Universal reference book for medicines
Product name: CEPHOPERAZONE-VIAL (CEFOPERAZONE-VIAL)

Active substance: cefoperazone

Type: Third generation cephalosporin

Manufacturer: VIAL (Russia)
Composition, form of production and packaging
Powder for solution preparation for
intravenous and intravenous administration 1 fl.

cefoperazone (in the form of sodium salt) 1 g

glass bottles (1) - packs of cardboard.

Glass bottles (10) - cardboard boxes.

glass bottles (50) - cardboard boxes.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Cephalosporin antibiotic III generation for parenteral administration.
It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide range of action.
It is active against gram-positive microorganisms - Staphylococcus aureus and Staphylococcus epidermidis (strains producing and not producing penicillinase), Streptococcus pneumonia, Streptococcus pyogenes (beta-hemolytic strain of group A), Streptococcus agalactiae (beta-hemolytic strain of group B), Enterococcus faecalis, many other strains of beta-hemolytic Streptococcus spp .;
Gram-negative microorganisms - Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Citrobacter spp., Haemophilus influenzae (strains producing and not producing beta-lactamases), Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri (formerly Proteus rettgeri), Providencia spp., Serratia spp. (including Serratia marcescens), Salmonella spp., Shigella spp., many strains of Pseudomonas aeruginosa and Pseudomonas of other species, some strains of Acinetobacter spp., Neisseria gonorrhoeae (strains producing and not producing beta-lactamases), Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica; anaerobic microorganisms - Gram - positive and Gram-negative cocci (including Peptococcus spp., Peptostreptococcus spp. and Veillonella spp.), Gram-positive sporo- and non-spore forming anaerobes (Clostridium spp., Eubacter spp., Lactobacillus spp.) and Gram-negative (including Fusobacterium spp. strains of Bacteroides fragilis spp., Prevotella spp., and other representatives of strains of Bacteroides spp.). Stable in relation to broad-spectrum plasmid beta-lactamases (TEM-1-2, SHV-1), but it is destroyed under the influence of broad-spectrum enzymes (TEM-3-2, SHV-2-5). Causes a teturus-like effect.
PHARMACOKINETICS

Cefoperazone binds to plasma proteins by 82-93%.
After the / m introduction, the time to reach C max of the drug is 1-2 hours, after intravenous administration - at the end of the infusion. C max after im / im 1 and 2 g are 65-75 and 97 μg / ml, respectively; after a single intravenous injection of 1, 2, 3 and 4 g (C max ) - 153, 252, 340 and 506 μg / ml, respectively.
Achieves therapeutic concentrations in such tissues and body fluids as peritoneal, ascitic fluid and cerebrospinal fluid (with meningitis), urine, bile, gallbladder walls, lungs, sputum, palatine tonsils and sinus mucosa, atria, kidneys, ureters, prostate , testicles, uterus, fallopian tubes, bones, cord blood and amniotic fluid.
The secretion of the drug in breast milk occurs in very small quantities. The drug does not displace bilirubin from the compound with plasma proteins.
V d of the drug is 0.14-2 l / kg.
T 1/2 irrespective of the mode of administration - 1.6-2.4 h; with hemodialysis - 2.8-4.2 h; in newborns and children from 2 months. up to 11 years - 2.2 hours. Cefoperazone is excreted unchanged mainly with bile (70-80%) and kidneys (20-30%). In patients with impaired liver function and biliary tract obstruction T 1/2 - 3-7 hours, excretion by the kidneys is 90% or more. Even with severe liver damage, therapeutic concentrations are achieved in bile, and T 1/2 iselongated only 2-4 times. In patients with renal-hepatic insufficiency can cumulate.
INDICATIONS

- Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

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

> infections of the kidneys and urinary tract (including pyelonephritis and cystitis);

> infections of the abdominal organs (including peritonitis, cholecystitis, cholangitis);

> sepsis, meningitis;

> infections of the 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.

DOSING MODE

Cefoperazone is administered intravenously (by drip and jet) and in / m.

Adults: The average daily dose of cefoperazone is 2-4 g, administered in equal parts every 12 hours. In severe infections, the daily dose can be increased to 8 g, administered also in equal parts every 12 hours. There were no complications in the administration of cefoperazone in the daily dose of 12 g and even 16 g divided into equal doses every 8 h. Treatment can be initiated before the results of a study of the sensitivity of microorganisms.

With uncomplicated gonococcal urethritis, a one-time intramuscular injection of 500 mg of the drug is recommended.

For the prevention of postoperative complications - 1 g or 2 g IV for 30-90 min before the operation.
The dose can be repeated every 12 hours, however, in most cases within no more than 24 hours.
In case of operations with an increased risk of infection (for example, operations in the colorectal area), or if the infection is especially dangerous (for example, in open-heart surgery or joint prosthetics), preventive use can continue for 72 hours after the operation is completed.

Patients with impaired renal function are given a usual daily dose (2-4 g).
Patients who have a glomerular filtration rate below 18 ml / min or serum creatinine above 3.5 mg / ml, daily dose should not exceed 4 g.
In patients with severe impairment of liver function, expressed by 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, if necessary, the dose should be adjusted.

Use in children

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

For IV injections, the maximum single dose for children is 50 mg / kg, the duration of administration is at least 3-5 minutes.
Newborns (<8 days) receive 50-200 mg / kg body weight per day in equal parts every 12 hours. Daily doses up to 300 mg / kg were applied without complications in young children and children with severe infections, including bacterial meningitis.
IV introduction

As a solvent, 5% dextrose solution, isotonic sodium chloride solution (0.9%), sterile water for injection can be used.

To prepare a solution for intravenous administration, 1 g of cefoperazone should be dissolved in 10 ml of sterile water for injection or another compatible solution and administered for a minimum of 3-5 minutes.
For intravenous administration the maximum single dose of cefoperazone for adults is 2 g, for children - 50 mg / kg of body weight.
When preparing the solution for intravenous administration, 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 administration depending on the volume of the solution can be from 10-30 minutes or more.
Intramuscular injection

For the preparation of solutions intended for intravenous injections, sterile water for injection or isotonic sodium chloride solution can be used.
To dilute 0.5 g of the drug should be used 2 ml of solvent, 1 g - 4 ml to obtain a final concentration of cefoperazone 250 mg / ml. To reduce the pain with I / m injections, when a solution with a concentration of 250 mg / ml or more is expected to be administered, a lidocaine solution is recommended for the preparation of the solution (in case the patient has no hypersensitivity reaction to lidocaine). This solution can be prepared using sterile water for injection in combination with a 2% solution of lidocaine.The following two-step dilution method is recommended: first add the required amount of sterile water for injection and shake until cefoperazone powder completely dissolves, then add the necessary amount of 2% lidocaine and mix.
Final concentration of cefoperazone 1 stage Volume of sterile water Stage 2 Volume of 2% lidocaine

Bottle 1 g 250 mg / ml 2.6 ml 0.9 ml

Vial 1 g 333 mg / ml 1.8 ml 0.6 ml

In / m injection is made deep into the large muscle (the gluteus maximus muscle or the anterior surface of the thigh).

SIDE EFFECT

Allergic reactions: urticaria, skin itching, maculopapular rash, fever, eosinophilia, multiforme exudative erythema (including Stevens-Johnson syndrome), rarely anaphylactic shock.

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

On the part of the organs of hematopoiesis and hemostasis system: bleeding (vitamin K deficiency), anemia, reversible neutropenia (with prolonged use).

Laboratory indices: hypoprothrombinemia, increased prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, Coombs positive reaction.

Local reactions: with iv injection, phlebitis;
with the / m introduction - soreness in the injection site.
CONTRAINDICATIONS

- hypersensitivity to cephalosporin and other beta-lactam antibiotics.

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

PREGNANCY AND LACTATION

The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.

If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

Take this medication with caution in case of kidney failure.

In patients with impaired liver function and with concomitant renal damage, it is necessary to monitor the concentration of the drug in the blood serum.
If the serum concentration is not measured, then in these cases the dose should not exceed 2 g / day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Take this medication with caution in case of liver failure.

In patients with impaired liver function and with concomitant renal damage, it is necessary to monitor the concentration of the drug in the blood serum.
If the serum concentration is not measured, then in these cases the dose should not exceed 2 g / day.
APPLICATION FOR CHILDREN

The application is possible according to the dosing regimen.

SPECIAL INSTRUCTIONS

Can be used with combination therapy in combination with other antibiotics.

In cases of bile duct obstruction, severe liver disease or concomitant renal dysfunction, there may be a need to change the dosing regimen.
In patients with impaired liver function and with concomitant renal damage, it is necessary to monitor the concentration of the drug in the blood serum. If the serum concentration is not measured, then in these cases the dose should not exceed 2 g / day.
Long-term use can lead to the development of resistance of the pathogen.

During the use of the drug, a false positive reaction to glucose in the urine with a solution of Benedict or Feling can take place.

During treatment should be refrained from taking ethanol - there may be effects similar to the action of disulfiram (facial skin hyperemia, stomach and stomach spasms, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).

Patients who adhere to a defective diet or who have a malabsorption of food (for example, suffering from cystic fibrosis), as well as patients who have been on parenteral nutrition for a long time, may have vitamin K deficiency. These patients should be monitored for prothrombin time, and if necessary the purpose of vitamin K is indicated. With the use of cefoperazone (as well as other antibiotics), superinfection may develop, which requires the withdrawal of the drug and the appointment of an appropriate treatment
I.
OVERDOSE

Symptoms: epileptic seizure.

Treatment: sedation with diazepam.

DRUG INTERACTION

Pharmaceutically incompatible with aminoglycosides (if necessary, combined therapy with cefoperazone and aminoglycoside drugs are prescribed as a sequential fractional intravenous drug administration using 2 separate intravenous catheters).

Indirect anticoagulants, heparin, thrombolytics, antiaggregants, non-steroidal anti-inflammatory drugs increase the risk of hypoprothrombinemia, bleeding.

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

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

It is not compatible with ethanol, development of disulfiram-like reactions in the form of hyperemia, nausea, vomiting, headache, dyspnea, tachycardia, lowering of blood pressure, abdominal cramps is possible.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a dry, protected from light at a temperature of no higher than 25 ° C.
The prepared solution is stable for 7 days when stored in a refrigerator (2-8 ° C). Keep out of the reach of children.
Shelf life - 3 years.
Do not use after the expiration date.
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