Beginning >> Drugs >> Subcategories >> System, antibacterial >> Gatinova

Drugs: A | B | With | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 2 | 5 | And | B | In | | D | E | | Z | And | Y | To | L | M | N | About | P | R | With | T | At | F | X | C | H | Sh | Shch | E | Yu | I |

Gatinova

Gatinova (GATINOVA)

General characteristic:

international and chemical name: gatifloxacin; (±)-1-cyclopropyl-6-fluorine-1, 4-digidro-8-metoksi-7-(3-methyl-1-piperazinil) - 4-oxo-3-quinoline carboxylic acid hemihydrate;

Main physical and chemical characteristics: tablets of white or almost white color, kaplepodobny form, coated;

Structure. 1 tablet of Gatinov contains a gatifloksatsin of 200 mg or 400 mg;

other components: cellulose microcrystallic, sodium krakhmalglikolit, magnesium stearate, a gidroksipropilmetiltsellyuloz, polysorbate 80;

cover: opadray white.

Form of production of medicine. Tablets, coated.

Farmakoterapevtichesky group. Antimicrobic drug of group of ftorkhinolon.

Code of automatic telephone exchange J01M A16.

Effect of the medicine. Pharmacodynamics. Bactericidal action of a gatifloksatsin, as well as other fluorinated hinolon, is caused by its ability to block bacterial DNK-girazu enzyme. DNK-giraza is the important enzyme involved in replication, a transcription and a reparation of bacterial DNA. Drug also suppresses topoisomerase IV. As for the last it is known that it plays a key role in division of chromosomal DNA during a distribution period of a bacterial cell. The action spectrum of a gatifloksatsin covers such species of microorganisms:

- gram-positive - Staphylococcus aureus, Streptococcus pneumoniae (including as are sensitive, and strains, resistant to penicillin), Streptococcus pyogenes, Streptococcus saprophiticus, Staphylococcus epidermidis (metitsillinchuvstvitelna strains), Staphylococcus (C, G groups, F), Streptococcus agalactiae;

- gram-negative - Escherichia coli, Haemophillus influenzae (including strains which produce β-lactamelements), Haemophilus parainfluenza, Klebsiella pneumoniae, Moraxella catarrhalis (including strains which produce β-lactamelements), Neisseria gonorrhoeae (including strains which produce β-lactamazu), Proteus mіrabilis, Acinetobacter lwoffii, Citrobacter koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Klebsiella oxytoca, Moragnella morganii, Proteus vulgaris, other microorganisms - Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae.

Vidminnost of a gatifloksatsin is high activity of rather anaerobic microorganisms, including Peptostreptococcus species is relative.

Pharmacokinetics. Gatifloksatsin is well soaked up in a digestive tract after reception of per os. Absolute bioavailability of a gatifloksatsin makes 96%. Peak concentration of a gatifloksatsin in plasma is reached in 1 - 2 hour after peroral introduction. Averages peak and minimum concentration which are reached when using the scheme of introduction of 400 mg of 1 times a day represent about 4, 2 mkg/ml and 0, 4 mkg/ml, respectively for peroral introduction. Linkng of a gatifloksatsin with proteins of serum makes nearly 20% and does not depend on concentration. Gatifloksatsin is widely distributed in an organism after many fabrics and to liquids, including alveolar macrophages, a bronchial mucous membrane, liquid of an epithelial vystilka of lungs, a parenchyma of lungs, a mucous membrane of sine, phlegms, an ejaculate, semen, a mucous membrane of a vagina and a neck of uterus. Fast distribution of a gatifloksatsin in fabric brings to higher of its concentration in the majority of target organs, than in serum. Gatifloksatsin at people gives in limited biotransformations. At the same time less than 1% of the entered dose are excreted in urine in the form of etilendiaminovy and metiletilendiaminovy metabolites. More than 70% of the entered dose of a gatifloksatsin are removed in not changed view with urine during the 48th hour after peroral introduction; 5% are brought with excrements.

Indications for use. Treatment of the infections caused by microorganisms, sensitive to drug:

infections of ENT organs, including acute sinusitis;

respiratory infections: pneumonia and exacerbation of chronic bronchitis;

infections of skin and soft tissues;

infections of kidneys and urinary tract: pyelonephritis, the complicated and not complicated infections of urinary tract;

venereal diseases of an urethra, neck of uterus, rectum.

Way of use and dose. Gatinova is accepted 1 time a day irrespective of reception of food. The recommended Gatinova's doses for adult patients with normal function of kidneys are given in the following table 1:

Table 1.

Diseases

Daily

dose

Therapy duration

Bacterial exacerbation of chronic bronchitis

400 mg

5 days

Acute sinusitis

400 mg

10 days

Extra hospital pneumonia

400 mg

7 - 14 days

Not complicated infections of urinary tract (cystitis)

200 - 400 mg

3 days

The complicated infections of urinary tract

400 mg

7 - 10 days

Acute pyelonephritis

400 mg

7 - 10 days

Infections of skin and soft tissues

400 mg

7 - 10 days

Not complicated urethral gonorrhea at men

Endocervical and rectal gonorrhea at women

400 mg

1 day

Doses for patients with an impaired renal function.

The initial dose of drug does not differ from a dose for patients with normal function of kidneys, further dosages - respectively to table 2:

Table 2.

Clearance of creatinine

Initial dose

Following dose

≥ 40 ml/minutes

400 mg

400 mg daily

<40 ml/minutes

400 mg

200 mg daily

Hemodialysis

400 mg

200 mg daily

Peritoneal dialysis

400 mg

200 mg daily

For an assessment of clearance of creatinine it is recommended to use such formula:

men:

clearance of creatinine (ml/minutes) = the body weight (kg) x (140 - age)/72 x the level of creatinine in serum (mg/dl);

women: 0, 85 x clearance of creatinine of men.

For patients with moderately broken function of a liver to reduce a dose there is no need.

Side effect. Symptoms ordinary arise seldom and quickly pass after drug withdrawal.

Digestive tract and liver: nausea, diarrhea, an abdominal pain, anorexia, a lock, dyspepsia, a meteorism, gastritis, a glossitis, ulcers in an oral cavity, stomatitis, an ulitis, vomiting, gastrointestinal bleeding.

Central nervous system: a headache, dizziness, a sleep disorder, agitation, uneasiness, the confused consciousness, sleeplessness, nervousness, paresthesia, drowsiness, a tremor, spasms, depersonalization, a depression, the panic attack, paranoia, photophobia, hostility, a hyperesthesia, migraine, an ataxy broken sight, disturbance of flavoring feelings, photosensitivity of eyes.

Cardiovascular system: tachycardia, bradycardia, hypertensia, cyanosis.

Allergic and skin reactions: face edema, makulopapulezny rashes, paraglossa, generalized hypostasis, vezikulobullyozny rash.

Others: a vaginitis, an ostealgia, a stethalgia, arthritis, a hypoglycemia, hyperventilation, a hamaturia, thirst, temperature, a xeroderma, a metrorrhagia, a bronchospasm, ear pain is increased.

Contraindications. Drug is contraindicated to patients with hypersensitivity to a gatifloksatsin or other ftorkhinolon in the anamnesis. Drug is also contraindicated to children till 16 flyings, to pregnant women and women who nurse.

Overdose. Symptoms: strengthening of side effects.

Treatment: there is no specific antidote; the recommended general measures of emergency medical service, the hemodialysis is dobavochno recommended to carry out.

Features of use. Gatifloksatsin can entail increase in QT of intervals of the electrocardiogram at some patients. Through insufficient clinical experience gatifloksatsin it should not be applied to patients with the prolonged QT intervals, to patients with a hypercalcemia and to patients who receive pro-thiarhythmic drugs of a class ІІ And (for example quinidine, procaineamide) or a class ІІІ (for example, Amiodaronum, sotalol). Gatifloksatsin has to be applied with care at simultaneous use with tsisapridy, erythromycin, antipsychotic drugs. Patients need to use drug with care with pro-arhythmic conditions and such defeats of cardiovascular system as bradycardia and acute ischemia of a myocardium. As well as other ftorkhinolona, gatifloksatsin it is necessary to apply with care at patients with such disturbances of TsNS as heavy cerebral atherosclerosis, epilepsy, and other diseases which can entail spasms. Gatifloksatsin should not be applied at the first manifestations of hypersensitivity - a vysipaniye on skin or other allergic reactions.

Gatinov's drug cannot be used together with alcoholic beverages.

Influence on driving by motor transport and work with unsafe mechanisms.

Speed of psychomotor reactions therefore it is worth abstaining from control of vehicles and mechanisms can be broken.

Disturbances of contents of glucose in blood, including symptomatic hyper - and a hypoglycemia, were revealed at patients who accepted gatifloksatsin or other ftorkhinolona together with hypoglycemic drugs. In such patients it is recommended to control glucose level in blood.

Interaction with other medicines. Gatifloksatsin it is necessary to accept the 4th hour prior to reception of ferrous sulfate, food additives which contain zinc, magnesium or iron (such as polyvitamins), or antacids which contain magnesium and aluminum. When sharing from calcium by a carbonate, Cimetidinum, theophylline, midazolam, digoxin of essential interactions it was not observed. System removal of a gatifloksatsin considerably increases at parallel use of a gatifloksatsin and probenotsid. 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 hinolona increase effect of warfarin of this drug a prothrombin time or other corresponding test for turnings it has to be controlled strictly if hinolon it is appointed together with warfarin, or its derivatives. Simultaneous administration of non-steroidal anti-inflammatory drugs with ftorkhinolony can strengthen risk of stimulation of the central nervous system.

Conditions and periods of storage. To store in the place, unavailable to children, at a temperature not above 25 °C. A period of validity – 2 years.

 
"Gatimak in/in   Gatispan"