Description of the active substance:
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Antimicrobial agent from the group of fluoroquinolones, acts bactericidal. It is active 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-lactams and macrolides. It is active against most strains of microorganisms: gram-positive strains - Staphylococcus aureus (including strains susceptible to methicillin), Streptococcus pneumoniae (including strains resistant to penicillin and macrolides), Streptococcus pyogenes (group A); gram-negative - Haemophilus influenzae (including both producing and not producing beta-lactamase strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including both producing and not producing beta-lactamase strains), Escherichia coli, Enterobacter cloacae; atypical - Chlamydia pneumoniae, Mycoplasma pneumoniae. According to in vitro studies, although the microorganisms listed below are sensitive to moxifloxacin, nevertheless, safety and efficacy in the treatment of infections have not been established. Gram-positive organisms: Streptococcus milleri, Streptococcus mitior, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohnii, Staphylococcus epidermidis ( including strains, methicillin sensitive), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae. Gram-negative microorganisms: Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter Intermedius, Enterobacter sakazaki, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii. Anaerobic microorganisms: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaornicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevotella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum. Atypical microorganisms: Legionella pneumophila, Caxiella burnettii.
It blocks topoisomerases II and IV, enzymes that control the topological properties of DNA, and participate in replication, repair and transcription of DNA. The effect of moxifloxacin depends on its concentration in the blood and tissues. The minimum bactericidal concentrations almost do not differ from the minimum suppressing concentrations.
Mechanisms of development of resistance, inactivating penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines, do not affect the antibacterial activity of moxifloxacin. Cross-resistance between moxifloxacin and these drugs is absent. Plasmid-mediated mechanism of resistance development was not observed.The overall incidence of resistance is low. In vitro studies have shown that resistance to moxifloxacin develops slowly as a result of a number of consecutive mutations. With repeated exposure to microorganisms with moxifloxacin in submminimal inhibitory concentrations, the MIC is only slightly increased. Between the drugs from the group of fluoroquinolones cross resistance is observed. However, some Gram-positive and anaerobic microorganisms resistant to other fluoroquinolones are susceptible to moxifloxacin.
After oral administration, moxifloxacin is absorbed quickly and almost completely. After a single dose of moxifloxacin 400 mg C max in the blood is reached within 0.5-4 h and is 3.1 mg / l.
After a single infusion 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 index when taken orally. With multiple IV infusions in a dose of 400 mg for 1 h, C max varies in the range from 4.1 mg / l to 5.9 mg / l. Mean C ss , equal to 4.4 mg / l, are achieved at the end of the infusion.
Absolute bioavailability is about 91%.
The pharmacokinetics of moxifloxacin when administered in single doses of 50 mg to 1200 mg, and at a dose of 600 mg / day for 10 days is linear.
The equilibrium state is reached within 3 days.
Binding to blood proteins (mainly with albumins) 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 alveolar macrophages), in bronchial mucosa, in nasal sinuses, in soft tissues, skin and subcutaneous structures, foci of inflammation. In the interstitial fluid and in the saliva, the drug is determined in a free, non-protein-binding form at a concentration higher than in the plasma. In addition, high concentrations of the active substance 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. Moxifloxacin is not biotransformed with microsomal liver enzymes of the cytochrome P450 system.
After passing the 2nd phase of biotransformation, moxifloxacin is excreted from the body by the kidneys and through the intestine both in unmodified form and in the form of inactive sulfo compounds and glucuronides.
It is excreted in the urine, as well as with feces, both in unmodified form and in the form of inactive metabolites. At a single dose of 400 mg, about 19% is excreted unchanged in the urine, about 25% - with feces. T 1/2 is approximately 12 hours. The average total clearance after taking in a dose of 400 mg is from 179 ml / min to 246 ml / min.
Infections of the upper and lower respiratory tract: acute sinusitis, exacerbation of chronic bronchitis, community-acquired pneumonia; infections of the skin and soft tissues.
Inside, 400 mg 1 time / day. The course of treatment for exacerbation of chronic bronchitis - 5 days, community-acquired pneumonia - 10 days, acute sinusitis, skin and soft tissue infections - 7 days.
On the part of the digestive system: abdominal pain, nausea, diarrhea, vomiting, indigestion, flatulence, constipation, increased activity of liver transaminases, perversion of taste.
From the central nervous system and peripheral nervous system: dizziness, insomnia, nervousness, anxiety, asthenia, headache, tremor, paresthesia, leg pain, convulsions, confusion, depression.
From the cardiovascular system: tachycardia, peripheral edema, increased blood pressure, palpitation, chest pain.
On the part of laboratory indicators: a decrease in the level of prothrombin, an increase in the activity of amylase.
On the part of the hematopoiesis system: leukopenia, eosinophilia, thrombocytosis, thrombocytopenia, anemia.
From the musculoskeletal system: back pain, arthralgia, myalgia.
On the part of the reproductive system: vaginal candidiasis, vaginitis.
Allergic reactions: rash, itching, hives.
Children and adolescence under 18, pregnancy, lactation (the period of breastfeeding), hypersensitivity to moxifloxacin.
PREGNANCY AND LACTATION
Moxifloxacin is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution is prescribed moxifloxacin in liver failure.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
During therapy with fluoroquinolones, inflammation and rupture of the tendon can develop in elderly patients. At the first signs of pain or inflammation of the tendons, patients should stop treatment and release the affected limb from loading.
Caution is prescribed moxifloxacin in case of epileptic syndrome (including in the anamnesis), epilepsy, hepatic insufficiency, syndrome of prolongation of the QT interval.
During therapy with fluoroquinolones, inflammation and rupture of the tendon can develop, especially in elderly patients and in patients receiving concomitant GCS.At the first signs of pain or inflammation of the tendons, patients should stop treatment and release the affected limb from loading.
With simultaneous use of antacids, minerals, multivitamins impair absorption (due to the formation of chelate complexes with polyvalent cations) and reduce the concentration of moxifloxacin in plasma (simultaneous reception is possible with an interval of 4 hours before or 2 hours after taking moxifloxacin).
When taking moxifloxacin against the background of the use of other fluoroquinolones, the development of phototoxic reactions is possible.
Ranitidine reduces the absorption of moxifloxacin.