Tab. ofloxacin 0,2 No. 10

General characteristics. Structure:

International and chemical names: ofloxacin; (±)-9-ftor-2,3-digidro-3-metil-10-(4-methyl-1 - piperazinit) - 7-oxo-7H-пиридо [1,2,3-de] - 1,4-benzoxazine-6-carboxylic acid; main physical and chemical properties: tablets of color, white with a yellowish shade; structure: 1 tablet contains an ofloksatsin of 0,2 g; excipients: lactoses monohydrate, potato starch, magnesium stearate, stearic acid, sodium of a kroskarmelloz.

Pharmacological properties:

Pharmacodynamics. Antibacterial agent of a broad spectrum of activity from group of ftorkhinolon. Works bakteritsidno. Inhibits DNK-girazu bacteria (topoisomerase II and IV), breaks process of superspiralling and a stitching of ruptures of DNA, cell fission oppresses, causes structural changes of cytoplasm and death of microorganisms.
It is highly active concerning the majority of gram-negative bacteria: Escherichia coli, Salmonella spp., Shigella spp., Proteus spp., Morganella morganii, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia spp., Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitides, Mycoplasma spp., Legionella pneumophila, Acinetobacter spp., Chlamydia spp.
It is active concerning some gram-positive microorganisms, including Staphylococcus spp., Streptococcus spp. (especially β-hemolitic streptococci).
Cross resistance of bacteria to an ofloksatsin and other ftorkhinolona is possible.
Are moderately sensitive to an ofloksatsin of Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas spp.
Anaerobic bacteria (except Bacteroides ureolyticus), viruses, mushrooms, the elementary are insensitive to drug.
Ofloxacin is steady against action β-лактамаз.

Pharmacokinetics. Absolute bioavailability – 96% is completely soaked up in digestive tract (about 95%). The maximum concentration is reached in 1 – 2 hour, depends on a dose: after intake of 100 mg, 300 mg and 600 mg it makes 1 mg/l, 3,4 mg/l and 6,9 mg/l respectively. About 25% contact proteins of plasma. The seeming distribution volume – 100 l. Semi-removal time (irrespective of a dose) – 4,5 – 7 hours. Gets into cells (leukocytes, alveolar macrophages) most bodies and fabrics, creates high concentration in urine, bile, saliva, a phlegm, a prostate secret, kidneys, a liver, a gall bladder, skin, lungs, gets through a blood-brain barrier and a placental barrier. In a liver (about 5%) turns into N-oxide of an ofloksatsin and деметилофлоксацин.
It is removed preferential by kidneys in an invariable look (80 – 90%); a small part is allocated with bile, excrements, breast milk (the extrarenal clearance makes less than 20%). After single use in 200 mg it is found in urine within 20 - 24 hours.

Indications to use:

Treatment of the infections caused by microorganisms, sensitive to an ofloksatsin:
– ENT organs (sinusitis, pharyngitis, average otitis, laryngitis, tracheitis);
– respiratory tracts (acute and chronic bronchitis, pneumonia);
– skin and soft tissues, heavy wound fevers;
– bones and joints (including osteomyelitis);
 urinary tract (cystitis, urethritis, pyelonephritis);
 bodies of a small pelvis and generative organs (a salpingitis, an endometritis, a parametritis, a cervicitis, a colpitis, prostatitis, an oophoritis, an orchitis, an epididymite, including caused gonokokky, chlamydias);
– infectious and inflammatory processes of an abdominal cavity (peritonitis, acute pancreatitis);
– digestive tract infections (typhoid, salmonellosis, shigellosis) and biliary tract (cholecystitis, cholangitis);   
– a septicaemia (together with intravenous administration of drug);
– endocarditis;
– prevention of infections at patients with the weakened immunity or a neutropenia, and also in the postoperative period at surgical patients.

Route of administration and doses:

The dose depends on a species of microorganism and severity of an infection, age, body weight and function of kidneys of the patient. In most cases the course of treatment makes 7 – 10 days, it is necessary to continue treatment 2 - 3 more days after elimination of symptoms of an infection. At the heavy and complicated infections therapy can be prolonged. The dose of drug makes from 200 mg of 1 times a day to 400 mg a day in 2 receptions. The dose of drug of 400 mg (2 tablets) can be accepted at one time, it is better in the morning. The single dose in a dose of 400 mg can be recommended at acute uncomplicated gonorrhea. At a renal failure the dose is established taking into account degree of manifestation of a renal failure and clearance of creatinine. The recommended initial dose of drug at a renal failure makes 200 mg; further the dose is korrigirut taking into account clearance of creatinine: at value of an indicator of 50 - 20 ml/min. – in a usual dose each 24 h; less than 20 ml/min. – 100 mg (1/2 tablets) each 24 h.

Features of use:

With care appoint to patients with atherosclerosis of vessels of a brain.
During treatment it is necessary to avoid stay to the sun and UF-radiations; it is recommended to abstain from the activity demanding speed of psychomotor reactions (management of transport, works with potentially dangerous mechanisms) and alcohol intake.
For prevention of development of a crystalluria it is necessary to provide the sufficient drinking mode.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, discomfort in a stomach, anorexia; seldom – stomatitis, increase in activity of liver enzymes.
From the central nervous system: dizziness, headache, sleep disorder, photophobia, weakness.
Allergic reactions: rash, fever, itch, hypostases.
Others: seldom – a heart consciousness, a cheilitis, thirst, a photosensitization.

Interaction with other medicines:

Antacids (drugs of aluminum and magnesium), gland sulfate, salt laxatives, сукральфат, zinc, Dedalonum – reduce absorption and reduce activity of an ofloksatsin (the interval between receptions has to be not less than 2 hours); пробеницид, Cimetidinum, furosemide and a methotrexate slow down removal and can increase toxicity of an ofloksatsin.
At simultaneous use of an ofloksatsin with β-laktamny antibiotics, aminoglycosides and metronidazole the additive interaction is noted.

Contraindications:

Pregnancy, feeding by a breast. Children's and teenage age (up to 16 years). The increased individual sensitivity to an ofloksatsin or other ftorkhi-nolona.

Overdose:

Symptoms: drowsiness, nausea, vomiting, dizziness, disorientation, block, confusion of consciousness.
Treatment: gastric lavage, maintenance of the vital functions.

Storage conditions:

To store in the dry, protected from light place at a temperature from 15 °C to 25 °C.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging.