Ofloxacin

General characteristics. Structure:

Active agent: ofloxacin - 200 mg, 400 mg. Excipients: starch corn, cellulose microcrystallic, talc, povidone (polyvinylpirrolidone low-molecular), calcium stearate, silicon dioxide colloid (aerosil). Cover: gipromelloz (oksipropilmetiltsellyuloz), talc, titanium dioxide, propylene glycol, macrogoal 4000 (poly(ethylene oxide) 4000).

Pharmacological properties:

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 spp., Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris - indolpositive and indolnegative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campylobacter jejuni, Aeromonas hydrophila, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acne, Brucella spp. Have various sensitivity to drug: Enterococcus faecalis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter spp, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, 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., Eubacter 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 at oral administration - 1-2 h, the maximum concentration after reception in a dose of 600 mg makes 6.9 mg/l respectively and depends on a dose: after a single dose of 200 and 400 mg it makes 2.5 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 small pelvis, respiratory system, urine, saliva, bile, prostate secret; well gets through a blood-brain barrier, a placental barrier, cosecretes with maternal milk. Gets into cerebrospinal fluid (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:

— infectious and inflammatory respiratory diseases (bronchitis, pneumonia);

— infectious and inflammatory diseases of ENT organs (sinusitis, pharyngitis, average otitis, laryngitis);

— infectious and inflammatory diseases of skin and soft tissues;

— infectious and inflammatory diseases of bones and joints;

— infectious and inflammatory diseases of an abdominal cavity (including GIT infections) and biliary tract;

— infectious and inflammatory diseases of kidneys (pyelonephritis) and urinary tract (cystitis, urethritis);

— infectious and inflammatory diseases of bodies of a small pelvis (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis) and generative organs (colpitis, orchitis, epididymite);

— gonorrhea;

— clamidiosis;

— 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, weight of a course of an infection, sensitivity of microorganisms, and also the general condition of the patient and function of a liver and kidneys.
The adult - on 200-600 mg/days, 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/days in 1 reception, it is preferable in the morning. At gonorrhea - 400 mg once. At heavy infections or at treatment of patients with excess body weight, the daily dose can be increased to 800 mg.
The maximum daily dose at a liver failure - 400 mg/days.
For prevention of infections at patients with the expressed decrease in immunity - on 400-600 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 body 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.

More than 2 months are not recommended to use drug. It is necessary to avoid influence of sunshine, to radiation by UV rays (mercury-quartz lamps, a sunbed).

In case of side effects from TsNS, 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.

It is necessary to consider that at use of Ofloksatsina-AKOS seldom arising tendinitis can lead to a rupture of sinews (preferential an Achilles tendon), especially at elderly patients. In case of symptoms of a tendinitis it is necessary to stop immediately treatment, to carry out an immobilization of an Achilles tendon and to consult at the orthopedist.

At drug use women are not recommended to use tampons like tampax, in connection with the increased risk of development of vaginal candidiasis.

Against the background of treatment deterioration in a current of a myasthenia, increase of attacks of a porphyria at predisposed patients is possible.

At use of drug false-negative results at bacteriological diagnosis of tuberculosis are possible (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).

During treatment by drug it is necessary to avoid alcohol intake.

Use in pediatrics

At children of Ofloksatsin-AKOS appoint 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.

Influence on ability to driving of motor transport and to control of mechanisms

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.

Side effects:

From the alimentary system: anorexia, nausea, vomiting, diarrhea, meteorism, abdominal pains (including gastralgia), increase in activity of hepatic transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous coloenteritis.

From TsNS: headache, dizziness, uncertainty of movements, tremor, spasms, numbness and paresthesias of extremities, intensive dreams, dreadful dreams, psychotic reactions, uneasiness, hypererethism, phobias, depression, confusion of consciousness, hallucination, increase in intracranial pressure; disturbance of color perception, diplopia, disturbances of taste, sense of smell, hearing and balance.

From a musculoskeletal system: the tendinitis, mialgiya, arthralgias, tendosinovit, a rupture of a sinew.

From cardiovascular system: tachycardia, vasculitis, collapse.

From integuments: dot hemorrhages (petechias), dermatitis violent hemorrhagic, papular rash, 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.

Allergic reactions: skin rash, itch, small tortoiseshell, allergic pneumonitis, allergic nephrite, eosinophilia, fever, Quincke's edema, bronchospasm, Stephens-Johnson's syndrome, Lyell's disease, photosensitization, multiformny erythema; seldom - an acute anaphylaxis.

Others: dysbacteriosis, superinfection, a hypoglycemia (at patients with a diabetes mellitus), a vaginitis.

Interaction with other medicines:

The foodstuff, antacids containing aluminum, calcium, magnesium, or salts of iron reduce absorption of an ofloksatsin, forming insoluble complexes (therefore the interval between purpose of Ofloksatsina-AKOS and these drugs has to be not less than 2 h).

Ofloxacin reduces clearance of theophylline by 25%. Therefore 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.

Ofloxacin increases concentration of Glibenclamidum in plasma.

At a concomitant use of an ofloksatsin with antagonists of vitamin K it is necessary to control system of a blood coagulation.

At purpose of Ofloksatsina-AKOS with NPVS, derivatives of a nitroimidazole and methylxanthines the risk of development of neurotoxic effects increases.

At co-administration of Ofloksatsina-AKOS with glucocorticosteroids the risk of a rupture of sinews, especially at elderly people increases.

At purpose of Ofloksatsina-AKOS with the drugs alkalizing urine (karboangidraza inhibitors, citrates, sodium bicarbonate), the risk of development of a crystalluria and nephrotoxic effects increases.

Contraindications:

— deficit glyukozo-6-fosfatdegidrogenazy;

— epilepsy (including in the anamnesis);

— decrease in a convulsive threshold (including after a craniocereberal injury, a stroke or inflammatory processes in TsNS);

— age up to 18 years (since growth of a skeleton is not complete);

— pregnancy;

— lactation (breastfeeding);

— hypersensitivity to drug components.

With care it is necessary to appoint drug at atherosclerosis of vessels of a brain, disturbances of cerebral circulation (in the anamnesis), a chronic renal failure, organic lesions of TsNS.

 

Use of the drug OFLOXACIN at pregnancy and feeding by a breast
Drug is contraindicated to use at pregnancy and in the period of a lactation (breastfeeding).

 

Use at abnormal liver functions
The maximum daily dose at a liver failure - 400 mg/days.

 

Use at renal failures
At patients with renal failures (at KK from 50 to 20 ml/min.) the single dose has to make 50% of an average dose at frequency rate of appointment 2, or the full single dose is appointed 1 time / At KK <20 ml/min. a single dose - 200 mg, then - on 100 mg / every other day.

At a hemodialysis and peritoneal dialysis drug is appointed on 100 mg by each 24 h.

 

Use for children
Drug is contraindicated to children and teenagers up to 18 years since growth of a skeleton is not complete.

At children of Ofloksatsin-AKOS appoint 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.

Overdose:

Symptoms: dizziness, confusion of consciousness, block, disorientation, drowsiness, vomiting.

Treatment: gastric lavage, purpose of symptomatic therapy.

Storage conditions:

List B. Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,2 g in packaging on 10 pieces.

Tablets on 0,4 g in packaging on 10 pieces.