international and chemical name: ofloxacin; (RS) - 9-ftoro-3-metil-10-(4-methylpiperazin-1-silt) - 7-oxo-2, 3-dihydro-7H-пиридо [1, 2, 3-where]-1, 4-benzoxazine-6-carboxyfishing acid;
Main physical and chemical characteristics: transparent solution of light-flavovirent color without mechanical impurity;
Structure. 100 ml of infusion solution contain an ofloksatsin of 200 mg;
other components: sodium chloride, an edetata of dinatrium a dihydrate, water for injections.
Form of production of medicine. Solution for infusions.
Farmakoterapevtichesky group. Antibacterial agents of group of hinolon. Code of automatic telephone exchange J01MA01.
Effect of the medicine. Pharmacodynamics. Ofloxacin – synthetic antimicrobic drug of the fluorinated hinolon of a broad spectrum of activity.
In the concentration identical with the minimum overwhelming concentration (M_S) or in a little highest, he shows bactericidal action (by braking DNK-girazy = the enzyme necessary for dublyuvannya and transcriptions of bacterial DNA).
The antimicrobic range covers: gram-negative and gram-positive bacteria, are sensitive to an ofloksatsin: Enterobacteriaceae (Escherichia coli, types of Citrobacter, Enterobacter, Klebsiella, Proteus, Providencia, Salmonella, Serratia, Shigella, Yersinia), Pseudomonas spp, including Pseudomonas aeruginosa, Haemophilus influenzae, Haemophilus ducreyi, Branhamella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Acinetobacter spp, Campylobacter spp, Gardnerella vaginalis, Helicobacter pylori, Pasteurella multocida, Vibrio spp, Brucella melitensis; staphylococcus, including strains that develop a penicillinase and some strains, resistant to Methicillinum; also it has activity concerning Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Ureaplasma urealyticum (at the M_S boundary values), Mycobacterium tuberculosis, Mycobacterium leprae and some other mycobacteria.
Sensitivity of streptococci of group A, B and C is boundary.
The majority of anaerobe bacterias, except for Clostridium perfringens, is resistant.
Ofloxacin inactive Treponema pallidum is relative.
Pharmacokinetics. Ofloxacin well gets into fabrics. It also well extends in body liquids, including in cerebrospinal. Its rather high concentration in bile. The volume of distribution fluctuates ranging from 1,5 to 2, 5 l/kg. Communication with plasmatic proteins makes 25%.
Ofloxacin only in limited to a measure turns into dezmetil-ofloxacin and ofloxacin-N-oxide. Dezmetil-ofloksatsin antimicrobic activity has weak.
The plasmatic half-cycle of an ofloksatsin makes about 5-8 hours, at a renal failure it lasts depending on degree of this insufficiency up to 15-60 hours. Ofloxacin is removed, generally by kidneys, tubular secretion and glomerular filtering. 75-80% of the removed dose are removed in a steady-state condition with urine within 24-48 hours, less, than 5% are brought in the form of metabolites. 4 – 8% of the removed dose are removed together with a stake. Patients can have a removal of an ofloksatsin slowly with heavy injury of a liver (for example, cirrhosis). Regardless of a dose renal allocation of an ofloksatsin makes 173 ml/minutes, the general allocation to reach 214 ml/min. Only insignificant volume can be removed by a hemodialysis (15 – 25%), the biological half-life during a hemodialysis makes about 8 - 12 hours. At a peritoneal dialysis biological half-decay fluctuates about 22 hours.
Ofloxacin shows post-antibiotichnoye action.
Ofloxacin passes through a placenta, getting to milk of nursing mothers.
Indications to use. Ofloxacin is appointed the adult for treatment of the moderately severe infections and heavy infections caused by sensitive strains of microorganisms. It is necessary to appoint ofloxacin, proceeding from results of microbiological inspection and clarification of sensitivity of this microorganism.
Lower respiratory tract infections. Infections of an ear, throat, nose. Infections of uric ways, prostatitis. Infections of bones, skin and soft tissues, including wound fevers. Vnutrennebryushny infections, including a cholangitis and infections of a small pelvis caused by sensitive microorganisms. Respiratory infections at cystous fibrosis; the pulmonary tuberculosis forms caused by mycobacteria with the mixed resistance including in the weakened patients in a combination with other antituberculous remedies. Infections which are transmitted sexually, except for syphilis. Shigellosis, salmonellosis. Sepsis, bakteriyamiya. Infections of patients with an immunodeficiency (including AIDS).
Way of use and dose. The dosage depends on type and weight of an infection and a clinical condition of the patient. If the state improves, then it is possible to continue after initial parenteral therapy by the drug "Ofloksin Inf" it by use of peroral drug (Ofloksin 200, tablets, coated) in that dosing. In general ofloxacin is applied within 7 – 10 days.
Adult patients with normal function of kidneys
The usual single dose is equal to 200 - 400 mg of an ofloksatsin (1 – 2 infusional bottles of Ofloksin Inf) in the range of 12 hours.
Patients with the lowered function of kidneys
Þ the clearance of creatinine – is higher for 50 ml/minutes.:
dosages do not need to be reduced;
Þ clearance of creatinine – 20 - 50 ml/minutes.:
the first dose of 200 mg, then 100 mg of 1 times for 24 hours;
Þ the clearance of creatinine – is lower than 20 ml/minutes.:
the first dose of 200 mg, then 100 mg of 1 times for 48 hours.
Patients with a severe damage of a liver
It is impossible to exceed a dose in days – 400 mg of an ofloksatsin.
Way of introduction: 1 infusional bottle of the drug "Ofloksin Inf" is entered intravenously within not less than 30 minutes.
100 ml of the drug "Ofloksin Inf" include 15, 4 mmol of ions of Na + and 15, 9 mmol of ions Sl-.
With the drug "Ofloksin Inf" you should not enter any other solutions and medicines into an infusional bottle. Ofloksin Inf is compatible to the following solutions: normal saline solution, 5% glucose, 10% glucose, solution Ringer of a lactate, Hartman's solution, % bicarbonate 4, 2.
Ofloksin Inf is incompatible with heparin and Mannitolum.
The rest of unused drug needs to be liquidated it agrees with the recipe. It cannot be kept in the refrigerator, to freeze or hold in any other way for possible further use.
Side effect. Side effects do not happen, as a rule, difficult character. Such disturbances of digestion as nausea, vomiting, a diarrhea were described. In isolated cases noted an abdominal pain, lack of appetite, dryness in a mouth, a meteorism, a lock. Sometimes neurologic complications – a headache, sleeplessness, dizziness, occasionally nervousness, misting of consciousness, trembling, drowsiness, hallucinations meet. Further observed an enanthesis and an itch, allergic reactions, vision disorders (deterioration in sight, doubling in eyes, disturbances of perception of color), a hearing disorder and balance, disturbance to a scent, a photosensitization. Noted excitement, anemia, thrombocytopenia, a leukopenia, a neutropenia, an agranulocytosis.
Intravenous administration of an ofloksatsin can be followed by tachycardia and to blood pressure drop.
At intravenous administration of an ofloksatsin can come irritations of a vein, on average lines from an injection site which is followed by reddening and morbidity (existence grows depending on speed raised injections). These by-effects disappear within several hours after the end of injection or when changing an injection site. They, as a rule, do not need a therapy suspension. In certain cases thrombophlebitis can be observed.
In some cases at treatment by ftorovanny hinolona observed an inflammation of sinews that can even lead to its gap. Risk factor for development such the inflammation (tendinitis) at treatment by ftorovanny hinolona is, including, simultaneous treatment by corticosteroid drugs. The suspicion on an inflammation of sinews is the reason for a suspension of a course of treatment ofloksatsiny.
Contraindications. Hypersensitivity to an ofloksatsin or other component of drug, or to antimicrobic means of a hinolon is known.
Also feeding by a breast is contraindicated to use drug during pregnancy.
Children's and teenage age (till 18 flyings), epilepsy, dysfunction of TsNS with a reduced convulsive threshold (craniocereberal injuries, a stroke, inflammatory diseases of TsNS).
Overdose. Overdose symptoms: dizziness, misting of consciousness, block, vomiting. Processing overdose includes standard reception, treatments is symptomatic and auxiliary, focusing attention on ensuring zhiznennoznachimy functions. Ofloxacin, is generally removed by kidneys (75 – 80% of the entered dose are removed in a steady-state condition together with urine within 24 – 48 hours), its elimination can be accelerated by the forced volume diuresis. Only in the ofloxacin limited quantities it is possible to remove from an organism with a hemodialysis (on average 15 – 25%) or a peritoneal dialysis (less than 2%).
Features of use. Care is necessary at patients with atherosclerosis of the main vessels. Continuous supervision at the combined use with insulin, caffeine, theophylline, dimetadinum, cyclosporine, non-steroidal anti-inflammatory drugs anticoagulants is necessary.
At fast intravenous administration perhaps falling of arterial pressure.
During a course of treatment it is not recommended to take alcoholic beverages.
At treatment ofloksatsiny it is worth avoiding solar radiation or exposure of UF of light of other sources.
Drug can do adverse action on activity which demands in special attention, coordination of movements, the high speed of mental and physical reactions (for example, control of vehicles, service of cars, work at height, etc.).
Interaction with other medicines. At simultaneous use of an ofloksatsin with nonsteroid antirheumatic means or medicines which reduce a threshold of spasms the risk of development of spasms can grow.
Simultaneous introduction of an ofloksatsin with procaineamide can lead to increase of level of procaineamide – at patients it is necessary to carry out careful monitoring of level of procaineamide in plasma, an ECG and in case of requirement to pick up its dosages.
At simultaneous use of an ofloksatsin with anti-hypertensive means or anestetichesky barbiturates it is possible to observe in some cases sudden blood pressure drop.
Simultaneous introduction of an ofloksatsin with theophylline can give in isolated cases to decrease theophylline removal which, however, does not happen clinically reliable.
Simultaneous introduction of an ofloksatsin in large doses with medicines which are emitted by tubular secretion can lead to increase of plasmatic concentration through them are reduced removal.
At simultaneous introduction with warfarin or its derivatives it is necessary to watch after prothrombin hour or to conduct other corresponding researches on turnings.
Considering on a possible hyperglycemia or a hypoglycemia at introduction of an ofloksatsin at patients who were treated antidiabetic means, it is necessary to carry out monitoring of parameters of their compensation surely. During treatment ofloksatsiny pseudo-positive results when determining opiates or porphyrines in urine can be observed.
Conditions and periods of storage. Drug needs to be kept in the unavailable to children, dry, protected from light place at a temperature of 10 - 25 °C. A period of validity – 3 years.