Universal reference book for medicines
Name of the preparation: CEPPAR SV (CEPHPAR SV)

Active substance: cefoperazone, sulbactam

Type: Cephalosporin III generation with a beta-lactamase inhibitor

Manufacturer: RUSYUROFARM (Russia) manufactured by KARNATAKA ANTIBIOTICS & PHARMACEUTICALS (India)
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

sulbactam (in the form of the sodium salt) 1 g

Vials (1) - packs of cardboard.

Bottles (50) - packs of cardboard.

Powder for solution preparation for intravenous and intravenous administration 1 fl.

sulbactam 500 mg

cefoperazone 500 mg

Vials (1) - packs of cardboard.

Bottles (50) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

The antibacterial component of cefoperazone + sulbactam is cefoperazone, a third generation cephalosporin that acts on sensitive microorganisms during their active propagation by inhibiting the biosynthesis of the cell wall mucopeptide.
Sulbactam does not have clinically significant antibacterial activity (except for Neisseriaceae and Acinetobacter). However, it was noted that it is an irreversible inhibitor of most of the major beta-lactamases that are produced by microorganisms resistant to beta-lactam antibiotics. The ability of sulbactam to prevent the destruction of penicillins and cephalosporins by resistant microorganisms was confirmed in studies using resistant strains for which sulbactam possessed a pronounced synergy with penicillins and cephalosporins. In addition, sulbactam interacts with certain penicillin-binding proteins, so cefoperazone + sulbactam often has a more pronounced effect on sensitive strains than one cefoperazone.
The combination of sulbactam and cefoperazone is active against all microorganisms sensitive to cefoperazone.
In addition, it has a synergistic effect on various microorganisms, in particular: Haemophilus influenzae, Bacteroides spp., Staphylococcus spp., Acinetobacter calcoaceticus, Enterobacter aerobes, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Morganella morganii, Citrobacter freundii, Enterobacter cloacae, Citrobacter freundii diversus.
Cefoperazone + sulbactam is active in vitro against a wide range of clinically relevant microorganisms.

Gram-positive microorganisms:

Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococcus), Streptococcus agalacliae (group B beta-hemolytic streptococcus), most other strains of beta-hemolytic streptococci, many strains of Enterococcus faecalis.

Gram-negative microorganisms:

Escherichia coli, Klebsiella spp., Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia spp., Serratia spp.
(including Serratia marcescens). Salmonella spp. and Shigella spp., Pseudomonas aeruginosa and several other Pseudomonas spp., Acinelobacler calcoaceticus, Neisseria gonorrhoeae, Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica.
Anaerobic microorganisms:

Gram-negative rods (including Bacteroides fragilis, other Bacteroides spp. And Fusobacterium spp.).
Gram-positive and Gram-negative cocci (Including Peplococcus spp., Peptostreptococcuspus. And Veillonellaspp.). Gram-positive rods (including Clostridium spp., Eubacterium spp. And Lactobacillus spp.).
PHARMACOKINETICS

The maximum concentrations of sulbactam and cefoperazone after intravenous administration (w / w) 2 g of cefoperazone + sulbactam (1 g of sulbactam, 1 g of cefoperazone) for 5 minutes averaged 130 and 237 μg / ml, respectively.
This reflects a higher volume of sulbactam distribution compared to that of cefoperazone.
Both sulbactam and cefoperazone are well distributed in various tissues and fluids, including bile, gall bladder, skin, appendix, fallopian tubes, ovaries, uterus, etc. Sulbactam and cefoperazone penetrate the placental barrier.
When repeated application of significant changes in the pharmacokinetics of both components of the drug is not noted. With the introduction of the drug every 8-12 hours cumulation was not observed. Approximately 84% of the dose of sulbactam and 25% of the dose of cefoperazone, administered as a combination - cefoperazone + sulbactam, is excreted by the kidneys. The rest of cefoperazone is excreted with bile. Cefoperazone does not displace bilirubin from its association with plasma proteins. T 1/2 of sulbactam averages about 1 hour, cefoperazone - 1.7 hours. Serum concentration is proportional to the administered dose.
When a violation of liver function

Cefoperazone is actively excreted with bile.
T 1/2 of cefoperazone usually lengthens, and the excretion of the drug by the kidneys increases in patients with liver disease and / or biliary tract obstruction. Even with a serious violation of liver function in bile, the therapeutic concentration of cefoperazone is reached, and the elimination half-life increases only 2-4 times.
In case of impaired renal function

In patients with varying degrees of renal dysfunction, receiving cefoperazone + sulbactam, a high correlation was found between the total clearance of sulbactam from the body and the estimated clearance of creatinine.
In patients with terminal renal failure, a significant elongation of T 1/2 of sulbactam (up to 9.7 h) was detected.Hemodialysis caused significant changes in the half-life, total clearance and volume of distribution of sulbactam.
Application in the elderly

The pharmacokinetics of cefoperazone + sulbactam has been studied in elderly people with renal insufficiency and impaired liver function.
In comparison with healthy volunteers, an increase in the duration of T 1/2 , a decrease in clearance and an increase in Vd of both sulbactam and cefoperazone were revealed. The pharmacokinetics of sulbactam correlated with the degree of impaired renal function, and the pharmacokinetics of cefoperazone - with a degree of impaired hepatic function.
Use in children

In studies in children, no significant changes in the pharmacokinetics of the components of cefoperazone + sulbactam were found in comparison with those in adults.T 1/2 of sulbactam in children ranged from 0.9 to 1.4 h, of cefoperazone from 1.4 to 1.9 h.

INDICATIONS

Infectious-inflammatory diseases caused by sensitive microorganisms:

- infections of the upper and lower respiratory tract;

- urinary tract infections;

- peritonitis, cholecystitis, cholangitis;

- sepsis, meningitis;

- skin and soft tissue infections;

- infections of bones and joints;

- inflammatory diseases of the pelvic organs, including endometritis, gonorrhea.

DOSING MODE

Intravenous (struino and drip) and intramuscularly.

Application in adults

In adults, cefoperazone + sulbactam is recommended for use in the following daily doses:

The ratio of cefoperazone to sulbactam dose (g) of cefoperazone dose (g) of sulbactam dose (g)

1: 1 2.0-4.0 1.0-2.0 1.0-2.0

The daily dose should be divided into equal parts and administered every 12 hours. In severe and resistant to standard doses, the daily dose of cefoperazone + sulbactam can be increased to 8 g at a 1: 1 ratio of the main components (ie 4 g of cefoperazone).
If you need more than 8 g (with a 1: 1 ratio of the main components), an increase in the dose is achieved by the additional administration of cefoperazone. The dose should be divided into equal parts and administered every 12 hours. The recommended maximum daily dose of sulbactam is 4 g.
Application for renal dysfunction

In patients with a creatinine clearance of 15-30 ml / min, the maximum dose of sulbactam is

1 g every 12 hours (maximum daily dose of sulbactam 2 g), and in patients with creatinine clearance less than 15 ml / min the maximum dose of sulbactam is 500 mg every 12 hours (maximum daily dose of sulbactam 1 g).
In severe infections, additional administration of cefoperazone may be required.
The pharmacokinetics of sulbactam significantly changes during hemodialysis.
The half-life of cefoperazone from the blood plasma is somewhat reduced during hemodialysis. Therefore, the administration of the drug should be planned after dialysis.
Application for violations of liver function

If regular monitoring of serum concentration of cefoperazone is not performed, the maximum daily dose should not exceed 2 g (see section "Special instructions").

Use in children

In children, cefoperazone + sulbactam is recommended for use in the following daily doses:

The ratio of cefoperazone + sulbactam dose (mg / kg / day) to the sulbactam dose (mg / kg / day) of cefoperazone dose (mg / kg / day)

1: 1 40-80 20-40 20-40

The dose should be divided into equal parts and administered every 6-12 hours.

With severe and resistant to standard doses of infections, the daily dose can be increased to 160 mg / kg / day with a 1: 1 ratio of the main components.
The daily dose is divided into 2-4 equal parts. If more than 80 mg / kg / sug, calculated from the activity of cefoperazone, are required, the dose is increased by additional administration of cefoperazone.
Neonatal application

In newborns during the first week of life, the drug should be injected every 12 hours. The maximum daily dose of sulbactam in children should not exceed 80 mg / kg / day.
Method of preparation of solutions for parenteral administration Breeding:
Total dose (g) Equivalent doses of cefoperazone + sulbactam Volume of solvent, ml Maximum final concentration mg / ml

1.0 0.5 + 0.5 3.4 125 + 125

2.0 1.0+ 1.0 6.7 125+ 125

Intramuscular administration:

Sterile water for injection is used for dissolution (see table).
If the drug is administered at a concentration in excess of 250 mg / ml, it is recommended to prepare the solution using lidocaine. Dilution is carried out in 2 stages - in a vial containing 1 g of the drug, add 1.3 ml of sterile water for injections, in a vial containing 2 g - 2.6 ml, shake until complete dissolution, and then add to a vial containing 1 g of the drug - 0.4 ml , into a vial containing 2 g - 0.8 ml of a 2% solution of lidocaine hydrochloride. The final solution will contain in 1 ml 0.5% lidocaine hydrochloride solution about 250 mg of cefoperazone and about 250 mg of sulbactam.
Intravenous administration:

For intravenous administration, the contents of the vial are dissolved in an adequate volume (see table) 5% dextrose solution, 0.9% sodium chloride solution, 5% dextrose solution in 0.225% sodium chloride solution, 5% dextrose solution in 0.9% sodium chloride solution or sterile water for injection and injected for 3 minutes.

For IV infusion introduction dissolve, as mentioned above, then dilute to 20-100 ml with the same solvent and injected for 15-60 minutes.

Preparation of the solution using Ringer's lactate.
Since Ringer's lactate is not suitable for initial dilution, the solution is prepared in two steps: first use sterile water for injection (see table), and then dilute the resulting solution with Ringer's lactate solution to a concentration of 5 mg / ml of sulbactam. Infusion is carried out for 15-60 minutes.
SIDE EFFECT

From the cardiovascular system: lowering blood pressure.

From the digestive system: diarrhea, nausea, vomiting, pseudomembranous colitis.

Allergic reactions: maculopapular rash, hives, itching, Stevens-Johnson syndrome, anaphylactic shock.

From the hemopoietic system: bleeding (vitamin K deficiency), a decrease in the number of neutrophils.
With long-term treatment, reversible neutropenia, a decrease in hemoglobin and hematocrit, transient eosinophilia, thrombocytopenia, leukopenia, hypoprothrombinemia develops.
Local reactions: sometimes after intravenous injection there is transient pain and burning at the injection site.
With iv administration of the drug, phlebitis may develop at the site of administration.
Laboratory indicators: hypercreatininaemia, transient increase in hepatic transaminases, alkaline phosphatase and bilirubin in blood serum, hematuria, false-positive Coombs test.
When using a solution of Benedict or Felling, a false positive reaction to glucose in the urine can be observed.
Other: headache, fever, chills, vasculitis.

CONTRAINDICATIONS

- hypersensitivity to sulbactam, cefoperazone, penicillins and other beta-lactam antibiotics.

With caution: severe impairment of kidney and liver function, colitis (including in history), children's age of up to 3 months.

PREGNANCY AND LACTATION

In pregnancy, the drug is used only if the expected benefit to the mother exceeds the potential risk to the fetus.
If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER

With caution: severe renal dysfunction.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution: severe liver dysfunction.

APPLICATION FOR CHILDREN

With caution: children under 3 months.

SPECIAL INSTRUCTIONS

The risk of hypersensitivity reactions, including those leading to death, is higher in patients who have a history of hypersensitivity reactions to many allergens.
In case of an allergic reaction, it is necessary to cancel the drug and prescribe adequate therapy.
Serious anaphylactic reactions require urgent epinephrine.
Intravenously injected glucocorticosteroids and provide airway patency, including intubation.
Dose changes may be required in cases of severe biliary obstruction, severe liver disease, and renal dysfunction associated with any of these conditions.

In patients with impaired liver function and concomitant renal dysfunction, monitoring the serum concentration of cefoperazone and correcting its dose should be necessary.
If regular monitoring of serum concentration of cefoperazone in such cases is not carried out, then its daily dose should not exceed 2 g.
When using a solution of Benedict or Felling, a false positive reaction to glucose in the urine can be observed.

With the simultaneous use of aminoglycosides, kidney function should be monitored.

In the treatment of cefoperazonom in rare cases, vitamin K deficiency developed. Patients receiving malnutrition, suffering from malabsorption (for example, in cystic fibrosis) and those who are long-term on intravenous artificial feeding may be classified as a risk group.
In such cases, as well as in patients receiving anticoagulants, it is necessary to monitor prothrombin time and, in the presence of indications, prescribe vitamin K.
With prolonged treatment, excessive growth of insensitive microorganisms can be observed.
With prolonged therapy, it is recommended to periodically monitor the performance of internal organs, including the kidneys, liver and hematopoiesis system.
OVERDOSE

Symptoms: neurological disorders, including convulsions.

Treatment: symptomatic, hemodialysis is effective, especially in patients with impaired renal function.

DRUG INTERACTION

Solutions cefoperazona + sulbactam and aminoglycosides should not be directly mixed, given the pharmaceutical incompatibility between them.
If combined therapy is provided, the two drugs are administered by successive infusions using separate secondary catheters, and the primary catheter is washed between doses of the drugs. Intervals between administration during the day should be as large as possible.
When ethanol is used during treatment with cefoperazone and for up to 5 days after its administration, development of disulfiram-like effects, characterized by "hot flashes", sweating, headache and tachycardia, is possible.

In patients who need artificial feeding (inside or parenteral), the use of solutions containing ethanol should be avoided.

TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

List B. Store in a dry, the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children. Shelf life - 3 years.
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