Suspension testosterone is rapidly and almost completely absorbed after oral administration. Food intake has little effect on the speed and completeness of removals. Bioavailability of 500 mg oral levofloxacin after is nearly 100%. After administration of a single 500 mg dose of levofloxacin is the maximum concentration of 5.2-6.9 g / ml, time to maximum concentration -. 1,3ch half-life – 8.6 hours.
Relationship to plasma proteins – 30-40%. It penetrates the tissues and organs: lungs, bronchial mucosa, sputum, organs of the urogenital system, bone tissue, cerebrospinal fluid, the prostate gland, polymorphonuclear leukocytes, alveolar macrophages.
In the liver, a small part of the oxidized and / or deacetylated. Report from the body mainly by the kidneys by glomerular filtration and tubular secretion. Following oral administration, approximately 87% of the dose is excreted in the urine unchanged within 48 hours, less than 4% in the faeces within 72 hours.
Infectious-inflammatory diseases, caused by susceptible microorganisms: acute sinusitis, acute exacerbations of chronic bronchitis, community-acquired pneumonia, complicated urinary tract infections (including pyelonephritis), uncomplicated urinary tract infections, prostatitis, infections of skin and soft tissues, septicemia / bacteremia related with the above indications, an intra-abdominal infection.
- hypersensitivity to levofloxacin or other quinolones;
- tendon injury during the earlier treatment of quinolones;
- childhood and adolescence (18 years);
- pregnancy and lactation.Precautions
The drug should be used with caution in the elderly, due to the high probability of the presence of a concomitant decrease in renal function, with a deficit of glucose-6-phosphate dehydrogenase.DOSAGE AND ADMINISTRATION
The drug is taken orally once or twice a day. Tablets do not chew and drink plenty of fluids (0.5 to 1 cup), can be taken before meals or between meals. Doses are determined by the nature and severity of the infection and the sensitivity of the alleged pathogen.
In patients with normal or mildly reduced kidney function (creatinine clearance> 50 mL / min.), The recommended drug dosage regimen: Sinusitis (inflammation of the sinuses): 500 mg 1 times per day – 10 -14 days. Exacerbation of chronic bronchitis: . 250 mg or 500 mg 1 time per day – 7-10 days Community-acquired pneumonia: 500 mg 1-2 times a day – 7-14 days. Uncomplicated urinary infections ways: . 250 mg 1 time per day – 3 days Prostatitis: 500 mg – 1 per day – 28 days. Complicated urinary tract infections, including pyelonephritis: 250 mg 1 time per day – 7-10 days. skin infections and soft tissues: 250 mg 1 time per day or 500 mg 1-2 times a day – 7-14 days. Septicemia / bacteremia: 250 mg or 500 mg 1-2 times a day – 10-14 days ( after intravenous administration to continue therapy). Intra-abdominal infections: 250 mg or 500 mg 1 time per day – 7-14 days (in combination with antibacterial drugs acting on the anaerobic flora, after intravenous administration to continue therapy).
Skin reactions and general hypersensitivity reaction times: the itching and redness of the skin. Rare: general reactions of hypersensitivity (anaphylactic and anaphylactoid reaction) with symptoms such as urticaria, bronchoconstriction and possibly – heavy gasps. In very rare cases, – swelling of the skin and mucous membranes ( for example in the areas of the face and throat), sudden drop in blood pressure and shock; increased sensitivity to sunlight and ultraviolet radiation (see “Cautions.”); hypersensitivity pneumonitis; vasculitis. In some cases: severe rash with blistering, such as Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome) and exudative erythema multiforme. General hypersensitivity reactions may sometimes be preceded by lighter skin reactions. The above-mentioned reaction may develop after the first dose in a few minutes or hours after administration.
Action on the gastrointestinal tract and metabolism Common: nausea, diarrhea. Sometimes: loss of appetite, vomiting, abdominal pain, dyspepsia. Rare: bloody diarrhea which in very rare cases, it may be a sign of bowel inflammation and even pseudomembranous colitis (see .. “Cautions”) Very rare: drop in blood sugar levels (hypoglycemia), which has particular importance for patients with diabetes; Possible symptoms of hypoglycemia: “wolf” appetite, nervousness, sweating, trembling. Experience with other quinolones suggests that they are capable of causing an exacerbation of porphyria (a very rare metabolic disease) in patients who are already suffering from the disease. Such an effect is not excluded the application Lefoktsin drug.
Nervous system Occasionally: headache, dizziness, and / or numbness, drowsiness, and sleep disorders. Rare: depression, anxiety, psychotic reactions (eg, hallucinations), discomfort (eg, paresthesias in the hands), tremor, agitation , confusion, convulsions, anxiety. Very rare: visual and hearing impairment, disturbances of taste and smell sensitivity, reduction of tactile sensitivity.
The action on the cardiovascular system Rare: increased heart rate, decreased blood pressure. Very rare: (shock-like) vascular collapse. In some cases: lengthening of the QT interval.
The action on the muscles, tendons and bones Rare: defeat tendons (including tendonitis), joint and muscle pain. Very rare: tendon rupture (eg Achilles tendon); this side effect may occur within 48 hours after the start of treatment and may be bilateral in nature (see “Cautions.”); muscle weakness, which is of particular importance for patients with bulbar syndrome. In some cases: muscle damage (rhabdomyolysis).
Action on the liver and kidney Common: increase in liver enzymes (eg, alanine aminotransferase and aspartate aminotransferase). Rare: increased levels of bilirubin and serum creatinine (sign of limitation of the liver or kidney). Very rare: hepatic reactions (eg, inflammation of the liver); deterioration of renal function until suspension testosterone the acute renal failure, for example, due to allergic reactions (interstitial nephritis).
Effects on blood Occasionally: increased number of eosinophils, a decrease in the number of white blood cells. Rare: neutropenia; thrombocytopenia, which may be accompanied by increased bleeding. Very rare: agranulocytosis and the development of severe infections (persistent or recurrent fever, deterioration of health). In some cases: haemolytic anemia; pancytopenia.
Other side effects sometimes: . General weakness (asthenia) Very rarely . Fever Any antibiotic therapy can cause changes in the microflora (bacteria and fungi), which is normally present in humans. For this reason, it may happen enhanced reproduction of bacteria and fungi that are resistant to antibiotics are used (secondary infection and superinfection), which in rare cases may require additional treatment.
Symptoms of overdose Lefoktsin occur at the level of the central nervous system (confusion, dizziness, impairment of consciousness and seizures seizures by type epipripadkov). In addition, it can be marked gastrointestinal symptoms (eg, nausea) and erosive lesions of the mucous membranes.
In the studies conducted by the supra-therapeutic doses of levofloxacin was shown lengthening the QT interval.
Treatment should be focused on presenting symptoms. Levofloxacin is not displayed by dialysis (hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). Specific antidote (counteracting agent) does not exist.
INTERACTION WITH OTHER DRUGS
There are reports of pronounced lowering the threshold of convulsive readiness, while the use of quinolones and substances that can, in turn, lower the cerebral seizure threshold. Equally, it also relates to the simultaneous use of quinolones and theophylline, fenbufena or similar to it nonsteroidal antiinflammatory drugs (for the treatment of rheumatic diseases).
The action of the drug Lefoktsin significantly attenuated while the use of sucralfate (means to protect the gastric mucosa). The same thing happens with the simultaneous use of magnesium-aluminum containing antacids or (drugs for the treatment of heartburn and gastralgia), as well as salts of iron (for the treatment of anemia). Lefoktsin should take no less than 2 hours before or 2 hours after the administration of these agents. With calcium carbonate interaction have been identified.
With the simultaneous use of vitamin K antagonists should be monitored for blood coagulation system.
Excretion (renal clearance) Lefoktsina slightly slowed down by the action of cimetidine and probenicid. It should be noted that this interaction is almost does not have any clinical significance. However, while the use of drugs such as probenicid and cimetidine, blocking certain way of deducing (tubular secretion) treatment Lefoktsinom should be made with caution.
This applies primarily to patients with reduced renal function.
Lefoktsin slightly increases the half-life of cyclosporin.
Receiving glucocorticoids increases the risk of tendon rupture.
Lefoktsin can not be used to treat children and adolescents because of the probability of destruction of the articular cartilage.
In the treatment of elderly patients should be aware that patients in this group often have impaired renal function (see. Section “Dosage and administration”).
In severe inflammation lung caused by pneumococcus Lefoktsin may not give the optimal therapeutic effect. Nosocomial infections caused by certain pathogens (P. aeruginosa), may require a combined treatment. During treatment with Lefoktsin may develop seizures attack in patients with previous brain damage caused by, for example, stroke or severe injury. Seizure may be increased, and while the application fenbufena similar to them of non-steroidal anti-inflammatory drugs, or theophylline (see. “Interactions”).
Despite the fact that the photosensitivity observed when applying Lefoktsina very rarely, to prevent it from patients is not recommended to be exposed unnecessarily to strong sunlight or artificial ultraviolet light.
If you suspect pseudomembranous colitis should immediately cancel Lefoktsin and start appropriate treatment. In such cases, you can not use drugs that suppress intestinal motility.
Rarely observed when using the drug Lefoktsin tendinitis (especially inflammation of the Achilles tendon) may lead to tendon rupture. Elderly patients are more prone to tendonitis. Corticosteroid treatment ( “cortisone preparations”) are likely to increase the risk of tendon rupture. If you suspect tendonitis, stop treatment with Lefoktsin and start appropriate treatment of the affected tendon, for example, providing him rest state (see. “Contraindications” and “Side effects”).
Patients with deficiency of glucose-6-phosphate dehydrogenase (an inherited metabolic disorder) fluoroquinolones can respond to the destruction of erythrocytes (hemolysis). In this regard, the treatment of such patients Lefoktsinom should be carried out with great care.
These side effects Lefoktsin drug like dizziness or numbness, drowsiness and visual disturbances (see. Also section “Side effects), can impair reactivity and ability to concentrate. this can be a risk in situations where these abilities are of special suspension testosterone importance (eg while driving, during maintenance of machines and mechanisms, when working in an unstable position). in particular as it concerns cases of drug interactions with alcohol.