Universal reference book for medicines
Name of the preparation: PEFLOXACIN-AKOS (PEFLOXACIN-AKOS)

Active substance: pefloxacin

Type: Antibacterial drug of the group of fluoroquinolones

Manufacturer: SYNTHESIS (Russia)
Composition, form of production and packaging
The tablets covered with a cover
white or white with a yellowish shade of color, round, biconcave.

1 tab.

pefloxacin mesylate 200 mg

Auxiliary substances: corn starch or potato, polyvinylpyrrolidone, lactose, calcium stearate, microcrystalline cellulose, talc.

Sheath composition: hydroxypropylcellulose, polyethylene oxide 4000, titanium dioxide, 1,2-propylene glycol, talc or Opadry.

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (2) - packs cardboard.
The tablets covered with a cover white or white with a yellowish shade of color, round, biconcave.

1 tab.

pefloxacin mesylate 400 mg

Auxiliary substances: corn starch or potato, polyvinylpyrrolidone, lactose, calcium stearate, microcrystalline cellulose, talc.

Sheath composition: hydroxypropylcellulose, polyethylene oxide 4000, titanium dioxide, 1,2-propylene glycol, talc or Opadry.

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (2) - packs cardboard.
The solution for infusions is transparent, yellowish or greenish-yellowish in color.

1 ml of 1 amp.

pefloxacin (in the form of mesylate) 80 mg 400 mg

Excipients: ascorbic acid, benzyl alcohol, sodium pyrosulfite, disodium ethylenediaminetetraacetic acid, sodium carbonate, water d / u.

5 ml - ampoules (5) - packs of cardboard.

5 ml - ampoules (10) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2005.

PHARMACHOLOGIC EFFECT

Antimicrobial preparation of a broad spectrum of action from the group of fluoroquinolones.
Has a bactericidal effect, blocking the DNA-gyrase, disrupts the replication of the A-subunit of DNA and RNA and the synthesis of bacterial proteins.
With respect to gram-negative bacteria, it acts on cells that are in the stage of rest and division, against gram-positive bacteria-only on cells that are in the process of mitotic division.
Resistant to the action of? -lactamases. Has a wide range of action.
The drug is active against aerobic Gram-negative bacteria: Escherichia coli, Klebsiella spp., Indole-positive and indole-negative Proteus spp.
(including Proteus mirabilis), Enterobacter spp., Helicobacter pylori, 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., Neisseria gonorrhoeae; aerobic Gram-positive bacteria: Staphylococcus spp., (including those producing and not producing penicillinase and methicillin-resistant), Streptococcus spp. (including Streptococcus pyogenes, Streptococcus agalactiae), Corynebacterium diphtheriae, Listeria monocytogenes; intracellular bacteria: Legionella spp. (including Legionella pneumophila), Brucella spp., Chlamydia spp., Mycoplasma spp.
The drug is moderately sensitive: Pneumococcus spp.
(Streptococcus pneumoniae), Acinetobacter spp., Clostridium perfringens, Pseudomonas spp., Chlamydia trachomatis.
The drug is resistant to gram-negative anaerobic bacteria - Bacteroides spp.
(with the exception of B. fragilis), Treponema spp., Mycobacterium tuberculosis.
PHARMACOKINETICS

Suction

After ingestion pefloxacin is rapidly absorbed from the digestive tract.
After a single oral administration of 400 mg of pefloxacin after 20 minutes, a 90% dose is absorbed, with C max being achieved after 90-120 minutes and 4 Ојg / ml. After repeated administration of C max in blood plasma - 10 Ојg / ml, the concentration in the bronchial mucosa is 5 Ојg / ml; the ratio between the concentration in the mucosa and in the blood - 100%.
After intravenous administration, C max is reached within 60 minutes.

Distribution

The binding with plasma proteins is 25-30%.
V d - 1.5-1.8 l / kg. Pefloxacin penetrates well into tissues and body fluids (bronchial secretion, lungs, prostate gland, cerebrospinal fluid, peritoneal fluid, bone tissue, heart, sputum, urine, bile). The concentration in these liquids and tissues is higher than the concentration in the blood plasma.
Concentration in the cerebrospinal fluid after a three-time administration at a dose of 400 mg - 4.5 mcg / ml, with increasing doses up to 800 mg - 9.8 mcg / 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 dose: thyroid gland - 11.4 Ојg / g, salivary glands - 2.2 Ојg / g, skin - 7.6 Ојg / g, tonsils - 9 Ојg / g, muscles - 5.6 Ојg / g.
Metabolism

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

Excretion

T 1/2 after oral administration is approximately 8-10 hours, with repeated administration - 12-13 hours;
T 1/2 after iv injection of a single dose - 7.2-13 h, with repeated administration - 14-15 h. It is excreted in urine (60%) and with feces unchanged, in part - in the form of metabolites. The content of unaltered pefloxacin in the urine 1-2 hours after ingestion is 25 Ојg / ml, after 12-24 h -15 Ојg / ml. Unchanged pefloxacin and its metabolites are detected in urine within 84 hours after the last administration of the drug. The extraction ratio of pefloxacin in hemodialysis is 23%.
INDICATIONS

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

-infection of the kidneys and urinary tract;

- GI tract infections (including salmonellosis, typhoid fever);

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

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

-infection of the pelvic organs (including adnexitis, prostatitis);

-infection of bones and joints (including osteomyelitis);

-infection of skin and soft tissues;

-infection of the lower respiratory tract;

-infections of ENT organs (including middle ear, paranasal sinuses, pharynx and larynx);

-infection of the eyes;

-sepsis, septicemia;

-Bacterial endocarditis;

-engingoencephalitis;

-infection of skin and soft tissues;

-gonorrhea;

- Chlamydia;

-prostatitis;

-epididymitis;

-chancroid;

- surgical and nosocomial infections;

-prophylaxis of infectious complications after surgical interventions.

DOSING MODE

Established individually, depending on the localization and severity of the infection, as well as the sensitivity of microorganisms.

In uncomplicated infections, adults are given oral 400 mg twice a day, the average daily dose is 800 mg.
Tablets should be taken orally, on an empty stomach, without chewing, with plenty of water.
With infections of severe course, the drug is administered intravenously (in 250 ml of a 5% solution of glucose for 1 hour): the first dose is 800 mg, then 400 mg every 12 hours. The average course of treatment is no more than 1-2 weeks.

For patients with impaired liver function, dosage regimen correction is required.
With minor violations, the drug is prescribed 400 mg 2 times / day, with more severe violations - every 36 hours, with severe liver disease, the interval between administrations is extended to 2 days. The course of treatment - no more than 30 days.
Patients with impaired renal function (with QC less than 20 ml / min) single dose is 50% of the average dose with a multiplicity of appointment 2 times / day, or a full single dose is administered 1 time / day.

For elderly patients, the dose of the drug is reduced by 1/3.

SIDE EFFECT

From the side of the central nervous system: depression, headache, dizziness, insomnia, increased fatigue, increased convulsive activity, 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 transaminase activity, cholestatic jaundice, hepatitis, hepatic necrosis.

From the urinary system: crystalluria;
rarely glomerulonephritis, dysuria.
On the part of the hematopoiesis system: leukopenia, neutropenia, thrombocytopenia (at doses of 1.6 g / day), agranulocytosis, eosinophilia.

Allergic reactions: skin rash, skin itching, urticaria, skin hyperemia, photosensitivity;
rarely - Quincke's edema, bronchospasm, arthralgia.
Other: tachycardia, myalgia, tendonitis, tendon rupture, candidiasis.

Local reactions: phlebitis.

CONTRAINDICATIONS

-epilepsy;

hemolytic anemia;

- Insufficiency of glucose-6-phosphate dehydrogenase;

-pregnancy;

-lactation (breastfeeding);

-Children and adolescents under 18;

-increased sensitivity to fluoroquinolones.

With caution appoint a drug for atherosclerosis of cerebral vessels, cerebral circulation, organic lesions of the central nervous system, convulsive syndrome of unknown etiology.

PREGNANCY AND LACTATION

The drug is contraindicated for use in pregnancy and lactation (breastfeeding).

APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with impaired renal function (with QC less than 20 ml / min) single dose is 50% of the average dose with a multiplicity of appointment 2 times / day, or a full single dose is administered 1 time / day.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

For patients with impaired liver function, dosage regimen correction is required.
With minor violations, the drug is prescribed 400 mg 2 times / day, with more severe violations - every 36 hours, with severe liver disease, the interval between administrations is extended to 2 days. The course of treatment - no more than 30 days.
APPLICATION FOR CHILDREN

The drug is contraindicated in children and adolescents under 18 years.

SPECIAL INSTRUCTIONS

With mixed infections, perforating processes in the abdominal cavity, with infections of the pelvic organs, Pefloxacin-AKOS is combined with drugs active against anaerobes (metronidazole, clindamycin).

During treatment, patients should receive a large amount of liquid to prevent crystalluria.

Due to possible photosensitization during the treatment with Pefloxacin-ACOS, UV radiation should be avoided.

With severe liver and kidney disease, a dosage regimen is required.

If severe and persistent diarrhea occurs during or after Pefloxacin-AKOS treatment, pseudomembranous colitis should be excluded (with immediate withdrawal of the drug and administration of appropriate therapy).

Influence on the ability to drive vehicles and control mechanisms

When using the drug should refrain from engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

OVERDOSE

At present, cases of overdose of pefloxacin-ACOS have not been reported.

In case of an accidental overdose, symptomatic therapy is prescribed.
If necessary, hemodialysis and peritoneal dialysis are performed. There is no specific antidote.
DRUG INTERACTION

Simultaneous use of Pefloxacin-AKOS and beta-lactam antibiotics prevents the development of resistance in the treatment of staphylococcal infection

With the simultaneous use of Pefloxacin-AKOS with aminoglycosides, piperacillin, azlocillin, ceftazidime, synergism of antibacterial action is noted (including with Pseudomonas aeruginosa).

With the simultaneous use of Pefloxacin-ACOS and indirect anticoagulants, a decrease in the prothrombin index is noted (therefore, if this combination is necessary, a picture of the peripheral blood should be monitored).

Pharmacokinetic interaction

Absorption of pefloxacin is slowed down by simultaneous administration with antacids containing aluminum hydroxide and magnesium hydroxide.

Simultaneous administration of pefloxacin and cimetidine leads to a decrease in overall clearance and an increase in the half-life of pefloxacin, but does not change the volume of distribution and renal clearance.

Pefloxacin-ACOS slows the metabolism of theophylline in the liver, which leads to an increase in the concentration of theophylline in the plasma and in the CNS (therefore, if necessary, this combination should reduce the dose of theophylline).

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

Pharmaceutical interaction

Pefloxacin should not be mixed with solutions containing chlorine ions, to avoid precipitation.

Incompatible with heparin.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C.
Shelf life of the drug in the form of tablets - 3 years, in the form of a solution for infusions - 2 years.
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