Storage
active substance: ofloxacin;

1 g of eye ointment contains 3 mg of ofloxacin; one dose (1 cm strip of ointment) contains 0.12 mg ofloxacin;

excipients: lanolin, white soft paraffin, liquid paraffin.

Medicinal form
Eye ointment.

Main physicochemical properties: light yellow ointment of soft consistency.

Pharmacotherapeutic group
Means used in ophthalmology. Antimicrobial agents. Ofloxacin. ATX code S01A E01.

Pharmacodynamics
Ofloxacin, a derivative of quinolic acid, is a fluoroquinolone (gyrase inhibitor), an antibiotic that has a bactericidal effect.

Limit values

Ofloxacin testing consists of using conventional dilution series. The following minimum inhibition concentrations have been established for sensitive and resistant bacteria:

EUCAST (European Committee for Antimicrobial Susceptibility Testing) cut-off values:

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 thresholds* ≤0.5 mg/l >1 mg/l
* Mainly based on serum pharmacokinetics.

The spectrum of effectiveness of ofloxacin includes obligate anaerobes, facultative anaerobes, aerobics and other microorganisms such as chlamydia.

The prevalence of acquired resistance in certain species may vary locally over time. Therefore, especially when dealing with severe infections, local information on the state of resistance is desirable. If the efficacy of ofloxacin is in doubt because of local resistance, expert therapeutic advice should be sought. In particular, in the case of severe infections or therapeutic failure, a microbiological diagnosis should be obtained with confirmation of the pathogen and its sensitivity to ofloxacin. Chronic resistance to ofloxacin with other fluoroquinolones is possible.

The information below is based primarily on a modern resistance study with 1,391 isolates of ocular origin (mostly external smears) from 31 German centers. These data serve as the basis for the systematic application of the above limit values. For topical use of ofloxacin in the anterior part of the eye, a significantly higher concentration of the antibiotic is achieved than in the case of systemic use, so clinical efficacy in the approved indications can also be provided for pathogens that have been determined to be resistant, e.g. Enterococcus spp., during the determination of in vitro resistance to in vitro.

Usually sensitive species:

Gram-positive aerobes: Bacillus spp., Staphylococcus aureus (sensitive to methicillin),

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, due to acquired resistance, may be insensitive to the use of the drug

Gram-positive aerobes: Corynebacterium spp., Enterococcus faecalis, Staphylococcus aureus (resistant to methicillin)1, Staphylococcus epidermidis, Streptococcus pneumoniae2, streptococci (except Streptococcus pneumoniae)2.

 Gram-negative aerobes: Pseudomonas aeruginosa, Stenotrophomonas maltophilia.

Species with natural resistance to the drug

Gram-positive aerobes: Enterococcus spp.

1 The level of resistance exceeds 50% in at least one region.

2 The natural sensitivity of most individual species lies in the middle range. However, in tear fluid, after one instillation, a concentration of at least 4 mg/l is reached within 4 hours, which is enough to kill 100% of microorganisms.

Pharmacokinetics
The effectiveness depends on the ratio of the maximum concentration of the drug in the tissues (C max) and the minimum inhibitory concentration (MIC) for the pathogen.

Experiments on animals have shown that after topical application, ofloxacin can be detected in the cornea, conjunctiva, eye muscle, sclera, iris, ciliary body and in the anterior chamber of the eye. Repeated administration also results in 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), the maximum concentrations of ofloxacin in the conjunctiva (9.72 mcg/g) and sclera (1.61 mcg/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 pathogens sensitive to ofloxacin: chronic conjunctivitis, keratitis, corneal ulcers 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 Studies of drug interaction, carried out with systemic application 

and ofloxacin, showed that the clearance of caffeine and theophylline metabolites depends to a small extent on ofloxacin.

Features of application
The safety and efficacy of the drug in children under 1 year of age have not been proven. There have been reports of severe and potentially fatal (anaphylactic and anaphylactoid) hypersensitivity reactions, sometimes after the first doses, in patients receiving quinolones, including ofloxacin, systemically. Some reactions have been associated with cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal, and facial edema), airway obstruction, dyspnoea, urticaria, and pruritus. If an allergic reaction occurs when using ofloxacin, its use should be stopped. Floxal 3 mg/g in the form of an eye ointment should be used with caution in patients who have already reacted hypersensitivity to other antibiotics - quinolones. When using an eye ointment containing ofloxacin, the risk of nasopharyngeal passage should be taken into account, which can lead to the emergence and development of bacterial resistance. As with other antibiotics, long-term use can lead to the emergence of non-susceptible microorganisms. If the infection worsens or clinical improvement is not observed within an appropriate time interval, the drug should be discontinued and an alternative treatment should be initiated. There is only 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 group of patients has not been studied. Clinical and non-clinical publications have reported the occurrence of corneal perforation in patients with corneal epithelial deficiency or corneal ulcers treated with topical fluoroquinolone antibiotics. However, many of these reports contain significant confounding factors such as older age, presence of large ulcers, concomitant ocular disease (eg, severe dry eye), systemic inflammatory disease (eg, rheumatoid arthritis), or concomitant administration of steroids or nonsteroidal anti-inflammatory drugs. medicines. However, given the risk of corneal perforation, caution should be exercised when administering this medicinal product to patients with pre-existing corneal epithelial defects or corneal ulcers. When using ophthalmic drugs containing ofloxacin, a deposit on the cornea was recorded. However, no causal relationship can be proven. During treatment with ofloxacin, excessive exposure to sunlight or ultraviolet radiation (for example, tanning beds, sun lamps) should be avoided - photosensitivity is possible. It is not recommended to use contact lenses while treating an eye infection. Lanolin can cause skin irritation (e.g. contact dermatitis). Before the first administration of the drug, it is advisable to conduct a microbiological examination of swabs taken from the conjunctival sac to determine the sensitivity of bacterial strains to the drug. With long-term use, the formation of bacterial resistance and the formation of microorganisms insensitive to the antibacterial agent are possible. If symptoms worsen or there is no clinical improvement, treatment should be discontinued and alternative therapy should be considered. Hard contact lenses should not be used 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 drug administration. Soft contact lenses should not be used 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, the eye ointment should be applied last. Systemic fluoroquinolone therapy, particularly ofloxacin, may cause tendon inflammation and rupture, particularly in elderly patients and those receiving concomitant corticosteroid therapy. Therefore, caution should be exercised and treatment with the drug Floxal, eye ointment should be stopped at the first signs of tendon inflammation (see the "Side effects" section). With systemic use of fluoroquinolones, the drug should be used with caution in patients with a risk of prolonging the QT interval, namely: with a congenital syndrome of prolongation of the QT interval, with the simultaneous use of drugs that prolong the QT interval (for example, antiarrhythmic drugs of class IA and III, tricyclic antidepressants, macrolides , antipsychotics), with uncorrected electrolyte balance (for example, hypokalemia, hypomagnesemia), elderly patients, patients with heart disease (for example, heart failure, myocardial infarction, bradycardia).

Ability in 

swim on the speed of reaction when driving a motor vehicle or other mechanisms
After injection into the conjunctival sac of the eye, the drug may cause loss of visual clarity for several minutes. Patients should refrain from driving vehicles or working with other mechanisms until the clarity of vision is restored.

Use during pregnancy or breastfeeding
Despite the lack of confirmation of any embryotoxic effects, Floxal, eye ointment, should not be used during pregnancy or breastfeeding.

Method of application and dosage
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) are injected with a 1 cm long strip of ointment (equivalent to 0.12 mg of ofloxacin) into the conjunctival sac of the affected eye 3 times a day (with chlamydial infections ˗ 5 times a day). Treatment with the drug Floxal, eye ointment, should not exceed 2 weeks. Instructions for use. Carefully pull the lower eyelid down and, slightly pressing the tube, inject the required amount of ointment into the conjunctival sac. Then close the eyelid and gently press the eyeball in different directions to evenly distribute the drug.

Note: if you additionally use other eye drops/ointments, the duration of the interval between applications should be 15 minutes, always apply the ointment last.

Children
Floxal, eye ointment, can be prescribed to children from 1 year old.

Overdose
There have been no reports of overdoses so far.

The treatment is symptomatic, it is necessary to immediately wash the eye(s) with water.

Adverse reactions
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. Despite the fact that a small amount of ofloxacin is absorbed into the systemic circulation when applied topically, the possibility of the side effects that have been reported cannot be excluded.

From the side of the immune system. Rare: 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 side of the nervous system: in isolated cases - dizziness.

From the side of the organs of vision. Often: eye discomfort, eye irritation; rarely: 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), deposits on the cornea may occur, especially if there is a history of corneal diseases.

There are reports that reactions such as toxic epidermal necrosis and Stevens-Johnson syndrome have occurred very rarely with local application. A cause-and-effect relationship with Floxal, an eye ointment, with regard to such manifestations has not been established.

From the side of the digestive tract: in isolated cases - nausea.

From the side of the skin and subcutaneous tissue: in isolated cases - swelling of the face, periorbital swelling.

Serious, sometimes fatal, hypersensitivity reactions, sometimes after the first dose, have been observed with systemic use of quinolones.

The drug contains lanolin, which can cause contact dermatitis.

Ruptures of the brachial tendon, 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 indicate that the risk of such tears may be increased in patients receiving corticosteroids, particularly in the elderly, and in patients with high loading of tendons, 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 no higher than 25 °C, in a place inaccessible to children.

Packaging
3 g of ointment in a laminated tube with a plastic tip and a screw-on cap.

One tube in a cardboard box.

Leave category
By prescription.