Cefoperabol

Cefoperabol is a third-generation cephalosporin.

Indications Cefoperabola

It is used for treatment in the following situations:

• infectious diseases affecting the gallbladder (such as cholangitis with cholecystitis and empyema in the gallbladder area);
• sepsis or peritonitis;
• neutropenic fever;
• infectious lesions in the urogenital system, which are severe;
• pneumonia (caused by the activity of gram-negative bacteria);
• infections developing in the pelvic organs (pelvic peritonitis or endometritis), as well as gonorrhea;
• nosocomial infectious processes with various locations;
• infections that affect people with immunodeficiency.

It is also used for the treatment or prevention of infections that may occur as a result of operations (gynecology and obstetrics, proctology, and the abdominal area).

Release form

The drug is released in the form of a lyophilisate for the manufacture of solutions administered intramuscularly or intravenously. The volume of 1 bottle is 0.5, 1 or 2 g. The kit also contains a solvent (5 ml capacity). Inside the box - 1 or 5 bottles.

Pharmacodynamics

Cefoperabol has a bactericidal and antibacterial effect with a wide range of activity.

Slows down the binding of peptide glycan inside the walls of bacteria. Has activity against a relatively large number of gram-negative aerobes (including hemophilic or pseudomonas aeruginosa, as well as other non-fermenting microbes and microorganisms from the intestinal group), as well as many anaerobes.

The degree of activity against gram-positive microflora (streptococci with staphylococci) is lower than that of cefotaxime or ceftriaxone. The drug demonstrates activity against some enterococcal strains (faecal or faecium).

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Pharmacokinetics

After intramuscular or intravenous use, the Cmax value is noted after 1 hour. The drug penetrates almost all tissues with organs and body fluids; penetrates the BBB (but the degree of this penetration is weaker than that of ceftazidime and ceftriaxone). A very small amount of the drug is excreted with breast milk.

In high medicinal concentrations it is registered for 12 hours after the injection. The medicine does not remove bilirubin from synthesis with plasma protein.

Excretion occurs to a greater extent with bile (approximately 70-80% of the dosage; the drug levels in bile reach their maximum after 1-2 hours after use, and also have a level exceeding blood values by 100 times), and also with urine (approximately 20-30%). The half-life is 2.5 hours (the method of drug administration does not matter).

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Dosing and administration

The medication should be administered intravenously (at a slow speed, by jet (over 5 minutes), or through a dropper (over 0.5-1 hour)), as well as intramuscularly.

For intravenous jet injection, 1000 mg of the substance must be dissolved in 10 ml of injection water (or sterile NaCl isotonic solution). When used through a dropper, 1000-2000 mg of the drug is diluted in 0.1 l of NaCl solution.

For intramuscular injections, the medication is dissolved in injection water or 0.5% lidocaine solution (for 1000 mg of the drug, 3 ml of liquid is required).

Teenagers aged 12 and over, and adults in addition, are required to administer 1-2 g of the drug 2 times a day. If the infection is severe, a single dose can be increased to 4 g (administered through a dropper). An adult is allowed to administer no more than 12 g of the drug per day.

Uncomplicated gonorrhea: 1-time intramuscular injection of 0.5 g of the substance.

Prevention of complications after surgery: jet intravenous administration of 1-2 g of the drug 0.5-1.5 hours before surgery, and later administered at 12-hour intervals, but often a maximum of 24 hours (for procedures in the cardiovascular system or in proctology - up to 72 hours after its completion). If surgery is performed on the rectum or colon, metronidazole can be additionally used (via a drip, intravenously).

Newborns and children under 12 years of age require an average dose of 0.05-0.1 g/kg per day, divided into 2 injections. Doses over 0.1 mg/kg are often administered intravenously via a drip. Children with severe infections require 0.2-0.3 g/kg per day, divided into 2-3 injections. The drug can be prescribed to infants under 3 months of age only if there are strict indications.

If the CC values are less than 18 ml/minute, the daily dose can be up to 4000 mg.

In case of obstruction of the biliary tract, severe liver pathology and simultaneous presence of kidney disorders, a maximum of 2000 mg of the drug per day is allowed.

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Use Cefoperabola during pregnancy

Should not be prescribed to pregnant women. Should be used with extreme caution during lactation.

Contraindications

Contraindicated for use in case of intolerance to the drug or in case of severe liver failure.

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Side effects Cefoperabola

The introduction of a medicinal product may cause the occurrence of side effects:

• lesions affecting the gastrointestinal tract: vomiting or nausea, as well as diarrhea (in case of severe diarrhea, it is necessary to immediately stop using the drug) and a temporary increase in alkaline phosphatase and transaminase levels;
• allergy symptoms: rash, eosinophilia, urticaria, and fever;
• others: neutropenia, and also vitamin K deficiency or hypothrombinemia (bleeding may occur in people with liver pathologies or intestinal absorption disorders and those on parenteral nutrition – it is necessary to monitor the PT values);
• local signs: phlebitis (after intravenous injection) or pain in the injection area (after intramuscular injection).

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Overdose

Overdose may cause an epileptic seizure.

Its treatment requires sedative procedures using diazepam.

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Interactions with other drugs

The drug potentiates the effect of anticoagulants.

The combination of Cefoperabol with agents that weaken platelet aggregation (salicylates or NSAIDs) leads to an increased risk of bleeding.

The use of ethyl alcohol in combination with the drug may cause the development of an antabuse-like syndrome.

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Storage conditions

Cefoperabol should be stored in a dark, dry place out of reach of children. Temperature indicators are a maximum of 25°C.

Shelf life

Cefoperabol can be used within 24 months from the date of production of the therapeutic agent. The finished drug has a shelf life of 24 hours (at a temperature of 5-25 ° C) or 5 days (temperature indicators - within 2-5 ° C).

Analogues

Analogues of the drug are the medications Cefoperus, Dardum, Operaz with Lorizone, as well as Cefpar, Medocef, Cefobid with Cefapison, Cefoperazone with Movoperiz, as well as Cefoperazone-Vial and Cefoperazone-Adgio.