Levofloxacin

Fluoroquinolone is a broad-spectrum antimicrobial bactericidal agent. It blocks DNA gyrase ( topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes deep morphological changes in the cytoplasm , cell wall and bacterial membranes .

Effective against Enterococcus faecalis , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pneumoniae , Streptococcus pyogenes , Streptococcus agalactiae , Viridans group streptococci , Enterobacter cloacae , Enterobacter aerogenes , Enterobacter agglomerans , Enterobacter sakazakii , Escherichia coli , Haemophilus influenzae , Haemophilus parainfluenzae , Klebsiella pneumoniae , Klebsiella oxytoca , Legionella pneumoniae , Moraxella catarrhalis , Proteus mirabilis , Pseudomonas aeruginosa , Pseudomonas fluorescens , Chlamydia pneumoniae , Mycoplasma pneumoniae , Mycoplasma hominis , Acinetobacter anitratus , Acinetobacter baumannii , Acinetobacter calcoaceticus , Bordetella pertussis , Citrobacter diversus , Citrobacter freundii , Morganella morganii , Proteus vulgaris , Providencia rettgeri , Providencia stuartii , Serratia marcescens , Clostridium perfringens .

When taken orally, it is rapidly and almost completely absorbed (food intake has little effect on the speed and completeness of absorption ). Bioavailability is 99%. TCmax - 1-2 hours; when taking 250 and 500 mg, Cmax is 2.8 and 5.2 μg / ml, respectively. Communication with plasma proteins - 30-40%. It penetrates well into organs and tissues: lungs , mucous membrane of the bronchi , sputum , organs of the genitourinary system , polymorphic nuclear leukocytes , alveolar macrophages . In the liver, a small portion is oxidized and / or deacetylated. Renal clearance is 70% of the total clearance. T _1/2 - 6-8 hours. It is excreted mainly by the kidneys by glomerular filtration and tubular secretion . Less than 5% of levofloxacin is excreted as metabolites . In unchanged form, with urine within 24 hours, 70% is excreted and in 48 hours - 87%; in feces for 72 hours, 4% of the oral dose is found. After intravenous infusion of 500 mg for 60 min, Cmax - 6.2 μg / ml. With intravenous single and multiple administration, the apparent volume of distribution after administration of the same dose is 89-112 L, Cmax - 6.2 μg / ml, T ^1/2 - 6.4 hours.

Infections of the lower respiratory tract ( chronic bronchitis , pneumonia ), ENT organs ( sinusitis , otitis media ), urinary tract and kidneys (including acute pyelonephritis , chronic prostatitis ), skin and soft tissues (suppurative atheromas , abscesses , boils ), tuberculosis (complex therapy of drug-resistant forms).

It is the drug of choice for chronic prostatitis (at a dosage of 500 mg per day, for 28 days). The effectiveness of such treatment exceeds 77%. ^{[2] [3]}

Hypersensitivity , epilepsy , tendon damage with previous treatment with quinolones , pregnancy , lactation , childhood and adolescence (up to 18 years).

Caution

Elderly (high likelihood of a concomitant decrease in renal function), glucose-6-phosphate dehydrogenase deficiency .

Inside, before meals or in between meals, without chewing, drinking plenty of fluids.

• In acute sinusitis, by mouth, 500 mg 1 time per day, for 10-14 days, or 750 mg 1 time per day for 5 days;
• In case of an infectious exacerbation of COPD - 500 mg once a day, for 7-10 days, or 750 mg once a day for 5 days;
• In pneumonia, by mouth, 250-500 mg 1-2 times a day (0.5-1 g / day); intravenously - 500 mg 1-2 times a day, for 7-14 days, or 750 mg 1 time per day for 5 days.
• In case of urinary tract infections - inside, 250 mg once a day; intravenously, in the same dose, 7-10 days. With prostatitis, by mouth, 500 mg once a day for 28 days.
• For infections of the skin and soft tissues - inside, 250-500 mg 1-2 times a day; intravenously, 500 mg 2 times a day, for 7-14 days.
• With tuberculosis, by mouth, 500 mg 1-2 times a day for up to 3 months.

It is also used intravenously, after intravenous administration a few days later it is possible to switch to oral administration in the same dose.

In kidney diseases, the dose is reduced in accordance with the degree of dysfunction: with creatinine clearance (CC) 20-50 ml / min - 125-250 mg 1-2 times a day, 10-19 ml / min - 125 mg 1 time in 12 -48 hours, less than 10 ml / min (including hemodialysis) - 125 mg after 24 or 48 hours.

From the digestive system: nausea , vomiting , diarrhea (including blood ), indigestion, decreased appetite , abdominal pain, pseudomembranous enterocolitis ; increased activity of “liver” transaminases , hyperbilirubinemia , hepatitis , dysbiosis .
From the cardiovascular system: lowering blood pressure , vascular collapse , tachycardia, lengthening the QT interval .
From the side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling).
From the nervous system: headache , dizziness , weakness, drowsiness, insomnia , tremor , anxiety, paresthesia , fear, hallucinations , confusion, depression , motor disorders, epileptic seizures (in predisposed patients).
From the sensory organs: impaired vision, hearing, smell, taste and tactile sensitivity.
From the musculoskeletal system : arthralgia , muscle weakness, myalgia , tendon rupture, tendonitis .
From the urinary system: hypercreatininemia , interstitial nephritis , acute renal failure .
From the hemopoietic organs: eosinophilia , hemolytic anemia , leukopenia , neutropenia , agranulocytosis , thrombocytopenia , pancytopenia , hemorrhage .
Allergic reactions: photosensitivity , 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 , suffocation, anaphylactic shock , allergic pneumonia .
Other: asthenia , exacerbation of porphyria , rhabdomyolysis , persistent fever , the development of superinfection .

Overdose

Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract , lengthening of the QT interval, confusion, dizziness , convulsions .
Treatment: symptomatic, dialysis is ineffective.

After normalization of body temperature, it is recommended to continue treatment for at least 48-78 hours. The duration of intravenous infusion of 500 mg (100 ml of infusion solution) should be at least 60 minutes. During treatment, it is necessary to avoid solar and artificial UV radiation in order to avoid damage to the skin (photosensitivity). When there are signs of tendonitis, pseudomembranous colitis, levofloxacin is immediately canceled. It should be borne in mind that in patients with a history of brain damage ( stroke , severe trauma), seizures may develop, with glucose-6-phosphate dehydrogenase deficiency, there is a risk of hemolysis . During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Increases T _1/2 cyclosporine . The effect is reduced by drugs that inhibit intestinal motility, sucralfate , Al ³⁺ and Mg ²⁺ -containing antacid drugs and Fe salts (a break between intake of at least 2 hours is necessary). NSAIDs , theophylline increase convulsive readiness, corticosteroids increase the risk of tendon rupture. Cimetidine and tubular secretion blocking drugs slow down excretion. The solution for intravenous administration is compatible with 0.9% NaCl solution , 5% dextrose solution, 2.5% Ringer's solution with dextrose , combined solutions for parenteral nutrition ( amino acids , carbohydrates , electrolytes). Do not mix with heparin and solutions that have an alkaline reaction.

• Clinical nutrition
• Parenteral nutrition

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