In this article, you can read the instructions for using the medicinal product. Avelox... Reviews of website visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Avelox in their practice are presented. A big request is to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, which may not have been declared by the manufacturer in the annotation. Analogs of Avelox in the presence of available structural analogs. Use for the treatment of chlamydia, mycoplasmosis, chronic bronchitis and prostatitis in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Avelox- an antibacterial drug of the fluoroquinolone group. Has a bactericidal effect. The mechanism of action is due to the inhibition of bacterial topoisomerases 2 and 4, which leads to disruption of the DNA synthesis of the microbial cell and, as a consequence, to the death of the microbial cell. The minimum bactericidal concentration of the drug is generally comparable to its MIC.

The drug is active against a wide range of gram-negative and gram-positive microorganisms, anaerobes, acid-fast bacteria and atypical forms such as Mycoplasma spp. (mycoplasma), Chlamydia spp. (chlamydia), Legionella spp. (legionella), as well as bacteria resistant to beta-lactam and macrolide antibiotics.

Avelox is sensitive to gram-positive and gram-negative aerobic bacteria, anaerobic bacteria, atypical bacteria: Chlamydia pneumoniae, Mycoplasma pneumoniae, Legionella pneumophila, Coxiella burnettii, Chlamydia trachomatis, Mycoplasma hominis, Mycoplasma genitalium.

Moxifloxacin (active ingredient of the drug Avelox) is less active against Staphylococcus aureus (strains resistant to methicillin / ofloxacin), Staphylococcus epidermidis (strains resistant to methicillin / ofloxacin), Pseudomonas aeruginas.

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. So far, no cases of plasmid resistance have also been observed. The overall incidence of resistance development is very low (10-7-10-10). Moxifloxacin resistance develops slowly through multiple mutations. Repeated exposure of microorganisms to moxifloxacin at concentrations below the MIC is accompanied by only a slight increase in the MIC.

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

Composition

Moxifloxacin hydrochloride + excipients.

Pharmacokinetics

After oral administration, Avelox is absorbed quickly and almost completely. When moxifloxacin is taken with food, the duration of absorption does not change. The drug can be used regardless of food intake. The absolute bioavailability is about 91%. The binding to blood proteins (mainly albumin) is about 45%. Moxifloxacin is rapidly distributed in organs and tissues. High concentrations of the drug, exceeding those in plasma, are created in the lung tissue (including in alveolar macrophages), in the mucous membrane of the bronchi, in the nasal sinuses, in soft tissues, skin and subcutaneous structures, foci of inflammation. In the interstitial fluid and in saliva, the drug is determined in a free form, not bound to proteins, in a concentration higher than in plasma. In addition, high concentrations of the drug are determined in the organs of the abdominal cavity and peritoneal fluid, as well as in the tissues of the female genital organs.

Biotransformed to inactive sulfo compounds and glucuronides. After passing through the 2nd phase of biotransformation, moxifloxacin is excreted from the body by the kidneys and through the intestines both unchanged and in the form of inactive sulfo compounds and glucuronides. It is excreted in the urine, as well as in the feces, both unchanged and in the form of inactive metabolites.

No differences were found in the pharmacokinetic parameters of moxifloxacin depending on age, gender and race.

Pharmacokinetic studies of moxifloxacin in children have not been conducted.

Indications

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

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

Forms of issue

Film-coated tablets 400 mg.

Solution for infusion (injections in ampoules for injection).

Instructions for use and dosage regimen

The drug is administered orally and intravenously, 400 mg once a day.

The duration of treatment with Avelox when taken orally and intravenously is determined by the severity of the infection and the clinical effect and is: with exacerbation of chronic bronchitis - 5 days; with community-acquired pneumonia, the total duration of stepwise therapy (intravenous administration followed by oral administration) is 7-14 days, first intravenously, then inside, or 10 days inside; for acute sinusitis and uncomplicated infections of the skin and soft tissues - 7 days; with complicated infections of the skin and subcutaneous tissues - the total duration of stepwise therapy (intravenous administration followed by oral administration) is 7-21 days; with complicated intra-abdominal infections - the total duration of stepwise therapy (intravenous 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 intravenously can be up to 14 days, inside - 21 days.

Elderly patients, patients with minor liver dysfunction (class A or B on the Child-Pugh scale), patients with renal dysfunction (including CC<30 мл/мин/1.73 м2), а также пациентам, находящимся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе, изменений режима дозирования не требуется.

The tablets should be taken without chewing with a small amount of water, regardless of the meal.

The solution for infusion should be administered intravenously slowly over 60 minutes. The drug can be administered both diluted and undiluted. Avelox solution is compatible with the following solutions: water for injection, sodium chloride solution 0.9%, sodium chloride solution 1M, dextrose solution 5%, dextrose solution 10%, dextrose solution 40%, xylitol solution 20%, Ringer's solution, Ringer's lactate solution, aminofusin solution 10%, ionosteril solution. Only clear solution should be used.

Side effect

• lengthening of the QT interval (often in patients with concomitant hypokalemia, sometimes in other patients);
• tachycardia and vasodilation (flushing of the face);
• arterial hypotension;
• arterial hypertension;
• fainting;
• ventricular tachyarrhythmias;
• nonspecific arrhythmias (including extrasystole);
• polymorphic ventricular tachycardia (ventricular arrhythmia of the "pirouette" type) or cardiac arrest, predominantly in persons with predisposing conditions to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia;
• shortness of breath, including an asthmatic condition;
• nausea, vomiting;
• stomach ache;
• diarrhea;
• anorexia;
• constipation;
• dyspepsia;
• flatulence;
• gastroenteritis (except for erosive gastroenteritis);
• stomatitis;
• pseudomembranous colitis (in very rare cases associated with life-threatening complications);
• jaundice;
• hepatitis (mainly cholestatic);
• dizziness;
• headache;
• confusion of consciousness;
• disorientation;
• drowsiness;
• tremor;
• sleep disturbances;
• sense of anxiety;
• increased psychomotor activity;
• lack of coordination (including gait disturbances due to dizziness, in very rare cases leading to injuries as a result of a fall, especially in elderly patients);
• convulsive seizures with various clinical manifestations (including grand mal seizures);
• attention disorders;
• speech disorders;
• amnesia;
• depression (in very rare cases, behavior with a tendency to self-harm is possible);
• hallucinations;
• psychotic reactions (potentially manifested in behavior with a tendency to self-harm);
• disorders of taste;
• visual disturbances (blurred vision, decreased visual acuity, diplopia, especially in combination with dizziness and confusion);
• noise in ears;
• violation of the sense of smell, including anosmia;
• loss of taste sensitivity;
• anemia, leukopenia (including neutropenia), thrombocytopenia, thrombocytosis, prolonged prothrombin time and decreased INR;
• arthralgia;
• myalgia;
• tendinitis;
• increased muscle tone and cramps;
• tendon ruptures;
• candidal superinfection;
• vaginitis;
• dehydration (caused by diarrhea or decreased fluid intake);
• impaired renal function;
• renal failure as a result of dehydration, which can lead to kidney damage (especially in elderly patients with concomitant renal dysfunction);
• bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis (potentially life-threatening);
• hives;
• rash;
• eosinophilia;
• anaphylactic / anaphylactoid reactions;
• angioedema, including laryngeal edema (potentially life-threatening);
• anaphylactic shock (including life-threatening);
• general malaise (including symptoms of feeling unwell, nonspecific pain, and sweating);
• swelling.

Contraindications

• pregnancy;
• lactation (breastfeeding);
• children and adolescents up to 18 years old;
• hypersensitivity to moxifloxacin and other components of the drug.

Application during pregnancy and lactation

The safety of using Avelox during pregnancy has not been established, therefore its use is contraindicated.

Small amounts of moxifloxacin are excreted in breast milk. There are no data on the use of moxifloxacin in women during lactation. Therefore, the use of Avelox during breastfeeding is also contraindicated.

In experimental studies, when studying the effect of moxifloxacin on reproductive function in rats, rabbits and monkeys, it was proved that moxifloxacin penetrates the placental barrier. Studies carried out on rats (with the introduction of moxifloxacin orally and intravenously) and monkeys (with the introduction of moxifloxacin orally) did not reveal the teratogenic effect of moxifloxacin and its effect on fertility. With intravenous administration of moxifloxacin to rabbits at a dose of 20 mg / kg, skeletal malformations were observed. An increase in the number of miscarriages in monkeys and rabbits was revealed when using moxifloxacin in a therapeutic dose. In rats, a decrease in fetal weight, an increase in miscarriages, a slight increase in the duration of pregnancy and an increase in the spontaneous activity of offspring of both sexes were observed when using moxifloxacin, the dose of which was 63 times higher than the recommended one.

Use in elderly patients

Elderly patients do not need to change the dosage regimen.

Application in children

The drug is contraindicated in children and adolescents under 18 years of age.

special instructions

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

When using Avelox, some patients may experience a prolongation of the QT interval. In this regard, it is necessary to avoid prescribing the drug to patients with prolonged QT interval, hypokalemia, as well as during treatment with class 1 A (quinidine, procainamide) or class 3 (amiodarone, sotalol) antiarrhythmic drugs, since the experience of using moxifloxacin in these patients is limited. Care should be taken to prescribe Avelox together with drugs that prolong the QT interval (cisapride, erythromycin, antipsychotics, tricyclic antidepressants), as well as to patients with conditions predisposing to arrhythmias, such as bradycardia, acute myocardial ischemia. The degree of lengthening of the QT interval may increase with increasing drug concentration, therefore, 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. In patients with pneumonia, there was no correlation between the concentration of moxifloxacin in blood plasma and prolongation of the QT interval. None of the 9000 patients treated with moxifloxacin had cardiovascular complications or deaths associated with QT prolongation. However, in patients with conditions predisposing to arrhythmias, the use of moxifloxacin may increase the risk of developing ventricular arrhythmias.

During therapy with fluoroquinolones, incl. moxifloxacin, especially in the elderly and patients receiving glucocorticosteroids (GCS), tendinitis and tendon rupture may develop. If pain or signs of tendon inflammation appear, stop taking Avelox and relieve the affected limb.

The use of broad-spectrum antibacterial drugs is associated with the risk of developing pseudomembranous colitis. This should be borne in mind if severe diarrhea occurs during treatment with Avelox. In this case, the drug should be discontinued and appropriate therapy should be prescribed immediately.

Avelox should not be combined with ethanol (alcohol).

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

With the use of quinolones, photosensitization reactions are noted. However, during preclinical, clinical studies, as well as when using Avelox in clinical practice, photosensitization reactions were not observed. However, patients should avoid direct sunlight and UV radiation while taking the drug.

No dose adjustment is required for patients of different ethnic groups.

Influence on the ability to drive vehicles and use mechanisms

Despite the fact that moxifloxacin rarely causes side reactions from the central nervous system, the question of the possibility of driving a car or moving machinery is decided individually after evaluating the patient's response to taking the drug.

Drug interactions

No dose adjustment is required when Avelox is used together with atenolol, ranitidine, calcium supplements, theophylline, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenecid (no clinically significant interaction with moxifloxacin was confirmed).

The combined use of Avelox and antacids, minerals and vitamin-mineral complexes inside can interfere with the absorption of moxifloxacin due to the formation of chelate complexes with multivalent cations contained in these drugs, and therefore, reduce the concentration of moxifloxacin in the blood plasma. In this regard, antacids, antiretrovirals and other drugs containing calcium, magnesium, aluminum, iron, sucralfate should be taken at least 4 hours before or 2 hours after ingestion of Avelox.

With the combined use of Avelox with warfarin, the prothrombin time and other parameters of blood coagulation do not change.

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

Moxifloxacin and digoxin do not significantly affect the pharmacokinetic parameters of each other.

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

The absorption of moxifloxacin does not change with simultaneous ingestion of food (including dairy products). Moxifloxacin can be taken with or without food.

Analogs of the drug Avelox

Structural analogues for the active substance:

• Vigamox;
• Moximac;
• Moxin;
• Moxifloxacin;
• Moxifour;
• Plevilox.

Pharmacological group analogs (antibiotics quinolones and fluoroquinolones):

• Abaktal;
• Alcipro;
• Vigamox;
• Gatispan;
• Glevo;
• Zanocin;
• Zoflox;
• Quipro;
• Levolet R;
• Levofloxacin;
• Lomefloxacin;
• Microflox;
• Nevigramon;
• Negro;
• Nolitsin;
• Norbactin;
• Norfloxacin;
• Oflox;
• Ofloxacin;
• Oflocid;
• Oflocid forte;
• Palin;
• Pefloxacin;
• Recipro;
• Siflox;
• Tavanik;
• Uniflox;
• Factual;
• Floracid;
• Haileflox;
• Tsiprobay;
• Tsiprolet;
• Ciprofloxacin;
• Tsifran;
• Eleflox;
• Unicpef;
• Youtibid.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and see the available analogues for the therapeutic effect.

Antibacterial drug of the fluoroquinolone group

Active substance

Release form, composition and packaging

Solution for infusion transparent, yellow or yellow with a 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 - bottles of colorless glass with a capacity of 300 ml (1) - cardboard packs.
250 ml - polymer containers, sealed in protective bags (12) - cardboard boxes.

pharmachologic 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 DNA biosynthesis of the microbial cell and, as a consequence, to the death of microbial cells.

The minimum bactericidal concentration of the drug is 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 also been observed. The overall incidence of resistance development is very low (10 -7 -10 -10). Moxifloxacin resistance 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 susceptible to moxifloxacin.

It was found 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 the C7 position prevents the development of active efflux, a mechanism of resistance to fluoroquinolones.

Moxifloxacin in vitro is active 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.

Influence on human intestinal microflora

In two studies conducted on volunteers, the following changes in the intestinal microflora after oral administration of moxifloxacin were noted: a decrease in the concentrations of Escherichia coli, Bacillus spp., Bacteroides vulgatus, Enterococcus spp., Klebsiella spp., As well as anaerobes Bifidobacterium Pepto spp., spp. These changes were reversible within two weeks. Clostridium difficile toxins were not 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), cephalosporins of the second generation (for example), 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-susceptible strains) *		Staphylococcus aureus (methicillin / ofloxacin resistant strains) **
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 * (only strains susceptible to vancomycin and gentamicin)
	Enterococcus avium *
	Enterococcus faecicum *
Gram-negative
Haemophilus influenzae (including strains producing and non-producing β-lactamases) *
Haemophillus parainfluenzae *
Moraxella catarrhalis (including strains producing and non-producing β-lactamases) *
Bordetella pertussis
Legionella pneumophila	Escherichia coli * a
Acinetobacter baumanii	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 the drug Avelox is not recommended for the treatment of infections caused by methicillin-resistant strains of 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 spread of acquired resistance may differ by geographic region and over time. In this regard, when testing the susceptibility of a strain, it is desirable to have local information on resistance, especially in the treatment of severe infections.

If in patients undergoing treatment in a hospital, the AUC / MIC 90 value exceeds 125, and the 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 inhibitory curve (ratio AUC / MIC 90)

Pharmacokinetics

Suction

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

The absolute bioavailability for oral administration and intravenous infusion is about 91%.

The pharmacokinetics of moxifloxacin when taken in 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, C max in the blood is reached within 0.5-4 hours and is 3.1 mg / l. After oral administration of 400 mg moxifloxacin 1 time / day, C ss max and C ss min are 3.2 mg / l and 0.6 mg / l, respectively.

When moxifloxacin is taken with food, there is a slight increase in the time to reach C max (by 2 hours) and a slight decrease in C max (by about 16%), while the duration of absorption does not change. However, these data have no clinical significance, and the drug can be used regardless of food intake.

After a single infusion of Avelox at a dose of 400 mg for 1 hour, C max 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 for oral administration. The exposure of the drug, determined by the AUC indicator, slightly exceeds that when the drug is taken orally.

With multiple intravenous infusions at a dose of 400 mg for 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 of 4.4 mg / l are achieved at the end of the infusion.

Distribution

The equilibrium state is reached within 3 days.

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

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

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

Metabolism

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

Withdrawal

T 1/2 is approximately 12 hours. The average total clearance after oral administration and after intravenous administration at a dose of 400 mg is 179-246 ml / min.

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

The mass balance of the parent compound and the phase 2 metabolites is approximately 96-98%, which indicates 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

In a study of the pharmacokinetics of moxifloxacin in men and women, 33% differences were found in terms of AUC and C max. The absorption of moxifloxacin was independent of gender. Differences in AUC and C max 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 in children have not been conducted.

There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including 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 the concentration of moxifloxacin in patients with impaired liver function (classes A and B on the Child-Pugh scale) compared with healthy volunteers and patients with normal liver 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 caused by strains of microorganisms with multiple antibiotic resistance *);
• uncomplicated infections of the skin and soft tissues;
• complicated infections of the skin and subcutaneous structures (including an 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 such groups as penicillins (with MIC ≥2 mg / ml), II 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 introduction of moxifloxacin, a change in the electrophysiological parameters of the heart was observed, expressed in an extension 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 composition of the drug, its use is contraindicated in congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption (for tablets);
• due to the limited number 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 an increase in transaminases more than 5 times higher than ULN;
• pregnancy;
• lactation (breastfeeding);
• age under 18;
• hypersensitivity to moxifloxacin, other quinolones or any other component of the drug.

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

Dosage

The drug is administered orally and intravenously, 400 mg 1 time / day.

The duration of treatment with Avelox when taken 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 stepwise therapy (intravenous administration followed by oral administration) is 7-14 days, first intravenously, then inside, or 10 days inside; at acute sinusitis and uncomplicated infections of the skin and soft tissues- 7 days; at complicated infections of the skin and subcutaneous tissues the total duration of stepwise therapy (intravenous administration followed by oral administration) is 7-21 days; at complicated intra-abdominal infections the total duration of stepwise therapy (intravenous 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.

Dosing regimen changes in elderly patients not required.

The efficacy and safety of using moxifloxacin in children and adolescents not installed.

Patients with impaired liver function no change in the dosage regimen is required.

In patients with impaired renal function (including severe renal failure with CC ≤ 30 ml / min / 1.73 m 2), as well as in patients on continuous hemodialysis and long-term outpatient peritoneal dialysis, no change in the dosage regimen is required ...

In patients of different ethnic groups, changes in the dosage regimen are not required.

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

The solution for infusion should be administered intravenously within 60 minutes. The drug can be administered both diluted and 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. Since the solution cannot be frozen or refrigerated, it cannot be stored in the refrigerator. Upon cooling, the solution may precipitate, but the precipitate usually dissolves at room temperature. The solution should be stored in its original packaging.

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

Side effects

Data on adverse reactions reported with moxifloxacin 400 mg (by mouth, with stepwise therapy [intravenous administration of the drug followed by oral administration] and only intravenous) were obtained from clinical studies and post-marketing reports (highlighted in italics ). Adverse reactions listed in the "frequent" group occurred with a frequency below 3%, with the exception of nausea and diarrhea.

In each frequency group, adverse drug reactions are listed in decreasing 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: infrequently - anemia, leukopenia, neutropenia, thrombocytopenia, thrombocythemia, prolongation of prothrombin time and an increase in INR; rarely - a change in the concentration of thromboplastin; very rarely - an increase in the concentration of prothrombin and a decrease in INR.

From the immune system: infrequently - 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: infrequently - hyperlipidemia; rarely - hyperglycemia, hyperuricemia.

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 suicidal attempts, is possible ), hallucinations; very rarely - depersonalization, psychotic reactions ( potentially manifesting in behavior with a tendency to self-harm, such as suicidal thoughts or suicidal attempts).

From the nervous system: often - dizziness, headache; infrequently - paresthesia, dysesthesia, disturbances in taste sensitivity (including in very rare cases ageusia), confusion, disorientation, sleep disturbances, tremor, vertigo, drowsiness; rarely - hypesthesia, impaired sense of smell (including anosmia), atypical dreams, impaired coordination (including gait disturbances due to dizziness or vertigo, in very rare cases leading to injury from falls, especially in elderly patients) , convulsions with various clinical manifestations (including "grand mal" seizures), impaired attention, speech impairments, amnesia, peripheral neuropathy, polyneuropathy; very rarely - hyperesthesia.

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

On the part of the cardiovascular system: often - prolongation of the QT interval in patients with concomitant hypokalemia; infrequently - lengthening of the QT interval, palpitations, tachycardia, vasodilation; rarely - increased blood pressure, decreased blood pressure, syncope, 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 an asthmatic condition.

From the digestive system: often - nausea, vomiting, abdominal pain, diarrhea; infrequently - decreased appetite and reduced food intake, constipation, dyspepsia, flatulence, gastroenteritis (except for 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 hepatic transaminases; infrequently - liver dysfunction (including an increase in LDH activity), an increase in the concentration of bilirubin, an increase in the activity of GGT and ALP; rarely - jaundice, hepatitis (mainly cholestatic); very rarely - fulminant hepatitis, potentially leading to life-threatening liver failure (including fatalities).

From the side of 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 - 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: 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 renal impairment).

From the side of 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 step therapy: often - an increase in the activity of GGT; infrequently - ventricular tachyarrhythmias, arterial hypotension, edema, pseudomembranous colitis (in very rare cases associated with life-threatening complications), seizures with various clinical manifestations (including "grand mal" seizures), hallucinations, impaired renal function, renal failure (as a result of dehydration, which can lead to kidney damage, especially in elderly patients with pre-existing renal impairment).

Overdose

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

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

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

Drug interactions

No dose adjustment is required when Avelox is used together with atenolol, ranitidine, calcium supplements, theophylline, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenecid (no clinically significant interaction with moxifloxacin was confirmed).

Consideration should be given to the possible additive effect of lengthening the QT interval of moxifloxacin and other drugs that affect the prolongation of the QT interval. Due to the combined use of moxifloxacin and drugs that affect the prolongation of the QT interval, the risk of developing ventricular arrhythmias, 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); antipsychotics (including phenothiazine, pimozide, sertindole, haloperidol, sultopride); tricyclic antidepressants; antimicrobial drugs (sparfloxacin, IV erythromycin, pentamidine, antimalarial drugs, especially halofantrine); antihistamines (terfenadine, astemizole, mizolastine); others (cisapride, vincamine i.v.), bepridil, diphemanil.

Ingestion of the drug Avelox and antacids, multivitamins and minerals can disrupt the absorption of moxifloxacin due to the formation of chelate complexes with polyvalent cations contained in these drugs. As a result, the concentration of moxifloxacin in the blood plasma can be significantly lower than the therapeutic one. 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 ingestion of Avelox.

With the combined use of Avelox with warfarin, the prothrombin time and other parameters of blood coagulation do not change.

In patients who received anticoagulants in combination with antibiotics, incl. with moxifloxacin, there have been cases of an increase in the anticoagulant activity of anticoagulant drugs. Risk factors are the presence of an infectious disease (and a concomitant inflammatory process), the age and general condition of the patient. Despite the fact that the interaction between moxifloxacin and warfarin is not detected, in patients receiving combined 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 significantly affect the pharmacokinetic parameters of each other. With repeated administration of moxifloxacin, the C max of digoxin 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 decreases by more than 80% as a result of slowing down its absorption. In case of an 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 charcoal, the systemic bioavailability of the drug is slightly reduced (by about 20%) due to the adsorption of moxifloxacin in the gastrointestinal tract lumen during enterohepatic circulation.

The absorption of moxifloxacin does not change with simultaneous ingestion of food (including dairy products). Moxifloxacin can be taken with or without food.

Incompatibility

Moxifloxacin infusion solution should not 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

In some cases, after the first use of the drug, hypersensitivity and allergic reactions may develop, which should be immediately reported to the doctor. 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 discontinued and the necessary therapeutic measures (including anti-shock) should be started immediately.

When using the drug Avelox, some patients may experience an increase in the QT interval.

Avelox should be used with caution in women and elderly patients. Because women have a longer QT interval compared to 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 lengthening of the QT interval may increase with increasing drug concentration, therefore, 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 the concentration of moxifloxacin in the blood plasma and prolongation of the QT interval was noted. None of the 9000 patients who received Avelox had cardiovascular complications and deaths associated with prolonged QT interval.

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

In this regard, Avelox is contraindicated:

• patients with an 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 cirrhosis of the liver (because in this category of patients, the risk of developing prolongation of the QT interval cannot be excluded).

When taking the drug Avelox, cases of fulminant hepatitis have been reported, potentially leading to the development of liver failure (including fatal cases). The patient should be informed that in the event of symptoms of hepatic failure, it is necessary to consult a doctor before continuing treatment with Avelox.

When taking the drug Avelox, cases of development of bullous skin lesions (such as Stevens-Johnson syndrome or toxic epidermal necrolysis) have been reported. The patient should be informed that in the event of symptoms of skin or mucous membrane lesions, it is necessary to consult a doctor before continuing treatment with Avelox.

The use of quinolone drugs is associated with a possible risk of seizures. Avelox should be used with caution in patients with diseases of the central nervous system and disorders of the central nervous system, predisposing to the occurrence of seizures or lowering the threshold of seizure activity.

The use of broad-spectrum antibacterial drugs, including Avelox, is associated with the risk of developing pseudomembranous colitis associated with antibiotic use. This diagnosis should be borne 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, tendinitis and tendon rupture may develop, especially in the elderly and patients receiving GCS. Cases are described that occurred within a few months after the completion of treatment. At the first symptoms of pain or inflammation at the site of injury, the drug should be discontinued and the affected limb should be relieved.

With the use of quinolones, photosensitivity reactions are noted. However, during preclinical and clinical studies, as well as when using the drug Avelox in practice, photosensitivity reactions were not 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).

It is not recommended to use moxifloxacin to treat 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 an in vitro interaction of moxifloxacin with a test for Mycobacterium spp., Leading to false negative results when analyzing samples of patients who are treated with Avelox during this period. In patients who have been treated with quinolones, including the drug Avelox, cases of sensory or sensorimotor polyneuropathy have been described, leading to paresthesia, hypesthesia, dysesthesia, or weakness. Patients undergoing treatment with Avelox should be warned about the need to immediately consult a doctor before continuing treatment in case of symptoms of neuropathy, including pain, burning, tingling, numbness or weakness.

Mental reactions may occur even after the first administration of fluoroquinolones, including moxifloxacin. In very rare cases, depression or psychotic reactions progress to suicidal thoughts and self-harming behaviors, including suicidal attempts. If such reactions develop in patients, Avelox should be discontinued and the necessary measures should be taken. Care should be taken when prescribing the drug Avelox to patients with psychoses 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 it is not possible to exclude the presence of fluoroquinolone-resistant N. gonorrhoeae, it is necessary to consider supplementing empiric therapy with moxifloxacin with an appropriate antibiotic that is active against N. gonorrhoeae (eg, cephalosporin).

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

Influence on the ability to drive vehicles and use mechanisms

Fluoroquinolones, including moxifloxacin, can interfere with the ability of patients to drive 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.

Pregnancy and lactation

The safety of using moxifloxacin during pregnancy has not been established and its use is contraindicated. Cases of reversible joint damage have been reported in children receiving certain quinolones, but this effect has not been reported in the fetus (when used by the mother during pregnancy).

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

Like other quinolones, moxifloxacin causes damage to the cartilage of large joints in premature animals. In preclinical studies, it has been established that a small amount of moxifloxacin is excreted in breast milk. There are no data on its use in women during lactation. Therefore, the appointment of moxifloxacin during breastfeeding is contraindicated.

Childhood use

Contraindicated: children and adolescents under 18 years of age .

With impaired renal function

Patients with impaired renal function(including with QC<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 vials is 5 years, in polymer containers - 3 years.

Catad_pgroup Antibacterial quinolones and fluoroquinolones

Avelox tablets - instructions for use

INSTRUCTIONS
on the medical use of the drug

Registration number: P N012034 / 01

Trade name of the drug: Avelox ®

International non-proprietary name (INN): moxifloxacin

Dosage form: film-coated tablets

Composition: 1 tablet contains:
Active substance: moxifloxacin hydrochloride 436.8 mg, equivalent to 400.0 mg moxifloxacin.
Excipients: microcrystalline cellulose (136.0 mg), croscarmellose sodium (32.0 mg), lactose monohydrate (68.0 mg), magnesium stearate (6.0 mg), film shell- hypromellose (9.0 - 12.6 mg), iron dye red oxide (0.3 - 0.42 mg), macrogol 4000 (3.0 - 4.2 mg), titanium dioxide (2.7 - 3, 78 mg).

Description: Pink matte oblong biconvex beveled film-coated tablets with “BAYER” engraving on one side and “M400” on the other side.

Pharmacotherapeutic group: antimicrobial agent - fluoroquinolone
ATX code J01MA14

pharmachologic effect
Pharmacodynamics
Mechanism of action
Moxifloxacin is a broad-spectrum bactericidal antibacterial drug, 8-methoxyfluoroquinolone. The bactericidal effect of the drug is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of the processes of replication, repair and transcription of DNA biosynthesis of the microbial cell and, as a consequence, to the death of microbial cells.
The minimum bactericidal concentration of the drug is generally comparable to its minimum inhibitory concentration. Mechanisms of resistance
The 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 also been observed. The overall frequency of development of resistance is very low (10 -7 - 10 -10). Moxifloxacin resistance develops slowly through multiple mutations. Repeated exposure of microorganisms to moxifloxacin at concentrations below the minimum inhibitory concentration (MIC) is accompanied by only a slight increase in MIC. Cases of cross-resistance to quinolones have been reported. However, some gram-positive and anaerobic microorganisms resistant to other quinolones remain susceptible to moxifloxacin.
It was found 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 bicyclo-amine group at position C7 prevents the development of active efflux, a mechanism of resistance to fluoroquinolones.
Moxifloxacin in vitro active against a wide range of gram-negative and gram-positive microorganisms, anaerobes, acid-fasting bacteria and atypical bacteria such as Mycoplasma spp., Chlamydia spp., Legionella spp., as well as bacteria resistant to ß-lactam and macrolide antibiotics.
Influence on human intestinal microflora
In two studies conducted on volunteers, the following changes in intestinal microflora after oral administration of moxifloxacin were noted: 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. Toxins Clostridium difficile not found.
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), II generation cephalosporins (eg cefuroxime), macrolides, tetracyclines, trimethoprim / sulfamethoxazole
Streptococcus pyogenes(group A) *
Streptococcus milleri
Streptococcus mitior
Streptococcus agalactiae
Streptococcus dysgalactiae
Streptococcus anginosus*
Streptococcus constellatus*
Staphylococcus aureus(including strains sensitive to methicillin) *	Staphylococcus aureus
Staphylococcus cohnii
Staphylococcus epidermidis(including strains sensitive to methicillin)	Staphylococcus epidermidis(including strains susceptible to methicillin / ofloxacin) **
Staphylococcus haemolyticus
Staphylococcus hominis
Staphylococcus saprophyticus
Staphylococcus simulans
Corynebacterium diphtheriae
Enterococcus faecalis(only strains susceptible to vancomycin and gentamycin) *
Gram-negative
Haemophilus influenzae
Haemophillus parainfluenzae*
Moraxella catarrhalis(including strains producing and non-producing β-lactamases) *
Bordetella pertussis
Escherichia coli*
Klebsiella pneumoniae*
Klebsiella oxytoca
Enterobacter aerogenes
Enterobacter agglomerans
Enterobacter cloacae *
Enterobacter intermedius
Enterobacter sakazaki
	Pseudomonas aeruginosa
	Pseudomonas fluorescens
	Burkholderia cepacia
	Stenotrophomonas maltophilia
	Proteus mirabilis *
Proteus vulgaris
Morganella morganii
	Neisseria gonorrhoeae *
Providencia rettgeri
Providencia stuartii
Anaerobes
Bacteroides distasonis
Bacteroides eggerthii
Bacteroides fragilis *
Bacteroides ovatus
Bacteroides thetaiotaomicron *
Bacteroides uniformis
Fusobacterium spp.
Peptostreptococcus spp.*
Porphyromonas spp.
Porphyromonas anaerobius
Porphyromonas asaccharolyticus
Porphyromonas magnus
Prevotella spp.
Propionibacterium spp.
Clostridium perfringens *
Clostridium ramosum
Atypical
Chlamydia pneumoniae *
Chlamydia trachomatis *
Mycoplasma pneumoniae *
Mycoplasma hominis
Mycoplasma genitalium
Legionella pneumophila *
Coxiella burnettii

* Clinically confirmed susceptibility to moxifloxacin
** When identifying strains Staphylococcus containing MesA genes, the use of moxifloxacin is not recommended

For certain strains, the spread of acquired resistance may differ by geographic region and over time. In this regard, when testing the susceptibility of a strain, it is desirable to have local information on resistance, especially in the treatment of severe infections. If in patients undergoing treatment in a hospital, the value of AUC / MIC 90 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

Pharmacokinetics
Absorption and bioavailability
When taken orally, moxifloxacin is rapidly and almost completely absorbed. The absolute bioavailability is about 91%.
The pharmacokinetics of moxifloxacin when taken in a dose of 50 to 1200 mg once, as well as 600 mg / day for 10 days, is linear. The equilibrium state is reached within 3 days.
After a single application of 400 mg of moxifloxacin, the maximum concentration (C max) in the blood is reached within 0.5-4 hours and is 3.1 mg / l. After oral administration of 400 mg of moxifloxacin once a day, Css max and Css mim are 3.2 mg / l and 0.6 mg / l, respectively.
When moxifloxacin is taken 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 have no clinical significance, and the drug can be used regardless of food intake.
Distribution
Moxifloxacin is rapidly distributed in tissues and organs and binds to blood proteins (mainly albumin) by about 45%. The volume of distribution is approximately 2 L / kg.
High concentrations of the drug, exceeding those in the blood plasma, are created in the lung tissue (including in the epithelial fluid, alveolar macrophages), in the nasal sinuses (maxillary and ethmoidal sinuses), in the nasal polyps, in the foci of inflammation (in the contents of the blisters with skin lesions). In the interstitial fluid and in saliva, the drug is determined in a free form, not bound to proteins, in a concentration higher than in blood plasma. In addition, high concentrations of the drug are determined in the tissues of the abdominal organs, peritoneal fluid and female genital organs.
Metabolism
Moxifloxacin undergoes biotransformation of the 2nd phase and is excreted from the body by the kidneys, as well as through the intestine, both unchanged and in the form of inactive sulfo compounds (Ml) and glucuronides (M2). Moxifloxacin is not biotransformed by the cytochrome P450 microsomal system. Metabolites Ml and M2 are present in blood plasma at concentrations lower than the parent compound. According to the results of preclinical studies, it was proved that these metabolites do not have a negative effect on the body in terms of safety and tolerability.
Withdrawal
The half-life of the drug is approximately 12 hours. The average total clearance after administration at a dose of 400 mg is 179-246 ml / min. Renal clearance is 24-53 ml / min. This indicates a partial tubular reabsorption of the drug.
The mass balance of the parent compound and the phase 2 metabolites is approximately 96-98%, which indicates 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 different patient groups
Age, gender and ethnicity
Age and sex differences in the pharmacokinetics of moxifloxacin have not been established. There were no clinically significant differences in the pharmacokinetics of moxifloxacin in patients of different ethnic groups.
Children
The pharmacokinetics of moxifloxacin in children have not been studied.
Renal failure
There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including patients with creatinine clearance<30 мл/мин/ 1,73 м 2), находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе.
Liver dysfunction
There were no significant differences in the concentration of moxifloxacin in patients with impaired liver function (classes A, B, C according to Child-Pugh classification) compared with healthy volunteers and patients with normal liver function (for use in patients with cirrhosis, see also "Special instructions ").

Indications for use
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 antibiotic resistance *,
• Complicated infections of the skin and subcutaneous structures (including an infected diabetic foot),
• Complicated intra-abdominal infections, including polymicrobial infections, including intraperitoneal abscesses,
• Uncomplicated inflammatory diseases of the pelvic organs (including salpingitis and endometritis).
• Streptococcus pneumoniae with multiple antibiotic resistance include strains resistant to penicillin and strains resistant to two or more antibiotics from groups such as penicillins (with MIC> 2 μg / ml), II 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

• Hypersensitivity to moxifloxacin, other quinolones or any other component of the drug,
• Age under 18,
• Pregnancy and the period of breastfeeding,
• A history of tendon pathology that developed as a result of treatment with quinolone antibiotics
• In preclinical and clinical studies, after the introduction of moxifloxacin, a change in the electrophysiological parameters of the heart was observed, expressed in an increase in 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 congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
• 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 an increase in transaminases more than five times higher than the upper limit of the norm.

Carefully
- in diseases of the central nervous system (including those suspicious of involvement of the central nervous system), predisposing to the occurrence of seizures and lowering the threshold of seizure activity; in patients with potentially proarrhythmic conditions, such as acute myocardial ischemia, especially in women and elderly patients; with myasthenia gravis; with cirrhosis of the liver; when taken simultaneously with drugs that reduce potassium.

Application during pregnancy and during breastfeeding
The safety of using moxifloxacin during pregnancy has not been established and its use is contraindicated. Cases of reversible joint damage have been reported in children receiving certain 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 damage to the cartilage of large joints in premature animals. In preclinical studies, it has been established that a small amount of moxifloxacin is excreted in breast milk. There are no data on its use in women during lactation. Therefore, the appointment of moxifloxacin during breastfeeding is contraindicated.

Method of administration and dosage
Recommended dosage regimen of moxifloxacin: 400 mg (1 tablet) once a day for the above infections. Do not exceed the recommended dose.
The tablets should be swallowed whole, without chewing, with plenty of water, regardless of the meal.
Duration of treatment
The duration of treatment is determined by the localization 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: the total duration of sequential therapy (intravenous followed by oral administration) is 7-14 days,
• Complicated infections of the skin and subcutaneous structures: the total duration of sequential 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 pelvic inflammatory disease - 14 days.

The recommended duration of treatment should not be exceeded.
According to clinical studies, the duration of treatment with Avelox ® tablets can be up to 21 days.
Elderly patients
Dosage regimen changes in elderly patients are not required.
Children
The efficacy and safety of using moxifloxacin in children and adolescents has not been established.
Liver dysfunction
Patients with impaired liver function do not need to change the dosage regimen (for use in patients with liver cirrhosis, see the "Special Instructions" section).
Renal failure
In patients with impaired renal function (including severe renal failure with creatinine clearance< 30 мл/мин/1,73 м 2), а также у пациентов, находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе, изменения режима дозирования не требуется.
Use in patients of different ethnic groups
No dosage changes are required.

Side effect
Data on adverse reactions reported with moxifloxacin 400 mg (by mouth, with sequential therapy [intravenous followed by oral administration] and only intravenously) are obtained from clinical studies and post-marketing reports (in italics). Adverse reactions listed in the "frequent" group occurred with a frequency below 3%, with the exception of nausea and diarrhea.
In each frequency group, adverse drug reactions are listed in decreasing order of importance. The frequency is determined as follows:
often (> 1/100 to<1/10),
infrequently (from> 1/1000 to<1/100),
rarely (from> 1/10000 to<1/1000),
very rarely (<1/10000).

Systemic organ classes (MedDRA)	Often	Infrequently	Rarely	Very rarely
Infections and infestations	Fungal superinfections
Disorders of the circulatory and lymphatic system		Anemia Leukopenia Neutropenia Thrombocytopenia Thrombocythemia Prolongation of prothrombin time / increase in international normalized ratio (MHO)	Changes in thromboplastin concentration	Increase in prothrombin concentration / decrease in MHO Change in prothrombin concentration / change in MHO
Immune system disorders		Allergic reactions Itching Rash Hives Eosinophilia	Anaphylactic / Anaphylactoid Reactions Angioedema, including laryngeal edema (potentially life-threatening)	Anaphylactic / anaphylactoid shock (including potentially life threatening)
Metabolic disorders		Hyperlipidemia	Hyperglycemia Hyperuricemia
Mental disorders		Anxiety Psychomotor hyperactivity / agitation	Emotional lability Depression ( in very rare cases, behavior with a tendency to self-harm, such as suicidal thoughts or suicidal attempts, is possible) Hallucinations	Depersonalization Psychotic reactions ( potentially manifesting in behavior with a tendency to self-harm, such as suicidal thoughts or suicidal attempts)
Nervous system disorders	Headache Dizziness	Paresthesias / Dysesthesias Taste disorders (including in very rare cases ageusia) Confusion and disorientation Sleep disturbances Tremor Vertigo Drowsiness	Hypesthesia Smell disorders (including anosmia) Atypical dreams Impaired coordination (including gait disturbances due to dizziness or vertigo, in very rare cases leading to injury from falls, especially in elderly patients) Seizures with various clinical manifestations (including "grand mal" seizures) Attention disorders Speech disorders Amnesia Peripheral neuropathy and polyneuropathy	Hyperesthesia
Violations of the organ of vision		Visual impairment (especially with reactions from the central nervous system)		Transient loss of vision (especially against the background of reactions from the central nervous system)
Hearing and labyrinth disorders			Noise in ears Hearing impairment including deafness (usually reversible)
Cardiovascular disorders	Prolongation of the QT interval in patients with concomitant hypokalemia	Prolongation of the QT interval Feeling of heartbeat Tachycardia Vasodilation	Ventricular tachyarrhythmias Fainting Hypertension Hypotension	Nonspecific arrhythmias Polymorphic ventricular tachycardia (Torsade de Pointes) Cardiac arrest, (predominantly in individuals with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia)
Respiratory, Chest and Mediastinal Disorders		Shortness of breath (including asthmatic conditions)
Gastrointestinal disorders	Nausea Vomit Stomach ache Diarrhea	Decreased appetite and reduced food intake Constipation Dyspepsia Flatulence Gastroenteritis (other than erosive gastroenteritis) Increased amylase activity	Dysphagia Stomatitis Pseudomembranous colitis (very rarely associated with life-threatening complications)
Liver and biliary tract disorders	Increased activity of "hepatic" transam inases	Liver dysfunction (including increased lactate dehydrogenase levels) Increased bilirubin levels Increased activity of gammaglutamyl transferase Increased blood alkaline phosphatase activity	Jaundice Hepatitis (predominantly cholestatic)	Fulminant hepatitis, potentially leading to life-threatening liver failure (including fatalities)
Skin and soft tissue disorders				Bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis (potentially life-threatening)
Musculoskeletal and connective tissue disorders		Arthralgia Myalgia	Tendinitis Increased muscle tone and cramps Muscle weakness	Tendon ruptures Arthritis Gait disorders due to damage to the musculoskeletal system Increased symptoms of myasthenia gravis
Kidney and urinary tract disorders		Dehydration (caused by diarrhea or decreased fluid intake)	Impaired renal function Renal impairment (due to dehydration, which can damage the kidneys, especially in older patients with pre-existing renal impairment)
General disorders and disorders at the injection site	Injection / infusion site reactions	General malaise Nonspecific pain Sweating Phlebitis / thrombophlebitis at the infusion site	Edema

The incidence of the following adverse reactions was higher in the group receiving step therapy:
Often: Increased activity of gamma glutamyl transferase
Infrequently: Ventricular tachyarrhythmias, hypotension, edema, pseudomembranous colitis (in very rare cases associated with life-threatening complications), seizures with various clinical manifestations (including "grand mal" seizures), hallucinations, impaired renal function, renal failure (as a result of dehydration which can lead to kidney damage, especially in elderly patients with pre-existing renal impairment)

Overdose
There are limited data on moxifloxacin overdose. No side effects were noted when using moxifloxacin in a dose of up to 1200 mg once and 600 mg for 10 days or more. In case of overdose, one should be guided by the clinical picture and carry out symptomatic supportive therapy with ECG monitoring.

Interaction with other medicinal products
When used together with atenolol, ranitidine, calcium supplements, theophylline, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenecid (no clinically significant interaction with moxifloxacin has been confirmed), dose adjustment is not required.
Antacids, multivitamins and minerals
Taking moxifloxacin simultaneously with antacids, multivitamins and minerals can lead to impaired absorption of moxifloxacin, due to the formation of chelate complexes with multivalent cations contained in these drugs. As a result, the concentration of moxifloxacin in the blood plasma can be significantly lower than the desired one. Therefore, antacids, antiretroviral drugs (such as didanosine) and other drugs containing magnesium or aluminum, sucralfate, and other drugs containing iron or zinc should be used at least 4 hours before or 4 hours after oral administration. moxifloxacin.
Warfarin
When combined with warfarin, prothrombin time and other parameters of blood coagulation do not change.
Changing the MHO value... In patients who received anticoagulants in combination with antibiotics, including moxifloxacin, there have been cases of an increase in the anticoagulant activity of anticoagulant drugs. Risk factors are the presence of an infectious disease (and a concomitant inflammatory process), the age and general condition of the patient. Despite the fact that the interaction between moxifloxacin and warfarin has not been identified, in patients receiving concomitant treatment with these drugs, it is necessary to monitor MHO and, if necessary, adjust the dose of indirect anticoagulants.
Digoxin
Moxifloxacin and digoxin have no significant effect on the pharmacokinetic parameters of each other. With the appointment of repeated doses of moxifloxacin, the maximum concentration of digoxin increased by approximately 30%, while the area under the concentration-time curve (AUC) and the minimum concentration of digoxin did not change.
Activated carbon
With the simultaneous use of activated carbon and moxifloxacin orally at a dose of 400 mg, the systemic bioavailability of the drug decreases by more than 80% as a result of inhibition of its absorption. In case of an 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 immediately reported to the doctor. Very rarely, even after the first use of the drug, anaphylactic reactions can progress to life-threatening anaphylactic shock. In these cases, treatment with moxifloxacin should be canceled and the necessary therapeutic measures (including anti-shock) should be carried out.
When using moxifloxacin, some patients may experience prolongation of the QT interval. When analyzing ECGs obtained during clinical studies, the corrected QT interval was 6 msec +/- 26 msec, 1.4% compared to baseline. Because women have a longer QT interval compared to 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 lengthening of the QT interval can increase with an increase in the concentration of the drug, therefore, the recommended should not be exceeded. However, in patients with pneumonia, a correlation between the concentration of moxifloxacin in the blood plasma and prolongation of the QT interval was noted. Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including polymorphic ventricular tachycardia. None of the 9000 patients treated with moxifloxacin had cardiovascular complications and deaths associated with prolonged QT interval. However, in patients with conditions predisposing to arrhythmias, the use of moxifloxacin may increase the risk of developing ventricular arrhythmias.
In this regard, moxifloxacin should not be prescribed to patients with an established prolongation of the QT interval, patients with uncorrected hypokalemia, as well as patients receiving class IA (quinidine, procainamide) and class III (amiodarone, sotalol, ibutilide) antiarrhythmic drugs.
Due to the risk of developing an additive effect on the QT interval, moxifloxacin should not be administered concurrently with drugs that prolong the QT interval (cisapride, erythromycin, antipsychotics, tricyclic antidepressants) in patients with conditions predisposing to arrhythmias such as clinically significant bradycardia, acute and also for those patients with cirrhosis of the liver who cannot exclude the risk of developing prolongation of the QT interval, especially women and elderly patients (since these categories of patients are more sensitive to drugs that prolong the QT interval).
When taking moxifloxacin, cases of fulminant hepatitis, potentially leading to the development of liver failure (including fatal cases), have been reported (see the "Side Effects" section). The patient should be informed that in the event of symptoms of hepatic failure, it is necessary to consult a doctor before continuing treatment with moxifloxacin.
When taking moxifloxacin, cases of development of bullous skin lesions (Stevens-Johnson syndrome, toxic epidermal necrolysis) have been reported. The patient should be informed that in the event of symptoms of skin or mucous membrane lesions, it is necessary to consult a doctor before continuing treatment with moxifloxacin.
The use of quinolone drugs is associated with a possible risk of seizures. Moxifloxacin should be used with caution in patients with CNS diseases and conditions suspicious of CNS involvement, predisposing to seizures or lowering the seizure threshold.
The use of broad-spectrum antibacterial drugs, including moxifloxacin, is associated with the risk of developing pseudomembranous colitis associated with antibiotic use. This diagnosis should be borne in mind in patients who experience severe diarrhea during treatment with moxifloxacin. In this case, appropriate therapy should be prescribed immediately. Drugs that inhibit intestinal motility are contraindicated in the development of severe diarrhea.
Moxifloxacin should be used with caution in patients with myasthenia gravis due to possible exacerbation of the disease.
Against the background of therapy with quinolones, including moxifloxacin, especially in the elderly and patients receiving glucocorticosteroids, tendinitis and tendon rupture may develop. At the first symptoms of pain or inflammation at the site of injury, the drug should be discontinued and the affected limb should be relieved. With the use of quinolones, photosensitivity reactions are noted. However, during preclinical and clinical studies, as well as with the use of moxifloxacin in practice, photosensitivity reactions were not observed. However, patients receiving moxifloxacin 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).
Patients on a diet with a low salt content (with heart failure, renal failure, with nephrotic syndrome) should take into account that the solution for infusion contains sodium chloride.
Dairy products and food intake
The absorption of moxifloxacin does not change with simultaneous ingestion of food (including dairy products). Moxifloxacin can be taken with or without food.

Influence on the ability to drive a car and moving machinery
Fluoroquinolones, including moxifloxacin, can interfere with the ability of patients to drive 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.

Release form
Film-coated tablets, 400 mg.
5 tablets in a blister of aluminum foil and PA / Al / PVC or aluminum foil and 1111. 1 or 2 blisters each with instructions for use in a cardboard box, or
7 tablets in a blister made of aluminum and PA / Al / PVC foil or aluminum and PP foil. 1 blister with instructions for use in a cardboard box.

Shelf life
5 years. Do not use after the expiration date printed on the package.

Storage conditions
At a temperature not higher than 25 ° C.
Keep out of the reach of children.

Vacation conditions
On prescription.

The legal entity in whose name the registration certificate was issued:
Bayer Pharma AG, Müllerstrasse 178, 13353 Berlin, Germany
Bayer Pharma AG, Mullerstrasse 178, 13353 Berlin, Germany

Manufacturer:
Bayer Pharma AT, D-51368, Leverkusen, Germany
Bayer Pharma AG, D-51368, Leverkusen, Germany

For more information, contact:
107113 Moscow, 3rd Rybinskaya st., 18, building 2.

Dosage form

Solution for infusion 400 mg / 250 ml

Composition

1 bottle contains

active substance - moxifloxacin hydrochloride 436.0 mg

(equivalent to moxifloxacin 400.0 mg),

excipients: sodium chloride, hydrochloric acid 1 M, sodium hydroxide solution 2 M, water for injection.

Description

Transparent yellow solution

Pharmacotherapeutic group

Antibacterial drugs for systemic use. Antimicrobial drugs are quinolone derivatives. Fluoroquinolones. Moxifloxacin.

ATX code J01MA14

Pharmacological properties

Pharmacokinetics

Absorption and bioavailability

After a single infusion of Avelox® at a dose of 400 mg for 1 hour, the maximum concentration of the drug (Cmax) is reached at the end of the infusion and is approximately 4.1 mg / l, which corresponds to an increase of approximately 26% compared with the value of this indicator when taking the drug inside. The exposure of the drug, determined by the AUC indicator (area under the concentration-time ratio) and equal to 39 mg * h / l, slightly exceeds that when the drug is taken orally (35 mg * h / l). The absolute bioavailability is approximately 91%.

After multiple intravenous infusions of the drug at a dose of 400 mg for 1 hour, the peak and minimum plasma concentrations in a stable state (400 mg once daily) reached values ​​from 4.1 to 5.9 mg / l and from 0.43 to 0.84 mg / l, respectively. In a stable state, the effect of the drug within the dosing interval is approximately 30% higher than after the first dose. Average stable concentrations of 4.4 mg / l are achieved at the end of the first hour of infusion.

Distribution

Moxifloxacin is very rapidly distributed in the extravascular bed. There is a large area under the AUC pharmacokinetic curve (AUCnorm = 6 kg * hours / L) with an equilibrium volume of distribution (Vss) of moxifloxacin of approximately 2 L / kg. The peak concentration of moxifloxacin in saliva is higher than in plasma. In in-vitro and in-vivo studies in the concentration range from 0.02 to 2 ml / L, the binding of moxifloxacin to proteins was approximately 45%, regardless of the concentration of the drug.

Moxifloxacin mainly binds to plasma albumin.

There is a high peak in free concentration> 10xMIC due to the low volume.

High concentrations of the drug, exceeding those in plasma, are created in the lung tissue (epithelial fluid, alveolar macrophages, biological tissue), in the sinuses and polyps, in the foci of inflammation. In saliva, interstitial fluid (intermuscular and subcutaneous), a high concentration of the drug in a free state is determined.

In addition, high concentrations of the drug are determined in the organs of the abdominal cavity and peritoneal fluid, as well as in the female genital organs.

After a single dose of 400 mg moxifloxacin, comparable maximum concentrations were observed with both routes of administration compared to plasma concentrations in different target tissues.

Metabolism

After passing through the 2nd phase of biotransformation, moxifloxacin is excreted from the body by the kidneys and the gastrointestinal tract (GIT) both unchanged and in the form of inactive sulfo compounds (M1) and glucuronides (M2). These metabolites are applicable only to the human body and do not have antimicrobial activity, Moxifloxacin is not biotransformed by the cytochrome P450 microsomal system.

Regardless of the method of administration, metabolites M1 and M2 are found in blood plasma at a concentration lower than the concentration of unchanged moxifloxacin.

Withdrawal

The half-life of the drug is approximately 12 hours. The average total clearance after administration at a dose of 400 mg ranges from 179 to 246 ml / min. Renal clearance of approximately 24-53 ml / min occurs by partial tubular reabsorption of the drug in the kidneys. The combined use of ranitidine and probenecid does not affect the renal clearance of the drug. Regardless of the route of administration, the starting substance moxifloxacin is almost completely metabolized 96-98% to metabolites of the II stage of metabolism without signs of oxidative metabolism.

Pharmacokinetics in different patient groups

Elderly patients

Differences in the pharmacokinetics of moxifloxacin have not been established.

There were revealed differences (33%) in pharmacokinetics (AUC, Cmax) between males and females. The revealed differences in AUC and Cmax were explained by differences in body weight rather than gender. Thus, they are not clinically relevant.

Ethnic differences

Possible interethnic differences were studied in Caucasian, Japanese, Negroid and other ethnic groups. No clinically significant differences in the pharmacokinetics of moxifloxacin have been established.

The pharmacokinetics of moxifloxacin in children have not been studied.

There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including patients with creatinine clearance< 30 мл/мин/1,73 кв.м) и у находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе.

Patients with impaired liver function

A study of the plasma concentration of moxifloxacin in patients with mild to severe hepatic impairment (stage A to stage C according to Child Pugh) did not reveal clinically significant differences in comparison with healthy volunteers or patients with normal liver function, respectively (See also in the section “ Special instructions "use in patients with liver cirrhosis).

Comparison of pharmacokinetic / pharmacodynamic processes for intravenous administration of a single dose of 400 mg Avelox

In patients requiring hospitalization, the AUC / MIC90 values ​​(area under the concentration-time to minimum inhibitory concentration curve) are higher than 125, and the Cmax / MIC90 in 8-10 are predictable for clinical treatment (Schentag). In outpatients, these indicators are generally lower: AUC / MIC90 above 30-40 (Dudley and Ambrose).

The table shows the corresponding pharmacokinetic / pharmacodynamic parameters for intravenous administration of Avelox® 400 mg, calculated from the data for a single dose:

a) 1 hour infusion

Pharmacodynamics

Mechanism of action

Avelox is an 8-methoxy-fluoroquinolone antibiotic with a broad spectrum of activity and bacterial action. Avelox has in vitro activity against a wide range of gram-positive and gram-negative organisms, anaerobic organisms, acid-fast bacteria and atypical forms, for example Chlamidia spp., Mycoplasma spp. and Legionella spp.

The bactericidal effect of the drug is due to the inhibition of bacterial topoisomerases II and IV - important enzymes that control DNA topology (responsible for replication, repair and transcription of microbial cell DNA).

The bactericidal effect of moxifloxacin depends on its concentration. The minimum bactericidal concentration of the drug is generally close to the minimum inhibitory concentration.

Avelox has a bactericidal effect on bacteria resistant to β-lactams and macrolides.

Resistance

The mechanisms leading to the development of resistance to penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not interfere with the antibacterial activity of the drug. Cross-resistance between these groups of antibacterial drugs and Avelox is not observed. Plasmid-mediated resistance has not yet been observed.

It was found that the C8-methoxy group in the structure of the drug increases the activity against gram-positive microorganisms and helps to reduce the development of selection mutants of resistant gram-positive bacteria compared to the C8-H-group. The presence of the azabicyclostructure at position C7 in the structure prevents active efflux (i.e., active release of fluoroquinolone from the cell), the mechanism underlying the development of resistance of microorganisms to fluoroquinolones.

Resistance to Avelox develops slowly through multiple mutations. The overall incidence of resistance development is very low (10-7 -

10-10). Repeated exposure of microorganisms to microorganisms at concentrations below the minimum inhibitory concentration (MIC) is accompanied by only a slight increase in MIC.

Cases of cross-resistance to quinolones have been reported. Nevertheless, some gram-positive and anaerobic microorganisms resistant to other quinolones remain sensitive to Avelox.

In vitro susceptibility data

Susceptible microorganisms:

Gram-positive bacteria:

Gardnerella vaginalis

Streptococcus pneumoniae (including multi-resistant strains of Streptococcus pneumoniae (MDRSP), including strains known as PRSP (penicillin-resistant St. Pneumoniae) and strains resistant to the following two or more antibiotics: penicillin (MIC ≥ 2 μg / ml), second generation cephalosporins (eg cefuroxime), macrolides, tetracyclines, and 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 dysgalactiae

Staphylococcus aureus (methicillin susceptible strains) *

Coagulase-negative staphylococci (S. cohnii, S. epidermidis, S. haemolyticus, S. hominis, S. saprophyticus, S. simulans) methicillin-susceptible strains

Gram-negative bacteria

Haemophillus influenzae (including strains producing and non-producing β-lactamases) *

Haemophillus parainfluenzae *

Moraxella catarrhalis (including strains producing and non-producing β-lactamases) *

Bordetella pertussis

Legionella pneumophilia Acinetobacter baumanii

Proteus vulgaris

Anaerobes:

Fusobacterium spp

Porphyromonas spp

Prevotella spp

Propionibacterium spp.

Atypical:

Chlamydia pneumoniae *, Chlamydia trachomatis **, Mycoplasma pneumoniae *, Mycoplasma hominis, Mycoplasma genitalium, Legionella pneumophila *, Coxiella burnetti

Intermediate microorganisms:

Gram-positive bacteria:

Enterococcus faecalis * (only strains susceptible to vancomycin and gentamicin)

Enterococcus avium *

Enterococcus faecium *

Gram negative bacteria:

Escherichia coli *

Klebsiella pneumoniae *

Klebsiella oxytoca Citrobacter freundii *

Enterobacter species (E. aerogenes, E. intermedius, E. sakazaki)

Enterobacter cloacae *

Pantoea agglomerans

Pseudomonas fluorescens

Burkholderia cepacia

Stenotrophomonas maltophilia

Proteus mirabilis *

Morganella morganii

Neisseria gonorrhoea **

Providencia species (P. rettgeri, P. stuartii)

Anaerobes:

Bacteroides sp (B. fragilis *, B. distasoni *, B. thetaiotaomicron *, B. ovatus *, B. uniformis *, B. vulgaris *)

Peptostreptococcus spp. *

Clostridium sp *

Resistant

Gram positive:

Staphylococcus aureus (methicillin / ofloxacin resistant strains) +

Coagulase-negative staphylococci (S. cohnii, S. epidermidis, S. haemolyticus, S. hominis, S. saprophyticus, S. simulans) methicillin-resistant strains

Gram-negative

Pseudomonas aeruginosa

* / ** Sensitivity to Avelox is confirmed by clinical data.

The use of Avelox® is not recommended for the treatment of infections caused by methicillin-resistant Staphylococcus aureus (MRSA). If an infection is suspected or confirmed to be caused by these strains (MRSA), treatment with an appropriate antibiotic should be initiated.

The incidence of acquired resistance in some strains of microorganisms can vary over time, depending on the geographic area.

It is desirable to have information on the local resistance of microorganisms, especially in the treatment of severe infections.

The above information serves as a guide for determining the susceptibility of microorganisms to Avelox.

Indications for use

Avelox® solution for infusion is indicated for the treatment of the following bacterial infections caused by microorganisms sensitive to the drug:

Community-acquired pneumonia, including those caused by multidrug-resistant

strains *

Complicated infections of the skin and soft tissues, including infected

"Diabetic foot"

Complicated intra-abdominal infections, including polymicrobial

infections such as abscesses.

* Multidrug-resistant Streptococcus pneumoniae (MDRSP) includes isolates known as PRSPs (penicillin-resistant S. pneumoniae) and strains resistant to the following two or more antibiotics: penicillin (MIC ≥2 μg / ml), second generation cephalosporins (such as cefuroxime) , macrolides, tetracyclines, and trimethoprim / sulfamethoxazole.

Official guidelines for the proper use of antibacterial drugs should be taken into account.

Method of administration and dosage

Duration of therapy

The duration of treatment is determined by the severity of the indications or the clinical effect.

At the initial stages of treatment, Avelox® solution for infusion can be used, and then, in the presence of clinical indications, the drug can be administered orally in tablets to continue therapy.

Complicated infections of the skin and soft tissues - the total duration of treatment for stepwise therapy (intravenous followed by oral therapy) is 7-21 days.

Complicated intra-abdominal infections - the total duration of treatment for stepwise therapy (intravenous followed by oral therapy) is 5-14 days.

Avelox® solution for infusion and Avelox® tablets have been tested in clinical trials for up to 21 days (for complicated infections of the skin and skin structure).

Children and adolescents

The efficacy and safety of Avelox® in children and adolescents under 18 years of age has not been established.

Elderly patients

Dosage regimen changes in elderly patients are not required.

Ethnic differences

No dosage change required by ethnicity

Patients with impaired liver function

Patients with impaired liver function do not need to change the dosage regimen.

Patients with impaired renal function

In patients with renal impairment (including creatinine clearance< 30 мл/мин/1,73 кв.м), а также у пациентов, находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе, изменения режима дозирования не требуется.

Instructions for use

The drug is administered intravenously as an infusion lasting at least 60 minutes.

Avelox® solution can be administered directly or through a T-shaped catheter with compatible infusion solutions.

A mixture of Avelox® solution with the infusion solutions below remains stable for 24 hours at room temperature, and therefore they can be considered compatible with Avelox® solutions for infusion.

· Water for injections

Sodium chloride 0.9%

Sodium chloride 1 molar

Glucose 5%

Glucose 10%

Glucose 40%

Xylitol 20%

Ringer's solution

Ringer's lactate solution

If Avelox® solution is prescribed together with another drug, each drug should be administered separately. Since the solution cannot be frozen or refrigerated, it cannot be stored in the refrigerator. On cooling, a precipitate may form and dissolve at room temperature. The solution must be stored in its original packaging.

Only a clear solution should be injected.

Side effects

Adverse events categorized as "frequent" were observed in less than 3% of patients, in addition to nausea and diarrhea.

Often (> 1/100 and 1 /< 10 %)

Candidal superinfection

Dizziness, headache

Prolongation of the QT interval on the ECG in patients with hypokalemia

Nausea, vomiting, abdominal pain, diarrhea

Increase in the level of transaminases in the blood

Injection and infusion site reactions

Infrequently (> / 1,000 and<1/10 %)

Anemia, leukopenia, neutropenia, trobocytopenia,

thrombocytosis, prolongation of the prothrombin time and an increase in the international normalized ratio

Allergic reactions, urticaria, pruritus, rash, eosinophilia

Hyperlipidemia

Feeling of anxiety, increased psychomotor activity, agitation

Paresthesia / dysesthesia

Taste disorders, including ageusia (loss of gustatory sensitivity) in very rare cases

Confusion of consciousness, disorientation, sleep disturbances, dizziness, tremors, somnolence

Visual impairment, especially in combination with reactions from the central nervous system

Prolongation of the QT interval on the ECG in patients, palpitations, tachycardia, vasodilation

Shortness of breath, including an asthmatic condition

Decreased appetite, constipation, dyspepsia, flatulence, gastroenteritis (except for erosive gastroenteritis)

Increased levels of amylase, bilirubin, liver dysfunction, including increased levels of lactate dehydrogenase, increased levels of gamma glutamyl transferase and alkaline phosphatase

Arthralgia, myalgia

Dehydration (caused by diarrhea or decreased fluid intake)

General malaise, non-specific pain, sweating

Thrombophlebitis at the infusion site

Rarely (> 1/10 0000 and<1/1 000)

Change in the concentration of thromboplastin

Anaphylactic / anaphylactoid reactions, allergic / angioedema, including laryngeal edema (potentially life-threatening)

Hyperglycemia, hyperuricemia

Emotional lability, depression (in very rare cases, potentially manifesting itself in behavior with a tendency to self-harm, such as suicidal thoughts or attempts), hallucinations

Hyposthesia, impaired sense of smell, including anosmia

Pathological dreams, impaired coordination (including gait disturbances mainly due to dizziness or vertigo (leading to injuries as a result of falls, especially in elderly patients in very rare cases), seizures with various clinical manifestations (including generalized), attention disorders, disorders speech, amnesia

Peripheral neuropathy and polyneuropathy

Tinnitus, hearing impairment, including deafness (usually reversible)

Syncope, hypotension, hypertension, ventricular tachyarrhythmias

Dysphagia, stomatitis, pseudomembranous colitis (associated with life-threatening complications in very rare cases), jaundice, hepatitis (mainly cholestatic)

Tendonitis, increased muscle tone and muscle cramps, muscle weakness

Renal impairment, renal failure (as a result of dehydration, especially in elderly patients with concomitant renal impairment)

Very rarely (<1/10 000)

Increase in the concentration of prothrombin and a decrease in the international normalized ratio or change in the concentration of prothrombin and the indicator of the international normalized ratio

Anaphylactic / anaphylactoid shock (including potentially life threatening)

Hypoglycemia

Depersonalization, psychotic reactions, potentially manifest

in behavior with a tendency to self-harm

Hyperesthesia

Transient visual impairment, especially in combination with reactions from the central nervous system

Nonspecific arrhythmias (including extrasystole), polymorphic ventricular tachycardia of the "pirouette" type, cardiac arrest, mainly in persons with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia

Fulminant hepatitis, potentially life-threatening

liver failure, including fatal

Bullous skin reactions such as Stevens-Johnson syndrome or

toxic epidermal necrolysis (potentially life-threatening)

Tendon ruptures, arthritis, gait disturbances due to muscle, tendon or joint damage, exacerbation of myasthenia gravis symptoms

The following adverse events were observed in the subgroup of patients on the stepwise therapy with Avelox® solution / Avelox® tablets:

Increased levels of gamma glutamyltransferase

Ventricular tachyarrhythmias, arterial hypotension, edema, antibiotic-induced pseudomembranous colitis (in very rare cases associated with life-threatening complications), seizures with various clinical manifestations (including generalized), hallucinations, impaired renal function and renal failure (as a result of dehydration, especially in elderly patients with concomitant renal impairment).

Contraindications

Known hypersensitivity to moxifloxacin or other quinolones, as well as to any of the components of the drug

Children and adolescents up to 18 years old

Pregnancy and lactation

Drug interactions

No dosage adjustment is required when used together with atenolol, ranitidine, calcium supplements, theophylline, cyclosporine, oral contraceptives, glibenclamide, itraconazole, digoxin, morphine, probenicide (the absence of clinically significant interaction with Avelox® was confirmed).

Warfarin

When combined with warfarin, the pharmacokinetics, prothrombin time and other parameters of blood coagulation do not change.

Change in INR (International Normalized Ratio)

In patients who received anticoagulants in combination with antibiotics, including Avelox®, there have been cases of an increase in the anticoagulant activity of anticoagulants. Risk factors are the presence of an infectious disease (and a concomitant inflammatory process), the age and general condition of the patient. Despite the fact that the interaction between Avelox® and warfarin is not detected, in patients receiving combined treatment with these drugs, it is necessary to monitor the INR and, if necessary, adjust the dose of oral anticoagulants.

Digoxin

Avelox® and digoxin do not significantly affect the pharmacokinetic parameters of each other. With the appointment of repeated doses of the drug in healthy individuals, the maximum concentration of digoxin increased by approximately 30%, while the ratio of the area under the concentration-time curve (AUC) and the minimum concentration of digoxin did not change.

Activated carbon

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

Food and dairy products

The absorption of the drug does not change with the simultaneous intake of food (including dairy products). Avelox® can be taken with or without food.

Incompatibility

The following solutions are incompatible with Avelox® solution:

Sodium chloride solution 10% and 20%

Sodium bicarbonate solution 4.2% and 8.4%

special instructions

In some cases, after the first use of the drug, hypersensitivity and allergic reactions may develop, which must be immediately informed by the doctor.

Very rarely, anaphylactic reactions can progress to life-threatening anaphylactic shock, in some cases after the first use of the drug. In these cases, Avelox® should be canceled and the necessary therapeutic measures (including anti-shock) should be carried out.

The use of drugs of the quinolone series is associated with a possible risk of seizure development. Avelox® should be used with caution in patients with diseases of the central nervous system and with conditions suspicious of involvement of the central nervous system, predisposing to the occurrence of seizures or lowering the threshold of seizure activity.

With the use of Avelox® in some patients, there may be an increase in the QT interval on the electrocardiogram.

Given that women tend to lengthen the QT interval compared to men, they may be more sensitive to drugs that prolong the QT interval. Elderly patients may also be more sensitive to these drugs.

The degree of lengthening of the QT interval may increase with increasing drug concentration, therefore, the recommended dose and infusion rate (400 mg in 60 minutes) should not be exceeded. However, in patients with pneumonia, no correlation was found between the concentration of the drug in the blood plasma and the prolongation of the QT interval. Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including pirouette-type polymorphic ventricular tachycardia. When taking the drug, there were no cardiovascular complications and deaths associated with prolongation of the QT interval. However, in patients with certain conditions predisposing to arrhythmias, the use of Avelox® may increase the risk of ventricular arrhythmias.

In this regard, the prescription of the drug should be avoided in the following patients, since the experience of using Avelox in these patients is limited:

With prolongation of the QT interval

With untreated hypokalemia

Who are receiving class IA (quinidine, procainamide) or class III (amiodarone, sotalol) antiarrhythmic drugs

Avelox® should be prescribed with caution, since the additive effect of moxifloxacin cannot be ruled out under the following conditions:

In patients receiving concomitant treatment with drugs that prolong the QT interval (cisapride, erythromycin, antipsychotics, tricyclic antidepressants)

In patients with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia

In patients with cirrhosis of the liver, since the presence of prolongation of the QT interval in them cannot be ruled out

In women or elderly patients who may be more sensitive to drugs that prolong the QT interval

With the use of Avelox®, cases of fulminant hepatitis have been reported, potentially leading to life-threatening liver failure, including death. If signs of liver failure appear, patients should immediately consult a doctor before continuing treatment.

Cases of bullous skin reactions have been reported, such as Stevens-Johnson syndrome or toxic epidermal necrolysis (potentially life-threatening). In case of reactions from the skin and / or mucous membranes, you should also immediately consult a doctor before continuing treatment.

Since the use of broad-spectrum antibacterial drugs, including Avelox®, is associated with the risk of developing pseudomembranous colitis associated with antibiotic use, this diagnosis should be borne in mind in patients who have severe diarrhea during treatment with the drug. In this case, appropriate therapy should be prescribed immediately. In patients with severe diarrhea, drugs that inhibit intestinal motility are contraindicated.

Avelox® should be used with caution in patients with myasthenia gravis, as the drug may exacerbate the symptoms of this disease.

Against the background of therapy with fluoroquinolones, including Aveloxom®, especially in the elderly and patients receiving glucocorticosteroids, tendinitis and tendon rupture may develop; there were isolated cases of development within several months after completion of therapy. At the first symptoms of pain or inflammation at the site of injury, the drug should be discontinued and the affected limb should be relieved.

With the use of quinolones, photosensitivity reactions are noted. However, with the use of Avelox®, photosensitivity reactions were not observed, neither in specially designed clinical studies, nor in normal clinical practice. However, patients receiving the drug should avoid direct sunlight and ultraviolet radiation.

For patients with complicated pelvic inflammatory diseases (for example, associated with tubo-ovarian or pelvic abscesses), for whom intravenous treatment is indicated, taking Avelox® in tablets of 400 mg is not recommended.

Avelox® is not recommended for the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infection. In case of suspicion or confirmation of the specified infection, you should start with the use of an appropriate antibacterial drug (see section "Pharmacodynamic properties").

In vitro studies of the activity of monoxifloxacin have shown that interaction with the culture of Mycobacterium is possible due to the suppression of mycobacterial growth, which can lead to a false-negative result in samples obtained from patients receiving Avelox®.

With the use of quinolones, including Avelox, cases of sensory and sensorimotor polyneuropathy have been reported, leading to paresthesia, hypoesthesia, dysesthesia, or weakness. If symptoms of neuropathy develop, such as pain, burning, tingling, numbness or weakness in patients undergoing treatment with Avelox®, you should immediately consult a doctor before continuing treatment.

Mental reactions may appear even after the first use of fluoroquinolone drugs, including Avelox®.

In very rare cases, depression or psychotic reactions have progressed to the development of suicidal thoughts or behavior with a tendency to self-harm (see section "Side effects").

If the patient develops these reactions, it is necessary to stop treatment with Avelox and take appropriate measures. Caution is advised when using the drug in psychotic patients or in patients with a history of psychiatric illness.

Given the widespread prevalence and increasing frequency of fluoroquinolone-resistant forms of Neisseria gonorrhoeae infection, it is recommended to prescribe Avelox® monotherapy in patients with pelvic inflammatory disease after excluding N. gonorrhoeae resistance to fluoroquinolones.

If resistance of Neisseria gonorrhoeae infection to fluoroquinolones cannot be ruled out, an appropriate antibiotic that works against N. gonorrhoeae (eg, cephalosporins) should be considered in addition to Avelox® therapy.

For patients on a low sodium diet (with congestive heart failure, renal failure, nephrotic syndrome, etc.), additional sodium intake with an infusion solution should be taken into account.

Dysglycemia

Taking Avelox®, like other fluoroquinolones, can cause fluctuations in blood sugar levels: cases of hypoglycemia and hyperglycemia have been reported. In the treatment of Aveloxom, dysglycemia mainly occurs in elderly patients with diabetes mellitus and receiving therapy with oral hypoglycemic drugs (for example, sulfonylureas) or insulin.

Pregnancy and lactation

The safety of Avelox® during pregnancy has not been established. Reversible joint damage has been reported in children treated with some quinolone antibiotics, but no fetal effects have been reported. The potential risk to humans is unknown.

Therefore, the use of Avelox® during pregnancy is contraindicated.

There are no data on the use of Avelox® in women during lactation and lactation. Therefore, the use of Avelox® in lactating women is contraindicated.

Features of the influence of the drug on the ability to drive vehicles and potentially dangerous mechanisms.

Fluoroquinolones, including Avelox®, can impair the ability to drive or operate machinery due to reactions from the central nervous system.

Overdose

Symptoms - single doses of up to 1200 mg and multiple doses of 600 mg for 10 days were administered to healthy people and were not accompanied by any side effects.

Treatment - in case of overdose, one should be guided by the clinical picture and carry out symptomatic supportive therapy with ECG monitoring.

Storage period

Do not use after the expiration date printed on the package.

Conditions of dispensing from pharmacies

On prescription

Manufacturer

Bayer Pharma AG,

D-51368 Leverkusen, Germany.

Avelox (in Latin) is used to treat inflammatory diseases of various etiologies. The systematic use of the drug does not lead to the development of resistance of pathogens to the active substance.

Taking pills can cause undesirable reactions in the body, which in most cases leads to dysfunction of the digestive tract.

ATX

J01MA14 - anatomical-therapeutic-chemical classification code.

Composition and dosage forms

The product is produced in 2 dosage forms.

Pills

1 oblong tablet contains 400 mg of moxifloxacin (active ingredient).

The drug is produced in blisters of 5 or 7 tablets each.

Solution for infusion

The medication used for intravenous administration is produced in 250 ml glass vials. The concentration of the active substance is 1.6 mg / ml.

Pharmacological group

The antibacterial drug belongs to the group of fluoroquinolones.

pharmachologic effect

It is important to consider the following features:

1. The active component of the antibiotic has a destructive effect on the cell membrane of infectious agents, preventing the replication of pathogenic agents.
2. The use of the medication does not cause severe intoxication of the body.
3. The agent has selective activity against bacteria resistant to beta-lactam and macrolide antibiotics.

Pharmacokinetics

After a single oral administration, the active substance of the agent is absorbed into the systemic circulation from the intestine by 90%. Food intake insignificantly affects the rate of absorption of the active ingredient.

When the drug is administered intravenously in the form of a solution, the maximum concentration of moxifloxacin in the blood plasma is observed within a few minutes after the injection and is 3.2 mg / l.

Decomposition products of the active component are excreted in the urine and in small quantities in the faeces.

Metabolites do not have a negative effect on the organs of various body systems.

What are they prescribed for?

The medication is indicated for use in a number of such clinical cases:

• with otitis media, acute sinusitis and chronic sinusitis;
• with infections of the skin and subcutaneous structures;
• with exacerbation of chronic bronchitis against the background of a short remission;
• with community-acquired pneumonia, the causative agents of which are multidrug-resistant strains;
• with accumulation of pus in the abdominal cavity (intra-abdominal abscess);
• with chlamydia and trichomoniasis;
• with a venereal disease, which is provoked by ureaplasma;
• with urinary tract infection;
• with inflammation of the pelvic organs (endometritis, salpingitis).

How to take Avelox

The agent is administered intravenously once a day. Intramuscular injections cause intense pain at the injection site.

Use only a clear solution (no sediment or turbidity), mixing it with 5% dextrose solution.

Average duration of treatment

A number of such features should be taken into account:

1. The chronic form of the inflammatory process in the bronchi requires taking pills for 5 days.
2. In case of pneumonia, oral and parenteral administration of the drug is recommended for 1-2 weeks.
3. In the case of diabetic foot syndrome, the agent is taken within 21 days.
4. With an intra-abdominal abscess, the doctor prescribes a 5-day course of treatment.

How many days does it keep working

The drug has a long-term therapeutic effect (at least 7 days), because its main function is to disrupt the reproductive activity of pathogenic agents, which leads to their death.

Avelox dosage

For any infectious diseases, the dosage of the active ingredient is 0.4 g.

With prostatitis

Prior consultation with a specialist is required to select the exact dosage of moxifloxacin in order to avoid complications.

special instructions

During pregnancy and breastfeeding

The drug has high reproductive toxicity. Avelox is contraindicated in any trimester of pregnancy, because the remedy leads to problems of intrauterine development.

During lactation, you can also not take medicine.

In childhood

Reversible joint damage in children is not uncommon.

In old age

No dose adjustment is required if the drug is prescribed to patients over 60 years of age.

For violations of liver function

No complications were observed in patients with severe hepatic dysfunction.

With impaired renal function

With renal failure, taking pills is not contraindicated.

Side effects of Avelox

The drug causes a number of such side effects:

• anemia;
• anaphylactic shock and urticaria in case of hypersensitivity to moxifloxacin (Steven-Johnson syndrome);
• hyperglycemia (high blood sugar);
• mental disorders: anxiety, depression, accompanied by the appearance of suicidal thoughts;
• headache and dizziness, confusion, drowsiness, impaired coordination of movements, convulsions in elderly patients, hyperesthesia (a sharp increase in the sensitivity of the sense organs);
• violation of visual function;
• vomiting, upset stools, and decreased appetite;
• polymorphic ventricular tachycardia;
• increased activity of liver enzymes;
• increased sweating.

Contraindications

You can not use the drug in any dosage form for:

• heart disease: decreased heart rate (bradycardia), acute myocardial ischemia, arrhythmias;
• diseases of the central nervous system;
• lactose intolerance;
• cirrhosis of the liver.

Overdose

There is little data on cases of overdose with Avelox.

Interoperability and compatibility

You should pay attention to the following features:

1. There is no need to adjust the dose when using oral contraceptives together.
2. The risk of developing arrhythmias increases with the simultaneous use of drugs that lengthen the QT interval.
3. With the combined use of Activated Carbon and Avelox, the absorption process of moxifloxacin slows down.
4. The drug increases the activity of anticoagulants when used simultaneously.
5. Sumamed or Doxycycline capsules together with Avelox are prescribed for the treatment of chlamydia. The drugs enhance each other's therapeutic effects.
6. Longidaza increases the effectiveness of Avelox.
7. With the simultaneous administration of Amoxiclav (the dosage of the active substance is 500 mg), the symptoms of pneumonia disappear in a shorter time.

With alcohol

There is a high risk of intoxication of the body against the background of a decrease in the effectiveness of the therapeutic effect of moxifloxacin when drinking alcohol.

Manufacturer

Conditions of dispensing from pharmacies

You can get the product at the pharmacy with a doctor's prescription.

Price

The cost of Avelox is about 750 rubles. for 5 tablets.

Conditions and shelf life

It is important to store the drug at a temperature not exceeding + 15 ° C for no more than 3 years from the date of production.

Analogs

There are such synonymous drugs (contain the same active ingredient): Moxifloxacin, Moxin, Vigamox. These medicines are cheaper, but they are no less effective analogues of Avelox premium.

Other drugs of the fluoroquinolone group can be attributed to drug substitutes: Tavanik, Moflaxia.