Instructions Floxal eye ointment 3 mg/g tube 3 g
Composition
active ingredient: ofloxacin;
1 g of eye ointment contains 3 mg of ofloxacin; one dose (1 cm strip of ointment) contains 0.12 mg of ofloxacin;
excipients: lanolin, white soft paraffin, liquid paraffin.
Dosage form
Eye ointment.
Main physicochemical properties: light yellow ointment of soft consistency.
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.
Limit values
Ofloxacin testing involves using conventional dilution series. The following minimum inhibitory concentrations have been established for susceptible and resistant bacteria:
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 |
| Non-species-specific threshold values* | ≤0.5 mg/l | >1 mg/l |
* Mostly based on serum pharmacokinetics.
The spectrum of effectiveness of ofloxacin includes obligate anaerobes, facultative anaerobes, aerobic and other microorganisms, such as chlamydia.
The prevalence of acquired resistance of certain species may vary locally over time. Therefore, especially when dealing with severe infections, local information on the resistance status is desirable. If local resistance raises doubts about the efficacy of ofloxacin, expert advice on treatment should be sought. In particular, in cases of severe infections or therapeutic failure, microbiological diagnosis should be obtained to confirm the pathogen and its susceptibility to ofloxacin. Chronic resistance to ofloxacin with other fluoroquinolones is possible.
The information below is based primarily on a current resistance study with 1391 isolates of ocular origin (mainly external smears) from 31 German centers. These data serve as the basis for the systematic application of the above breakpoints. For topical application of ofloxacin in the anterior segment of the eye, significantly higher antibiotic concentrations are achieved than with systemic application, so that clinical efficacy in the approved indications can also be provided for pathogens that have been identified as resistant, e.g. Enterococcus spp., during in vitro resistance determination.
Typically sensitive species
Gram-positive aerobes: Bacillus spp., Staphylococcus aureus (methicillin-sensitive),
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, Staphylococcus aureus (methicillin-resistant)1, 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 reached within 4 hours, which is sufficient to kill 100% of microorganisms.
Pharmacokinetics
Efficacy depends on the ratio of the maximum concentration of the drug in the tissues (Cmax) and the minimum inhibitory concentration (MIC) for the pathogen.
Animal experiments have shown that after topical application ofloxacin can be detected in the cornea, conjunctiva, ocular muscle, sclera, iris, ciliary body and anterior chamber of the eye. Repeated administration also leads to therapeutic concentrations in the vitreous.
After a single application of a strip of ointment approximately 1 cm long (equivalent to 0.12 mg of ofloxacin), maximum concentrations of ofloxacin in the conjunctiva (9.72 μg/g) and sclera (1.61 μg/g) are reached after 5 minutes. Then the concentrations slowly decrease.
After one hour, concentrations in the intraocular fluid and cornea reach maximum values of 0.69 μg and 4.87 μg, respectively.
Indication
Infections of the anterior segment of the eye caused by pathogenic microorganisms sensitive to ofloxacin: chronic conjunctivitis, keratitis, corneal ulcer and chlamydial infections.
Contraindication
Hypersensitivity to any of the components of the drug, other quinolones.
Interaction with other medicinal products and other types of interactions
Unknown. Drug interaction studies conducted with systemic ofloxacin showed that the clearance of caffeine and theophylline metabolites is slightly dependent on ofloxacin.
Application features
The safety and efficacy of the drug in children under 1 year of age have not been established. Severe and potentially fatal (anaphylactic and anaphylactoid) hypersensitivity reactions have been reported, sometimes after the first doses, in patients receiving systemic quinolones, including ofloxacin. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, throat and facial swelling), airway obstruction, dyspnea, urticaria and pruritus.
If an allergic reaction occurs when using ofloxacin, its use should be discontinued. Floxal® 3 mg/g in the form of eye ointment should be used with caution in patients who have already reacted hypersensitivity to other quinolone antibiotics. When using eye ointment containing ofloxacin, the risk of nasopharyngeal passage formation should be taken into account, which may lead to the emergence and development of bacterial resistance. As with other antibiotics, prolonged use may lead to the emergence of insensitive microorganisms.
If the infection worsens or clinical improvement is not observed within an appropriate time interval, the drug should be discontinued and alternative treatment initiated. There is limited evidence of the efficacy and safety of ophthalmic preparations containing 0.3% ofloxacin in the treatment of neonatal conjunctivitis. The use of ofloxacin ophthalmic preparations in neonates for the treatment of neonatal ophthalmia caused by Neisseria gonorrhoeae or Chlamydia trachomatis is not recommended as their use in this patient population has not been studied.
Clinical and nonclinical publications have reported the occurrence of corneal perforation in patients with corneal epithelial defects or corneal ulcers treated with topical fluoroquinolone antibiotics. However, many of these reports contain significant confounding factors such as older age, the presence of large ulcers, concomitant ocular disease (e.g., severe dry eye), systemic inflammatory disease (e.g., rheumatoid arthritis), or concomitant steroid or nonsteroidal anti-inflammatory drug administration. Nevertheless, given the risk of corneal perforation, caution should be exercised when administering this drug to patients with pre-existing corneal epithelial defects or corneal ulcers.
Corneal deposits have been reported with ofloxacin-containing ophthalmic preparations. However, no causal relationship can be proven.
During treatment with ofloxacin, excessive exposure to sunlight or ultraviolet radiation (e.g., solarium, sunlamps) should be avoided - photosensitivity is possible.
It is not recommended to wear contact lenses during the treatment of eye infections. Lanolin may cause skin irritation (e.g. contact dermatitis). 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 are possible. In case of worsening symptoms or lack of clinical improvement, treatment should be discontinued and alternative therapy should be used. 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 of the drug. Soft contact lenses should not be worn during treatment with Floxal®, eye ointment. Floxal®, eye ointment should be used together with other eye drops/eye ointments no earlier than 15 minutes after using another drug. In any case, eye ointment should be used last.
Tendonitis and tendon rupture may occur with systemic fluoroquinolone therapy, particularly in elderly patients and those receiving concomitant corticosteroid therapy. Therefore, caution should be exercised and treatment with Floxal® eye ointment should be discontinued at the first sign of tendonitis (see section 4.8).
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).
Use during pregnancy or breastfeeding
Despite the lack of evidence of any embryotoxic effects, Floxal® eye ointment should not be used during pregnancy or breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
After instillation into the conjunctival sac of the eye, the drug may cause loss of visual acuity for several minutes. Until visual acuity is restored, patients should refrain from driving or operating other mechanisms.
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 age of the patient. Unless otherwise prescribed, adults and children (from 1 year of age) are injected into the conjunctival sac of the affected eye with a 1 cm strip of ointment (equivalent to 0.12 mg of ofloxacin) 3 times a day (for chlamydial infections - 5 times a day). Treatment with Floxal®, eye ointment, should not exceed 2 weeks.
Instructions for use.
Carefully pull the lower eyelid down and, by slightly pressing on the tube, inject the required amount of ointment into the conjunctival sac. Then close the eyelid and, gently pressing on the eyeball in different directions, evenly distribute the drug.
Note: If you are using other eye drops/eye ointments, leave 15 minutes between applications, always apply the ointment last.
Children
Floxal® eye ointment can be prescribed to children from 1 year of age.
Overdose
There have been no reports of overdose cases to date.
Treatment is symptomatic, it is necessary to 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 following systemic use of ofloxacin are rare, and 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.
Immune system disorders: Rare: conjunctival redness and/or mild burning sensation in the eye. In most cases, these symptoms are short-lived. Very rare (<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.
On the part of the organs of vision. Often: eye discomfort, eye irritation;
Rare: keratitis, conjunctivitis, blurred vision, photophobia, eye swelling, eye redness, foreign body sensation, increased lacrimation, dry eyes, eye pain, itching, eyelid swelling. In rare cases (from 1/10,000 to 1/1,000), corneal deposits may occur, especially in the presence of a history of corneal diseases.
There are reports that reactions such as toxic epidermal necrosis and Stevens-Johnson syndrome have occurred very rarely with topical application. A causal relationship with Floxal® eye ointment 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.
The product contains lanolin, which may cause contact dermatitis.
Tendon ruptures of the shoulder, hand, 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 fluoroquinolones suggest that the risk of such ruptures may be increased in patients receiving corticosteroids, particularly in the elderly, and in patients with high tendon loads, particularly the Achilles tendon.
Expiration date
The shelf life of the drug is 3 years.
The shelf life after opening the tube is 6 weeks.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store at a temperature not exceeding 25 °C, out of the reach of children.
Packaging
3 g of ointment in a laminated tube with a plastic tip and screw cap.
One tube in a cardboard box.
Vacation category
According to the recipe.
Producer
Dr. Gerhard Mann Chem.-Pharm. Fabrik GmbH, Germany.
Address
Brunsbütteler Damm 165/173, 13581 Berlin, Germany.
