Ofloksatsin-Borimed

General characteristics. Structure:

Active ingredient: 200 mg of an ofloksatsin in each tablet.

Excipients: cellulose microcrystallic, povidone, calcium stearate, talc, starch 1500, опадрай (including the polyvinyl alcohol which is partially hydrolyzed a macrogoal 3350, talc, lecithin (soy), titanium dioxide (Е 171), an aluminum varnish on the basis of carmoisin (Е 122), an aluminum varnish on the basis of indigo a carmine (Е 132)).

Pharmacological properties:

Pharmacodynamics. Antimicrobic drug of a broad spectrum of activity 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.

Drug is active concerning the microorganisms producing beta lactamelements and fast-growing atypical mycobacteria.

Are sensitive to drug: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris - an indole - positive and an indole - negative strains), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campylobacter 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, Brucella spp.

Have various sensitivity to drug: Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Serrratia marcescens, Pseudomonas aeruginosa, Acinetobacter spp., Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacteriurn fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

Nocardia asteroides, anaerobic bacteria are steady against drug (Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile).

Drug is inactive concerning Treponema pallidum.

Pharmacokinetics. After administration of drug inside absorption bystry and full (95%). Bioavailability - more than 96%.

Distribution. Linkng with proteins of plasma – 25%. After a single dose of drug in a dose of 200 mg and 400 mg of Cmax makes 2,5 mkg/ml and 5 mkg/ml, respectively. Meal can slow down absorption, but has no significant effect on bioavailability.

The seeming Vd - 100 l. Ofloxacin is distributed in leukocytes, alveolar macrophages, skin, soft tissues, bones, abdominal organs and a small pelvis, respiratory system, urine, saliva, bile, a prostate secret. Well gets through a blood-brain and placental barrier, it is allocated with breast milk. Gets into cerebrospinal fluid at the inflamed and uninflammed meninx (14-60%). Does not kumulirut.

Metabolism. N-oxide of an ofloksatsin and dimetilofloksatsin is metabolized in a liver (about 5%) with education.

Removal. T1/2 is 4,5-7 h (irrespective of a dose). It is removed by kidneys in not changed look – 75-90%, with bile - about 4%. Extrarenal clearance - less than 20%.

After single use in a dose of 200 mg in urine it is found during 20-24 h.

Pharmacokinetics in special clinical cases. At a renal or liver failure removal can be slowed down.

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 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 (orchitis, epididymite);

– gonorrhea;

– clamidiosis;

– meningitis.

Route of administration and doses:

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.

Drug is appointed inside the adult - on 200 - 800 mg/days, frequency rate of use - 2 times/days. A course of treatment – 7 - 10 days. It is possible to appoint a dose to 400 mg/days in 1 reception, it is preferable in the morning.

At acute 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 purpose of 2 times/days, or the full single dose is appointed by 1 times/days. At clearance of creatinine less than 20 ml/min. a single dose - 200 mg, then - on 100 mg/days each 24 h.

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

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

Pill should be taken entirely, washing down with a full glass of water, to or during meal.

Duration of a course of treatment is defined by sensitivity of the activator and a clinical picture.

At treatment of salmonelloses a course of treatment – 7 - 8 days, at uncomplicated infections of the lower urinary tract – 3 - 5 days.

Drug should be used during a full course of the treatment appointed by the doctor.

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 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.

It is necessary to consider that at use Ofloksatsin-Borimed 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 Ofloksatsin-Borimed 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:

Side effects arise at 4 – 8% of patients.

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 the central nervous system: headache, dizziness, uncertainty of movements, tremor, spasms, numbness and paresthesias of extremities, 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 antacids containing aluminum, calcium, magnesium, or salts of iron reduce absorption of an ofloksatsin, forming insoluble complexes, these drugs should be accepted in 2 hours prior to or after reception Ofloksatsin-Borimed.

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 appointment Ofloksatsin-Borimed with the non-steroidal anti-inflammatory drugs derivative of a nitroimidazole and methylxanthines raises risk of development of neurotoxic effects.

At co-administration Ofloksatsin-Borimed with glucocorticosteroids raises risk of a rupture of sinews, especially at elderly people.

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

Precautionary measures. 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, QT lengthening, organic lesions of the central nervous system.

Pregnancy and lactation. Drug is contraindicated to use at pregnancy and in the period of a lactation (breastfeeding).

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 the central nervous system);

– damage of sinews at earlier carried out treatment of a ftorkhinolonama;

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

– pregnancy;

– lactation (breastfeeding);

– hypersensitivity to drug components.

Overdose:

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

Treatment: gastric lavage, purpose of symptomatic therapy.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use medicine after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging No. 10х1, No. 10х2, No. 10х3, No. 10х4.