Zarkvin

General characteristics. Structure:

Active ingredient: 200 mg or 400 mg of a gatifloksatsin.

Excipients: calcium hydrophosphate, corn starch, karmelloz, silicon dioxide colloid, polyvinylpirrolidone, magnesium stearate, talc, sodium lauryl sulfate, gidroksipropilmetiltsellyuloza, ethyl cellulose, PEG 6000, propylene glycol, titanium dioxide, dye yellow iron oxide.

The highly active synthetic chemotherapeutic broad-spectrum agent which is characterized by good pharmacokinetic properties, high extent of penetration into fabrics and cells of a macroorganism and bacterial cells. Gatifloksatsin in various publications rank to "respiratory", "anti-pneumococcal", "with an expanded antibacterial range" to ftorkhinolona or as ftorkhinolona of the IV generation. Later researches showed what гатифлоксацин has high ability of fight against numerous microorganisms, including M. tuberculosis.

Pharmacological properties:

Pharmacodynamics. Zarkvin - antimicrobic means of group of ftorkhinolon (the fourth generation) with a wide range of antibacterial action. The mechanism of bactericidal action of a gatifloksatsin is connected with inhibition of bacterial DNK-girazy enzyme and topoisomerase IV of type that blocks cell fission and leads of bacteria to death. It is highly active concerning gram-negative and gram-positive bacteria, (including located intracellularly).

Are sensitive to drug: Mycobacterium tuberculosae, E. Coli, Salmonella spp., Shigella spp., Klebsiella spp., Proteus spp., Pseudomonas spp., Enterobacter spp., Serratia spp., Staphylococcus spp., Streptococcos spp., Neisseria spp., Haemophilus influenzae, Brucella spp., Chlamydia spp., Campylobacter spp. Zarkvin is also effective in relation to the bacteria producing β-lactamelements. Besides, such activators as H. Pylori, anaerobe bacterias are sensitive to Zarkvin.

Pharmacokinetics. At Zarkvin's reception inside it quickly and almost completely (bioavailability of 96-98%) is soaked up, reaching peak concentration in blood within 1,0-2,28 hours. At the same time its absorbing capacity does not depend on whether it is accepted on an empty stomach or after food. This property of a gatifloksatsin in combination with a long elimination half-life provides to it high комплаенс treatments. Gatifloksatsin has bioequivalence at intake and introduction intravenously, and therefore its therapeutic doses do not depend on an introduction form.

Gatifloksatsin well gets into liquids, fabrics and cells of a human body, reaching in them the concentration considerably exceeding plasma at various values of the rn-environment. The highest concentration of a gatifloksatsin are observed in lungs, liquids and fabrics of urogenital system, a mucous membrane of a middle ear, cerebrospinal fluid. Plasma concentration of a gatifloksatsin reaches the peak by 7th day at intake and to the 3rd — at intravenous administration. Ability to contact serum proteins does not depend on concentration in blood and makes no more than 20%. The elimination half-life of drug makes 7–14 h and does not depend on a dose. Gatifloksatsin has the minimum hepatic metabolism and in an invariable look is allocated with kidneys. Over 70% of drug are removed with urine for 48 h, 5% are removed with a stake

Indications to use:

Tuberculosis — as a part of complex therapy for patients with allocation of MBT steady against an isoniazid and rifampicin (MLU), sharply progressing forms, including concerning strains of MBT sensitive to antitubercular drugs; and also in the empirical modes of chemotherapy. The infectious diseases caused by strains, sensitive to a gatifloksatsin: acute and chronic respiratory diseases, community-acquired pneumonia; acute sinusitis, the uncomplicated and complicated infections of urinary tract, pyelonephritis, infections of skin and soft tissues. Drug is used for preoperative prevention and postoperative treatment of surgical infections at patients with the reduced immune status.

Route of administration and doses:

For treatment of tuberculosis appoint 800 mg once a day. At treatment of other infectious diseases of 200-400 mg once a day. At chronic bronchitis in a phase of an aggravation enter 400 mg (200 ml) of drug of 1 times a day for 7–10 days. At acute sinusitis — 400 mg of 1 times a day for 10 days. At extra hospital pneumonia — 400 mg of 1 times a day for 7–14 days. At uncomplicated infections of uric ways enter 400 mg once or on 200 mg for 3 days, and at complicated — 400 mg of 1 times a day for 7–10 days. For treatment of infections of skin and soft tissues appoint on 200 mg for 5–7 days. <40 ml/min. (including the patients who are on a long peritoneal out-patient hemodialysis) dose adjustment is necessary for patients with clearance of creatinine: the initial dose makes 400 mg/days, in the next days — 200 mg/days.

Features of use:

In view of lack of sufficient clinical data about use of drug during pregnancy and feeding by a breast its appointment is possible only if the expected therapeutic effect for mother exceeds potential risk for a fruit. Zarkvin's introduction can cause lengthening of an interval of Q-T on an ECG therefore in view of lack of sufficient clinical experience patients are recommended to avoid purpose of drug with similar changes on an ECG, and also with the expressed bradycardia and ischemia of a myocardium. It is necessary to appoint drug with care the patient with pathology of TsNS and the expressed atherosclerosis of vessels of a brain as administration of drug leads to increase in intracranial pressure and can cause development of psychoses. With care appoint to persons whose professional activity is connected with control of cars and mechanisms or demands the increased concentration of attention.

Side effects:

In clinical tests at purpose of single and multiple doses of drug the side reactions which are found in ≤ 3% of cases were classified as it is possible, possibly and obviously connected with reception of a zarkvin: nausea, diarrhea, hyperbilirubinemia. a headache, dizziness, local reactions in the form of erubescence in the place of an injection. At ≥ 0.1% - less than 3% of patients were noted: allergic reactions, fever, temperature increase, dorsodynias, breasts, strengthening of heartbeat, abdominal pain, vomiting, dyspepsia, lock, glossitis, candidiasis of a mucous membrane, stomatitis, peripheral hypostases, sleep disorders, sleeplessness, paresthesia, tremor, vazodilatation, вертиго, short wind, pharyngitis, sweating strengthening, vision disorder, food faddism, sonitus, dysuria, hamaturia.

Interaction with other medicines:

It is not necessary to appoint Zarkvin to patients who receive treatment by antiarrhythmic drugs. Co-administration of Zarkvin and digoxin leads to increase in concentration of the last in blood serum. Zarkvin's reception strengthens effect of indirect anticoagulants.

Contraindications:

Hypersensitivity to a gatifloksatsin and other hinolona. It is not necessary to appoint it to patients aged up to 18 years, to pregnant women and the feeding women.

Overdose:

In case of acute overdose it is necessary to stop administration of drug, to provide adequate hydration, carrying out monitoring of an ECG, to appoint symptomatic therapy.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store solution, unprotected from light, no more than 3 days.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 200 mg, 400 mg. On 5 tablets in the blister from a film of PVC and aluminum foil. On 1 blister in a cardboard pack with the application instruction.