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Active ingredients
Levofloxacin
Release form
Pills
Composition
Active ingredient: Levofloxacin (Levofloxacinum) Active ingredient concentration (mg): 500
Pharmacological effect
Levofloxacin is a broad spectrum antimicrobial anti-bactericide drug, blocks dyn-gyrase and topoisomerase IV, inhibits DNA synthesis active in respect of aerobic gram-positive microorganisms, enterococcus faecalis, staphylococcus aureus (strains of methicillin, culture, and tissue, stroke, etc. , staphylococcus saprophyticus, streptococcus c and g groups, streptococcus agalactiae, streptococcus pneumoniae, streptococcus pyogenes; Aerobic Gram-negative Microorganisms: acinetobacter baumannii, citrobacter freundii, eikenella corrodens, enterobacter aerogenes, enterobacter agglomerans, enterobacter cloacae, escherichia coli, haemophilus influenzae, haemophilus parainfluenzae, klebsiella oxytoca, klebsiella pneumoniae, moraxella catarrhalis, morganella morganii, pasteurella multocida, proteus mirabilis, proteus vulgaris, providencia rettgeri, providencia stuartii, pseudomonas aeruginosa, serratia marcescens; anaerobic microorganisms: bacteroides fragilis, clostridium perfringens, peptostreptococcus spp .; other microorganisms: chlamydia pneumoniae, chlamydia psittaci, legionella pneumophila, mycoplasma pneumoniae. aerobic gram-positive microorganisms are intermediately sensitive to the preparation: staphylococcus haemolyticus (methicillin-resistant strains); aerobic gram-negative microorganisms: burkholderia cepacia; anaerobic microorganisms: bacteroides ovatus, bacteroides thetaiotamicron, bacteroides vulgatus, clostridium difficile. staphylococcus aureus (methicillin-resistant strains) are insensitive to levofloxacin.
Pharmacokinetics
When ingested, levofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability of the drug is approximately 100%. Cmax in plasma is achieved within 1 hour. Food intake has practically no effect on the absorption of levofloxacin. Distribution: Plasma protein binding is 30-40%. Cumulation of levofloxacin when taken in a dose of 500 mg 1 time / day is practically not observed. A slight cumulation of levofloxacin is observed when taken in a dose of 500 mg 2 times / day. Css is reached within 3 days. When ingested, levofloxacin at a dose of 500 mg Cmax in the bronchial mucosa and bronchial secretion is reached approximately 1 hour after taking the drug and is 8.3 mcg / ml and 10.8 mcg / ml, respectively; Cmax in the lung tissue is reached 4-6 hours after taking the drug and is approximately 11.3 mcg / ml. Concentrations in the lungs exceed plasma concentrations. Levofloxacin poorly penetrates into the cerebrospinal fluid. The average concentration of the drug in the urine after 8-12 hours after taking single doses of 150 mg, 300 mg or 500 mg is 44 mg / l, 91 mg / l and 200 mg / l, respectively. Metabolism Levofloxacin is metabolized to a slight degree with the formation of desmethyl-levofloxacin and levofloxacin-N-oxide.The share of these metabolites accounts for less than 5% of the dose excreted through the kidneys. Withdrawal As a result of ingestion, levofloxacin is excreted from the plasma relatively slowly (T1 / 2 - 6-8 hours). The excretion of the drug is mainly carried out by the kidneys (> 85% of the administered dose). Pharmacokinetics in special clinical situations. Impaired renal function affects the pharmacokinetics of levofloxacin. The excretion through the kidneys decreases with a decrease in kidney function and, accordingly, T1 / 2 increases, as shown in the table below. The pharmacokinetics of levofloxacin in elderly patients have no significant differences, except for those associated with changes in creatinine clearance.
Indications
Infections caused by susceptible strains of microorganisms: - infections of upper respiratory tract (acute sinusitis); - infections of the lower respiratory tract (acute bronchitis, chronic bronchitis, community-acquired pneumonia); - uncomplicated urinary tract and kidney infections; - complicated urinary tract infections and kidneys (including pyelonephritis); - prostatitis; - infections of the skin and soft tissues.
Contraindications
Epilepsy; - tendon lesions that occurred during the previous treatment with fluoroquinolones; - children and adolescents under 18 years; - pregnancy; - lactation (breastfeeding); - hypersensitivity to levofloxacin or other quinolones, and / or to other components of the drug. Caution must be exercised: - when prescribing levofloxacin in combination with drugs that affect tubular secretion, such as probenecid and cimetidine, especially in the treatment of patients with impaired renal function; - in the treatment of patients with predras position to epileptic seizures, during treatment with fenbufen and similar non-steroidal anti-inflammatory drugs (NSAIDs) or drugs that reduce the threshold of epileptic seizures, such as theophylline; development of hemolytic reactions.
Precautionary measures
The drug should be stored out of the reach of children at a temperature not higher than 25 ° C.
Use during pregnancy and lactation
The drug is contraindicated during pregnancy and during breastfeeding.
Dosage and administration
Tablets should be taken orally 1 or 2 times / day, regardless of the meal, not chewed and squeezed with a sufficient amount of liquid. The dose of the drug and the duration of treatment depend on the indication for use and the severity of the disease. When selecting doses, the pill can be divided into parts according to the separation risk. Treatment with Flexid should last at least another 48-72 hours after the disappearance of the symptoms of the disease. The maximum duration of treatment is not more than 14 days. Doses for patients with normal renal function (CC> 50 ml / min)
Side effects
Allergic reactions: not common - itching, skin rash; rare - urticaria, bronchospasm, shortness of breath; very rare - angioedema, hypotension, anaphylactic shock, allergic pneumonitis, photosensitization; in some cases - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), erythema multiforme. From the alimentary system and metabolism: common - nausea, diarrhea (including with blood), increased activity of liver enzymes (ALT AST); not common - loss of appetite, vomiting, abdominal pain, dyspepsia, hyperbilirubinemia; rare - enterocolitis; very rare - hypoglycemia, hepatitis, pseudomembranous colitis. From the nervous system: not common - headache, dizziness, sleep disturbance; rare - paresthesias, tremor, anxiety, agitation, confusion, convulsions; very rare - hallucinations, extrapyramidal disorders and other coordination disorders. From the sense organs: very rare - visual, hearing, smell, taste and tactile sensations. From the cardiovascular system: rare - tachycardia, hypotension; very rare - vascular collapse. From the side of the musculoskeletal system: rare - arthralgia, myalgia, tendonitis; very rare - tendon rupture (for example, Achilles tendon), muscle weakness (is of particular importance for patients with myasthenia); in some cases - rhabdomyolysis. From the urinary system: non-prevalent - hypercreatininemia; very rare - interstitial nephritis, deterioration of renal function up to acute renal failure. On the side of the blood system and hematopoietic organs: non-prevalent - eosinophilia, leukopenia; rare - neutropenia, thrombocytopenia; very rare - agranulocytosis; in some cases - hemolytic anemia, pancytopenia. Other: non-prevalent - asthenia; very rare - fever, vasculitis.
Overdose
Symptoms: nausea, erosion of the mucous membranes of the gastrointestinal tract, confusion, dizziness, loss of consciousness and convulsions. Treatment: symptomatic therapy is carried out, monitoring of ECG parameters. Hemodialysis is ineffective. There is no specific antidote.
Interaction with other drugs
Iron salts, antacids containing magnesium or aluminum, reduce the absorption of levofloxacin. Sucralfate reduces the bioavailability of levofloxacin. There is no pharmacokinetic interaction between levofloxacin and theophylline. However, with the concomitant use of quinolones and theophylline and NSAIDs, the threshold of convulsive readiness may decrease. In the presence of fenbufen, the concentration of levofloxacin is about 13% higher than when it is used as a monotherapy. taking levofloxacin and vitamin K antagonists (warfarin), an increase in blood clotting parameters (prothrombin time) and / or bleeding is observed.
special instructions
Flexid pills should be taken 2 hours before or 2 hours after taking iron salts, antacids and sucralfate, since there may be a decrease in its absorption. If necessary, the simultaneous use of sucralfate should be taken 2 hours after taking Flexid. In patients simultaneously taking vitamin K antagonists, it is necessary to control blood clotting parameters. In rare cases that tendinitis observed during quinolone treatment can sometimes lead to rupture of ligaments, especially Achilles tendons. This side effect occurs within 48 hours after initiation of therapy. For older people and patients taking GCS, there is an increased risk of tendinitis. Therefore, during treatment with levofloxacin, careful monitoring of the condition of such patients is necessary. If there is a suspicion of tendonitis (it is necessary to inform patients about its symptoms), taking Flexid should be immediately stopped and appropriate treatment should be started (for example, immobilization). Diarrhea (especially in cases of severe, persistent and / or mixed with blood) during or after taking the drug Flexid can be a symptom of a disease caused by Clostridium difficile, the most severe form of which is pseudomembranous colitis.If pseudomembranous colitis is suspected, taking Flexid should be stopped immediately and symptomatic treatment should be administered (for example, vancomycin orally). In this state, drugs that inhibit peristalsis are contraindicated. Combination therapy is necessary for the treatment of nosocomial infections caused by Pseudomonas aeruginosa. During treatment with Flexid, it is necessary to avoid direct solar and artificial UV radiation (solarium) to avoid photosensitization. and control mechanisms. Care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased centration of attention and psychomotor speed reactions.