)

Labeled By

Manufacturing Packaging Farmaca, MPF B.V. (Netherlands)

Quality Control Release

SANTEN, OY (Finland)

Contact Information

SANTEN LLC (Russia)

ATC Code

S01AE05 (Levofloxacin)

Active Substance

Levofloxacin (Rec.INN registered by WHO)

Dosage Form

Oftaquix®

Eye drops 5 mg/1 ml: bottle 5 ml with dropper tip

Dosage Form, Packaging, and Composition

Eye drops in the form of a light yellow or light greenish-yellow solution.

Excipients : benzalkonium chloride – 0.05 mg, sodium chloride – 9 mg, hydrochloric acid – q.s., sodium hydroxide – q.s., purified water – up to 1 ml.

5 ml – polyethylene bottles (1) with a dropper tip – cardboard packs.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group for topical use in ophthalmology

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

Antimicrobial drug from the fluoroquinolone group.

Levofloxacin is the L-isomer of the racemic drug substance ofloxacin. The antibacterial activity of ofloxacin is attributed mainly to the L-isomer.

Levofloxacin blocks DNA gyrase and topoisomerase IV, disrupts DNA supercoiling and cross-linking of breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall, and membranes.

Active against gram-negative aerobes Branhamella (Moraxella) cataralis, Haemophilus influenzae, Neisseria gonorrhoeae, Pseudomonas aeruginosa; gram-positive aerobes Staphyloccocus aureus, Streptococcus pneumoniae, Streptococcus pyogenes.

Pharmacokinetics

After instillation into the eye, Levofloxacin is well retained in the tear film.

Studies in healthy volunteers have shown that the mean concentrations of levofloxacin in the tear film, measured 4 and 6 hours after topical application, were 17 µg/ml and 6.6 µg/ml, respectively.

In five out of six subjects, levofloxacin concentrations were 2 µg/ml and above 4 hours after instillation. In four out of six subjects, this concentration persisted 6 hours after instillation.

The mean concentration of levofloxacin when using Oftaquix^® eye drops in the aqueous humor is statistically significantly (p=0.0008) higher than the mean concentration of ofloxacin (1139.9±717.1 ng/ml and 621.7±368.7 ng/ml, respectively).

The mean concentration of levofloxacin in blood plasma 1 hour after application is from 0.86 ng/ml to 2.05 ng/ml.

The C_max of levofloxacin in plasma, equal to 2.25 ng/ml, was detected on the fourth day after 2 days of using the drug every 2 hours up to 8 times/day.

The C_max of levofloxacin, reached on the fifteenth day, was more than 1000 times lower than the concentration observed after oral administration of standard doses of levofloxacin.

Indications

• Treatment of superficial bacterial infections of the eye in patients aged 1 year and older;
• Prevention of complications after surgical and laser operations on the eye.

ICD codes

Dosage Regimen

Instill topically into the conjunctival sac of the affected eye.

For treatment of bacterial infections: administer 1-2 drops into the affected eye every 2 hours while awake during the first two days, up to a maximum of 8 times per day.

From the third to the fifth day of treatment, reduce the frequency to 1-2 drops into the affected eye 4 times per day.

The typical treatment course duration is 5 days; the physician will determine the final duration based on clinical response.

For surgical prophylaxis: follow the specific instillation schedule prescribed by the ophthalmologist, typically involving a series of drops prior to and immediately following the procedure.

When using multiple topical ophthalmic products, maintain an interval of at least 15 minutes between instillations.

To prevent contamination of the solution, avoid contact between the dropper tip and the eye, eyelids, or any other surface.

Do not wear soft contact lenses during treatment due to the presence of benzalkonium chloride.

Adverse Reactions

Side effects may occur in approximately 10% of patients.

Common (1-10%) burning sensation in the eye, decreased visual acuity, appearance of mucous strands.

Uncommon (0.1-1%) blepharitis, chemosis, conjunctival papillae, eyelid edema, eye discomfort, eye itching, eye pain, conjunctival hyperemia, conjunctival follicles, dry eye syndrome, eyelid erythema, eye irritation, contact dermatitis, photophobia and allergic reactions.

Other: during clinical trials – headache, rhinitis.

Contraindications

• Pregnancy;
• Lactation period (breastfeeding);
• Hypersensitivity to quinolone drugs;
• Hypersensitivity to the components of the drug.

Use with caution in children.

Use in Pregnancy and Lactation

Oftaquix^® eye drops are contraindicated during pregnancy and lactation (breastfeeding).

Pediatric Use

Use with caution in children.

Special Precautions

Oftaquix^® eye drops should not be administered subconjunctivally or directly into the anterior chamber of the eye.

When using other ophthalmic agents simultaneously, the interval between instillations should be at least 15 minutes.

Due to the presence of benzalkonium chloride in the composition, the eye drops should not be used while wearing hydrophilic (soft) contact lenses.

To avoid contamination of the dropper tip and the solution, do not touch the dropper tip to the periocular tissues.

Overdose

The total amount of levofloxacin contained in one bottle of eye drops is too small to cause toxic reactions even after accidental ingestion. After topical application of an excessive dose of Oftaquix^® eye drops, the eye should be rinsed with clean (tap) water at room temperature.

Drug Interactions

No specific studies on the interaction of Oftaquix^® eye drops have been conducted. Since the maximum concentration of levofloxacin in plasma after topical application in the eye is at least 1000 times lower than after oral administration of standard doses, interactions with other drugs characteristic of systemic use are most likely clinically insignificant.

Storage Conditions

The drug should be stored out of the reach of children at a temperature below 25°C (77°F).

Shelf Life

Shelf life – 3 years.

After opening the bottle, the shelf life is 1 month.

Dispensing Status

The drug is dispensed by prescription.

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.