Zopercin

Zopercin is a drug containing penicillins in combination with substances that inhibit the activity of β-lactamases. It has a wide range of antimicrobial effects.

Indications Zopercina

It is used for the following disorders:

• lesions of the lower and upper parts of the respiratory tract (including pneumonia (hospital-acquired pneumonia, as well as VAP));
• infections of the urethra (eg, pyelonephritis);
• infections affecting the peritoneum (also with complications) – cholecystitis with peritonitis, as well as endometritis and inflammation in the pelvic area (also in 2-12 year old children);
• lesions of bones with soft tissues, epidermis and joints (this includes diabetic foot);
• bacteremia.

It can be prescribed to children, as well as adults with fever caused by neutropenia that developed in connection with an infection of bacterial etiology.

Release form

The substance is released in the form of a lyophilisate for injection liquids, inside 4.5 g vials.

Pharmacodynamics

This antimicrobial drug contains a complex of 2 components - piperacillin with tazobactam. It combines the parameters of an antibiotic and a β-lactamase inhibitor.

Piperacillin is a semi-artificial penicillin that has high therapeutic activity, suppressing bacterial properties - slowing down the formation of cell membranes and the binding of cell membranes.

Tazobactam is a derivative of triazolylmethylpenicillanic acid. It inhibits the activity of β-lactamases, and at the same time expands the range of piperacillin activity and potentiates its effect on strains that are resistant to cephalosporins and penicillins.

Pharmacokinetics

Suction.

The administered drug almost immediately reaches plasma Cmax values. When using 4 g of piperacillin, its values are equal to 298 mcg/ml. The use of 0.5 g of tazobactam creates a Cmax value in plasma equal to 34 mcg/ml.

Distribution processes.

Both piperacillin and tazobactam participate in protein synthesis. Its rates are approximately 30%.

These components are rapidly distributed within the female reproductive system (ovaries with uterus and fallopian tubes), lungs, bile with gall bladder, intestinal mucosa and intercellular fluid. Tissue values of LS are generally 50-100% compared to plasma levels.

The distribution volume of the cerebrospinal fluid elements inside the cerebrospinal fluid is low (provided there is no inflammation of the meninges).

Metabolic processes.

During metabolism, piperacillin is converted into a desethyl metabolic product with a weak microbiological effect. Metabolic processes of tazobactam lead to the formation of a single metabolic product that does not have microbiological activity.

Excretion.

With single or multiple use of the drug in volunteers, the half-life was 0.7-1.2 hours. The dose size and duration of infusion do not affect these values. The half-life of both components increased with a decrease in renal clearance.

The use of tazobactam did not significantly affect the pharmacokinetic parameters of piperacillin, and it did not reduce the excretion rate of tazobactam.

Substances are excreted through the kidneys via tubular secretion and glomerular filtration. Piperacillin has rapid excretion because it is a non-exchangeable component (68% excreted in urine). At the same time, tazobactam with its metabolic products is excreted through the kidneys by 80%.

Dosing and administration

The medication should be administered intravenously, in the form of an infusion procedure lasting 20-30 minutes.

The duration of therapy and the dose size are selected by the attending physician, taking into account the patient’s condition and the severity of the lesion.

The standard adult dose (teenagers over 12 years of age and people weighing over 50 kg) for conditions caused by acute lesions (accompanied by complications) may vary, starting from 4.5 g in total for 1 infusion (the procedure is performed 3 times a day). In case of neutropenia, the drug is administered 4 times a day (with 6-hour intervals).

For elderly people, dosage adjustment is not necessary. In case of liver or kidney failure, the dose is changed taking into account the severity of the pathology (it can be reduced to 8 g of piperacillin per day).

For children aged 2-12 years and weighing less than 50 kg in case of neutropenia, the dose is calculated in a ratio of up to 90 mg/kg (in total); it should be administered at 6-hour intervals, combined with aminoglycosides (maximum 4.5 g in total; also with 6-hour breaks). In case of infections with complications, the dosage is increased to 112.5 mg/kg in total (maximum 4.5 g); the procedure is carried out at 8-hour intervals.

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Use Zopercina during pregnancy

Zopercin should not be prescribed to pregnant women, because there is no reliable information regarding the safety of its use. Therefore, it is allowed to be used only in situations where the possible benefit from the introduction is more expected than the likelihood of any complications.

The drug is excreted in breast milk, so breastfeeding should be discontinued during therapy.

Contraindications

Contraindicated for use in case of intolerance to cephalosporins, penicillins, and substances that inhibit the action of β-lactamases.

Side effects Zopercina

Patients often experience the following negative symptoms:

• gastrointestinal dysfunction: anorexia, vomiting, bloating, diarrhea or loose stools;
• signs of allergy: eczema, dyspnea, rash, anaphylaxis, runny nose or hives;
• thrombocyto-, neutro- or leukopenia, as well as hemolytic anemia;
• headaches, cramps, arrhythmia, dizziness, and in addition chills, severe fatigue and tachycardia;
• muscle weakness or arthralgia;
• candidiasis;
• manifestations in the injection area and a feeling of heat.

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Overdose

Poisoning with Zopercin may provoke a potentiation of negative symptoms (for example, seizures).

It is necessary to carry out symptomatic measures (to relieve convulsions, barbiturates or diazepam are used), as well as hemodialysis.

Interactions with other drugs

The combination of probenecid with the drug causes an extension of the half-life and a decrease in the renal clearance rate of both components of Zopercin. But this fact has no effect on the plasma Cmax values of one of the drugs.

Due to the lack of physical compatibility between aminoglycosides and β-lactam antibiotics in vitro, it is prohibited to mix the drug with aminoglycosides - these substances are administered separately (dilution and dissolution of both drugs also occurs separately).

Use together with oral anticoagulants, heparin and other drugs that can affect the blood coagulation system (for example, the functioning of platelets) should occur with constant monitoring of coagulation test data.

Piperacillin in combination with vecuronium causes prolongation of muscle and nerve block. Because of the similar principle of action, it can be expected that neuromuscular blockade induced by any non-polarizing muscle relaxant may be prolonged by piperacillin. This should be taken into account when prescribing Zopercin during surgery.

Piperacillin can reduce the excretion of methotrexate, so serum levels of methotrexate should be monitored in individuals using methotrexate.

Impact on laboratory test results.

As with other penicillins, a false-positive response to glucose in the urine (when determined using the reduction method) may occur when the drug is administered. Sugar tests that work by enzymatic glucose oxidase reactions should be used.

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Storage conditions

Zopercin should be stored at temperatures not exceeding 25°C. The prepared liquid can be used within a 24-hour period (if it is kept at temperatures up to 25°C) or a 48-hour period (if the drug is kept in a refrigerator at temperatures of 2-8°C).

Shelf life

Zopercin can be used within a 2-year period from the date of manufacture of the therapeutic product.

Application for children

Do not use in infants under 2 years of age.

Analogues

Analogues of the drug are Aurotaz-R, Tazar with Piperacillin-Tazobactam Teva, and Tazpen.