Moxifloxacin Canon, 400 mg 5 pcs

An antimicrobial agent of the group of fluoroquinolones, acts bactericidally. It is active against a wide range of Gram-positive and Gram-negative microorganisms, anaerobic, acid-resistant and atypical bacteria: Mycoplasma spp., Chlamydia spp., Legionella spp.

Effective against bacterial strains resistant to beta-lactams 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-producing strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including both beta-lactamase producing and non-producing strains), Escherichia coli, Enterobacter cloacae; atypical – Chlamydia pneumoniae, Mycoplasma pneumoniae. According to studies in vitro, although the microorganisms listed below are sensitive to moxifloxacin, its safety and efficacy in the treatment of infections has not been established.

Gram-positive microorganisms: Streptococcus milleri, Streptococcus mitior, 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 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.

Blocks topoisomerases II and IV, enzymes controlling the topological properties of DNA and involved in DNA replication, repair and transcription. Action of moxifloxacin depends on its concentration in blood and tissues. Minimum bactericidal concentrations are almost indistinguishable from minimum suppressive concentrations.

The mechanisms of resistance development inactivating penicillins, cephalosporins, aminoglycosides, macrolides and tetracyclines do not affect the antibacterial activity of moxifloxacin. There is no cross-resistance between moxifloxacin and these drugs.

The plasmid-mediated mechanism of resistance development was not observed. The overall incidence of resistance development is low. In vitro studies have shown that resistance to moxifloxacin develops slowly as a result of a series of sequential mutations. When repeated exposure of microorganisms to moxifloxacin in subminimal suppressive concentrations only a slight increase in IPC.

There is cross-resistance between drugs from the group of fluoroquinolones. However, some gram-positive and anaerobic microorganisms resistant to other fluoroquinolones are sensitive to moxifloxacin.

Pharmacokinetics

After oral administration moxifloxacin is absorbed rapidly and almost completely. 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 a single infusion of a dose of 400 mg for 1 hour the C_max is reached at the end of infusion and is 4.1 mg/l, which corresponds to its increase by approximately 26% compared to the value of this parameter when administered orally. For multiple intravenous infusions at a dose of 400 mg lasting 1 h, C_max ranges in the range of 4.1 mg/L to 5.9 mg/L. Average C_ss, equal to 4.4 mg/L, is reached at the end of the infusion.

The 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.

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

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

High concentrations of moxifloxacin, higher than those in plasma are formed in the lung tissue (including alveolar macrophages), the mucous membrane of the bronchi, the sinuses, soft tissues, skin and subcutaneous structures, inflammation foci. In interstitial fluid and in saliva the drug is determined in free, not bound to proteins, in concentrations higher than in 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 reproductive organs.

It is biotransformed to inactive sulfonic compounds and glucuronides. Moxifloxacin is not biotransformed by liver microsomal enzymes of cytochrome P450 system.

After passing the second phase of biotransformation moxifloxacin is excreted by the kidneys and through the intestine both as unchanged and in the form of inactive sulfonic compounds and glucuronides.

Extracted in the urine as well as in the feces both unchanged and as inactive metabolites. At a single dose of 400 mg, about 19% is excreted unchanged in the urine, about 25% in the feces. T_1/2 is approximately 12 h. Mean total clearance after administration at a dose of 400 mg is between 179 ml/min to 246 ml/min.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

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

When using moxifloxacin against the background of other fluoroquinolones phototoxic reactions are possible.

Ranitidine decreases absorption of moxifloxacin.

Special Instructions

Contraindications

Children and adolescents under 18 years of age, pregnancy, lactation (period of breast-feeding), hypersensitivity to moxifloxacin.

With caution moxifloxacin is prescribed in liver failure.

The use in elderly patients

During therapy with fluoroquinolones, inflammation and tendon rupture may develop in elderly patients. At the first signs of pain or tendon inflammation patients should discontinue treatment and relieve the affected limb from stress.

Side effects

Digestive system disorders: abdominal pain, nausea, diarrhea, vomiting, dyspepsia, flatulence, constipation, increased liver transaminase activity, perversion of taste.

CNS and peripheral nervous system disorders: dizziness, insomnia, nervousness, anxiety, asthenia, headache, tremor, paresthesia, leg pain, seizures, confusion, depression.

Cardiovascular system: tachycardia, peripheral edema, increased BP, palpitations, chest pain.

Laboratory findings: decreased prothrombin levels, increased amylase activity.

Hematopoietic system disorders: leukopenia, eosinophilia, thrombocytosis, thrombocytopenia, anemia.

Muscular system disorders: back pain, arthralgia, myalgia.

Perior genital system disorders: vaginal candidiasis, vaginitis.

Allergic reactions: rash, itching, urticaria.

Overdose

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