Merexide

Merexide is a drug from the subgroup of β-lactam antibiotics – antimicrobial substances that are intended for systemic use.

The active element of the drug is meropenem. It has very strong bactericidal activity against a large number of pathogenic bacteria. The high therapeutic effectiveness of the drug is ensured by its ability to very quickly and easily pass through membranes into microbial cells. [ 1 ]

Indications Merexide

It is used for the treatment of infections associated with bacteria that demonstrate high sensitivity to meropenem. Among such diseases are:

• lower respiratory tract lesions ( cystic fibrosis, chronic infections and pneumonia (also nosocomial)) or pulmonary inflammation;
• urogenital infections and pathologies affecting the urinary tract;
• lesions in the abdominal area;
• gynecological infections (including endometritis and complications developing after childbirth);
• disorders affecting subcutaneous tissues and epidermis;
• septicemia or meningitis of bacterial etiology.

Release form

The drug is released in the form of powder for the preparation of injection liquid - 0.5 or 1 g of meropenem.

Pharmacodynamics

The very strong bactericidal effect of Merexid on a relatively wide range of anaerobes and aerobes is due to several factors:

• high resistance against most β-lactamases;
• ease of passage through microbial membranes;
• strong affinity for penicillin-synthesizing proteins.

In addition, the drug demonstrates high efficiency against gram-negative and -positive microbial strains. [ 2 ]

Meropenem is highly effective against various strains of streptococci and enterococci with staphylococci, as well as listeria, rhodococci, lacto- and corynebacteria, salmonella, acienobacteria with hemophilic rods, shigella, peptostreptococci with helicobacter, clostridia and other anaerobes with aerobes.

Pharmacokinetics

The administration of a single dose of the drug to volunteers via a half-hour infusion resulted in the development of a Cmax value equal to approximately 11 mcg/ml (using a dosage of 0.25 g), 23 mcg/ml (0.5 g dose) and 49 mcg/ml (1 g dose).

However, proportionality of pharmacokinetics between the dosage used and the Cmax and AUC values is not observed. In addition, when administering portions in the range of 0.25-2 g, there was a decrease in the clearance level from 287 to 205 ml/mm.

Administration of bolus injections to volunteers over 5 minutes produced plasma Cmax values of approximately 52 μg/mL (0.5 g dose) and 112 μg/mL (1 g dose).

A 3-way crossover test was performed with intravenous infusions (1 g dose) lasting 2, 3, and 5 minutes. The intraplasma Cmax values in these cases were 110, 91, and 94 μg/mL, respectively.

When using a 0.5 g dose, plasma meropenem values decrease to 1 mcg/mL or less within 6 hours after the infusion.

In individuals with healthy renal function, multiple administration of the drug with an 8-hour interval does not lead to accumulation of meropenem.

The half-life of the substance in people with healthy renal function is approximately 1 hour.

Protein synthesis of meropenem is approximately 2%.

About 70% of the applied dose is excreted unchanged with urine (over a period of 12 hours), and then this route is followed by insignificant excretion. The values of meropenem in urine, which are more than 10 mcg/ml, remain at this level for up to 5 hours in the case of using a dose of 0.5 g. No accumulation of the drug in urine or plasma with healthy renal function was observed in the case of using a 0.5 g portion with an 8-hour break or a 1 g portion with a 6-hour interval.

The only metabolic component of Merexid does not have microbiological activity.

The substance passes into tissue fluids without complications (also into the cerebrospinal fluid in individuals with bacterial meningitis), reaching levels that exceed those required to slow down the activity of most microbes.

Dosing and administration

The duration of the therapeutic cycle and the size of the dosage portions are selected by the attending physician, who takes into account the nature of the disease and the patient's well-being.

The medication is administered by intravenous injection (at least 5 minutes) or intravenous infusion (within 15-30 minutes). An 8-hour interval should be observed between procedures.

Dosage sizes for different diseases:

• infections and diseases of moderate severity (urogenital infections, pneumonia or endometritis) - 0.5 g;
• pathologies and lesions of severe intensity (peritonitis, nosocomial pneumonia or septicemia) – 1 g of substance;
• cystic fibrosis - 2 g of medicine;
• neutropenic fever – 1 g of medication;
• meningitis – 2 g Merexide.

In case of problems with kidney function, it is necessary to reduce the dosage of the drug.

The portion size for a child weighing less than 50 kg is selected based on 25-40 mg/kg. In addition, the patient's condition and the type of infection are taken into account.

To dissolve the medicine, NaCl, mannitol, glucose, bicarbonate, and potassium chloride are used.

The drug must not be mixed with other medications in the same bottle.

Before administration, the prepared medicinal liquid must be shaken.

• Application for children

Merexid can be used in persons over 3 years of age. It is prohibited to prescribe the drug to children with liver/renal insufficiency.

Use Merexide during pregnancy

The medication may be used during pregnancy only in cases of vital indications, after a thorough assessment of the therapeutic benefits and possible risks.

During the treatment period, you must stop breastfeeding.

Contraindications

Contraindicated for use in the presence of an allergy to any of the components of the drug (including excipients).

Side effects Merexide

Side effects include:

• paresthesia, headaches or convulsions;
• pain in the peritoneum, diarrhea, vomiting, pseudomembranous colitis and nausea;
• temporary increase in serum levels of LDH, transaminases, bilirubin and alkaline phosphatase;
• signs of anaphylaxis and Quincke's edema;
• itching, erythema multiforme, rashes, urticaria of allergic origin, TEN and SJS;
• pain or inflammation in the form of thrombophlebitis or phlebitis at the injection site;
• vaginal or oral candidiasis.

Overdose

In case of poisoning with Merexide, potentiation of negative manifestations is observed. Usually such problems are observed in people with renal dysfunctions.

Symptomatic procedures are required. Hemodialysis can be used to excrete excess medication.

Interactions with other drugs

It is necessary to be extremely careful when combining the drug with substances that can potentially have a toxic effect on the kidneys.

Probenecid is a competitor of meropenem with respect to tubular excretion, therefore it inhibits renal excretion processes, which results in prolongation of the half-life and an increase in the plasma level of Merexide. It is prohibited to prescribe these drugs in combination.

Meropenem can reduce intra-serum levels of valproic acid. In some individuals, they can reach subtherapeutic levels.

Storage conditions

Merexid is prohibited from freezing. Temperature indicators are no more than 25°C.

Shelf life

Merexide can be used for a period of 24 months from the date of manufacture of the medicinal substance.

Analogues

The analogs of the drug are Meropenem, Meronoxol with Mepenem, Nerinam and Meronem, as well as Meropidel, Sayronem with Genem, Propinem and Meropenabol with Penemera.