Cefoperazone

Cefoperazone is an antibiotic with a wide spectrum of therapeutic activity.

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Indications Cefoperazone

It is used for the treatment of infections caused by the activity of Pseudomonas aeruginosa, Streptococcus, Proteus and Influenza bacilli, as well as gonococci, Escherichia coli, Staphylococcus aureus with Enterobacter and Klebsiella. Among these diseases:

• septicemia of bacterial origin;
• infections in the female genital area;
• infections affecting the respiratory tract;
• inflammation affecting the pelvic organs;
• enterococcal infections associated with polymicrobial infection;
• epidermal infections;
• lesions in the peritoneum;
• infectious infections in the urinary tract caused by the activity of Escherichia coli or Pseudomonas aeruginosa.

The antibiotic can also be used to prevent the development of complications due to surgical operations in the gynecological, orthopedic, abdominal or cardiovascular areas.

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Release form

The product is released in the form of a lyophilisate for injection liquid (intramuscular or intravenous administration). The volume of the bottle is 1000 mg. There are 10 such bottles inside the box.

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Pharmacodynamics

Cefoperazone is a bactericidal drug whose effect is due to the suppression of the processes of binding of microbial cell membranes. It has an acetylating effect on membrane-bound transpeptidases, preventing cross-linking of peptide glycans necessary for strengthening the membrane wall.

The drug has an effect on anaerobes and aerobes, as well as Pseudomonas aeruginosa. It has resistance to many β-lactamases.

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Pharmacokinetics

The degree of protein synthesis of the drug inside the plasma is approximately 85%. After penetrating the body, the substance is distributed inside the fluids with tissues. The Cmax level in bile is noted after 1-2 hours. The drug also passes through the placenta and is excreted with mother's milk.

The drug is excreted with bile. Over the course of a day, 30% of the used portion is excreted unchanged in the urine.

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Dosing and administration

The finished medicinal substance must be administered intramuscularly or intravenously. It is necessary to check the patient's sensitivity to lidocaine or antibiotic by performing a skin test.

Injection solutions from the lyophilisate must be prepared immediately before the injection.

The daily dose for adults is 2000-3000 mg. This dosage should be divided into several parts. Injections should be administered at approximately 12-hour intervals. If a severe infection is observed, the dose can be increased to 8000 mg per day (it is also divided into several separate injections at 12-hour intervals).

For the treatment of gonococcal urethritis without complications, 0.5 g of the drug must be administered intramuscularly, once.

Prevention of bacterial contamination after surgical procedures is carried out by administering a dose of 1000-2000 mg of the drug - it is used 30-90 minutes before the operation. This dose is allowed to be repeated at 12-hour intervals, but usually for a maximum of 24 hours. If the risk of infection is increased or there is a high probability of causing excessive harm (for example, if the procedure is performed on an open heart), the drug is allowed to be used for a maximum of 3 days after the surgical procedure.

Children should be administered doses of 50-200 mg/kg (maximum 12 g per day). For newborns, the dosage is no more than 0.3 g/kg. The daily dose is divided into 2 administrations, and injections should be administered at 12-hour intervals.

If the patient has kidney and liver problems, he is allowed to administer no more than 2000 mg of the substance per day.

If only renal function is impaired, the dosage may remain unchanged. For patients undergoing hemodialysis, the drug should be administered after the procedure.

The medication must be administered intramuscularly into the area of the large gluteal muscle or into the anterior thigh.

To perform an intermittent injection, dilute 1 vial of the substance in sterile liquid (20-100 ml). The amount of injection water used should be a maximum of 20 ml. The medicine is administered over 15-60 minutes.

In case of continuous infusion, each gram of Cefoperazone should be diluted in sterile liquid (5 ml). This liquid is then added to the solvent for intravenous injections.

The maximum single adult dose (IV injection) is 2000 mg. For children, the maximum dose is 50 mg/kg. The medication is diluted in a solvent until a concentration of 0.1 g/ml is reached. The substance should be administered over approximately 4 minutes.

To prepare a product for intravenous injection, the lyophilisate is diluted by mixing with a solvent (0.9% NaCl liquid, 5-10% glucose solution; in addition, a combination of 5% glucose solution with 0.2% and 0.9% NaCl substance or Normosol type M and R solutions can be used). The lyophilisate must be mixed in a ratio of 2.8-5 ml/g of medication. This liquid is then diluted using a solvent (in volumes required to prepare the infusion).

It is allowed to use injection water for the preparation of the intramuscular solution. If the concentration of the substance is expected to be more than 250 mg/ml, it is recommended to use 0.5% lidocaine solution. In this case, the injection water is mixed with 2% lidocaine solution.

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Use Cefoperazone during pregnancy

It is prohibited to prescribe the medication during pregnancy.

Contraindications

Main contraindications:

• renal failure;
• lactation period;
• intolerance to cephalosporins and other β-lactam antibiotics.

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Side effects Cefoperazone

The use of the drug may lead to the following side effects:

• lesions affecting the liver and gastrointestinal tract: diarrhea, vomiting, pseudomembranous colitis, hepatitis, nausea, as well as cholestatic jaundice and transient increase in the activity of liver transaminases;
• disorders of hematopoietic function: changes in the activity of peripheral blood flow (if the drug is used for a long time in large doses);
• urinary disorders: tubulointerstitial nephritis;
• local symptoms: phlebitis (with intravenous injections) or pain in the injection area (with intramuscular administration);
• signs of allergy: eosinophilia, rash or itching;
• disorders of blood coagulation processes: development of hypoprothrombinemia.

The chemotherapeutic effect can provoke the development of candidiasis. Occasionally, the use of drugs leads to the appearance of Quincke's edema.

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Overdose

In case of intoxication, potentiation of negative manifestations of the drug may occur. Due to high concentration of the drug in the cerebrospinal fluid, neurological signs may develop.

In case of overdose, stop the administration of the drug immediately and seek medical help. The active component of Cefoperazone is excreted during hemodialysis procedures.

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Interactions with other drugs

The drug slows down the processes of vitamin K binding. Because of this, when combined with drugs that reduce platelet aggregation, the risk of bleeding increases. At the same time, when combining drugs with anticoagulants, potentiation of the anticoagulant effect is possible.

The medicine is prohibited to be combined with alcoholic beverages and drugs that contain alcohol. After the last injection of Cefoperazone, you need to wait another 5 days (this is due to the fact that there is a high risk of developing disulfiram-like symptoms).

False positive results of urine tests for sugar may be observed when performing tests with Fehling's or Benedict's solutions.

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Storage conditions

Cefoperazone should be stored in a dark place, out of the reach of small children. Temperature values are within 25°C.

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Shelf life

Cefoperazone can be used for 24 months from the date of manufacture of the pharmaceutical product.

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Analogues

Analogues of the drug are Cefobid, Cefoperus, Cefpar with Movoperiz and Dardum, and in addition to this, Medocef, Operaz, Cefoperazone Sodium with Ceperone G and Cefoperabol with Cefoperazone-Vial and Cefoperazone-Adgio.

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Reviews

Cefoperazone receives quite contradictory reviews. Many patients note that the drug did not produce the desired result. At the same time, there are almost no comments that talk about the development of negative symptoms. The advantages of the drug include its low cost, as well as the lack of need to adjust the dose in case of renal dysfunction.