Mesonex

Mesonex is a systemic antimicrobial drug. It belongs to the carbapenem category.

Indications Mesonexa

It is used for infectious lesions caused by the activity of one or more microbes that are sensitive to the drug:

• lesions affecting the lower respiratory tract (pneumonia, including nosocomial forms);
• urinary tract lesions;
• infections inside the abdominal area;
• gynecological disorders, including endometritis and pelvic organ lesions;
• having uncomplicated lesions of the subcutaneous layer and epidermis (also similar disorders occurring with complications);
• meningitis or septicemia of bacterial origin;
• empirical procedures when there is a suspicion of bacterial infection in an adult with febrile seizures during neutropenia.

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Release form

The pharmaceutical element is released in a lyophilisate for the preparation of injection liquid, 0.5 or 1 g of the substance inside a vial. There is 1 such vial in a pack.

Pharmacodynamics

Meropenem is considered an antibiotic from the carbapenem subgroup; it has resistance to human hydropene-1. It is administered parenterally. It has a bactericidal effect by affecting the binding of bacterial cell membranes.

The substance easily passes through the membranes of bacterial cells, has a significantly high stability in relation to most lactamases, as well as significant affinity in relation to proteins that perform penicillin synthesis (element PBSs). All this explains the significant bactericidal activity of meropenem in relation to a fairly wide range of pathogenic anaerobes with aerobes.

Bactericidal values are usually 1-2 times the bacteriostatic value of meropenem (except for Listeria monocytogenes, for which a lethal effect does not develop).

In vitro and in vivo tests have shown that meropenem has a post-antibiotic effect.

The antibacterial therapeutic range, registered in vitro, contains a large number of clinically important Gram(-) and Gram(+) microbes, as well as pathogenic anaerobes and aerobes.

Pharmacokinetics

After a half-hour intravenous injection of the 1st portion of the drug to a healthy person, a plasma Cmax value of approximately 23 μg/ml (with a 0.5 g portion) and 49 μg/ml (with a dosage of 1 g) was noted. However, no absolute corresponding pharmacokinetic relationship was found between the AUC, Cmax values and the size of the portion used. In addition, a decrease in the clearance rate was noted from 287 to 205 l/min when the dosage of the drug was increased from 0.25 g to 2 g.

Administration of a 1 g bolus injection over 2, 3 and 5 minutes to a healthy subject results in plasma Cmax values of approximately 110, 91 and 94 μg/mL.

Intravenous bolus administration of 1 portion of the drug over a 5-minute period to a healthy individual results in the development of a plasma Cmax value of approximately 52 mcg/ml (0.5 g portion) and 112 mcg/ml (1 g dosage).

After 6 hours from the moment of administration of 0.5 g Mesonex, the plasma level of meropenem decreases to 1 mcg/ml or lower.

After administration of multiple doses at 8-hour intervals, no accumulation of meropenem was observed in subjects with healthy renal function.

In individuals with healthy renal function, the half-life is approximately 1 hour. Intraplasmic synthesis with protein is about 2%.

Approximately 70% of the dose is excreted unchanged in the urine within 12 hours. Subsequent urinary excretion is negligible.

The values of meropenem in urine that exceed 10 mcg/ml are maintained at this level for 5 hours (if a dosage of 0.5 g was administered). In the case of using 0.5 g of the drug at 8-hour intervals, or 1 g at 6-hour intervals, no accumulation of meropenem in urine or blood plasma was observed.

Mesonex is able to penetrate most tissues with fluids (including cerebrospinal fluid in people with bacterial meningitis), reaching levels exceeding those required to suppress most microbes.

Dosing and administration

The medication should be administered in the form of a bolus injection (the injection lasts at least 5 minutes) or through intravenous administration lasting 15-30 minutes.

When administering intravenous bolus injections, the drug is first diluted with a special sterile injection fluid (5 ml per 0.25 g of meropenem) to obtain a concentration of the substance of 50 mg/ml.

In case of intravenous injections, the medicine is diluted with sterile injection fluid or physiological fluid to a volume of 50-200 ml.

The following infusion fluids are suitable for diluting Mesonex:

• 0.9% NaCl infusion;
• 5% or 10% glucose liquid;
• 5% glucose liquid together with 0.02% sodium bicarbonate;
• 0.9% NaCl with 5% glucose liquid;
• 5% glucose liquid together with 0.225% NaCl;
• 5% glucose liquid together with 0.15% potassium chloride infusion;
• 2.5%, as well as 10% mannitol solution for intravenous injections.

The medicine inside such a liquid dissolves completely, without forming a sediment.

The dosage portions and duration of the treatment cycle for adults are selected taking into account the person’s condition and the type of severity of the lesion.

Recommended daily servings of LS include:

• accompanied by complications of urinary system damage - 0.5 g at 8-hour intervals;
• lesions of the epidermis with the subcutaneous layer (with or without complications) - 0.5 g at 8-hour intervals;
• infections of a gynecological nature (including lesions of the pelvic organs) - 0.5 g of the substance at an 8-hour interval;
• lesions of the lower respiratory tract - 0.5 g with an 8-hour interval (for nosocomial pneumonia, the dosage is 1 g);
• lesions of the abdominal area (with complications) or septicemia - 1 g of medication, maintaining an 8-hour interval;
• meningitis - 2 g of the drug, maintaining an 8-hour interval.

People with renal insufficiency.

For individuals with a CC level below 51 ml/minute, portion sizes are reduced as follows:

• CC, which is ≥51 ml per minute - 1 injection is 0.5-1 g (an 8-hour interval is required);
• CC in the range of 26-50 ml per minute – 1 injection is equal to 0.5 g (with a 12-hour interval);
• CC within 10-25 ml in 60 seconds – 1 injection equals 0.25 g (with a 12-hour interval);
• the value of CC <10 ml in 1 minute – 1 injection is 0.25 g (with a 24-hour interval).

Mesonex can be excreted during hemodialysis. If long-term use of the drug is necessary, a 1-time dose (selected taking into account the intensity and form of the developed lesion) should be used after completion of the hemodialysis session - to restore the therapeutically active plasma levels of the drug.

There is no experience with the use of the drug in people receiving peritoneal dialysis.

Use in the elderly.

Elderly people with kidney problems or CC values above 51 ml/minute require a dosage adjustment.

Mode of use and dosage for children.

Children under 12 years of age are required to be administered 10-20 mg/kg of the pharmaceutical element at 8-hour intervals (taking into account the complexity of the lesion and the child’s condition, and along with this, his sensitivity to pathogenic microbes).

Recommended daily dosages of the medication:

• urinary system lesions with complications – 10 mg/kg with an 8-hour time interval;
• lesions of subcutaneous tissue and epidermis (without complications) or the lower respiratory tract (pneumonia) – 10-20 mg/kg of the component in 8-hour intervals;
• Intra-abdominal infections (with complications) – 20 mg/kg of the drug at 8-hour intervals;
• meningitis – 40 mg/kg of drug (intervals are 8 hours).

Children weighing over 50 kg should be prescribed adult portion doses.

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Use Mesonexa during pregnancy

There is no information regarding the safety of Mesonex administration during pregnancy. Animal tests have shown that there is no negative impact on the fetus. The drug is prescribed to pregnant women as long as the benefit from it is more likely than the risk of negative consequences for the fetus. The drug should be used exclusively under constant medical supervision.

Only extremely low levels of the drug are found in animal milk. It is only allowed to be prescribed to nursing women in cases where the benefit from its use is higher than the risk to the baby. It is recommended to stop breastfeeding during therapy.

Contraindications

Contraindicated for use in people with intolerance to β-lactam antibiotics.

Side effects Mesonexa

Side effects include:

• local manifestations after intravenous injection: thrombophlebitis, inflammation or pain;
• epidermal lesions: itching, rashes or hives;
• disorders affecting the gastrointestinal tract: nausea, hepatitis, abdominal pain, diarrhea and vomiting;
• blood system disorders: treatable thrombocythemia, as well as neutropenia or thrombocythemia with eosinophilia. Some patients may develop a direct or indirect positive Coombs test. There are reports of a partial reduction in the thromboplastin formation period;
• liver function problems: treatable increase in serum bilirubin, alkaline phosphatase, transaminases, and lactic dehydrogenase levels;
• lesions affecting the cardiovascular system: bradycardia, heart failure, myocardial infarction, tachycardia or pulmonary embolism;
• CNS dysfunction: paresthesia, convulsions along with severe headaches, depression and a feeling of excitement;
• renal dysfunction: hematuria or dysuria;
• other manifestations: thrush or oral candidiasis.

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Overdose

Mesonex poisoning often develops in people with problems related to renal function. Manifestations include dyspnea, ataxia and convulsions.

In case of overdose, symptomatic measures are taken. In people with renal dysfunction, meropenem and its metabolic elements can be excreted by hemodialysis.

Interactions with other drugs

The drug must be administered with extreme caution in combination with medications that have potential nephrotoxicity.

Probenecid competes with the meropenem element in tubular excretion, thereby enhancing renal excretion while simultaneously prolonging the half-life of the substance and increasing its plasma levels. Since the intensity and duration of the medicinal effect of Mesonex dosed without probenecid are similar, these medicinal substances should not be combined.

The drug reduces serum levels of valproic acid.

The medicine can be mixed with solutions containing other medicinal substances.

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Storage conditions

Mesonex in the form of dry lyophilisate should be stored in a place completely closed to small children. Temperature marks - not higher than 25°C.

Shelf life

Mesonex can be prescribed for a period of 24 months from the date of manufacture of the therapeutic agent.

Application for children

Should not be administered to infants under 3 months of age.

Analogues

The analogs of the drug are Demopenem, Meronem, Romenem with Europenem, Merocef with Invanz and Meropenem with Inemplus. In addition, Sinerpen, Lastinem, Meromak with Mepenam, Prepenem with Merobocide, Tienam and Meromek with Ronem and Merospen.