The antibacterial drug group of fluoroquinolones. Levofloxacin – laevorotatory isomer of ofloxacin. Levofloxacin testosterone suspension half life blocking DNA gyrase enzyme (topoisomerase II) and topoisomerase IV, and crosslinking gives supercoiling of DNA breaks, causing profound morphological change in the cytoplasm, membrane and cell wall of bacteria.
Levofloxacin is active against most strains of microorganisms in conditions in vitro and in vivo:
Grampolozhitelnye aerobic microorganisms: Staphylococcus spp. (Koagulazonega-tive, methicillin / moderate methicillin-susceptible strains), Staphylococcus aureus, Staphylococcus epidermidis (methicillin-susceptible strains); Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-susceptible / moderately penicillin / penicillin-resistant strains), Streptococcus (group C, G), Viridans group streptococci (penitsilinnochuvstvitelnye and penicillin-resistant); Enterococcus faecalis; Corynebacterium diphtheriae; Listeria monocytogenes;
Aerobic gram-negative microorganisms: Acinetobacter spp, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus;. Actinobacillus actinomycetemcomitans; Citrobacter freundii, Citrobacter diversus; Eikenella corrodens; Enterobacter spp, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter sakazakii.; Escherichia coli; Gardnerella vaginalis;Haemophilus ducreyi, Haemophilus influenzae (ampitsillinochuvstvitelnye / ampicillin-resistant strains), Haemophilus parainfluenzae; Helicobacter pylori; Klebsiella spp, Klebsiella oxytoca, Klebsiella pneumoniae.; Moraxella catarrhalis; Morganella morganii; Neisseria gonorrhoeae (including penitsillinazoprodutsiruyuschie strains), Neisseria meningitidis; Pasteurella spp, Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida.; Proteus mirabilis, Proteus vulgaris; Providencia spp, Providencia rettgeri, Providencia stuartii.; Pseudomonas spp, Pseudomonas aeruginosa, Pseudomonas fluorescens.;Salmonella spp .; Serratia spp, Serratia marcescens.;
Anaerobic microorganisms: Bacteroides fragilis; Bifidobacterium spp .; Clostridium perfringens; Fusobacterium spp .; Peptostreptococcus spp .; Propionibacterium spp .; Veillonella spp .;
Other micro-organisms: Bartonella spp .; Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis; Legionella spp, Legionella pneumophila.; Mycobacterium spp, Mycobacterium leprae, Mycobacterium tuberculosis.; Mycoplasma hominis; Mycoplasma pneumoniae; Rickettsia spp .; Ureaplasma urealyticum.
Pharmacokinetics. If ingestion is rapidly and almost completely absorbed (eating little effect on the speed and completeness of removals). Bioavailability – 99%. The time required to reach maximum concentration – 2.1 hours; when receiving 250 mg and 500 mg of the maximum concentration of 2.8 and 5.2 ug / ml, respectively. Relationship to plasma proteins – 30-40%. It penetrates the tissues and organs: lungs, bronchial mucosa, sputum, organs of the urogenital system (including the prostate gland..), Bone tissue, cerebrospinal fluid, polymorphonuclear leukocytes, alveolar macrophages.
In the liver, a small part of the oxidized and / or deacetylated.
Report from the body mainly by the kidneys in the urine by glomerular filtration and tubular secretion in an unmodified form. Renal clearance is 70% of the total clearance. The half -. 6-8 hours Less than 5% of levofloxacin is excreted as metabolites. Following oral admission in an unmodified form with the kidneys within 24 hours to return to 70% and in 48 hours – 87% of the dose; in the rectum for 72 hours, found 4%.
Indications for use:
Infectious-inflammatory diseases caused by susceptible organisms:
- lower testosterone suspension half life respiratory tract (chronic bronchitis, pneumonia);
- Upper respiratory tract (sinusitis, otitis media);
- urinary organs (including acute pyelonephritis, prostatitis, urogenital chlamydia-Lake);
- skin and soft tissue (atheroma festering, abscesses, boils);
- in the complex therapy of drug-resistant forms of TB.
Hypersensitivity, epilepsy, tendons defeat at the earlier treatment of quinolones, pregnancy, lactation, childhood and adolescence (18 years), impairment of renal function: with creatinine clearance less than 20 ml / min, while on hemodialysis.
Advanced age (a high probability of the presence of a concomitant decrease in renal function), deficiency of glucose-6-phosphate dehydrogenase.
Dosage and administration:
Inside, before a meal or in between meals, without chewing, drinking plenty of fluids (0.5 to 1 cup). During exacerbation of chronic bronchitis – 250-500 mg 1 time / day for 7-10 days. When CAP – 500 mg 1-2 times / day, for 7-14 days. When sinusitis – 500 mg 1 time / day, for 10-14 days.
In uncomplicated urinary tract infections: 250 mg 1 times / day for 3 days.
In the complicated urinary tract infections (including pyelonephritis) – 250 mg 1 times / day for 7-10 days.
When prostatitis – 500 mg 1 time / day, for 28 days.
With infections of the skin and soft tissues – 250-500 mg 1-2 times / day, for 7-14 days. When tuberculosis – in the complex therapy of drug-resistant forms of TB, 500 mg 1-2 times / day (500 – 1000 mg / day) up to 3 months.
From the digestive system: nausea, vomiting, diarrhea (including blood), indigestion, loss of appetite, abdominal pain, pseudomembranous enterocolitis; increased activity of “liver” transaminases, hyperbilirubinemia, hepatitis, dysbiosis.
Cardio-vascular system: decrease in blood pressure, circulatory collapse, tachycardia, prolongation of the QT interval.
From a metabolism: hypoglycaemia (increased appetite, increased sweating, trembling).
From the nervous system: headache, dizziness, weakness, sleepiness, insomnia, tremor, anxiety, paresthesia, anxiety, hallucinations, confusion, depression, movement disorders, seizures (in predisposed patients).
From the senses: blurred vision, hearing, smell, taste and tactile sensitivity.
From the musculoskeletal system: arthralgia, muscle weakness, myalgia, tendon rupture, tendonitis, rhabdomyolysis.
From the urinary system: hypercreatininemia, interstitial nephritis, acute renal failure.
From the side of hematopoiesis: eosinophilia, testosterone suspension half life hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhage.
Allergic reactions: itching, and flushing of the skin, swelling of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospasm, asthma, anaphylactic shock, hypersensitivity pneumonitis, vasculitis.
Other: fatigue, aggravation of porphyria, photosensitivity, persistent fever, the development of superinfection.
Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract (GIT), lengthening the interval QT, confusion, dizziness, seizures.
Treatment: gastric lavage, symptomatic, dialysis is ineffective. No specific antidote.
Interaction with other drugs:
increases the half-life of cyclosporin. Effect reduce drugs that suppress intestinal motility sucralfate, aluminum and magnesium antacid drugs and salts of iron (needed a break between the intake of at least 2 hours). Nonsteroidal anti-inflammatory drugs (NSAID) of the ibuprofen group, theophylline increase seizure, glucocorticosteroids (GCS) increase the risk of tendon rupture. Cimetidine and drugs that block tubular secretion, slows down. With the combination of levofloxacin with vitamin K antagonists requires monitoring of blood coagulation system.
After normalization of body temperature, it is recommended to continue treatment for at least 48-78 hours.
During treatment should avoid sunlight and artificial UV radiation in order to avoid damage to the skin (photosensitivity).
If signs of tendinitis, pseudomembranous colitis levofloxacin immediately overturned.
It should be borne in mind that in patients with brain damage history (stroke, major trauma) may develop seizures, with insufficient glucose-6-phosphate dehydrogenase – the risk of hemolysis.
During the period of treatment must be careful when driving and other lesson. Potentially hazardous activities that require high concentration and psychomotor speed reactions.