Avelox is an effective drug that successfully copes with bacterial infections. Avelox analogues and prices Instructions for use. Contraindications and release form

Release form

Solution for infusion

Package

pharmachologic effect

Antibacterial drug of the fluoroquinolone group. Has a bactericidal effect. The mechanism of action is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of the DNA synthesis of the microbial cell. In vitro, the drug is active against a wide range of gram-negative and gram-positive bacteria, anaerobes, acid-fast bacteria and atypical forms, incl. Mycoplasma, Chlamydia, Legionella. Effective against bacteria resistant to beta-lactam and macrolide antibiotics.
To Avelox Gram-positive bacteria are sensitive: Staphylococcus aureus (including strains sensitive to methicillin), Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A); Streptococcus milleri, Streptococcus mitior, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohni, Staphylococcus epidermidis (including strains sensitive to methicillin), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Coryne bacterium diphtheriae; gram negative bacteria: Haemophilus influenzae (including strains producing beta-lactamases), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including strains producing beta-lactamases), Escherichia coli, Enterobacter cloacae; Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazakii, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii; anaerobic bacteria: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides unoformis, Fusobacterium spp., Porphyromonas spp. (including Porphyromonas anaerobus, Porphyromonas asaccharolytica, Porphyromonas magnus), Prevotella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum.
Avelox is also active against Chlamydia pneumoniae, Mycoplasma pneumoniae, Legionella pneumophila, Caxiella burnettii.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug in adults (18 years and older):
– acute sinusitis;
– exacerbation of chronic bronchitis;
– community-acquired pneumonia;
– infections of the skin and soft tissues.

Contraindications

– pregnancy;
– lactation (breastfeeding);
– childhood and adolescence;
– hypersensitivity to the components of the infusion solution and other quinolone drugs.

Use during pregnancy and breastfeeding

Avelox is contraindicated for use during pregnancy.
If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

special instructions

The use of quinolone drugs is associated with a possible risk of developing seizures. Given this, Avelox should be used with caution in patients with diseases of the central nervous system that predispose to seizures. The drug should not be prescribed to patients with epilepsy.
When using moxifloxacin, a slight increase in the QT interval is possible. There is a direct relationship between increasing moxifloxacin concentrations and increasing the QT interval. Taking this into account, you should not exceed the recommended dose (400 mg) and time of administration of the drug (60 minutes). An increase in the QT interval is associated with an increased risk of developing ventricular arrhythmias, including torsade de pointes. No morbidity or mortality associated with QT prolongation has been reported in more than 8,000 patients treated with moxifloxacin (either tablet or infusion). However, the drug should be prescribed with caution to patients with diseases accompanied by an increased risk of developing ventricular arrhythmias, with congenital or acquired diseases accompanied by prolongation of the QT interval, or receiving drugs that potentially slow cardiac conduction (including antiarrhythmics of classes Ia, II, III, tricyclic antidepressants, antipsychotics).
Currently, there is insufficient clinical data on the use of moxifloxacin in patients with clinically significant bradycardia and signs of acute myocardial ischemia. Due to the risk of developing arrhythmia, Avelox should be prescribed to these patients with caution.
Considering that during fluoroquinolone therapy in elderly patients and patients receiving corticosteroids, there is a risk of tendon rupture or tenosynovitis, it is recommended to stop using Avelox if pain or signs of tendon inflammation occur. Clinical studies have not reported cases of tendon rupture while taking moxifloxacin. However, Avelox should be used with caution during treatment with corticosteroids.
There is a risk of developing hypersensitivity reactions and anaphylactic reactions during the initial use of the drug; such cases should be reported to the doctor immediately. It is extremely rare that an anaphylactic reaction can progress to anaphylactic shock. In such cases, you should immediately stop administering the drug and carry out appropriate resuscitation measures.
Patients with impaired renal function (including those with CC2) do not require adjustment of the dosage regimen. Data on the pharmacodynamics and pharmacokinetics of moxifloxacin in patients on hemodialysis are currently insufficient.
In case of liver dysfunction (Child Pugh A, B), no dosage adjustment is required. The pharmacodynamics and pharmacokinetics of moxifloxacin in patients with impaired liver function Child Pugh C have not been studied, so the drug should be prescribed with caution to this category of patients.
In elderly patients, no dosage adjustment is required.
When moxifloxacin and itraconazole are used simultaneously, no change in dosage regimen is required.
Moxifloxacin has no potential phototoxicity.
Use in pediatrics
The use of Avelox for infusion in children and adolescents is not recommended.

Compound

1 fl. contains moxifloxacin (hydrochloride form) 400 mg

Directions for use and doses

As an intravenous infusion (slowly, over 60 minutes) - 400 mg once a day. The course of treatment for exacerbation of chronic bronchitis is 5 days, community-acquired pneumonia is 10 days, acute sinusitis, skin and soft tissue infections is 7 days. No change in dosage regimen is required in elderly patients, with hepatic (groups A, B on the Child-Pug scale) and/or renal (including with CC less than 30 ml/min/1.73 sq.m.) insufficiency.

Side effects

Frequency of side effects: often - >=1%=0.1%=0.01% From the digestive system: often - abdominal pain, nausea, diarrhea, vomiting, symptoms of dyspepsia, taste disturbances, changes in liver tests; rarely - dry mouth, flatulence, constipation, candidiasis of the oral mucosa, lack of appetite, stomatitis, glossitis, dysfunction of the gastrointestinal tract, increased GGT activity; in some cases - gastritis, change in tongue color, dysphagia, transient jaundice.
From the central nervous system and peripheral nervous system: often - headache, dizziness; rarely - insomnia, nervousness, drowsiness, anxiety, tremor, paresthesia; in isolated cases - hallucinations, depersonalization, increased muscle tone, coordination disorders, agitation, amnesia, aphasia, emotional lability, sleep disorders (including parasomnias), speech disorders, cognitive impairment, hypoesthesia, convulsions, confusion, depression .
From the cardiovascular system: often - prolongation of the QT interval in patients with concomitant hypokalemia; rarely - tachycardia, arterial hypertension, palpitations, prolongation of the QT interval with normal potassium levels in the blood; in some cases - arterial hypotension, vasodilation, peripheral edema.
From the hematopoietic system: rarely - leukopenia, increased prothrombin time, eosinophilia, thrombocytosis; in isolated cases - decreased thromboplastin levels, decreased prothrombin time, thrombocytopenia, anemia.
From the side of metabolism: rarely - increased amylase activity; in isolated cases - hyperglycemia, hyperuricemia, increased LDH (due to changes in liver tests).
From the musculoskeletal system: rarely - arthralgia, myalgia; in isolated cases - arthritis, tendinopathy.
From the respiratory system: rarely - shortness of breath; in isolated cases - bronchial asthma.
From the reproductive system: rarely - vaginal candidiasis, vaginitis.
From the urinary system: in isolated cases - impaired renal function.
From the senses: in isolated cases - visual impairment, amblyopia, loss of taste sensitivity, parosmia.
Dermatological reactions: rarely - rash, itching, increased sweating.
Allergic reactions: in isolated cases - urticaria.
Local reactions: often - swelling, allergic reactions, inflammation, pain in the area where the drug was administered; rarely - phlebitis at the infusion site.
Other: rarely - asthenia, candidiasis, feeling of general discomfort, chest pain; in some cases - pain in the pelvis, swelling of the face, back pain, abnormal laboratory tests, allergic reactions, pain in the legs. During clinical trials, the majority of side effects (90%) were mild or moderate in severity.
In a number of cases, changes in laboratory parameters were observed, the occurrence of which is not directly related to the use of the drug: an increase or decrease in hematocrit, leukocytosis, erythrocytosis, erythropenia, a decrease in blood glucose levels, a decrease in hemoglobin levels, an increase in alkaline phosphatase levels, an increase in GGT/AST levels, an increase in levels GGT/ALT, increased levels of bilirubin, uric acid, creatinine, urea.

Drug interactions

With the simultaneous use of Avelox and corticosteroids, the risk of developing tenosynovitis or tendon rupture increases.
Clinical studies have not revealed any interaction of Avelox with probenecid, warfarin, or oral contraceptives. No clinically significant interaction has been established between moxifloxacin and glibenclamide.
Pharmacokinetic interaction
Moxifloxacin slightly changes the pharmacokinetic parameters of digoxin.
When used concomitantly, moxifloxacin does not affect the pharmacokinetics of theophylline.
With parenteral use of morphine and moxifloxacin, there is no decrease in the bioavailability of the latter.
Pharmaceutical interactions
Moxifloxacin infusion solution is incompatible with the following infusion solutions: sodium chloride 10%, sodium chloride 20%, sodium bicarbonate 4.2%, sodium bicarbonate 8.4%.

Overdose

There were no side effects observed when using Avelox in healthy volunteers in single doses of up to 1.2 g or at a dose of 600 mg/day for 10 days.
Treatment: in case of overdose, symptomatic therapy is carried out in accordance with the clinical situation. The use of activated carbon is advisable only in case of an overdose of moxifloxacin in tablet form. After intravenous administration, activated charcoal slightly (approximately 20%) reduces the systemic exposure of moxifloxacin.

Storage conditions

The drug should be stored in a dry place, protected from light, at a temperature of 8° to 25°C, do not freeze.

Preparations containing Moxifloxacin (Moxifloxacin - ATC codes J01MA14, S01AX22):

Common forms of release (more than 100 offers in Moscow pharmacies)
Name	Release form	Packaging, pcs.	Manufacturer country	Price in Moscow, r	Offers in Moscow
Avelox	solution for infusion 1.6 mg/ml 250 ml in polymer bags	1	Germany, Bayer	845- (average 1790↘) -2678	161↗
Avelox	tablets 400mg	5	Germany, Bayer	727- (average 811) -878	513↗
Vigamox	eye drops 0.5% 5ml	1	USA, Alcon	129- (average 235↗) -301	554↗
Rarely encountered forms of release (less than 100 offers in Moscow pharmacies)
Moxin	injection solution 1.6 mg in 1 ml 250 ml in a bottle	1	India, Belko	2408	41↘
Plevilox	tablets 400mg	5	India, Plethiko for Pharmasyntez	719- (average 817↗) - 844	32↗

Avelox (original Moxifloxacin) - instructions for use. The drug is a prescription, information for healthcare professionals only!

Clinical and pharmacological group:

Antibacterial drug of the fluoroquinolone group.

pharmachologic effect

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

The minimum bactericidal concentrations of the drug are generally comparable to its minimum inhibitory concentrations (MICs).

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 been observed either. The overall incidence of resistance is very low (10-7-10-10). Resistance to moxifloxacin develops slowly through multiple mutations. Repeated exposure of microorganisms to moxifloxacin at concentrations below the MIC is accompanied by only a slight increase. Cases of cross-resistance to quinolones have been reported. However, some gram-positive and anaerobic microorganisms resistant to other quinolones remain sensitive to moxifloxacin.

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

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

Effect on human intestinal microflora

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

Pharmacokinetics

Suction

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

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

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

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

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

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

With multiple intravenous infusions at a dose of 400 mg over 1 hour, Cssmax and Cssmin range from 4.1 mg/l to 5.9 mg/l and from 0.43 mg/l to 0.84 mg/l, respectively. Average Css of 4.4 mg/l is achieved at the end of the infusion.

Distribution

The equilibrium state is achieved within 3 days.

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

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

High concentrations of the drug, exceeding those in plasma, are created in the lung tissue (including alveolar macrophages), in the bronchial mucosa, in the nasal sinuses, in soft tissues, skin and subcutaneous structures, and foci of inflammation. In interstitial fluid and 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 abdominal organs and peritoneal fluid, as well as in the tissues of the female genital organs.

Metabolism

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

Removal

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

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

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

Pharmacokinetics in special clinical situations

No age or gender differences have been established in the pharmacokinetics of moxifloxacin. There were no clinically significant differences in the pharmacokinetics of moxifloxacin in patients of different ethnic groups.

Pharmacokinetic studies of moxifloxacin have not been conducted in children.

There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including those with CC<30 1="" 73="" 2="" p="">

There were no significant differences in moxifloxacin concentrations in patients with impaired liver function (Child-Pugh grades A, B, C) compared with healthy volunteers and patients with normal liver function.

Indications for use of the drug AVELOX®

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

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

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

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

Dosage regimen

The drug is prescribed orally and intravenously at a dose of 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: for exacerbation of chronic bronchitis - 5-10 days; for community-acquired pneumonia, the total duration of stepwise therapy (intravenous administration followed by oral administration) is 7-14 days, first intravenously, then orally, or 10 days orally; for acute sinusitis and uncomplicated infections of the skin and soft tissues - 7 days; for complicated infections of the skin and subcutaneous tissues, the total duration of stepwise therapy (iv administration followed by oral administration) is 7-21 days; for complicated intra-abdominal infections, the total duration of step-down therapy (iv administration of the drug followed by oral administration) is 5-14 days; for uncomplicated inflammatory diseases of the pelvic organs - 14 days.

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

No change in dosage regimen is required in elderly patients.

The effectiveness and safety of moxifloxacin in children and adolescents has not been established.

Patients with impaired liver function do not require a change in dosage regimen.

In patients with impaired renal function (including severe renal failure with CC< 30 мл/мин/1.73 м2), а также у пациентов, находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе, изменения режима дозирования не требуется.

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

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

The solution for infusion should be administered intravenously over 60 minutes. The drug can be administered either diluted or undiluted using a T-piece). Avelox solution is compatible with the following solutions: 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.

Only clear solution should be used.

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

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

Side effect

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

In each frequency group, adverse drug reactions are listed in descending order of importance. The frequency is determined as follows: often (from ≥ 1/100 to< 1/10), нечасто (от >1/1000 to< 1/100), редко (от >1/10,000 to< 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 increase in INR; rarely - changes in thromboplastin concentration; very rarely - an increase in prothrombin concentration and a decrease in INR, a change in prothrombin concentration and a change in INR.

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

From the side of metabolism: 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 suicide attempts), hallucinations is possible; very rarely - depersonalization, psychotic reactions (potentially manifested in behavior with a tendency to self-harm, such as suicidal thoughts or suicide attempts).

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

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

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

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

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

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

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

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

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

Reactions associated with the administration of the drug: often - reactions at the injection/infusion site; infrequently - phlebitis/thrombophlebitis at the infusion site.

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

Contraindications to the use of AVELOX®

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

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

Use of AVELOX® during pregnancy and breastfeeding

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

Reproductive toxicity has been shown in animal studies. The potential risk to humans is unknown.

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

Use for liver dysfunction

Patients with minor liver dysfunction (class A or B on the Child-Pugh scale) do not require changes in the dosage regimen.

Use with caution in severe liver failure.

Use for renal impairment

Patients with impaired renal function (including those with CC<30 1="" 73="" 2="" p="">

Use in elderly patients

Elderly patients do not require changes in the dosage regimen.

Use in children

Contraindicated: children and adolescents under 18 years of age.

special instructions

In some cases, after the first use of the drug, hypersensitivity and allergic reactions may develop, which should be reported to your doctor immediately. Very rarely, even after the first use of the drug, anaphylactic reactions can progress to life-threatening anaphylactic shock. In these cases, treatment with moxifloxacin should be discontinued and the necessary therapeutic measures (including anti-shock) should be taken.

QT interval prolongation may occur in some patients when using moxifloxacin. When analyzing ECGs obtained during clinical trials, the corrected QT interval was 6 ms +/- 26 ms, 1.4% compared to baseline. Because women have a longer QT interval than men, they may be more sensitive to drugs that prolong the QT interval. Elderly patients are also more susceptible to drugs that affect the QT interval.

The degree of QT interval prolongation may increase with increasing drug concentrations, so do not exceed the recommended dose. However, in patients with pneumonia, a correlation between moxifloxacin plasma concentrations 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 9,000 patients treated with moxifloxacin experienced cardiovascular events or deaths associated with QT prolongation. However, in patients with conditions predisposing to arrhythmias, the risk of developing ventricular arrhythmias may be increased when using moxifloxacin.

In this regard, moxifloxacin should not be prescribed to patients with established prolongation of the QT interval, patients with uncorrected hypokalemia, as well as patients receiving class I A (quinidine, procainamide) and class III antiarrhythmic drugs (amiodarone, sotalol, ibutilide).

Due to the risk of additive effects on the QT interval, moxifloxacin should not be administered concomitantly 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, and also to those patients with liver cirrhosis in whom the risk of developing a prolongation of the QT interval cannot be excluded, especially women and elderly patients (since these categories of patients are more sensitive to drugs that prolong the QT interval).

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

Cases of bullous skin lesions (Stevens-Johnson syndrome, toxic epidermal necrolysis) have been reported when taking moxifloxacin. The patient should be informed that if symptoms of skin or mucous membrane lesions occur, they should consult a doctor before continuing treatment with moxifloxacin.

The use of quinolone drugs is associated with a possible risk of developing seizures. Moxifloxacin should be used with caution in patients with diseases of the central nervous system and with conditions suspected of involving the central nervous system, predisposing to seizures or lowering the threshold for seizure activity.

The use of broad-spectrum antibacterial drugs, including moxifloxacin, is associated with the risk of developing antibiotic-associated pseudomembranous colitis. This diagnosis should be considered 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.

During therapy with quinolones, incl. moxifloxacin, especially in the elderly and patients receiving corticosteroids, tendonitis and tendon rupture may develop. At the first symptoms of pain or inflammation at the site of injury, the drug should be stopped and the affected limb should be unloaded.

When using quinolones, photosensitivity reactions are observed. However, during preclinical and clinical studies, as well as with the use of moxifloxacin in practice, no photosensitivity reactions were 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 low-salt diet (with heart failure, renal failure, nephrotic syndrome) should take into account that the solution for infusion contains sodium chloride.

Impact on the ability to drive vehicles and operate machinery

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

Overdose

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

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

In case of overdose when taking tablets, the use of activated carbon at an early stage of absorption prevents a further increase in systemic exposure.

Drug interactions

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

The combined oral use of Avelox and antacids, multivitamins and minerals may interfere with the absorption of moxifloxacin due to the formation of chelate complexes with polyvalent cations contained in these drugs, and therefore reduce the concentration of moxifloxacin in the blood plasma. In this regard, antacids, antiretrovirals (for example, didanosine) and other drugs containing calcium, magnesium, aluminum, iron, sucralfate, zinc should be taken at least 4 hours before or 4 hours after taking Avelox orally.

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

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

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

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

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

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

Incompatibility

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

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

List B. Tablets should be stored out of the reach of children, in a dry place at a temperature not exceeding 25°C. Shelf life - 5 years.

The solution for infusion should be stored out of the reach of children at a temperature of 15° to 30°C. Shelf life - 5 years.

International name

Moxifloxacin

Group affiliation

Antimicrobial agent, fluoroquinolone

Dosage form

Solution for infusion, film-coated tablets

pharmachologic effect

An antimicrobial agent from the fluoroquinolone group, it has a bactericidal effect. Shows activity against a wide range of gram-positive and gram-negative microorganisms, anaerobic, acid-fast and atypical bacteria: Mycoplasma spp., Chlamydia spp., Legionella spp. Effective against bacterial strains resistant to beta-lactam antibiotics and macrolides.

Active against most strains of microorganisms: gram-positive - Staphylococcus aureus (including strains insensitive to methicillin), Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A); gram-negative - Haemophilus influenzae (including both beta-lactamase-producing and non-beta-lactamase-producing strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including both beta-lactamase-producing and non-beta-lactamase-producing strains), Escherichia coli, Enterobacter cloacae; atypical – Chlamydia pneumoniae, Mycoplasma pneumoniae.

Based on in vitro studies, although the following microorganisms are sensitive to moxifloxacin, its safety and effectiveness in the treatment of infections have not been established. Gram-positive microorganisms: Streptococcus milleri, Streptococcus mitis, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohnii, Staphylococcus epidermidis (including strains sensitive to methicillin), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae. Gram-negative microorganisms: Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazakii, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii.

Anaerobic microorganisms: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevot ella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum. Atypical microorganisms: Legionella pneumophila, Coxiella burnetii.

Blocks topoisomerases II and IV enzymes that control the topological properties of DNA and are involved in DNA replication, repair and transcription. The effect of moxifloxacin depends on its concentration in the blood and tissues. Minimum bactericidal concentrations are almost the same as the MIC.

There is no cross-resistance with penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines. The overall incidence of resistance is low. In vitro studies have shown that resistance to moxifloxacin develops slowly as a result of a series of sequential mutations. Cross-resistance is observed between drugs from the fluoroquinolone group. However, some gram-positive and anaerobic microorganisms that are resistant to other fluoroquinolones are sensitive to moxifloxacin.

Does not have a photosensitizing effect.

Indications

Infections of the upper and lower respiratory tract: acute sinusitis, exacerbation of chronic bronchitis, community-acquired pneumonia; skin and soft tissue infections.

Contraindications

Hypersensitivity, age under 18 years, epilepsy, severe diarrhea, pregnancy, lactation. With caution. Convulsive syndrome (history), liver failure (group C on the Child-Pug scale), prolongation of the Q-T interval; bradycardia, myocardial ischemia, simultaneous use of drugs that slow down cardiac conduction (including class Ia, II, III antiarrhythmics, tricyclic antidepressants, antipsychotics); patients on hemodialysis (insufficient experience of use); diarrhea, pseudomembranous colitis; simultaneous administration of corticosteroids.

Side effects

Often - 1-10%, rarely - 0.1-1%, extremely rarely - 0.01-0.1%.

From the digestive system: often - abdominal pain, dyspepsia (including flatulence, nausea, vomiting, constipation, diarrhea), increased activity of liver transaminases; rarely - dry mouth, candidiasis of the oral mucosa, anorexia, stomatitis, glossitis, increased gamma-glutamine transferase; extremely rarely - gastritis, discoloration of the tongue, dysphagia, transient jaundice.

From the nervous system: often – dizziness, headache; rarely - asthenia, insomnia or drowsiness, nervousness, anxiety, tremor, paresthesia; extremely rare - hallucinations, depersonalization, increased muscle tone, impaired coordination of movements, agitation, amnesia, aphasia, emotional lability, sleep disturbance, speech disorders, cognitive impairment, hypoesthesia, convulsions, confusion, depression.

From the senses: often – change in taste; extremely rarely - visual impairment, amblyopia, loss of taste sensitivity, parosmia.

From the cardiovascular system: rarely - tachycardia, increased blood pressure, palpitations, chest pain, prolongation of the Q-T interval; extremely rarely - decreased blood pressure, vasodilation,

From the respiratory system: rarely - shortness of breath; extremely rarely - bronchial asthma.

From the musculoskeletal system: rarely – arthralgia, myalgia; extremely rarely - back pain, leg pain, arthritis, tendinopathy.

From the genitourinary system: rarely – vaginal candidiasis, vaginitis; extremely rarely - pain in the lower abdomen, facial swelling, peripheral edema, impaired renal function.

Allergic reactions: rarely - rash, itching; extremely rarely - urticaria, anaphylactic shock.

Local reactions: often - swelling, inflammation, pain at the injection site; rarely – phlebitis.

Laboratory indicators: rarely - leukopenia, increased prothrombin time, eosinophilia, thrombocytosis, increased amylase activity; extremely rarely - decreased thromboplastin concentration, decreased prothrombin time, thrombocytopenia, anemia, hyperglycemia, hyperlipidemia, hyperuricemia, increased LDH activity. The connection with taking the drug has not been proven: an increase or decrease in hematocrit, leukocytosis, erythrocytosis or erythropenia, a decrease in the concentration of glucose, Hb, urea, an increase in alkaline phosphatase activity.

Other: rarely – candidiasis, general discomfort, sweating.

Application and dosage

Orally or as an intravenous infusion (slowly, over 60 minutes) – 400 mg once a day. The tablet is swallowed whole, without chewing, regardless of food intake. The course of treatment for exacerbation of chronic bronchitis is 5 days, community-acquired pneumonia is 10 days, acute sinusitis, skin and soft tissue infections is 7 days.

No change in dosage regimen is required in elderly patients, with hepatic (groups A, B on the Child-Pug scale) and/or renal (including with CC less than 30 ml/min/1.73 sq.m.) insufficiency.

special instructions

During fluoroquinolone therapy, inflammation and tendon rupture may develop, especially in elderly patients and in patients simultaneously receiving corticosteroids. At the first sign of pain or inflammation of the tendons, patients should stop treatment and immobilize the affected limb.

There is a direct relationship between increased concentrations of moxifloxacin and an increase in the QT interval (risk of developing ventricular arrhythmias, including torsades de pointes). As a result, the recommended dose (400 mg) and infusion rate (at least 60 minutes) should not be exceeded.

If severe diarrhea develops during treatment, the drug should be discontinued.

Interaction

Antacids, minerals, and multivitamins impair absorption (due to the formation of chelate complexes with polyvalent cations) and reduce the concentration of moxifloxacin in plasma (simultaneous administration is possible with an interval of 4 hours before or 2 hours after taking moxifloxacin).

Concomitant use with other quinolones increases the risk of QT interval prolongation.

Ranitidine reduces the absorption of moxifloxacin.

Does not interact with probenecid, warfarin, oral contraceptives, theophylline, glibenclamide, morphine, itraconazole.

Has little effect on the pharmacokinetic parameters of digoxin.

GCS increases the risk of developing tenosynovitis or tendon rupture.

The solution for infusion is compatible with the following drug solutions: 0.9% and 1 molar NaCl solution, water for injection, dextrose solution (5, 10 and 40%), 20% xylitol solution, Ringer's solution, Ringer-lactate, 10% Aminofusin solution, solution Yonosteryl.

Incompatible with 10 and 20% NaCl solutions, 4.2 and 8.4% Na bicarbonate solution.

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Instructions:

Clinical and pharmacological group

06.038 (Antibacterial drug of the fluoroquinolone group)

Release form, composition and packaging

The solution for infusion is transparent, greenish-yellow in color.

Excipients: sodium chloride, sodium hydroxide, hydrochloric acid, water for injection.

250 ml - polyolefin bags (1) - polyethylene bags laminated with foil (12) - cardboard boxes.

pharmachologic effect

Antibacterial drug of the fluoroquinolone group. Has a bactericidal effect. The mechanism of action is due to the inhibition of bacterial topoisomerases II and IV, which leads to disruption of microbial cell DNA synthesis and, as a consequence, to the death of the microbial cell. The minimum bactericidal concentrations of the drug are generally comparable to its MIC.

In vitro, 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., Chlamydia spp., Legionella spp., as well as bacteria resistant to β-lactam and macrolide antibiotics.

Gram-positive aerobic bacteria are sensitive to Avelox: Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A)*, Streptococcus milleri, Streptococcus mitis, Streptococcus agalactiae*, Streptococcus dysgalactiae, Streptococcus anginosus*, Streptococcus constellatus *, Staphylococcus aureus (including methicillin-sensitive strains)*, Staphylococcus cohnii, Staphylococcus epidermidis (including methicillin-sensitive strains), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae, Enterococcus faecalis (vancomycin and gent sensitive strains only amycin) *; gram-negative aerobic bacteria: Haemophilus influenzae (including strains that produce and do not produce β-lactamases)*, Haemophilus parainfluenzae*, Klebsiella pneumoniae*, Moraxella catarrhalis (including strains that produce and do not produce β-lactamases)*, Escherichia coli*, Enterobacter cloacae*, Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis*, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii, Gardnerella vaginalis; anaerobic bacteria: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis*, Bacteroides ovatus, Bacteroides thetaiotaomicron*, Bacteroides uniformis, Fusobacterium spp., Peptostreptococcus spp.*, Porphyromonas spp. (including Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus), Prevotella spp., Propionibacterium spp., Clostridium perfringens*, Clostridium ramosum; atypical bacteria: Chlamydia pneumoniae*, Mycoplasma pneumoniae*, Legionella pneumophila*, Coxiella burnettii, Chlamydia trachomatis, Mycoplasma hominis, Mycoplasma genitalium.

Moxifloxacin is less active against Staphylococcus aureus (strains resistant to methicillin/ofloxacin)*, Staphylococcus epidermidis (strains resistant to methicillin/ofloxacin)*, Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholderia cepacia, Stenotrophomonas maltophilia, Neisseria gonorrhea oea.

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 been observed either. The overall incidence of resistance is very low (10-7-10-10). Resistance to moxifloxacin develops slowly through multiple mutations. Repeated exposure of microorganisms to moxifloxacin at concentrations below the MIC is accompanied by only a slight increase in the MIC.

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

*sensitivity to moxifloxacin is confirmed by clinical data.

Pharmacokinetics

Suction

After oral administration, moxifloxacin is absorbed quickly and almost completely. After a single dose of moxifloxacin at a dose of 400 mg, Cmax in the blood is reached within 0.5-4 hours and is 3.1 mg/l. When taking moxifloxacin with food, there is a slight increase in the time to reach Cmax (by 2 hours) and a slight decrease in Cmax (by approximately 16%), while the duration of absorption does not change. However, these data do not have clinical significance, and the drug can be used regardless of food intake.

After a single infusion of Avelox at a dose of 400 mg over 1 hour, Cmax is reached at the end of the infusion and is 4.1 mg/l, which corresponds to an increase of approximately 26% compared to the value of this indicator when taken orally. With multiple intravenous infusions at a dose of 400 mg lasting 1 hour, Cmax varies from 4.1 mg/l to 5.9 mg/l. Average Css of 4.4 mg/l is achieved at the end of the infusion.

Absolute bioavailability is about 91%.

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

Distribution

The equilibrium state is achieved within 3 days.

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

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

Metabolism

Biotransforms to inactive sulfo compounds and glucuronides.

Moxifloxacin is not biotransformed by liver microsomal enzymes of the cytochrome P450 system.

Removal

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 and also in feces, both unchanged and in the form of inactive metabolites. With a single dose of 400 mg, about 19% is excreted unchanged in the urine, and about 25% in feces. T1/2 is approximately 12 hours. The average total clearance after administration at a dose of 400 mg ranges from 179 ml/min to 246 ml/min.

Pharmacokinetics in special clinical situations

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

Pharmacokinetic studies of moxifloxacin have not been conducted in children.

There were no significant changes in the pharmacokinetics of moxifloxacin in patients with impaired renal function (including those with CC<30 мл/мин/1.73 м2) и у находящихся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе.

In patients with mild to moderate hepatic impairment (class A or B on the Child-Pugh scale), the pharmacokinetics of moxifloxacin does not change. In patients with severe hepatic impairment (Child-Pugh class C), there are no data on the pharmacokinetics of moxifloxacin.

Dosage

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

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

The duration of treatment with Avelox IV can be up to 14 days, orally - 21 days.

Elderly patients, patients with minor liver dysfunction (class A or B on the Child-Pugh scale), patients with impaired renal function (including those with 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 meals.

The solution for infusion should be administered intravenously slowly over 60 minutes. The drug can be administered either diluted or 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-lactate solution, aminofusin solution 10%, ionosteril solution. Only clear solution should be used.

Overdose

There were no side effects observed when using Avelox at a dose of up to 1200 mg once and 600 mg for more than 10 days.

Treatment: in case of overdose, symptomatic therapy with ECG monitoring is carried out in accordance with the clinical situation. The use of activated carbon is advisable only in case of an overdose of moxifloxacin in tablet form.

Drug interactions

The combined oral use of Avelox and antacids, minerals and vitamin-mineral complexes may interfere with the absorption of moxifloxacin due to the formation of chelate complexes with polyvalent 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.

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

In patients receiving anticoagulants in combination with antibiotics, incl. with moxifloxacin, there have been cases of increased anticoagulant activity of anticoagulant drugs. Risk factors are the presence of an infectious disease (and concomitant inflammatory process), age and general condition of the patient. Although no interaction has been identified between moxifloxacin and warfarin, patients receiving concomitant treatment with these drugs should have their INR monitored and the dosage of oral anticoagulants adjusted if necessary.

Moxifloxacin and digoxin do not have a significant effect on each other's pharmacokinetic parameters. When moxifloxacin was re-administered, digoxin Cmax increased by approximately 30%. At the same time, the ratio of AUC and Cmix of digoxin does not change.

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

Use during pregnancy and lactation

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

A small amount of moxifloxacin is 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 studying the effect of moxifloxacin on reproductive function in rats, rabbits and monkeys, it was proven that moxifloxacin penetrates the placental barrier. Studies conducted on rats (with the administration of moxifloxacin orally and intravenously) and monkeys (with the administration of moxifloxacin orally) did not reveal the teratogenic effect of moxifloxacin and its effect on fertility. When moxifloxacin was administered intravenously 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 detected when moxifloxacin was used at 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 dose.

Side effects

Data on the side effects of moxifloxacin 400 mg (oral and step-down therapy) are obtained from clinical studies and post-marketing reports.

Determination of the frequency of adverse reactions: often (> 1%,< 10%), иногда (> 0.1%, <1%), редко (> 0.01%, <0.1%), очень редко (< 0.01%).

Adverse events classified as “common” were observed in less than 3% of patients, except nausea and diarrhea.

From the cardiovascular system: prolongation of the QT interval (often in patients with concomitant hypokalemia, sometimes in other patients); sometimes - tachycardia and vasodilation (flushing of the face); rarely - arterial hypotension, arterial hypertension, fainting, ventricular tachyarrhythmias; very rarely - nonspecific arrhythmias (including extrasystole), polymorphic ventricular tachycardia (pirouette-type ventricular arrhythmia) or cardiac arrest, mainly in persons with conditions predisposing to arrhythmias, such as clinically significant bradycardia, acute myocardial ischemia.

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

From the digestive system: often - nausea, vomiting, abdominal pain, diarrhea, transient increase in transaminase levels; sometimes - anorexia, constipation, dyspepsia, flatulence, gastroenteritis (except erosive gastroenteritis), increased levels of amylase, bilirubin, liver dysfunction (including increased levels of LDH), increased activity of GGT and alkaline phosphatase; rarely - dysphagia, stomatitis, pseudomembranous colitis (in very rare cases associated with life-threatening complications), jaundice, hepatitis (mainly cholestatic); very rarely - fulminant hepatitis, potentially leading to life-threatening liver failure.

From the central nervous system and peripheral nervous system: often - dizziness, headache; sometimes - confusion, consciousness, disorientation, vertigo, drowsiness, tremor, paresthesia, dysesthesia, sleep disturbances, anxiety, increased psychomotor activity, agitation; rarely - hypoesthesia, pathological dreams, loss of coordination (including gait disturbances due to dizziness, in very rare cases leading to injury due to a fall, especially in elderly patients), seizures with various clinical manifestations (including grand mal seizures), attention disorders, speech disorders, amnesia, emotional lability, depression (in very rare cases, behavior with a tendency to self-harm is possible), hallucinations; very rarely - hyperesthesia, depersonalization, psychotic reactions (potentially manifested in behavior with a tendency to self-harm).

From the senses: sometimes - taste disturbances, visual disturbances (blurredness, decreased visual acuity, diplopia, especially in combination with dizziness and confusion); rarely - tinnitus, impaired sense of smell, including anosmia; very rarely - loss of taste sensitivity.

From the hematopoietic system: sometimes - anemia, leukopenia (including neutropenia), thrombocytopenia, thrombocytosis, prolongation of prothrombin time and decrease in INR; rarely - changes in thromboplastin concentration; very rarely - an increase in the concentration of prothrombin and a decrease in INR, a change in the concentration of prothrombin and INR.

From the musculoskeletal system: sometimes - arthralgia, myalgia; rarely - tendinitis, increased muscle tone and cramps; very rarely - tendon ruptures, arthritis, gait disturbance due to damage to the musculoskeletal system.

From the reproductive system: often - candidal superinfection, vaginitis.

From the urinary system: sometimes - 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 concomitant impaired renal function).

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

Allergic reactions: sometimes - urticaria, itching, rash, eosinophilia; rarely - anaphylactic/anaphylactoid reactions, angioedema, including laryngeal edema (potentially life-threatening); very rarely - anaphylactic shock (including life-threatening).

Metabolism: hyperlipidemia, hyperglycemia, hyperuricemia.

From the body as a whole: sometimes - general malaise (including symptoms of poor health, nonspecific pain and sweating); rarely - swelling.

Storage conditions and periods

List B. Tablets should be stored out of the reach of children, in a dry place at a temperature not exceeding 25°C. Shelf life - 5 years.

List B. Solution for infusion should be stored in a dry place, protected from light and out of reach of children, at a temperature of 8° to 25°C; do not freeze. Shelf life - 5 years.

Indications

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

- acute sinusitis;

— community-acquired pneumonia (including those caused by strains of microorganisms with multiple antibiotic resistance*);

- exacerbation of chronic bronchitis;

- uncomplicated infections of the skin and soft tissues;

- complicated infections of the skin and subcutaneous structures (including infected diabetic foot);

- complicated intra-abdominal infections, including polymicrobial infections, incl. intraperitoneal abscesses;

- uncomplicated inflammatory diseases of the pelvic organs (including salpingitis and endometritis).

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

Contraindications

- pregnancy;

- lactation (breastfeeding);

- children and adolescents up to 18 years of age;

- hypersensitivity to moxifloxacin and other components of the drug.

Use with caution in diseases of the central nervous system (including diseases suspected of involving the central nervous system), predisposing to the occurrence of convulsive seizures and reducing the threshold of convulsive readiness, with prolongation of the QT interval, hypokalemia, bradycardia, acute myocardial ischemia, while taking with drugs that prolong the QT interval, and antiarrhythmic drugs of classes IA and III, for severe liver failure.

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 when such diseases and conditions are suspected.

When using Avelox, some patients may experience prolongation of the QT interval. In this regard, the drug should be avoided in patients with prolongation of the QT interval, hypokalemia, as well as during treatment with class I A (quinidine, procainamide) or class III antiarrhythmic drugs (amiodarone, sotalol), since experience with moxifloxacin in these patients is limited. Avelox® should be prescribed with caution along with drugs that prolong the QT interval (cisapride, erythromycin, antipsychotic drugs, tricyclic antidepressants), as well as in patients with conditions predisposing to arrhythmias, such as bradycardia, acute myocardial ischemia. The degree of QT interval prolongation may increase with increasing drug concentrations, so the recommended dose should not be exceeded. Prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including polymorphic ventricular tachycardia. In patients with pneumonia, there was no correlation between moxifloxacin plasma concentrations and QT interval prolongation. None of the 9,000 patients treated with moxifloxacin experienced QT prolongation-related cardiovascular events or deaths. However, in patients with conditions predisposing to arrhythmias, the risk of developing ventricular arrhythmias may be increased when using moxifloxacin.

During therapy with fluoroquinolones, incl. moxifloxacin, especially in the elderly and patients receiving corticosteroids, tendonitis and tendon rupture may develop. If pain or signs of tendon inflammation occur, stop taking 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 kept in mind if severe diarrhea occurs during treatment with Avelox. In this case, the drug should be discontinued and appropriate therapy should be immediately prescribed.

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

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

Patients of different ethnic groups do not require dose adjustment.

Use in pediatrics

The effectiveness and safety of Avelox® in children and adolescents have not been established.

Impact on the ability to drive vehicles and operate machinery

Despite the fact that moxifloxacin rarely causes adverse reactions from the central nervous system, the question of the ability to drive a car or move machinery is decided individually after assessing the patient’s response to taking the drug.

Experimental results

The following pathological changes are manifestations of the toxic effects of moxifloxacin, as well as other fluoroquinolones: the hematopoietic system (bone marrow hypoplasia in dogs and monkeys), the central nervous system (convulsions in monkeys) and the liver (increased activity of liver enzymes, isolated necrosis of hepatocytes in rats, dogs and monkeys) . These disorders usually occur after a long period of administration of moxifloxacin in high doses.

Use for renal impairment

Patients with impaired renal function (including those with CC<30 мл/мин/1.73 м2), а также пациентам, находящимся на непрерывном гемодиализе и длительном амбулаторном перитонеальном диализе, изменений режима дозирования не требуется

Use for liver dysfunction

Patients with minor liver dysfunction (class A or B on the Child-Pugh scale) do not require changes in the dosage regimen.

Use with caution in severe liver failure.

Avelox– an antibiotic of the fluoroquinol group, active against a number of gram-positive and gram-negative bacteria, as well as chlamydia, mycoplasma, legionella, anaerobic and atypical pathogens, Escherichia coli and Pseudomonas aeruginosa and other infections.

The active substance of the drug Avelox, moxifloxacin, disrupts DNA biosynthesis in microbial cells. When taken orally, the medicine is well absorbed into the blood from the gastrointestinal tract and is evenly distributed throughout the tissues and fluids in the human body.

Indications and contraindications for use

Belonging to the group of antibiotics, Avelox is used in the treatment of many diseases of infectious etiology, such as:

Chronical bronchitis;
pneumonia;
skin infections and soft tissue inflammation;
intra-abdominal abscess;
urogenital infections.

Attention! Avelox is a powerful antibiotic, so only a specialist can recommend it for use, having determined the dosage and methods of taking the drug, taking into account the general condition of the patient, the location and severity of the infectious disease.

Avelox and its analogues should be used exactly following the instructions, without chewing the tablets and drinking a small amount of water. And even if the dosage and rules of administration are observed when treating with Avelox, pronounced side effects may be observed:

dysfunction of the heart (arrhythmia, tachycardia, etc.);
nausea and vomiting;
dizziness and headaches;
fainting conditions;
sleep disorders;
increase and decrease in pressure;
digestive system disorder, etc.

There are a number of contraindications to the use of the drug. These include:

period of pregnancy and lactation;
childhood and adolescence;
hypersensitivity to the components of the drug.

Patients with pathologies of the central nervous system and functional disorders of the liver or kidneys are also advised to take the medicine with caution.

How to replace Avelox?

A significant number of contraindications and the presence of many side effects raise a logical question: what can replace Avelox?

Today, the pharmaceutical industry produces quite a few analogues of Avelox. Thus, along with Avelox, Moxifloxacin belongs to the 4th generation fluoroquinolones. The group of quinolones, introduced into medical practice at the end of the 20th century and having a detrimental effect on a wide range of infectious pathogens, includes:

Vigamox;
Moxin;
Moximac;
Levofloxacin and a number of other drugs.

Based on the fact that all the indicated drugs act approximately the same, they have similar contraindications and side complications. It should also be noted that both Avelox and all analogues of the drug are not cheap and have approximately the same cost. In this regard, when If there are serious contraindications and troubling complications, you should consult your doctor with a request to replace Avelox or one of its analogues with an antibiotic belonging to a different pharmaceutical group.

Experts recommend that if you have chronic diseases of the digestive system, do not use antibiotic tablets, but purchase an infusion solution for intravenous injection to prevent exacerbation of the underlying disease. Ciprofloxacin, available as eye drops, is used to treat severe eye infections. In case of mycoplasma, with the permission of the attending physician, Avelox can be replaced with Doxycycline monohydrate.