Zopperin

Zopercine is a tool containing penicillins in combination with substances that slow down the activity of β-lactamase. It has a large range of antimicrobial effects.

Indications Zopperin

It is used for such violations:

• lesions of the lower and upper parts of the respiratory ducts (among them, pneumonia (hospital, as well as VAP));
• infection of the urethra (for example, pyelonephritis);
• infections of the peritoneum (also with complications) - cholecystitis with peritonitis, as well as endometritis and inflammation in the pelvic organs (also in 2-12-year-old children);
• lesions of soft tissue bones, epidermis, and joints (this includes diabetic foot);
• bacteremia.

May be administered to children, as well as adults with a fever caused by neutropenia, which has developed in connection with an infection of bacterial etiology.

Release form

The release of the substance is realized in the form of a lyophilisate for injection liquids, inside the bottles with a capacity of 4.5 g.

Pharmacodynamics

This antimicrobial drug contains a complex of 2 components - piperacillin with tazobactam. Combines the parameters of the antibiotic and the agent that slows down the action of β-lactamase.

Piperacillin is a semi-artificial penicillin, which has a high therapeutic activity, inhibiting bacterial properties - slows the formation of cell membranes and the binding of cell membranes.

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

Pharmacokinetics

Suction.

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

Distribution processes.

Both piperacillin and tazobactam are involved in protein synthesis. Its figures are about 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 drug values are generally 50-100% compared to plasma levels.

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

Metabolic processes.

In case of metabolism, piperacillin is converted to dezethyl metabolic product, which has a weak microbiological effect. The metabolism of tazobactam leads to the formation of a single metabolic product that does not have microbiological activity.

Excretion.

With 1-time or reusable use of the drug in volunteers, the half-life was 0.7-1.2 hours. The batch size and duration of infusion do not affect these values. The half-life of both components increased with decreasing renal clearance.

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

Substances are excreted through the kidneys by tubule secretion and filtration of the glomeruli. Piperacillin has fast excretion, because it is a non-exchanging component (68% is excreted in the urine). In this case, tazobactam with its metabolic products - through the kidneys by 80%.

Dosing and administration

The drug should be administered intravenously, in the form of an infusion procedure that lasts 20-30 minutes.

The duration of therapy and the size of the portion are selected by the attending doctor, taking into account the patient's condition and the severity of the lesion.

The standard adult portion (adolescents older than 12 years of age and people weighing more than 50 kg) with conditions provoked by acute lesions (accompanied by complications) can fluctuate from 4.5 g in total for 1 well infusion (the procedure is performed 3 times per day). In the case of neutropenia, the drug is administered 4 times per day (with 6-hour intervals).

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

Children in the range of 2-12 years of age and weighing less than 50 kg in the case of neutropenia, the portion is calculated in a ratio of up to 90 mg / kg (in total); It must be administered at 6-hour intervals, combined with amine glycosides (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 Zopperin during pregnancy

Zopercine 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 exclusively in situations where the potential benefits of administering are more expected than the likelihood of any complications.

The drug is excreted in breast milk, which should stop breastfeeding during therapy.

Contraindications

It is contraindicated to use in case of intolerance against cephalosporins, penicillins, as well as substances that slow down the action of β-lactamase.

Side effects Zopperin

Often, patients have the following negative symptoms:

• gastrointestinal dysfunction: anorexia, vomiting, bloating, diarrhea, or diarrhea;
• signs of allergy: eczema, dyspnea, rash, anaphylaxis, runny nose or urticaria;
• platelet, neutro or leukopenia, and anemia of a hemolytic nature;
• 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.

[1]

Overdose

Zopercine poisoning can trigger the potentiation of negative symptoms (for example, seizures).

Symptomatic interventions should be performed (to remove cramps, use barbiturates or diazepam), 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 level of kidney clearance of both components of Zopercin. But this fact has no effect on the plasma values of Cmax of one of the medicines.

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

Use together with anticoagulants for oral administration, heparin and other drugs that can affect the blood-clotting system (for example, platelet activity), should occur while constantly monitoring the coagulation test data.

Piperacillin in combination with vecuronium causes prolongation of the blockade of muscle and nerve activity. Due to a similar effect principle, it can be expected that the neuromuscular blockade provoked by any non-polarizing muscle relaxant can last when using piperacillin. This should be taken into account when Zophercin is prescribed during operations.

Piperacillin is able to reduce the excretion of methotrexate, so for individuals who use methotrexate, it is necessary to monitor its serum indicators.

Impact on laboratory test results.

As with the use of other penicillins, with the introduction of the drug may develop a false positive response to the presence of glucose inside the urine (when this is determined using the reduction method). Testing for the presence of sugars that work by using enzymatic glucose oxidase reactions should be carried out.

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Storage conditions

Zopercin must be maintained at temperatures not exceeding 25 ° C. The finished liquid can be used within a 24-hour (if it is contained at rates up to 25 ° C) or a 48-hour gap (if the drug is kept in a refrigerator with indicators 2-8 ° C).

Shelf life

Zopercin can be used within a 2-year period from the time the therapeutic product is manufactured.

Application for children

Cannot be used in infants younger than 2 years of age.

Analogs

Analogues of the medication are Aurotaz-P, Tazar with Piperacillin-Tazobaktam Teva, and Tazpen.