Maxiflox - instructions for use, dose, side effects, contraindications

auxiliary components: Boric acid - 3,000 mg, sodium chloride - 6,500 mg, 1 M hydrochloric acid solution / 1 M sodium hydroxide solution to pH = 6.7-7.0, purified water to 1,000 ml.

Description:

Greenish yellow, clear solution.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A.14 Moxifloxacin

Pharmacodynamics:

Mechanism of action

Moxifloxacin is a fluoroquinolone antibacterial preparation of the IV generation, inhibits DNA gyrase and topoisomerase IV, which in the bacterial cell performs DNA replication, recombination and repair.

Mechanisms of development of resistance

Resistance to antibiotics of the fluoroquinolone series, including 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 macrolides, aminoglycosides and tetracyclines and 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.

Moxifloxacin active in respect of most strains of microorganisms (as in vitro, and in vivo):

Gram-positive bacteria

Corynebacterium spp., including Corynebacterium diphtheriae;

Micrococcus luteus (including strains that are 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 insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprim);

Staphylococcus haemolyticus (including strains insensitive to methicillin, erythromycin, 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 that are insensitive to penicillin, erythromycin, tetracycline, and / or trimethoprim).

Gram-negative bacteria:

Acinetobacter lwoffii, Haemophilus influenzae (including strains not susceptible to ampicillin); Haemophilus parainfluenzae; Klebsiella spp.

Other microorganisms:

Chlamydia trachomatis.

Moxifloxacin acts in vitro against most of the listed below microorganisms, but the clinical significance of these data 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, 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 of the inhibitory concentration of moxifloxacin for various microorganisms are as follows:

Corynebacterium - no data

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

Pharmacokinetics:

When topical application occurs systemic absorption of moxifloxacin. The concentration of moxifloxacin in plasma was determined in 21 male and female patients who received moxifloxacin in a dosage form, eye drops in both eyes 1 drop 3 times a day for 4 days. The mean maximum concentration (C_mOh) moxifloxacin in plasma in the equilibrium state was 2.7 ng / ml, the area under the concentration-time curve (AUC) - 41.9 ng h / ml. These values are approximately 1600 and 1200 times less than the mean C_mOh and AUC after oral administration of a therapeutic dose of moxifloxacin 400 mg. The half-life (T_1/2) of moxifloxacin is about 13 hours.

Indications:

Bacterial conjunctivitis caused by microflora-sensitive moxifloxacin.

Contraindications:

Individual hypersensitivity to the components of the drug; hypersensitivity to drugs quinolone, children under 1 year.

Pregnancy and lactation:

Pregnancy and the period of breastfeeding

There is no sufficient experience on the use of 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 oral administration of moxifloxacin with breast milk, small amounts of substance are excreted.Nevertheless, if the therapeutic doses of the drug are observed, development of unwanted reactions in infants is not expected.

Teratogenicity

In pre-clinical animal studies moxifloxacin did not have a teratogenic effect at doses of 500 mg / kg / day (which is approximately 21,700 times higher than the recommended daily dose for humans), but there was some decrease in fetal weight and a delay in the development of the musculoskeletal system. Against the background of a dose of 100 mg / kg / day there was an increase in the frequency of decrease in the growth of newborns.

Fertility

Studies on the effect of moxifloxacin on fertility when applied as instillations have not been conducted.

Dosing and Administration:

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

For local ophthalmic use only. Not intended for use as subconjunctival injections or for administration to the anterior chamber of the eye.

Application in adults (including in elderly patients over 65 years of age)

1 drop 3 times a 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.

Use in the pediatric population

It is not necessary to correct the dosage regimen when used in children.

Liver and kidney failure

Correction of the dose is not required.

To prevent microbial contamination of the tip of the vial - dropper and the drug to avoid their contact with lids, wheel periorbital area and other surfaces.

In order to prevent absorption of the drug through the nasal mucosa is necessary to pinch finger nasolacrimal duct for 2-3 minutes after instillation.

When applying several drugs for topical use in ophthalmology interval between their application should be at least 5 minutes, eye ointment should be applied last.

Side effects:

General information on the safety profile of moxifloxacin in the dosage form of eye drops

In clinical trials of the dosage form of moxifloxacin for use in ophthalmology, 2252 patients received the study drug 1 drop, up to 8 times a day, 1,900 of which received moxifloxacin in the mode of 1 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 pain in the eye, 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" (more than 1/10); "often" (more than 1/100, less than 1/10); "infrequently" (more than 1/1000, less than 1/100), "rarely" (more than 1/10000, less than 1/1000) and "very rarely" (less than 1/10000).

System-basedadministrative classification	Frequency occurrence	Unwanted reaction
Violations of the blood and lymphatic system	Rarely	Decreased hemoglobin level
Immune system disorders	With unknown frequency	Hypersensitivity
Violations from side of the nervous systems	Infrequently	Headache
	Rarely	Paresthesia
	With unknown frequency	Dizziness
Violations by the body view	Often	Pain in the eye, eye irritation
	Infrequently	Point keratitis, dry eye syndrome, subconjunctival hemorrhage, itchy eyes, conjunctival injection, eyelid edema, discomfort in the eye.
	Rarely	Defective corneal epithelium, corneal abnormalities, conjunctivitis, blepharitis, edema of the conjunctiva. blurred vision, reduced visual acuity, asthenopia, erythema eyelids.
	With unknown frequency	Endophthalmitis, ulcerative keratitis, corneal erosion, increased intraocular pressure, corneal opacity, corneal edema, corneal infiltrates, corneal deposits, eye allergies, keratitis, corneal edema, photophobia, lachrymation, detached from the eyes, foreign body sensation in the eye
Heart Disease	With unknown frequency	Heart palpitations
Violations from hand respiratory system, chest and mediastinum	Rarely	Discomfort in the nose, pain in the larynx and pharynx, a sense of foreign body in the throat
	With unknown frequency	Dyspnea
Violations from the authorities digestion	Infrequently	Dysgeusia
	Rarely	Vomiting
	With unknown frequency	Nausea
Infringements from hepatobiliary systems	Rarely	Increased levels of aminotransferases and gamma-glutamyltransferases
Disturbances from the skin and subcutaneous fat	With unknown frequency	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-registration application, the risk of rupture of tendons in the receipt of systemic fluoroquinolone therapy may increase with the inclusion of corticosteroids in the regimen, elderly patients are at a particular risk.Most of the damage affects the tendons of the supporting joints, including the Achilles tendon.

Use in children

In clinical trials involving children, including newborns, a safety profile of moxifloxacin similar to the adult population was demonstrated in the form of instillations. In patients younger than 18 years, the most common pain in the eye 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.

Overdose:

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.

Interaction:

Special studies of the interaction of the drug 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.

Special instructions:

Patients using systemic quinolone-based drugs may experience severe, in some cases, fatal reactions of hypersensitivity (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 to MAXIFLOX develops, the drug should be discontinued. Severe acute hypersensitivity reactions to moxifloxacin and other components of the drug may require immediate resuscitation: according to indications, oxygen therapy with airway patency control can be performed.

With prolonged use of the drug, excessive growth of non-susceptible microorganisms, including fungi, can occur. In case of superinfection, it is necessary to cancel the drug and prescribe the appropriate therapy.

Inflammation and rupture of tendons were noted in systemic use of fluoroquinolones, mainly in elderly patients, as well as in patients, who received 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 effectiveness 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 ex juvantibus (empirical treatment) of gonococcal conjunctivitis, including in the therapy of ophthalmia of newborn gonococcal etiology, due to the presence of a large number of strains resistant to moxifloxacin Neisseria gonorrhoeae. Patients with infectious eye diseases 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 younger than 2 years, 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.

Effect on the ability to drive transp. cf. and fur:

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.

Form release / dosage:

Eye drops, 5 mg / ml.

Packaging:

5 ml of the drug are placed in a 5 ml polyethylene bottle, closed with a stopper and a lid with a safety ring made of polyethylene. A label is attached to the vial.

One bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

Shelf life:

3 years.

After opening the bottle, the drops should be used within 4 weeks.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003810

Date of registration:23.08.2016

Expiration Date:23.08.2021

The owner of the registration certificate:K.O. Ромфарм Компани С.Р.Л.K.O. Ромфарм Компани С.Р.Л. Romania

Manufacturer: & nbsp

S.C. ROMPHARM Company, S.R.L. Romania

Representation: & nbspРомфарма ОООРомфарма ООО

Information update date: & nbsp29.03.2018

Illustrated instructions

Instructions

Maxiflox (Maxiflox )