Merexid

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

Indications Merexid

It is used to treat infections associated with bacteria showing high sensitivity to meropenem. Among such diseases:

• lesions of the lower part of the respiratory tract ( cystic fibrosis , chronic infections and pneumonia (also nosocomial)) or pulmonary inflammation;
• urogenital infections and pathologies affecting the urethra;
• lesions in the abdomen;
• infections of a gynecological nature (including endometritis and complications that develop after childbirth);
• disorders affecting subcutaneous tissues and epidermis;
• septicemia or meningitis of bacterial etiology.

Release form

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

Pharmacodynamics

The very strong bactericidal effect of a relatively wide range of anaerobes with aerobes, which Merexid provides, develops due to several factors:

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

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

Meropenem is highly effective against different strains of streptococci and enterococci with staphylococci, as well as listeria, rhodococci, lactobacilli and corynebacteria, salmonella, acyentobacteria with haemophilus influenzae, shigella, peptostreptococci with helicobacteria and the rest, clobostasis.

Pharmacokinetics

The introduction of a single serving of the drug to volunteers through a half-hour infusion led to the development of a Cmax index of about 11 μg / ml (when using a dosage of 0.25 g), 23 μg / ml (0.5 g portion) and 49 ti μg / ml (dosage 1 g).

But the proportionality of pharmacokinetics between the dosage used and the Cmax values with AUC is not observed. In addition, with the introduction of portions in the range of 0.25-2 g, the clearance level decreased from 287 to 205 ml / mm.

The administration of bolus injections to volunteers after 5 minutes formed plasma Cmax values of approximately 52 μg / ml (0.5 g portion) and 112 μg / ml (1 g portion).

A 3-sided cross-over test was performed with the introduction of IV infusions (dosage 1 g), lasting 2, 3, and 5 minutes. The indices of intraplasma Cmax in these cases were equal to 110, 91 and 94 μg / ml, respectively.

When using a 0.5 g portion, plasma values of meropenem decrease to 1 μg / ml or lower after 6 hours from the moment of infusion.

In individuals with healthy renal function, repeated administration of drugs with an 8-hour interval does not lead to the cumulation of meropenem.

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

Protein synthesis of meropenem - about 2%.

About 70% of the applied dosage is excreted unchanged along with the urine (over a period of 12 hours), and then an insignificant excretion occurs in this way. The values of meropenem inside urine, which are more than 10 μg / ml, remain at this level for up to 5 hours if a dosage of 0.5 g is used. With an 8-hour break or 1 g portions with a 6-hour interval were not observed.

The only metabolic component of Merexidum has no microbiological activity.

The substance passes without complications into fluids with tissues (also into the cerebrospinal fluid in persons with meningitis of a bacterial nature), reaching a level that exceeds the values 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 course of the disease and the patient's well-being.

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

Dosage sizes for different diseases:

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

In case of problems with renal function, it is necessary to reduce the dosage of drugs.

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

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

Do not mix the drug with other medicines inside the same bottle.

Shake the finished medicinal liquid before administration.

• Application for children

You can use Merexid in people over 3 years old. It is forbidden to prescribe the medicine to children who have insufficient hepatic / renal function.

Use Merexid during pregnancy

The medication can be used during pregnancy only in case of vital indications, after a careful assessment of the therapeutic benefits and possible risks.

For the period of treatment, it is necessary to stop breastfeeding.

Contraindications

It is contraindicated to use in the presence of allergies in relation to any of the elements of the medication (also excipients).

Side effects Merexid

Among the side effects:

• paresthesias, headaches or convulsions;
• pain in the peritoneal area, diarrhea, vomiting, pseudomembranous colitis and nausea;
• a temporary increase in serum values of LDH, transaminases, bilirubin and alkaline phosphatase;
• signs of anaphylaxis and Quincke's edema;
• itching, erythema polyformis, 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 Merexid, the potentiation of negative manifestations is observed. Typically, these problems occur in people with renal dysfunction.

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

Interactions with other drugs

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

Probenecid is a competitor to meropenem with respect to tubular excretion, therefore, it inhibits the processes of excretion through the kidneys, which is why the term half-life is prolonged and the plasma level of Merexide increases. Prescribing these drugs in combination is prohibited.

Meropenem is able to reduce the intraserum values of valproic acid. In some individuals, they can reach the subtherapeutic level.

Storage conditions

Merexid is prohibited from freezing. Temperature indicators - no more than 25 ° С.

Shelf life

Merexide can be used within 24 months from the date of manufacture of the medicinal substance.

Analogs

The analogues of the medication are the drugs Meropenem, Meronoxol with Mepenem, Nerinam and Meronem, and in addition Meropidel, Cyronem with Dzhenem, Propinem and Meropenabol with Penemera.