Grepafloxacin - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

АТХ:

J.01.M.A.11 Grepafloxacin

Pharmacodynamics:

Has a pronounced bactericidal activity against a wide range of gram-negative, gram-positive and atypical bacteria.Sensitive Gram-positive aerobes: Staphylococcus aureus - strains sensitive to methicillin, Staphylococcus epidermidis - strains sensitive to methicillin, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes. Gram-negative aerobes: Acinetobacter calcoaceticus, Citrobacter diversus, Citrobacter freundii, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains that produce beta-lactamase), Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis (including strains , producing beta-lactamases), Morganella morganii, Neisseria gonorrhoeae (including strains resistant to tetracyclines and penicillins), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri. Moderately sensitive gram-negative aerobes: Burkholderia cepacia, Pseudomonas aeruginosa, Serratia marcescens, Stenotrophomonas maltophilia. Resistant Gram-positive aerobes: Staphylococcus aureus (strains resistant to methicillin). Other microorganisms: sensitive - Chlamydia pneumoniae, Chlamydia trachomatis, Legionella pneumophila, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis; moderately sensitive - Ureaplasma urealyticum.

Pharmacokinetics:

After ingestion, quickly and completely absorbed from the digestive tract, regardless of the presence of food and acidity of gastric juice. Bioavailability is about 72%, Cmax - after 2 hours, binding to plasma proteins - about 50%, does not change with age and in violation of liver and kidney function. The volume of distribution after a single intake of 400 mg - 5 l / kg. Penetrates into bile, bile excretory system, alveolar fluid, alveolar macrophages, bronchial mucus, genital tissues, skin, tonsils.The concentration in the tissues depends on that in the blood. Plasma and urine show unchanged grapafloxacin and five of its metabolites, another additional metabolite is present in the feces. Excreted in various ways (with bile, through the kidneys - 5-14%, with feces - 27% of the dose). Oxidation products have a weak antimicrobial activity and do not cause significant toxic effects. After repeated administration (400 or 600 mg once a day), T1 / 2 is about 12 hours. Age and renal dysfunction do not significantly affect the pharmacokinetics of Raxar. However, with hepatic disorders, its concentration in plasma and the area under the plasma concentration-time curve increase by 56-137%, depending on the severity of the disorders.

Indications:

Community-acquired pneumonia (including pneumococcal, non-pneumococcal and atypical), acute bacterial complications of chronic bronchitis; uncomplicated gonorrhea; urethritis and cervicitis caused by Chlamydia trachomatis.

ICD-10

I.A50-A64.A54 Gonococcal infection

X.J10-J18.J18 Pneumonia without clarification of the pathogen

X.J40-J47.J42 Chronic bronchitis, unspecified

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N70-N77.N72 Inflammatory disease of the cervix

XIV.N70-N77.N74.3 * Gonococcal inflammatory diseases of female pelvic organs (A54.2 +)

Contraindications:

Hypersensitivity (including to other fluoroquinolones), moderate and severe violations of liver function, prolongation of the QT interval on the ECG.

Carefully:

May cause seizures, which should be considered when prescribing the drug to patients with impaired CNS, predisposing to the occurrence of convulsive seizures, as well as psychosis. When the first signs of tendovaginitis or the slightest pain in the tendons appear, the treatment is stopped. It is not recommended to take children, patients with heart rhythm disturbances, or in conditions predisposing to the development of arrhythmias (hypokalemia, myocardial ischemia, congestive heart failure, etc.). With caution appoint with a deficiency of glucose-6-phosphate dehydrogenase (in t.ch. at close relatives). It is impossible to combine without cardiomonitoring with drugs that cause lengthening of the interval QT and / or rhythm disturbance of the "pirouette" type.

Pregnancy and lactation:

Contraindications to use during pregnancy and lactation.

Dosing and Administration:

Inside, at a dose of 400-600 mg once a day, depending on the nature of the infection. Duration of treatment - up to 7-10 days. To treat uncomplicated gonorrhea prescribed 400 mg once.With a mild violation of liver function, the maximum daily dose is 400 mg.

Side effects:

Headache, dizziness, insomnia, anxiety, fatigue, asthenia, depression, hallucinations, confusion, convulsions, impaired vision, hearing, smelling, nausea, bad taste and dry mouth, decreased appetite, abdominal pain, constipation, diarrhea, dyspepsia, vomiting, photosensitivity, itching, skin rash, tendovaginitis, vaginitis, fever, arthralgia, myalgia, exfoliative dermatitis, thrombocytopenia, increased levels of uric acid, creatinine, hepatic enzymes and residual nitrogen in the blood, hyperlipidemia, hyperglycemia Ikem, allergic reactions of varying severity, including anaphylactic shock.

Overdose:

Possible arrhythmias and lengthening of the interval QT. It is necessary ECG-monitoring for at least 24 hours, maintain the water-electrolyte balance and conduct symptomatic therapy appropriate to the clinical condition of the patient.

Interaction:

Enhances the effect (reduces Cl and extends T_1/2) theophylline and caffeine. Antacids, sucralfate and iron-containing drugs reduce absorption (a 4-hour interval between admission is necessary).

Special instructions:

Do not drive or work with moving gear in the event of dizziness. During treatment, exposure to sunlight should be avoided and UV radiation.

Instructions

Grepafloxacin (Grepafloxacinum)