Maxiflox eye drops 5mg / ml, 5 ml

Bacterial conjunctivitis caused by microorganisms sensitive to moxifloxacin.

The drug is intended only for topical use in ophthalmic practice. Not intended for use as a subconjunctival injection or for injection into the anterior chamber of the eye.

When carrying out treatment, it is necessary to take into account the official recommendations for antibiotic therapy.

Adults (including elderly patients over 65 years of age) are prescribed 1 drop 3 times / day in the affected eye. Improvement of the condition occurs after 5 days of therapy, but treatment should be continued for another 2-3 days. In the absence of a therapeutic effect after 5 days of therapy, it is recommended to reconsider the diagnosis and the choice of treatment tactics.

The duration of the course of therapy depends on the severity of the patient's condition, clinical and bacteriological characteristics of the infectious process.

In children, no dosage adjustment is required.

No dose adjustment is required in patients with hepatic and renal impairment.

To prevent microbial contamination of the tip of the dropper bottle and the drug, it is necessary to avoid their contact with the eyelids, the skin of the periorbital region and other surfaces.

In order to prevent absorption of the drug through the nasal mucosa, it is necessary to squeeze the nasolacrimal canal with a finger for 2-3 minutes after instillation.

When using several drugs for topical use in ophthalmology, the interval between their use should be at least 5 minutes, eye ointments should be used last.

Eye drops in the form of a clear solution of greenish-yellow color.

1 ml

moxifloxacin hydrochloride 5.45 mg,

which corresponds to the content of moxifloxacin 5 mg

Excipients: boric acid - 3 mg, sodium chloride - 6.5 mg, hydrochloric acid solution 1M / sodium hydroxide solution 1M - up to pH 6.7-7.0, purified water - up to 1 ml.

• Children under 1 year old;

• individual hypersensitivity to the components of the drug;

• hypersensitivity to antibiotics of the quinolone group.

pharmachologic effect

Antibacterial drug from the IV generation group of fluoroquinolones. Inhibits DNA gyrase and topoisomerase IV, which replicate, recombine and repair DNA in a bacterial cell.

Moxifloxacin is active against most strains of microorganisms (both in vitro and in vivo).

Gram-positive bacteria: Corynebacterium spp., Including Corynebacterium diphtheriae; Micrococcus luteus (including strains insensitive to erythromycin, gentamicin, tetracycline and / or trimethoprim); Staphylococcus aureus (including strains insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprim); Staphylococcus epidermidis (including strains that are insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprim); Staphylococcus haemolyticus (including strains insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprim); Staphylococcus hominis (including strains insensitive to methicillin, erythromycin, tetracycline and / or trimetroprim); Staphylococcus warneri (including erythromycin insensitive strains);Streptococcus mitis (including strains insensitive to penicillin, erythromycin, tetracycline and / or trimethoprim); Streptococcus pneumoniae (including strains insensitive to penicillin, gentamicin, erythromycin, tetracycline and / or trimethoprim); Streptococcus of the viridian group (including strains insensitive to penicillin, erythromycin, tetracycline and / or trimethoprim).

Gram-negative bacteria: Acinetobacter lwoffii , Haemophilus influenzae (including ampicillin insensitive strains); Haemophilus parainfluenzae; Klebsiella spp.

Other microorganisms: Chlamydia trachomatis.

Moxifloxacin acts in vitro against most of the microorganisms listed below, but the clinical significance of these findings is unknown.

Gram-positive bacteria: Listeria monocytogenes, Staphylococcus saprophyticus, Streptococcus agalactiae, Streptococcus mitis, Streptococcus pyogenes, Streptococcus groups C, G, F.

Gram-negative bacteria: Acinetobacter baumannii, Acinetobacter calcoaceticus, Citrobacter freundii, Citrobacter koseri, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumonia, Moraxella catarrhalis, Morgansellus gum, Moraxella catarrhalis, Morganisella vulutomonus

Anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Propionibacterium acnes.

Other microorganisms: Chlamydia pneumoniae, Legionella pneumophila, Mycobacterium avium, Mycobacterium marinum, Mycoplasma pneumoniae.

There is no data on the relationship between the clinical and bacteriological outcome of infectious diseases of the organ of vision during therapy with moxifloxacin. According to the epidemiological data of the European Committee for the determination of antimicrobial susceptibility, the threshold values ??of the inhibitory concentration of moxifloxacin for various microorganisms are as follows:

• Corynebacterium - no data available;

• Staphylococcus aureus - 0.25 mg / l;

• Staphylococcus, coag-neg. - 0.25 mg / l;

• Streptococcus pneumoniae - 0.5 mg / l;

• Streptococcus pyogenes - 0.5 mg / l;

• Streptococcus, viridans group - 0.5 mg / l;

• Enterobacter spp. - 0.25 mg / l;

• Haemophilus influenzae - 0.125 mg / l;

• Klebsiella spp. - 0.25 mg / l;

• Moraxella catarrhalis - 0.25 mg / l;

• Morganella morganii - 0.25 mg / l;

• Neisseria gonorrhoeae - 0.032 mg / l;

• Pseudomonas aeruginosa - 4 mg / l;

• Serratia marcescens - 1 mg / l.

Mechanisms of development of resistance

Resistance to antibiotics of the fluoroquinolone series, incl. to moxifloxacin, develops by chromosomal mutations in the genes encoding DNA gyrase and topoisomerase IV. In gram-negative bacteria, resistance to moxifloxacin is associated with mutations in the multiple antibiotic resistance system and the quinolone resistance system. The development of resistance is also associated with the expression of efflux proteins and inactivating enzymes. Cross-resistance with antibiotics of the macrolide, aminoglycoside and tetracycline groups is not expected due to differences in the mechanism of action. The development of resistance can have significant geographical differences, as well as vary significantly at different periods of time, and therefore, before starting therapy, it is necessary to obtain information about the resistance of microorganisms in a particular area,which is of particular importance in the treatment of severe infections.

Pharmacokinetics

Absorption and distribution

When applied topically, systemic absorption of moxifloxacin occurs. The concentration of moxifloxacin in plasma was determined in 21 male and female patients who received moxifloxacin in the dosage form of eye drops in both eyes, 1 drop 3 times / day for 4 days. The average Cmax of moxifloxacin in blood plasma in the equilibrium state was 2.7 ng / ml, the AUC value was 41.9 ng h / ml. These values ??are approximately 1600 and 1200 times less than the average Cmax and AUC after oral administration of a therapeutic dose of 400 mg moxifloxacin.

Withdrawal

T1 / 2 of moxifloxacin is about 13 hours.

Side effect

During clinical studies of moxifloxacin in a dosage form for use in ophthalmology, 2252 patients received the study drug 1 drop up to 8 times / day, 1900 of which received moxifloxacin in a 1 drop mode 3 times / day. The population for safety assessment included 1389 patients in the United States and Canada, 586 patients in Japan, and 277 patients in India. According to clinical studies, no information has been received about serious adverse events from both the organ of vision and the body as a whole. The most common treatment-related adverse reactions were eye irritation and eye pain, and the cumulative incidence of these events ranged from 1% to 2%. In 96% of patients, the severity of these reactions was mild, while in one of the patients who participated in the study,the severity of the adverse event led to the end of participation in the study.

The following adverse reactions are classified according to the following frequency gradation: very common (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100), rarely (> 1/10 000, <1/1000) and very rarely (less than 1/10 000).

On the part of the hematopoietic system: rarely - a decrease in hemoglobin.

From the immune system: frequency unknown - hypersensitivity.

From the nervous system: infrequently - headache; rarely - paresthesia; frequency unknown - dizziness.

From the side of the organ of vision: often - eye pain, eye irritation; infrequently - punctate keratitis, dry eye syndrome, subconjunctival hemorrhage, itchy eyes, conjunctival injection, eyelid edema, eye discomfort; rarely - defect of the corneal epithelium, corneal disorders, conjunctivitis, blepharitis, conjunctival edema, blurred vision, decreased visual acuity, asthenopia, erythema of the eyelids; frequency unknown - endophthalmitis, ulcerative keratitis, corneal erosion, increased intraocular pressure, corneal opacity, corneal edema, corneal infiltrates, corneal deposits, eye allergies, keratitis, corneal edema, photophobia, lacrimation, discharge from the eyes, In eyes.

From the side of the cardiovascular system: the frequency is unknown - a feeling of palpitations.

From the respiratory system: rarely - discomfort in the nose, pain in the larynx and pharynx, feeling of a foreign body in the throat; frequency unknown - shortness of breath.

From the digestive system: infrequently - dysgeusia; rarely - vomiting, increased activity of aminotransferases and GGT; frequency unknown - nausea.

On the part of the skin and subcutaneous fat: the frequency is unknown - erythema, rash, urticaria, itching.

Description of selected adverse reactions

There have been reports of ruptured tendons in the shoulder joint, arm joints, Achilles tendon, and other tendons that have resulted in long periods of disability or surgery. These phenomena have been observed in patients receiving systemic therapy with fluoroquinolones. According to clinical studies and post-registration use, the risk of tendon ruptures during systemic therapy with fluoroquinolones may increase when corticosteroids are included in the therapy regimen; elderly patients are at particular risk. Most often, injuries affect the tendons of the supporting joints, incl. Achilles tendons.

Application in children

During clinical trials involving children, incl. neonates demonstrated a safety profile of moxifloxacin in the form of instillations similar to the adult population. In patients under the age of 18, the most common were eye pain and eye irritation, the frequency of occurrence was about 0.9%. According to the results of clinical studies in the pediatric population, there were no differences from the adult population in the profile of adverse events and their severity.

Application during pregnancy and lactation

There is no sufficient experience in using the drug during pregnancy and during breastfeeding. The use of the drug during pregnancy and during breastfeeding is possible when the expected therapeutic effect exceeds the potential risk to the fetus and child.

Animal studies have shown that after oral administration of moxifloxacin, a small amount of the substance is excreted in breast milk. However, when using the drug in therapeutic doses, the development of adverse reactions in infants is not expected.

In preclinical studies in animals, moxifloxacin did not have a teratogenic effect when used at a dose of 500 mg / kg / day (which is about 21,700 times higher than the recommended daily dose for humans), however, there was a slight decrease in fetal weight and a delay in the development of the musculoskeletal system. When used in a dose of 100 mg / kg / day, there was an increase in the frequency of decrease in the growth of newborns.

The study of the effect of moxifloxacin on fertility when used as instillations has not been conducted.

Application for violations of liver function

No dose adjustment is required in patients with hepatic impairment.

Application for impaired renal function

No dose adjustment is required in patients with renal impairment.

Application in children

The use of the drug in children under 1 year of age is contraindicated.

special instructions

Patients receiving quinolone drugs for systemic use may experience severe, in some cases fatal hypersensitivity reactions (anaphylaxis), in some cases after taking the first dose. Some reactions were accompanied by collapse, loss of consciousness, Quincke's edema (including edema of the larynx, pharynx, or face), airway obstruction, shortness of breath, hives, and pruritus.

If an allergic reaction develops, the drug should be discontinued. Severe acute hypersensitivity reactions to moxifloxacin and other components of the drug may require immediate resuscitation: if indicated, oxygen therapy with airway control can be performed.

With prolonged use of the drug, excessive growth of refractory microorganisms is possible, incl. mushrooms. In case of superinfection, it is necessary to discontinue the drug and prescribe appropriate therapy.

Inflammation and rupture of tendons were observed with systemic use of fluoroquinolones, mainly in elderly patients, as well as in patients receiving corticosteroids along with fluoroquinolones. Despite the fact that the systemic concentrations of moxifloxacin after topical application in ophthalmology are significantly lower than those for oral administration, the drug should be discontinued when the first signs of tendon inflammation appear.

There is no sufficient amount of data to draw a conclusion about the efficacy and safety of the drug Maxiflox in the treatment of bacterial conjunctivitis in newborns, and therefore the use in patients of this age group is not recommended.

Maxiflox is not recommended for prophylactic use or ex juvantibus therapy (empirical treatment) of gonococcal conjunctivitis, incl. in the treatment of gonococcal ophthalmia of newborns, due to the presence of a large number of strains of Neisseria gonorrhoeae resistant to moxifloxacin. Patients with Neisseria gonorrhoeae eye infections should receive appropriate systemic therapy.

The use of the drug Maxiflox in the treatment of infectious diseases of the organ of vision caused by Chlamydia trachomatis in patients under 2 years of age is not recommended, since there is no information about the study of the drug in this category of patients. The use of Maxiflox in patients over 2 years of age with eye diseases caused by Chlamydia trachomatis should be combined with systemic therapy.

For ophthalmia of newborns, patients should receive treatment appropriate to their condition; so, with the development of conjunctivitis of chlamydial and gonorrheal etiology, this type of treatment will be systemic therapy.

In the presence of infectious diseases of the anterior segment of the eyeball, it is not recommended to wear contact lenses.

Influence on the ability to drive vehicles and use mechanisms

As in the case of instillations of other drugs, temporary blurred vision is possible after using the drug. Until the clarity of visual perception is restored, it is not recommended to drive a car and other mechanisms.

Overdose

Due to the small capacity of the conjunctival cavity, the possibility of developing a local overdose when using drugs in the form of instillations is practically absent. The total content of moxifloxacin in the preparation is too small for the development of adverse events if the contents of the vial are accidentally swallowed.

Drug interactions

Special studies of the interaction of the drug Maxiflox with other drugs have not been conducted. Due to the low systemic concentration after topical application in the form of instillations, interaction with other drugs is unlikely.