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

Excipients: ascorbic acid, benzyl alcohol, sodium disulfite (sodium metabisulphite), disodium edetate (ethylenediaminetetraacetic acid disodium salt [Trilon B]), sodium hydrogen carbonate (sodium bicarbonate), water for injection - up to 5 ml.

Description:Transparent solution is yellowish or greenish-yellowish in color.

Pharmacotherapeutic group:antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A.03 Pefloxacin

Pharmacodynamics:

Antimicrobial agent from the group of fluoroquinolones.It has a bactericidal effect, inhibiting the replication of bacterial DNA by blocking the DNA-gyrase enzyme. 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. It has a wide spectrum of antimicrobial action.
Active with respect to: majority aerobic gram-negative bacteria (including those that produce beta-lactam azes): 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. (incl. Streptococcus pyogenes, Streptococcus agalactiae, Besides Streptococcus pneumoniae), Corynebacterium diphtheriae, Listeria monocytogenes; intracellular bacteria: Legionella spp. (incl. Legionella pneumophila), Brucella spp., Chlamydia spp. Suppresses vital functions Mycoplasma spp. and Helicobacter spp.
Moderately sensitive to pefloxacin microorganisms: Streptococcus pneumoniae, Acinetobacter spp., Clostridium perfringens, Pseudomonas spp., Chlamydia trachomatis.
Stable to pefloxacin: gram-negative anaerobes, Treponema spp., Mycobacterium tuberculosis.

Pharmacokinetics:

After intravenous administration, the maximum serum concentration of the drug is reached within 60 minutes. The therapeutic concentration is held for 12-15 hours. The half-life (T1 / 2) period is from 7.2 to 13 hours after a single dose administered. After repeated administration, the elimination half-life is 14-15 hours.

Pefloxacin penetrates well into the tissues of the body (bronchial mucosa, bones, heart, spinal fluid, sputum, urine, secretion of the prostate gland, bile, peritoneal fluid). Metabolised in the liver.

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 admission 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:

Infectious-inflammatory diseases caused by microorganisms sensitive to pefloxacin:

- infections of the kidneys and urinary tract;

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

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

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

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

- infection of bones, joints, skin and soft tissues;

- infections of the lower respiratory tract and ENT organs;

- sepsis;

- endocarditis;

- bacterial meningitis;

- gonorrhea;

- chlamydia, epididymitis, soft chancre;
- prevention of surgical infection.

Contraindications:

Hypersensitivity, deficiency of glucose-6-phosphate dehydrogenase (hemolytic anemia), pregnancy, lactation period, epilepsy, age to 18 years.

Carefully:

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

Pregnancy and lactation:contraindicated

Dosing and Administration:

Intravenously drip, infusion is carried out for 1 hour. The first dose is 400-800 mg; then - 400 mg every 12 hours. The course of treatment - 1-2 weeks (no more than 4 weeks). Preparation of a solution for infusion: the contents of one ampoule (400 mg = 5 ml of concentrate) are dissolved in 250 ml of a 5% solution of dextrose.As a solvent, you can not use a solution of sodium chloride or any solvent containing chlorine ions!

For prevention of infectious complications in surgery recommend IV administration of the drug at a dose of 400-800 mg per hour before the operation.

For patients with liver disease, a single dose for intravenous drip administration is 8 mg / kg body weight; duration of infusion - 1 hour; frequency of infusion in patients with jaundice - 1 time per 24 hours; in patients with ascites - 1 time per 36 hours; in patients with jaundice and ascites - 1 time in 48 hours.

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.

Due to the equivalence of doses for oral and / or intravenous administration, the drug can be used for sequential therapy (the course started in / in the administrations continues to be ingested).

Side effects:

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

From the side of 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, skin itch, hives, skin hyperemia, rarely - angioedema, bronchospasm, arthralgia.

From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia (at doses of 1600 mg / day), agranulocytosis, eosinophilia.

Local reactions: phlebitis.

Other: tachycardia, myalgia, tendonitis, candidiasis, photosensitivity.

Overdose:

Treatment: a specific antidote is unknown. Symptomatic therapy, if necessary - hemodialysis and peritoneal dialysis.

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).Pharmaceutically incompatible with heparin. Do not dilute with sodium chloride solution or any solvent containing chlorine ions.

Cimetidine and other inhibitors of microsomal oxidation increase T1 / 2, reduce overall clearance, but do not affect the volume of distribution and renal clearance.

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.

Special instructions:

It is used as a monotherapy or in combination with other antimicrobial drugs.

With mixed infections, perforated processes in the abdominal cavity, with infections of the pelvic organs are combined with drugs active against anaerobes (metronidazole, clindamycin).

During treatment, patients should receive a large amount of fluid with 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, the development of pseudomembranous colitis should be ruled out (immediate withdrawal of the drug and the 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:

Concentrate for the preparation of a solution for infusions 400 mg / 5 ml.

To 5 ml in ampoules of colorless or light-protective neutral glass.

10 ampoules are placed in a box of cardboard.

For 5 or 10 ampoules are placed in a contour mesh package.

1 circuit cell package with 10 ampoules or 1, 2 contoured cells with 5 ampoules are placed in a pack of cardboard.

In each pack, the box is attached instructions for use, the ampullar scarifier.

Ampoule scapper does not invest when using ampoules with a kink ring or with an incision and a point.

Packaging:(1) - ampoule (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - cardboard boxes
(1) - ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging contour plastic (pallets)
(1) - ampoules (5) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging contour plastic (pallets)
(1) - ampoules of dark glass (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - cardboard boxes
(1) - ampoules of dark glass (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging contour plastic (pallets)
(1) - ampoules of dark glass (5) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging contour plastic (pallets)

Storage conditions:

List B. In the dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002431 / 02

Date of registration:30.10.2008

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)