Cefoperabol

Cefoperabol is a third-generation cephalosporin.

Indications Cefoperabol

It is used for treatment in the following situations:

• infectious diseases affecting the GPD (such as cholangitis with cholecystitis and empyema in the gallbladder);
• sepsis or peritonitis;
• neutropenic fever;
• infectious lesions in the urogenital system, having a severe form;
• pneumonia (triggered by the activity of gram-negative bacteria);
• infections developing in the pelvic organs (pelvioperitonitis or endometritis), as well as gonorrhea;
• having a diverse location of nosocomial infectious processes;
• infections affecting people with immunodeficiency.

It is also used to treat or prevent infections that may occur as a result of operations (gynecology and obstetrics, coloproctology, and the abdominal area).

Release form

The release of the drug is in the form of a lyophilisate for the manufacture of intramuscularly or intravenously injected solutions. The volume of the 1st bottle - 0.5, 1 or 2 g. Also included is a solvent (capacity 5 ml). Inside the box - 1 or 5 bottles.

Pharmacodynamics

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

It slows down the binding of peptidoglycan inside the walls of bacteria. It has activity of a relatively large number of gram-negative aerobes (among them hemophilic or Pseudomonas aeruginosa, as well as other non-fermentative 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 exhibits activity against some enterococcal strains (fecal or fetium).

[1], [2], [3], [4], [5], [6]

Pharmacokinetics

After intramuscular or intravenous use, Cmax is noted after the expiration of the 1st hour. The drug passes into almost all tissues with organs and body fluids; penetrates the BBB (but the degree of this passage is weaker than that of ceftazidime and ceftriaxone). With mother's milk a very small amount of drugs is excreted.

In large drug concentrations recorded within 12 hours after the injection. The drug does not remove bilirubin from the synthesis with plasma protein.

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

[7], [8], [9], [10], [11], [12], [13], [14]

Dosing and administration

The medication should be injected intravenously (at a slow speed, jet (for 5 minutes), or through an IV (for 0.5-1 hour)), as well as intramuscularly.

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

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

Adolescents from 12 years old, and besides that, adults need to administer 1-2 g of drugs 2 times a day. If the infection is severe, a single dose can be increased to 4 g (administered through an IV line). An adult is allowed to enter no more than 12 g of medicine per day.

Gonorrhea without complications: 1 single intramuscular injection of 0.5 g of the substance.

Preventing the occurrence of complications after surgery: jet intravenous administration of 1-2 x g of the drug for 0.5-1.5 hours before the operation, and later administered at 12-hour intervals, but often a maximum of 24 hours (during the procedures in SSS areas or during coloproctology - up to 72 hours after its completion). If the operation is performed on the rectum or colon, metronidazole may additionally (via an IV drip) be used.

Newborn babies, as well as children under 12 years of age, require an average portion of 0.05-0.1 g / kg per day, and it should be divided into 2 injections. A dosage of more than 0.1 mg / kg is often administered intravenously via an IV. Children with severe stages of infection need to apply 0.2-0.3 g / kg per day, which is divided into 2-3 injections. Infants up to 3 months of age can be prescribed medication only if there are strict indications.

If the QC values are less than 18 ml / minute, the size of the daily portion may be a maximum of 4000 mg.

In the case of obstruction of the GWP, hepatic pathology in severe and with the simultaneous presence of disorders in the work of the kidneys, the use of a maximum of 2000 mg of drugs per day is allowed.

[20]

Use Cefoperabol during pregnancy

You can not assign pregnant. When lactating should be used very carefully.

Contraindications

It is contraindicated to use in case of intolerance with respect to the drug or in case of insufficiency of the hepatic function in the severe stage.

[15], [16], [17], [18]

Side effects Cefoperabol

The introduction of the drug can cause side effects:

• lesions affecting the gastrointestinal tract: vomiting or nausea, as well as diarrhea (with a severe degree of diarrhea, you must immediately cancel the use of drugs) and a temporary increase in alkaline phosphatase and transaminases;
• allergy symptoms: rash, eosinophilia, urticaria, and fever;
• others: neutropenia, and in addition, vitamin K deficiency or hypothrombinemia (possible bleeding in people with hepatic abnormalities or intestinal absorption disorder and being on parenteral nutrition - it is required to monitor PTV values);
• local signs: phlebitis (after intravenous injection) or pain in the injection area (after intramuscular injection).

[19]

Overdose

With an overdose, an epilepsy attack may occur.

Treatment requires sedation using diazepam.

[21]

Interactions with other drugs

The drug potentiates the effect of anticoagulants.

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

The use of ethyl alcohol in combination with the drug can cause antabus-like syndrome.

[22], [23]

Storage conditions

Cefoperabol required to keep in a closed from the access of children, dark and dry place. Temperature indications are maximum 25 ° C.

Shelf life

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

Analogs

Analogues of drugs are Cefoperus, Dardum, Operaz with Lorizon, and also Cefpar, Medocef, Cefobid with Cephapisone, Cefoperazone with Movoperis, as well as Cefoperazone-Vial and Cefoperazone-Agio.