Ofloxacin

General characteristics. Structure:

Active ingredient: 200 mg of an ofloksatsin.

Excipients: silicon dioxide colloid (aerosil), calcium stearate, cellulose microcrystallic, talc, povidone (Kollidon 30), lactose (sugar milk), sodium of a kroskarmelloz (primelloz).

Excipients for a cover: gipromelloz (gidroksipropilmetiltsellyuloz), macrogoal-6000 (polyethyleneglycol 6000), titanium dioxide.

Antimicrobic means of bactericidal action. It is applied to treatment of a wide range of the infections caused by sensitive bacterial activators

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.

The antimicrobic range includes gram-positive aerobes: Staphylococcus aureus (Methicillinum - sensitive), Staphylococcus epidermidis (Methicillinum - sensitive), Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin - sensitive), Streptococcus pyogenes.

Gram-negative aerobes: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Citrobacter koseri, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Klebsiella oxytoca, Moraxella catarrhalis, Morganella morganii, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas aeruginosa (quickly develop stability), Serratia marcescens.

Anaerobe bacterias: Clostridium perfringens.

Others: Chlamydia trachomatis, Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophila, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum.

Are in most cases insensitive: Nocardia asteroides, anaerobic bacteria (including Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile), Enterococcus spp., most Streptococcus spp., does not affect 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 (TCmax) at oral administration – 1-2 h. The maximum concentration (Cmax) after reception in a dose of 200, 400 and 600 mg makes 2,5, 5 and 6,9 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 the blood-brain barrier (BBB), 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.

Elimination half-life (T1/2) – 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 from 10 to 30% of drug are removed.

Indications to use:

The infectious and inflammatory diseases caused by sensitive microorganisms:

- respiratory tracts (bronchitis, pneumonia);

- ENT organs (sinusitis, pharyngitis, average otitis, laryngitis, tracheitis);

- skin, soft tissues;

- bones and joints;

- abdominal organs and biliary tract;

- kidneys (pyelonephritis);

- lower urinary tract (cystitis, urethritis);

- generative organs and bodies of a small pelvis (endometritis, salpingitis, oophoritis, cervicitis, parametritis, bacterial prostatitis, colpitis, orchitis, epididymite);

- gonorrhea, clamidiosis;

- prevention of infections at patients with disturbance of the immune status (including at a neutropenia).

Route of administration and doses:

Inside. A pill is taken entirely, washing down with water, to or during food. Duration of treatment is defined by sensitivity of the activator. Therapy duration on average 7-10 days.

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 200-600 mg a day, 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. Doses over 400 mg/days should be divided into 2 receptions with an equal period. At heavy infections or at treatment of patients with an excess weight the daily dose can be increased to 800 mg.

At treatment the uncomplicated and complicated infections of the lower urinary tract a course of treatment – 7 and 10 days respectively, at prostatitis – up to 6 weeks, at infections of bodies of a small pelvis – 10-14 days, at infections of a respiratory organs and skin – 10 days.

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 dose is appointed 1 time a day.

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

Features of use:

It is not shown at treatment of acute tonsillitis. Is not choice drug at the pneumonia caused by pneumococci.

It is not recommended to be affected by sunshine, to radiation by UV rays (mercury-quartz lamps, a sunbed).

For prevention of hyper concentration of urine and the subsequent crystalluria, during treatment it is recommended to carry out adequate hydration.

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 impossible to use ethanol.

At drug use women are not recommended to use hygienic 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 (the dose decline is required).

Side effects:

From the alimentary system: gastralgia, loss of appetite, nausea, vomiting, diarrhea, lock, meteorism, abdominal pain, increase in activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous colitis, dryness of a mucous membrane of an oral cavity, pharyngitis.

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, sleeplessness, nervousness.

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

From sense bodys: disturbance of color perception, diplopia, disturbances of taste, sense of smell, hearing and balance.

From cardiovascular system: tachycardia, increase or lowering of arterial pressure.

Allergic reactions: skin rash, itch, small tortoiseshell, allergic pneumonitis, allergic nephrite, eosinophilia, fever, Quincke's disease, bronchospasm; a multiformny exudative erythema (including Stephens-Johnson's syndrome) and a toxic epidermal necrolysis (Lyell's disease), a vasculitis, an acute anaphylaxis, an itch of external genitals at women.

From integuments: dot hemorrhages (petechias), violent hemorrhagic dermatitis, papular rash with a crust, testimonial of defeat of vessels (vasculitis).

From bodies of a hemopoiesis: leukopenia, agranulocytosis, anemia (including aplastic and hemolitic), thrombocytopenia, pancytopenia.

From an urinary system: acute intersticial nephrite, renal failure, giperkreatininemiya, increase in concentration of urea, dysuria, ischuria.

Others: an intestinal dysbiosis, superinfection, a hypoglycemia (at patients with a diabetes mellitus), a vaginitis, a stethalgia, fatigue, an adynamy, a photosensitization, the general weakness, allocations from a vagina, nasal bleeding, thirst, decrease in body weight.

Interaction with other medicines:

Reduces clearance of theophylline by 25% (at simultaneous use it is necessary to reduce a theophylline dose).

Increases concentration of Glibenclamidum in plasma.

Increases serumal concentration of cyclosporine.

Cimetidinum, furosemide, methotrexate and medicines blocking canalicular secretion increase concentration of an ofloksatsin in a blood plasma.

At a concomitant use with indirect anticoagulants (coumarin derivatives, including warfarin) 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, including spasms 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, Natrii hydrocarbonas) the risk of a crystalluria and nephrotoxic effects increases.

At co-administration with hypoglycemic means it is possible both hypo - and a hyperglycemia in this connection it is necessary to control concentration of glucose in a blood plasma.

At joint appointment with the drugs extending QT (IA and the III classes of antiarrhytmic drugs, tricyclic antidepressants, macroleads) the risk of lengthening of an interval of QT increases.

The foodstuff, antacids containing compounds of aluminum, calcium, magnesium or salt of iron reduce absorption of an ofloksatsin, forming insoluble complexes (time interval between purpose of these medicines has to be not less than 2 h).

Contraindications:

Hypersensitivity to an ofloksatsin and other ftorkhinolona, 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; lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption; age up to 18 years (growth of a skeleton is not completed yet), pregnancy, the lactation period; clearance of creatinine less than 20 ml/min.

With care: atherosclerosis of vessels of a brain, disturbance of cerebral circulation (in the anamnesis), a chronic renal failure, a liver failure, organic diseases of the central nervous system, predisposition to convulsive reactions, a myasthenia, a hepatic porphyria, deficit glyukozo-6-fosfatdegidrogenazy, a diabetes mellitus, a syndrome of inborn lengthening of an interval of QT, a heart disease (heart failure, a myocardial infarction, bradycardia), psychoses and other mental disturbances in the anamnesis; a concomitant use of the medicines extending QT interval (antiarrhytmic IA and the III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macroleads, antifungal, derivative an imidazole, some antihistaminic, including астемизол, терфенадин, эбастин), for the general anesthesia from group of barbiturates, the medicines reducing arterial pressure; advanced age.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy. The hemodialysis deletes 10-30% of drug.

Storage conditions:

Period of validity - 2 years. Not to use after expiry date. List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 200 mg. On 10 or 20 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1 or 2 blister strip packagings with the application instruction place in a pack from a cardboard.