Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antimicrobial agent of the group of fluoroquinolones. The bactericidal effect of gatifloxacin, as well as of other fluorinated quinolones, is due to its ability to block the bacterial DNA-gyrase enzyme. DNA gyrase is an important enzyme involved in the replication, transcription and repair of bacterial DNA. Gatifloxacin also suppresses topoisomerase IV, which plays a key role in the separation of chromosomal DNA during the division of the bacterial cell. Antibacterial spectrum covers resistant to penicillins, aminoglycosides, cephalosporins, as well as multiresistant microorganisms.
It is active against gram-positive microorganisms: Staphylococcus aureus, Streptococcus pneumoniae (including penicillin-sensitive and penicillin-resistant strains), Streptococcus pyogenes, Streptococcus saprophyticus, Staphylococcus epidermidis (methicillin-sensitive strains), Streptococcus spp. (groups C, G, F), Streptococcus agalactiae; Gram-negative microorganisms: Escherichia coli, Haemophillus influenzae (including strains producing ОІ-lactamases), Haemophillus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including strains producing ОІ-lactamases), Neisseria gonorrhoeae (including ОІ-lactamase producing strains), Proteus mirabilis , Acinetobacter iwoffii, Citrobacter koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Klebsiella oxytoca, Moragnella morganii, Proteus vulgaris; other microorganisms: Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae.
Highly active against anaerobes , in particular Peptostreptococcus spp.
PHARMACOKINETICS
The pharmacokinetics of gatifloxacin is linear and does not depend on time when applied at doses of 200 to 800 mg for up to 14 days.
After oral administration, gatifloxacin is well absorbed from the digestive tract. Absolute bioavailability of gatifloxacin is 96%. C max gatifloxacin in blood plasma is usually achieved 1-2 hours after ingestion.
The binding of gatifloxacin to plasma proteins is about 20% and does not depend on the concentration. Gatifloxacin is widely distributed in many tissues and body fluids (including bronchial mucous membranes, alveolar macrophages, vagina and cervix). The rapid distribution of gatifloxacin in tissue leads to its higher concentrations in most target organs than in serum.
Gatifloxacin undergoes limited biotransformation in the body. Less than 1% of the administered dose is excreted in the urine in the form of ethylenediamine and methylethylenediamine metabolites. In unchanged form is excreted mainly by the kidneys (more than 70% within 48 hours after ingestion); 5% is excreted with feces.
After installation in the eye of gatifloxacin in the appropriate dosage form, the concentration of gatifloxacin in the blood plasma remains below the analytical determination threshold (5 ng / ml).
INDICATIONS
Infectious-inflammatory diseases caused by sensitive microorganisms: pneumonia, chronic bronchitis in the exacerbation phase, pyelonephritis, complicated and uncomplicated urinary tract infections, ENT infections, including acute sinusitis, skin and soft tissue infections, sexually transmitted diseases (urethritis, cervicitis , proctitis).
In ophthalmology: treatment of bacterial conjunctivitis caused by drug-susceptible pathogens.
DOSING MODE
Take inside at a dose of 200-400 mg 1 time / day. The duration of treatment depends on the indications and severity of the infection.
The initial dose of the drug for renal failure does not differ from the dose for patients with normal renal function, the further dosage regimen is established depending on the QC.
In ophthalmology apply for 7 days according to a special scheme.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, abdominal pain, anorexia, diarrhea, constipation, dyspepsia, flatulence, gastritis, glossitis, stomatitis, gingivitis, gastrointestinal bleeding; with a local application in ophthalmology, there was a change in taste sensations.
From the NCS and the peripheral nervous system: headache, dizziness, migraines, insomnia and other sleep disorders, agitation, anxiety, nervousness, confusion, drowsiness, paresthesia, tremor, convulsions, lower limb muscle cramps, depersonalization, depression, panic attack, paranoia, hostility, photophobia, ataxia, hyperesthesia, visual impairment, photosensitivity of the eyes, distortion of taste sensations, parosmia, peripheral neuropathy.
From the cardiovascular system: tachycardia, bradycardia, arterial hypertension.
From the musculoskeletal system: increased risk of rupture of tendons, ossalgia, arthritis.
On the part of the respiratory system: hyperventilation, bronchospasm.
Allergic reactions: face edema, edema of the oral cavity and tongue, generalized edema, maculopapular rash, vesicle-bulbous rash.
Other: chest pain, pain in the ears, thirst, dry skin, fever, vaginitis, hypoglycemia, hematuria, metrorrhagia.
Local reactions: irritation of the conjunctiva, increased lacrimation, keratitis, papillary conjunctivitis, chemosis. hemorrhage in the conjunctiva, dry eye mucosa (dry eye syndrome), discharge from the eyes, eye irritation, eye pain, eyelid edema, redness of the eyes, decreased visual acuity.
CONTRAINDICATIONS
Children and adolescence under 18, pregnancy, lactation (breastfeeding), hypersensitivity to gatifloxacin or other fluoroquinolones.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
The initial dose of the drug for renal failure does not differ from the dose for patients with normal renal function, the further dosage regimen is established depending on the QC.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
SPECIAL INSTRUCTIONS
Gatifloxacin can cause an increase in the duration of QT intervals on the ECG in some patients. Due to the lack of clinical experience, gatifloxacin should not be used in patients with prolonged QT interval, hypercalcemia and concomitant administration of antiarrhythmic drugs of class IA (quinidine, procainamide) or class III (amiodarone, sotalol).
Gatifloxacin should be used with caution in patients with bradycardia and acute myocardial ischemia.
Like other fluoroquinolones, gatifloxacin should be used with caution in patients with severe atherosclerosis of the cerebral vessels, epilepsy and diseases that can cause seizures.
Long-term (more than 28 days) use of gatiflokasacin, as well as other antibacterial drugs, can lead to growth of insensitive microorganisms, as well as fungi. With the development of superinfection, gatifloxacin should be discontinued and an alternative therapy should be prescribed.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, the speed of psychomotor reactions may decrease, so patients should refrain from driving and working with dangerous mechanisms.
DRUG INTERACTION
During the treatment period, changes in blood glucose levels (symptomatic hyper- and hypoglycemia) in patients with diabetes mellitus taking oral hypoglycemic drugs are possible (regular blood glucose monitoring is recommended).
Gatifloxacin should be taken 4 hours before the intake of ferrous sulfate, food additives containing zinc, magnesium or iron, antacids containing magnesium and aluminum compounds.
Excretion of gatifloxacin increases with simultaneous application with probenecid.
With the simultaneous use of gatifloxacin with warfarin, no significant changes in clotting time have been detected. But given the ability of some quinolones to enhance the effect of warfarin or other indirect anticoagulants, when they are used simultaneously, prothrombin time or other blood coagulation should be monitored.
The simultaneous use of NSAIDs with fluoroquinolones may increase the risk of side effects from the CNS.
With caution apply simultaneously with cisapride, erythromycin, antipsychotic drugs.
