Mezonex

Mezonex is a systemic antimicrobial drug. Included in the category of carbapenems.

Indications The mausoleum

It is used for infectious lesions provoked by the activity of one or several microbes that are sensitive to the medication:

• lesions affecting the lower region of the respiratory tract (pneumonia, among which is also the nosocomial form);
• lesions of the urinary system;
• infection within the abdominal area;
• gynecological disorders, including endometritis and pelvic lesions;
• having uncomplicated damage to the subcutaneous layer and the epidermis (also similar disorders occurring with complications);
• meningitis or septicemia having a bacterial nature;
• empirical procedures in case of suspicion of bacterial genesis infection in an adult with febrile seizures during neutropenia.

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

Release form

The release of the pharmaceutical element occurs in the lyophilisate for the preparation of injection fluid, 0.5 or 1 g of the substance inside the vial. In a pack - 1 similar bottle.

Pharmacodynamics

Meropenem is considered an antibiotic of the carbapenem subgroup; is resistant to human hydropent-1. Introduced by parenteral method. It has a bactericidal effect, affecting the binding of the membranes of bacterial cells.

The substance easily passes through the membranes of bacterial cells, has a significantly high stability against most lactamases, as well as significant affinity for proteins that carry out the synthesis of penicillin (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 indicator of meropenem (except for Listeria, monocytogenes, in relation to which the lethal effect does not develop).

When performing in vitro tests, and with it in vivo, it was determined that meropenem possesses a post-antibiotic effect.

The antibacterial therapeutic range registered in vitro contains a large number of clinically important gram (-) and gram (+) microbes, and at the same time, pathogenic anaerobes and aerobes.

Pharmacokinetics

After a half-hour intravenous injection of the 1st dose of the drug to a healthy person, plasma Cmax was noted, which was approximately 23 μg / ml (with a portion of 0.5 g), as well as 49 μg / ml (at a dosage of 1 g). But the absolute corresponding pharmacokinetic binding between the values of AUC, Cmax and the size of the applied portion was not detected. In addition, there was a decrease in the level of clearance from the mark of 287 to 205 l / min, when the dosage of drugs was increased from 0.25 g to 2 g.

The injection of a bolus injection with a portion of 1 g for 2, 3, and 5 minutes to a healthy person leads to plasma Cmax values of approximately 110, 91, and 94 mcg / ml.

Intravenous bolus administration of the 1st dose of drugs over a 5-minute period to a healthy person leads to the development of a plasma Cmax value of approximately 52 μg / ml (a dose of 0.5 g), as well as 112 μg / ml (1 g dosage).

After 6 hours from the moment of applying 0.5 g of Mezonex, the plasma indicator meropenem is reduced to 1 μg / ml or lower.

After using multiple doses with an 8-hour interval, accumulation of meropenem is not observed in people with healthy renal activity.

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

Approximately 70% of the dosage is excreted unchanged in the urine for 12 hours. Subsequent elimination of the substance with urine is negligible.

The values of meropenem inside the urine, which exceed the mark of 10 μg / ml, are maintained at this level within 5 hours (if a dosage of 0.5 g has been introduced). In the case of the use of 0.5 g of drugs with 8-hour or 1-g with 6-hour intervals, accumulation of meropenem inside the urine and blood plasma was not observed.

Mezonex is able to penetrate into the majority of tissues with liquids (among them, the cerebrospinal fluid in people with meningitis of bacterial origin), reaching elevations exceeding those required to suppress most of the microbes.

Dosing and administration

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

When conducting intravenous bolus-type pricks, the preparation is preliminarily diluted with a special injection liquid of sterile nature (5 ml per 0.25 g of meropenem) in order to obtain a concentration of the substance that is 50 mg / ml.

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

The following infusion fluids are suitable for breeding Mezonex:

• 0.9% infusion NaCl;
• 5% or 10% glucose fluid;
• 5% glucose fluid along with 0.02% sodium bicarbonate;
• 0.9% NaCl with 5% glucose fluid;
• 5% glucose fluid with 0.225% NaCl;
• 5% glucose fluid along with 0.15% potassium chloride infusion;
• 2.5%, as well as a 10% mannitol solution for intravenous injection.

The drug inside such a liquid dissolves fully, without forming a precipitate.

Dosing portions and duration of the treatment cycle for adults are selected, taking into account the human condition and the type of severity of the lesion.

Among the recommended daily portions of drugs:

• accompanied by complications of the urinary system - 0.5 g with an 8-hour interval;
• lesions of the epidermis with a subcutaneous layer (with or without complications) - 0.5 g with an 8-hour interval;
• gynecological infections (among them pelvic organs lesions) - 0.5 g of substance with an 8-hour interval;
• lesions of the lower region of the respiratory ducts - 0.5 g with an 8-hour interval (with nosocomial pneumonia, the dosage is 1 g);
• lesions of the abdominal zone (with complications) or septicemia - 1 g of the drug with preservation of the 8-hour interval;
• meningitis - 2 g of the drug with preservation of the 8-hour interval.

People with renal failure.

In persons with a QC level below 51 ml / min, the size of the portions is reduced in this way:

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

Mezonex can be excreted during hemodialysis. If necessary, prolonged use of the medication should be 1-fold portion (selected, taking into account the intensity and form of the developed lesion) to apply after completion of the hemodialysis session - to restore therapeutically effective plasma levels of drugs.

Experience with the use of drugs in individuals receiving peritoneal dialysis, absent.

Use in the elderly.

Elderly persons with problems in the kidney activity or QC numbers above 51 ml / min need to adjust the dosage of the drug.

The mode of use and dosage in children.

Children up to the age of 12 are required to inject 10–20 mg / kg of a pharmaceutical element with 8-hour sections (given the complexity of the lesion and the condition of the child, and with it its sensitivity regarding pathogenic microbes).

Recommended daily dosage of the drug:

• lesions of the urinary system, occurring with complications - 10 mg / kg with an 8-hour time period;
• lesions of the subcutaneous tissue and the epidermis (without complications) or the lower region of the respiratory system (pneumonia) - 10-20 mg / kg component with 8-hour lengths;
• infections of the intra-abdominal zone (with complications) - 20 mg / kg of the drug with intervals lasting 8 hours;
• meningitis - 40 mg / kg of the drug (the intervals are 8 hours).

Children weighing more than 50 kg are required to prescribe adult portion doses.

[5]

Use The mausoleum during pregnancy

There is no information regarding the safety of introducing Mezoneks during pregnancy. Animal tests have shown that no adverse effects on the fetus develop. The drug is prescribed to pregnant women, as long as the benefits of it are more likely than the risk of negative consequences for the fetus. Use the medication only under constant medical supervision.

Inside milk in animals there are only extremely low rates of medication. Assign it to lactating women is allowed only in cases where the benefits of its use are higher than the risk to the infant. It is recommended to refuse breastfeeding during therapy.

Contraindications

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

Side effects The mausoleum

Among the side effects:

• local manifestations after i / v injection: throbophlebitis, inflammation or pain;
• lesions of the epidermis: itching, rash, or urticaria;
• disorders affecting the gastrointestinal tract: nausea, hepatitis, abdominal pain, diarrhea and vomiting;
• disorders of the blood system: curable thrombocythemia, and in addition, neutropenia or thrombocythemia with eosinophilia. Individual patients may develop a direct or indirect positive Coombs test response. There are reports of a partial reduction in the formation of thromboplastin;
• problems with the activity of the liver: a treatable increase in serum values of bilirubin, alkaline phosphatase, transaminases, as well as milk dehydrogenase;
• lesions affecting the cardiovascular system: bradycardia, HF, myocardial infarction, tachycardia or pulmonary embolism;
• disorders of the central nervous system: paresthesia, convulsions, along with severe headaches, depression and a feeling of excitement;
• renal impairment: hematuria or dysuria;
• Other manifestations: thrush or oral candidiasis.

[4]

Overdose

Mezonex poisoning often develops in individuals with problems related to renal function. Among the manifestations - dyspnea, ataxia and convulsions.

In case of overdose, symptomatic measures are taken. In people with impaired renal activity, hemodialysis can excrete meropenem with its metabolic elements.

Interactions with other drugs

It is necessary to administer the drug very carefully in combination with medicines that have potential nephrotoxicity.

Probenecid acts as a competitor to the element meropenem in relation to tubular excretion, as a result of which it enhances the excretion through the kidneys, at the same time prolonging the half-life of the substance and increasing its plasma elevations. Because the intensity and duration of the drug effect exerted by Mezonex, dosed without the use of probenecid, are similar, these medicinal substances should not be combined.

The drug reduces serum markers of valproic acid.

The drug is allowed to mix with solutions that contain other medicinal substances.

[6], [7]

Storage conditions

Mezonex in the form of a dry lyophilisate must be kept in a place completely closed to small children. Temperature marks are not higher than 25 ° С.

Shelf life

Mezonex can be administered for a 24-month period from the time the therapeutic agent is manufactured.

Application for children

Do not assign to infants up to 3 months of age.

Analogs

Analogues of the drug are the substances Demopenem, Meronem, Romain with Europenem, Merocef with Invanz and Meropenem with Inemplus. In addition, Sinerpen, Lastin, Meromak with Mepenam, Prep, with Merobocid, Tien, and Meromek with Ronem and Merospin.