Floksium

General characteristics. Structure:

Active ingredient: levofloxacin; 1 tablet, film coated, contains a levofloksatsin of a gemigidrat in terms of levofloxacin of 500 mg; excipients: полипласдон XL (кросповидон), cellulose microcrystallic, potato starch, talc, a gidroksipropilmetiltsellyuloz (gipromeloz), sodium lauryl sulfate, sodium krakhmalglikolit (sodium carboxymethylstarch), calcium stearate, mix for a covering of "Opadry II Yellow".

Pharmacological properties:

Pharmacodynamics. Floksium as the representative of group of ftorkhinolon, is characterized by a wide range of antibacterial action. The Bystry bactericidal effect is provided owing to oppression of bacterial DNK-girazy enzyme, belonging to the II type of topoisomerases. DNK-giraza is important enzyme of bacteria and the main catalyst of processes of duplication, a transcription and reparation of bacterial DNA. The impossibility of division (reproduction) of bacterial cells is result of such oppression. A range of activity of drug Floksium includes gram-positive, gram-negative bacteria, together with nonfermentative bacteriums, often
pneumoniae causing a nozokomialny infection, and also atypical microorganisms, such as S., C.trachomatis, M.pneumoniae, L.pneumophila, Ureaplasma, such pathogens as the mycobacteria, H.pylori and anaerobe bacterias sensitive to a levofloksatsin. Like other ftorkhinolona, Floksium is inactive concerning spirochetes. Gram-positive aerobes are sensitive to drug: Enterococcus faecalis,
Staphylococcus aureus (strains sensitive to Methicillinum), Staphylococcus saprophyticus, streptococci of the groups C,G, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes;
gram-negative aerobes: Acinetobacter baumannii, Citrobacter freundii, Eikenella corrodens, Enterobacter agglomerans, Enterobacter cloacae, Escherichia col і, Haemofilus 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; anaerobe bacterias: Bacteroides fragilis, Clostridium perfringens, Peptostreptococcus; others, such as Chlamydia pneumoniae, Chlamydia psittaci, Legionella pneumophila, Mycoplasma pneumoniae. Are changeably sensitive to effect of drug: gram-positive aerobe of Staphylococcus haemolyticus;
gram-negative aerobe of Burkholderia cenocepacia; anaerobe bacterias: Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus, Clostridium difficile.

Pharmacokinetics. After intake Floksium quickly and almost is completely soaked up with the peak of concentration in plasma in 1 hour. Absolute bioavailability – nearly 100%. Meal influences drug absorption a little. After reception of a single dose of 0,25 g the maximum concentration is established in 1,6+1,0 hours and makes 2,8+0,4 mkg/ml, after reception of 0,5 g 1,3+0,6 hours and 5,1+0,8 mkg/ml respectively. About 30-40% of drug contact a serum protein. Stable indicators of distribution are reached for 3 days. Also N-oxide levofloxacin is metabolized in very insignificant quantity to a dezmetillevofloksatsin. These metabolites make less than 5% of amount of drug which is emitted with urine. After oral administration levofloxacin is removed from plasma rather slowly (T1/2 makes 6 – 8 hours). Removal is carried out generally by kidneys (more than 85% of the entered dose).
Pharmaceutical characteristics.
Main physical and chemical properties: tablets, film coated, creamy-yellow color, an oval form with a biconvex surface, from a risky on the one hand tablet and a stamping of "KMP" on the other hand. On cross section a noticeable kernel of yellowish color.

Indications to use:

The infections caused by microorganisms, sensitive to a levofloksatsin: lower respiratory tract infections (an exacerbation of chronic bronchitis, not hospital pneumonia), acute sinusitis, the complicated infections of urinary tract, including pyelonephritis, infections of skin and soft tissues.

Route of administration and doses:

Floksium accept 1 or 2 times a day. The dose depends on type and weight of an infection, and
also sensitivity of the activator.
Duration of treatment depends on disease and makes no more than 14 days.
It is recommended to continue treatment at least for 48 – 72 hours later
normalization of body temperature or confirmed with microbiological tests
destructions of activators. Floksium it is necessary to swallow of drug tablets not
chewing, to wash down with enough liquid, it is possible to accept as together with
food, and separately. In the table recommendations concerning a dosage for adults are given below
patients with normal function of kidneys (at value of clearance of creatinine more
50 ml/min.).

Indications                            Daily dose              treatment Duration
Acute sinusitis                  of 0,5 g for 1 reception                 of 10 - 14 days
Aggravation of chronic
bronchitis
                                           0,25 g - 0,5 g for 1 reception        of 7 - 10 days
Not hospital pneumonia of 0,5 g – 1 g for 1 – 2 reception       of 7 - 14 days
The complicated infections
urinary tract,
including pyelonephritis
                                               0,25 g for 1 reception                of 7 - 10 days
Infections of skin and soft
fabrics
                                               0,5 g of 1 - 2 time                 of 7 - 14 days

This form of drug is not recommended for patients with an impaired renal function,
at which the clearance of creatinine makes less than 50 ml/min.
For patients with the broken function of a liver dose adjustment is not necessary as
levofloxacin in insignificant degree is metabolized in a liver.
At patients of advanced age with normal function of kidneys a drug dosing not
demands correction.

Features of use:

During treatment by drug Floksium development of attacks of spasms in patients with the damage of a brain in the anamnesis caused, for example, by a stroke or a severe injury is possible. In spite of the fact that the effect of a photosensitization is noted quite seldom, for its prevention by the patient it is not recommended to be submitted influence of power solar irradiation. At suspicion of pseudomembranous colitis it is necessary to cancel urgently Floksium and to begin the corresponding treatment. Tendenit which is seldom observed, can lead to a rupture of a sinew. Patients of advanced age are more inclined to such complication. At suspicion on a tendinitis it is necessary to stop urgently treatment by drug Floksium and to begin treatment of the affected sinew. Ability to influence speed of response at control of motor transport or work with other mechanisms. It is recommended to abstain from the activity demanding speed of psychomotor reactions (management of transport, work with potentially dangerous mechanisms), considering possible undesirable reactions from a nervous system (dizziness, an okocheneniye, drowsiness, confusion of consciousness, a visual disturbance and hearing, disturbance of the movement).

Side effects:

The general hypersensitivity reactions and reactions from skin and its appendages: itch and reddening; seldom - anaphylactic and anaphylactoid reactions with such signs as a small tortoiseshell, a spasm of bronchial tubes, an asthma and, perhaps, heavy suffocation; seldom or never cutaneous dropsies and mucous membranes (for example, face skin and mucous membrane of a throat). Are very seldom possible: sudden lowering of arterial pressure and shock; hypersensitivity to solar and ultraviolet radiation. There are single cases of a strong enanthesis and mucous membranes to formation of bubbles, such as Stephens-Johnson's syndrome, toxic epidermal necrolysis (Lyell's disease) and exudative multiformny erythema. Easier reactions from skin can sometimes precede the general hypersensitivity reactions. The above-named reactions can appear after the first dose of drug for several minutes or hours after reception.
From digestive tract and a metabolism: often – nausea, a diarrhea, in certain cases – lack of appetite, vomiting, an abdominal pain. Are seldom possible diarrhea with blood impurity which can be intestines inflammation signs, including pseudomembranous colitis. Very seldom - decrease in sugar in blood (hypoglycemia) that has special value for patients with a diabetes mellitus. The increased appetite, nervousness, perspiration, a tremor of extremities can be signs of a hypoglycemia.
Perhaps poyaleny typical side reaction on hinolona – porphyria attacks at patients on a porphyria.
From a nervous system: in single cases the headache, dizziness, an okocheneniye, drowsiness, frustration of a dream are possible. Seldom there are unpleasant feelings, for example, of paresthesia in brushes, trembling, concern, a condition of fear, convulsive attacks and confusion of consciousness. Very seldom – a visual disturbance and hearing, disturbance of taste and sense of smell, decrease in feeling of a touch, and also psychopathic reactions, such as hallucinations and depressive changes of mood, disorder of processes of the movement, including disturbance when walking.
From cardiovascular system: tachycardia, a lowering of arterial pressure, it is very rare – a collapse (similar to shock).
From a musculoskeletal system: seldom – damages of sinews, including their inflammation, a joint pain or muscles are possible. Very seldom – a rupture of sinews (for example, a rupture of an Achilles sinew). This side effect can be shown for 48 hours from an initiation of treatment and strike Achilles tendons of both legs. Muscular weakness which can have special value at patients with a heavy myasthenia. Single cases of damage of muscles (рабдомиолиз).
From a liver and kidneys: often – increase in indicators of liver enzymes (ALT, nuclear heating plant). In certain cases – increase in indicators of bilirubin and creatinine in blood serum. Very seldom – hepatic reactions, such as a liver inflammation. Deterioration in function of kidneys, up to an acute renal failure, for example, owing to allergic reactions (intersticial nephrite).
From system of a hemopoiesis: in certain cases – the eosinophilia, a leukopenia are possible. Seldom – a neutropenia, thrombocytopenia that can cause the increased tendency to hemorrhages or bleedings. Very seldom – an agranulocytosis which can be followed by heavy symptoms of a disease (a long or recurrent fever, pharyngitis, the expressed painful health). Single cases – hemolitic anemia, a pancytopenia. Other side effects: in certain cases – the general weakness (adynamy). Very seldom – fever, allergic reactions from lungs (an allergic pneumonitis) or small blood vessels (vasculitis). Use of any antibacterial agents can lead to the disturbances connected with their influence on normal microflora of an organism. For this reason the consecutive infection demanding additional treatment can develop.

Interaction with other medicines:

Efficiency of drug Floksium significantly decreases at a concomitant use with the antacids containing magnesium and aluminum and also with the drugs containing iron salts. The recommended term between administrations of drug Floksium and the called drugs has to make not less than 2 hours. Bioavailability of drug Floksium considerably decreases at a concomitant use with sukralfaty. The span between receptions of these drugs has to make not less than 2 hours. Though during clinical tests interaction between drug Floksium and theophylline, nevertheless perhaps essential decrease in a convulsive threshold at simultaneous use of hinolon with theophylline, non-steroidal anti-inflammatory drugs and other agents reducing a convulsive threshold is not established. Probenitsid, the methotrexate and other drugs which are subject to canalicular secretion in kidneys block furosemide excretion (reduction of efficiency of furosemide). The renal clearance of drug Floksium decreases in the presence of a probenitsid by 34%, and in the presence of Cimetidinum – for 24%. It is necessary to be careful at co-administration of the drugs influencing renal secretion, in particular, of a probenitsid and Cimetidinum, especially to patients with the broken renal function. The elimination half-life of cyclosporine increases by 33% at a concomitant use with
drug Floksium. At simultaneous use with antagonists of vitamin K (for example, warfarin)
it is necessary to control coagulation indicators in connection with a possibility of increase in indicators of coagulative tests and/or a possibility of bleeding. At simultaneous use with glucocorticoids the risk of a rupture of a sinew increases. Drug use Floksium along with alcohol is not recommended.

Contraindications:

- hypersensitivity to a levofloksatsin or other ftorkhinolona, and also to drug components;
- epilepsy;
- damages of sinews at treatment of a hinolonama;
- age up to 18 years;
- pregnancy;
- the women nursing.

Use during pregnancy and feeding by a breast. Due to the lack of researches in public and possible injury of a joint cartilage by hinolona to the growing organism Floksium pregnant women and the feeding women cannot apply. If during treatment by drug Floksium the woman becomes pregnant, use of drug should be stopped.
Children.
Floksium is contraindicated for use to children and teenagers aged up to 18 years because of risk of injury of a joint cartilage.

Overdose:

Overdose symptoms first of all are noted from the central nervous system (confusion of consciousness, dizziness, disturbance of consciousness and convulsive attacks). Besides, there can be frustration from digestive tract (nausea, vomiting), and also damage of mucous membranes. Extension of an interval of QT is possible. At overdose careful observation of the patient, including monitoring of an ECG is necessary. Treatment - symptomatic. Floksium is not brought by means of dialysis. There is no specific antidote.

Storage conditions:

Period of validity. 2 years. To store in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 5 or 10 tablets in the blister. 1 blister in a pack.