Instructions Floxal eye drops solution 3 mg/ml bottle with dropper 5 ml
Composition
active ingredient: ofloxacin;
1 ml of solution contains 3 mg of ofloxacin; 1 drop contains 0.1 mg of ofloxacin;
Excipients: benzalkonium chloride, hydrochloric acid, sodium hydroxide, sodium chloride, water for injections.
Dosage form
Eye drops, solution.
Main physicochemical properties: transparent, yellowish aqueous solution.
Pharmacotherapeutic group
Drugs used in ophthalmology. Antimicrobials. Ofloxacin.
ATX code S01A E01.
Pharmacological properties
Pharmacodynamics.
Ofloxacin, a quinolone acid derivative, is a fluoroquinolone (gyrase inhibitor), an antibiotic that has a bactericidal effect.
Threshold values
Ofloxacin was tested using a dilution series. Minimum inhibitory concentrations were determined for susceptible and resistant bacteria (see table).
EUCAST (European Committee on Antimicrobial Susceptibility Testing) breakpoints
| Pathogen | Sensitive | Resistant |
| Enterobacteriaceae | ≤0.5 mg/l | >1 mg/l |
| Staphylococcus spp. | ≤1 mg/l | >1 mg/l |
| Streptococcus pneumoniae | ≤0.125 mg/l | >4 mg/l |
| Haemophilus influenzae | ≤0.5 mg/l | >0.5 mg/l |
| Moraxella catarrhalis | ≤0.5 mg/l | >0.5 mg/l |
| Neisseria gonorrhoeae | ≤0.12 mg/l | >0.25 mg/l |
| Threshold values not specific to species* | ≤0.5 mg/l | >1 mg/l |
*Mostly determined based on serum pharmacokinetics.
Antibacterial spectrum
The spectrum of action of ofloxacin includes obligate anaerobes, facultative anaerobes, aerobes and other microorganisms such as Chlamydia.
The prevalence of acquired resistance to individual species may vary by location and over time, so obtaining local information on resistance is essential for appropriate treatment of severe infections.
Microbiological determination of the type of pathogens and their sensitivity to ofloxacin is mandatory in case of severe infections or lack of therapeutic effect of treatment. Cross-resistance of ofloxacin to other fluoroquinolones is possible.
The information below is taken from a resistance study conducted using 1391 isolates from test eyes (mainly external washes) from 31 centers in Germany.
This study provides representative data on the aerobes that cause eye infections in Germany. It can be assumed that the prevalence of bacteria that can cause ophthalmic diseases in other countries will not be identical, but will be similar, and therefore the bacteria listed below are the most common causes of bacterial infections of the external part of the eye.
Resistance data refer to systemic use. Local ocular administration achieved significantly higher concentrations of the antibiotic, so clinical efficacy is observed even with pathogens that have been identified as resistant in laboratory studies. This effect is observed, for example, with Enterococcus species.
Typically sensitive species
Gram-positive aerobes: Bacillus spp., methicillin-susceptible Staphylococcus aureus,
Gram-negative aerobes: Acinetobacter baumannii, Acinetobacter lwoffi, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Serratia marcescens.
Species that may be insensitive to the drug due to acquired resistance
Gram-positive aerobes: Corynebacterium spp., Enterococcus faecalis, methicillin-resistant1 Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae2, streptococci (except Streptococcus pneumoniae)2.
Gram-negative aerobes: Pseudomonas aeruginosa, Stenotrophomonas maltophilia.
Species naturally resistant to the drug
Gram-positive aerobes: Enterococcus spp.
1 Resistance rate exceeds 50% in at least one region.
2 The natural sensitivity of most individual species is in the medium range. However, in tear fluid, after a single instillation, a concentration of at least 4 mg/l is achieved within 4 hours, which is sufficient to kill 100% of microorganisms.
Pharmacokinetics.
Efficacy largely depends on the ratio of the maximum tissue concentration (Cmax) and the minimum inhibitory concentration (MIC) of the pathogen.
Animal experiments have shown that after topical application of ofloxacin can be detected in the cornea, conjunctiva, ocular muscle, sclera, iris, ciliary body and anterior chamber of the eye. With repeated use, the drug accumulates in therapeutic concentrations in the vitreous.
By analogy with the results of animal studies, it can be assumed that other ocular tissues contain higher concentrations of the drug than the intraocular fluid. Since ofloxacin can bind to tissues containing melanin, a slower excretion of substances from these tissues should be expected. The half-life of ofloxacin from plasma with its systematic use is from 3.5 to 6.7 hours.
Indication
Infections of the anterior segment of the eye caused by pathogenic microorganisms sensitive to ofloxacin, such as bacterial inflammations of the conjunctiva, cornea, eyelid margins and lacrimal sac; barley and corneal ulcer.
Contraindication
Hypersensitivity to any of the components of the drug, other quinolones.
Interaction with other medicinal products and other types of interactions
Not yet known. Drug interaction studies conducted with systemic ofloxacin have shown that the clearance of caffeine and theophylline metabolites is only slightly dependent on ofloxacin.
Application features
Safety and effectiveness for children under 1 year of age have not been proven.
There is only limited evidence of the efficacy and safety of 0.3% ofloxacin eye drops in the treatment of conjunctivitis in newborns.
The use of ofloxacin-containing eye drops in neonates for the treatment of ophthalmia neonatorum caused by Neisseria gonorrhoeae or Chlamydia trachomatis is not recommended as administration has not been performed in this age group.
If an allergic reaction to the drug develops, it is necessary to discontinue its use.
Before the first administration of the drug, it is advisable to conduct a microbiological examination of smears taken from the conjunctival sac to determine the sensitivity of bacterial strains to the drug.
With prolonged use, bacterial resistance and the formation of microorganisms insensitive to the antibacterial agent may develop. In case of worsening symptoms or lack of clinical improvement, treatment should be discontinued and alternative therapy should be used.
Corneal perforation has been reported in patients with corneal epithelial defects or corneal ulcers treated with topical fluoroquinolone antibiotics. However, in many cases, risk factors such as older age, the presence of large ulcers, concomitant ocular disease (e.g., severe dry eyes), systemic inflammatory disease (e.g., rheumatoid arthritis), or concomitant use of steroids or nonsteroidal anti-inflammatory drugs were present. Nevertheless, due to the risk of corneal perforation, caution should be exercised when using this medicinal product in patients with pre-existing corneal epithelial defects or corneal ulcers.
During treatment with Ofloxacin, excessive tanning or ultraviolet light (e.g., solarium, sunlamps, etc.) should be avoided - photosensitivity is possible.
Hard contact lenses should not be worn during treatment. Therefore, it is recommended to remove hard lenses before using the drug and put them back on no earlier than 20 minutes after instillation.
The drug contains the preservative benzalkonium chloride, which may cause conjunctival irritation.
When using Floxal® eye drops together with other eye drops/eye ointments, the medications should be applied at least 15 minutes apart. In any case, the eye ointment should be applied last.
When using fluoroquinolones systemically, the drug should be used with caution in patients at risk of QT interval prolongation, namely: with congenital QT interval prolongation syndrome, with concomitant use of drugs that prolong the QT interval (e.g., class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics), with uncorrected electrolyte balance (e.g., hypokalemia, hypomagnesemia), elderly patients, patients with cardiac diseases (e.g., heart failure, myocardial infarction, bradycardia).
Tendonitis and rupture may occur with systemic fluoroquinolone therapy, including ofloxacin, particularly in elderly patients and patients receiving concomitant corticosteroids. Therefore, caution should be exercised and treatment with Floxal® eye drops should be discontinued at the first sign of tendonitis.
Benzalkonium chloride may be absorbed by soft contact lenses and may discolour contact lenses. Contact lenses should be removed before instillation of this medicinal product and reinserted 20 minutes later. Benzalkonium chloride may also cause eye irritation, particularly in the presence of dry eyes or corneal disorders. Limited data suggest that there is no difference in the adverse event profile in children compared to adults. However, children's eyes are generally more sensitive to benzalkonium chloride than adults. Irritation may affect treatment recommendations for children. 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 eyes and in patients where the cornea may be compromised. Patients should be monitored during prolonged use.
Use during pregnancy or breastfeeding
Despite the lack of evidence of any embryotoxic effects, Floxal® eye drops should, if possible, not be used during pregnancy or breastfeeding.
The ability to influence the reaction speed when driving or working with other mechanisms
The use of Floxal® eye drops does not affect the patient's reaction speed.
After instillation of the drug into the conjunctival sac of the eye, blurred vision may occur for several minutes. While vision is blurred, patients should refrain from driving or operating other machinery.
Method of administration and doses
The dose of the drug and the duration of treatment are always determined by the doctor depending on the severity of the disease and the patient's age.
Unless otherwise prescribed, Floxal® eye drops should be instilled into the conjunctival sac of the affected eye 1 drop 4 times daily. The duration of treatment with Floxal® eye drops should not exceed 2 weeks.
Instructions for use
Carefully pull the lower eyelid down and, by lightly pressing the dropper bottle, instill 1 drop into the conjunctival sac of the affected eye.
Children
Floxal® eye drops can be prescribed to children from 1 year of age.
Overdose
There have been no reports of overdose cases to date.
Treatment is symptomatic, immediately rinse the eye(s) with water.
Side effects
Immediately after administration of the drug, blurred vision may occur for several minutes.
General manifestations.
Serious reactions after systemic use of ofloxacin are rare, most symptoms are reversible. Although only a small amount of ofloxacin is absorbed into the systemic circulation after topical application, the possibility of the reported side effects cannot be excluded.
From the immune system.
Sometimes there is redness of the conjunctiva and/or a slight burning sensation in the eye. In most cases, these symptoms are short-lived.
In very rare cases (<1/10,000): hypersensitivity, including angioedema, shortness of breath, anaphylactic reactions/shock, swelling of the oropharynx and tongue, itching of the eyes and eyelids.
From the nervous system: in rare cases - dizziness.
From the organs of vision.
Common: eye discomfort, eye irritation.
Sometimes: keratitis, conjunctivitis, blurred vision, photophobia, eye swelling, eye redness, foreign body sensation, increased lacrimation, dry eyes, eye pain, itching, eyelid swelling.
In rare cases (1/10,000 to 1/1,000), corneal deposits may occur, especially if there is a history of corneal disease.
There are reports that, with topical application, reactions such as toxic epidermal necrolysis and Stevens-Johnson syndrome have occurred very rarely. A causal relationship with Floxal® eye drops has not been established for these manifestations.
On the part of the digestive tract: in rare cases - nausea.
Skin and subcutaneous tissue disorders: in rare cases - facial edema, periorbital edema.
Serious, sometimes fatal, hypersensitivity reactions, sometimes after the first dose, have been observed with systemic use of quinolones.
Fractures of the shoulder, arm, Achilles tendon, or other tendons requiring surgical repair or resulting in long-term disability have been reported in patients receiving systemic fluoroquinolones. Studies and post-marketing experience with systemic quinolones suggest that the risk of these ruptures may be increased in patients receiving corticosteroids, particularly in the elderly, and that this risk primarily affects tendons that are under high stress, including the Achilles tendon.
Expiration date
The shelf life of the drug in a closed bottle is 3 years.
Shelf life after opening the bottle is 6 weeks.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C, out of the reach of children.
Packaging
5 ml of the drug in a bottle with a dropper and a screw cap. One bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
Dr. Gerhard Mann Chem.-Pharm. Factory LLC
Address
Brunsbütteler Damm 165/173, 13581 Berlin, Germany.
