Pharmacological properties: gatifloxacin (+)-1-cyclopropyl-6-fluoro-1 ,4-dihydro-8-methoxy-7-(3-methyl-1-piperazine)-4-oxo-3-acid hinolinkarboksilnaya seskvigidrat. Gatifloxacin - 8-methoxy fluoroquinolone - active against a broad spectrum of gram-positive and gram-negative microorganisms. The antibacterial action of gatifloxacin is associated with inhibition of DNA gyrase and topoisomerase IV.
In vitro gatifloxacin is active against a broad spectrum of microorganisms, including bacteria that produce b-lactamases, and Pseudomonas: Gram - Enterobacteriaceae, including E. coli, Klebsiella pneumoniae, Enterobacter cloacae, Proteus mirabilis, Proteus vulgaris, indolpolozhitelnye strains of Proteus, Morganella morganii , Providencia stuartii, Citrobacter freundii, Serratia marcescens. As well as Pseudomonas aeruginosa, Acinetobacter spr, H. influenzae, including strains producing β-lactamases, Salmonella typhy, Salmonella enteritidis, Shigella boydii, Shigella dysenteriae, Shigella flexneri, Shigella sonnei, Yersinia enterocolitica, Aeromonas hydrophilia, Vibrio parahaemolyticus, Vibrio cholerae, Campylobacter jejuni and N. gonorrhoeae, including strains that produce β-lactamases.
Gram-positive bacteria - most strains of Staphylococcus, including Staphylococcus aureus, Str. pyogenes, S. epidermidis, including methicillin strains of Streptococcus pneumoniae, including MDRSP: Multidrug-resistant Streptococcus pneumoniae, ie strains of multidrug-resistant (resistant to penicillin, trimethoprim / sulfometoksazolu, potentiated penicillins, cephalosporins, macrolides, tetracyclines, aminoglycosides), Staphylococcus saprophyticus, and enterococci that are sensitive to ofloxacin, atypical Chl. pneumoniae, L. pneumoniae, M. pneumoniae, anaerobic Peptococcus spr.
Gatifloxacin is not effective against Bacteroides, Clostridia and Fusobacteria spp.
Gatifloxacin is active against bacterial strains resistant to gentamicin, cefazolin, and Carbenicillin.
Oral and i / in the introduction gatifloxacin considered interchangeable because the pharmacokinetics of gatifloxacin after 1 h after i / v application is similar to that after oral administration of gatifloxacin at the same dose. The absolute bioavailability of gatifloxacin is 96%. The maximum concentration of gatifloxacin in plasma usually achieved within 1-2 hours after oral administration. The pharmacokinetics of gatifloxacin in the linear range of doses from 200 to 800 mg and the duration of admission to 14 days. The equilibrium state is achieved to the 3 rd day of oral or / in the introduction of gatifloxacin. Average maximum and minimum concentration in plasma at equilibrium which is achieved when the scheme dosage of 400 mg 1 time per day, approximately 4,2 and 0,4 g / ml, respectively, with oral and 4,6 and 0,4 g / ml, respectively, in in / introduction.
The degree of binding of gatifloxacin in plasma proteins is about 20% and does not depend on concentration. The average volume of distribution of gatifloxacin in an equilibrium state varies from 1,5 to 2 l / kg body weight. Gatifloxacin distributed in tissues and body fluids. Rapid distribution of gatifloxacin into tissues leads to the achievement of most tissues of higher concentrations than in serum. Gatifloxacin released in the form of unchanged drug primarily in the urine. Over 70% of gatifloxacin released in the form of unchanged drug in urine within 48 h after oral and / in use, 5% is excreted in the feces. The average half-life of gatifloxacin ranges from 7-14 h and is not dependent on the dose and method of application. Renal clearance is not dependent on the dose and an average of 124-161 ml / min.
INDICATIONS: infectious-inflammatory diseases caused by microorganisms susceptible to gatifloxacin.
APPLICATION:
Application
Daily dose, mg *
The duration of treatment, days
Chronic bronchitis exacerbation
400
7.10
Acute sinusitis or chronic sinusitis in acute
400
10-14
Community-acquired pneumonia
400
7-14
Infections of skin and soft tissue
400
7.10
Pyelonephritis
400
7.10
Uncomplicated urinary tract infections
400
The initial dose, further dose determined on the basis of nosology
Complicated urinary tract infections
400
7.10
Uncomplicated gonococcal urethritis in men, gonococcal endocervicitis and proctitis in women
400
One time
* The drug is used 1 times per day.
Since gatifloxacin is derived mainly by renal excretion, patients with creatinine clearance <40 ml / min, including patients on hemodialysis or prolonged ambulatory peritoneal dialysis, must be corrected dosing regimen.
No need for dose adjustment Dasikona in patients with moderate hepatic impairment. Data on the use of the drug in patients with severe hepatic impairment is not.
The age of the patient does not affect the pharmacokinetics of the drug, but because elderly patients renal dysfunction more likely to be careful to choose dose and regular monitoring of renal function.
Dasikon rr can be used only by the in / infusion, it is not designed for a / m, intrarectal, intraperitoneal or sc injection. Infusion should be carried out for 60 min.
Concentrated rr for infusion should be diluted with the corresponding p-rum in front of / in the application. The concentration obtained diluted p-ra should be 2 mg / ml.
Be compatible p-holders are 5% p-p dextrose injection, 0.9% p-r sodium chloride for injection, p-p 5% dextrose, pp Ringer's lactate, 5% p-r sodium bicarbonate injection and water injection.
CONTRAINDICATIONS: Hypersensitivity to Dasikonu or group of fluoroquinolone antibacterial drugs, pregnancy, age 15 years, the deficit of glucose-6-phosphate dehydrogenase.
SIDE EFFECTS: generally well tolerated, and may sometimes be vomiting, vaginitis, diarrhea, headache, dizziness. In patients taking Quinolone, noted increased intracranial pressure and the development of psychotic excitement.
Cautions: Dasikon can increase the Q-T interval on the electrocardiogram in some patients. Due to insufficient clinical experience Dasikon should not be considered in patients with extended Q-T interval and patients taking antiarrhythmics, IA (quinidine, procainamide) or class III (amiodarone, cotalol). Pharmacokinetic studies of the interaction between gatifloxacin and drugs that can increase the range of Q-T (tsizaprid, erythromycin, antipsychotic tools and tricyclic antidepressants), were not conducted.
Patients driving a motor vehicle or working with dangerous machinery, be aware that Dasikon can cause the development of dizziness and sensitivity to light.
Use of the drug during pregnancy and lactation may be the case, if the expected therapeutic effect for the mother outweighs the potential risk to the fetus or infant.
Safety and efficacy of the drug in children under the age of 15 is not installed.
In applying the drug to refrain from alcohol.
INTERACTION: systemic exposure gatifloxacin significantly increases after the simultaneous application of probenecid.
In the application of drugs of quinolones detect elevated levels of theophylline in blood plasma. In this regard, some noted side effects of the simultaneous application of theophylline with Dasikonom. There is therefore a need to control the level of theophylline in blood plasma, while application of these drugs.
Patients simultaneously receiving digoxin should watch for symptoms of intoxication.
Quinolone, including gatifloxacin, increase anticoagulant effect of warfarin or its derivatives. After the cessation of the simultaneous reception of these drugs is necessary to monitor the prothrombin time and other indices of coagulation.
OVERDOSE: lack of information on cases of overdose. In the case of acute overdose spend symptomatically. Provide a sufficient level of hydration. Haemodialysis and prolonged ambulatory peritoneal dialysis does not lead to effective elimination Dasikona from the body (contained at 14% after 4 h and 11% - in 8 days).
Storage: Store in dark place at a temperature of 25 ° C. Do not freeze.
In vitro gatifloxacin is active against a broad spectrum of microorganisms, including bacteria that produce b-lactamases, and Pseudomonas: Gram - Enterobacteriaceae, including E. coli, Klebsiella pneumoniae, Enterobacter cloacae, Proteus mirabilis, Proteus vulgaris, indolpolozhitelnye strains of Proteus, Morganella morganii , Providencia stuartii, Citrobacter freundii, Serratia marcescens. As well as Pseudomonas aeruginosa, Acinetobacter spr, H. influenzae, including strains producing β-lactamases, Salmonella typhy, Salmonella enteritidis, Shigella boydii, Shigella dysenteriae, Shigella flexneri, Shigella sonnei, Yersinia enterocolitica, Aeromonas hydrophilia, Vibrio parahaemolyticus, Vibrio cholerae, Campylobacter jejuni and N. gonorrhoeae, including strains that produce β-lactamases.
Gram-positive bacteria - most strains of Staphylococcus, including Staphylococcus aureus, Str. pyogenes, S. epidermidis, including methicillin strains of Streptococcus pneumoniae, including MDRSP: Multidrug-resistant Streptococcus pneumoniae, ie strains of multidrug-resistant (resistant to penicillin, trimethoprim / sulfometoksazolu, potentiated penicillins, cephalosporins, macrolides, tetracyclines, aminoglycosides), Staphylococcus saprophyticus, and enterococci that are sensitive to ofloxacin, atypical Chl. pneumoniae, L. pneumoniae, M. pneumoniae, anaerobic Peptococcus spr.
Gatifloxacin is not effective against Bacteroides, Clostridia and Fusobacteria spp.
Gatifloxacin is active against bacterial strains resistant to gentamicin, cefazolin, and Carbenicillin.
Oral and i / in the introduction gatifloxacin considered interchangeable because the pharmacokinetics of gatifloxacin after 1 h after i / v application is similar to that after oral administration of gatifloxacin at the same dose. The absolute bioavailability of gatifloxacin is 96%. The maximum concentration of gatifloxacin in plasma usually achieved within 1-2 hours after oral administration. The pharmacokinetics of gatifloxacin in the linear range of doses from 200 to 800 mg and the duration of admission to 14 days. The equilibrium state is achieved to the 3 rd day of oral or / in the introduction of gatifloxacin. Average maximum and minimum concentration in plasma at equilibrium which is achieved when the scheme dosage of 400 mg 1 time per day, approximately 4,2 and 0,4 g / ml, respectively, with oral and 4,6 and 0,4 g / ml, respectively, in in / introduction.
The degree of binding of gatifloxacin in plasma proteins is about 20% and does not depend on concentration. The average volume of distribution of gatifloxacin in an equilibrium state varies from 1,5 to 2 l / kg body weight. Gatifloxacin distributed in tissues and body fluids. Rapid distribution of gatifloxacin into tissues leads to the achievement of most tissues of higher concentrations than in serum. Gatifloxacin released in the form of unchanged drug primarily in the urine. Over 70% of gatifloxacin released in the form of unchanged drug in urine within 48 h after oral and / in use, 5% is excreted in the feces. The average half-life of gatifloxacin ranges from 7-14 h and is not dependent on the dose and method of application. Renal clearance is not dependent on the dose and an average of 124-161 ml / min.
INDICATIONS: infectious-inflammatory diseases caused by microorganisms susceptible to gatifloxacin.
APPLICATION:
Application
Daily dose, mg *
The duration of treatment, days
Chronic bronchitis exacerbation
400
7.10
Acute sinusitis or chronic sinusitis in acute
400
10-14
Community-acquired pneumonia
400
7-14
Infections of skin and soft tissue
400
7.10
Pyelonephritis
400
7.10
Uncomplicated urinary tract infections
400
The initial dose, further dose determined on the basis of nosology
Complicated urinary tract infections
400
7.10
Uncomplicated gonococcal urethritis in men, gonococcal endocervicitis and proctitis in women
400
One time
* The drug is used 1 times per day.
Since gatifloxacin is derived mainly by renal excretion, patients with creatinine clearance <40 ml / min, including patients on hemodialysis or prolonged ambulatory peritoneal dialysis, must be corrected dosing regimen.
No need for dose adjustment Dasikona in patients with moderate hepatic impairment. Data on the use of the drug in patients with severe hepatic impairment is not.
The age of the patient does not affect the pharmacokinetics of the drug, but because elderly patients renal dysfunction more likely to be careful to choose dose and regular monitoring of renal function.
Dasikon rr can be used only by the in / infusion, it is not designed for a / m, intrarectal, intraperitoneal or sc injection. Infusion should be carried out for 60 min.
Concentrated rr for infusion should be diluted with the corresponding p-rum in front of / in the application. The concentration obtained diluted p-ra should be 2 mg / ml.
Be compatible p-holders are 5% p-p dextrose injection, 0.9% p-r sodium chloride for injection, p-p 5% dextrose, pp Ringer's lactate, 5% p-r sodium bicarbonate injection and water injection.
CONTRAINDICATIONS: Hypersensitivity to Dasikonu or group of fluoroquinolone antibacterial drugs, pregnancy, age 15 years, the deficit of glucose-6-phosphate dehydrogenase.
SIDE EFFECTS: generally well tolerated, and may sometimes be vomiting, vaginitis, diarrhea, headache, dizziness. In patients taking Quinolone, noted increased intracranial pressure and the development of psychotic excitement.
Cautions: Dasikon can increase the Q-T interval on the electrocardiogram in some patients. Due to insufficient clinical experience Dasikon should not be considered in patients with extended Q-T interval and patients taking antiarrhythmics, IA (quinidine, procainamide) or class III (amiodarone, cotalol). Pharmacokinetic studies of the interaction between gatifloxacin and drugs that can increase the range of Q-T (tsizaprid, erythromycin, antipsychotic tools and tricyclic antidepressants), were not conducted.
Patients driving a motor vehicle or working with dangerous machinery, be aware that Dasikon can cause the development of dizziness and sensitivity to light.
Use of the drug during pregnancy and lactation may be the case, if the expected therapeutic effect for the mother outweighs the potential risk to the fetus or infant.
Safety and efficacy of the drug in children under the age of 15 is not installed.
In applying the drug to refrain from alcohol.
INTERACTION: systemic exposure gatifloxacin significantly increases after the simultaneous application of probenecid.
In the application of drugs of quinolones detect elevated levels of theophylline in blood plasma. In this regard, some noted side effects of the simultaneous application of theophylline with Dasikonom. There is therefore a need to control the level of theophylline in blood plasma, while application of these drugs.
Patients simultaneously receiving digoxin should watch for symptoms of intoxication.
Quinolone, including gatifloxacin, increase anticoagulant effect of warfarin or its derivatives. After the cessation of the simultaneous reception of these drugs is necessary to monitor the prothrombin time and other indices of coagulation.
OVERDOSE: lack of information on cases of overdose. In the case of acute overdose spend symptomatically. Provide a sufficient level of hydration. Haemodialysis and prolonged ambulatory peritoneal dialysis does not lead to effective elimination Dasikona from the body (contained at 14% after 4 h and 11% - in 8 days).
Storage: Store in dark place at a temperature of 25 ° C. Do not freeze.
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