Oftakvix eye drops 5 mg/ml bottle with dropper 5 ml

Instructions for use Oftakvix eye drops 5 mg/ml bottle with dropper 5 ml

Composition

active ingredient: levofloxacin;

1 ml of eye drops contains 5 mg of levofloxacin as levofloxacin hemihydrate;

Excipients: benzalkonium chloride, sodium chloride, concentrated hydrochloric acid, sodium hydroxide, water for injections.

Dosage form

Eye drops.

Main physicochemical properties: transparent, light yellow to light greenish-yellow solution, practically free from visible mechanical particles.

Pharmacotherapeutic group

Agents used in ophthalmology. Antimicrobial agents. Fluoroquinolones. Levofloxacin.

ATX code S01A E05.

Pharmacological properties

Pharmacodynamics

Levofloxacin is the L-isomer of the racemic drug substance ofloxacin. The antibacterial activity is predominantly that of the L-isomer of ofloxacin.

Mechanism of action.

Levofloxacin is a fluoroquinolone antibacterial agent that inhibits the activity of bacterial type II topoisomerases - DNA gyrase and topoisomerase IV. The action of levofloxacin in gram-negative bacteria is directed mainly at DNA gyrase, and in gram-positive bacteria - at topoisomerase IV.

Mechanisms of resistance.

There are two main mechanisms by which bacteria develop resistance to levofloxacin: a decrease in the concentration of the drug inside the bacterial cell or a change in the set of enzymes against which the drug acts. Such changes occur as a result of mutations in the chromosomal genes encoding DNA gyrase (gyrA and gyrB) and topoisomerase IV (parC and parE; grlA and grlB in Staphylococcus aureus). Resistance due to a decrease in the concentration of the drug inside the bacterial cell is caused by changes in the outer membrane porins (OmpF), which reduce the possibility of penetration of fluoroquinolones into gram-negative bacteria, or pumps that facilitate the efflux of substances. Resistance due to efflux of substances has been described in pneumococci (PmrA), staphylococci (NorA), anaerobic and gram-negative bacteria. In addition, plasmid-mediated resistance to quinolones (determined by the qnr gene) has been reported in Klebsiella pneumoniae and E. coli.

Cross-resistance.

Cross-resistance between fluoroquinolones is possible. A single mutation does not confer clinical resistance, but multiple mutations usually confer clinical resistance to all drugs in the fluoroquinolone class. Alterations in outer membrane porins and efflux systems can have broad substrate specificity, be directed against multiple classes of antibacterial agents, and lead to the emergence of multiple resistance.

Limit values.

The MIC (minimum inhibitory concentration) breakpoints that separate susceptible and moderately resistant organisms from resistant organisms according to the EUCAST (European Committee on Antimicrobial Susceptibility Testing) breakpoint are as follows:

Pseudomonas spp., Staphylococcus spp., Streptococcus A, B, C, G:

sensitive ≤ 1 mg/l, resistant > 2 mg/l;

Streptococcus pneumoniae: susceptible ≤ 2 mg/l, resistant > 2 mg/l;

Haemophilus influenzae, Moraxella catarrhalis: susceptible ≤ 1 mg/l, resistant > 1 mg/l.

Other pathogenic microorganisms: sensitive ≤ 1 mg/l, resistant > 2 mg/l.

Spectrum of antibacterial action.

The prevalence of acquired resistance in individual organisms may vary geographically and over time, and it is therefore desirable to have local information on resistance, especially when treating severe infections. Therefore, the information provided provides only approximate guidance and recommendations on the possible susceptibility or non-susceptibility of microorganisms to levofloxacin. As necessary, specialist advice should be sought if the prevalence of local resistance is such that the usefulness of the drug against at least some types of infections is questionable.

The table below only lists the types of bacteria that commonly cause external eye infections, such as conjunctivitis.

Antibacterial spectrum of activity: susceptibility categories and resistance characteristics according to EUCAST requirements.

* MSSA – methicillin-sensitive Staphylococcus aureus strains.

The resistance data presented in the table are based on the results of a multicenter observational study (ophthalmology study) on the prevalence of resistance among bacterial isolates obtained from patients with eye infections in Germany, June–November 2004.

Microorganisms were classified as susceptible to levofloxacin based on in vitro susceptibility and plasma concentrations after systemic therapy. Higher peak concentrations were achieved with topical administration than with plasma. However, it is unknown whether and how the kinetics of the drug after topical ocular administration may alter the antibacterial activity of levofloxacin.

Pediatric patients.

The pharmacodynamic properties are the same in adults and children aged 1 year and older.

Pharmacokinetics

After instillation into the eyes, levofloxacin is well preserved in the tear film.

In a study in healthy volunteers, the mean tear film concentrations of levofloxacin measured 4 and 6 hours after topical application were 17.0 and 6.6 μg/mL, respectively. Five of the six volunteers studied had concentrations of 2 μg/mL or greater at 4 hours post-dose. Four of the six volunteers studied had these concentrations at 6 hours post-dose.

Levofloxacin plasma concentrations were measured in 15 healthy adult volunteers at various time points during a 15-day course of treatment. The mean plasma levofloxacin concentration 1 hour after dosing ranged from 0.86 ng/mL on day 1 to 2.05 ng/mL on day 15. The highest maximum levofloxacin concentration of 2.25 ng/mL was observed on day 4 after 2 days of dosing every 2 hours (total of 8 doses per day). Maximum levofloxacin concentrations increased from 0.94 ng/mL on day 1 to 2.15 ng/mL on day 15, which is 1000-fold lower than the concentrations reported after standard oral doses of levofloxacin.

The plasma concentrations of levofloxacin achieved after application to the affected eye are unknown.

Indication

Topical treatment in patients aged 1 year and older of external bacterial ocular infections caused by microorganisms susceptible to levofloxacin.

Contraindication

Hypersensitivity to the active substance levofloxacin, hypersensitivity to other quinolones or to any of the components of the drug, such as benzalkonium chloride.

Interaction with other medicinal products and other types of interactions

No specific studies have been conducted on the interaction of this drug with other medications.

Since the maximum plasma concentrations of levofloxacin after instillation into the eyes are at least 1000 times lower than those observed after standard oral doses, the interactions noted for systemic use are unlikely to be clinically significant when using Oftaquix® eye drops.

Pediatric patients.

Drug interaction studies have not been conducted.

Application features

The drug should not be administered subconjunctivally. The solution should not be administered directly into the anterior chamber of the eye.

As with other anti-infectives, prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If the patient's condition worsens due to infection or if there is no clinical improvement within an appropriate period of time, the drug should be discontinued and an alternative treatment should be initiated.

As clinically indicated, the patient should be examined using magnifying devices, such as slit-lamp biomicroscopy and, if necessary, fluorescein staining.

The use of systemic fluoroquinolones has been associated with the occurrence of hypersensitivity reactions, even after a single dose. If an allergic reaction to levofloxacin occurs, the drug should be discontinued.

Tendon inflammation and rupture may occur with systemic fluoroquinolone therapy, including levofloxacin, especially in elderly patients receiving concomitant corticosteroids. Therefore, caution should be exercised and Oftakvix® should be discontinued at the first sign of tendon inflammation.

Oftaquix® contains benzalkonium chloride as a preservative. Before instillation, lenses should be removed and wait at least 15 minutes before reinsertion. Benzalkonium chloride may discolor soft contact lenses.

Patients with bacterial external eye infections should not wear contact lenses.

Benzalkonium chloride has been reported to cause eye irritation, dry eye symptoms and may affect the tear film and corneal surface. It should be used with caution in patients with dry eye and in patients who may have corneal damage. Patients should be monitored during prolonged use.

Use during pregnancy or breastfeeding

There are no adequate data from the use of levofloxacin in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive function. The potential risk to humans is unknown. Oftakvix® 5 mg/ml eye drops should be prescribed during pregnancy only if the expected benefit to the pregnant woman outweighs the potential risk to the fetus.

Breast-feeding.

Levofloxacin passes into breast milk. However, no effects on the breastfed child are expected when therapeutic doses of Oftakvix® are used. Oftakvix® eye drops should be used during breastfeeding only if the expected benefit to the mother justifies the potential risk to the infant.

Fertility.

Levofloxacin did not impair fertility in rats at exposures significantly in excess of the maximum human exposure following ophthalmic administration.

Ability to influence reaction speed when driving vehicles or other mechanisms

Oftakvix® has a minor influence on the ability to drive and use machines.

If any temporary visual effects are observed, the patient should wait until vision clears before driving or using machines.

Method of administration and doses

1-2 drops in the affected eye(s) every 2 hours up to 8 times a day, immediately upon awakening for the first 2 days, then 4 times a day from the 3rd to the 5th day.

When using different topical ophthalmic medications concurrently, the interval between instillations should be at least 15 minutes.

To prevent contamination of the pipette tip and solution, the pipette tip should not come into contact with the eyelids and areas around the eye.

The duration of treatment depends on the severity of the disorder, as well as the clinical and bacteriological course of the disease. Usually the duration of treatment is 5 days.

Safety and efficacy in the treatment of corneal ulcers and ophthalmia neonatorum have not been established.

Due to the lack of safety and efficacy data, Oftakvix® is not recommended for use in patients under 1 year of age.

Use in elderly patients.

There is no need to adjust the dose for elderly patients.

Method of application.

Ophthalmic use.

Children

The doses of the drug used in adults and children over 1 year of age are similar.

The safety and efficacy of Oftakvix® in children aged 1 year and older have been established.

The safety and efficacy of Oftakvix® in children under 1 year of age have not been established. There are no relevant data.

Overdose

The total amount of levofloxacin in a bottle of eye drops is too small to cause toxic effects after accidental oral administration. If necessary, the patient should be clinically examined and supportive measures should be taken. After local overdose of the drug, the eyes should be washed with clean water at room temperature.

Pediatric patients.

The measures taken in case of overdose are similar for adults and children aged 1 year and over.

Side effects

Adverse reactions can be expected in approximately 10% of patients. These reactions are usually mild to moderate, transient, and mainly confined to the eye area.

Since the product contains benzalkonium chloride, the active ingredient of this preservative may cause contact eczema and/or irritation.

The following adverse reactions are definitely, probably or possibly related to treatment and have been reported during clinical trials and post-marketing surveillance.

From the immune system.

Rare (≥1/10,000 - <1/1,000): extraocular ocular allergic reactions, including skin rash.

Rare (<1/10,000): anaphylaxis.

From the nervous system.

Uncommon (≥1/1000 - <1/100): headache.

From the organs of vision.

Common (≥1/100 - <1/10): burning in the eyes, decreased vision and the appearance of mucus streaks.

Uncommon (≥1/1000 - <1/100): eyelid opacification, chemosis, conjunctival papillary reaction, eyelid edema, ocular discomfort, foreign body sensation, ocular itching, ocular pain, conjunctival infection, conjunctival follicles, dry eye, eyelid erythema, and photophobia.

Corneal deposits were not observed during clinical studies.

On the part of the respiratory system, chest organs and mediastinum.

Uncommon (≥1/1000 - <1/100): rhinitis.

Rare (<1/10,000): laryngeal edema.

Additional adverse reactions observed with systemic use of the active substance (levofloxacin) and may potentially occur during the use of Oftakvix®.

Tendon ruptures of the shoulder, hand, Achilles, and other tendons requiring surgical intervention or resulting in long-term disability have been reported in patients receiving systemic fluoroquinolones. Postmarketing studies and experience with systemic quinolones have suggested that there may be an increased risk of rupture in patients receiving corticosteroids, particularly in the elderly, and in tendons under heavy load, including the Achilles tendon.

Pediatric patients.

The frequency, type and severity of adverse reactions in children are expected to be similar to those in adults.

Reporting suspected adverse reactions after a medicinal product has been authorised is important. This allows for continuous monitoring of the benefit/risk balance of the medicinal product. Doctors are asked to report any suspected adverse reactions.

Expiration date

3 years.

An opened bottle should be used within 1 month.

Storage conditions

Store in the original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Packaging

5 ml in a bottle with a dropper. 1 bottle in a cardboard box.

Vacation category

According to the recipe.

Producer

Santen Oy.

Location of the manufacturer and its business address

Kelloportinkatu 1, Tampere, 33100, Finland/Kelloportinkatu 1, Tampere, 33100, Finland