Cefoperazone, vial, 1g

Composition

1 fl. cefoperazone (in the form of sodium salt) 1 g

Pharmacological action

Semisynthetic cephalosporin antibiotic of the third generation for parenteral use only. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Cefoperazone is active in vitro against a large number of different clinically significant microorganisms. It is resistant to many beta-lactamases.

Active against gram-positive microorganisms:  Staphylococcus aureus (strains that produce and do not produce penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic streptococcus group A), Streptococcus agalactiae (beta-hemolytic streptococcus group B), Streptococcus Faecalis; gram-negative microorganisms:  Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia spp. (including Providencia rettgeri), Serratia spp. (including Serratia marcescens), Salmonella spp., Shigella spp., Pseudomonas spp. (including Pseudomonas aeruginosa), some strains of Acinetobacter spp., Neisseria gonorrhoeae (strains that produce and do not produce beta-lactamases), Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica; anaerobic microorganisms:  Gram-positive cocci (including Peptococcus spp., Peptostreptococcus spp. ), Clostridium spp., Eubacterium spp., Fusobacterium spp., Bacteroides fragilis, other strains of Bacteroides spp.

Indications

-Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

> bacterial infections of the upper and lower respiratory tract infections (including bronchitis, pneumonia, empyema and lung abscess);

> kidney infection and urinary tract infections (including pyelonephritis and cystitis);

> infection of the abdominal cavity (including peritonitis, cholecystitis, cholangitis);

> sepsis, meningitis;

> infections of skin and soft tissues;

> infections of bones and joints;

> infectious-inflammatory diseases of the pelvic organs (including endometritis, gonorrhea, and other infections of the genital tract).

– Prevention of infectious complications after abdominal, gynecological and orthopedic operations, as well as in cardiovascular surgery.

Contraindications

: hypersensitivity to cephalosporin and other beta-lactam antibiotics.

With caution:  renal and hepatic insufficiency, colitis in the anamnesis.

Side effects

Allergic reactions:  urticaria, pruritus of the skin, maculopapular rash, fever, eosinophilia, erythema multiforme (including Stevens-Johnson syndrome), rarely – anaphylactic shock.

From the gastrointestinal tract:  nausea, vomiting, diarrhea, pseudomembranous colitis.

Hematopoietic and hemostatic disorders:  bleeding (vitamin K deficiency), anemia, reversible neutropenia (with prolonged use).

Laboratory parameters:  hypoprothrombinemia, increased prothrombin time, increased activity of “hepatic” transaminases and alkaline phosphatase, hypercreatininemia, positive Coombs reaction.

Local reactions:  with intravenous use – phlebitis; with intravenous use-soreness at the injection site.

Interaction

Pharmacologically incompatible with aminoglycosides (if combination therapy with cefoperazone and aminoglycoside is necessary, drugs are prescribed in the form of sequential fractional intravenous use of drugs using 2 separate intravenous catheters).

Indirect anticoagulants, heparin, thrombolytics, antiplatelet agents, and nonsteroidal anti-inflammatory drugs increase the risk of hypoprothrombinemia and bleeding.

Aminoglycosides and loop diuretics increase the risk of nephrotoxicity, especially in individuals with renal insufficiency.

Drugs that reduce tubular secretion increase the concentration of the drug in the blood and slow down its excretion.

Not compatible with ethanol, disulfiram-like reactions may develop in the form of hyperemia, nausea, vomiting, headache, shortness of breath, tachycardia, decreased blood pressure, abdominal cramps.

How to take, course of use and dosage

of Cefoperazone is administered intravenously (drip and jet) and intravenously.

For adults:  the average daily dose of cefoperazone is 2-4 g, administered in equal parts every 12 hours. For severe infections, the daily dose can be increased to 8 g, as well as administered in equal parts every 12 hours. There were no complications with the introduction of cefoperazone in a daily dose of 12 g or even 16 g, divided into equal doses every 8 hours. Treatment can be started until the results of a study of the sensitivity of microorganisms are obtained.

In uncomplicated gonococcal urethritis, a single intravenous injection of 500 mg of the drug is recommended.

For the prevention of postoperative complications – 1 g or 2 g IV 30-90 minutes before the operation. The dose can be repeated every 12 hours, however, in most cases for no more than 24 hours.

For operations with an increased risk of infection (for example, operations in the colorectal area), or if the infection is particularly dangerous (for example, in open heart operations or joint prosthetics), preventive use can continue for 72 hours after the operation is completed.

Patients with impaired renal function are prescribed the usual daily dose (2-4 g). In patients with a glomerular filtration rate below 18 ml / min or a serum creatinine level above 3.5 mg / ml, the daily dose should not exceed 4 g.

In patients with severe hepatic impairment, severe obstruction of the bile ducts, the daily dose of the drug should not exceed 2 g.

In patients with renal-hepatic insufficiency, the concentration of cefoperazone in the blood should be monitored and the dose adjusted if necessary.

Use in children

In children, the daily dose of cefoperazone is 50-200 mg / kg of body weight, administered in equal parts in two doses every 12 hours or more if necessary. The maximum daily dose is 12 g.

With intravenous jet use, the maximum single dose for children is 50 mg / kg, the duration of use is at least 3-5 minutes. For newborns ( Daily doses up to 300 mg / kg were used without complications in young children and children with severe infections, including bacterial meningitis.

I / O introduction

As a solvent, you can use a 5% dextrose solution, an isotonic sodium chloride solution (0.9%), and sterile water for injection.

To prepare the solution for intravenous injection,1 g of cefoperazone should be dissolved in 10 ml of sterile water for injection or another compatible solution and administered for at least 3-5 minutes. For intravenous jet use, the maximum single dose of cefoperazone for adults is 2 g, for children-50 mg/kg of body weight.

When preparing a solution for intravenous drip use,1 g of cefoperazone is dissolved in 5 ml of sterile water for injection, the resulting solution is added to the infusion solution (Ringer’s lactate solution,5% dextrose solution, isotonic sodium chloride solution) to a concentration of 20-100 mg / ml. The duration of use, depending on the volume of the solution, can range from 10-30 minutes or more.

Intramuscular use

Sterile water for injection or isotonic sodium chloride solution can be used to prepare solutions intended for intravenous injection. For dilution of 0.5 g of the drug,2 ml of solvent should be used,1 g-4 ml in order to obtain the final concentration of cefoperazone 250 mg/ml. To reduce pain during intravenous injections, in cases where it is intended to introduce a solution with a concentration of 250 mg/ml or more, it is recommended to use a lidocaine solution for the preparation of the solution (if the patient does not have a hypersensitivity reaction to lidocaine). This solution can be prepared using sterile water for injection in combination with a 2% lidocaine solution. The following two-step dilution method is recommended: first add the required amount of sterile water for injection and shake until the cefoperazone powder is completely dissolved, then add the required amount of 2% lidocaine and mix.

An intravenous injection is made deep into a major muscle (gluteus maximus or anterior thigh).

Overdose

Symptoms:  neurological disorders, including seizures.

Treatment:  symptomatic therapy. Hemodialysis is effective.

Special instructions

Before prescribing cefoperazone, it is necessary to collect a detailed allergic history in order to identify the patient’s hypersensitivity to cephalosporins, penicillins and other medications.

If an allergic reaction occurs during treatment, the use of cefoperazone should be discontinued and appropriate treatment should be initiated.

In some patients, treatment with cefoperazone may lead to vitamin K deficiency in the body, which is associated with suppression of the intestinal flora that synthesizes this vitamin. Patients with malabsorption syndrome (for example, cystic fibrosis), as well as patients who follow an inadequate diet or are on parenteral nutrition for a long time, are most at risk. In such patients, prothrombin time should be monitored during treatment and, if necessary, vitamin K should be prescribed.

With long-term therapy, it is recommended to periodically monitor the function of the kidneys, liver and hematopoietic organs. This is especially important for newborns, including premature babies.

Clostridium difficile-associated diarrhea is observed with almost all antibacterial drugs, including cefoperazone, and is manifested from mild forms of diarrhea to severe colitis. with a fatal outcome. Treatment with antibacterial drugs leads to a violation of the normal microflora of the colon, as a result of which there is an increased growth of Clostrifium difficile, toxins A and B are produced, which lead to the development of Clostridium difficile associated diarrhea. Hypertoxin-producing strains of Clostridium difficile lead to increased morbidity and mortality, as they may be resistant to current antibacterial therapy. All cases of diarrhea in patients treated with antibiotics should be considered as suspicious for the development of Clostridium difficile-associated diarrhea.

During the treatment period, a false positive reaction to glucose in the urine is possible when conducting a study using Benedict or Fehling solutions.

If it is necessary to use the drug in newborns, including premature babies, the expected positive effects of therapy and the possible risk associated with treatment should be taken into account. In newborns with nuclear jaundice, cefoperazone does not displace bilirubin from plasma protein binding sites.

Influence on the ability to drive motor vehicles and manage mechanisms

Use with caution.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf life

2 years

Active ingredient

Cefoperazone

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Indications

Skin Infections, Gastrointestinal Infections, Bronchitis, Pyelonephritis, Pneumonia, Vaginal Infections, Sepsis, Urinary Tract Infections