Levoflotsin

General characteristics. Structure:

Active agent: a levofloksatsina of hemihydrate in terms of 500 mg of a levofloksatsin;

excipients: a gipromelloza, cellulose microcrystallic, кроссповидон, magnesium stearate, a covering for drawing a cover of Opadry II Yellow.

Pharmacological properties:

Drug possesses a wide range of antimicrobic action. The Bystry bactericidal effect is provided owing to oppression levofloksatsiny bacterial DNK-girazy enzyme which belongs to?? to type of topoisomerases. The volume structure of DNA of bacteria is as a result broken and their division is blocked. The range of activity of a levofloksatsin includes below-mentioned microorganisms. Gram-positive aerobes: Enterococcus faecalis, Staphylococcus aureus methy-S, Staphylococcus haemolyticus methy-S, Staphylococcus saprophyticus, Streptococci group C, G, Streptococcus agalactiae, Streptococcus pneumoniae peni-I/S/R, Streptococcus pyogenes. Gram-negative aerobes: Acinetobacter baumannii, Citobacter freundii, Eikenella corrodens, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Haemophilus influenze ampi-S/R, Haemophilus para-influenze, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis?????, Morganella morganii, Pasteurella multocida, Proteus mirabilis, Proteus vulgaris, aaprovidencia rettgeri, Providencia stuartii, Pseudomonas aeruginosa, Serratia marcescens. Anaerobe bacterias: Bacteroides fragilis, Clostridium perfringens, Peptostreptococcus. Others: Chlamydia pneumoniae, Chlamydia psittaci, Legionella pneumophila, Mycoplasma pneumoniae. Are changeably sensitive to effect of drug - gram-positive aerobes: Staphylococcus haemolyticus methy-R; - gram-negative aerobes: Bukholderia cepacia; - anaerobe bacterias: Bacteroides ovatus, Bacteroides thetaiiotamicron, Bacteroides vulgaris, Clostridium difficile. To effect of drug of a rezistentna - gram-positive aerobes: Staphylococcus aureus methy-R.

Pharmacokinetics. Levoflotsin quickly and almost is completely soaked up in a digestive tract with the peak of concentration in plasma which is observed in an hour after administration of drug. Absolute bioavailability – nearly 100%. Is exposed to linear pharmacokinetics in the range from 50 to 600 mg. Meal insignificantly influences drug absorption. About 30 - 40% of Levoflotsin contact a serum protein. The cumulative effect at a dosage of 500 mg has no clinical значення once a day. There is insignificant, but predicted Levoflotsin's cumulation at a dosage of 500 mg two times a day. Stable indicators of distribution are reached within 3 days. At a dose over 500 mg the maximum concentration of drug in mucous bronchial tubes and a secret of a bronchial epithelium made 8,3? g/ml and 10,8? g/ml respectively; in tissues of lungs – about 11,3? g/ml (it was reached within 4 – 6 hours after introduction). Levoflotsin badly gets into cerebrospinal fluid. Average concentration of drug in urine within 8 – 12 hours after a single dose of 150 mg, 300 mg, 500 mg of per os made 44? g/ml, 91? g/ml, 200? g/ml respectively. It is metabolized in very insignificant degree; metabolites make less than 5% of amount of the drug removed with urine. It is brought out of plasma rather slowly (the elimination half-life makes 6 – 8 hour). 85% are removed through kidneys. The way of introduction of Levoflotsin has no essential distinctions for drug pharmacokinetics.

Indications to use:

Drug appoint the adult for treatment of infections easy and moderately severe, caused by the microorganisms sensitive to a levofloksatsin: – acute sinusitis; – exacerbations of chronic bronchitis; – community-acquired pneumonia; – the complicated infections of urinary tract (including pyelonephritises); – infections of skin and soft tissues.

Route of administration and doses:

Drug is accepted by one or two times a day, irrespective of meal. Swallow, without chewing, washing down with enough liquid. Levoflotsin it is necessary to accept, at least, in two hours prior to or after administration of drugs, the containing salt of iron, antacids and a sukralfat as the last can reduce drug absorption. The general dose depends on type and weight of an infection, and also sensitivity of the possible activator to a levofloksatsin. Duration of treatment makes no more than 14 days. It is recommended to continue treatment by Levoflotsin within 48 – 72 hours after normalization of body temperature or the lack of the activator confirmed with microbiological tests. At acute sinusitis it is necessary to accept 500 mg of Levoflotsin of 1 times a day within 10 – 14 days; at an exacerbation of chronic bronchitis – 250 – 500 mg of 1 times a day 7 – 10 days; at community-acquired pneumonia – 500 mg of 1 - 2 time a day 7 – 14 days; at the complicated infection of urinary tract – 250 mg of 1 times a day 7 – 10 days; at skin infections – 150 – 500 mg of 1 - 2 time a day 7 – 14 days. To patients with renal failures (the clearance of creatinine is less than 50 ml/min.) in the first days appoint a full dose of drug, in the subsequent – reduce a dose depending on clearance of creatinine. Such patients have to be under control of the doctor. For patients with abnormal liver functions, and also for people of advanced age there is no need for dose adjustment.

Features of use:

Due to a possibility of injury of a joint cartilage by hinolona to the growing organism, cannot use drug pregnant women, the nursing women, children and teenagers up to 18 years. At use of drug for treatment of patients of advanced age it is necessary to consider that at such patients restriction of function of kidneys often takes place. Due to the possibility of undesirable side effect from a nervous system in the form of dizziness, drowsiness, vision disorders, hearing, etc., drug with care is appointed to the patients managing vehicles. During treatment it is necessary to avoid power solar or artificial ultra-violet irradiation; at emergence of phototoxic reactions (for example, skin rash) needs to stop treatment.

Side effects:

In certain cases the itch and erubescence takes place, it is rare – hypersensitivity reactions with symptoms of a small tortoiseshell or a cutaneous dropsy and mucous membranes; dispeptic phenomena; headache, dizziness, drowsiness; tachycardia; lowering of arterial pressure; increase in indicators of hepatic enzymes, bilirubin and creatinine of blood serum; eosinophilia, leukopenia, neutropenia, thrombocytopenia; general weakness (adynamy); inflammation of sinews, joint pain or muscles.

Interaction with other medicines:

Levoflotsin's adsorption significantly decreases at a concomitant use of the antacids containing magnesium and aluminum and also the drugs containing iron salts. Bioavailability of drug significantly decreases at a concomitant use with sukralfaty. The interval between reception of these drugs has to be not less than two hours. Care at co-administration of the drugs influencing renal secretion, in particular, of a probenitsid and Cimetidinum, especially to patients with renal failures is necessary. The elimination half-life of cyclosporine increases by 33% at a concomitant use with levofloksatsiny.

Contraindications:

Levoflotsin it is impossible to apply at hypersensitivity to drugs of this group, at epilepsy, to children and teenagers up to 18 years, to pregnant women, when feeding by a breast, and also to patients with complaints to side effect from sinews after use of hinolon.

Overdose:

The most important estimated symptoms of overdose touch the central nervous system: confusion of consciousness, dizziness, disturbance of consciousness and convulsive attacks. Treatment – symptomatic. Levofloxacin is not removed when carrying out dialysis. Has no specific antidote.

Storage conditions:

To store in the place, unavailable to children, at a temperature of 15 - 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 5 tablets, coated, in a blister strip packaging; on 1 planimetric packaging in a pack cardboard.