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Gatimak

Gatimak (Gatimac)

international and chemical name: gatifloxacin; the name chemical (±)-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: tablets are round, coated, white or almost white color, oboyevypukly, with a smooth surface from both sides;

Structure. 1 tablet contains a gatifloksatsin of sexivihydrat that 200 mg or 400 mg of a gatifloksatsin are equivalent;

other components: cellulose microcrystallic, sodium krakhmalglikolit, sodium lauryl sulfate, silicon dioxide colloid anhydrous, povidone (PVP K-30), sodium of a kroskarmeloz, the talc purified of magnesium stearate, a gidroksipropilmetiltsellyuloz,

titanium dioxide, propylene glycol, diethyl phthalate.

Form of production of medicine. Tablets, coated.

Farmakoterapevtichesky group. Antimicrobic means for system use. Ftorkhinolona. Code of automatic telephone exchange J01MA16.

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 can act against pathogens which are resistant to these antibiotics. There is no cross firmness between gatifloksatsiny and the specified antibiotics.

Gatifloksatsin has antibacterial activity against the broad range of gram-negative and gram-positive microorganisms. Antibacterial action of a gatifloksatsin is provided thanks to suppression of DNA - giraza and topoisomerases IV. DNA - a 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 activators - gram-positive microorganisms are sensitive for treatment corresponding to a nosology which reason is: 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 – 96%. The concentration peak in plasma comes in 1-2 hours after peroral use.

Linkng with proteins of a blood plasma makes nearly 20%.

Gatifloksatsin well gets into the most part of body tissues and is quickly distributed on 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, 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.

It is removed by kidneys. The average of removal of a gatifloksatsin – also does not depend from 7 to 14 hours 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 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 revealed by age till 18 flyings.

Renal failure: clearance of a gatifloksatsin reduced and system influence more expressed at people with a renal failure.

Indications to use. Gatimak is shown to patients 18 years for treatment of the infectious and inflammatory processes caused by microorganisms, sensitive to drug, such as are more senior:

respiratory infections (acute bronchitis, chronic bronchitis, cystous fibrosis, pneumonia);

infections of kidneys and urinary system (acute and chronic pyelonephritis, prostatitis, cystitis; persistent infections of an urinary system);

infections of skin and soft tissues;

infections of bones and joints;

infections of a digestive tract;

postoperative infectious complications;

not complicated urethral gonorrhea at men;

endocervical and rectal gonorrhea at women.

Way of use and dose. Drug is accepted irrespective of reception of food.

At the acute and complicated chronic bronchitis, pneumonia, infections of skin and hypodermic cellulose, acute pyelonephritis and the complicated infections of an urinary path the dose of drug makes 400 mg, once a day or on 200 mg two times a day, within 7-10 days.

At acute sinusitis appoint 400 mg of drug once a day or 200 mg 2 times a day, within 7-14 days.

At not complicated infections of an uric path (cystitis) an initial dose of drug are 400 mg or 200 mg once a day, within 3 days.

At not complicated urethral gonorrhea at men, cervical gonorrhea at women – 400 mg once a day.

As Gatimak is brought generally by renal excretion, to patients with clearance of creatinine <40 ml/minutes, including patients who are on a hemodialysis or a long out-patient peritoneal dialysis, correction of the mode of a dosage is necessary. Such changes of a dosage of drug at patients with a renal failure are recommended:

Clearance of creatinine, ml/minutes

Initial dose, mg

Following dose

=> 40

400

400 mg daily

<40

400

200 mg daily

Hemodialysis

400

200 mg daily

Long out-patient peritoneal dialysis

400

200 mg daily

The scheme with single application of drug in a dose of 400 mg (for treatment of not complicated infections of uric ways and gonorrhea) and 200 mg of 1 times a day within 3 days does not demand dose adjustment from patients with a renal failure.

Side effect. Faints, vomiting, diarrhea, a vaginitis, abdominal pain, a headache, taste disturbance, 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, paresthesias, a tremor, vasodilatation, dispnoe, pharyngitis, perspiration, a vision disorder, a ring in ears, a dysuria and a hamaturia.

Gatimak can be the cause of disturbances of the central nervous system, including irritability, concern, sleeplessness, nightmares or Parana.

Contraindications. Gatimak 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.

Symptoms: strengthening of side effects.

In case of peroral Gatimak's overdose it is necessary to carry out a gastric lavage. The patient has to be under control and receive the symptomatic and supporting treatment. It is necessary to apply the hydration therapy corresponding to a state. Gatimak is insufficiently effectively brought from an organism by a hemodialysis (about 14% within 4 hours) or by means of the forced hemodialysis (about 11% in 8 days).

Features of use. Gatimak can entail increase in QT of intervals of the electrocardiogram at some patients. Through insufficient clinical experience gatifloksatsin it should not be applied by patients with the intervals prolonged by QT, patients with an inadequate hypercalcemia and patients who receive a class І And (for example, kvinidin, procaineamide) or a class ІІІ (for example, Amiodaronum, sotalol) pro-thiarhythmic drugs.

Pharmacokinetic researches were not conducted for Gatimak and drugs which extend QT intervals, such as tsizaprid, erythromycin, protipsikhotiks and tricyclic antidepressants. Gatimak has to be applied with care at parallel use with these drugs. Patients need to use drug with care with bradycardia and acute ischemia of a myocardium.

Serious and fatal cases of hypersensitivity and anaphylactic reactions were observed at patients who passed treatments kvinolony.

Gatimak it is not necessary to apply at the first manifestations of hypersensitivity - an enanthesis or other allergic reactions.

It is necessary to apply carefully during the period control of vehicles (possibly dizziness).

With care it is necessary to appoint Gatimak sick with a renal failure. Careful clinical inspection and the corresponding laboratory analyses need to be carried out to and during a course of treatment, if necessary it is necessary to lower Gatimak's dose. To patients with the broken renal function (clearance of creatinine <40 ml/minutes) it is necessary to carry out dose adjustment (dose decline) to avoid accumulation of a gatifloksatsin through decrease in clearance. <30 ml \are recommended minutes to patients with clearance of creatinine Gatimak's doses are lowered.

In most cases at the patients sick with diabetes who receive parallel treatment peroral hypoglycemic drugs (for example, Glyburidum) or insulin disturbance of contents of glucose in blood, including symptomatic hyper - and a hypoglycemia was revealed. In such patients it is recommended to carry out control of level of glucose to blood.

Interaction with other medicines. Gatimak's reception in 1 hour after Cimetidinum (once a day, orally, in a dose of 200 mg) does not influence pharmacokinetics of a gatifloksatsin. These results demonstrate that absorption of a gatifloksatsin is influenced by antagonists of H2 receptors, such as Cimetidinum.

Gatimak's use 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 Gatimak and theophylline did not influence pharmacokinetics of any of drugs.

Parallel use of Gatimak and warfarin did not influence pharmacokinetics of any of drugs, the prothrombin time not to change.

Parallel use of Gatimak and Glyburidum (at a stable state once a day) patients with the 2nd like a diabetes mellitus of much considerable influence on arrangements of any of drugs, glucose levels on an empty stomach did not change.

Parallel 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 modified respectively.

System removal of a gatifloksatsin considerably increases at parallel use of Gatimak and a probenetsid.

At patients who received warfarin serious changes in time of turning of blood at parallel use of Gatimak were not revealed.

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 store at a temperature not above 25 °C, in the place, dry and unavailable to children.

Period of validity – 2 years.

 
"Gatidzhem   Gatimak in/in"