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1 ml of almost transparent solution contains 4 mg of a pefloksatsin in the form of a mezilat (1 large bottle – 400 mg).
1 tablet contains 400 mg of an antibiotic of Pefloksatsin in the form of Methansulfonas natricum in a cover.
The medicine Pefloksatsin is issued in the tableted form, in the form of solution. Solution is packed into large bottles on 100 ml, tablets – into blisters.
In each cardboard pack there is an instruction from the producer, 1 bottle from dark glass or 1-2 blisters with tablets on 10 pieces.
Antimicrobic medicine. Active ingredient belongs to group of ftorkhinolon. The principle of antimicrobic influence is based on ability of active component to block DNK-girazu, on an obstacle of replication of A-subunit of RNA, DNA, disturbance of synthesizing of bacterial proteins.
Possesses a wide range protivo-and antimicrobic influence. Concerning gram-positive microorganisms antimicrobic effect to be shown only on cells which are in process of a mitosis.
Concerning gram-negative bacteria — on cells which are in a stage of division and in a rest stage. Active agent is steady against influence beta laktamaz.
Pharmacodynamics and pharmacokinetics
Antimicrobic means is quickly soaked up from a gleam of a digestive tract after reception of a tablet inside. In 20 minutes after one-time use of 400 mg of Pefloksatsin about 90% of the accepted dose pass absorption, and the indicator of Cmax makes 4 mkg/ml and is reached in 1,5-2 hours.
After intravenous injection the indicator of Cmax is reached quicker — in 1 hour. After repeated use concentration of active antimicrobic agent in mucous bronchial tubes makes 5 mkg/ml.
Pefloksatsin is capable to contact plasma proteins of 25-30%. The operating component well gets into all fabrics in an organism and liquid:
- bronchial secret;
- cerebrospinal fluid;
- bone tissue;
- peritoneal liquid;
In above-mentioned fabrics and liquids concentration of antimicrobic substance is higher, than in blood.
After 3-fold reception of 400 mg Pefloksatsin's concentration in cerebrospinal fluid makes 4,5 mkg/ml; at increase of a dose twice this indicator reaches value of 9.8 mkg/ml, and the ratio between concentration of an antibiotic and in liquid is equal in plasma to 89%.
The metabolism is carried out in hepatic system where active agent as a result of methylation will be transformed to a dimetilpefloksatsin at whom antibacterial activity is expressed much stronger, than at his predecessor.
The metabolite is capable to be oxidized to N-oxide, and further to conjugate with glucuronic acid before formation of a pefloksatsina-glyukoronid.
At intake the indicator of T1\2 makes 8-10 hours, and at repeated use — 12-13 hours. After one-time intravenous injection of T1\2 makes 7.2-13 hours, and at repeated introduction — 14-15 hours. It is removed partially in the form of metabolites, and also in not changed view with a stake and urine (60%) through renal system.
After single use of a medicine its metabolites can be found in urine within 84 hours. At a hemodialysis the coefficient of extraction of active ingredient is equal to 23%.
Indications to use
Pefloksatsin is appointed at infectious defeats which activator is the microorganism, sensitive to an antibiotic:
- diseases of soft tissues;
- empyema of a gall bladder;
- intrahospital infections;
- intraabdominal abscesses;
- skin diseases;
- infections of eyes;
- diseases of joints and bones;
- surgical infections;
- damages of adnexal bosoms;
- damages of a middle ear;
- venereal ulcer;
- diseases of ENT organs;
- infections of a respiratory path;
- damages of a throat, throat.
Medicine can be applied to prevention of infectious diseases after surgical, operative measures.
- hemolitic anemia;
- pregnancy incubation period;
- individual intolerance of ftorkhinolon;
- insufficiency glyukozo-6-fosfatdegidrogenazy;
- restriction by the producer on age — till 18 flyings.
- convulsive syndrome which etiology is unknown;
- pathology of blood circulation of a brain;
- organic changes / defeats of TsNS;
- atherosclerosis of vessels of the head.
- spasms (seldom are registered);
- headaches of migrenozny type;
- fast fatigue;
- tremor of extremities;
- contagious excitation;
- cholestatic jaundice;
- abdominal pains;
- diarrheal syndrome;
- increase of the ALT, nuclear Heating Plant level;
- pseudomembranous colitis;
- hepatic necrosis;
- glomerulonephritis (is registered seldom);
- phlebitis (injection forms);
- Quincke's edema;
- skin itch;
- rupture of sinews;
- hyperemia of integuments;
- skin rashes;
Application instruction of Pefloksatsin (Way and dosage)
The scheme of treatment, selection of a single dose of Pefloksatsin is carried out in an individual order taking into account the accompanying pathology, weight of an infectious disease, localization of inflammatory process, sensitivity of flora.
The application instruction of Pefloksatsin at uncomplicated infectious diseases: twice a day on 400 mg (the average daily dosage makes 800 mg of a pefloksatsin). Tablets cannot be chewed. It is recommended to wash down with enough liquid. It is more preferable to accept on an empty stomach.
At tyazheloprotekayushchy infectious diseases the medicine is entered intravenously kapelno, previously having dissolved a medicine in 5% glucose solution (250 ml). Originally enter one-time 800 mg, further each 12 hours on 400 mg. Duration of antimicrobic therapy should not exceed 1-2 weeks.
At pathology of hepatic system correction of the scheme of treatment is carried out. At uncomplicated diseases appoint 400 mg twice a day; at hard proceeding infectious defeats – each 36 hours on 400 mg. An interval between uses of an antibiotic at the expressed defeats of hepatic system – about 2 days. Duration of antimicrobic therapy – is no more than 30 days.
At pathology of renal system it is one-time possible to enter only 50% of an expected dose. To elderly patients appoint 2/3 from an expected dose.
Medical and specialized literature does not contain the description of manifestations and a clinical picture of overdose by drug Pefloksatsin.
Carrying out posindromny therapy is recommended. The specific antidote is not developed. Carrying out a peritoneal dialysis and hemodialysis is effective.
At treatment of staphylococcal infectious diseases Pefloksatsin's combination with a beta laktamnymi antibacterial agents allows to prevent stability/resistance development.
The antibacterial synergism is noted at simultaneous therapy with Azlotsillin, Piperatsillin, Aminoglycosides, the Ceftazidime.
This effect is registered also concerning the diseases caused by a pyocyanic stick.
Decrease in a prothrombin ratio is observed at simultaneous treatment by indirect anticoagulating medicines that demands a constant control over indicators of coagulability of blood.
The antacids containing Mg and/or Al hydroxide interfere with absorption of an antibacterial component of a medicine.
Removal of active ingredient is slowed down at treatment by medicines which are capable to block canalicular secretion.
Medicine slows down the Theophylline metabolism in hepatic system that can lead to increase of its concentration in TsNS and plasma that can demand correction of the scheme of treatment.
Cimetidinum does not influence indicators of renal clearance and volumes of distribution, but at the same time is capable to reduce indicators of an elimination half-life and the general clearance of an antibiotic.
The medicine is incompatible with Heparin. Mixing with solutions which contain Cl ions because of risk of loss of rainfall is inadmissible.
Terms of sale
Transportation and storage demand observance temperature the mode – to 25 degrees.
Period of validity
Solution can be stored in large bottles and ampoules 3 years. The tableted form – 2 years.
At the diagnosed mixed infectious defeats of bodies of a small pelvis and an abdominal cavity Pefloksatsin is recommended to appoint together with other antibiotics, active concerning a mephitic gangrene (Clindamycin, Metronidazole).
Prevention of a crystalluria during antibacterial therapy consists in the use of a large amount of liquid. It is recommended to limit influence of an ultraviolet because of a possible photosensitization. The expressed pathology of renal system demands an individual approach and selection of the scheme of treatment.
At development of the long, expressed diarrhea it is necessary to conduct examinations for an exception of pseudomembranous colitis. In case of reliable confirmation of the diagnosis Pefloksatsin cancel and carry out posindromny treatment.
Coincidence on the ATH code of the 4th level:
- To Peflatsina.
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