international and chemical name: gatifloxacin; (±)-1-cyclopropyl-6-floro-1, 4-digidro-8-metoksi-7-(3-methyl-1-piperazinil) - 4-oxo-3-kvinolinekarboksilin acids seskivi-hydrate;
Main physical and chemical characteristics: tablets of yellow color, oboyevypukly, coated with a notch on one party, extended, a kapsulopodobny form on 200 mg and an oval form on 400 mg;
Structure. 1 tablet of Gatidzhem contains a gatifloksatsin of sexivihydrat that is equivalent a gatifloksatsina of 200 mg or 400 mg;
other components: cellulose microcrystallic, starch corn, starch dioxide, corn in the form of paste, silicon, colloid, the talc purified magnesium stearate, sodium of a kroskarmeloz, mix for a covering (untacoat sol (IC-s-673) – 1-yellow).
Form of production of medicine Gatidzhem. Tablets, coated.
Farmakoterapevtichesky group. Antibacterial agents for system use. Ftorkhinolona. Code of automatic telephone exchange J01M A16.
Effect of the medicine.
Pharmacodynamics. Gatifloksatsin - 8-metoksiflorokvinolon, has antibacterial activity against the broad range of gram-negative and gram-positive microorganisms. Antibacterial action of a gatifloksatsin is provided thanks to suppression DNK-girazy and topoisomerases IV. DNK-giraza is important enzyme which takes participation in DNA reduplication to activators. Topoisomerase IV is enzyme which plays the carrying-out role in division of chromosomes of DNA at division of a bacterial cell. It became clear that S-8-metoksicheskaya a half has big activity and slower development of resistance in comparison with nemetoksichesky S-8 a half.
It agrees with it gatifloksatsin it is shown for treatment corresponding to a nosology which reason is: activators - gram-positive microorganisms are sensitive: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes are also rather sensitive gram-positive microorganisms: Streptococcus milieri, Streptococcus mitior, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohnii, Staphylococcus epidermidis (including metitsillinrezistentny strains), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae; activators - gram-negative microorganisms are sensitive: Haemophillus influenzae (including strains which produce β-lactamelements), Haemophilias parainfluenzae: Klebsiella pneumoniae, Moraxella catarrhalis (including strains which produce β-lactamelements), Escherichia coli, Enterobacter cloacae, Neisseria gonorrhoeae (including strains which produce β-lactamelements);
also are rather sensitive - gram-negative microorganisms: Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mіrabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii;
anaerobe bacterias — Bacteroides distasonis are rather sensitive, Bacteroides eggerthi і, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevotella spp., Propionibacterium spp., Ctostridium perfringens, Clostridium ramosum; activators of an atypical form - C.pneumoniae are sensitive, C. trachomatis, M.pneumoniae, L. Pneumophilia, Ureaplasma; also atypical forms - Legionella pneumophila are rather sensitive, Caxiella burnettii.
Such activators as mycobacteria of tuberculosis, H. Pylori are sensitive to a gatifloksatsin.
Gatifloksatsin effective concerning bacteria resistant to β-laktamny and makrolidny antibiotics.
Pharmacokinetics. Absolute biological availability of a gatifloksatsin at patients – 96%. The concentration peak in plasma of a gatifloksatsin comes in 1 - 2 hour after peroral use.
Linkng with proteins of a blood plasma of a gatifloksatsin makes about 20%.
Gatifloksatsin well gets into the most part of body tissues and is quickly distributed on liquids biological, high concentration are formed in pulmonary fabric, mucous bronchial tubes, adnexal nasal cavities, in alveolar macrophages, tissues of a middle ear, skin tissues, fabrics and a secret of a prostate, saliva, bile, semyavyvodyashchy liquid, a vagina, a uterus, endo-and myometriums, uterine tubes, ovaries.
Gatifloksatsin in an organism biotransformirutsya with <1% allocation of a dose in urine.
Gatifloksatsin is brought by kidneys. The average of removal of a gatifloksatsin – also does not depend from 7 to 14 hour on a dose and to use mode.
At experiments with animals gatifloksatsin randomly passes through a placenta and gets to breast milk.
Differences in pharmacokinetics of a gatifloksatsin were revealed at women. Women of advanced age had 21% increase in the maximum concentration and 32% increase in AUC (0-), more slowly removal was observed at women of younger age.
Pediatrics: the pharmacokinetics of a gatifloksatsin at children till 18 flyings was not revealed.
Renal failure: clearance of a gatifloksatsin reduced and system influence is stronger expressed at people with a renal failure.
Indications to use. Treatment of the infectious and inflammatory processes caused by microorganisms, sensitive to drug:
- respiratory infections (including acute sinusitis, acute bronchitis, abscess of lungs, exacerbation of chronic diseases of pulmonary ways, cystous fibrosis, pneumonia);
- infections of kidneys and urinary system (including acute and chronic pyelonephritis, prostatitis, cystitis; persistent infections of an urinary system);
Way of use and dose. Acute sinusitis – 400 mg of 1 times a day or 200 mg 2 times a day within 7 - 14 days; the acute and complicated chronic bronchitis, pneumonia, infections of skin and hypodermic cellulose, acute pyelonephritis and the complicated infections of an urinary system – 400 mg of 1 times a day or on 200 mg two times a day within 7 - 10 days;
not complicated infections of an uric path (cystitis) – 400 mg an initial dose and 200 mg - 1 time a day within 3 days; not complicated urethral gonorrhea at men, gonorrhea at women – 400 mg of 1 times a day.
Side effect. The most widespread side effects of a gatifloksatsin – dizziness, vomiting, diarrhea, a vaginitis, abdominal and the main pain. Other side effects – disturbance of flavoring feelings, allergic reactions, a fever, heat, a dorsodynia, a stethalgia, a cardiopalmus, a lock, dyspepsia, a glossitis, candidiasis of an oral cavity, stomatitis, an ulcer of an oral cavity, peripheral hypostases, an uneasy dream, sleeplessness, paresthesia, a tremor, vasodilatation, dispnoe, pharyngitis, perspiration, a vision disorder, a ring in ears, a dysuria and a hamaturia.
Kvinolona sleeplessness, nightmares or Parana can be the cause of disturbances of the central nervous system, including nervousness, concern.
Neutropenia, increase of activity of transaminases, blood amylases.
Contraindications. Gatifloksatsin of contraindications to patients with hypersensitivity to a gatifloksatsin, kvinolonovy antibacterial components and other components of this drug, to pregnant women, women who nurse, to children till 18 flyings.
Overdose. There is no information about overdose.
At accidental overdose of drug it is necessary to wash out a stomach. The patient has to is under control and to receive the symptomatic and supporting treatments. It is necessary to apply the hydration therapy corresponding to a state. Gatifloksatsin is insufficiently effectively brought from an organism by a hemodialysis (about 14% during the 4th hour) or by means of the forced hemodialysis (about 11% in 8 days).
Features of use. Gatifloksatsin can entail increase in QT intervals of the electrocardiogram at some patients. Through insufficient clinical experience gatifloksatsin patients should not appoint with the prolonged QT intervals, the patient to an inadequate hypercalcemia and to patients who receive class drugs І And (for example, kvinidin, protsaynamid) or a class ІІІ (for example, Amiodaronum, sotalol) pro-thiarhythmic drugs.
Pharmacokinetic researches were not conducted for a gatifloksatsin and drugs which extend QT intervals, such as tsisaprayd, erythromycin and tricyclic antidepressants. Gatifloksatsin has to be applied with care at parallel use with these drugs. Gatidzhem patients need to apply with care with heart diseases, such as bradycardia and acute ischemia of a myocardium.
Serious and fatal cases of hypersensitivity and anaphylactic reactions were observed at patients who were treated kvinolony.
Gatifloksatsin should not be applied at the first manifestations of hypersensitivity – at an enanthesis or other allergic reactions.
With care appoint to patients with epilepsy and elderly people.
It is necessary to use carefully drug during the period control of vehicles (possibly dizziness).
Purpose of a gatifloksatsin has to be careful in the presence of a renal failure. Careful clinical inspection and the corresponding laboratory analyses need to be carried out to and during treatment, in need of dependence on the level of indicators, it is necessary to lower a dose of a gatifloksatsin. For patients with the broken renal function (the clearance of creatinine <40 ml/minutes) dose adjustment (reducing a dose) needs to be carried out for avoidance of accumulation of a gatifloksatsin through lowered clearance. For patients with clearance of creatinine <30 ml/minutes are recommended doses of a gatifloksatsin are lowered.
As well as with other kvinolona, disturbance of contents of glucose in blood, including symptomatic hyper - and a hypoglycemia, were revealed by the most part at the patients sick with diabetes who receive simultaneous treatment by peroral hypoglycemic drugs (for example, Glyburidum) or insulin. In these patients it is recommended to control glucose level in blood.
Interaction with other medicines. Reception of a gatifloksatsin in 1 hour after Cimetidinum (once a day, orally in a dose of 200 mg) does not influence pharmacokinetics of a gatifloksatsin. These results say that absorption of a gatifloksatsin is influenced by antagonists of H2 receptors, such as Cimetidinum.
Use of a gatifloksatsin does not influence systematic clearance of intravenous midazolam. The daily intravenous dose of midazolam (0,0145 mg/kg) does not influence pharmacokinetics of a gatifloksatsin. These results can be considered at insufficient efficiency of a gatifloksatsin when carrying out researches with CYP3A4 isoenzyme at people.
Simultaneous use of a gatifloksatsin and theophylline did not influence pharmacokinetics of any drug.
Simultaneous use of a gatifloksatsin and warfarin did not influence pharmacokinetics of any drug, a prothrombin time did not change.
Simultaneous use of a gatifloksatsin and Glyburidum (at a stable state once a day) patients with ІІ like a diabetes mellitus of much considerable influence on distribution in an organism of any drug, glucose levels on an empty stomach did not change.
Simultaneous use of a gatifloksatsin and digoxin did not give considerable effect concerning change of pharmacokinetics of a gatifloksatsin. Patients who accept digoxin have to be controlled on signs and symptoms of toxicity. At patients who revealed signs or symptoms of intoxication digoxin concentration of digoxin in serum has to be checked and the dose of digoxin is respectively modified.
System removal of a gatifloksatsin considerably increases at simultaneous use of a gatifloksatsin and probenetsid.
At patients who received warfarin serious changes in time of turning of blood at simultaneous use of a gatifloksatsin were not revealed.
During preclinical and clinical trials it is revealed that at simultaneous use with non-steroidal anti-inflammatory drugs, such as kvinolon, came to light that the last can increase risk of disturbances of TsNS and spasms.
Conditions and periods of storage. To store in the unavailable to children, dry, protected from light place at a temperature not above 25 °C. A period of validity – 2 years.