Moxifloxacin

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Clinical Pharmacology

Pharmacodynamics.
Moxifloxacin - fluoroquinolone antibacterial drug IV generation, has a bactericidal effect. It is active against a wide range of gram-positive and gram-negative microorganisms, anaerobic, acid-resistant and atypical bacteria.
The mechanism of action is associated with inhibition of topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an enzyme involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme involved in chromosomal DNA cleavage during bacterial cell division.
Resistance Development Mechanisms
Resistance to fluoroquinolone antibiotics, including moxifloxacin, is developed 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 system of multiple resistance to antibiotics and the system of resistance to quinolones. Resistance development is also associated with the expression of efflux proteins and inactivating enzymes. Cross-resistance with macrolides, aminoglycosides and tetracyclines is not expected due to differences in the mechanism of action. The development of resistance can have significant geographic differences, as well as significantly vary in different periods of time, and therefore, before starting treatment, it is necessary to obtain information on the resistance of microorganisms in a particular area, which is of particular importance in the treatment of severe infections.
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 that are insensitive to erythromycin, gentamicin, tetracycline and / or trimethoprim);
Staphylococcus aureus (including strains not sensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprim);
Staphylococcus epidermidis (including strains that are not sensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprimum);
Staphylococcus haemolyticus (including strains that are not sensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprimus);
Staphylococcus hominis (including strains not sensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and / or trimethoprim);
Staphylococcus warneri (including erythromycin insensitive strains);
Streptococcus mitis (including strains that are not sensitive to penicillin, erythromycin, tetracycline, and / or trimethoprimus);
Streptococcus pneumoniae (including strains not sensitive to penicillin, erythromycin, gentamicin, tetracycline, and / or trimethoprim);
Streptococcus of the viridans group (including strains not sensitive 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 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 pneumoniae; Morahella 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 during therapy with moxifloxacin. According to the epidemiological data of the European Committee for the determination of antimicrobial susceptibility, the threshold values of the inhibiting 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 applied topically, systemic absorption of moxifloxacin occurs: the maximum concentration of moxifloxacin in plasma (Cmax) is 2.7 ng / ml, the area under the concentration-time curve (AUC) is 45 ng * h / ml. These values are about 1600 times and 1000 times less than Cmax and AUC after applying a therapeutic dose of moxifloxacin 400 mg orally. The elimination half-life (T1 / 2) of moxifloxacin from plasma is about 13 hours.

Indications

Bacterial conjunctivitis caused by microorganisms sensitive to moxifloxacin.

Composition

Active substance:

Moxifloxacin hydrochloride

in terms of moxifloxacin

- 5.45 mg

- 5.00 mg

Excipients:

sodium chloride

- 6.4 mg

boric acid

- 3.0 mg

hydrochloric acid solution of 1 M or sodium hydroxide solution of 1 M

to pH 6.3 - 7.3

purified water

up to 1.0 ml

Moxifloxacin is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
			eye drops
Maxiflox	K.O.Romparm Company S.R.L	Romania	eye drops
Vigamox®	Alcon	USA	eye drops

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Dosage and Administration

The drug is intended only for local use in ophthalmic practice. Not intended for use as subconjunctival injections or for insertion into the anterior chamber of the eye.

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

Adults (including elderly patients over 65 years old) are prescribed 1 drop 3 times / day in the affected eye. Improvement occurs after 5 days of therapy, but treatment should continue 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 choice of treatment tactics.

The duration of the course of therapy depends on the severity of the patient’s condition, the clinical and bacteriological features of the infection process.

Children do not require correction dosing regimen.

In patients with hepatic and renal insufficiency, dose adjustment is not required.

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

In order to prevent the absorption of the drug through the nasal mucosa, it is necessary to squeeze the nasolacrimal canal with your 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.

Adverse reactions

In clinical studies, moxifloxacin in a dosage form for use in ophthalmology 2252 patients received the studied drug 1 drop up to 8 times / essence, 1900 of which received moxifloxacin 1 drop 3 times / day. The safety assessment population included 1389 patients in the United States and Canada, 586 patients in Japan and 277 patients in India. According to clinical studies, no information was obtained on serious adverse events from both the organ of vision and the organism as a whole. The most common adverse reactions associated with treatment were eye irritation and eye pain, the total frequency of occurrence of these phenomena 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 termination of participation in the study.

The following undesirable reactions are classified according to the following gradation of frequency: very often (> 1/10); often (> 1 / 100,1 / 1000,1 / 10 000,

From the hematopoietic system: rarely - decrease in hemoglobin.

On the part of the immune system: the frequency is unknown - hypersensitivity.

On the part of the nervous system: infrequently - headache; rarely, paresthesias; frequency unknown - dizziness.

On the part of the organ of vision: often - eye pain, eye irritation; infrequently - punctate keratitis, dry eye syndrome, subconjunctival hemorrhage, itchy eyes, conjunctival injection, eyelid edema, discomfort in the eyes; rarely - a defect in the corneal epithelium, abnormalities of the cornea, conjunctivitis, blepharitis, conjunctival edema, blurred vision, reduced visual acuity, asthenopia, eyelid erythema; Unknown frequency - endophthalmitis, ulcerative keratitis, corneal erosion, increased intraocular pressure, corneal opacification, corneal edema, corneal infiltrates, deposits on the cornea, allergic eye phenomena, keratitis, corneal edema, photophobia, tearing, eye discharge, and the eyes of a person's eyes, the eyes, the keratitis, corneal edema, photophobia, tearing, eye discharge, eye exposure, keratitis, cornea edema In eyes.

Since the cardiovascular system: the frequency is unknown - a sensation of 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 unknown - shortness of breath.

On the part of 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 individual unwanted reactions

There are reports of tendon ruptures of the shoulder joint, hand joints, Achilles tendons, as well as other tendons, which led to a long period of disability or required surgery. These phenomena were noted in patients receiving systemic therapy with fluoroquinolones. According to clinical studies and post-registration use, the risk of tendon ruptures during systemic treatment with fluoroquinolones may increase when corticosteroids are included in the treatment regimen, elderly patients are at particular risk. The most common injuries affect the tendons of the supporting joints, incl. Achilles tendons.

Use in children

In clinical studies involving children, incl. neonates, the profile of instillation of moxifloxacin in the form of instillations, similar to the adult population, was demonstrated. In patients under the age of 18, pain in the eyes and eye irritation were most frequently observed, 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.

Contraindications

- children's age up to 1 year;

- individual hypersensitivity to the drug components;

- Hypersensitivity to quinolone antibiotics.

Drug interactions

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

Pregnancy and Lactation

There is not enough experience with the drug during pregnancy and during breastfeeding. The use of the drug during pregnancy and during breastfeeding is possible in the case when the expected therapeutic effect exceeds the potential risk to the fetus and child.

Animal studies have shown that after taking moxifloxacin orally, a small amount of the substance is excreted in breast milk. However, with the use of the drug in therapeutic doses is not expected to develop adverse reactions in infants.

In preclinical animal studies, moxifloxacin did not have a teratogenic effect when used at a dose 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 delayed development of the musculoskeletal system. When used at a dose of 100 mg / kg / day, an increase in the frequency of reducing the growth of newborns was noted.

The study of the effect of moxifloxacin on fertility when used in the form of instillations was not conducted.

Special instructions

Patients who received quinolone 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, angioedema (including laryngeal, pharyngeal, or facial edema), airway obstruction, shortness of breath, urticaria, and pruritus.

In the case of an allergic reaction, the use of the drug should be discontinued. Severe acute hypersensitivity reactions to moxifloxacin and other components of the drug may require immediate resuscitation measures: according to the indications, oxygen therapy can be performed with control of the airway patency.

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

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

There is not enough data to conclude on the efficacy and safety of using Maxiflox in the treatment of bacterial conjunctivitis in the newborn, and therefore the use in patients of this age group is not recommended.

Maxiflox is not recommended for prophylactic use or treatment of ex juvantibus (empirical treatment) of gonococcal conjunctivitis, incl. in the treatment of gonococcal ophthalmia of the newborn, due to the presence of a large number of Moxifloxacin-resistant strains of Neisseria gonorrhoeae. Patients with infectious eye diseases caused by Neisseria gonorrhoeae 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 the age of 2 years 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 older than 2 years with eye diseases caused by Chlamydia trachomatis should be combined with systemic therapy.

In neonatal ophthalmia 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, wearing contact lenses is not recommended.

Influence on ability to drive motor transport and control mechanisms

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

Overdosage

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