Composition, form of production and packaging
Tablets coated with a film coat of white or yellowish white color, capsular-shaped, with a risk on one side.
1 tab.
pefloxacin mesylate dihydrate 558.56 mg,
which corresponds to the content of pefloxacin 400 mg
Auxiliary substances: corn starch, microcrystalline cellulose, sodium carboxymethyl starch (type A), colloidal silicon dioxide, magnesium stearate, Opadry II white dye 85F28751 (polyvinyl, partially hydrolysed, alcohol, titanium dioxide, macrogol 4000 / PEG 3000, talc).
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Antimicrobial agent from the group of fluoroquinolones. It has a bactericidal effect, blocks DNA gyrase, replicates the A-subunit of DNA, RNA and disrupts the synthesis of bacterial proteins.
With respect to Gram-negative strains, it effectively acts on both dividing cells and cells at rest; in the case of gram-positive strains - only on cells that are in the process of mitotic division. Has a wide range of action.
It is active against most aerobic Gram-negative bacteria: Escherichia coli, Klebsiella spp., Indole-positive and indole-negative Proteus spp. (including Proteus mirabilis), Enterobacter spp., Morganella morganii, Yersinia enterocolitica, Vibrio cholerae, Vibrio parahaemolyticus, Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Pseudomonas aeruginosa, Moraxella catarrhalis, Pasteurella multocida, Campylobacter spp., Serratia spp ., Citrobacter spp., Salmonella spp., Shigella spp., Haemophilus spp .; aerobic Gram-positive bacteria: Staphylococcus spp., (including producing and non-producing penicillinase and methicillin-resistant strains), Streptococcus spp. (including Streptococcus pyogenes, Streptococcus agalactiae), Corynebacterium diphtheriae, Listeria monocytogenes;intracellular bacteria: Legionella spp. (including Legionella pneumophila), Brucella spp., Chlamydia spp., as well as against bacteria that produce beta-lactamase.
Suppresses the life of Mycoplasma spp. and Helicobacter spp.
PHARMACOKINETICS
Absorption is high, after 20 minutes after ingestion of a single dose (400 mg), 90% is absorbed.
The time to reach C max (4 Ојg / ml) is 90-120 minutes, the therapeutic concentration is held for 12-15 hours. After repeated administration of Cmax in the blood, 10 Ојg / ml; concentration in bronchial mucosa - 5 mcg / ml; the ratio between the concentration in the mucosa and the blood is 100%. Connection with plasma proteins - 25 - 30%.
Well penetrates into tissues and body fluids, including. in the bronchial secretion, the lungs, the prostate gland, spinal fluid and bone tissue. V d - 1.5-1.8 l / kg.Concentration in the cerebrospinal fluid after a triple intake of 400 mg - 4.5 Ојg / ml, with an increase in the dose of up to 800 mg - 9.8 Ојg / ml; the ratio between the concentration in the plasma and the liquid is 89%. Concentration in other organs and tissues 12 hours after the last administration: thyroid gland 11.4 Ојg / g, salivary glands -2.2 Ојg / g, skin 7.6 Ојg / g, nasopharyngeal 6 Ојg / g, amygdala 9 Ојg / g , muscle -5.6 Ојg / g.
Metabolized in the liver by methylation to dimethylphexlocacin (has significant antibacterial activity), oxidized to N-oxide and conjugated with glucuronic acid to form pefloxacin-glucuronide.
T 1/2 - 8-10 hours, with repeated administration - 12-13 hours. It is excreted by the kidneys 60%, with bile - 30% unchanged; partially in the form of metabolites. The content of unchanged drug in the urine 1-2 hours after admission - 25 mcg / ml, after 12-24 h -15 mcg / ml. Unchanged pefloxacin and its metabolites are detected in urine within 84 hours after the last administration. Poor dialysis (extraction ratio - 23%).
INDICATIONS
Treatment of infections caused by microorganisms that are sensitive to the drug:
- infections of the kidneys and urinary tract;
- Gastrointestinal infections (including salmonellosis, typhoid fever);
- infections of the gallbladder and biliary tract (cholecystitis, cholangitis, empyema of the gallbladder);
- infections of the pelvic organs (including adnexitis and prostatitis);
- infection of bones, joints;
- skin and soft tissue infections;
- infections of the lower respiratory tract and ENT organs (middle ear and paranasal sinuses, pharynx and larynx);
- eye infections;
- intra-abdominal abscesses;
- peritonitis;
- sepsis;
- septicemia;
- endocarditis;
- meningoencephalitis;
- osteomyelitis;
- Gonorrhea;
- Chlamydia;
- epididymitis;
- soft chancre;
- surgical and neuropathic infections;
- prevention of surgical infection.
DOSING MODE
Inside, on an empty stomach, the doses are selected individually, depending on the localization and severity of the infection, as well as the sensitivity of microorganisms.
In uncomplicated infections - 0.4 g 2 times / day, the average daily dose - 0.8 g in 2 divided doses. Tablets are swallowed without chewing and drinking with a lot of water.
In patients with impaired liver function , correction of the dosing regimen is required: with minor violations, the drug is prescribed at a dose of 0.4 g / day; withmore severe violations - every 36 hours; with severe liver pathology, the interval between administrations is extended to 2 days. The course of treatment - no more than 30 days.
Patients with impaired renal function (with creatinine clearance below 20 ml / min) single dose should be 50% of the average dose - with a multiplicity of appointment 2 times / day, or a full single dose administered 1 time / day.
For elderly people, the dose of the drug is reduced by about 1/3.
SIDE EFFECT
From the nervous system: depression, headache, dizziness, fatigue, insomnia, increased convulsive alertness, anxiety, agitation, tremor; rarely convulsions.
On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia, flatulence, pseudomembranous colitis, transient increase in hepatic transaminases, cholestatic jaundice, hepatitis, liver necrosis.
From the urinary system: crystalluria; rarely glomerulonephritis, dysuria.
Allergic reactions: skin rash, skin itching, urticaria, skin hyperemia, photosensitivity; rarely - Quincke's edema, bronchospasm, arthralgia.
From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia (at doses of 1600 mg / day), agranulocytosis, eosinophilia.
Other: tachycardia, myalgia, tendonitis, tendon rupture, candidiasis.
CONTRAINDICATIONS
- epilepsy;
- hemolytic anemia;
- deficiency of glucose-6-phosphate dehydrogenase;
- Children's age (up to 18 years);
- Pregnancy;
- lactation period;
- Hypersensitivity.
With caution - atherosclerosis of cerebral vessels, cerebral circulation, organic lesions of the central nervous system, convulsive syndrome of unknown etiology, renal and / or hepatic insufficiency.
PREGNANCY AND LACTATION
Contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function (with creatinine clearance below 20 ml / min) single dose should be 50% of the average dose - with a multiplicity of appointment 2 times / day, or a full single dose administered 1 time / day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In patients with impaired liver function , correction of the dosing regimen is required: with minor violations, the drug is prescribed at a dose of 0.4 g / day; withmore severe violations - every 36 hours; with severe liver pathology, the interval between administrations is extended to 2 days. The course of treatment - no more than 30 days.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
APPLICATION IN ELDERLY PATIENTS
For elderly people, the dose of the drug is reduced by about 1/3.
SPECIAL INSTRUCTIONS
With mixed infections, perforated processes in the abdominal cavity, with infections of the pelvic organs - combined with drugs that are active against anaerobes (metronidazole, clindamycin).
During treatment, patients should receive a large amount of fluid (to prevent crystalluria).
Due to the possible appearance of photosensitization, during the treatment period one can not be exposed to UV radiation.
For patients with severe liver and kidney disease, dose adjustment is required, in proportion to the degree of damage.
If serious and persistent diarrhea occurs during or after treatment with pefloxacin, the development of pseudomembranous colitis should be ruled out (immediate withdrawal of the drug and the appropriate treatment).
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
OVERDOSE
Treatment: a specific antidote is unknown. Symptomatic therapy, if necessary - hemodialysis and peritoneal dialysis.
DRUG INTERACTION
Cimetidine and other microsomal oxidation inhibitors increase T 1/2 , reduce overall clearance, but do not affect V d and renal clearance.
Pefloxacin reduces the metabolism of theophylline in the liver, which leads to an increase in the concentration of theophylline in the plasma and the central nervous system (in order to avoid the development of intoxication, the dose of theophylline should be reduced).
Significantly reduces the prothrombin index (in patients taking indirect anticoagulants - a continuous monitoring of the blood picture is necessary).
Covering agents slow absorption.
The simultaneous use of beta-lactam antibiotics can prevent the development of resistance during the treatment of staphylococcal infection.
Aminoglycosides, piperacillin, azlocillin, ceftazidime increase the antibacterial effect (including infection with Pseudomonas aeruginosa).
Drugs that block tubular secretion, slow the excretion of pefloxacin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dark place at a temperature of no higher than 30 В° C. Keep out of the reach of children. Shelf life - 3 years. Do not use after the expiration date printed on the package.
