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

Pefloxabol® is a synthetic antimicrobial agent from the group of monofluoroquinolones. It acts bactericidal, inhibiting the DNA-gyrase enzyme and the replication of bacterial DNA; also disrupts the replication of the A-subunit of ribonucleic acid and the synthesis of proteins by a bacterial cell.Causes the death of gram-negative bacteria both in the fission phase and in the resting phase. The bactericidal effect against Gram-positive bacteria extends only to cells that are at process mitotic division. Characteristic postantibiotic effect.

Pefloxabol ® has a broad spectrum of antimicrobial activity. It is active against gram-positive cocci: Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus (activity in relation to Streptococcus spp., including Streptococcus pneumoniae, Enterococcus spp., low and clinically insignificant); Gram-negative cocci and bacteria: Acinetobacter spp. (moderately sensitive), Aeromonas spp., Campylobacter spp., Citrobacter spp., Enterobacter spp., Escherichia coli, Gardnerella vaginalis (moderately sensitive), Haemophilus ducreyi , Haemophilus influenzae, Klebsiella spp., Moraxella catarrhalis, Morganella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa, Salmonella spp., Serratia spp., Shigella spp., Vibrio spp., Yersinia spp.; obligate intracellular parasites: Chlamydia spp., Chlamydophila pneumoniae, Legionella spp., Mycoplasma spp. (moderately sensitive).

He is destroyed by beta-lactamases, acts on many strains resistant to penicillins, cephalosporins and aminoglycosides.

Insensitive to Pefloxabol®: strains Staphylococcus spp., resistant to methicillin, Listeria spp., Gram-negative anaerobes (Bacteroides fragilis, Bacteroides spp., Prevotella spp., Fusobacterium spp.), Clostridium spp., Treponema spp., Mycobacterium tuberculosis.

Pharmacokinetics:

The maximum concentration (Stach) in the serum after a single infusion of 400 mg of pefloxacin is observed after 60 minutes and is 4 μg / ml; therapeutic concentrations are maintained for 12-15 hours. After multiple infusions, the serum in the serum is 10 μg / ml. 25-30% of the administered dose bind to blood plasma proteins. Rapidly penetrates and is well distributed in many organs, tissues and body fluids. Therapeutically significant concentrations, exceeding serum concentrations are observed in saliva, sputum, aortic valves, mitral valve, myocardium, bones, mucosa and intestinal wall, peritoneal fluid, pancreatic juice and pancreatic tissue (including necrotic), gallbladder wall, bile, prostate gland, seminal fluid. The volume of distribution is 1.5-1.8 l / kg. Penetrates through the blood-brain barrier: after three-fold administration of 400 mg of pefloxacin, the concentrations in the CSF are 4.5 μg / ml, with an increase in the dose to 800 mg - 9.8 μg / ml; the ratio between the concentration of the drug in the blood plasma and cerebrospinal fluid is 89 %. Concentration in other organs and tissues 12 hours after the last administration: thyroid gland - 11.4 μg / g, salivary glands - 2.2 μg / g, skin - 7.6 μg / g,the mucous membrane of the nasopharynx - 6 μg / g, pharyngeal tonsils - 9 μg / g, muscles - 5.6 μg / g. Half-life (TVS) is equal to 7.2-13 hours (with a single infusion) and 14-15 hours - with repeated administration. Part of the administered dose is metabolized in the liver with the formation of the following metabolites: N- dimethylphefloxacin (norfloxacin, which has significant antibacterial activity), pefloxacin-] M-oxide and pefloxacin-glucuronide. 50-60 % from the administered dose is excreted by the kidneys both in unchanged form and in the form of metabolites; 30% is excreted with bile in the lumen of the intestine (also partially unchanged, in part - in the form of active metabolites (norfloxacin)). The content of unchanged drug in the urine 1-2 hours after the introduction - 25 μg / ml, after 12-24 hours - 15 μg / ml. Unchanged pefloxacin and its metabolites are detected in urine within 84 hours after the last administration of the drug. Poor dialysis: the extraction ratio of pefloxacin in hemodialysis is less than 23%.

Indications:

Antibiotic therapy the following infections, caused by sensitive microorganisms: infections of the central nervous system (bacterial meningitis,caused by meningococci or Gram-negative bacteria, including postoperative or post-traumatic); infections of the upper respiratory tract and ENT organs (acute and chronic sinusitis, mastoiditis); infections of the lower respiratory tract (acute and exacerbation of chronic bronchitis, bronchiectatic disease, community-acquired and hospital pneumonia, caused by gram-negative bacteria or intracellular pathogens); infection of the abdominal cavity (cholecystitis, cholangitis, treatment and prevention of infectious complications of acute destructive pancreatitis, local and widespread peritonitis, including postoperative); complicated and uncomplicated infections of the kidneys and urinary tract (acute and exacerbation of chronic pyelonephritis, infectious complications after operations on the urinary tract); infection of the pelvic organs in women (pelvioperitonitis, salpingoophoritis, tubo-ovarian abscess, endometritis, bartholinitis); infection of the reproductive system in men (orchitis, orchoepidymitis, prostatitis); infections of soft tissues; infection of bones and joints; sepsis; sexually transmitted infections (gonorrhea, urogenital chlamydia); bacterial infections of the gastrointestinal tract, incl.escherichiosis, shigellosis, cholera, salmonellosis, typhoid fever, paratyphoid A, B, C, yersiniosis.

It is used for antibiotic prophylaxis of postoperative purulent-septic complications in urology, abdominal surgery and gynecology.

Contraindications:Hypersensitivity to fluoroquinolones, children under 18, pregnancy and lactation, patients with deficiency of glucose-6-phosphate dehydrogenase.

Carefully:

Patients with neurological disorders (epilepsy, convulsive syndrome of unknown etiology, severe organic lesions of the central nervous system, disorders of cerebral circulation); severe renal and / or hepatic insufficiency.

Pregnancy and lactation:

contraindicated

Dosing and Administration:

Pefloxabol ® is administered by IV infusion of a minimum duration of 60 min.

The first dose is 800 mg. Then 400 mg every 12 hours.

In patients with a liver function disorder of 400 mg every 24 hours. In more severe disorders, 400 mg every 36 hours are administered. With severe liver pathology (jaundice and ascites), the interval between administrations is extended to 2 days.

In patients with severe renal dysfunction (creatinine clearance less than 10 ml / min) and on hemodialysis by 400 mg every 24 hours.

The duration of treatment is determined by the localization and severity of the infection. At the initial stages of treatment Pefloxabol can be used parenterally; after reaching positive dynamics and in the presence of indications for the continuation of therapy, they switch to taking the oral form of the drug.

To prevent infectious complications in surgical practice, it is recommended to administer 400-800 mg of the drug an hour before the operation.

Side effects:

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

On the part of the organs of the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, decreased appetite, flatulence, pseudomembranous colitis, transient increase in the activity of "liver" transaminases, cholestatic jaundice, hepatitis, and necrosis of the liver.

From the genitourinary system: crystalluria, rarely glomerulonephritis, dysuria.

Allergic reactions: skin rash, skin itching, hives, skin hyperemia, rarely - phototoxic reactions, Quincke's edema, bronchospasm, arthralgia.

On the part of the blood system and hemopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, eosinophilia.

Other: tachycardia, myalgia, tendonitis, candidiasis, lengthening of the interval Q-T. Local reactions: phlebitis.

Overdose:

Symptoms: confusion, convulsions, discoordination of movements. Treatment: the specific antidote is unknown. Recommended symptomatic therapy, which if necessary can be supplemented by hemodialysis and peritoneal dialysis.

Interaction:

Antibiotics: combinations of pefloxacin with aminoglycosides possess a synergistic effect against Gram-negative aerobic bacteria, incl. Pseudomonas aeruginosa, which allows you to reduce the dose of aminoglycosides and reduce the likelihood of their oto - and nephrotoxicity. Synergistic and additive effects are achieved with a combination of pefloxacin with beta-lactam antibiotics, phosphomycin and rifampicin.

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. To avoid the development of intoxication, the dose of theophylline should be reduced.

Reduces prothrombin index.During treatment with pefloxacin in patients taking indirect anticoagulants, continuous monitoring of blood clotting is necessary.

Cimetidine and other inhibitors of microsomal liver enzymes increase the half-life of pefloxacin, reduce overall clearance, but do not affect the volume of distribution and renal clearance.

Pharmaceutically incompatible with heparin. When concomitant use, do not mix heparin and pefloxabol®, infusion solution, in a single vial; when administered intravenously, separately.

Pefloxabol®, a solution for infusion, must not be mixed with solutions containing chlorine ions.

Special instructions:

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 (to prevent crystalluria).

As with other fluoroquinolones, due to possible photosensitization, it is recommended to avoid prolonged exposure to direct sunlight or ultraviolet 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 period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for infusion 4 mg / ml.

100 ml of the drug in bottles or bottles of glass with a capacity of 100 ml.

1 bottle (bottle) with instruction for use is placed in a pack of cardboard.

Packaging:bottles (1) - packs cardboard
vials (1) - packs cardboard

Storage conditions:

List B. In the dark place at a temperature of no higher than 25 ° C. Freezing is not allowed.

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:LSR-010039/09

Date of registration:09.12.2009

The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Pefloxbal (Pefloxabol)