Floksium solution
Producer: Arterium (Arterium) Ukraine
Code of automatic telephone exchange: J01MA12
Release form: Liquid dosage forms. Solution for infusions.
General characteristics. Structure:
Active ingredient: levofloxacin;
1 ml of solution contains a levofloksatsin гемигидрат in terms of levofloxacin of 5 mg;
excipients: glucose anhydrous, dinatrium эдетат, Acidum hydrochloricum, water for injections.
Pharmacological properties:
Pharmacodynamics. Levofloxacin (fluorine-2, metil-10-(1-piperazinit) - oxo-7H-piridol [1,2,3,-]-1,6-carboxyl acid) – synthetic antibacterial agent of group of ftorkhinolon. Has a wide range of antibacterial action. The Bystry bactericidal effect is provided as a result of oppression levofloksatsiny bacterial DNK-girazy enzyme which belongs to type topoisomerases II. 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 gram-positive and gram-negative bacteria, including nefermentuyushchy bacteria which often cause a nozokomialny infection, and also atypical microorganisms, such as S. of pneumoniae, S. of trachomatis, M. pneumoniae, L. pneumophila, Ureaplasma. Besides, pylorii such activators as mycobacteria, N. are sensitive to a levofloksatsin anaerobe bacterias.
Such microorganisms are sensitive to drug: gram-positive aerobes – Enterococcus faecalis, Staphylococcus aureus metitsilinchuvstvitelny, Staphylococcus haemolyticus of a metitsilinchustvitelna, Staphylococcus saprophyticus, Streptococci Z, G, Streptococcus agalactiae, Streptococcus pneumoniae, including resistant to penicillin, Streptococcus pyogenes; gram-negative aerobes – Acinetobacter baumannii, Citrobacter freundii, Eikenella corrodens, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, including resistant to ampicillin, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis including producing b-lactamelements, Morganella morganii, Pasteurella multocida, Proteus mirabilis, Proteus vulgaris, Providencia 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 drug: gram-positive aerobes: Staphylococcus haemolyticusmetitsilinrezistentnye; gram-negative aerobes: Burkholderia cepacia; anaerobe bacterias: Bacteroides ovatus, Bacteroides thetaiotamicron, Bacteroides vulgaris, Clostridium difficile.
To rezistentna drug: gram-positive aerobes: Staphylococcus aureus is metitsilinrezistentny.
As well as other ftorkhinolona, levofloxacin it is not active concerning spirochetes.
Pharmaceutical characteristics.
Main physical and chemical properties: transparent liquid of yellowish color.
Incompatibility.
Floksium is compatible to such infusion solutions – 0,9% solution of sodium of chloride, 5% dextrose solution, Ringer's solution combined by solutions for parenteral food (amino acids, carbohydrates, electrolytes). Floksium for intravenous administration it is impossible to mix with the heparin or solutions having alkali reaction (for example, Natrii hydrocarbonas solution).
Indications to use:
Pneumonia, the complicated infections of urinary tract (including pyelonephritises), infections of skin and soft tissues, septicaemia/bacteremia, intraabdominal infections, prostatitis.
Route of administration and doses:
Floksium it is necessary to apply immediately (for 3 hours) after perforation of a bottle, to prevention of any bacterial pollution. Protection against light at infusion is not necessary.
At room lighting solution for intravenous administration can be stored as much as possible for 3 days without protection against light.
Taking into account biological equivalence of peroral and parenteral forms perhaps identical dosing.
Dosing depends on a look and weight of an infection.
For treatment of adults with normal function of kidneys at which the clearance of creatinine makes over 50 ml/min. usually recommend the following doses of drug:
Indication Daily dose Quantity Duration
introductions in days of treatment
Not hospital pneumonia of 500 - 1000 mg 1-2 times of 7-14 days
The complicated infections
urinary path,
including pyelonephritis of 250 mg * 1 time of 7-10 days
Prostatitis of 500 mg ** 1 time of 28 days
Infections of skin and soft
fabrics of 500 - 1000 mg 1-2 times of 7-14 days
Septicaemia/bacteremia of 500 - 1000 mg 1-2 strike 10 - 14 days
Intraabdominal
infections *** 500 mg of 1 times of 7 - 14 days
* It is necessary to consider expediency of increase in a dose in cases of a heavy infection.
** According to a condition of the patient in several days transition from initial intravenous administration to oral administration with the same dosage is possible.
*** In a combination with antibiotics with impact on anaerobic activators.
As levofloxacin is removed preferential by kidneys, for patients with the weakened function of kidneys the dose has to be reduced.
Dosing for adult patients with an impaired renal function at whom the clearance of creatinine makes less than 50 ml/min.:
Clearance of creatinine the dosing Mode (depending on weight of an infection)
50-20 ml/min. first dose: 250 mg first dose: 500 mg first dose: 500 mg
the subsequent: 125 mg / 24 h the subsequent: 250 mg / 24 h the subsequent: 250 mg / 12 h
19-10 ml/min. first dose: 250 mg first dose: 500 mg first dose: 500 mg
the subsequent: 125 mg / 48 h the subsequent: 125 mg / 24 h the subsequent: 125 mg / 12 h
<10 ml/min.,
(and also at
hemodialysis and HAPD *) first dose: 250 mg first dose: 500 mg first dose: 500 mg
the subsequent: 125 mg / 48 h the subsequent: 125 mg / 24 h the subsequent: 125 mg / 24 h
Note: * after a hemodialysis or the chronic out-patient peritoneal dialysis (COPPD) additional doses are not necessary.
Dosing for patients with the broken function of a liver. Dose adjustment is not necessary as levofloxacin in insignificant degree is metabolized in a liver.
Dosing for patients of advanced age. If function of kidneys is not broken, there is no need for dose adjustment.
Solution for intravenous administration Floksium is entered intravenously slowly, by drop infusion. Duration of introduction of one bottle Floksiuma (100 ml of solution for intravenous administration from 500 mg of a levofloksatsin) has to make not less than 60 min.
Duration of treatment depends on disease and makes no more than 14 days. As well as at use of other antibacterial agents, it is recommended to continue treatment by drug Floksium at least for 48-72 hours after normalization of body temperature or the destruction of activators confirmed with microbiological tests.
Features of use:
With care apply levofloxacin to patients of advanced age (high probability of existence of the accompanying depression of function of kidneys). After normalization of temperature not less than 48 - 78 hours are recommended to continue treatment. Duration of intravenous injection of 500 mg (100 ml of infusion solution) has to make not less than 60 min. During treatment it is necessary to avoid solar and artificial UF-radiation, in order to avoid damage of integuments (photosensitization). With the advent of tendinitis signs levofloxacin is immediately cancelled. It must be kept in mind that at patients with damage of a brain in the anamnesis (a stroke, a severe injury) development of spasms is possible, at insufficiency glyukozo-6-fosfatdegidrogenazy – risk of development of hemolysis.
Ability to influence speed of response at control of motor transport or work with other mechanisms.
To patients who manage vehicles work with machines and mechanisms, it is necessary to consider possible undesirable actions of rather nervous system (dizziness, drowsiness, confusion of consciousness, a visual disturbance and hearing, disorder of processes of the movement also during walking).
Side effects:
Reactions from skin and the general hypersensitivity reactions: in certain cases - an itch and erubescence; seldom – the general hypersensitivity reactions (anaphylactic and anaphylactoid) with such manifestations as a small tortoiseshell, a spasm of bronchial tubes and, perhaps, heavy suffocation; very seldom - a cutaneous dropsy and mucous membranes (for example, face skin and a mucous membrane of a throat); very seldom - a sudden lowering of arterial pressure and shock, lengthening of a QT interval, hypersensitivity to solar and ultra-violet radiation; in isolated cases - a heavy enanthesis and mucous membranes with 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. Such reactions can appear after the first dose and for several minutes or hours after reception.
From a digestive tract: often - nausea, a diarrhea; in certain cases - lack of appetite, vomiting, an abdominal pain, digestive disturbances; seldom – bloody ponosa which can sometimes be an intestines inflammation sign, including pseudomembranous colitis; very seldom - the decrease in content of sugar in blood (hypoglycemia) having perhaps, special value for patients with a diabetes mellitus. The increased appetite, nervousness, the increased perspiration, trembling of extremities can be signs of a hypoglycemia.
As for other hinolon it is known that they, perhaps, are capable to cause porphyria attacks in patients with this disease. It can concern as well Floksium.
From a nervous system: in isolated cases - a headache, a dizziness/stupor, drowsiness, sleep disorders; seldom - unpleasant feelings, for example, paresthesia in brushes, trembling, concern, conditions of fear, attacks of spasms and confusion of consciousness; very seldom - a visual disturbance and hearing, disturbance of taste and sense of smell, disturbance of feeling of a touch, and also psychotic reactions, such as hallucinations and depressive changes of mood; disorders of processes of the movement, including during walking.
From cardiovascular system: seldom - tachycardia, a lowering of arterial pressure; very seldom – a collapse, similar to shock.
From a musculoskeletal system: seldom - damage of sinews, including their inflammation, a joint pain or muscles; very seldom - a rupture of a sinew (for example, a rupture of an Achilles sinew). This side effect can be shown for 48 hours from an initiation of treatment and affect an Achilles sinew of both legs. Muscular weakness which can have special value for patients with a heavy myasthenia is possible; in isolated cases - damages of muscles (рабдомиолиз).
From a liver: the raised indicators of hepatic enzymes (for example, ALT, nuclear heating plant); in certain cases - the raised indicators of bilirubin and creatinine of blood serum; very seldom - hepatic reactions, such as a liver inflammation.
From kidneys: deterioration in function of kidneys, up to an acute renal failure, for example, owing to allergic reactions (intersticial nephrite).
From system of blood: in certain cases - increase in quantity of certain blood cells (eosinophilia), reduction of quantity of leukocytes (leukopenia); seldom - decrease in quantity of certain leukocytes (neutropenia), reduction of quantity of thrombocytes (thrombocytopenia) that can cause the increased tendency to hemorrhages or bleedings; very seldom - considerable reduction of quantity of certain leukocytes (agranulocytosis) that can lead to heavy symptoms of a disease (long or recurrent fever, pharyngitis, the expressed painful health); in isolated cases - decrease in quantity of erythrocytes owing to their destruction (hemolitic anemia). The reduced number of all types of blood cells (pancytopenia).
Others: often - pain and reddening in the place of infusion; inflammation of veins (phlebitis); 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 a human body. For this reason consecutive infection which will demand additional treatment can develop.
Interaction with other medicines:
Though in clinical trials interactions between levofloksatsiny and theophylline, however 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 are not established. Concentration of a levofloksatsin in the presence of a fenbufen was about 13% higher, than at reception only a levofloksatsina.
Probenitsid and Cimetidinum statistically authentically influence removal of a levofloksatsin. The renal clearance of a levofloksatsin decreases in the presence of a probenitsid by 34%, and Cimetidinum – for 24%. Thanks to it both drugs are capable to block canalicular excretion of a levofloksatsin. The period of semi-life of cyclosporine increases by 33% at a concomitant use with levofloksatsiny.
At simultaneous use with antagonists of vitamin K, for example, warfarin, coagulative tests (PCh/the international normalized ratio) and/or bleedings which can be expressed raise. Therefore patients who receive in parallel antagonists of vitamin K need to exercise control of indicators of coagulation.
Use of a levofloksatsin along with alcohol is not recommended.
Contraindications:
Hypersensitivity to a levofloksatsin or to other hinolona. Epilepsy, patients with complaints to side reactions from sinews after the previous use of hinolon. Period of pregnancy and feeding by a breast. Children's age up to 18 years.
Overdose:
Symptoms: confusion and disturbance of consciousness, dizziness, attacks of spasms. At use of doses above therapeutic lengthening of a QT interval is observed.
Treatment: therapy is symptomatic.
In cases of overdose careful observation of the patient, including an ECG is made. The hemodialysis, including peritoneal dialysis or HAPD, is not effective for removal of a levofloksatsin from an organism. There are no specific antidotes.
Use during pregnancy or feeding by a breast.
During pregnancy or feeding by a breast use of drug is contraindicated.
Children.
Drug is not used to children and teenagers aged up to 18 years.
Storage conditions:
Period of validity. 2 years of date of production of in bulk. To store in original packaging at a temperature not above 25 °C. Not to freeze. To store in the place, unavailable to children.
Issue conditions:
According to the recipe
Packaging:
On 100 ml of solution in hermetically to the corked bottle with measured divisions from dense polyethylene, 1 bottle in a pack.
