Composition, form of production and packaging
Tablets, film-coated 1 tab.
gatifloxacin 200 mg
5 pieces. - packings of cellular contour (1) - packs cardboard.
Tablets, film-coated 1 tab.
gatifloxacin 400 mg
5 pieces. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Gatifloxacin acts bactericidal, affecting the replication of bacterial DNA (the target are topoisomers II and IV, which change the spatial configuration of the DNA molecule at various stages of its replication). Interacting with topoisomerase IV, causes the rupture of the DNA molecule after replication. It is active against many strains of microorganisms both in vitro and in vivo.
Gatifloxacin is active against gram-negative aerobic bacteria: Escherichiacoli, Haemophilusinfluenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria gonorrhoeae, Proteus mirabilis, Acinetobacter Iwoffii, Citrobacter koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Morganella morganii, Proteus vulgaris , Salmonella spp., Shigella spp .; for Gram-positive aerobic bacteria: Staphylococcus aureus, Staphylococcus saprophyticus, Streptococcus pneumoniae, Streptococcus pyogenes; for anaerobic bacteria: Peptostreptococcus spp., Bacteroides spp., Clostridium spp., Prevotella spp., Peptococcus spp., as well as against Chlamydia pneumoniae, Legionella pneumoniae, Mycoplasma pneumoniae.
PHARMACOKINETICS
Gatifloxacin is well absorbed from the gastrointestinal tract, food intake does not affect the absorption of the drug. Bioavailability is 96%. After ingestion of a single dose of 400 mg C max in the plasma is achieved after 1-2 hours and is 4.2 mg / l. Constant concentration in the plasma is achieved on the third day of treatment. The mean stable peak and the lowest plasma concentrations with a 400 mg dose of the drug once a day are approximately 4.2 mg / ml and 0.4 mg / ml, respectively. The binding of gatifloxacin to plasma proteins is approximately 20% and is independent of the concentration of the drug. Due to the low association with proteins, the concentration of gatifloxacin in saliva is approximately equal to the concentration in the plasma. The average V d of gatifloxacin ranges from 1.5 to 2.0 l / kg.Gatifloxacin well penetrates into many tissues and body fluids (including alveolar and pulmonary tissue, genital organs, saliva).
Gatifloxacin in humans undergoes limited biotransformation, less than 1% of the accepted dose is excreted by the kidneys in the form of metabolites - ethylenediamine and methylethylenediamine.
More than 70% of the dose after ingestion is excreted for 48 hours unchanged by the kidneys and 5% through the gastrointestinal tract. The half-life period of gatifloxacin ranges from 7 to 14 hours and is independent of the dose and route of administration of the drug. Kidney clearance is independent of the dose, the average value is from 124 to 161 ml / min.
Pharmacokinetics in special clinical cases
With a moderate violation of liver function, dose adjustment is not required. However, considering that gatifloxacin is mainly excreted by the kidneys, patients with a creatinine clearance less than 40 ml / min, as well as patients on hemodialysis or peritoneal ambulatory dialysis, require a reduction in the dose. Information on how the pharmacokinetics of gatifloxacin varies with severe liver damage is not available.
INDICATIONS
- Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation;
- exacerbation of chronic bronchitis;
- Community-acquired pneumonia.
DOSING MODE
Inside, 400 mg 1 time per day, regardless of food intake.
The course of treatment is 7-10 days.
The maximum single dose: 400 mg. The maximum daily dose: 400 mg.
For patients with impaired renal function, dosage adjustment is necessary.
With the clearance of creatinine to 40 ml / min - the initial dose is 400 mg.
Subsequent doses, starting from the second day of treatment - 400 mg daily.
When the creatinine clearance is <40 ml / min, the initial dose is 400 mg for patients on hemodialysis, permanent ambulatory peritoneal dialysis.
Subsequent doses, starting from the second day of treatment, are 200 mg daily.
In patients on hemodialysis, the drug is taken after the completion of the procedure for hemodialysis.
SIDE EFFECT
Most often (more than 3%) there are: nausea, diarrhea, headache, dizziness, vaginitis.
With a frequency of 0.1-3%:
From the nervous system: agitation, anxiety, paresthesia, insomnia, drowsiness, tremor, anxiety, excitement.
From the skin: dry skin, rash, itching.
From the urinary system: painful urination.
From the musculoskeletal system: the risk of tendonitis or rupture of the tendon increases, arthralgia.
From the digestive system: anorexia, dyspepsia, abdominal pain, gastritis, flatulence, constipation, glossitis, stomatitis, tongue ulcers, candidiasis.
From the respiratory system: shortness of breath, pharyngitis.
From the senses: visual impairment, taste distortion, ringing in the ears.
From the cardiovascular system: increased blood pressure, palpitations.
Allergic reactions: urticaria, angioedema, itching, bronchospasm, Stevens-Johnson syndrome, anaphylactic shock.
Other: chills, fever, swelling of the face and extremities, sweating, asthenia, back pain, breast, hypo- or hyperglycemia.
With a frequency of less than 0.1%:
from the side of the nervous system: ataxia, convulsions, depersonalization, depression, hallucinations, hostility, hyperesthesia, migraine, euphoria, attacks of fear.
On the part of the skin: a maculopapular rash, a vesicular rash.
From the genitourinary system: hematuria, metrorrhagia.
From the musculoskeletal system: arthritis, ossalgia, myalgia, myasthenia gravis.
From the digestive system: dysphagia, gingivitis, bad breath, swelling of the tongue, colitis (including pseudomembranous), gastrointestinal bleeding (including rectal).
On the part of the respiratory system: bronchospasm, hyperventilation.
From the senses: parosmia, ptosis, taste disorders (including its loss), pain in the ears, eyes, photophobia.
From the cardiovascular system: bradycardia, increased blood pressure, retrosternal pain.
On the part of the endocrine system: hypoglycemia, hyperglycemia, diabetes mellitus.
Laboratory indicators: neutropenia, increased levels of alanine transferase, asparagine transferase, alkaline phosphatase, amylase, hyperbilirubinemia, electrolyte disorders.
Other: intolerance to ethanol, cyanosis, lymphadenopathy, pain in the neck.
CONTRAINDICATIONS
- Hypersensitivity to gatifloxacin, other representatives of the quinolone class or other components of the drug;
- diabetes;
- prolongation of the QT interval;
- simultaneous administration of antiarrhythmic drugs of class IA (including quinidine, procainamide) or class III (including, amiodarone, sotalol);
uncontrolled hypokalemia;
- Children and adolescence (up to 18 years);
- Pregnancy;
lactation period.
Carefully:
- with diseases of the central nervous system (pronounced atherosclerosis of cerebral vessels, cerebral circulation disorders, epilepsy), predisposing to the occurrence of convulsive seizures and lowering the threshold of convulsive readiness;
- elderly patients;
- with conditions predisposing to arrhythmia (including bradycardia, acute myocardial ischemia);
- in patients taking antipsychotic drugs, tricyclic antidepressants, as well as drugs that can prolong the interval of QT (including cisapride, erythromycin), since it is not necessary to use antipsychotics. an additive effect is possible, and relevant pharmacokinetic studies have not been carried out to date;
- with renal insufficiency (creatinine clearance <40 ml / min).
PREGNANCY AND LACTATION
It is forbidden to use the drug during pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Take with caution in renal failure (creatinine clearance <40 ml / min).
For patients with impaired renal function, dosage adjustment is necessary.
In patients on hemodialysis, the drug is taken after the completion of the procedure for hemodialysis.
APPLICATION FOR CHILDREN
Contraindicated in childhood and adolescence (under 18 years).
APPLICATION IN ELDERLY PATIENTS
Prescribe cautiously to elderly patients.
SPECIAL INSTRUCTIONS
Gatifloxacin can cause neurological side effects, so people on treatment with the drug should not drive motor vehicles or other mechanisms that require increased attention and coordination.
It is necessary to monitor the concentration of glucose in the blood plasma, especially in patients with risk factors for diabetes mellitus, chronic renal failure, in elderly patients, while taking with hypoglycemic drugs.
During the period of treatment, ECG monitoring (prolongation of the QT interval, ventricular arrhythmias) is necessary. The degree of elongation of the QT interval may increase with increasing drug concentration, therefore, do not exceed the recommended dose. The prolongation of the QT interval is associated with an increased risk of ventricular arrhythmias, including flicker-flutter.
Against the background of therapy with fluoroquinolones, including gatifloxacin, especially in elderly patients receiving glucocorticosteroids, tendonitis and tendon rupture are possible. At the first symptoms of pain or inflammation at the site of damage, taking the drug should stop and unload the affected limb.
The use of broad-spectrum antibacterial drugs is associated with a risk of developing pseudomembranous colitis. This diagnosis should be borne in mind in patients who have severe diarrhea on the background of treatment with gatifloxacin. In this case, appropriate therapy should be given immediately.
In some cases, after the first use of the drug may develop hypersensitivity and allergic reactions. Very rarely, allergic reactions can progress to a life-threatening anaphylactic shock even after the first use of the drug. In these cases, gatifloxacin should be discontinued and necessary measures (including anti-shock) should be carried out.
Patients taking the drug should avoid direct sunlight and ultraviolet radiation.
OVERDOSE
Symptoms: nausea, vomiting, diarrhea; in more severe cases - tachypnea, tremor, convulsions, agitation.
Treatment: gastric lavage (in the first two hours after poisoning), observation, symptomatic therapy with ECG monitoring. There is no specific antidote. It is necessary to ensure a sufficient supply of fluid in the body while maintaining the appropriate diuresis. With hemodialysis and peritoneal dialysis is withdrawn slightly.
DRUG INTERACTION
With the simultaneous use of gatifloxacin and:
- antiarrhythmic drugs (including quinidine, procainamide, amiodarone, sotalol), tricyclic antidepressants (including amitriptyline, imipramine, nortriptyline, doxepin, amoxapine), phenothiazine derivatives (including chlorpromazine, fluphenazine, perphenazine, mesoridazine, thioridazine), erythromycin, cisapride, the risk of heart rhythm disorders increases;
- glibenclamide or insulin, the risk of hypo- or hyperglycemia is increased;
- warfarin, changes in the pharmacokinetics of both drugs are not observed, prothrombin time does not change. However, due to the fact that some quinolones increase the effect of warfarin and similar agents, control of prothrombin time is required;
- digoxin, no significant changes in the pharmacokinetics of gatifloxacin, but in some patients there was an increase in the level of digoxin concentration in the blood.It is required to control the concentration of digoxin in the blood serum and, if necessary, dose adjustment of digoxin;
- probenicida, systemic exposure of gatifloxacin may be increased;
- Cimetidine, taken 1 hour prior to gatifloxacin, there was no change in the pharmacokinetics of the latter.
Preparations containing ions of zinc, magnesium, iron and aluminum, didanosine reduce the effectiveness of gatifloxacin (should be taken at intervals of 4 hours).
With the simultaneous use of quinolones and theophylline, it is possible to increase the concentration of theophylline in the blood plasma and increase the risk of developing toxic effects associated with theophylline.
With the simultaneous administration of quinolones and cyclosporine, the nephrotoxic effect of cyclosporin can be enhanced.
With simultaneous use of quinolones and non-steroidal anti-inflammatory drugs, the risk of side effects from the central nervous system, including convulsions, may increase.
When a combination of quinolones with other antimicrobial agents (beta-lactam antibiotics aminoglycosides, clindamycin, metronidazole), synergy is usually observed.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children.
Shelf life - 3 years.
Do not use after the expiry date printed on the package.
