Cefoperazone

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

[1], [2], [3], [4], [5]

Indications Cefoperazone

It is used for the treatment of infections, whose development is caused by the activity of Pseudomonas aeruginosa, streptococci, Proteus and Influenza sticks, as well as gonococci, Escherichia coli, Staphylococcus aureus with enterobacteria and Klebsiell. Among these diseases are:

• bacterial genesis septicemia;
• infections in the female genital area;
• affecting respiratory duct infections;
• inflammation affecting the pelvic organs;
• enterococcal infections associated with polymicrobial infection;
• epidermal infections;
• lesions in the peritoneum;
• infectious infections in the area of the urinary ducts caused by the activity of intestinal 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.

[6], [7]

Release form

The release of funds is implemented in the form of a lyophilisate for injection fluid (intramuscular or intravenous administration). The volume of the bottle - 1000 mg. Inside the box - 10 of these flakonchikov.

[8], [9], [10], [11], [12],

Pharmacodynamics

Cefoperazone is a bactericidal drug whose effect is due to the suppression of the binding processes of the cell membranes of microbes. It exerts an acetylating effect on membrane-bound transpeptidases, preventing cross-linking of the peptidoglycans necessary to strengthen the membrane wall.

The drug has an effect on anaerobes and aerobes, as well as Pseudomuscular bacilli. It is resistant to many β-lactamase.

[13], [14]

Pharmacokinetics

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

The excretion of the drug is carried out with bile. During the day, 30% of the used portion is excreted unchanged with the urine.

[15], [16], [17], [18], [19], [20]

Dosing and administration

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

It is necessary to prepare injection solutions from a lyophilisate immediately before the injection.

The size of an adult portion per day is 2000-3000 mg. Distribute this dosage into several parts. Injections should be administered at approximately 12-hour intervals. If a severe degree of infection is noted, the portion can be increased to 8000 mg per day (it is also distributed to several separate injections with a 12-hour interval).

For the treatment of urethritis of gonococcal nature, occurring without complications, it is necessary to administer 0.5 g of the drug in a / m method, 1-fold.

Prevention of bacterial infection after surgical procedures is performed by administering a portion of 1000-2000 mg of drugs - it is used 30-90 minutes before the operation. This portion is allowed to be repeated at 12-hour intervals, but usually a maximum during the day. With an increased risk of infection or a high probability of causing excessively strong harm (for example, if the procedure is performed on an open heart), medication is allowed for a maximum of 3 days after the surgical procedure.

Children need to enter portions that make up 50-200 mg / kg (maximum 12 g per day). For newborns, the dosage is not more than 0.3 g / kg. The daily portion is divided into 2 administrations, and injections should be given at 12-hour intervals.

If a patient has a disorder in the work of the kidneys and liver, he is allowed to inject no more than 2000 mg of substance per day.

If only disturbance of renal activity is observed, the dosage may remain unchanged. Patients who are on hemodialysis, the drug should be administered after the procedure.

It is necessary to inject the medication intramuscularly into the region of the big muscle of the buttock or into the anterior thigh.

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

In the case of continuous infusion, each gram of Cefoperazone should be diluted in sterile liquid (5 ml). Next, this liquid is added to the solvent for IV injection.

The size of the maximum single adult dose (IV injection) is 2000 mg. For children, the dose is a maximum of 50 mg / kg. The drug is diluted in a solvent until it reaches a concentration of 0.1 g / ml. It is necessary to enter substance approximately 4 minutes.

To make an 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 solutions of Normosol type M and R). Mix the lyophilisate is necessary in the ratio of 2.8-5 ml / g of the drug. Next, this liquid is diluted using a solvent (in the volumes required for the manufacture of infusion).

For the manufacture of intramuscular solution is allowed to use injectable water. Under the assumption that the concentration of the substance will be more than 250 mg / ml, it is recommended to use a 0.5% lidocaine solution. In this case, injectable water is mixed with a 2% lidocaine solution.

[28], [29], [30], [31]

Use Cefoperazone during pregnancy

It is forbidden to prescribe medication during pregnancy.

Contraindications

Main contraindications:

• renal failure;
• lactation period;
• intolerance against cephalosporins, as well as other β-lactam antibiotics.

[21], [22], [23]

Side effects Cefoperazone

The use of a medicinal product may cause the following side effects:

• lesions affecting the liver with the digestive tract: diarrhea, vomiting, pseudomembranous colitis, hepatitis, nausea, and in addition cholestatic jaundice and transient enhancement of liver transaminase activity;
• hematopoietic dysfunction: changes in the activity of peripheral blood flow (if the drug is used in large portions for a long time);
• urinary disorders: tubulointerstitial nephritis;
• local symptoms: phlebitis (with intravenous injections) or pain in the injection area (with intramuscular injection);
• signs of allergies: eosinophilia, rash or itching;
• disorders of blood coagulation: the development of hypoprothrombinemia.

Chemotherapeutic effect may provoke the development of candidiasis. Occasionally the use of drugs leads to the appearance of angioedema.

[24], [25], [26], [27]

Overdose

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

In case of overdose, you should immediately stop the introduction of the drug and seek help from doctors. The active component of cefoperazone is excreted during hemodialysis procedures.

[32], [33], [34],

Interactions with other drugs

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

The drug should not be combined with alcoholic beverages and drugs that contain alcohol. After completing 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 sugar analysis can be observed when performing tests with Fehling or Benedict solutions.

[35], [36], [37], [38]

Storage conditions

Cefoperazone needs to be kept in a dark place, closed from access for young children. The temperature values are within 25 ° С.

[39], [40], [41],

Shelf life

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

[42], [43]

Analogs

Analogues of the drugs are Cefobid, Cefoperus, Cefpar with Movoperis and Dardum, and in addition, Medocef, Operaz, Cefoperazone Sodium with Ceperone J and Cefoperabol with Cefoperazone-Vial and Cefoperazon-Agio.

[44], [45], [46], [47], [48]

Reviews

Cefoperazone gets rather controversial reviews. Many patients note that the drug did not have the desired result. At the same time, there are almost no comments that speak of the development of negative symptoms. From the advantages of the medicine, it is distinguished by its low cost, as well as the absence of the need to adjust the portion in case of a disorder of renal function.