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

Meropenem is an antibiotic from the group of carbapenems for parenteral use, interacts with receptors-specific penicillin-binding proteins on the surface of the cytoplasmic membrane, suppresses transpeptidase, inhibits the synthesis of peptidoglycans of the cell wall (due to structural similarity), which eventually causes damage and death of bacteria. Resistant to renal dehydropeptidase-1, it acts bactericidal, easily penetrates the bacterial cell wall, is resistant to the action of most beta-lactamases, has a high affinity for penicillin-binding proteins (PBPs). Among the known beta-lactam antibiotics has the highest activity against most aerobic and anaerobic gram-positive and gram-negative microorganisms.

Active with respect to Gram-positive aerobes:. Bacillus spp, Corynebacterium diphtheriae, Enterococcus liquifaciens, Enterococcus avium, Enterococcus faecalis, Listeria monocytogenes, Lactobacillus spp, Nocardia asteroides, Staphylococcus aureus (including penitsillinazoprodutsiruyuschih), Staphylococcus spp.. (coagulase-negative), incl. Staphylococcus saprophyticus, Staphylococcus capitis, Streptococcus pneumoniae (including strains resistant to penicillin), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus equi, Streptococcus bovis. Streptococcus mitis. Streptococcus viridans, Streptococcus salivarius, Streptococcus morbillorum, Streptococcus spp. (groups G and F), Rhodococcus equi;

Gram-negative aerobes: Achromobacter xylosoxidans, Acinetobacter anitratus, Acinetobacter Iwoffii, Acinetobacter baumannii, Aeromonas hydrophila, Aeromonas sorbria, Aeromonas caviae, Alcaligenes faecalis, Bordetella bronchiseptica. Brucella melitensis, Campylobacter coli, Campylobacter jejuni, Citrobacter freundii, Citrobacter diversus, Citrobacter amalonaticus, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae (including beta-lactamase-producing and ampicillin-resistant strains), Haemophilus parainfluenzae, Haemophilus ducreyi , Helicobacter pylori, Neisseria meningitidis, Neisseria gonorrhoeae (including beta laktamazopolozhitelnye strains resistant to penicillin and spectinomycin), Hafhia alvei, Klebsiella pneumoniae, Klebsiella aerogenes, Klebsiella ozaenae, Klebsiella oxytoca, Moraxella catarrhalis, Morganella morganii, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia alcalifaciens, Pasteurella multocida, Pseudomonas shigelloides, Pseudomonas aeru ginosa, Pseudomonas putida, Pseudomonas alcaligenes, Burkholdcria cepacia, Pseudomonas fluorescens, Pseudomonas stutzeri, Stenotrophomonas. Salmonella spp., Including Salmonella typhi, Serratia marcescens, Serratia liquifaciens, Serratia spp., Shigella sonnei, Shigella flexneri, Shigella dysenteria, Vibrio cholerae, Vibrio parahaemolyticus, Vibrio vulnificus, Yersinia enterocolitica;

anaerobic bacteria: Actinomyces israelii, Bacteroides spp. (including Bacteroides fragilis, Bacteroides vulgatus, Bacteroides variabilis, Bacteroides pneumosintes, Bacteroides coagulans, Bacteroides uniformis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicronron), Prevotella spp. (including Prevotella melaninogenica, Prevotella buccae, Prevotella denticola, Prevotella levii), Porphyromonas spp. (including Porphyromonas asaccharolyticus). Bifidobacterium spp., Clostridium perfringens, Clostridium difficile, Clostridium sporogenes, Clostridium cadaveris, Clostridium sordellii, Clostridium butyricum, Clostridium clostridiiformis, Clostridium tetani, Eubacter lentum, Eubacter aerofaciens, Fusobacterium mortiferum, Fusobacterium necrophorum, Mobiluncus curtisii, Mobiluncus mulieris, Peptostreptococcus anaerobius, Peptostreptococcus micros, Peptostreptococcus saccharolyticus, Peptococcus magnus, Peptococcus prevotii, Propionibacterium acne, Propionibacterium avidium, Propionibacterium granulosum.

Pharmacokinetics:

When intravenous (iv) 250 mg for 30 minutes, the maximum concentration) Cmax - 11 μg / ml, for a dose of 500 mg - 23 μg / ml, 1 g - 49 μg / ml (absolute pharmacokinetic proportional dependence on the administered dose for Stam and AUC no). When the dose is increased from 0.25 to 2 g, the clearance decreases from 287 to 205 ml / min. With IV bolus administration for 5 minutes, 500 mg of C max is 52 μg / ml, 1 g is 112 μg / ml. Connection with plasma proteins -2%.

Well penetrates into most tissues and body fluids, incl. in CSF of patients with bacterial meningitis, reaching concentrations exceeding those required for suppression of the majority of bacteria (bactericidal concentrations are created 0.5-1.5 h after the start of infusion). In small amounts penetrates into breast milk.

Exposed to a slight metabolism in the liver with the formation of a single inactive metabolite. The half-life period (T1 / 2) is 1 hour, in children under 2 years is 1.5-2.3 hours. In the dose range of 10-40 mg / kg in adults and children, a linear dependence of pharmacokinetic parameters is observed. Do not cumulate.

It is excreted by the kidneys - 70 % at unchanged for 12 hours. The concentration of meropenem in the urine, exceeding 10 μg / ml, is maintained for 5 hours after the administration of 500 mg. In patients with renal insufficiency, clearance is correlated with QC.In elderly patients, a decrease in meropenem clearance correlates with a decrease in QC associated with age. T1 / 2 - 1.5 hours. It is excreted in hemodialysis.

Indications:Infectious-inflammatory diseases caused by sensitive pathogens: infections of the lower respiratory tract (including pneumonia, including hospital, infections caused by Pseudomonas aeruginosa), abdominal infections (complicated appendicitis, peritonitis, pelvicperitonitis), pyelonephritis, pyelitis, skin and soft skin infections tissues (including erysipelas, impetigo, secondarily infected dermatoses), dysentery, endocarditis, bacterial meningitis, sepsis, pelvic inflammatory diseases (including endometritis), suspicion of bacterial and fektsiyu adults with febrile episodes of neutropenia (empirical treatment).

Contraindications:

Hypersensitivity, including to other beta-lactam antibiotics; children's age (up to 3 months).

Pregnancy and lactation:

Safety of use during pregnancy is not defined.

For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Meropenabol should be administered as an intravenous bolus injection for at least 5 minutes, or as an intravenous infusion for 15 to 30 minutes.

Dosage and duration of therapy should be determined depending on the type and severity of the infection and the condition of the patient.

The following daily doses are recommended:

Adults

500 mg intravenously every 8 hours for the treatment of pneumonia, urinary tract infections, gynecological infections such as endometritis, and pelvic inflammatory diseases, skin and soft tissue infections.

1 g intravenously every 8 hours in the treatment of hospital pneumonia, peritonitis, suspected bacterial infection in patients with neutropenia, and septicemia.

In the treatment of meningitis, the recommended dose is 2 g every 8 hours.

In chronic renal failure, the dose is adjusted depending on the creatinine clearance (CK): with a KC of 26-50 ml / min, 0.5-1 g

2 times a day, 10-25 ml / min - 250-500 mg twice a day, less than 10 ml / min - 500 mg once a day.

Meropenem is excreted in hemodialysis. If prolonged treatment is required, it is recommended that the dose unit (determined depending on the type and severity of the infection) be introduced at the end of the hemodialysis procedure to restore the effective plasma concentration.

Children

For children aged 3 months to 12 years, the recommended dose for intravenous administration is 10-20 mg / kg every 8 hours, depending on the type and severity of the infection, the sensitivity of the pathogen and the patient's condition. For children weighing more than 50 kg, dosages should be used for adults.

With meningitis, the recommended dose is 40 mg / kg every 8 hours.

Meropenabol is not recommended for use in children less than 3 months of age.

No experience in children with impaired liver and kidney function.

Preparation of solutions

For intravenous bolus injections Meropenabol should be diluted with sterile water for injection (10 ml per 500 mg of meropenem). This provides a solution concentration of 50 mg / ml.

For intravenous infusions meropenabol diluted with sterile water for injection or a compatible infusion fluid and then another compatible infusion fluid (50-200 ml).

Meropenabol is compatible with the following infusion liquids:

- 0,9 % sodium chloride for intravenous infusions;

- 5 % or 10% dextrose for intravenous infusions;

- 5 % dextrose for intravenous infusions with 0.02 % sodium bicarbonate;

- 0,9 % sodium chloride and 5% dextrose for intravenous infusions;

- 5 % dextrose from 0.225 % sodium chloride for intravenous infusions;

- 5 % dextrose with 0.15% potassium chloride for intravenous infusions;

- mannitol 2.5% and 10% for IV infusion.

Meropenabol should not be mixed with solutions containing other drugs.

Side effects:

From the digestive system: pain in the epigastric region, nausea, vomiting, diarrhea, cholestatic hepatitis, hyperbilirubinemia, increased activity of "liver" transaminases and alkaline phosphatase, lactate dehydrogenase, rarely - candidiasis of the oral cavity, pseudomembranous colitis.

From the side of the cardiovascular system: tachy- or bradycardia, a decrease or increase in blood pressure, the development or exacerbation of heart failure, fainting, myocardial infarction, thromboembolism of the branches of the pulmonary artery, cardiac arrest.

From the urinary system: dysuria, edema, renal dysfunction (hypercreatininaemia, increased urea concentration in plasma), hematuria.

Allergic reactions: skin itching, skin rash, urticaria, multiforme exudative erythema, angioedema, anaphylactic shock.

From the nervous system: headache, paresthesia, insomnia, increased excitability, anxiety, depression, impaired consciousness, hallucinations, epileptiform seizures, convulsions.

From the laboratory indicators: eosinophilia, neutropenia, leukopenia, rarely - agranulocytosis, reversible thrombocytopenia, reduction of partial thromboplastin time.

Local Reactions: inflammation, thrombophlebitis, tenderness at the injection site.

Other: positive direct or indirect samples of Coombs, anemia, dyspnea, vaginal candidiasis.

Overdose:

Accidental overdose is possible during treatment, especially in patients with impaired renal function. Treatment in case of an overdose should be symptomatic. Normally, there is a rapid elimination of the drug during hemodialysis.

Interaction:

Compatible with 0.9% solution of sodium chloride, 5% or 10% % solutions of dextrose, 5 % dextrose solution and 0.02 % solution of sodium hydrogen carbonate, 0.9 % solution of sodium chloride and 5% solution of dextrose, 5 % solution of dextrose with 0.225% sodium chloride, 5% dextrose solution with 0.15 % potassium chloride, 2.5% and 10% % solution of mannitol.

Compatibility of meropenem with other drugs,except those listed above, is not established. therefore meropenem and its solutions should not be mixed or added to solutions, containing other drugs.

Drugs that block tubular secretion, slow down excretion and increase the concentration of meropenem in the plasma.

Special instructions:

Patients who have a history of hypersensitivity to carbapenems, penicillins or other beta-lactam antibiotics may exhibit hypersensitivity to meropenem.

Treatment of patients with liver diseases should be carried out under careful monitoring of the activity of "liver" transaminases and bilirubin concentrations.

In the course of treatment, the development of resistance of pathogens is possible, and therefore prolonged treatment is carried out under the constant control of the distribution of resistant strains. In individuals with gastrointestinal complaints, especially those suffering from colitis, it is necessary to consider the possibility of developing pseudomembranous colitis (toxin produced Clostridium difficile, is one of the main causes of colitis associated with antibiotics), the first symptom of which can be the development of diarrhea on the background of treatment.

In monotherapy of a known or suspected lower respiratory tract infection of severe course caused by Pseudomonas aeruginosa, a regular determination of the sensitivity of the pathogen is recommended.

Form release / dosage:Powder for the preparation of a solution for intravenous administration of 0.5 g and 1 g.

Packaging:

0.5 g or 1.0 g of active substance into glass vials.

1 bottle with the drug, along with instructions for use, is placed in a pack of cardboard.

Storage conditions:

In a dry, sheltered from the world spot,at a temperature of no higher than 25 ° C.

Keep out of the reach of children place.

For intravenous injection and infusion is recommended freshly prepared solution meropenem, however diluted Meropenem can retain its activity for 6 hours at storage solution at a temperature of 25 ° C and 36 hours, if the solution Store at a temperature not higher than 5 ° C. DO NOT freeze solution Meropenem!

Shelf life:

3 years. Do not use after the expiration date on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002218/07

Date of registration:15.08.2007 / 12.02.2018

Expiration Date:Unlimited

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

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp01.05.2018

Illustrated instructions

Instructions

Meropenabol® (Meropenabol)