international and chemical names: Gatifloxacin, (±)-1-cyclopropyl-6-floro-1, 4-digidro-8-metoksi-7-(3-methyl-1-piperazinil) - 4-oxo-3-kvinolinekarboksilin acids sexivihydrat;
Main physical and chemical characteristics: transparent solution that can have a shade of yellow or greenish-yellow color.
The structure of 1 ml of solution includes a gatifloksatsin of sexivihydrat 2 mg of a gatifloksatsin are equivalent;
other components: the dextrose is anhydrous, dinatrium edetat, water for injections, Acidum hydrochloricum (10%) for a correcting rn.
Form of production of medicine. Solution for infusions.
Farmakoterapevtichesky group. Antimicrobic means for system use. Ftorkhinolona. Code of automatic telephone exchange J01M A16.
Effect of the medicine. Pharmacodynamics. The mechanism of action of a gatifloksatsin differs from the mechanism of effect of penicillin, cephalosporins, aminoglycosides, macroleads and tetracyclines. Gatifloksatsin affects microorganisms which resistant to the listed antibiotics. There is no cross firmness between gatifloksatsiny and the specified classes of antibiotics. Gatifloksatsin - 8-metoksiftor-hinolon has antibacterial activity of rather wide range of gram-negative and gram-positive microorganisms: gram-positive microorganisms: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes;
activators - gram-negative microorganisms of Haemophillus influenzae (including the strains producing β-lactamelements) are sensitive, Haemophilias parainfluenzae: Klebsiella pneumoniae, Moraxella catarrhalis (including the strains producing β-lactamelements), Escherichia coli, Enterobacter cloacae, Neisseria gonorrhoeae (including the strains producing β-lactamelements);
are rather sensitive - gram-negative microorganisms of Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mіrabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii;
anaerobe bacterias of Bacteroides distasonis, Bacteroides eggerthi і are rather sensitive, 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, the atypical forms C.pneumoniae, C. trachomatis, M. pneumoniae, L. Pneumophilia, Ureaplasma are sensitive;
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.
Antibacterial action of a gatifloksatsin is provided thanks to suppression of DNA of a giraza and topoisomerase IV. DNA of a giraz 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.
Pharmacokinetics. Absolute biological availability of a gatifloksatsin at patients – 96%. Linkng with proteins of a blood plasma makes about 20%.
Gatifloksatsin well gets into the most part of body tissues and is quickly distributed after liquids biological, high concentration are formed in pulmonary tissue, a mucous membrane of bronchial tubes, adnexal nasal cavities, in alveolar macrophages, tissues of a middle ear, skin tissues, fabrics and a secret of a prostate, saliva, bile, sperms, a vagina, a uterus, endo-and a myometrium, uterine tubes, ovaries.
Gatifloksatsin in an organism biotransformirutsya with <1% allocation of a dose in urine.
Gatifloksatsin is brought through kidneys. The average elimination half-life of a gatifloksatsin – also does not depend from 7 to 14 hour on a dose and to use mode.
At experiments on 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 Smaks and 32% increase in AUC (0-) and slower removal in comparison with women of younger age.
Pediatrics: the pharmacokinetics of a gatifloksatsin at children was not studied by age till 18 flyings.
Renal failure: the clearance of a gatifloksatsin reduced and system influence most often occurs at people with a renal failure. For patients with clearance of creatinine <30 ml \are recommended minutes doses of a gatifloksatsin are lowered.
Indications to use.
The infectious and inflammatory diseases caused by microorganisms, sensitive to a gatifloksatsin, namely: an exacerbation of chronic bronchitis, acute bacterial sinusitis, not hospital pneumonia, not complicated infections of urinary tract (cystitis), the complicated infections of urinary tract, not complicated urethral gonorrhea at men, endocervical and rectal gonorrhea at women
Way of use and dose.
Acute bronchitis, exacerbation of chronic bronchitis, pneumonia, – 400 mg, once a day within 7 - 10 days.
Acute sinusitis – 400 mg of 1 times a day within 7 - 14 days.
Not complicated infections of urinary tract – 400 mg once or 200 mg of 1 times a day within 3 days.
The complicated infections of urinary tract – 400 mg a day within 7 – 14 days.
Not complicated urethral gonorrhea at men and not complicated endocervical and rectal gonorrhea at women – 400 mg once.
Dose adjustments for patients with a renal failure.
As gatifloksatsin it is removed generally by renal excretion, the patient with clearance of creatinine <40 ml/minutes including patients on a hemodialysis or on a long-term out-patient peritoneal dialysis, correction is necessary for the dosage mode.
Such dosages of drug at patients with renal dysfunction are recommended:
Clearance of creatinine
> 40 ml/minutes.
400 mg of every day
200 mg of every day
200 mg of every day
Long out-patient peritoneal dialysis
200 mg of every day
Chronic liver failure: there is no need to carry out correction of the mode of a dosage of Gatimak In/in for patients with abnormal liver functions.
Gatimak In/in it is necessary to apply only by infusions, he is not appointed for intramuscular, intrarektalny, intra belly or hypodermic use.
Infusion should be carried out within 60 minutes.
This strong solution for infusions should be diluted by means of corresponding solution before intravenous use. Concentration of the received weak solution has to make 2 mg/ml before use.
Compatible intravenous solutions are 5% of Dextrosum for injections, 0, 9% of sodium chloride for injections, 5% of Dextrosum and 0, 9% of sodium chloride for injections, Ringer's lactate and 5% of Dextrosum for injections, water for injections.
The most widespread side effects of a gatifloksatsin - vomiting, diarrhea, a vaginitis, abdominal pain, a headache, dizziness.
Other side effects – taste disturbance, allergic reactions, a fever, heat, a dorsodynia, a stethalgia, heartbeat, a lock, dyspepsia, a glossitis, candidiasis of an oral cavity, stomatitis, an ulcer of an oral cavity, peripheral hypostases, an uneasy dream, sleeplessness, paresthesias, a tremor, vasodilatation, dispnoe, pharyngitis, perspiration, a vision disorder, a ring in ears, a dysuria and a hamaturia.
The photosensitization was observed not more often than at placebo use.
Kvinolona sleeplessness, hallucinations and paranoia can be the cause of disturbances of the central nervous system (CNS), including nervousness, concern.
Contraindications. Gatifloksatsin of contraindications to patients with hypersensitivity to a gatifloksatsin, kvinolonovy antibacterial components and other components of this drug.
Pregnant women and women who nurse, age till 18 flyings.
In case of overdose of a gatifloksatsin the patient has to is under control and to receive the symptomatic and supporting treatment. It is necessary to carry out the regidratation corresponding states. Gatifloksatsin is not rather effectively brought from an organism by a hemodialysis (about 14% within 4 hours) or by means of CAPD (about 11% - in 8 days).
Features of use.
It is necessary to appoint gatifloksatsin with care in the presence of a renal failure. Detailed clinical inspection and the corresponding laboratory analyses need to be carried out before and during a course of treatment and in case of need to lower a dose of a gatifloksatsin. At patients with the broken renal function (the clearance of creatinine <40 ml \minutes) dose adjustment needs to be carried out for avoidance of accumulation of a gatifloksatsin because of reduced clearance.
As well as in case of use of other kvinolon, disturbance of contents of glucose in blood, including symptomatic hyper - and a hypoglycemia, were revealed in most cases at the patients sick with diabetes who receive parallel treatment, using orally hypoglycemic drugs (for example, Glyburidum) or insulin. In these patients it is recommended to carry out control of level of glucose to blood.
Gatifloksatsin can entail increase in QT of intervals of the electrocardiogram at some patients. Thanks to insufficient clinical experience, gatifloksatsin patients should not apply with the intervals prolonged by QT, to patients with an inadequate hypercalcemia and to patients who receive class drugs І And (for example, kvinidin, protsaunamid) or a class ІІІ (for example, Amiodaronum, sotalol), protiaritmichesk drugs.
Pharmacokinetic researches were not conducted concerning a gatifloksatsin and drugs which extend QT intervals, such as tsisaprayd, erythromycin, protipsikhotiks and tricyclic antidepressants. Gatifloksatsin it is necessary to apply carefully at parallel use with these drugs. Drug should be used carefully to patients with heart diseases (acute ischemia of a myocardium).
Serious and fatal cases of hypersensitivity and\or anaphylactic reactions were observed at patients who passed treatments kvinolony.
Gatifloksatsin should not be applied at the first manifestations of hypersensitivity - an enanthesis or other allergic reactions.
Solution of a gatifloksatsin for infusions cannot be used if solution muddy or if are available a deposit. If a bottle it was damaged, that is it is broken sterility, solution cannot be applied. As anticoagulants and bacteriostatic components are not a part of drug, it is necessary to follow the rules of an asepsis at preparation and administration of final solution. The prepared solution of a gatifloksatsin is used right after preparation.
There is no information the concerning compatibility of a gatifloksatsin with other intravenous solutions therefore it is necessary to limit uses of additional drugs, and also their introductions through one catheter. At introduction through one catheter of other drugs consistently it needs to be washed out before introduction of a gatifloksatsin by means of solution which is compatible with gatifloksatsiny and other drugs.
Gatimak's interaction with other medicines. Use of a gatifloksatsin does not influence system 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.
Parallel use of a gatifloksatsin and theophylline did not influence pharmacokinetics of any of drugs.
Parallel use of a gatifloksatsin and warfarin did not influence pharmacokinetics of any of drugs, a prothrombin time did not change.
Parallel use of a gatifloksatsin and Glyburidum (at a stable state once a day) patients from the 2nd type of a diabetes mellitus of much considerable influence on arrangements of any of drugs, glucose levels on an empty stomach did not change.
Interactions at parallel use of the drugs stated above with gatifloksatsiny were not revealed.
Parallel use of a gatifloksatsin and digoxin not of a distance of considerable effect concerning change of pharmacokinetics of a gatifloksatsin, however, increase of concentration of digoxin was observed at 3-11 patients. Patients who accept digoxin should be controlled on signs and\or symptoms of development of intoxication. At patients who have signs and\or symptoms of intoxication of digoxin concentration of digoxin in serum has to be checked, and the dose of digoxin is modified respectively.
System removal of a gatifloksatsin considerably increases at parallel use of a gatifloksatsin and probenetsid.
At patients who received warfarin serious changes in time of turning of blood at parallel use of a gatifloksatsin were not revealed. However, thanks to the fact that some kvinolona increase effect of warfarin or equivalents of this drug a prothrombin time or other corresponding test for turnings it has to be controlled strictly if kvinolon antibacterial is appointed together with warfarin or equivalents of this drug.
During preclinical and clinical trials it is revealed that at parallel use with non-steroidal anti-inflammatory drugs, such as kvinolon, came to light that kvinolon can increase risk of disturbances of TsNS and spasms.
Conditions and periods of storage.
To be stored at a temperature not above 25 °C, in protected from light and the place, unavailable to children.