Ofloxacin

General characteristics. Structure:

Acting substance: 200 mg of an ofloksatsin.

Excipients: starch corn, lactose, magnesium stearate.

Antimicrobic broad-spectrum agent.

Pharmacological properties:

Pharmacodynamics. Ofloxacin is active concerning a wide range of gram-positive and gram-negative aerobic and anaerobic bacteria, has bactericidal effect on microorganisms, sensitive to it, inhibition DNK-girazy.

Ofloxacin is active concerning the majority of strains of the following microorganisms: Chlamydia trachomatis, Citrobacter diversus, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes.

Ofloxacin shows in vitro a minimum of the inhibiting concentration of 2 mkg/ml and less against the majority of gram-positive aerobes: Enterococcus faecalis, Staphylococcus epidermidis (including the strains steady against Methicillinum), Staphylococcus saprophyticus, Streptococcus agalactiae (group B); gram-negative aerobes: Acinetobacter calcoaceticus, Aeromonas hydrophila, Bordetella parapertussis, Bordetella pertussis, Campylobacter jejuni, Citobacter freundii, Enterobacter cloacae, Haemophilus ducreyi, Klebsiella axytoca, Moraxella (Branhalmella) catarrhalis, Morganella morganii, Neisseria miningitidis, Plesiomonas shigelloides, Proteus vulgaris, Providencia rettgeri, Providensia stuartii, Pseudomonas fluorescens, Serratia marcescens; anaerobe bacterias: Bacteroides fragilis, Bacteroides intermedius, Clostridium perfringens, Clostridium welchii, Eikenella corrodens, Gardnerella vaginalis, Peptococcus niger, Petrostreptococcus species; other organisms: Chlamydia pneumoniae, Legionella pneumophila, Mycrobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum. Ofloxacin is not active concerning Treponema pallidum.

Pharmacokinetics. After oral administration bioavailability of an ofloksatsin makes about 98%. Drug gets in high concentration into bodies and fabrics, and also into a phlegm, saliva, bile, skin, fabric and a secret of a prostate. The maximum concentration in serum is reached in 1-2 hours after administration of drug; elimination half-life about 6-7 hours.

Drug is practically not metabolized; 75-90% are removed with urine, and even after a single dose drug is found in urine during 20-24 h.

Indications to use:

At adults ofloxacin is applied to treatment of the slight and average infections caused by sensitive strains of microorganisms:

Diseases of lower parts respiratory the putey:ostry bacterial exacerbation of bronchitis, pneumonia caused by Haemophilus influenzae or Streptococcus pneumoniae.

Diseases the kozhi:neoslozhnenny diseases of skin caused by Staphylococcus aureus, Streptococcus pyogenes or Proteus mirabilis.

The diseases which are transmitted sexual the putem:ostry, uncomplicated urethral or cervical gonorrhea caused by Neisseria gonorrhoeae.

Not gonococcal urethritis and cervicitis the caused Chlamydia trachomatis.

The multi-infections of uric ways and necks of uterus caused by Chlamydia trachomatis and Neisseria gonorrhoeae.

Diseases urinary the putey:neoslozhnenny cystitis caused by Citrobacter diversus, Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis or Pseudomonas aeruginosa.

The complicated infections of uric ways caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Citrobacter diversus or Pseudomonas aeruginosa.

Zhelezy:prostatit diseases of prostatic, the caused Escherichia coli and other activators sensitive to an ofloksatsin.

Route of administration and doses:

Inside, in 1 hour prior to or in 2 hours after food. To accept capsules entirely without chewing, washing down with a small amount of water.

At uncomplicated infections of uric ways - on 200 mg 2 times a day within              7-10 days, at uncomplicated cystitis - 3-7 days, at the complicated infections of uric ways - on 400 mg 2 times a day within 10-20 days, at a persistent recurrent infection of uric ways - 12 weeks.

At an acute, uncomplicated gonococcal urethritis, pharyngitis, a proctitis, a tservitita - once 800-1200 mg.

At prostatitis – on 300-400 mg 2 times a day.

At an acute bacterial gastroenteritis - 5 days, for prevention of a bacterial gastroenteritis - on 400 mg once a day, at a typhoid - on 400 mg 3 times a day within 14 days.

For prevention of sepsis at a neutropenia - on 400 mg 2-3 times a day. Duration of antimicrobic action - about 12 hours.

At patients with renal failures the dose of drug is defined depending on values of clearance of creatinine. At clearance of creatinine of 20-50 ml/min. the first dose makes 200 mg, then on 100 mg each 24 h;

at clearance of creatinine less than 20 ml/min. the first dose – 200 mg, then on 100 mg each   48 h.

To the patients who are on a hemodialysis appoint a half of a therapeutic dose.

At patients with the expressed abnormal liver functions the daily dose should not exceed 400 mg.

Features of use:

It is necessary to apply with care ofloxacin at patients with a renal and liver failure. At such patients it is necessary to conduct careful clinical examination. At patients with a renal failure (clearance of creatinine <50 mg/ml) correction of a dose is necessary.

At the patients accepting HP which part ofloxacin is serious and heavy reactions to influence of direct sunshine are possible. Such patients should avoid long stay to the sun and UF-radiations. In case of such reactions (for example, skin rash, etc.) it is necessary to stop treatment.

As well as all drugs of a hinolon, ofloxacin should be applied with care at patients with disturbance of activity of TsNS as its reception can become the reason of an epileptic seizure.

Patients with the diabetes applying ofloxacin along with hypoglycemic drugs or insulin can have a disturbance of level of glucose in blood, including symptomatic hyper - and a hypoglycemia. At such patients it is necessary to control carefully glucose level in blood. If hypoglycemic reactions are shown at the patients who began treatment ofloksatsiny, its use should be stopped.

During prolonged treatment it is necessary to conduct periodic examination of all bodies, including kidneys and a liver.

Ofloxacin is not effective at treatment of syphilis.

The antimicrobic drugs used in high doses for a short span of treatment of gonorrhea can mask or detain a syphilis incubation period. All patients with gonorrhea have to pass serological researches on syphilis during diagnosis. The patients applying ofloxacin need to pass a serological research in three months.

Side effects:

At use of an ofloksatsin can arise: a dispeptic syndrome (anorexia, nausea, vomiting, bitterness in a mouth, an abdominal pain, diarrhea), dysfunctions of an urinary system (a glomerulonephritis, a dysuria, a polyuria, a proteinuria, a crystalluria, a kreatininemiya, urethral bleedings), dysfunctions of TsNS (a headache, dizziness, insomnia, hallucinations, faints), dysfunctions of cardiovascular system (tachycardia, disturbances of a cordial rhythm, arterial hypotonia), dysfunction of organs of sight (burning and eye pain, a conjunctiva hyperemia, хемоз, a photophobia, etc.), dysfunctions of a musculoskeletal system (tendinites, ruptures of sinews, an arthralgia), a vasculitis, pseudomembranous colitis, dysbacteriosis, candidiasis, Stephens-Jones's syndrome, a leukopenia, an eosinophilia, decrease in a hematocrit, tranzitorny increase in liver enzymes in blood serum, allergic reactions (a skin itch, a small tortoiseshell, hypostases).

Interaction with other medicines:

Use of an ofloksatsin with antacids, calciferous, magnesium or aluminum, with sulfates, with bivalent or trivalent drugs, such as iron, or with the multivitamins containing iron, magnesium, zinc can interfere substantially with absorption of an ofloksatsin in an organism. These drugs should not be used within 2 hours before reception of an ofloksatsin.

Use of Cimetidinum considerably increases an elimination half-life of some hinolon.

At simultaneous use of cyclosporine and an ofloksatsin increase in level of concentration of cyclosporine in serum is noted.

The majority of antimicrobic drugs of a hinolon inhibit fermental activity of R-450 cytochrome. The concomitant use with ofloksatsiny some drugs (for example, cyclosporine, theophylline, metilksantit, warfarin, etc.) can increase their elimination half-life.

The concomitant use of non-steroidal anti-inflammatory drugs with ofloksatsiny can lead to increase in risk of stimulation of TsNS and cause an epileptic seizure.

The concomitant use of a probenetsid and ofloksatsin influences secretory tubules of kidneys.

Simultaneous use of an ofloksatsin and theophylline increases an elimination half-life of theophylline and can increase risk of reactions to theophylline. It is necessary to control carefully the level of theophylline and if it is necessary, to make correction of a dose of theophylline.

Increase in efficiency of anticoagulant of warfarin or its derivatives is possible, therefore, at a concomitant use of an ofloksatsin and warfarin it is necessary to control a prothrombin time carefully.

At disturbance of level of glucose in blood, including a hyperglycemia and a hypoglycemia, at the patients using along with ofloksatsiny anti-diabetic drugs it is necessary to control carefully glucose level in blood.

Contraindications:

Ofloxacin is contraindicated to patients with hypersensitivity to drug.

It is contraindicated to patients with epilepsy, including with a low threshold of epileptic seizures.

Children's age up to 15 years.

Pregnancy.

Breastfeeding period.

Overdose:

At overdose ofloksatsiny (3 g in 45 min.) dizziness, nausea, vomiting, drowsiness, emergence of cold sweat (without changes of the main hemodynamic indicators), a convulsive syndrome are possible. In these cases it is necessary to make a gastric lavage, to carry out adequate hydration therapy with an artificial diuresis, to appoint a symptomatic treatment.

Storage conditions:

List B. To store in the place protected from moisture and light at a temperature not above + 25 °C. To store in the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 or 14 capsules in a polymeric can for medicines. Bank together with a leaf insert in a cardboard pack.