Pharmacological effect of Vigamox Eye Drops
Vigamox Eye Drops Antimicrobial agents of the fluoroquinolones, acts bactericidal. Is active against a broad spectrum 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 – Haemophilus influenzae (including both producing as well and not producing beta-lactamase strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including both producing and non-producing beta-lactamase strains), Escherichia coli, Enterobacter cloacae; atypical – Chlamydia pneumoniae, Mycoplasma pneumoniae. According to studies in vitro, although the following microorganisms are susceptible to moxifloxacin, however the safety and efficacy of its treatment of infections has not been established. Gram-positive microorganisms: Streptococcus milleri, Streptococcus mitior, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohnii, Staphylococcus epidermidis (including strains that are 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 organisms: Legionella pneumophila, Caxiella burnettii.
Blocks topoisomerase II and IV, enzymes that control the topological properties of DNA, and participating in replication, repair and transcription of DNA. Effect of moxifloxacin depends on its concentration in the blood and tissues. Minimum bactericidal concentrations do not differ much from the minimum inhibitory concentration.
Mechanisms of resistance that inactivate penicillins, cephalosporins, aminoglycosides, macrolides, tetracyclines, and do not affect the antibacterial activity of moxifloxacin. Cross-resistance between moxifloxacin and these drugs is absent. Plasmid-mediated mechanism of resistance 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 series of successive mutations. With repeated exposure to microorganisms moxifloxacin subminimalnyh inhibitory concentration only slightly increased rates of the IPC. Between preparations of the fluoroquinolones observed cross-resistance. However, some gram-positive and anaerobic organisms that are resistant to other fluoroquinolones, are sensitive to moxifloxacin.
Pharmacokinetics Vigamox Eye Drops
After oral administration, moxifloxacin is absorbed rapidly and almost completely. After a single dose of moxifloxacin 400 mg Cmax in the blood is reached within 0.5-4 h and is 3.1 mg / liter.
After a single infusion at a dose of 400 mg over 1 h Cmax achieved at the end of infusion of 4.1 mg / l, which corresponds to its increase by approximately 26% compared with the value of this indicator if swallowed. When multiple IV infusion at a dose of 400 mg, duration 1 h Cmax ranges from 4.1 mg / l to 5.9 mg / liter. Mean Css, equal to 4.4 mg / l, achieved at the end of infusion.
The absolute bioavailability of approximately 91%.
Pharmacokinetics of moxifloxacin at a reception in single doses from 50 mg to 1200 mg and a dose of 600 mg / day. within 10 days is linear.
The equilibrium state is reached within 3 days.
Binding to blood proteins (mainly albumin) is about 45%.
Moxifloxacin rapidly distributed in tissues and organs. Vd is approximately 2 l / kg.
High concentrations of moxifloxacin, higher than those in plasma, created in lung tissue (including alveolar macrophages) in the bronchial mucosa in the sinuses, soft tissue, skin and subcutaneous structures, foci of inflammation. In the interstitial fluid and saliva drug is determined in a free, not protein-bound form, in concentrations higher than in plasma. In addition, high concentrations of the active substance are determined in the abdominal cavity and peritoneal fluid and in tissues of female genital mutilation.
Biotransformed to inactive sulfosoedineny and glucuronides. Moxifloxacin does not Biotransformation liver enzymes of cytochrome P450.
After passing the second phase of biotransformation of moxifloxacin is excreted by the kidneys and through the intestine as unchanged and as inactive sulfosoedineny and glucuronides.
Excreted in the urine and the faeces as unchanged and as inactive metabolites. When a single dose of 400 mg of approximately 19% is excreted unchanged in urine, about 25% – with the feces. T1 / 2 of approximately 12 h. The average total body clearance after taking a dose of 400 mg from 179 ml / min to 246 ml / min.
Indications Vigamox Eye Drops
Infections of the upper and lower respiratory tract: Acute sinusitis, exacerbation of chronic bronchitis, community-acquired pneumonia, skin infections and soft tissue.
Dosing regimen
Inside, 400 mg 1 time per day. The course of treatment during exacerbations of chronic bronchitis – 5 days, pneumonia – 10 days, acute sinusitis, infections of the skin and soft tissue – 7 days.
Side effects of Vigamox Eye Drops
From the digestive system: abdominal pain, nausea, diarrhea, vomiting, dyspepsia, flatulence, constipation, elevated liver enzymes, taste perversion.
CNS and peripheral nervous system: dizziness, insomnia, nervousness, anxiety, fatigue, headache, tremor, paresthesia, pain in legs, cramps, confusion, depression.
Cardio-vascular system: tachycardia, peripheral edema, increased blood pressure, palpitations, chest pain.
From the laboratory indicators: reduction in prothrombin time, increased amylase activity.
From the hemopoietic system: leukopenia, eosinophilia, thrombocytosis, thrombocytopenia, and anemia.
From the musculoskeletal system: back pain, arthralgia, myalgia.
From the sexual system: vaginal candidiasis, vaginitis.
Allergic reactions: rash, itching, hives.
Contraindications
Childhood and adolescence to 18 years, pregnancy, lactation (lactation), increased sensitivity to moxifloxacin.
Application of pregnancy and breastfeeding
Moxifloxacin is contraindicated in pregnancy and lactation (breastfeeding).
Cautions
With carefully administered moxifloxacin in the epileptic syndromes (including history), epilepsy, liver failure, syndrome prolongation QT.
During fluoroquinolone therapy may develop inflammation and tendon rupture, especially in elderly patients and in patients concurrently receiving corticosteroids. At the first sign of pain or inflammation of tendons, patients should discontinue treatment and release of the load affected limb.
Drug Interactions
With the 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 (the simultaneous reception is possible at intervals of 4 hours before or 2 hours after taking moxifloxacin).
When receiving moxifloxacin against the use of other fluoroquinolones may develop phototoxic reactions.
Ranitidine reduces the absorption of moxifloxacin.
