Ofloxacin

General characteristics. Structure:

Active ingredient: 400 mg of an ofloksatsin in 1 tablet.

Excipients: lactoses monohydrate, starch corn, hypro rod, croscarmellose sodium, magnesium stearate; cover: опадрай the II white (polyvinyl alcohol, titanium dioxide, macrogoal, talc).

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-chuvstvitslnye), Staphylococcus epidermidis (Methicillinum - sensitive). Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin - sensitive). Streptococcus pyogenes.

Gramotrinatelny aerobes: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Citrobacter koseri, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae. Klebsiella oxytoca, MoraxelIa catarrhalis, Morganella morganii, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stucirtii, 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 100, 300 and 600 mg makes 1, 3,4 and 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 gemato-en a tsefalichesky barrier, a placental barrier, it sekrstirutsya with maternal milk. Gets into cerebrospinal fluid at the inflamed and uninflammed meninx (14-60%).

N-oxide of an ofloksatsin and dimetilofloksatsin is metabolized in a liver (about 5%) with education. The elimination half-life (T1/2) is equal to 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:

The infectious and inflammatory diseases caused by microorganisms, sensitive to an ofloksatsin:

- an upper respiratory tract infection and LOR-bodies (sinusitis, pharyngitis, average otitis, laryngitis except for cases of acute tonsillitis);

- lower respiratory tract infections (tracheitis, bronchitis, pneumonia, except for cases of a pneumococcal infection);

- infections of skin, soft tissues, bones and joints;

- infectious and inflammatory diseases of an abdominal cavity and biliary tract, kidneys (pyelonephritis);

- infections of urinary tract (cystitis, urethritis, including gonococcal nature);

- infections of generative organs and bodies of small gas (endometritis, salpingitis, oophoritis, cervicitis, parametritis, 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. 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.

For prevention of infections at patients with the expressed decrease in immunity - on 400 mg/days.

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

At gonorrhea - 400 mg once.

At patients with renal failures (at the clearance of creatinine (CC) less than 50 ml/min.) administration of drug in a dose of 400 mg is not recommended. If necessary to use other dosage form in the form of tablets of 200 mg.

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

Duration 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 the uncomplicated and complicated infections of the lower urinary tract a course of treatment of 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.

Features of use:

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

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.

Emergence of diarrhea, especially in a severe form, persistent and/or with blood impurity.

in time or after treatment ofloksatsiny can be display of pseudomembranous colitis. At suspicion on development of pseudomembranous colitis treatment ofloksatsiny has to be immediately stopped, and the corresponding specific antibacterial therapy (for example, Vancomycinum inside, тейкопланин inside or metronidazole) has to be appointed urgently. The drugs braking an intestines peristaltics are contraindicated.

In case of side effects from the central nervous system, allergic reactions, drug withdrawal is necessary.

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.

The pas a background of treatment is possible deterioration in a current of a myasthenia, increase of attacks of a porphyria.

Can result in false-negative results at bacteriological diagnosis of tuberculosis (interferes with Mycobacterium tuberculosis allocation).

At patients with abnormal liver functions control of concentration of an ofloksatsin in plasma is necessary. At a heavy liver failure the risk of development of toxic effects increases (the reducing dose adjustment is required).

At the patients applying ftorkhinolona, including ofloxacin cases of the touch and sensomotor axonal polyneuropathy affecting small and (or) large axons, and leading to paresthesia, a giposteziya, a dizesteziya and weakness are registered. Symptoms can soon be shown after the beginning of use and to be irreversible. If at the patient neuropathy symptoms, including pain, burning, a pricking, numbness and (or) weakness or other disturbances of sensitivity, including tactile, painful, temperature, vibration sensitivity and feeling of situation develop, drug use ofloxacin needs to be stopped immediately.

Reception of an ofloksatsin, especially long, can cause the consecutive infection connected with growth of microorganisms, steady against drug. Repeated assessment of a condition of the patient is necessary.

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. At emergence of such undesirable phenomena as dizziness, drowsiness, it is necessary to refrain from performance of the specified types of activity.

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, coloenteritis, hepatitis, anorexia.

From a nervous system: a headache, dizziness, a tremor, spasms, onemeyony and paresthesias of extremities, intensive dreams, "dreadful" dreams, psychotic reactions, uneasiness, a condition of excitement, a phobia, a depression, confusion of consciousness, a hallucination, increase in intracranial pressure, sleeplessness, a soplivost, extrapyramidal frustration and other frustration of muscular coordination, peripheral touch or sensory-motor neuropathy, a depression with causing to harm, up to suicide thoughts and attempts, a sonitus.

From a musculoskeletal system: the tendinitis, mialgiya, arthralgias, tendosinovit, a rupture of a sinew, extremity pain, рабдомиолиз and/or a myopathy.

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; multiformny exudative erythema (including Stephens-Johnson's syndrome) and toxic epidermal necrolysis (Lyell's disease), photosensitization, vasculitis. acute anaphylaxis. an itch of external genitals at women.

From integuments: dot hemorrhages (petechias), violent hemorrhagic dermatitis, papular rash with a crust, (vasculites), "inflows" of blood testimonial of defeat of vessels to face skin.

From bodies of a hemopoiesis: leukopenia, agranulocytosis, anemia (including aplastic and hemolitic), trombotsitopsniya, 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, increased fatigue, an adynamy, the general weakness, allocations from a vagina, nasal bleeding, thirst, decrease in body weight, pharyngitis, short wind, cough, rhinitis, a photophobia, irritation of a mucous membrane of an eye, a vision disorder, porphyria attacks at patients with a porphyria.

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 use with the non-steroidal anti-inflammatory drugs derivative of a nitroimidazole and methylxanthines the risk of development of neurotoxic effects, including spasms increases.

At a concomitant use with glucocorticosteroids the risk of a rupture of sinews, especially at elderly people increases.

At use with the medicines alkalizing urine (karboangidraza inhibitors, citrates, Natrii hydrocarbonas) the risk of a crystalluria and nephrotoxic effects increases.

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

At simultaneous use with the drugs capable to reduce arterial pressure, medicines for not inhalation general anesthesia from group of barbiturates, perhaps sharp and considerable lowering of arterial pressure therefore in this case especially careful monitoring of indicators of a functional condition of cardiovascular system is required.

The foodstuff, antacids containing Al3 +, Sa2 +, Mg2 + or Fe salts reduce absorption of an ofloksatsin. forming insoluble complexes (time interval between reception of these medicines has to be not less than 2 h).

Contraindications:

Hypersensitivity to an ofloksatsin, other hinolona or components of drug, 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, renal failure (clearance of creatinine less than 50 ml/min.), age up to 18 years, pregnancy, the period of a lactation (breastfeeding), a lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption.

With care. Atherosclerosis of vessels of a brain, disturbance of cerebral circulation (in the anamnesis), a liver failure, organic diseases of the central nervous system, predisposition to convulsive reactions, a myasthenia, a hepatic porphyria, deficit glyukozo-6-fosfatdsgidrogsnazy, a syndrome of inborn lengthening of an interval of Q-T, a heart disease (heart failure, a myocardial infarction, bradycardia), psychoses and other mental disturbances in the anamnesis; a concomitant use of the medicines extending Q-T 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; at the patients who are at the same time receiving the medicines reducing a threshold of convulsive readiness of a brain such as фенбуфен, theophylline; patients with the known risk factors have lengthenings of an interval of Q-T: at patients of advanced age, at patients with not adjusted electrolytic disturbances (for example, a hypopotassemia, a hypomagnesiemia). at the patients with a diabetes mellitus receiving hypoglycemic means for oral administration (for example, глибекламид) or insulin.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 400 mg. Packaging: on 5 or 10 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1 blister strip packaging together with the application instruction in a cardboard pack.