Pefloxacin-AKOS - instructions for use, dose, side effects, contraindications

Shell: hypromellose (hydroxypropylmethylcellulose), titanium dioxide (titanium dioxide), propylene glycol, macrogol (polyethylene oxide 4000, polyethylene glycol 4000), talc.

Description:The tablets covered with a film membrane, of the round form, biconcave white or white with a yellowish shade of color.

Pharmacotherapeutic group:antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A.03 Pefloxacin

Pharmacodynamics:

Antimicrobial agent from the group of fluoroquinolones. Has a bactericidal effect, blocks DNA-gyrase. With respect to Gram-negative strains effectively acts as dividing cells, and cells in the resting stage; in the case of gram-positive strains - only on cells that are in the process of mitotic division. Has a wide range of action.

Active for most aerobic Gram-negative bacteria: Escherichia coli, Klebsiella spp., indole-positive and indolar Proteus spp., in t.ch. 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 .; aerobic gram-positive bacteria: Staphylococcus spp., (incl. producing and not producing penicillinase and methicillin-resistant), Streptococcus spp., in t.ch. Streptococcus pyogenes, Streptococcus agalactiac, Corynebacterium diphtheriae, Listeria monocytogenes; intracellular bacteria: Legionella spp. (incl. Legionella pneumophila), Brucella spp., Chlamydia spp., as well as against bacteria that produce beta-lactamase. Suppresses vital functions Mycoplasma spp. and Helicobacter spp.

Moderately sensitive microorganisms:

Streptococcus pneumoniae, Acinetobacter spp., Clostridium perfringens, Pseudomonas spp., Chlamydia trachomatis. Stable microorganisms: gram-negative anaerobes. Treponema spp., Mycobacterium tuberculosis. In diseases caused by moderately sensitive microorganisms, sensitivity is required in vitro. Oppresses microsomal oxidation in liver cells.

Pharmacokinetics:

Absorption is high, after 20 minutes after ingestion of a single dose (400 mg), 90% is absorbed. The time to reach the maximum concentration (4 μg / ml) is 90 to 120 minutes, the therapeutic concentration is held for 12-15 hours. After repeated administration, the maximum concentration (Stach) in the blood is 10 μg / ml; concentration in the bronchial mucosa - 5 mcg / ml; the ratio between the concentration in the mucosa of the bronchi and blood - 100%. The connection with plasma proteins is 25-30%.

Well penetrates into tissues and body fluids, including. in the bronchial secretion, the lungs, the prostate gland, cerebrospinal fluid and bone tissue. The volume of distribution is 1.5-1.8 l / kg. Concentration in the cerebrospinal fluid after a 3-fold intake of 400 mg is 4.5 μg / ml, with an increase in the dose to 800 mg - 9.8 μg / ml; concentration in the cerebrospinal fluid is 89% of that in

plasma. Concentration in other organs and tissues 12 hours after the last dose: thyroid gland - 11.4 μg / g, salivary glands - 2.2 μg / g, skin -

7.6 mkg / g, nasopharyngeal mucosa - 6 mcg / g, amygdala - 9 mcg / g, muscle -

5.6 μg / g.

Metabolised in the liver by methylation to dimethylphexlocacin (has significant antibacterial activity), oxidized to Noxide and conjugated with glucuronic acid to form pefloxacin-glucuronide.

The half-life period is 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 concentration of unchanged drug in the urine 1-2 hours after the administration is 25 μg / ml. after 12-24 hours, 15 μg / ml. Unchanged pefloxacin and its metabolites are detected in the urine within 84 hours after the final administration. Poor dialysis (extraction ratio 23%).

Indications:

Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- infections of the kidneys and urinary tract;

- infections of the pelvic organs (including adnexitis and prostatitis);

- infections of the gastrointestinal tract (including salmonellosis, typhoid fever);

- infection of the gallbladder and biliary tract (cholecystitis, cholangitis, empyema of the gallbladder);

- infection of the abdominal cavity (intra-abdominal abscesses);

- infection of bones, joints;

- skin and soft tissues (including those caused by staphylococcus, resistant to penicillin);

- infections of the lower respiratory tract;

- infection of the ENT organs (incl.chronic sinusitis, severe external otitis);

- gonorrhea;

- chlamydia, soft chancre.

Contraindications:

Hypersensitivity, deficit glucose-6-phosphate dehydrogenase (hemolytic anemia), pregnancy, lactation, age under 18 years.

Carefully:

Atherosclerosis of cerebral vessels, cerebral circulation disorder, organic lesions of the central nervous system, epileptic syndrome of unidentified etiology, renal and / or hepatic insufficiency.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Inside, on an empty stomach, doses are selected individually depending on the localization and severity of the infection, as well as the sensitivity of microorganisms. Assign the drug 1 tablet (400 mg) 2 times a day (every 12 hours), the average daily dose - 800 mg in 2 divided doses. The maximum daily dose is 1200 mg.

Tablets are swallowed without chewing and drinking with a lot of water.

In the treatment of certain infections of the genitourinary system, the drug is prescribed 1 (400 mg) tablet per day.

For the treatment of gonorrhea in men and women appoint the drug once in a dose of 800 mg.

A correction is required in patients with impaired liver functiondosing regimen: with minor violations, the drug is prescribed at a dose of 400 mg / day; with more pronounced violations - every 36 hours; with severe liver pathology, the interval between administrations is extended to 2 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 a day, or a full single dose administered once a day. For elderly people, the dose of the drug is reduced by about 1/3.

Side effects:

From the side of the nervous system, depression, headache, dizziness, fatigue, insomnia, increased convulsive alertness, anxiety, agitation, tremor, rarely - convulsions.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, decreased appetite, flatulence, pseudomembranous colitis, transient increase in "hepatic" transaminases, cholestatic jaundice, hepatitis, and necrosis of the liver.

From the urinary system. crystalluria, rarely glomerulonephritis, dysuria.

Allergic reactions: skin rash, itchy skin, urticaria, skin hyperemia, photosensitivity, rarely - angioedema, bronchospasm, arthralgia.

From the hematopoietic system, leukopenia, neutropenia, thrombocytopenia, agranulocytosis, eosinophilia.

Other: tachycardia, myalgia, tendonitis, candidiasis.

Overdose:

Symptoms: nausea, vomiting, confusion, mental agitation; in severe cases - loss of consciousness, convulsions.

Treatment: gastric lavage, Activated carbon. It is necessary to ensure the medical control of the patient's condition, sufficient supply of liquid to the patient's body; if necessary, conduct symptomatic therapy. Hemodialysis is not an effective method of removing quinolone derivatives from the body.

Interaction:

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, continuous monitoring of the blood picture is necessary). Cimetidine and other inhibitors of microsomal oxidation increase the half-life, reduce overall clearance, but do not affect the volume of distribution and renal clearance.

Enveloping drugs 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 caused by Pseudomonas aeruginosa).

Drugs that block tubular secretion, slow the excretion of pefloxacin.

Special instructions:

With mixed infections, with infections of the pelvic organs combined with drugs that are active against anaerobes (metronidazole, clindamycin).

During the treatment period, patients should receive a large amount of fluid while observing adequate diuresis (to prevent crystalluria).

Due to the possible appearance of photosensitivity during the treatment period, it is not possible to 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 pelefloxacin occurs during or after treatment with severe and prolonged diarrhea, it is necessary to exclude the development of pseudomembranous colitis (immediate withdrawal of the drug andpurpose of appropriate treatment).

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets 200 mg, 400 mg.

For 10 tablets in a planar cell package.

1, 2 contour mesh packages together with instructions for use in the pack from cardboard.

Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings, cellular, outline (2) - packs, cardboard

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002431 / 01

Date of registration:11.09.2008

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Pefloxacin-AKOS (Pefloxacin-AKOS)