Avelox instructions for use of the tablet for adults. Avelox is an effective drug that successfully copes with bacterial infections. Composition of Avelox ®

Moxifloxacin (1-cyclopropyl-7((S,S)-2,8-diaza-bicyclonone-8-ue)-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid hydrochloride ) - antibacterial drug of the fluoroquinolone series wide range actions. The bactericidal effect of the drug is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of DNA biosynthesis of the microbial cell and its death. The activity of moxifloxacin depends on its concentration in the blood plasma: the minimum bactericidal concentrations correspond to the minimum bacteriostatic concentrations. The mechanisms of resistance of microorganisms that inactivate penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not affect the antibacterial effectiveness of moxifloxacin. Cross-resistance between the drug Avelox and the listed antibiotics has not been observed. There were also no cases of plasmid resistance. The overall incidence of resistance is very low (10-7-10-10). Resistance to moxifloxacin develops slowly through numerous mutations.
Repeated action of moxifloxacin on microorganisms at concentrations below the minimum inhibitory concentration (MIC) is accompanied by only a slight increase in the MIC. Between antibacterial agents groups of quinolones tend to show cross-resistance. However, some gram-positive and anaerobic microorganisms that are resistant to other quinolones are sensitive to moxifloxacin. Moxifloxacin in vitro active against a wide range of gram-negative and gram-positive microorganisms, anaerobes, acid-fast bacteria and such atypical forms as Micoplasma, Chlamydia, Legionella. Moxifloxacin is effective against bacteria resistant to β-lactam and macrolide antibiotics.
The following are sensitive to the drug:
Staphylococcus aureus(including methicillin-sensitive strains), Streptococcus pneumoniae(including strains resistant to penicillin and macrolides), Streptococcus pyogenes(group A);
gram-negative microorganisms - Haemophillus influenzae Haemophillus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis(including strains producing β-lactamases), Escherichia coli, Enterobacter cloacae;
atypical forms — Chlamydia pneumoniae, Mycoplasma pneumoniae,Legionella pneumoniae.
The following are relatively sensitive to moxifloxacin:
gram-positive microorganisms - Streptococcus milleri, Str. mitior, Str. agalactiae, Str. dysgalactiae, Staphylococcus cohnii, S. epidermidis(including methicillin-resistant strains), S. haemolyticus, S. hominis, S. saprophyticus, S. simulans, Corynebacterium diphtheriae;
gram-negative microorganisms - Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii;
anaerobes - Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevotella sp p., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum ;
atypical forms - Legionella pneumophila, Caxiella burnettii.
Sensitivity to moxifloxacin was confirmed by clinical data.
Moxifloxacin is less active relative to Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholderia cepacia, Stenotrophomonas maltophilia.
When taken orally, moxifloxacin is absorbed quickly and almost completely. Absolute bioavailability reaches almost 91%.
In the dose range from 50 to 1200 mg for a single dose and at a dose of 600 mg/day for 10 days, the pharmacokinetics are linear. Stable blood concentrations are achieved after 3 days of use. After a single dose of 400 mg of the drug, the maximum concentration in the blood plasma is reached within 0.5-4 hours and is 3.1 mg/l. When taking moxifloxacin simultaneously with food, there is a slight increase in the time to reach maximum concentration (by 2 hours) and a slight decrease in maximum concentration (by approximately 16%), while the duration of absorption does not change. However, these data do not have clinical significance and the drug can be taken regardless of meals.
Moxifloxacin is rapidly distributed in tissues and organs and binds to plasma proteins (mainly albumin) by approximately 45%. The volume of distribution is approximately 2 l/kg. High concentrations of the drug, exceeding the concentration in the blood plasma, are achieved in lung tissue(alveolar macrophages), bronchial mucosa, nasal paranasal sinuses and especially in areas of inflammation. In interstitial fluid and saliva, moxifloxacin is determined in a free state, not bound to proteins, in a higher concentration than in blood plasma.
Moxifloxacin does not undergo biotransformation by the microsomal cytochrome P450 system in the liver and is excreted from the body by the kidneys both unchanged and in the form of inactive sulfo compounds and glucuronides. 45% of the unchanged drug is excreted in urine and feces. The half-life of the drug is approximately 12 hours. The average total clearance after administration of a dose of 400 mg is 179-246 ml/min. About 19% of a single dose is excreted unchanged in the urine and 25% in feces.
Age (not studied in children) and sex differences in the pharmacokinetics of moxifloxacin have not been established. There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (creatinine clearance 30 ml/min. 1.73 m2) and in those on continuous hemodialysis and long-term ambulatory peritoneal dialysis. In patients with minor and moderate liver dysfunction (stages A and B according to the Child-Pugh classification), the pharmacokinetics of the drug does not change. There are no data on use in cases of severe liver dysfunction (Child-Pugh stage C).

Indications for use of the drug Avelox

Treatment bacterial infections caused by microorganisms sensitive to the drug.
Infectious diseases of the respiratory tract:

chronic bronchitis during exacerbation;
community-acquired pneumonia, the causative agents of which are strains of microorganisms with multiple resistance to antibiotics;

Uncomplicated skin and soft tissue infections.
Uncomplicated inflammatory diseases of the pelvic organs (including infectious diseases upper section genital area in women, including salpingitis and endometritis).
Complicated infectious diseases of the skin and subcutaneous structures (including infected diabetic foot).
Complicated intra-abdominal infections, including polymicrobial infections (such as abscess formation).
Streptococcus pneumoniae with multiple resistance to antibiotics, including strains resistant to penicillin and strains resistant to two or more antibiotics from groups such as penicillins (with minimal inhibitory activity ≥2 μg/ml), second generation cephalosporins (cefuroxime), macrolides, tetracyclines and trimethoprim /sulfamethoxazole.

Use of the drug Avelox

Adults: 400 mg 1 time per day for any infections.
Duration of therapy
The duration of therapy is determined by the severity of the infection and clinical effect. At the initial stages of treatment it can be used Avelox solution for infusion, and then to continue therapy, if indicated, the drug can be prescribed orally in tablets.
Exacerbation chronic bronchitis- 5 days.
Community-acquired pneumonia - 10 days.
Acute sinusitis - 7 days.
Uncomplicated skin and soft tissue infections - 7 days.
Uncomplicated inflammatory diseases of the pelvic organs - 14 days.
Complicated infections of the skin and subcutaneous structures - total duration step therapy moxifloxacin (iv administration of the drug followed by oral administration) is 7-21 days.
Complicated intra-abdominal infections - the total duration of step-down therapy (iv administration of the drug followed by oral administration) is 5-14 days.
According to clinical trials The duration of therapy with tablets and Avelox infusion solution was up to 21 days (for the treatment of complicated infections of the skin and subcutaneous structures).
In elderly patients and in patients with impaired liver function, the dosage regimen does not change.
In patients with impaired renal function (including those with creatinine clearance ≤30 ml/min. 1.73 m2) and in those on continuous hemodialysis and long-term ambulatory peritoneal dialysis, there is no need for dose adjustment.
Application for the treatment of patients of different ethnic groups— There is no need to change the dosage regimen.
The tablets should be taken without chewing, with plenty of water, regardless of meals.
Moxifloxacin infusion solution is used both for antibacterial monotherapy and in combination with other compatible drugs. Moxifloxacin solution remains stable for 24 hours at room temperature and when using the following solvents: water for injection, solutions of sodium chloride 0.9%, sodium chloride 1M, glucose 5%, 10% and 40%, xylitol solution 20%, Ringer’s and Ringer’s lactate solutions, drugs Aminofusin 10% and Ionosteril D5. The infusion solution should be administered intravenously slowly over 60 minutes. Maximum dose is 600 mg once or 400 mg once a day for 7-21 days. Avelox is prescribed intravenously at a dose of 400 mg once a day. The drug can be used intravenously throughout the course of treatment or at the initial stages of treatment, followed by a transition to taking moxifloxacin in tablet form.

Contraindications to the use of the drug Avelox

Hypersensitivity to moxifloxacin (or to any component of the drug); to other quinolones; children's and adolescence(up to 18 years old); The drug is contraindicated in patients with epilepsy, pregnancy and breastfeeding.

Side effects of the drug Avelox

Moxifloxacin is well tolerated in most patients. During clinical trials moxifloxacin most side effects(90%) were mild or moderate. The rate of discontinuation of treatment using the Avelox infusion solution due to the development of side effects did not exceed 3.8%.
With a development frequency ≥1%≤10%
interval extension Q-T in patients with concomitant hypokalemia.
From the gastrointestinal tract - abdominal pain, nausea, diarrhea, vomiting, symptoms of dyspepsia, changes in liver tests.
From the central nervous system, sensory organs - dizziness, headache.
With a development frequency ≥0.1%≤1%
General reactions - asthenia, hyperhidrosis, general weakness, pain in the area chest.
- tachycardia, increased blood pressure, palpitations, prolongation of the interval Q-T.
From the gastrointestinal tract- dry mouth, nausea, vomiting, flatulence, constipation, stomatitis, lack of appetite, candidiasis oral cavity, glossitis, increased gamma-glutamyl transpeptidase and amylase.
From the blood system and lymphatic system - leukopenia, decreased prothrombin levels, eosinophilia, thrombocytopenia.
- arthralgia, myalgia.
From the outside nervous system — insomnia, dizziness, nervousness, drowsiness, anxiety, tremor, paresthesia.
- shortness of breath.
From the skin- rashes, itching, sweating.
From the genitourinary system — vaginal candidiasis, vaginitis.
With a development frequency ≥0.01%≤0.1%
General reactions- pelvic pain, facial swelling, back pain, changes in laboratory tests, allergic reactions, pain in the legs.
From the outside of cardio-vascular system — decreased blood pressure, loss of consciousness, peripheral edema, vasodilation (flush of blood to the face).
From the gastrointestinal tract - gastritis, change in tongue color, dysphagia, jaundice (predominantly cholestatic), diarrhea (caused Clostridium difficile).
From the blood and lymphatic system- decreased thromboplastin levels, increased prothrombin levels, thrombocytopenia, anemia.
Metabolism- hyperglycemia, hyperlipidemia, hyperuricemia, increased LDH in combination with abnormal liver tests.
From the musculoskeletal system- arthritis, tendon damage.
From the nervous system- hallucinations, depersonalization, increased muscle tone, impaired coordination, agitation, amnesia, aphasia, emotional lability, sleep disturbance, speech disturbance, thinking process, decreased tactile sensitivity, pathological dreams, convulsions, confusion, depression.
From the outside respiratory system - bronchospasm.
From the skin- rashes (maculopapular, pustular, purpura), urticaria.
From the senses- tinnitus, visual impairment, loss taste sensations, parosmia (including changes in the sense of smell, decrease and loss of smell), amblyopia.
From the genitourinary system- impaired renal function (increased creatinine or urea levels).
With a development frequency ≤0.01%
Allergic reactions - anaphylactic reactions, anaphylactic shock (including life-threatening), angioedema (including life-threatening laryngeal edema).
From the gastrointestinal tract- pseudomembranous colitis (in isolated cases life-threatening), hepatitis (mainly cholestatic).
From the musculoskeletal system- tendon rupture.
From the skin- Stevens-Johnson syndrome.
From the nervous system- psychotic reactions.
From the cardiovascular system- ventricular tachyarrhythmia (very rare), ventricular fibrillation and flutter and cardiac arrest, mainly in people prone to arrhythmia.
From the laboratory parameters- increase or decrease in hematocrit and decrease or increase in red blood cell content, leukocytosis, hypoglycemia, decrease in hemoglobin, increase in the level of alkaline phosphatase, ALT, AST, bilirubin, uric acid, creatinine, urea.
The relationship between changes in these laboratory parameters and the use of moxifloxacin has not been established.

Special instructions for the use of Avelox

When combined use Avelox infusion solution and other drugs for intravenous administration, each of these drugs must be administered separately. Only clear infusion solutions of moxifloxacin are allowed.
Special warnings and precautions
The use of quinolone drugs is associated with possible risk development of a seizure. Moxifloxacin should be used with caution in patients with diseases of the central nervous system that predispose to the occurrence of seizures or reduce the threshold for their occurrence. The drug should not be prescribed to patients with epilepsy.
In patients with moderately severe liver failure, dosage adjustment of moxifloxacin is not performed. The use of the drug in patients with severe liver dysfunction (Child-Pugh stage C) is not recommended due to the lack of sufficient clinical experience.
When using moxifloxacin, as well as during therapy with other quinolones and macrolides, the interval may slightly increase (up to 1.2% of the initial level). Q-T. None of the 9000 patients receiving moxifloxacin experienced any associated prolongation of the interval. Q-T cardiovascular complications and deaths. However, moxifloxacin should be prescribed with caution to patients with congenital or acquired diseases accompanied by prolongation of the interval Q-T, hypokalemia, or receiving drugs that potentially slow cardiac conduction (for example, class Ia antiarrhythmic drugs (quinidine, procainamide) or class III(amiodarone, sotalol)). Degree of interval extension Q-T may increase with increasing concentration of the drug, so do not exceed the recommended dose.
The safety of moxifloxacin during pregnancy and lactation has not been established and its use is contraindicated. A small amount of the drug is excreted in breast milk.
Effect on ability to drive vehicles and work with machinery
Although moxifloxacin rarely causes adverse reactions from the central nervous system, patients should determine their individual reaction to the drug before driving or driving machinery.
It must be taken into account that during therapy with fluoroquinolones, including moxifloxacin, especially in elderly patients and patients receiving corticosteroids, the development of tenosynovitis and tendon rupture is possible. If pain and signs of inflammation of the tendon appear at the site of injury, it is recommended to stop taking the drug and reduce the load on the affected limb.
It should be taken into account that the use of broad-spectrum antibacterial drugs is associated with the risk of developing pseudomembranous colitis. Cases of pseudomembranous colitis have not been reported with the use of moxifloxacin, but caution should be exercised in prescribing the drug to patients with a history of severe diarrhea during antibiotic therapy. If severe diarrhea occurs, the drug should be discontinued and appropriate therapy should be prescribed.
In some cases, hypersensitivity and allergic reactions may develop after the first dose of the drug. Very rarely, allergic reactions can progress to the point of developing anaphylactic shock, even after the first dose of the drug. In such cases, moxifloxacin should be discontinued and appropriate therapeutic measures(including anti-shock).
When using quinolones, photosensitivity reactions are observed, although moxifloxacin does not have phototoxic properties. Patients receiving the drug should avoid direct sun rays and ultraviolet irradiation.
Children
The use of moxifloxacin in children and adolescents is not recommended, since the effectiveness and safety of the drug have not been reliably established.

Avelox drug interactions

Antacids, minerals and multivitamins. The combined use of moxifloxacin with antacids, minerals and multivitamins may cause malabsorption of the drug due to the formation of chelate complexes with polyvalent cations contained in these medicines, and this can in turn lead to a decrease in their concentration in the blood plasma. Therefore, antacids, antiretrovirals and other drugs containing calcium, magnesium, aluminum, iron should be taken at least 4 hours before or 2 hours after oral administration of moxifloxacin.
Ranitidine
The combined use of ranitidine and moxifloxacin slightly changes the absorption of the latter.
Preparations containing calcium
When taking moxifloxacin in combination with high doses preparations containing calcium did not have a clinically significant effect on the absorption of moxifloxacin, with the exception of a slight decrease in the rate of absorption.
Theophylline
Moxifloxacin does not affect the pharmacokinetics of theophylline (and vice versa), therefore, does not interact with cytochrome P450 isoenzymes of subtype 1A2.
Warfarin
When moxifloxacin is combined with warfarin, prothrombin time and other blood coagulation parameters do not change. But sometimes in patients receiving anticoagulants simultaneously with fluoroquinolones, cases of increased anticoagulant activity of antithrombotic drugs were noted. Risk factors are the presence infectious diseases(and accompanying inflammatory process), age and general state patient. Therefore, in the case of combined use of warfarin and moxifloxacin, it is necessary to adjust the dose of oral antithrombotic drugs.
Oral contraceptives
No interactions were observed between moxifloxacin and oral contraceptives.
Antidiabetic drugs
No clinically significant interaction has been established between glibenclamide and moxifloxacin.
Itraconazole
When combined with moxifloxacin, the AUC of itraconazole changes slightly. There was no significant mutual influence of the drugs, so there is no need to change the dosage regimen of any of the drugs.
Digoxin
The pharmacokinetics of digoxin did not change under the influence of moxifloxacin and vice versa.
Morphine
At parenteral administration morphine and simultaneous oral administration of moxifloxacin, a decrease in the bioavailability of the latter was not noted; The maximum concentration of moxifloxacin in blood plasma decreases slightly (17%).
Atenolol
The pharmacokinetics of atenolol are slightly altered by moxifloxacin. After taking a single dose, the AUC of atenolol increases by 4%, and the maximum plasma concentration decreases by 10%.
Probenecid
Probenecid does not affect the total and renal clearance of moxifloxacin, so there is no need for dose adjustment when used in combination.
Infusion solution of moxifoloxacin is incompatible with solutions of sodium chloride 10% and 20%, sodium bicarbonate 4.2% and 8.4%. The drug should not be administered simultaneously with other antibiotics.

Overdose of the drug Avelox, symptoms and treatment

No side effects were observed when using Avelox in healthy volunteers in single doses of up to 1.2 g or at a dose of 600 mg/day for 10 days.
In case of overdose, symptomatic therapy is carried out, combined with ECG monitoring, in accordance with the clinical situation. The use of activated carbon is advisable only in case of an overdose of moxifloxacin in tablet form; this will prevent systemic exposure to moxifloxacin at an early stage. After its intravenous administration Activated carbon slightly (20%) reduces the systemic exposure of the drug.

Storage conditions for the drug Avelox

In a dry place, protected from light, at a temperature of 8-25 ° C. Do not freeze.

List of pharmacies where you can buy Avelox:

Saint Petersburg

Antibacterial drug of the fluoroquinolone group. Has a bactericidal effect. The mechanism of action is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of the DNA synthesis of the microbial cell. In vitro, the drug is active against a wide range of gram-negative and gram-positive bacteria, mycoplasmas, chlamydia, ureaplasma, legionella, and anaerobic pathogens. Effective against bacteria resistant to beta-lactam and macrolide antibiotics.

To Avelox sensitive gram-positive aerobic bacteria: Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A), Streptococcus milled, Streptococcus mitis, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus aureus (including methicillin-sensitive strains), Staphylococcus cohnii, Staphylococcus epidermidis (including sensitive e strains to methicillin), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae; gram-negative aerobic bacteria: Haemophilus influenzae (including β-lactamase producing and non-producing strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including β-lactamase producing and non-producing strains), Escherichia coli, Enterobacter cloacae, Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii; anaerobic bacteria: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp. (including Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus), Prevotella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum; as well as Chlamydia pneumoniae, Mycoplasma pneumoniae, Legionella pneumophila, Coxiella burnettii.

Moxifloxacin less active in relation to Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholderia cepacia, Stenotrophomonas maltophilia.

The mechanisms leading to the development of resistance to penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not interfere with the antibacterial activity of moxifloxacin. There is no cross-resistance between these groups of antibacterial drugs and moxifloxacin. The overall incidence of resistance development is very low (10 -7 -10 -10). Resistance to moxifloxacin develops slowly through multiple mutations.

Cases of cross-resistance to quinolones have been reported. However, some gram-positive and anaerobic microorganisms resistant to other quinolones are sensitive to moxifloxacin.

Indications for use

Infectious and inflammatory diseases in adults caused by microorganisms sensitive to the drug:

acute sinusitis;
community-acquired pneumonia (including those caused by strains of microorganisms with multiple antibiotic resistance*);
exacerbation of chronic bronchitis;
uncomplicated skin and soft tissue infections;
complicated infections of the skin and subcutaneous structures (including infected diabetic foot).

Streptococcus pneumoniae with multiple antibiotic resistance includes strains resistant to penicillin and strains resistant to two or more antibiotics from groups such as penicillins (with minimal inhibitory activity ≥2 mg/ml), second generation cephalosporins (cefuroxime), macrolides, tetracyclines and trimethoprim/sulfamethoxazole.

Directions for use and doses

The drug is prescribed orally at 400 mg 1 time/day.

The duration of treatment for oral and intravenous administration is determined by the severity of the infection and the clinical effect and is:

at exacerbation of chronic bronchitis- 5 days;
at community-acquired pneumonia the total duration of stepwise therapy is 7-14 days, first intravenously, then orally, or 10 days orally;
at acute sinusitis and uncomplicated skin and soft tissue infections- 7 days;
at complicated infections of the skin and subcutaneous tissues- total duration of step therapy Avelox (IV administration followed by oral administration) is 7-21 days.

Tablets should be taken without chewing, washed down a small amount water, regardless of meals.

Contraindications

pregnancy;
lactation (breastfeeding);
children and adolescents up to 18 years of age;
increased sensitivity to moxifloxacin and other components of the drug.

special instructions

It should be taken into account that when prescribing Aveloxa the risk of convulsive seizures increases, therefore, the drug is prescribed with caution to patients with diseases of the central nervous system that are accompanied by seizures or predispose to their development or a decrease in the threshold of convulsive readiness, as well as when such diseases and conditions are suspected.

Due to the lack of sufficient clinical data, the use of moxifloxacin in patients with severe hepatic impairment (Child-Pugh class C) is not recommended.

During therapy with fluoroquinolones, incl. moxifloxacin, especially in the elderly and patients receiving corticosteroids, tendonitis and tendon rupture may develop. If pain or signs of tendon inflammation occur, stop taking Aveloxa and unload the affected limb.

When using Aveloxa Some patients may experience QT prolongation. In this regard, the drug should be avoided in patients with prolongation of the QT interval, hypokalemia, and also during treatment antiarrhythmic drugs class I A (quinidine, procainamide) or class III (amiodarone, sotalol), since experience with moxifloxacin in these patients is limited. Should be prescribed with caution Avelox together with drugs that prolong the QT interval (cisapride, erythromycin, antipsychotic drugs, tricyclic antidepressants), as well as in patients with conditions predisposing to arrhythmias, such as bradycardia, acute ischemia myocardium. The degree of QT interval prolongation may increase with increasing drug concentrations, so the recommended dose should not be exceeded. Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including polymorphic ventricular tachycardia. None of the 8000 patients treated with moxifloxacin experienced QT prolongation. cardiovascular complications and deaths. However, in patients with conditions predisposing to arrhythmias, the risk of developing ventricular arrhythmias may be increased when using moxifloxacin.

The use of antibiotics is associated with the risk of developing pseudomembranous colitis. This should be kept in mind if symptoms occur during treatment. Avelox severe diarrhea. In this case, the drug should be discontinued and appropriate therapy should be immediately prescribed.

There is a risk of developing hypersensitivity reactions and anaphylactic reactions during the initial use of the drug; such cases should be reported to the doctor immediately. Very rarely, an anaphylactic reaction can progress to anaphylactic shock. In such cases, you should immediately stop administering the drug and carry out appropriate resuscitation measures (including anti-shock).

When using quinolones, photosensitivity reactions are observed. However, when conducting preclinical and clinical studies, as well as when using Aveloxa V clinical practice no photosensitivity reactions were observed. However, patients should avoid direct sunlight and UV radiation while taking the drug.

Patients of different ethnic groups do not require dose adjustment.

Antibacterial drug of the fluoroquinolone group

Active substance

Release form, composition and packaging

Solution for infusion transparent, yellow or yellow with greenish color.

Excipients: - 2 g, sodium hydroxide solution 2N - 0-50 mg, hydrochloric acid 1N - 0-20 mg, water d/i - 248.659-248.664 g.

250 ml - clear glass bottles with a capacity of 300 ml (1) - cardboard packs.
250 ml - polymer containers, sealed in protective bags (12) - cardboard boxes.

pharmachologic effect

The minimum bactericidal concentrations of the drug are generally comparable to its MIC.

Mechanisms of resistance

The mechanisms leading to the development of resistance to penicillins, cephalosporins, aminoglycosides, macrolides and do not affect the antibacterial activity of moxifloxacin. There is no cross-resistance between these groups of antibacterial drugs and moxifloxacin. So far, no cases of plasmid resistance have been observed either. The overall incidence of resistance development is very low (10 -7 -10 -10). Resistance to moxifloxacin develops slowly through multiple mutations. Repeated exposure of microorganisms to moxifloxacin at concentrations below the MIC is accompanied by only a slight increase. Cases of cross-resistance to quinolones have been reported. However, some gram-positive and anaerobic microorganisms resistant to other quinolones remain sensitive to moxifloxacin.

It has been established that the addition of a methoxy group at position C8 to the structure of the moxifloxacin molecule increases the activity of moxifloxacin and reduces the formation of resistant mutant strains of gram-positive bacteria. The addition of a bicycloamine group at position C7 prevents the development of active efflux, a mechanism of resistance to fluoroquinolones.

Moxifloxacin is active in vitro against a wide range of gram-negative and gram-positive microorganisms, anaerobes, acid-fast bacteria and atypical bacteria, such as Mycoplasma spp.., Chlamydia spp., Legionella spp., as well as bacteria resistant to beta-lactam and macrolide antibiotics.

Effect on human intestinal microflora

In two studies conducted on volunteers, the following changes were noted: intestinal microflora after oral administration of moxifloxacin: decreased concentrations of Escherichia coli, Bacillus spp., Bacteroides vulgatus, Enterococcus spp., Klebsiella spp., as well as anaerobes Bifidobacterium spp., Eubacterium spp., Peptostreptococcus spp. These changes were reversible within two weeks. No Clostridium difficile toxins were detected.

In vitro susceptibility testing

The spectrum of antibacterial activity of moxifloxacin includes the following microorganisms:

Sensitive	Moderately sensitive	Resistant
*Gram-positive*
Gardnerella vaginalis
Streptococcus pneumoniae (including strains resistant to penicillin and strains with multiple antibiotic resistance), as well as strains resistant to two or more antibiotics, such as penicillin (MIC≥2 μg/ml), second generation cephalosporins (eg), macrolides , tetracyclines, trimethoprim/sulfamethoxazole
Streptococcus pyogenes (group A)*
Streptococcus milleri group (S. anginosus, S. constellatus and S. intermedius)
Streptococcus viridans group (S. viridans, S. mutans, S. mitis, S. sanguinis, S. salivarius, S. thermophilus, S. constellatus)
Streptococcus agalactiae
Streptococcus dysagalactiae
Staphylococcus aureus (methicillin-sensitive strains)*		Staphylococcus aureus (strains resistant to methicillin/ofloxacin)**
Coagulase-negative Staphylococcus spp. (S. cohnii, S. epidermidis, S. haemolyticus, S. hominis, S. saprophyticus, S. simulans), methicillin-sensitive strains		Coagulase-negative Staphylococcus spp. (S. cohnii, S. epidermidis, S. haemolyticus, S. hominis, S. saprophyticus, S. simulans), methicillin-resistant strains
	Enterococcus faecalis* (strains sensitive to vancomycin and gentamicin only)
	Enterococcus avium*
	Enterococcus faecicum*
Gram-negative
Haemophilus influenzae (including β-lactamase-producing and non-β-lactamase-producing strains)*
Haemophillus parainfluenzae*
Moraxella catarrhalis (including β-lactamase-producing and non-β-lactamase-producing strains)*
Bordetella pertussis
Legionella pneumophila	Escherichia coli* a
Acinetobacter baumannii	Klebsiella pneumoniae*a
	Klebsiella oxytoca
	Citrobacter freundii*
	Enterobacter spp. (E. aerogenes, E. intermedius, E. sakazaki)
	Enterobacter cloacae*
	Pantoea agglomerans
		Pseudomonas aeruginosa
	Pseudomonas fluorescens
	Burkholderia cepacia
	Stenotrophomonas maltophilia
	Proteus mirabilis*
Proteus vulgaris
	Morganella morganii
	Neisseria gonorrhoeae*
	Providencia spp. (P. rettgeri, P. stuartii)
Anaerobes
	Bacteroides spp. (B. fragilis, B. distasoni, B. thetaiotaomicron, B. ovatus, B. uniformis, B. vulgaris)
Fusobacterium spp.
	Peptostreptococcus spp.*
Porphyromonas spp.
Prevotella spp.
Propionibacterium spp.
	Clostridium spp.*
Atypical
Chlamydia pneumoniae*
Chlamydia trachomatis*
Mycoplasma pneumoniae*
Mycoplasma hominis
Mycoplasma genitalium
Legionella pneumophila*
Coxiella burnettii

* - sensitivity to moxifloxacin is confirmed by clinical data.

** - the use of Avelox is not recommended for the treatment of infections caused by methicillin-resistant Staphylococcus aureus (MRSA). Suspected or confirmed MRSA infections should be treated with appropriate antibacterial drugs.

a - development of acquired resistance is possible.

For certain strains, the distribution of acquired resistance may vary across geographic regions and over time. Therefore, it is desirable to have local information on resistance when testing strain susceptibility, especially when treating severe infections.

If in patients undergoing treatment in a hospital, the AUC/MIC 90 value exceeds 125, and C max /MIC 90 is in the range of 8-10, then this suggests clinical improvement. In outpatients, the values of these surrogate parameters are usually lower: AUC/MIC 90 >30-40.

* AUIC - area under the inhibition curve (AUC/MIC ratio 90)

Pharmacokinetics

Suction

After oral administration, moxifloxacin is absorbed quickly and almost completely.

Absolute bioavailability after oral administration and intravenous infusion is about 91%.

The pharmacokinetics of moxifloxacin when taken at a dose of 50 to 1200 mg once, as well as 600 mg/day for 10 days, is linear.

After a single dose of moxifloxacin at a dose of 400 mg, Cmax in the blood is reached within 0.5-4 hours and is 3.1 mg/l. After oral administration of 400 mg of moxifloxacin 1 time/day, C ss max and C ss min are 3.2 mg/l and 0.6 mg/l, respectively.

When taking moxifloxacin with food, there is a slight increase in the time to reach Cmax (by 2 hours) and a slight decrease in Cmax (by approximately 16%), while the duration of absorption does not change. However, these data do not have clinical significance, and the drug can be used regardless of food intake.

After a single infusion of Avelox at a dose of 400 mg over 1 hour, Cmax is reached at the end of the infusion and is 4.1 mg/l, which corresponds to an increase of approximately 26% compared to the value of this indicator when taken orally. The exposure of the drug, determined by AUC, is slightly higher than that when taking the drug orally.

With multiple intravenous infusions at a dose of 400 mg lasting 1 hour, C ss max and C ss min vary from 4.1 mg/l to 5.9 mg/l and from 0.43 mg/l to 0.84 mg/l, respectively. Average C ss equal to 4.4 mg/l is achieved at the end of the infusion.

Distribution

The equilibrium state is achieved within 3 days.

Binding to blood proteins (mainly albumin) is about 45%.

Moxifloxacin is rapidly distributed in organs and tissues. Vd is approximately 2 l/kg.

High concentrations of moxifloxacin, exceeding those in plasma, are created in the lung tissue (including in epithelial fluid, alveolar macrophages), in the nasal sinuses (maxillary and ethmoid sinuses), in nasal polyps, foci of inflammation (in the contents of blisters in skin lesions ). In interstitial fluid and saliva, moxifloxacin is determined in a free form, not bound to proteins, in a concentration higher than in plasma. In addition, high concentrations of moxifloxacin are determined in the tissues of the abdominal organs, peritoneal fluid, as well as in the tissues of the female genital organs.

Metabolism

Moxifloxacin undergoes phase 2 biotransformation and is excreted from the body by the kidneys and also through the intestines, both unchanged and in the form of inactive sulfo compounds (M1) and glucuronides (M2). Moxifloxacin is not biotransformed by the microsomal cytochrome P450 system. Metabolites M1 and M2 are present in plasma in concentrations lower than the parent compound. Based on the results of preclinical studies, it was proven that these metabolites do not have a negative effect on the body in terms of safety and tolerability.

Removal

T1/2 is approximately 12 hours. The average total clearance after taking the drug orally and after intravenous administration at a dose of 400 mg is 179-246 ml/min.

Renal clearance is 24-53 ml/min. This indicates partial tubular reabsorption of the drug.

The mass balance of parent compound and phase 2 metabolites is approximately 96-98%, indicating the absence of oxidative metabolism. About 22% of a single dose (400 mg) is excreted unchanged by the kidneys, about 26% through the intestines.

Pharmacokinetics in special clinical situations

A study of the pharmacokinetics of moxifloxacin in men and women revealed differences of 33% in terms of AUC and Cmax. The absorption of moxifloxacin did not depend on gender. Differences in AUC and Cmax were due to differences in body weight rather than gender and are not considered clinically significant.

There were no clinically significant differences in the pharmacokinetics of moxifloxacin in patients of different ethnic groups and different ages.

Pharmacokinetic studies of moxifloxacin have not been conducted in children.

There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including those with CC<30 мл/мин/1.73 м 2) и у пациентов, находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе.

There were no significant differences in moxifloxacin concentrations in patients with hepatic impairment (Child-Pugh classes A and B) compared with healthy volunteers and patients with normal hepatic function.

Indications

Infectious and inflammatory diseases in adults caused by microorganisms sensitive to the drug:

acute sinusitis;
exacerbation of chronic bronchitis;
community-acquired pneumonia (including those caused by strains of microorganisms with multiple antibiotic resistance*);
uncomplicated skin and soft tissue infections;
complicated infections of the skin and subcutaneous structures (including infected diabetic foot);
complicated intra-abdominal infections, including polymicrobial infections, incl. intraperitoneal abscesses;
uncomplicated inflammatory diseases of the pelvic organs (including salpingitis and endometritis).

* - Streptococcus pneumoniae with multiple antibiotic resistance includes strains resistant to penicillin and strains resistant to two or more antibiotics from groups such as penicillins (with MIC ≥2 mg/ml), second generation cephalosporins (cefuroxime), macrolides, tetracyclines and trimethoprim/sulfamethoxazole.

Current official guidelines on the use of antibacterial agents must be taken into account.

Contraindications

a history of tendon pathology that developed as a result of treatment with quinolone antibiotics;
in preclinical and clinical studies, after the administration of moxifloxacin, changes in electrophysiological parameters of the heart were observed, expressed in prolongation of the QT interval. In this regard, the use of moxifloxacin is contraindicated in patients of the following categories: congenital or acquired documented prolongation of the QT interval, electrolyte disturbances, especially uncorrected hypokalemia; clinically significant bradycardia; clinically significant heart failure with reduced left ventricular ejection fraction; a history of rhythm disturbances accompanied by clinical symptoms;
moxifloxacin should not be used with other drugs that prolong the QT interval;
due to the presence of lactose in the drug, its use is contraindicated in cases of congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption (for tablets);
due to the limited amount of clinical data, the use of moxifloxacin is contraindicated in patients with impaired liver function (class C according to the Child-Pugh classification) and in patients with increased transaminases more than 5 times the ULN;
pregnancy;
lactation (breastfeeding);
age under 18 years;
hypersensitivity to moxifloxacin, other quinolones or any other component of the drug.

WITH caution used for diseases of the central nervous system (including diseases suspected of involving the central nervous system), predisposing to the occurrence of convulsive seizures and reducing the threshold of convulsive readiness; in patients with potentially proarrhythmic conditions such as acute myocardial ischemia, especially women and elderly patients; for myasthenia gravis; with cirrhosis of the liver; when taken simultaneously with drugs that reduce potassium levels.

Dosage

The drug is prescribed orally and intravenously at 400 mg 1 time/day.

The duration of treatment with Avelox when administered orally and intravenously is determined by the severity of the infection and the clinical effect and is: exacerbation of chronic bronchitis- 5-10 days; at community-acquired pneumonia the total duration of step therapy (IV administration followed by oral administration) is 7-14 days, first IV, then orally, or 10 days orally; at acute sinusitis and uncomplicated skin and soft tissue infections- 7 days; at complicated infections of the skin and subcutaneous tissues the total duration of stepwise therapy (iv administration followed by oral administration) is 7-21 days; at complicated intra-abdominal infections the total duration of stepwise therapy (iv administration of the drug followed by oral administration) is 5-14 days; at uncomplicated inflammatory diseases of the pelvic organs - 14 days.

The duration of treatment with Avelox can be up to 21 days.

Changes in dosage regimen elderly patients not required.

Efficacy and safety of moxifloxacin in children and teenagers not installed.

Patients with liver dysfunction no change in dosage regimen is required.

In patients with impaired renal function (including severe renal failure with CC ≤ 30 ml/min/1.73 m2), as well as in patients on continuous hemodialysis and long-term ambulatory peritoneal dialysis, no change in dosage regimen is required .

In patients of different ethnic groups, no change in dosage regimen is required.

The tablets should be taken without chewing, with a small amount of water, regardless of meals. Do not exceed the recommended dose.

The solution for infusion should be administered intravenously over 60 minutes. The drug can be administered either diluted or undiluted using a T-piece). Avelox solution is compatible with the following solutions: sodium chloride solution 0.9%, sodium chloride solution 1M, dextrose solution 5%, dextrose solution 10%, dextrose solution 40%, xylitol solution 20%, Ringer's lactate solution.

Only clear solution should be used.

After dilution with compatible solvents, the Avelox solution remains stable for 24 hours at room temperature. Because the solution cannot be frozen or refrigerated, it should not be stored in the refrigerator. When cooled, the solution may precipitate, but at room temperature the precipitate usually dissolves. The solution should be stored in its original packaging.

If the solution for infusion is prescribed together with other drugs, then each drug should be administered separately.

Side effects

Data on adverse reactions reported with moxifloxacin 400 mg (orally, step-down therapy [IV followed by oral administration] and IV alone) are derived from clinical studies and post-marketing reports (highlighted). italics ). Adverse reactions listed in the "common" group occurred with an incidence of less than 3%, with the exception of nausea and diarrhea.

In each frequency group, adverse drug reactions are listed in descending order of importance. Determination of the frequency of adverse reactions: often (from ≥1/100 to<1/10), нечасто (от ≥1/1000 до <1/100), редко (от ≥1/10 000 до <1/1000), очень редко (<1/10 000).

Infections: fungal infections.

From the hematopoietic system: uncommon - anemia, leukopenia, neutropenia, thrombocytopenia, thrombocythemia, prolongation of prothrombin time and increase in INR; rarely - changes in thromboplastin concentration; very rarely - an increase in prothrombin concentration and a decrease in INR.

From the immune system: uncommon - allergic reactions, urticaria, itching, rash, eosinophilia; rarely - anaphylactic/anaphylactoid reactions, angioedema, including laryngeal edema (potentially life-threatening); very rarely - anaphylactic/anaphylactoid shock (including potentially life-threatening).

From the exchange side substances: uncommon - hyperlipidemia; rarely - hyperglycemia, hyperuricemia.

Mental disorders: infrequently - anxiety, psychomotor hyperreactivity, agitation; rarely - emotional lability, depression ( in very rare cases, self-harming behavior such as suicidal ideation or suicide attempts may occur ), hallucinations; very rarely - depersonalization, psychotic reactions ( potentially manifesting in self-harming behavior such as suicidal ideation or suicide attempts).

From the nervous system: often - dizziness, headache; uncommon - paresthesia, dysesthesia, taste disturbances (including in very rare cases ageusia), confusion, disorientation, sleep disturbances, tremor, vertigo, drowsiness; rarely - hypoesthesia, olfactory disturbances (including anosmia), atypical dreams, loss of coordination (including gait disturbances due to dizziness or vertigo, in very rare cases leading to injury due to a fall, especially in elderly patients) , seizures with various clinical manifestations (including “grand mal” seizures), attention disorders, speech disorders, amnesia, peripheral neuropathy, polyneuropathy; very rarely - hyperesthesia.

From the side of the organ of vision: infrequently - visual impairment (especially with reactions from the central nervous system); very rarely - transient loss of vision (especially with reactions from the central nervous system).

On the part of the hearing organ: rarely - tinnitus, hearing impairment, including deafness (usually reversible).

From the cardiovascular system: often - prolongation of the QT interval in patients with concomitant hypokalemia; uncommon - prolongation of the QT interval, palpitations, tachycardia, vasodilation; rarely - increased blood pressure, decreased blood pressure, fainting, ventricular tachyarrhythmias; very rarely - nonspecific arrhythmias, polymorphic ventricular tachycardia (pirouette type), cardiac arrest (mainly in persons with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia).

From the respiratory system: infrequently - shortness of breath, including asthmatic conditions.

From the digestive system: often - nausea, vomiting, abdominal pain, diarrhea; uncommon - decreased appetite and reduced food consumption, constipation, dyspepsia, flatulence, gastroenteritis (except erosive gastroenteritis), increased amylase activity; rarely - dysphagia, stomatitis, pseudomembranous colitis (in very rare cases associated with life-threatening complications).

From the liver and biliary tract: often - increased activity of liver transaminases; uncommon - liver dysfunction (including increased LDH activity), increased bilirubin concentration, increased GGT and alkaline phosphatase activity; rarely - jaundice, hepatitis (mainly cholestatic); very rarely - fulminant hepatitis, potentially leading to life-threatening liver failure (including fatal cases).

From the skin: very rarely - bullous skin reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis (potentially life-threatening).

From the musculoskeletal system: infrequently - arthralgia, myalgia; rarely - tendinitis, increased muscle tone and cramps, muscle weakness; very rarely - arthritis, tendon ruptures, gait disturbance due to damage to the musculoskeletal system, increased symptoms of myasthenia gravis.

From the urinary system: infrequently - dehydration (caused by diarrhea or decreased fluid intake); rarely - impaired renal function, renal failure as a result of dehydration, which can lead to kidney damage, especially in elderly patients with pre-existing impaired renal function).

From the body as a whole: infrequently - general malaise, nonspecific pain, sweating.

Local reactions: often - reactions at the injection/infusion site; infrequently - phlebitis/thrombophlebitis at the infusion site.

The incidence of the following adverse reactions was higher in the group receiving stepwise therapy: often - increased GGT activity; uncommon - ventricular tachyarrhythmias, arterial hypotension, edema, pseudomembranous colitis (in very rare cases associated with life-threatening complications), convulsions with various clinical manifestations (including “grand mal” seizures), hallucinations, impaired renal function, renal failure (due to dehydration, which can lead to kidney damage, especially in older patients with pre-existing renal impairment).

Overdose

There are limited data on overdose with moxifloxacin. There were no side effects observed when using Avelox at a dose of up to 1200 mg once and 600 mg for 10 days or more.

Treatment: in case of overdose, symptomatic and supportive therapy with ECG monitoring is carried out in accordance with the clinical situation.

The use of activated charcoal immediately after oral administration of the drug may help prevent excessive systemic exposure to moxifloxacin in cases of overdose.

Drug interactions

No dose adjustment is required when using Avelox together with atenolol, ranitidine, calcium-containing supplements, theophylline, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenecid (the absence of clinically significant interaction with moxifloxacin has been confirmed).

The possible additive QT interval prolonging effect of moxifloxacin and other drugs that affect QT prolongation should be considered. Due to the combined use of moxifloxacin and drugs that affect the prolongation of the QT interval, the risk of developing ventricular arrhythmia, including polymorphic ventricular tachycardia of the "pirouette" type, increases. The combined use of moxifloxacin with the following drugs that affect the prolongation of the QT interval is contraindicated: class IA antiarrhythmic drugs (including quinidine, hydroquinidine, disopyramide); class III antiarrhythmic drugs (including amiodarone, sotalol, dofetilide, ibutilide); neuroleptics (including phenothiazine, pimozide, sertindole, haloperidol, sultopride); tricyclic antidepressants; antimicrobials (sparfloxacin, IV erythromycin, pentamidine, antimalarials, especially halofantrine); antihistamines (terfenadine, astemizole, mizolastine); others (cisapride, IV vincamine), bepridil, difemanil.

Ingestion of Avelox and antacids, multivitamins and minerals may interfere with the absorption of moxifloxacin due to the formation of chelate complexes with polyvalent cations contained in these drugs. As a result, moxifloxacin plasma concentrations may be significantly lower than therapeutic levels. In this regard, antacids, antiretrovirals (for example, didanosine) and other drugs containing calcium, magnesium, aluminum, iron, sucralfate, zinc should be taken at least 4 hours before or 4 hours after taking Avelox orally.

When Avelox is used in combination with warfarin, prothrombin time and other blood coagulation parameters do not change.

In patients receiving anticoagulants in combination with antibiotics, incl. with moxifloxacin, there have been cases of increased anticoagulant activity of anticoagulant drugs. Risk factors are the presence of an infectious disease (and concomitant inflammatory process), age and general condition of the patient. Despite the fact that there is no interaction between moxifloxacin and warfarin, in patients receiving concomitant treatment with these drugs, it is necessary to monitor the INR and, if necessary, adjust the dose of indirect anticoagulants.

Moxifloxacin and digoxin do not have a significant effect on each other's pharmacokinetic parameters. When moxifloxacin was re-administered, digoxin C max increased by approximately 30%. In this case, the ratio of AUC and C min of digoxin does not change.

With the simultaneous use of activated carbon and moxifloxacin orally at a dose of 400 mg, the systemic bioavailability of the drug is reduced by more than 80% as a result of slower absorption. In case of overdose, the use of activated carbon at an early stage of absorption prevents a further increase in systemic exposure.

When administered intravenously with simultaneous oral administration of activated carbon, the systemic bioavailability of the drug is slightly reduced (by approximately 20%) due to the adsorption of moxifloxacin in the gastrointestinal tract during enterohepatic circulation.

The absorption of moxifloxacin is not affected by concomitant ingestion of food (including dairy products). Moxifloxacin can be taken with or without food.

Incompatibility

Moxifloxacin infusion solution cannot be administered simultaneously with the following drugs: sodium chloride solution 10%, sodium chloride solution 20%, solution 4.2%, sodium bicarbonate solution 8.4%.

special instructions

When using the drug Avelox, some patients may experience prolongation of the QT interval.

Avelox should be used with caution in women and elderly patients. Because women have a longer QT interval than men, they may be more sensitive to drugs that prolong the QT interval. Elderly patients are also more susceptible to drugs that affect the QT interval.

The degree of QT interval prolongation may increase with increasing drug concentrations, so the recommended dose should not be exceeded. Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including polymorphic ventricular tachycardia. However, in patients with pneumonia, a correlation between moxifloxacin plasma concentrations and prolongation of the QT interval was noted. None of the 9,000 patients receiving Avelox experienced cardiovascular complications or deaths associated with QT prolongation.

When using Avelox, the risk of developing ventricular arrhythmias may increase in patients with conditions predisposing to arrhythmias.

In this regard, Avelox is contraindicated:

patients with established prolongation of the QT interval;
patients with uncorrected hypokalemia;
patients with conditions predisposing to arrhythmias, such as clinically significant bradycardia.

Avelox should be used with caution:

in patients with potentially proarrhythmic conditions such as acute myocardial ischemia;
in patients with liver cirrhosis (since in this category of patients the risk of developing QT prolongation cannot be excluded).

Cases of fulminant hepatitis, potentially leading to liver failure (including fatal cases), have been reported while taking Avelox. The patient should be informed that if symptoms of liver failure occur, it is necessary to consult a doctor before continuing treatment with Avelox.

Cases of bullous skin lesions (such as Stevens-Johnson syndrome or toxic epidermal necrolysis) have been reported while taking Avelox. The patient should be informed that if symptoms of skin or mucous membrane lesions occur, it is necessary to consult a doctor before continuing treatment with Avelox.

The use of quinolone drugs is associated with a possible risk of developing seizures. Avelox should be used with caution in patients with diseases of the central nervous system and disorders of the central nervous system that predispose to seizures or lower the threshold for seizure activity.

The use of broad-spectrum antibacterial drugs, including Avelox, is associated with a risk of developing pseudomembranous colitis associated with antibiotic use. This diagnosis should be kept in mind in patients who develop severe diarrhea during treatment with Avelox. In this case, appropriate therapy should be prescribed immediately. Drugs that inhibit intestinal motility are contraindicated in the development of severe diarrhea.

Avelox should be used with caution in patients with myasthenia gravis due to a possible exacerbation of the disease.

During therapy with quinolones, incl. moxifloxacin, tendonitis and tendon rupture may develop, especially in the elderly and patients receiving corticosteroids. Cases have been described that occurred within several months after completion of treatment. At the first symptoms of pain or inflammation at the site of injury, the drug should be stopped and the affected limb should be unloaded.

When using quinolones, photosensitivity reactions are observed. However, during preclinical and clinical studies, as well as when using the drug Avelox in practice, no photosensitivity reactions were observed. However, patients receiving Avelox should avoid exposure to direct sunlight and ultraviolet light.

The use of the drug in the form of tablets for oral administration is not recommended in patients with complicated inflammatory diseases of the pelvic organs (for example, associated with tubo-ovarian or pelvic abscesses).

The use of moxifloxacin is not recommended for the treatment of infections caused by methicillin-resistant strains of Staphylococcus aureus. Suspected or confirmed MRSA infections should be treated with appropriate antibacterial drugs.

The ability of Avelox to inhibit the growth of mycobacteria may cause in vitro interaction of moxifloxacin with the test for Mycobacterium spp., leading to false negative results when analyzing samples from patients who are being treated with Avelox during this period. In patients treated with quinolones, including Avelox, cases of sensory or sensorimotor polyneuropathy leading to paresthesia, hypoesthesia, dysesthesia or weakness have been described. Patients being treated with Avelox should be advised to seek immediate medical attention before continuing treatment if symptoms of neuropathy, including pain, burning, tingling, numbness or weakness, occur.

Psychiatric reactions can occur even after the first prescription of fluoroquinolones, including moxifloxacin. In very rare cases, depression or psychotic reactions progress to suicidal thoughts and behavior with a tendency to self-harm, including suicide attempts. If patients develop such reactions, the drug Avelox should be discontinued and the necessary measures taken. Caution should be exercised when prescribing Avelox to patients with psychosis and patients with a history of psychiatric diseases.

Due to the widespread and increasing incidence of infections caused by fluoroquinolone-resistant Neisseria gonorrhoeae, moxifloxacin monotherapy should not be used in the treatment of patients with pelvic inflammatory disease, unless the presence of fluoroquinolone-resistant N. gonorrhoeae is excluded. If the presence of fluoroquinolone-resistant N. gonorrhoeae cannot be excluded, consideration should be given to supplementing empiric moxifloxacin therapy with an appropriate antibiotic that is active against N. gonorrhoeae (eg, a cephalosporin).

Patients on a low-salt diet (with heart failure, renal failure, nephrotic syndrome) should take into account that the solution for infusion contains sodium chloride.

Impact on the ability to drive vehicles and operate machinery

Fluoroquinolones, including moxifloxacin, may impair the ability of patients to drive a car and engage in other potentially hazardous activities that require increased attention and speed of psychomotor reactions due to their effects on the central nervous system and visual impairment.

Pregnancy and lactation

IN animal research reproductive toxicity has been shown. The potential risk to humans is unknown.

Like other quinolones, moxifloxacin causes cartilage damage in large joints in premature animals. Preclinical studies have shown that small amounts of moxifloxacin are excreted into breast milk. There are no data on its use in women during lactation. Therefore, the use of moxifloxacin during breastfeeding is contraindicated.

Use in childhood

Contraindicated: children and adolescents under 18 years of age .

For impaired renal function

Patients with impaired renal function(including with CC<30 мл/мин/1.73 м 2), а также

Storage conditions and periods

The solution for infusion should be stored out of the reach of children at a temperature of 15° to 30°C. The shelf life of the drug in bottles is 5 years, in polymer containers - 3 years.

Instructions for use

Active ingredients

Release form

Pills

Compound

1 tablet contains: Active substance: moxifloxacin hydrochloride 436.8 mg (corresponds to moxifloxacin base - 400 mg)

Pharmacological effect

Broad-spectrum antibacterial bactericidal drug, 8-methoxyfluoroquinolone. The bactericidal effect of moxifloxacin is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of the processes of replication, repair and transcription of microbial cell DNA biosynthesis and, as a consequence, to the death of microbial cells. The minimum bactericidal concentrations of the drug are generally comparable to its MIC. Resistance mechanisms: Mechanisms leading to the development of resistance to penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not affect the antibacterial activity of moxifloxacin. There is no cross-resistance between these groups of antibacterial drugs and moxifloxacin. So far, no cases of plasmid resistance have been observed either. The overall incidence of resistance is very low (10-7-10-10). Resistance to moxifloxacin develops slowly through multiple mutations. Repeated exposure of microorganisms to moxifloxacin at concentrations below the MIC is accompanied by only a slight increase. Cases of cross-resistance to quinolones have been reported. However, some gram-positive and anaerobic microorganisms resistant to other quinolones remain sensitive to moxifloxacin. It has been established that the addition of a methoxy group at position C8 to the structure of the moxifloxacin molecule increases the activity of moxifloxacin and reduces the formation of resistant mutant strains of gram-positive bacteria. The addition of a bicycloamine group at position C7 prevents the development of active efflux, a mechanism of resistance to fluoroquinolones. Moxifloxacin is active in vitro against a wide range of gram-negative and gram-positive microorganisms, anaerobes, acid-fast bacteria and atypical bacteria, such as Mycoplasma spp., Chlamydia spp., Legionella spp., as well as bacteria resistant to beta-lactam and macrolide antibiotics. Effect on human intestinal microflora: In two studies conducted on volunteers, the following changes in intestinal microflora were noted after oral administration of moxifloxacin: decreased concentrations of Escherichia coli, Bacillus spp., Bacteroides vulgatus, Enterococcus spp., Klebsiella spp., as well as the anaerobes Bifidobacterium spp. , Eubacterium spp., Peptostreptococcus spp. These changes were reversible within two weeks. No Clostridium difficile toxins were detected.

Pharmacokinetics

Absorption: After oral administration, moxifloxacin is absorbed quickly and almost completely. Absolute bioavailability is about 91%. The pharmacokinetics of moxifloxacin when taken at a dose of 50 to 1200 mg once, as well as 600 mg/day for 10 days, is linear. After a single dose of moxifloxacin at a dose of 400 mg, Cmax in the blood is reached within 0.5-4 hours and is 3.1 mg/l. After oral administration of moxifloxacin at a dose of 400 mg 1 time/day, Cssmax and Cssmin are 3.2 mg/l and 0.6 mg/l, respectively. When taking moxifloxacin with food, there is a slight increase in the time to reach Cmax (by 2 hours) and a slight decrease in Cmax (by approximately 16%), while the duration of absorption does not change. However, these data do not have clinical significance, and the drug can be used regardless of food intake. Distribution: Equilibrium state is achieved within 3 days. Binding to blood proteins (mainly albumin) is about 45%. Moxifloxacin is rapidly distributed in organs and tissues. Vd is approximately 2 l/kg. High concentrations of moxifloxacin, exceeding those in plasma, are created in the lung tissue (including in epithelial fluid, alveolar macrophages), in the nasal sinuses (maxillary and ethmoid sinuses), in nasal polyps, foci of inflammation (in the contents of blisters in skin lesions ). In interstitial fluid and saliva, moxifloxacin is determined in a free form, not bound to proteins, in a concentration higher than in plasma. In addition, high concentrations of moxifloxacin are determined in the tissues of the abdominal organs, peritoneal fluid, as well as in the tissues of the female genital organs. Metabolism: Moxifloxacin undergoes phase 2 biotransformation and is excreted from the body by the kidneys, as well as through the intestines, both unchanged and in the form of inactive sulfo compounds (M1) and glucuronides (M2). Moxifloxacin is not biotransformed by the microsomal cytochrome P450 system. Metabolites M1 and M2 are present in plasma in concentrations lower than the parent compound. Based on the results of preclinical studies, it was proven that these metabolites do not have a negative effect on the body in terms of safety and tolerability. Elimination: T1/2 is approximately 12 hours. The average total clearance after taking the drug orally at a dose of 400 mg is 179-246 ml/min. Renal clearance is 24-53 ml/min. This indicates partial tubular reabsorption of the drug. The mass balance of parent compound and phase 2 metabolites is approximately 96-98%, indicating the absence of oxidative metabolism. About 22% of a single dose (400 mg) is excreted unchanged by the kidneys, about 26% through the intestines. Pharmacokinetics in special patient populations: When studying the pharmacokinetics of moxifloxacin in men and women, differences of 33% were found in AUC and Cmax. The absorption of moxifloxacin did not depend on gender. Differences in AUC and Cmax were due to differences in body weight rather than gender and are not considered clinically significant. There were no clinically significant differences in the pharmacokinetics of moxifloxacin in patients of different ethnic groups and different ages. Pharmacokinetic studies of moxifloxacin have not been conducted in children. There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including those with CC less than 30 ml/min/1.73 m2) and in patients on continuous hemodialysis and long-term ambulatory peritoneal dialysis. There were no significant differences in moxifloxacin concentrations in patients with hepatic impairment (Child-Pugh classes A and B) compared with healthy volunteers and patients with normal hepatic function.

Indications

Infectious and inflammatory diseases in adults caused by microorganisms sensitive to the drug: Acute sinusitis. Exacerbation of chronic bronchitis. Community-acquired pneumonia (including those caused by strains of microorganisms with multiple resistance to antibiotics *). Uncomplicated infections of the skin and soft tissues. Complicated infections of the skin and subcutaneous structures (including infected diabetic foot). Complicated intra-abdominal infections, including polymicrobial infections, incl. Intraperitoneal abscesses. Uncomplicated inflammatory diseases of the pelvic organs (including salpingitis and endometritis).* streptococcus pneumoniae with multiple antibiotic resistance includes strains resistant to penicillin and strains resistant to two or more antibiotics from groups such as penicillins ( with MIC ≥2 mg/ml), second generation cephalosporins (cefuroxime), macrolides, tetracyclines and trimethoprim/sulfamethoxazole. It is necessary to take into account the current official guidelines on the rules for the use of antibacterial agents.

Contraindications

A history of tendon pathology that developed as a result of treatment with quinolone antibiotics. In preclinical and clinical studies, after the administration of moxifloxacin, a change in the electrophysiological parameters of the heart was observed, expressed in a lengthening of the interval. In this regard, the use of moxifloxacin is contraindicated in patients of the following categories: congenital or acquired documented prolongation of the interval, electrolyte disturbances, especially uncorrected hypokalemia. Clinically significant bradycardia. Clinically significant heart failure with reduced left ventricular ejection fraction. A history of rhythm disturbances accompanied by clinical symptoms. Moxifloxacin should not be used with other drugs that prolong the interval. Due to the presence of lactose in the drug, its use is contraindicated in cases of congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption (for tablets). Due to the limited amount of clinical data, the use of moxifloxacin is contraindicated in patients with impaired liver function (class C according to the Child-Pugh classification) and in patients with elevated transaminases more than 5 times the maximum value. Pregnancy. Lactation (breastfeeding). Age up to 18 years. Hypersensitivity to moxifloxacin, other quinolones or any other component of the drug. The drug should be prescribed with caution for diseases of the central nervous system (including diseases suspected of involving the central nervous system), predisposing to the occurrence of convulsive seizures and reducing the threshold of convulsive readiness. In patients with a history of psychosis and/or psychiatric illness. In patients with potentially proarrhythmic conditions such as acute myocardial ischemia and cardiac arrest, especially women and elderly patients. For myasthenia gravis. For cirrhosis of the liver. When taken simultaneously with drugs that reduce potassium levels. In patients with a genetic predisposition or actual deficiency of glucose-6-phosphate dehydrogenase. Use during pregnancy and breastfeeding The safety of moxifloxacin during pregnancy has not been established and its use is contraindicated. Cases of reversible joint damage have been described in children receiving some quinolones, but this effect has not been reported in the fetus (when used by the mother during pregnancy). Reproductive toxicity has been shown in animal studies. The potential risk to humans is unknown. Like other quinolones, moxifloxacin causes cartilage damage in large joints in premature animals. Preclinical studies have shown that small amounts of moxifloxacin are excreted in breast milk. There are no data on its use in women during lactation. Therefore, the use of moxifloxacin during breastfeeding is contraindicated.

Precautionary measures

The drug should be prescribed with caution for diseases of the central nervous system (including diseases suspected of involving the central nervous system), predisposing to the occurrence of convulsive seizures and reducing the threshold of convulsive readiness; in patients with a history of psychosis and/or psychiatric illness, in patients with potentially proarrhythmic conditions such as acute myocardial ischemia and cardiac arrest, especially in women and elderly patients, with myasthenia gravis, with cirrhosis of the liver, when taken simultaneously with drugs, reducing potassium content; in patients with a genetic predisposition or actual deficiency of glucose-6-phosphate dehydrogenase.

Use during pregnancy and breastfeeding

The safety of moxifloxacin during pregnancy has not been established and its use is contraindicated. Cases of reversible joint damage have been described in children receiving some quinolones, but this effect has not been reported in the fetus (when used by the mother during pregnancy). Reproductive toxicity has been shown in animal studies. The potential risk to humans is unknown. Like other quinolones, moxifloxacin causes cartilage damage in large joints in premature animals. Preclinical studies have shown that small amounts of moxifloxacin are excreted in breast milk. There are no data on its use in women during lactation. Therefore, the use of moxifloxacin during breastfeeding is contraindicated.

Directions for use and doses

The drug is prescribed orally at 400 mg 1 time/day. The tablets should be taken without chewing, with plenty of water, regardless of meals. Do not exceed the recommended dose. The duration of treatment with Avelox when taken orally is determined by the severity of the infection and the clinical effect and is: for exacerbation of chronic bronchitis - 5-10 days; for community-acquired pneumonia, the total duration of stepwise therapy (IV administration followed by oral administration) is 7-14 days, first IV, then orally, or 10 days orally; for acute sinusitis and uncomplicated infections of the skin and soft tissues - 7 days; for complicated infections of the skin and subcutaneous tissues, the total duration of stepwise therapy (iv administration followed by oral administration) is 7-21 days; for complicated intra-abdominal infections, the total duration of step-down therapy (iv administration of the drug followed by oral administration) is 5-14 days; for uncomplicated inflammatory diseases of the pelvic organs - 14 days. The duration of treatment with Avelox can be up to 21 days. No change in dosage regimen is required in elderly patients. The effectiveness and safety of moxifloxacin in children and adolescents has not been established. Patients with impaired liver function do not require a change in dosage regimen. In patients with impaired renal function (including severe renal failure with CC ≤30 ml/min/1.73 m2), as well as in patients on continuous hemodialysis and long-term ambulatory peritoneal dialysis, no change in dosage regimen is required. In patients of different ethnic groups, no change in dosage regimen is required.

Side effects

Adverse reactions reported with moxifloxacin 400 mg (oral, step-down [IV followed by oral] and IV alone) are derived from clinical studies and post-marketing reports (shown in italics). Adverse reactions listed in the frequent group occurred with a frequency of less than 3%, with the exception of nausea and diarrhea. Within each frequency group, adverse drug reactions are listed in descending order of importance. Determination of the frequency of adverse reactions often (from ≥1/100 to less than 1/10), infrequently (from ≥1/1000 to less than 1/100), rarely (from ≥1/10,000 to less than 1/1000), very rarely (less than 1/10 000).Infections often - fungal superinfections. From the hematopoietic system, infrequently - anemia, leukopenia, neutropenia, thrombocytopenia, thrombocythemia, prolongation of prothrombin time / increase in INR. rarely - a change in thromboplastin concentration. very rarely - increased prothrombin concentration/decreased INR. From the immune system: rarely - allergic reactions, urticaria, itching, rash, eosinophilia. rarely - anaphylactic/anaphylactoid reactions, angioedema, including laryngeal edema (potentially life-threatening). very rarely - anaphylactic/anaphylactoid shock (including potentially life-threatening). On the metabolic side, rarely - hyperlipidemia. rarely - hyperglycemia, hyperuricemia. very rarely - hypoglycemia. Mental disorders infrequently - anxiety, psychomotor hyperreactivity, agitation. rarely - emotional lability, depression (in very rare cases, behavior with a tendency to self-harm, such as suicidal thoughts or suicide attempts), hallucinations is possible. very rarely - depersonalization, psychotic reactions (potentially manifested in behavior with a tendency to self-harm, such as suicidal thoughts or suicide attempts). From the nervous system often - dizziness, headache. uncommon - paresthesia, dysesthesia, taste disturbances (including in very rare cases ageusia), confusion, disorientation, sleep disturbances, tremor, vertigo, drowsiness. rarely - hypoesthesia, olfactory disturbances (including anosmia), atypical dreams, loss of coordination (including gait disturbances due to dizziness or vertigo, in very rare cases leading to injury due to a fall, especially in elderly patients), seizures with various clinical manifestations (including .h. grand mal seizures), attention disorders, speech disorders, amnesia, peripheral neuropathy, polyneuropathy. very rarely - hyperesthesia. On the part of the organ of vision, rarely - visual impairment (especially with reactions from the central nervous system). very rarely - transient loss of vision (especially with reactions from the central nervous system). On the part of the hearing organ, rarely - tinnitus, hearing impairment, including deafness (usually reversible). From the cardiovascular system, often - prolongation of the QT interval in patients with concomitant hypokalemia. uncommon - prolongation of the QT interval, palpitations, tachycardia, vasodilation. rarely - increased blood pressure, decreased blood pressure, fainting, ventricular tachyarrhythmias. very rarely - nonspecific arrhythmias, polymorphic ventricular tachycardia (pirouette type), cardiac arrest (mainly in persons with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia). From the respiratory system: rarely - shortness of breath, including asthmatic condition. side of the digestive system often - nausea, vomiting, abdominal pain, diarrhea. uncommon - decreased appetite and reduced food consumption, constipation, dyspepsia, flatulence, gastroenteritis (except erosive gastroenteritis), increased amylase activity. rarely - dysphagia, stomatitis, pseudomembranous colitis (in very rare cases associated with life-threatening complications). From the liver and biliary tract, often - increased activity of liver transaminases. uncommon - liver dysfunction (including increased LDH activity), increased bilirubin concentration, increased GGT and alkaline phosphatase activity. rarely - jaundice, hepatitis (mainly cholestatic). very rarely - fulminant hepatitis, potentially leading to life-threatening liver failure (including fatal cases). On the skin side, very rarely - bullous skin reactions, for example, Stevens-Johnson syndrome or toxic epidermal necrolysis (potentially life-threatening). On the bone side, muscular system infrequently - arthralgia, myalgia. rarely - tendonitis, increased muscle tone and cramps, muscle weakness. very rarely - arthritis, tendon ruptures, gait disturbance due to damage to the musculoskeletal system, increased symptoms of myasthenia gravis. From the urinary system, rarely - dehydration (caused by diarrhea or decreased fluid intake). rarely - impaired renal function, renal failure as a result of dehydration, which can lead to kidney damage, especially in elderly patients with pre-existing impaired renal function). From the body as a whole, often - reactions at the injection/infusion site. infrequently - general malaise, nonspecific pain, sweating. The frequency of the following adverse reactions was higher in the group receiving step-by-step therapy often - increased GGT activity. uncommon - ventricular tachyarrhythmias, arterial hypotension, edema, pseudomembranous colitis (in very rare cases associated with life-threatening complications), convulsions with various clinical manifestations (including grand mal seizures), hallucinations, impaired renal function, renal failure (in resulting from dehydration, which can lead to kidney damage, especially in older patients with pre-existing renal impairment).

Overdose

There are limited data on overdose with moxifloxacin. There were no side effects observed when using Avelox at a dose of up to 1200 mg once and 600 mg for 10 days or more. Treatment: in case of overdose, symptomatic and supportive therapy with ECG monitoring is carried out in accordance with the clinical situation. The use of activated charcoal immediately after oral administration of the drug may help prevent excessive systemic exposure to moxifloxacin in cases of overdose.

Interaction with other drugs

No dose adjustment is required when using Avelox together with atenolol, ranitidine, calcium-containing supplements, theophylline, cyclosporine, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenecid (the absence of clinically significant interaction with moxifloxacin has been confirmed). The possible additive QT interval prolonging effect of moxifloxacin and other drugs that affect QT prolongation should be considered. Due to the combined use of moxifloxacin and drugs that affect the prolongation of the QT interval, the risk of developing ventricular arrhythmia, including polymorphic ventricular tachycardia of the torsades de pointes type, increases. The combined use of moxifloxacin with the following drugs that affect the prolongation of the QT interval is contraindicated: class IA antiarrhythmic drugs (including quinidine, hydroquinidine, disopyramide); class III antiarrhythmic drugs (including amiodarone, sotalol, dofetilide, ibutilide); neuroleptics (including phenothiazine, pimozide, sertindole, haloperidol, sultopride); tricyclic antidepressants; antimicrobials (sparfloxacin, IV erythromycin, pentamidine, antimalarials, especially halofantrine); antihistamines (terfenadine, astemizole, mizolastine); others (cisapride, IV vincamine, bepridil, difemanil). Ingestion of Avelox and antacids, multivitamins and minerals may interfere with the absorption of moxifloxacin due to the formation of chelate complexes with polyvalent cations contained in these drugs. As a result, moxifloxacin plasma concentrations may be significantly lower than therapeutic levels. In this regard, antacids, antiretrovirals (for example, didanosine) and other drugs containing magnesium, aluminum, sucralfate, iron, zinc should be taken at least 4 hours before or 4 hours after oral administration of moxifloxacin. When Avelox is used in combination with warfarin, prothrombin time and other blood coagulation parameters do not change. In patients receiving anticoagulants in combination with antibiotics, incl. with moxifloxacin, there have been cases of increased anticoagulant activity of anticoagulant drugs. Risk factors are the presence of an infectious disease (and concomitant inflammatory process), age and general condition of the patient. Despite the fact that there is no interaction between moxifloxacin and warfarin, in patients receiving concomitant treatment with these drugs, it is necessary to monitor the INR and, if necessary, adjust the dose of indirect anticoagulants. Moxifloxacin and digoxin do not have a significant effect on each other's pharmacokinetic parameters. When moxifloxacin was re-administered, digoxin Cmax increased by approximately 30%. In this case, the AUC and Cmin values of digoxin do not change. With the simultaneous use of activated carbon and moxifloxacin orally at a dose of 400 mg, the systemic bioavailability of the drug is reduced by more than 80% as a result of slower absorption. In case of overdose, the use of activated carbon at an early stage of absorption prevents a further increase in systemic exposure.

special instructions

In some cases, after the first use of the drug, hypersensitivity and allergic reactions may develop, which should be reported to your doctor immediately. Very rarely, even after the first use of the drug, anaphylactic reactions can progress to life-threatening anaphylactic shock. In these cases, treatment with Avelox should be stopped and the necessary therapeutic measures (including anti-shock) should be started immediately. When using the drug Avelox, some patients may experience prolongation of the QT interval. Avelox should be used with caution in women and elderly patients. Because women have a longer QT interval than men, they may be more sensitive to drugs that prolong the QT interval. Elderly patients are also more susceptible to drugs that affect the QT interval. The degree of QT interval prolongation may increase with increasing drug concentrations, so the recommended dose should not be exceeded. Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including polymorphic ventricular tachycardia. However, in patients with pneumonia, a correlation between moxifloxacin plasma concentrations and prolongation of the QT interval was noted. None of the 9,000 patients receiving Avelox experienced cardiovascular complications or deaths associated with QT prolongation. When using Avelox, the risk of developing ventricular arrhythmias may increase in patients with conditions predisposing to arrhythmias. In this regard, Avelox is contraindicated in case of: changes in electrophysiological parameters of the heart, expressed in prolongation of the QT interval (congenital or acquired documented prolongation of the QT interval, electrolyte disturbances, especially uncorrected hypokalemia, clinically significant bradycardia, clinically significant heart failure with reduced left ventricular ejection fraction, presence history of indications of rhythm disturbances, accompanied by clinical symptoms), use with other drugs that prolong the QT interval. Avelox should be used with caution: in patients with potentially proarrhythmic conditions, such as acute myocardial ischemia, in patients with liver cirrhosis (since in this category of patients the risk of developing QT prolongation cannot be excluded). Cases of fulminant hepatitis, potentially leading to liver failure (including fatal cases), have been reported while taking Avelox. The patient should be informed that if symptoms of liver failure occur, it is necessary to consult a doctor before continuing treatment with Avelox. Cases of bullous skin lesions (such as Stevens-Johnson syndrome or toxic epidermal necrolysis) have been reported while taking Avelox. The patient should be informed that if symptoms of skin or mucous membrane lesions occur, it is necessary to consult a doctor before continuing treatment with Avelox. The use of quinolone drugs is associated with a possible risk of developing seizures. Avelox should be used with caution in patients with diseases of the central nervous system and disorders of the central nervous system that predispose to seizures or lower the threshold for seizure activity. The use of broad-spectrum antibacterial drugs, including Avelox, is associated with a risk of developing pseudomembranous colitis. This diagnosis should be kept in mind in patients who develop severe diarrhea during treatment with Avelox. In this case, appropriate therapy should be prescribed immediately. Drugs that inhibit intestinal motility are contraindicated in the development of severe diarrhea. Avelox should be used with caution in patients with myasthenia gravis due to a possible exacerbation of the disease. During therapy with quinolones, incl. moxifloxacin, tendonitis and tendon rupture may develop, especially in the elderly and patients receiving corticosteroids. Cases have been described that occurred within several months after completion of treatment. At the first symptoms of pain or inflammation at the site of injury, the drug should be stopped and the affected limb should be unloaded. When using quinolones, photosensitivity reactions are observed. However, during preclinical and clinical studies, as well as when using the drug Avelox in practice, no photosensitivity reactions were observed. However, patients receiving Avelox should avoid exposure to direct sunlight and ultraviolet radiation. The use of the drug in the form of tablets for oral administration is not recommended in patients with complicated inflammatory diseases of the pelvic organs (for example, associated with tubo-ovarian or pelvic abscesses). Moxifloxacin is not recommended for the treatment of infections caused by methicillin-resistant Staphylococcus aureus (MRSA). Suspected or confirmed MRSA infections should be treated with appropriate antibacterial drugs. The ability of Avelox to inhibit the growth of mycobacteria may cause in vitro interaction of moxifloxacin with the test for Mycobacterium spp., leading to false negative results when analyzing samples from patients who are being treated with Avelox during this period. In patients treated with quinolones, including Avelox, cases of sensory or sensorimotor polyneuropathy leading to paresthesia, hypoesthesia, dysesthesia or weakness have been described. Patients being treated with Avelox should be advised to seek immediate medical attention before continuing treatment if symptoms of neuropathy, including pain, burning, tingling, numbness or weakness, occur. Psychiatric reactions can occur even after the first prescription of fluoroquinolones, including moxifloxacin. In very rare cases, depression or psychotic reactions progress to suicidal thoughts and behavior with a tendency to self-harm, including suicide attempts. If patients develop such reactions, the drug Avelox should be discontinued and the necessary measures taken. Caution should be exercised when prescribing Avelox to patients with a history of psychosis and/or psychiatric illness. Due to the widespread and increasing incidence of infections caused by fluoroquinolone-resistant Neisseria gonorrhoeae, moxifloxacin monotherapy should not be used in the treatment of patients with pelvic inflammatory disease, unless the presence of fluoroquinolone-resistant N. gonorrhoeae is excluded. If the presence of fluoroquinolone-resistant N. gonorrhoeae cannot be excluded, consideration should be given to supplementing empiric moxifloxacin therapy with an appropriate antibiotic that is active against N. gonorrhoeae (eg, a cephalosporin). As with other fluoroquinolones, changes in blood glucose concentrations, including hypo- and hyperglycemia, were observed when using Avelox. During therapy with Avelox, dysglycemia occurred predominantly in elderly patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, sulfonylureas) or insulin. When treating patients with diabetes mellitus, careful monitoring of blood glucose concentrations is recommended. Effect on the ability to drive vehicles and operate machinery Fluoroquinolones, including moxifloxacin, may impair the ability of patients to drive a car and engage in other potentially hazardous activities that require increased attention and speed of psychomotor reactions due to the effect on the central nervous system and visual impairment.

Infectious and inflammatory diseases caused by microorganisms sensitive to moxifloxacin: acute sinusitis, exacerbation of chronic bronchitis, uncomplicated infections of the skin and subcutaneous structures, community-acquired pneumonia, including community-acquired pneumonia caused by strains of microorganisms with multiple resistance to antibiotics, complicated infections of the skin and subcutaneous structures ( including infected diabetic foot), complicated intra-abdominal infections, including polymicrobial infections, including intraperitoneal abscesses, uncomplicated inflammatory diseases of the pelvic organs (including salpingitis and endometritis).

Contraindications Avelox tablets 400 mg

Hypersensitivity to moxifloxacin, other quinolones or any other component of the drug, age under 18 years, pregnancy and breastfeeding, a history of tendon pathology that developed as a result of treatment with quinolone antibiotics. In preclinical and clinical studies, after the administration of moxifloxacin, changes in electrophysiological parameters of the heart were observed, expressed in prolongation of the QT interval. In this regard, the use of moxifloxacin is contraindicated in patients of the following categories: congenital or acquired documented prolongation of the QT interval, electrolyte disturbances, especially uncorrected hypokalemia; clinically significant bradycardia; clinically significant heart failure with reduced left ventricular ejection fraction; a history of rhythm disturbances accompanied by clinical symptoms. Moxifloxacin should not be used with other drugs that prolong the QT interval. Due to the presence of lactose in the drug, its use is contraindicated in cases of congenital lactose intolerance, lactase deficiency, and glucose-galactose malabsorption. Due to limited clinical data, the use of moxifloxacin is contraindicated in patients with impaired liver function (Child-Pugh class C) and in patients with transaminase elevations more than five times the upper limit of normal.

Method of administration and dosage of Avelox tablets 400 mg

Recommended dosage regimen for moxifloxacin: 400 mg (1 tablet) once a day for the infections listed above. Do not exceed the recommended dose. The tablets should be swallowed whole, without chewing, with plenty of water, regardless of meals. Duration of treatment. The duration of treatment is determined by the location and severity of the infection, as well as the clinical effect: exacerbation of chronic bronchitis: 5-10 days, acute sinusitis: 7 days, uncomplicated infections of the skin and subcutaneous structures: 7 days, community-acquired pneumonia: total duration of step therapy (intravenous administration followed by oral administration) is 7-14 days, complicated infections of the skin and subcutaneous structures: the total duration of stepwise therapy with moxifloxacin (intravenous administration followed by oral administration) is 7-21 days, complicated intra-abdominal infections: the total duration of stepwise therapy (intravenous administration followed by oral administration ) is 5-14 days, uncomplicated inflammatory diseases of the pelvic organs - 14 days. The recommended duration of treatment should not be exceeded. According to clinical studies, the duration of treatment with the drug in tablets can reach 21 days. Elderly patients. No change in dosage regimen is required in elderly patients. Children. The effectiveness and safety of moxifloxacin in children and adolescents has not been established. Liver dysfunction. For patients with impaired liver function, no change in dosage regimen is required. Kidney failure. In patients with impaired renal function (including severe renal failure with creatinine clearance