Gatifloksatsin

General characteristics. Structure:

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

Antibacterial agent of a wide range of antimicrobic action.

Pharmacological properties:

Pharmacodynamics. Gatifloksatsin is 8-metoksiftorkhinolon, active rather wide range of gram-negative and gram-positive microorganisms.

Are sensitive to effect of drug:

- gram-positive microorganisms: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes;

- gram-negative microorganisms: Haemophillus influenzae (including the strains producing β-lactamazu), Haemophillus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including the strains producing β-lactamazu), Escherichia coli, Enterobacter cloacae, Neisseria gonorrhoeae (including the strains producing β-lactamazu);

- atypical activators: C. pneumoniae, C. trachomatis, M. pneumoniae, L. pneumophilia, Ureaplasma;

Are moderately sensitive:

- gram-positive microorganisms: Streptococcus milieri, Streptococcus mitior, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohnii, Staphylococcus epidermidis (including metitsilinrezistentny strains), Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae;

- gram-negative microorganisms: Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgerri, Providencia stuartii;

- anaerobe bacterias: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroidesovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevotella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum;

- atypical activators: Legionella pneumophila, Caxiella burnettii.

Also such activators as mycobacteria of tuberculosis, H. pylori are sensitive to a gatifloksatsin.

It inhibits DNK-girazu enzyme and ІV topoisomerase which are responsible for process of drawing up chromosomal DNA in a superspiral around nuclear RNA, breaks DNA biosynthesis, growth and division of bacteria; causes the expressed morphological changes (including a cell wall and membranes) and bystry death of microorganisms.

The mechanism of action of ftorkhinolon differs from effect of penicillin, cephalosporins, aminoglycosides, macroleads and tetracyclines.

Indications to use:

The infectious and inflammatory processes caused by microorganisms, sensitive to drug:

- lower respiratory tract infections (acute bronchitis and aggravation chronic, cystous fibrosis, acute 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;

- uncomplicated urethral gonorrhea at men;

- endocervical and rectal gonorrhea at women;

- acute otitises.

Route of administration and doses:

The dose and duration of therapy are always defined by the doctor individually. As a rule, to adults and persons 18 years of age or over at the acute and complicated bronchitis, pneumonia, infections of skin and hypodermic cellulose, acute pyelonephritis and the complicated infections of urinary tract the dose of drug makes 400 mg once a day or on 200 mg two times a day for 7 - 10 days.

at acute sinusitis appoint 400 mg of drug once a day or 200 mg two times a day for 7 - 14 days.

At uncomplicated infections of urinary tract (cystitis) an initial dose of drug are 400 mg or 200 mg once a day, for 3 days.

At uncomplicated urethral gonorrhea at men, cervical gonorrhea at women – 400 mg once a day.

As Gatifloksatsin is allocated generally by renal secretion, to patients with clearance of creatinine <40 ml/min., including the patients who are on a hemodialysis or long out-patient peritoneal dialysis correction of the mode of dosing is necessary. The scheme with single use of drug a dose of 400 mg (for treatment of uncomplicated infections of uric ways and gonorrhea) and 200 mg once a day for 3 days does not need dose adjustment at patients with a renal failure.

Use of drug does not depend on meal.

Features of use:

Elderly persons and at patients with an impaired renal function have no need to change a dosage.

Gatifloksatsin can extend QT an electrocardiogram interval therefore it is not appointed to patients from the extended QT an interval which is not adjusted by a hypopotassemia and to the patients receiving antiarrhythmic means of a class ІА (quinidine, новокаинамид) or a class ІІІ (Amiodaronum, соталол).

As well as other hinolona, Gatifloksatsin with care appoint at pathology of the central nervous system in the anamnesis: at mental diseases, epilepsy, heavy atherosclerosis of vessels of a brain (risk of disturbance of blood supply, a stroke), and also at renal failures, when clearance of creatinine less than 40 ml/min. (control of concentration of drug in a blood plasma is necessary).

Influence on glucose level in blood. At Gatifloksatsin's reception change of level of glucose in blood, including a symptomatic hypoglycemia and a hyperglycemia is observed. Disturbances most often develop at the patients suffering from a diabetes mellitus. However cases of a hypoglycemia and a hyperglycemia at the patients who do not have a diabetes mellitus in the anamnesis are described. In addition to a diabetes mellitus, other risk factors of development of dysglycemias are defined: advanced age (≥ 65 years), a renal failure and a concomitant use of the medicines influencing glucose level (in particular, hypoglycemic medicines). With a renal failure it is necessary to make correction of a dose depending on clearance of creatinine for patients. At patients with the above-stated risk factors it is necessary to make constant control of level of glucose in blood. In case of symptoms of a hypoglycemia or a hyperglycemia at the patient accepting Gatifloksatsin it is necessary to take measures for normalization of level of glucose in blood and to stop Gatifloksatsin's reception.

If heavy diarrhea develops, it is necessary to exclude pseudomembranous colitis (at which hinolona are contraindicated). Drug can cause dizziness that should be considered to the patients working with potentially dangerous mechanisms, the managing director of vehicles, or connected with the activity demanding attentiveness and coherence of actions.

To avoid alcohol intake at administration of drug.

It is necessary to be careful at co-administration of Gatifloksatsin and a probenitsid as at the same time Gatifloksatsin's AUC raises that can serve as a cause of infringement of carbohydrate metabolism. Drug is removed by kidneys therefore the risk of toxic reactions is increased at patients with a renal failure. As people of old age (65 years are more senior) are more inclined to similar reactions, it is necessary to select doses with care, and also it is necessary to control functions of kidneys. Elderly patients who have an undetected diabetes mellitus age depression of function of kidneys, the accompanying pathology and/or at the same time accept the medicines influencing glucose level in blood, enter into group of high risk of development of serious violations of carbohydrate metabolism.

Side effects:

General state: fever, perspiration, dorsodynia and thorax.

From a nervous system and sense bodys: sleep disorder, paresthesia, tremor, expansion of blood vessels, dizziness.

From cardiovascular system: tachycardia.

From system of digestion: abdominal pain, lock, dyspepsia, glossitis, stomatitis, vomiting.

From a respiratory organs: short wind, pharyngitis.

From urinogenital system: hamaturia, dysuria.

Allergic reactions: skin rash.

Disturbances of carbohydrate metabolism: a hyperglycemia (with a frequency> 0,1% and <3 %), a diabetes mellitus, a hypoglycemia (with a frequency <0,1%), a giperosmolyarny neketoatsidotichesky hyper glycemic coma, diabetic ketoacidosis.

Interaction with other medicines:

The antacids containing ions of aluminum, magnesium or calcium, vitamins C microelements, gland sulfate zinc reduce absorption (it is recommended to apply for 4 h before reception of these drugs).

Probenitsid increases concentration in blood.

At combined use of milk, calcium of a carbonate, Cimetidinum, theophylline, midazolam with Gatifloksatsin any considerable interaction is not observed therefore correction of a dose is not necessary.

Combined use of Gatifloksatsin and digoxin does not cause considerable change in Gatifloksatsin's pharmacokinetics, however increase in concentration of digoxin was observed. Patients at whom symptoms of intoxication are observed by digoxin need determination of its level in plasma, and also correction of a dose.

At combined use of Gatifloksatsin with warfarin of change in a blood clotting time were not noted. However because some hinolona can strengthen effect of warfarin and other anticoagulants, it is necessary to control a prothrombin time or to hold other corresponding anticoagulating testing.

The concomitant use of a gatifloksatsin (once a day in a dose of 400 mg for 10 days) and Glyburidum (constant reception once a day) patients with the second type of a diabetes mellitus does not affect distribution of both drugs. In the researches in vitro lack of influence of a gatifloksatsin on activity of an isoenzyme of CYP3A4 was confirmed. However pharmakodinamichesky interaction at simultaneous use of a gatifloksatsin with Glyburidum and other hypoglycemic medicines was revealed.

Increases risk of increase in excitement of the central nervous system and convulsive reactions against the background of non-steroidal anti-inflammatory drugs.

Contraindications:

Hypersensitivity (including to other ftorkhinolona), pregnancy, a lactation, children's age up to 18 years, a diabetes mellitus.

Overdose:

Symptoms. Slackness and decrease in a respiration rate, vomiting, tremor and spasms.

Treatment. Gastric lavage, use of emetic drugs, introduction of a large amount of liquid. The patient has to be under fixed supervision, including control of the electrocardiogram. All events need to be held against the background of support of the vital functions.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 200 mg and 400 mg on 10 tablets in bank.