Medopenem

Medopenem is an antibacterial systemic medicine. Included in the group of β-lactam antibiotics.

[1], [2], [3], [4],

Indications Medopenema

It is used for therapy in infections provoked by the activity of microbes that have sensitivity with respect to drugs:

• pneumonia (this includes her nosocomial form);
• infections that affect the urethra;
• diseases in the intra-abdominal area;
• Gynecological lesions (eg, endometritis);
• infections affecting soft structures and epidermis;
• septicemia or meningitis ;
• an empirical form of therapy in situations where bacterial damage is suspected in an adult with neutropenic fever (in the form of monotherapy or in combination with antimycotics or drugs with antiviral effect).

Medopenem is used in monotherapy or in complex therapy with other antimicrobial medications in people with polymicrobial forms of infection (eg, cystic fibrosis or chronic lesions in the lower respiratory tract).

Release form

The drug is produced in the form of lyophilizate for the production of injectable or infusion substances. The bottle has a volume of 500 or 1000 mg. Inside the pack - 1 such a bottle.

Pharmacodynamics

Medopenem is a carbapenem antibiotic administered by the parenteral method. It has relative stability with respect to the effect of the human element DHP-1, which means that it does not need to add a substance that slows DHP-1 activity.

The drug has a bactericidal effect, interfering with the important for the life of microbes, the process of binding their cell membranes. It very easily passes into the cell membranes of bacteria, has high stability indices relative to all serine β-lactamases, and also a pronounced affinity for the penicillin-synthesizing proteins. This is what ensures the potency of bactericidal properties of the drug in relation to a large range of aerobes with anaerobes. The minimum bactericidal indexes (MIA) are often similar to the minimum decelerating indicators (MIS). In 76% of microbes, the proportions of MIA / MIS are 2 or lower.

The medication shows stability when testing its sensitivity. In vitro studies demonstrate that it has a synergistic interaction with a variety of antibiotics. Tests in vitro, as well as in vivo, showed that the drug has a post-antibiotic effect.

The antibacterial range of drugs in vitro includes most of the clinically important Gram-negative and-positive microbial strains, as well as anaerobes and aerobes, which are listed below.

Gram-positive aerobics:

• hay bacillus, diphtheria corynebacterium, Enterococcus liquifaciens, enterococcus fecal and avian enterococcus, as well as Nocardia asteroids, listeria monocytogenes and Lactobacillus spp .;
• Staphylococcus cohnii, epidermal staphylococcus, S. Xylosus, saprophytic staphylococcus, staphylococcus capitis, Staphylococcus simulans, staphylococcus varvers, Staphylococcus hominis, and in addition S.sciuri, S.intermedius and Staphylococcus lugdunensis ;
• pneumococcus (sensitive or resistant to penicillin), Str.equi, pyogenic streptococcus, Str.bovis, Str.mitior, streptococcus mitis, as well as Str.milleri, streptococcus agalactia, Streptococcus morbillorum, streptococcus viridance, Str.sanguis, salivary streptococcus, R .equi and streptococci from categories G and F.

Aerobics having a gram-negative type:

• Acinetobacter anitratus, Aeromonas sorbria, hydrophilic aeromonas, Achromobacter xylosoxidans, Baumann akinetobacterium, Acinetobacter lwoffii, hydrophilic aeronad and fecal alkali-forming agent;
• Bordetella bronchiseptic, Brucella Maltese, Citrobacter diversus, Campylobacter coli, Campylobacter vellum, Citrobacter amalonaticus, and in addition Citrobacter koseri and Citrobert bacteria;
• Enterobacter aerogenes, Enterobacter cloaca, Enterobacter (Pantoea) aglomeran and Enterobacter sakazakii;
• E. Coli, Escherichia hermannii;
• gardnerella vaginalis, hemophilic rod (this includes strains sensitive to β-lactamases and resistant to ampicillin), Ducrea's stick and Heamophilus parainfluenzae;
• Helicobacter pylori, meningococcus, gonococcus (this includes strains sensitive to β-lactamases, and resistant to spectinomycin) and H. Alvei;
• Klebsiella pneumonia, Klebsiella ozaenae, klebsiella aerogenes and klebsiella oxytoca;
• Moraxella cataralis and Morgan's bacterium;
• ordinary protaeus, proteus mirabilis and Proteus penneri;
• Providence of Röttger, Stewart's Providence, P.alcalifaciens, the Multicidula Pasteurella and Plesiomonas shigelloides;
• Pseudomonas pathogen, Pseudomonas alcaligenes, B. Cepacia, fluorescent pseudomonas, Pseudomonas stutzeri, Burkholderia mallia and Pseudomonas acidovorans;
• Salmonella, among which salmonella enteric and Salmonella typhi;
• Serceria marcescenza, Serratia rubidaea and Serratia liquefaciens;
• Shigella Sonne, Shigella Flexner, Shigella Boyd and the bacterium Grigoriev-Shigi;
• cholera vibrio, paragemolytic vibrio, vibrio vulviphicus and Yersinia enterocolitis.

Anaeroby:

• Actinomyces meyeri и Actinomyces odontolyticus;
• Bacteroides-Prevotella-Porphynomonas spp., Bacteroidia fraigilis, B.distasonis, bacteroides vulgatus, B.pneumosintes, B.gracilis, and in addition B.coagulans, B.variabilis and B.levii. Also on the list are B.capsillosis, B.ovatus, the bacterium tetiothaomicron, Bacteroides eggerthii, and in addition B.uniformis and Bacteroides ureolyticus;
• P.bivia, P.buccalis, P.melaninogenica, Prevotella splanchnicus, P.disiens, P.intermedia, P.oris, Prevotella oralis, P.buccae, P.rumenicola, Prevotella denticola, P.corporis;
• porphyromonas gingivalis, bifidobacteria and Bilophila wadsworthia;
• clostridium perfrigence, Clostridium sordellii, C.bifermentalis, clostridium sporogenes, C.cadaveris, C.clostridiiformis, C.subterminale, Clostridium branched, C.butyricum, harmless bacteria и C.tertium;
• Eubacterium aerofaciens и E.lentum;
• F.mortiferum, Schmorl's wand, Plaut's wand and Fusobacterium varium;
• M.mulieris, а also Mobiluncus curtisii;
• peptostreptococcus anaerobius, Peptostreptococcus saccharolyticus, P.magnus, Peptostreptococcus micros, as well as Peptostreptococcus asaccharolyticus and P.prevotii;
• propionibacteria acne, Propionibacterium granulosum, and Propionibacterium avidum.

It was found that stentrofomonas maltophilia, enterococcus fecium and staphylococci, resistant to methicillin, are resistant to Medopenem.

Pharmacokinetics

In IV injections, taking into account the size of the dose (500 or 1000 mg), as well as the method of administration (bolus or through a dropper), the C max values inside the blood serum are, respectively, 23, 45, 49 and 112, respectively gt; μg / ml.

Protein synthesis, carried out inside the plasma, is 2%. The drug easily passes inside a variety of liquids (eg, cerebrospinal fluid) and tissues; bactericidal values are noted after 30-90 minutes after the injection.

Inside the liver, there are weak biotransformation processes in which a single metabolic product (not having drug activity) is formed. The half-life is 60 minutes.

Most of the substance is excreted through the kidneys (more than 70% - in the unchanged state).

In persons with a deficiency of renal activity, the drug clearance is in direct proportion to the decrease in QC.

Pharmacokinetic characteristics of the drug in children are similar to adults. The half-life of children under 2 years of age is about 1.5-2.3 hours; there is also a linear dependence of LS values on the dosage size within the range of 10-40 mg / kg.

In elderly people, the level of clearance of Medopenem decreases, correlating with a decrease in CC values associated with age.

[5], [6], [7], [8], [9], [10], [11], [12], [13]

Dosing and administration

Scheme for an adult.

The size of the portion and duration of treatment are selected taking into account the patient's condition, as well as the intensity and type of the infection.

For a day, it is recommended to take the medicine in such dosages:

• with infections in the area of the organs of urination, pneumonia, and at the same time for infections of a gynecological nature (for example, endometritis) and lesions affecting the subcutaneous layer and epidermis - 0.5 g of LS with intervals equal to 8 hours;
• with peritonitis or nosocomial pneumonia or if there is a suspicion of the development of infection in people with septicemia or neutropenia - 1 g of the drug with 8-hour intervals;
• in cystic fibrosis, 2000 mg of medication is used at 8-hour intervals;
• with meningitis, you need to inject 2000 mg of LS with 8-hour breaks.

As with the use of other antibiotics, meropenem for monotherapy in people with severe pathologies and diagnosed or suspected presence of Pseudomonas aeruginosa in the lower part of the respiratory ducts should be used very carefully.

During treatment with Pseudomonas aeruginosa, it is necessary to constantly test for sensitivity.

Dosage regimen in adults with insufficient renal function.

In persons with QC values less than 51 ml / minute, the dosage should be lowered according to the scheme described below:

• Values of SC within 26-50 ml / minute - 1 dosage unit *, applied with intervals equal to 12 hours;
• QC values within 10-25 ml / minute - 0.5 dosage unit, applied at intervals of 12 hours;
• CK level <10 ml / minute - 0.5 dosage unit used with a 24-hour interval.

* is compiled on the basis of dosage units equal to 0.5, 1 and 2 g.

Excretion of Medopenem can be carried out with hemodialysis. If prolonged drug use is required, one dosage unit should be given (with regard to the intensity and type of lesion) at the end of the hemodialysis session. This is required to restore medically effective plasma values of the drug.

People who are on peritoneal dialysis, the medicine was not used.

Portions for the child.

Children in the range from 3 months to 12 years of age need to be administered 10-20 mg / kg of substance at 8-hour intervals, given the type and degree of lesion intensity, the patient's condition and the sensitivity of the pathogen. Children whose weight is more than 50 kg, you need to appoint adult dosages.

Children aged 4-18 years with cystic fibrosis, and in addition, with exacerbations of chronic lesions in the lower part of the respiratory tract, appoint portions of 25-40 mg / kg with 8-hour intervals. To treat meningitis, you need to use 40 mg / kg with 8-hour intervals.

Methods of using drugs.

The prepared liquid must be shaken before use.

The bolus is administered for 5 minutes, and the infusion is approximately 15-30 minutes.

For the bolus prick, the substance is diluted using sterile injectable water (5 ml per 0.25 g of the preparation), giving a concentration equal to 50 mg / ml. The finished liquid becomes colorless (or has a pale yellow hue) and is transparent.

For infusions medication is manufactured using compatible infusion liquids (50-200 ml volume is required). Among compatible medicinal substances:

• 0.9% NaCl solution;
• 5% or 10% glucose solution;
• 5% glucose solution supplemented with 0.02% sodium bicarbonate;
• 5% glucose solution with 0.9% NaCl;
• 5% glucose solution with 0.225% NaCl;
• 5% glucose solution with 0.15% potassium chloride;
• 2.5% or 10% mannitol solution.

Use Medopenema during pregnancy

It is forbidden to use the drug during pregnancy or lactation, except for situations when it is likely that the benefits for a woman are more expected than the development of a fetus or child of severe consequences. Use the medicine only under the supervision of the treating doctor.

For the duration of therapy, it is necessary to cancel breastfeeding of the baby.

Contraindications

It is contraindicated to prescribe to people with hypersensitivity to the medication.

Side effects Medopenema

The use of medication can trigger the emergence of various side effects:

• lesions in the lymphatic and circulatory system: often thrombocytopenia occurs. Occasionally, eosinophilia occurs. Possible development of neutrophilic or leukopenia, hemolytic form of anemia or agranulocytosis;
• disorders affecting the work of the National Assembly: headaches often develop. Cramps appear sporadically. Perhaps the development of paresthesias;
• problems with the digestive function: often there is vomiting, abdominal pain, diarrhea or nausea, and in addition there is an increase in the values of AP or transaminases, as well as LDH inside the serum. There may be a pseudomembranous form of colitis;
• lesions of the subcutaneous layer and epidermis: often there is an itch or a rash. Possible occurrence of polyformiform erythema, urticaria, TEN and Stevens-Johnson syndrome;
• systemic disorders and signs at the site of injection: often develop pain or inflammation. Perhaps the emergence of candidiasis (vaginal or oral form) or thrombophlebitis;
• disorders of hepatobiliary system function: occasionally an increase in bilirubin values is noted;
• immune lesions: there may be signs of anaphylaxis or Quinnke edema.

[14]

Overdose

When intoxication develops symptoms described as side effects.

Symptomatic measures and hemodialysis sessions are used to eliminate disorders.

Interactions with other drugs

It is necessary with great care to use the medication together with drugs that carry potential toxicity to the kidneys.

Probenecid is a competitor of meropenem in relation to tubular excretion, therefore it inhibits secretion through the kidneys, which causes an extension of the half-life and an increase in plasma LS values. Because the duration and severity of the influence of the drug, applied without probenecid, is identical, it is forbidden to use them in combination.

Medopenem is able to lower the values of valproic acid inside the serum. In individual people, these indicators can reach subtherapeutic levels.

The drug is used together with other medicines without any negative therapeutic interaction (excluding the above probenecid).

[15]

Storage conditions

Medopenem must be kept in a place that is closed from the infiltration of children. The temperature is a maximum of 25 ° C.

Ready for intravenous administration, the liquid should be used immediately, although the stability of such solutions persists for a while at temperatures of 2-8 ° C and up to 25 ° C.

Do not freeze the finished injection liquid. Bottles can be used only 1-fold.

When manufacturing medicines and injections, it is necessary to follow the standards of existing aseptic conditions.

Shelf life

Medopenem can be used within 24 months from the date of manufacture of the drug.

Application for children

Medopenem is not used in infants until 3 months of age, but at the same time in children with kidney problems with the liver.

There is no experience of administering to children with immunodeficiency, having a primary or secondary stage, and also with neutropenia.

Analogues

Analogues of the medication are medications Merospen, Aris, Mepenem with Europenem, Meronem with Excipenem, and also Merobocid, Alvopenem, Romen and Merogram.

Reviews

Medopenem receives good reviews from the people who used him. The drug demonstrates high efficiency even in severe forms of diseases. With such a qualitative therapeutic effect, even the high cost of a medicine is not considered a minus.