Тарицин®

General characteristics. Structure:

Active ingredient: 200 mg of an ofloksatsin.

Excipients: cellulose microcrystallic, potato starch, povidone, croscarmellose sodium, magnesium stearate, gipromelloz (gidroksipropilmetiltsellyuloz), macrogoal (polyethyleneglycol), глицерол (glycerin), talc, titanium dioxide, lactose (milk sugar).

Antimicrobic drug from group of ftorkhinolon of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Antimicrobic drug from group of ftorkhinolon of a broad spectrum of activity. The mechanism of action of an ofloksatsin is connected with blockade of DNK-girazy enzyme in bacterial cells. Works bakteritsidno.

It is active concerning the microorganisms producing beta lactamelements and fast-growing atypical bacteria. Are sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter, Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafnia, Proteus spp. (including Proteus mirabilis, Proteus vulgaris — indolpositive and indolnegative), 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 acne, Brucella spp.

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

Are in most cases insensitive: Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacter spp., Fusobacterium spp., Clostridium difficile). Does not affect Treponema pallidum.

Pharmacokinetics. Absorption after intake bystry and full (95%). Bioavailability — over 96%, communication with proteins of plasma — 25%. The maximum concentration 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.

It is distributed: in cells (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 barrier (GEB), a placental barrier, cosecretes with maternal milk. Gets into cerebrospinal fluid (SMZh) (14-60%).

N-oxide of an ofloksatsin and dimetilofloksatsin is metabolized in a liver (about 5%) with education. An elimination half-life — 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 or liver failure removal can be slowed down. Does not kumulirut. At a hemodialysis 10-30% of drug are removed.

Indications to use:

Respiratory infections (bronchitis, pneumonia); infections of ENT organs (sinusitis, pharyngitis, average otitis, laryngitis); infections of skin, soft tissues; bones, joints; infectious and inflammatory diseases of an abdominal cavity and biliary tract (except for bacterial enteritis); kidneys (pyelonephritis), urinary tract (cystitis, urethritis); bodies of a small pelvis (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis); generative organs (colpitis, orchitis, epididymite), gonorrhea, clamidiosis; meningitis; prevention of infections at patients with disturbance of the immune status (including at a neutropenia).

Route of administration and doses:

Inside. The dose of an ofloksatsin and duration of treatment depend on weight and a type of an infection, sensitivity of microorganisms, the general condition of the patient and function of a liver, kidneys.

Average daily dose for adults — from 200 mg to 800 mg. Treatment duration — 7-10 days. 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. At gonorrhea — 400 mg once.

At patients with renal failures (at clearance of creatinine of 50-20 ml/min.) the dose has to make 50% of an average dose at frequency rate of appointment 2 times a day or a full single dose enter 1 time a day. At clearance of creatinine less than 20 ml/min. a single dose — 200 mg, then — on 100 mg a day every other day.

At a hemodialysis and peritoneal dialysis — on 100 mg each 24 hours. The maximum daily dose at a liver failure — 400 mg.

Pill is taken entirely, washing down with water to or during food. 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 salmonelloses a course of treatment — 7-8 days, at uncomplicated infections of the lower urinary tract a course of treatment — 3-5 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 apply more than 2 months, to be affected by sunshine, to uviolizing (mercury-quartz lamps, a sunbed).

In case of side effects from TsNS, 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 reducing dose adjustment is required).

At children it is applied only at threat of life, taking into account estimated clinical performance and potential risk of development of side effects when it is impossible to apply other, less toxic medicines. An average daily dose in this case — 7,5 mg/kg, maximum — 15 mg/kg.

During treatment it is necessary to abstain from driving of motor transport and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: gastralgia, loss of appetite, nausea, vomiting, diarrhea, meteorism, abdominal pain, increase in activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous coloenteritis.

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.

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

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

From cardiovascular system: tachycardia, 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.

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, thrombocytopenia, pancytopenia, hemolitic and aplastic anemia.

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

Others: an intestinal dysbiosis, superinfection, a hypoglycemia (at patients with a diabetes mellitus), a vaginitis.

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

At a concomitant use with antagonists of vitamin K 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 increases.

At co-administration with glucocorticosteroids the risk of a rupture of sinews, especially at elderly people increases.

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

Let's combine with the following infusion solutions: 0,9% chloride sodium solution, Ringer's solution, 5% solution of fructose, 5% dextrose solution.
Not to mix with heparin (risk of precipitation).

The foodstuff, antacids containing ions 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, deficit glyukozo-6-fosfatdegidrogenazy; epilepsy (including in the anamnesis); decrease in a convulsive threshold (after a craniocereberal injury, a stroke, inflammatory processes in the central nervous system); age up to 18 years (growth of a skeleton is not completed yet); pregnancy and period of a lactation.

With care. Atherosclerosis of vessels of a brain, disturbance of cerebral circulation (in the anamnesis), a chronic renal failure, organic lesions of the central nervous system.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Not to use after the expiry date specified on packaging. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 200 mg. On 10 tablets in a blister strip packaging. On 1, 2, 3, 4 or 5 blister strip packagings together with the application instruction in a pack from a cardboard.