Composition, form of production and packaging
Drops of the eye in the form of a transparent solution of a greenish-yellow color.
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.
5 ml - bottles of polyethylene with a capacity of 5 ml (1) with a stopper-dropper - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
Antibacterial drug from the group of fluoroquinolones IV generation. Inhibits DNA-gyrase and topoisomerase IV, which in the bacterial cell carry out DNA replication, recombination and repair.
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 not susceptible 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 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 trimethroprim); Staphylococcus warneri (including strains, insensitive to erythromycin); Streptococcus mitis (including strains that are insensitive to penicillin, erythromycin, tetracycline, and / or trimethoprim); Streptococcus pneumoniae (including strains that are insensitive to penicillin, gentamicin, erythromycin, tetracycline, and / or trimethoprim); Streptococcus group of viridians (including strains, insensitive to penicillin, erythromycin, tetracycline and / or trimethoprim).
Gram-negative bacteria: Acinetobacter lwoffii , Haemophilus influenzae (including strains, insensitive to ampicillin); Haemophilus parainfluenzae; Klebsiella spp.
Other microorganisms: Chlamydia trachomatis.
Moxifloxacin acts in vitro against most of the microorganisms listed below, but the clinical significance of this data is not known.
Gram-positive bacteria: Listeria monocytogenes, Staphylococcus saprophyticus, Streptococcus agalactiae, Streptococcus mitis, Streptococcus pyogenes, Streptococcus group 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, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas stutzeri.
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 against the background of moxifloxacin therapy. According to the epidemiological data of the European Committee for the Determination of Antimicrobial Susceptibility, the threshold values вЂ‹вЂ‹of the inhibitory concentration of moxifloxacin for various microorganisms are as follows:
- Corynebacterium - nda;
- 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 fluoroquinolone series, incl. to moxifloxacin, develops through chromosomal mutations in genes encoding DNA-gyrase and topoisomerase IV. In Gram-negative bacteria, resistance to moxifloxacin is associated with mutations in a system of multiple resistance to antibiotics and a system of resistance to quinolones. The development of resistance is also associated with the expression of efflux proteins and inactivating enzymes. Cross-resistance with antibiotics of macrolide, aminoglycoside and tetracycline groups is not expected due to differences in the mechanism of action. The development of resistance may have significant geographical differences, and also vary significantly at different periods of time, so before starting therapy it is necessary to obtain information about the resistance of microorganisms in a particular locality, which is of particular importance in the treatment of severe infections.
Suction and distribution
When topical application occurs systemic absorption of moxifloxacin. The concentration of moxifloxacin in the plasma was determined in 21 male and female patients who received moxifloxacin in the drug form, eye drops in both eyes 1 drop 3 times / day for 4 days. The mean C max of moxifloxacin in the blood plasma in equilibrium was 2.7 ng / ml, the AUC value was 41.9 ng h / ml. These values вЂ‹вЂ‹are approximately 1600 and 1200 times less than the mean C max and AUC after oral administration of a therapeutic dose of moxifloxacin 400 mg.
T 1/2 of moxifloxacin is about 13 hours.
- bacterial conjunctivitis caused by microflora-sensitive moxifloxacin.
The drug is intended only for topical application in ophthalmic practice. Not intended for use as subconjunctival injections or for administration to the anterior chamber of the eye.
When administering treatment, it is necessary to take into account the official recommendations for antibiotic therapy.
Adults (including patients older than 65 years) are prescribed 1 drop 3 times / day in the affected eye. Improvement of the condition occurs after 5 days of therapy, but treatment should continue for another 2-3 days. In the absence of therapeutic effect after 5 days of therapy, it is recommended to revise the diagnosis and choice of therapeutic tactics.
The length of the course of therapy depends on the severity of the patient's condition, clinical and bacteriological features of the infection process.
Children do not need a dosage adjustment.
In patients with hepatic and renal insufficiency, dose adjustment is not required.
To prevent microbial contamination of the tip of the dropper and the drug, avoid contact with eyelids, the skin of the peri-ocular area and other surfaces.
In order to prevent the absorption of the drug through the nasal mucosa, it is necessary to pinch the nasolacrimal canal with a finger for 2-3 minutes after instillation.
When using several drugs for topical application in ophthalmology, the interval between their use should be at least 5 minutes, ophthalmic ointments should be used last.
In clinical trials of moxifloxacin in a dosage form for use in ophthalmology, 2252 patients received the study drug 1 drop up to 8 times / essence, 1900 of which received moxifloxacin in a 1 drop drop 3 times a day. The population for safety assessment included 1,389 patients in the US and Canada, 586 patients in Japan and 277 patients in India. According to clinical studies, no serious adverse events were reported from either the organ of vision or the body as a whole. The most common adverse reactions associated with treatment were eye irritation and eye pain, the total 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 completion of the study.
The following undesirable reactions are classified according to the following gradation frequency: very often (> 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).
From the hemopoietic system: rarely - reduction of hemoglobin.
From the immune system: the frequency is unknown - hypersensitivity.
From the nervous system: infrequently - a headache; rarely paresthesia; frequency unknown - dizziness.
From the side of the organ of vision: often - pain in the eyes, eye irritation; infrequently - point keratitis, dry eye syndrome, subconjunctival hemorrhage, itchy eyes, conjunctival injection, edema of the eyelids, discomfort in the eyes; rarely - corneal epithelial defect, 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, lachrymation, detachable from the eyes, foreign body sensation In eyes.
From the side of the cardiovascular system: the frequency is unknown - the sensation of the heartbeat.
On the part of the respiratory system: rarely - discomfort in the nose, pain in the larynx and pharynx, foreign body sensation in the throat; frequency is unknown - dyspnea.
From the side of the digestive system: infrequently - dysgeusia; rarely - vomiting, increased activity of aminotransferases and GGT; frequency is unknown - nausea.
From the skin and subcutaneous fat: the frequency is unknown - erythema, rash, hives, itching.
Description of individual adverse reactions
There are reports of ruptures of the tendons of the shoulder joint, the joints of the hands, the Achilles tendon, and other tendons that led to a long period of incapacity for work or required surgical intervention. These phenomena were noted in patients who received systemic therapy with fluoroquinolones. According to clinical research and post-marketing application, the risk of rupture of tendons in systemic fluoroquinolone therapy may increase when corticosteroids are included in the regimen, elderly patients are at a particular risk. Most damage affects the tendons of the supporting joints, incl. Achilles tendon.
Use in children
In the course of clinical trials involving children, incl. newborns showed a similar safety profile to the adult population of moxifloxacin in the form of instillations. In patients under the age of 18, the most common pain in the eyes 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 undesirable phenomena and their severity.
- Children's age up to 1 year;
- individual hypersensitivity to the components of the drug;
- Hypersensitivity to antibiotics of a group of quinolones.
PREGNANCY AND LACTATION
There is no sufficient experience of using the drug during pregnancy and during breastfeeding. The use of the drug during pregnancy and during breastfeeding is possible if the expected therapeutic effect exceeds the potential risk to the fetus and the baby.
Studies in animals have shown that after taking moxifloxacin, a small amount of the substance is excreted in breast milk. Nevertheless, when the drug is used in therapeutic doses, unwanted reactions in infants are not expected to develop.
In pre-clinical studies in animals, moxifloxacin did not have a teratogenic effect when administered at a dose of 500 mg / kg / day (approximately 21,700 times the recommended daily dose for humans), but there was some decrease in fetal mass and delayed development of the musculoskeletal system. When applied at a dose of 100 mg / kg / day, there was an increase in the incidence of a decrease in neonatal growth.
The effect of moxifloxacin on fertility was not investigated when applied as instillations.
APPLICATION FOR FUNCTIONS OF THE LIVER
In patients with renal insufficiency, dose adjustment is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In patients with hepatic insufficiency, dose adjustment is not required.
APPLICATION FOR CHILDREN
Contraindicated use of the drug in childhood up to 1 year.
Patients treated with 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, Quinck's edema (including swelling of the larynx, pharynx or face), airway obstruction, dyspnoea, urticaria and skin itching.
If the allergic reaction develops, the drug should be discontinued. Severe acute hypersensitivity reactions to moxifloxacin and other components of the drug may require immediate resuscitation: according to the indications, oxygen therapy with airway patency control can be performed.
With prolonged use of the drug, excessive growth of non-susceptible microorganisms is possible, incl. mushrooms. In case of superinfection, it is necessary to cancel the drug and prescribe the appropriate therapy.
Inflammation and rupture of tendons was noted in the systemic use of fluoroquinolones, mainly in elderly patients, as well as in patients receiving corticosteroids along with fluoroquinolones. Although 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 inflammation of the tendons appear.
There is insufficient data to make a conclusion about the efficacy and safety of 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 therapy of ex juvantibus (empirical treatment) of gonococcal conjunctivitis, incl. in the treatment of gonococcal ophthalmia of newborns, due to the presence of a large number of strains resistant to moxifloxacin Neisseria gonorrhoeae. Patients with infectious diseases of the eye caused by Neisseria gonorrhoeae should receive appropriate systemic therapy.
It is not recommended to use Maxiflox in the treatment of infectious diseases of the organ of vision caused by Chlamydia trachomatis in patients under 2 years of age, since there is no information on the study of the drug in this category of patients. The use of Maxiflox in patients older than 2 years with eye diseases caused by Chlamydia trachomatis should be combined with systemic therapy.
Patients should receive appropriate treatment for ophthalmia of newborns; 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, contact lenses are not recommended.
Impact on the ability to drive vehicles and manage mechanisms
As in the case of instillations of other drugs, a temporary blurring of vision after application of the drug is possible. Before the restoration of clarity of visual perception is not recommended to drive and other mechanisms.
Due to the small capacity of the conjunctival cavity, there is practically no possibility of developing a local overdose with the use of drugs in the form of instillations.The total content of moxifloxacin in the preparation is too low for the development of undesirable phenomena with accidental ingestion of the contents of the vial.
Special studies of the interaction of Maxiflox with other drugs have not been conducted. Due to low systemic concentration after topical application in the form of instillations, interaction with other drugs is unlikely.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in its original packaging in a place inaccessible to children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
After opening the bottle, the drops should be used within 4 weeks.