Producer: Zentiva (Zentiva) Czech Republic
Code of automatic telephone exchange: J01MA01
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agent: ofloxacin - 400 mg.
Excipients: lactoses monohydrate, starch corn, povidone, кросповидон, half-oxameasures, magnesium stearate, talc; cover: gipromelloza, macrogoal, titanium dioxide, talc.
White or almost white, biconvex, oblong tablets, film coated, with risky for division on both sides and an engraving "400" on the one hand.
Pharmacodynamics. Antimicrobic broad-spectrum agent from group of ftorkhinolon, affects bacterial DNK-girazu enzyme, the providing superspiralling and, thus, stability of DNA of bacteria (destabilization of chains of DNA leads to their death). Renders bactericidal effect.
It is active concerning the microorganisms producing beta lactamelements and fast-growing atypical mycobacteria. Are sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter, Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafhia, Proteus spp. (including Proteus mirabilis, Proteus vulgaris - an indole - positive and an indole - negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campilobacter jejuni, Aeromonas hydrophila, Plesiomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Staphylococcus spp., Brucella spp.
Have various sensitivity to drug: Enterococcus faecalis, Streptococcus pyogenes, pneumoniae and viridans, Serratio marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and pneumoniae, Mycobacterium tuberculosis, and also Mycobacterium fortuim, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.
Are in most cases insensitive: Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile). He acts on Treponema pallidum.
Pharmacokinetics. Absorption after intake bystry and full (95%). Bioavailability - over 96%, communication with proteins of plasma - 25%, time of achievement of the maximum concentration (Tstakh) at oral administration - 1-2 h, the maximum concentration (Stakh) after reception in a dose of 100 mg, 300 mg 600 mg makes 1, 3, 4 and 6.9 mg/l and depends on a dose: after a single dose of 200 mg and 400 mg it makes 2.5 mkg/ml and 5 mkg/ml, respectively. Food can slow down absorption, but has no significant effect on bioavailability.
The seeming distribution volume - 100 l. Distribution: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal organs and a small pelvis, the respiratory system, urine, saliva, bile, a prostate secret, well gets through a blood-brain barrier, a placental barrier, cosecretes with maternal milk. Gets into cerebrospinal fluid at the inflamed and uninflammed meninx (14-60%).
N-oxide of an ofloksatsin and dimetilofloksatsin is metabolized in a liver (about 5%) with education. An elimination half-life - 4.5-7 h (irrespective of a dose). It is removed by kidneys - 75-90% (in not changed look), about 4% - with bile. Extrarenal clearance - less than 20%.
After single use in a dose of 200 mg in urine it is found during 20-24 h. At a renal/liver failure removal can be slowed down. Does not kumulirut. At a hemodialysis 10-30% of drug are removed.
Indications to use:
Respiratory infections (bronchitis, pneumonia), ENT organs (sinusitis, pharyngitis, average otitis, laryngitis), skin, soft tissues, bones, joints, infectious and inflammatory diseases of an abdominal cavity and biliary tract (except for bacterial enteritis), kidneys (pyelonephritis), urinary tract (cystitis, an urethritis), bodies of a small pelvis (an endometritis, a salpingitis, an oophoritis, a cervicitis, a parametritis, prostatitis), generative organs (a colpitis, an orchitis, an epididymite), gonorrhea, clamidiosis; a septicaemia (only for in/in introductions), meningitis; prevention of infections at patients with disturbance of the immune status (including at a neutropenia).
Route of administration and doses:
Inside. Doses are selected individually depending on localization and weight of a course of an infection, and also sensitivity of microorganisms, the general condition of the patient and function of a liver and kidneys.
The adult - on 200-800 mg a day, a course of treatment - 7-10 days, frequency rate of use - 2 times a day. It is possible to appoint a dose to 400 mg a day in 1 reception, it is preferable in the morning. At gonorrhea - 400 mg once.
At patients with renal failures (at clearance of creatinine of 50-20 ml/min.) the single dose has to make 50% of an average dose at frequency rate of appointment 2 times a day, or the full single dose is entered 1 time a day. At clearance of creatinine less than 20 ml/min. a single dose - 200 mg, then - on 100 mg a day every other day.
At a hemodialysis and peritoneal dialysis - on 100 mg each 24 h. The maximum daily dose at a liver failure - 400 mg/days.
Pill is taken entirely, washing down with water to or during food. Duration of a course of treatment is defined by sensitivity of the activator and a clinical picture; it is necessary to continue treatment at least 3 more days after disappearance of symptoms of a disease and full normalization of temperature. At treatment of salmonelloses a course of treatment - 7-8 days, at uncomplicated infections of the lower urinary tract a course of treatment - 3-5 days.
Features of use:
Is not choice drug at the pneumonia caused by pneumococci. It is not shown at treatment of acute tonsillitis.
It is not recommended to apply more than 2 months, to be affected by sunshine, to uviolizing (mercury-quartz lamps, a sunbed).
In case of side effects from the central nervous system, allergic reactions, pseudomembranous colitis drug withdrawal is necessary. At the pseudomembranous colitis confirmed kolonoskopichesk and/or histologically peroral purpose of Vancomycinum and metronidazole is shown.
Seldom arising tendinitis can lead to a rupture of sinews (preferential an Achilles tendon), especially at elderly patients. In case of signs of a tendinitis, it is necessary to stop immediately treatment, to make an immobilization of an Achilles tendon and to consult at the orthopedist.
During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions it is impossible to use ethanol.
At drug use women are not recommended to use tampons, in connection with the increased risk of development of the milkwoman.
Against the background of treatment deterioration in a current of a myasthenia, increase of attacks of a porphyria at predisposed patients is possible.
Can result in false-negative results at bacteriological diagnosis of tuberculosis (interferes with Mycobacterium tuberculosis allocation).
At patients with abnormal liver functions or kidneys control of concentration of an ofloksatsin in plasma is necessary. At a heavy renal and liver failure the risk of development of toxic effects increases (dose adjustment is required).
At children it is applied only at threat of life, taking into account estimated advantage and potential risk of development of side effects when it is impossible to use other, less toxic drugs. An average daily dose in this case - 7.5 mg/kg, maximum - 15 mg/kg.
From the alimentary system: gastralgia, anorexia, nausea, vomiting, diarrhea, meteorism, abdominal pains, increase in activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous coloenteritis.
From a nervous system: headache, dizziness, uncertainty of movements, tremor, spasms, numbness and paresthesias of extremities, intensive dreams, "dreadful" dreams, psychotic reactions, uneasiness, condition of excitement, phobia, depression, confusion of consciousness, hallucination, increase in intracranial pressure.
From a musculoskeletal system: the tendinitis, mialgiya, arthralgias, tendosinovit, a rupture of a sinew.
From sense bodys: disturbance of color perception, diplopia, disturbances of taste, sense of smell, hearing and balance.
From cardiovascular system: tachycardia, lowering of arterial pressure, vasculitis, collapse.
Allergic reactions: skin rash, itch, small tortoiseshell, allergic pneumonitis, allergic nephrite, eosinophilia, fever, Quincke's edema, bronchospasm, Stephens-Johnson and Layell's syndrome, photosensitization, multiformny exudative erythema, acute anaphylaxis.
From integuments: dot hemorrhages (petechias), dermatitis violent hemorrhagic, papular rash with a crust, testimonial of defeat of vessels (vasculitis).
From bodies of a hemopoiesis: leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolitic and aplastic anemia.
From an urinary system: acute intersticial nephrite, renal failure, giperkreatininemiya, increase in content of urea.
Others: dysbacteriosis, superinfection, a hypoglycemia (at patients with a diabetes mellitus), a vaginitis.
Interaction with other medicines:
The foodstuff, antacids containing A13+, Sa2+ of Mg2 + or iron salts, reduce absorption of an ofloksatsin, forming insoluble complexes (time interval between purpose of these drugs has to be not less than 2 h).
Reduces clearance of theophylline by 25% (at simultaneous use it is necessary to reduce a theophylline dose).
Cimetidinum, furosemide, methotrexate and drugs blocking canalicular secretion - increase concentration of an ofloksatsin in plasma.
Increases concentration of Glibenclamidum in plasma.
At a concomitant use with antagonists of vitamin K it is necessary to exercise control of coagulant system of blood.
At appointment with the non-steroidal anti-inflammatory drugs derivative of a nitroimidazole and methylxanthines the risk of development of neurotoxic effects increases.
At co-administration with glucocorticosteroids the risk of a rupture of sinews, especially at elderly people increases.
At appointment with the drugs alkalizing urine (karboangidraza inhibitors, citrates, sodium bicarbonate), the risk of a crystalluria and nephrotoxic effects increases.
Hypersensitivity, deficit glyukozo-6-fosfatdegidrogenazy, epilepsy (including in the anamnesis), decrease in a convulsive threshold (including after a cherepnomozgovy injury, a stroke or inflammatory processes in the central nervous system); age up to 18 years (growth of a skeleton is not completed yet), pregnancy, the lactation period.
With care - atherosclerosis of vessels of a brain, disturbance of cerebral circulation (in the anamnesis), a chronic renal failure, organic lesions of the central nervous system.
List B. In the dry place, at a temperature from 10 °C to 25 °C. To store in places, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.
According to the recipe
Tablets, coated, on 400 mg.
On 10 tablets in the blister from aluminum foil / ПВХ-пленки. Each blister together with the application instruction is placed in a cardboard pack.