Properties
What is it?
Trade name of the preparation: Aifloxi® International Nonproprietary Name: Levofloxacin Dosage form: Eye drops, solution Composition: 1 ml of solution contains: Active substance: 5.12 mg Levofloxacin hemihydrate, equivalent to 5 mg Levofloxacin. Excipients: Benzalkonium chloride; Sodium chloride; Sodium hydroxide or hydrochloric acid (for pH adjustment); Water for injection. Description: Clear, greenish-yellow solution. Pharmacotherapeutic group: Antibacterial ophthalmic preparations, fluoroquinolones. ATC code: S01AE05 Pharmacological properties Pharmacodynamics Levofloxacin is the L-isomer of the racemic medicinal substance ofloxacin. The antibacterial activity of ofloxacin is mainly due to the L-isomer. As an antibacterial drug of the fluoroquinolone group, levofloxacin inhibits bacterial topoisomerases of type II - DNA gyrase and topoisomerase IV. The primary target of levofloxacin is DNA gyrase in Gram-negative bacteria and topoisomerase IV in Gram-positive bacteria. Resistance may vary geographically and over time; it is desirable to have local information on resistance, especially when treating severe infections. Therefore, the information presented is only an approximate indication of whether microorganisms will be susceptible to levofloxacin. The table lists only bacterial species that typically cause infections of the outer part of the eye, such as conjunctivitis. Antibacterial spectrum – susceptibility category and resistance characterization are given according to EUCAST Category I: Usually susceptible species Aerobic Gram-positive microorganisms Staphylococcus aureus (MSSA)* Streptococcus pneumoniae Streptococcus pyogenes Viridans group streptococci Aerobic Gram-negative microorganisms Escherichia coli Haemophilus influenzae Moraxella catarrhalis Pseudomonas aeruginosa (non-hospital isolates) Other microorganisms Chlamydia trachomatis (treatment of patients with chlamydial conjunctivitis requires concomitant systemic antimicrobial treatment) Category II: Species for which acquired resistance may be a problem Aerobic Gram-positive microorganisms Staphylococcus aureus (MRSA)** Staphylococcus epidermidis Aerobic Gram-negative microorganisms Pseudomonas aeruginosa (hospital isolates) * MSSA = Methicillin-susceptible strains of Staphylococcus aureus ** MRSA = Methicillin-resistant strains of Staphylococcus aureus Pharmacodynamic data are similar in adults and children over 1 year of age. Pharmacokinetics After instillation into the eye, levofloxacin is well retained in the tear film. Studies in healthy volunteers showed that the mean concentration of levofloxacin measured in the tear film 4 and 6 hours after topical application was 17.0 mcg/ml and 6.6 mcg/ml, respectively. In five out of six subjects, the levofloxacin concentration was 2 mcg/ml or more 4 hours after instillation. In four out of six subjects, this concentration was maintained 6 hours after instillation. Levofloxacin concentration in plasma was measured in 15 healthy adult volunteers at different time points during a 15-day course of treatment with the preparation. The mean plasma concentration of levofloxacin 1 hour after administration ranged from 0.86 ng/ml to 2.05 ng/ml on day 15. The maximum plasma concentration of levofloxacin of 2.25 ng/ml was observed on day 4, after administration every 2 hours for 2 days (a total of 8 times per day). The maximum levofloxacin concentration increased from 0.94 ng/ml on day 1 to 2.15 ng/ml on day 15, which is 1000 times lower than after standard oral doses of levofloxacin. Plasma concentrations of levofloxacin achieved after administration into an infected eye are not yet known. Indications Aifloxi is indicated for the local treatment of superficial bacterial infections of the eye caused by microorganisms susceptible to levofloxacin in patients over 1 year of age. Aifloxi is indicated in adults, children aged 1 to 12 years, and adolescents aged 12 to 18 years. Dosage and administration of Aifloxi For all patients: During the first two days, during the period of wakefulness - 1-2 drops in the affected eye every 2 hours, 8 times a day, and from the 3rd to the 5th day - 4 times a day. If other local ophthalmic preparations are used simultaneously, an interval of at least 15 minutes must be observed between instillations. To avoid contamination of the dropper and solution, the dropper should not touch the eyelids and surrounding areas. The duration of treatment depends on the severity of the disease and the clinical and bacteriological course of the infection. Usually, the duration of treatment is 5 days. Safety and efficacy have not been established for the treatment of corneal ulcers and neonatal ophthalmia. The use of the preparation is not recommended in children under one year of age due to lack of safety and efficacy data. Dose adjustment is not required in elderly patients. Children Dosage is the same in adults and children over 1 year of age. Safety and efficacy of Aifloxi in children under one year of age have not been established. Data are not available. Use in the elderly Dose adjustment is not required. Method of administration For topical use, for instillation into the eye. Side effects Side effects may occur in approximately 10% of patients. Side effects are mostly mild or moderate, transient, and generally limited to ocular reactions. Since the preparation contains benzalkonium chloride, contact dermatitis and/or eye irritation may be caused by both the active substance and this preservative. Frequency categories of side effects are defined as: Frequent (≥1/100 - <1/10); Infrequent (≥1/1,000 - <1/100); Rare (≥1/10,000 - <1/1,000); Very rare (<1/10,000): Immune system disorders Rare: Extraocular allergic reactions, including rash. Very rare: Anaphylaxis. Nervous system disorders: Infrequent: Headache Eye disorders: Frequent: Eye burning, blurred vision, and mucous strands. Infrequent: Blepharitis, chemosis, conjunctival papillary reaction, eyelid edema, eye discomfort, eye itching, eye pain, conjunctival hyperemia, conjunctival follicle formation, dry eye, eyelid erythema, and photophobia. Corneal precipitates were not detected in clinical trials. Respiratory, thoracic and mediastinal disorders Infrequent: Rhinitis Very rare: Laryngeal edema In children, the frequency, type, and severity of adverse reactions are likely to be the same as in adults. Contraindications of Aifloxi Hypersensitivity to the active substance, other quinolones, or any of the excipients, such as benzalkonium chloride. Interactions with other medicinal products and other types of interactions No specific studies on drug interactions have been conducted. Since the maximum plasma concentration of levofloxacin after topical ocular administration is 1000 times lower than after standard oral doses, interactions characteristic of systemic administration are unlikely to be clinically significant. When used simultaneously with other local ophthalmic preparations, an interval of at least 15 minutes must be observed between instillations. In children, no studies on interactions have been conducted. Overdose The total amount of levofloxacin in the vial is too small to cause toxic effects if accidentally ingested orally. In case of overdose with topical use of Aifloxi, rinse the eyes with running clean water at room temperature. In case of overdose in children over 1 year of age, the actions to be taken are the same as in adults. Fertility, pregnancy and lactation Pregnancy There is insufficient data on the use of levofloxacin in pregnant women. Animal studies do not indicate direct or indirect harmful effects on reproductive toxicity. The potential risk to humans is unknown. Aifloxi may be prescribed during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus. Breastfeeding Levofloxacin is excreted in breast milk. However, when used at therapeutic doses, no effect on the breastfed infant is expected. Aifloxi may be prescribed during lactation only if the expected benefit to the mother outweighs the potential risk to the breastfed infant. Fertility Levofloxacin did not affect fertility in rats at doses significantly exceeding the maximum human dose for ophthalmic use. Warnings and precautions Aifloxi should not be administered subconjunctivally or directly into the anterior chamber of the eye. Systemic fluoroquinolones, even with a single dose, can cause allergic reactions. If an allergic reaction to levofloxacin occurs, discontinue the use of Aifloxi. As with other anti-infective agents, prolonged use may lead to overgrowth of resistant microorganisms, including fungi. If infection worsens or if there is no clinical improvement after a certain period, discontinue the use of Aifloxi and initiate alternative treatment. Aifloxi contains benzalkonium chloride, which may cause eye irritation and discolor contact lenses. Remove contact lenses before using the preparation. Reinsertion of lenses is permitted no earlier than 15 minutes after using the preparation. Patients with external eye infections should not wear contact lenses. Warnings and precautions for children over 1 year of age are the same as for adults. Effect on ability to drive and use machines Aifloxi has a negligible effect on the ability to drive and use machines. If there are any transient effects on vision, the patient should be advised to wait for vision to recover before driving or operating machinery. Incompatibility No studies on incompatibility have been conducted, therefore mixing Aifloxi with other preparations is not allowed. Packaging 5 ml sterile solution in a vial (LDPE), 1 vial together with instructions for use is placed in a cardboard box. Storage conditions Store at a temperature not exceeding 25°C. Keep out of reach of children. Shelf life 3 years. After the first opening of the vial, it can be used for 4 weeks. Dispensing category: Pharmaceutical product group III, available without a prescription. See also: Levofta - Levofta eye drops 5mg/ml 5ml
