Levofloxacin 500 mg
Active substance: levofloxacin 500 mg (in the form of hemihydrate).
Floxaval – is a strong antimicrobial drug from the group of fluoroquinalones of the 3rd generation.
Pharmachologic effect
Levofloxacin is a broad-spectrum antimicrobial bactericidal agent from the group of fluoroquinolones. It blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts superspiralization and cross-linking of DNA breaks, inhibits DNA synthesis, causes deep morphological changes in the cytoplasm, cell wall and membranes of bacteria.
Sensitive to the drug in vitro
Aerobic gram-positive microorganisms:
Corynebacterium diphtheria, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing, coagulase-negative strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Streptococcus spp. Groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-susceptible/moderately sensitive/resistant strains), Streptococcus pyogenes, Streptococcus spp. Groups of viridans (penicillin-susceptible/resistant strains).
Aerobic grammatical microorganisms:
Acinetobacter spp. (including Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenza (ampicillin-sensitive/resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella pylori spp. (including producing and non-producing beta-lactamase strains), Morganella morganii, Neisseria gonorrhoeae (including producing and non-producing penicillinase strains), Neisseria meningitides, Pasteurella spp. (including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Salmonella spp., Seratia spp. (including Serratia marcescens).
Anaerobic microorganisms:
Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spa., Propionibacterium spp., Veilonella spp.
Other microorganisms:
Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Mycrobacterium spp. (including Mycrobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pmneumoniae, Ricketsia spp., Ureaplasma urealyticum.
Moderately sensitive microorganisms
Aerobic gram-positive microorganisms:
Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains).
Aerobic gram-negative microorganisms:
Burkholderia cepacia, Campylobacter jejuni, Campylobacter coli.
Anaerobic microorganisms:
Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.
Resistant gram-positive organisms:
Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp (coagulase-negative methicillin-resistant strains).
Aerobic gram-negative microorganisms:
Alcaligenes xylosoxidans.
Other microorganisms:
Mycobacterium avium
Pharmacokinetics
When taken orally, levofloxacin is rapidly and almost completely absorbed (food intake has little effect on the rate and completeness of absorption). Bioavailability -99%. The time to reach Cmax in blood plasma is 1-2 hours; when taking 250 and 500 mg Cmax in plasma is about 2.8 and 5.2 μg / ml, respectively. Communication with plasma proteins – 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages. In the liver, a small part is oxidized and/or deacetylated. Renal clearance is 70% of the total clearance. T1 / 2-8 h. Excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. 70% is excreted unchanged by the kidneys within 24 hours and 87% in 48 hours; 4% of the oral dose of levofloxacin is excreted by the intestines in 72 hours.
Floxaval indications
Infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin, incl.
Contraindications for use
Hypersensitivity to levofloxacin and other fluoroquinolones, epilepsy, tendon damage with previous treatment with quinolones, pregnancy, breastfeeding, childhood and adolescence (up to 18 years).
Carefully
Older age (high probability of having a concomitant decrease in kidney function), deficiency of glucose-6-phosphate dehydrogenase.
Dosing regimen
The drug is taken orally once or twice a day. Do not chew the tablets and take a sufficient amount of liquid (from 0.5 to 1 glass), you can take it before drinking or between meals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen.
For patients with normal or moderately reduced renal function (creatinine clearance> 50 ml / min), the following dosing regimen is recommended:
Acute bacterial sinusitis: 500 mg once a day for 10-14 days.
Exacerbation of chronic bronchitis: 500 mg once a day – 7-10 days.
Uncomplicated urinary tract infections: 500 mg once a day for 3 days.
Chronic bacterial prostatitis: 500 mg – 1 time per day – 28 days.
Complicated urinary tract infections, including pyelonephritis: 500 mg once a day – 7-10 days.
Infections of the skin and soft tissues: 500 mg 1-2 times a day – 7-14 days.
Intra-abdominal infection: 500 mg 1 time per day – 7-14 days (in combination with antibacterial drugs acting on the anaerobic flora).
For tuberculosis (as part of complex therapy) – 500 mg 1-2 times a day, the course of treatment is up to 3 months.
Clinical trials of levofloxacin in skin and subcutaneous tissue infections.
| Author and year. | Type of infection | Study drug and dosage | Duration of therapy | Clinical cure rate | Bacteriological cure rate |
| Tarshis et al. 2001 | Uncomplicated | Levofloxacin 500 mg orally daily | for 7–10 days | 84% | 84% |
| Nichols et al. 1997 | Uncomplicated | Levofloxacin 500 mg orally daily | for 7-10 days | 98% | 98% |
| Graham et al., 2002 | Complicated
|
Levofloxacin 750 mg intravenous/oral daily | for 7-14 days | 84% | 91% |
Forms of admission: 10 tablets per pack.
Manufacturer: Delorbis Pharmaceuticals LTD, Cyprus.
Distributor: DEMI PHARM LLC, Yerevan, Armenia