Universal reference book for medicines
Product name: CEFOBID ® (CEFOBID ® )

Active substance: cefoperazone

Type: Third generation cephalosporin

Manufacturer: PFIZER (USA) manufactured by HAUPT PHARMA LATINA (Italy)
Composition, form of production and packaging
Powder for the preparation of a solution for IV and / or injection of
crystalline, white or white with a yellowish hue.

1 f.

sodium cefoperazone 1.034 g,

which corresponds to the content of cefoperazone 1 g

Glass bottles (1) - cardboard packs.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2008.

PHARMACHOLOGIC EFFECT

Semisynthetic cephalosporin antibiotic with a wide spectrum of action, intended only for parenteral administration.

The bactericidal action of cefoperazone is due to the inhibition of bacterial cell wall synthesis.

Cefoperazone is active in vitro against a large number of different clinically relevant microorganisms.
At the same time, he shows resistance to the action of many? -lactamases.
Cefoperazone is active against aerobic Gram-positive bacteria : Staphylococcus aureus (strains producing and not producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae (formerly Diplococcus pneumoniae), Streptococcus pyogenes (group A beta beta-hemolytic streptococcus), Streptococcus agalactiae (beta-hemolytic group streptococcus B), many strains of Enterococcus faecalis, many other strains of beta-hemolytic streptococci;
aerobic Gram-negative bacteria: Escherichia coli, Klebsiella spp., Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus mirabilis, Proteus vulgaris, Morganella morganii (formerly Proteus morganii), Providencia spp. (including Providencia rettgeri), Serratia spp. (including Serratia marcescens), Salmonella spp., Shigella spp., Pseudomonas spp. (including Pseudomonas aeruginosa), Acinetobacter calcoaceticus, Neisseria gonorrhoeae, Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica; anaerobic Gram-positive bacteria: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Eubacterium spp., Lactobacillus spp .; anaerobic gram-negative bacteria: Veillonella spp., Fusobacterium spp., Bacteroides spp. (including many strains of Bacteroides fragilis).
PHARMACOKINETICS

Suction

High levels of cefoperazone are achieved in the blood, bile and urine after a single injection.

The tables show the concentration of cefoperazone in the blood serum of adult healthy volunteers after a 15-minute uniform intravenous infusion of the drug at a dose of 1, 2, 3 or 4 g or after a single IM injection at a dose of 1 or 2 g.

Doses Mean concentrations of cefoperazone in serum (μg / ml)

0 * 30 minutes 1 hour 2 hours

IV introduction

1 g 153 114 73 38

2 g 252 153 114 70

3 g 340 210 142 90

4 g 506 325 251 161

Intramuscular injection

1 g 32 ** 52 65 57

2 g 40 ** 69 93 97


Doses Mean concentrations of cefoperazone in serum (μg / ml)

4 hours 8 hours 12 hours

IV introduction

1 g 16 4 0.5

2 g 32 8 2

3 g 41 9 2

4 g 71 19 6

Intramuscular injection

1 g 33 7 1

2 g 58 14 4

* The time elapsed after the administration of the drug.

0 - time corresponding to the end of the drug administration;

** results obtained 15 minutes after drug administration.

Distribution

Cefoperazone reaches therapeutic levels in all tissues and biological fluids of the body, subjected to research, including.
aspirin, kidney, ureter, prostate, testis, uterus, fallopian tubes, bones, cord blood and amniotic liquid. Repeated administration of the drug to healthy individuals does not result in the cumulation of cefoperazone.
Excretion

T 1/2 of cefoperazone from the blood is approximately 2 hours, regardless of the route of administration.

Cefoperazone is excreted with bile and urine.
The concentration of cefoperazone in bile reaches its maximum level usually 1-3 hours after the administration of Cephobide and exceeds its concentration in the blood 100 times during this period of time. The following concentrations in bile were recorded: from 66 μg / ml after 30 minutes to 6,000 μg / ml 3 h after iv administration of 2 g of the drug to patients without obstruction of the bile duct.
12 hours after the administration in different doses and in different ways in persons with normal renal function, the concentration of cefoperazone in the urine reaches on average 20-30% of the administered dose of the drug.
Concentrations in urine exceeding 2200 μg / ml were obtained 15 minutes after intravenous administration of 2 g of Cefobide. After a / m administration of 2 g of the drug, the maximum concentration in the urine was approximately 1000 μg / ml.
Pharmacokinetics in special clinical cases

Pharmacokinetic parameters do not differ in patients with normal renal excretory function and in patients with renal insufficiency (C max , AUC, T 1/2 ).

In patients with impaired liver function, T 1/2 of cefoperazone is prolonged from the plasma and its excretion in the urine also increases.

In patients with renal-hepatic insufficiency, cefoperazone can accumulate in the blood plasma.

INDICATIONS

Treatment of the following infectious diseases caused by microorganisms sensitive to cefoperazone:

- infections of the upper and lower respiratory tract;

- infections of the upper and lower parts of the urinary tract;

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

- septicemia;

- meningitis;

- skin and soft tissue infections;

- infections of bones and joints;

- Infectious-inflammatory diseases of pelvic organs, endometritis;

- Gonorrhea;

- genital tract infections.

Prevention of infectious postoperative complications in abdominal, gynecological, cardiovascular and orthopedic operations.

A wide spectrum of action of cefoperazone allows for the monotherapy of most infections, but cefoperazone can also be used in combination with other antibiotics.

DOSING MODE

The average daily dose given to an adult ranges from 2 to 4 g;
the dose is given in 2 divided doses every 12 hours.
In case of serious infections, the daily dose can be increased to 8 g (in 2 injections every 12 hours). No complications were found with the administration of Cephobide in a daily dose of 12 g divided into equal doses every 8 hours, and even 16 g divided into equal doses.
Treatment with the drug can be started before the results of a study of the sensitivity of microorganisms.
With uncomplicated gonococcal urethritis , a single IV dose of 500 mg of the drug is recommended.

For the prevention of infectious postoperative complications , 1 g or 2 g IV preparation for 30-90 minutes before the operation is prescribed.
The dose can be repeated every 12 hours, but in most cases for no more than 24 hours. For operations with an increased risk of infection (eg, operations in the colorectal area), or if the infection that has occurred can be particularly harmful (for example, in open operations heart or joint replacement), preventive use can continue for 72 hours after the operation is completed.
If liver function is impaired, dose adjustment may be required in cases of severe biliary obstruction, severe liver disease, or with concomitant renal dysfunction.
The daily dose should not exceed 2 g, while there is no need to monitor the concentration of cefoperazone in the blood serum.
Patients with impaired renal function drug can be prescribed in an average daily dose (2-4 g) without correction.
Patients who have a glomerular filtration rate below 18 ml / min or a serum creatinine level above 3.5 mg / dl should not exceed a daily dose of 4 g. When hemodialysis, the half-life of cefoperazone from the blood serum decreases slightly, so the drug should be administered after the end of dialysis.
With a simultaneous violation of the liver and kidneys should monitor the concentration of cefoperazona in the blood serum and, if necessary, adjust the dose.
There is no need to monitor serum concentrations provided that the daily dose does not exceed 2 g.
Children Cephobide should be given in daily doses at a rate of 50 to 200 mg per 1 kg of body weight;
the drug should be injected every 8-12 hours. The maximum daily dose is 12 g.
With intravenous infusion of slow injection, the maximum single dose is 50 mg / kg of body weight;
duration of administration - at least 3-5 minutes.
Newborn (less than 8 days) daily dose is from 50 to 200 mg / kg;
the drug should be injected every 12 hours.
Rules for the preparation and administration of a solution for intravenous administration

To prepare solutions intended for intravenous administration, sterile water for injection or bacteriostatic water for injection can be used.
In cases where it is proposed to administer the drug at a concentration in excess of 250 mg / ml, a solution of lidocaine is recommended for solution preparation. This solution can be prepared using sterile water for injection in combination with a 2% solution of lidocaine, which is close to a 0.5% solution of lidocaine hydrochloride.
It is recommended to dilute the drug in 2 stages: first add the necessary amount of sterile water for injection and shake until the powder is completely dissolved, then add the necessary amount of 2% lidocaine solution and mix.

Final concentration of cefoperazone Sterilized water volume Volume 2% of lidocaine solution Entered volume *

250 mg / ml 2.6 ml 0.9 ml 4.0 ml

333 mg / ml 1.8 ml 0.6 ml 3.0 ml

* excess volume allows to fully fill the syringe of the specified volume.

Intramuscular injection is performed deep into the large gluteus muscle or in the anterior surface of the thigh.

Rules for the preparation and administration of a solution for intravenous administration

The contents of the vial are first diluted in any compatible solution for intravenous administration (at a rate of at least 2.8 ml / 1 g of cefoperazone).
To facilitate dissolution, it is recommended to use 5 ml of solvent per g of Cefobide.
The following solutions are used for initial dilution: 5% dextrose injection, 10% dextrose solution, 0.9% sodium chloride solution for injection, 5% dextrose solution and 0.9% sodium chloride solution for injection, 5% dextrose solution and 0.2% sodium chloride solution for injection, sterile water for injection, normosol R, normosol M in a 5% solution of dextrose for injection.

Then the entire amount of the solution obtained should be diluted with one of the following solvents for IV administration: 5% dextrose injection, 10% dextrose injection, 5% dextrose and lactated Ringer's injection, lactated Ringer's solution, 5% solution dextrose and 0.9% solution of sodium chloride for injection, 0.9% solution of sodium chloride for injection, normosol R, normosol M in 5% dextrose solution for injection, 5% dextrose solution and 0.2% sodium chloride solution for injection.

For IV injection, the contents of each Cefobide vial (1 g) are dissolved in 20-100 ml of a compatible sterile IV solution and injected for 15 minutes to 1 hour. If sterile water is used as the solvent, then the vial with the drug it is added no more than 20 ml.

For long-term intravenous infusion, the contents of 1 vial (1 g) are dissolved in either 5 ml of sterile water for injection or in 5 ml of bacteriostatic water for injection;the resulting solution is added to a suitable solvent for intravenous administration.

For IV injection of slow slow administration, the drug is dissolved in a suitable solvent with a final concentration of 100 mg / ml and injected for at least 3-5 minutes.

SIDE EFFECT

On the part of the hematopoiesis system: cases of a slight decrease in the level of neutrophils, reversible neutropenia (with prolonged treatment), a positive direct antiglobulin test of Coombs, a decrease in hematocrit and hemoglobin;
in some cases - short eosinophilia and hypoprombinemia.
On the part of the digestive system : mild to moderate dyspepsia (these symptoms disappeared after withdrawal of the drug and / or symptomatic therapy), a moderately expressed transient increase in the activity of AST, ALT, and APF.

Allergic reactions: makulo-papular rash, urticaria, eosinophilia and drug fever (most often such reactions to treatment with Cefobid appear in patients who have a history of susceptibility to allergic reactions, especially penicillin).

Local reactions: i / m administration is sometimes accompanied by painful sensations;
with intravenous infusion in some patients at the infusion site develops phlebitis.
During the postmarketing observations, the following undesirable phenomena were also noted.

On the part of the digestive system : vomiting, pseudomembranous colitis.

Other: allergic reactions, anaphylactoid reactions (including shock), itching, Stevens-Johnson syndrome, bleeding.

CONTRAINDICATIONS

- Hypersensitivity to cefoperazone and other cephalosporin antibiotics.

PREGNANCY AND LACTATION

The purpose of the drug during pregnancy is possible only in cases where the intended use 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

Patients with impaired renal function drug can be prescribed in an average daily dose (2-4 g) without correction.
Patients who have a glomerular filtration rate below 18 ml / min or a serum creatinine level above 3.5 mg / dl should not exceed a daily dose of 4 g. When hemodialysis, the half-life of cefoperazone from the blood serum decreases slightly, so the drug should be administered after the end of dialysis.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

If liver function is impaired, dose adjustment may be required in cases of severe biliary obstruction, severe liver disease, or with concomitant renal dysfunction.
The daily dose should not exceed 2 g, while there is no need to monitor the concentration of cefoperazone in the blood serum.
SPECIAL INSTRUCTIONS

A wide spectrum of action of cefoperazone allows for the monotherapy of most infections.
Nevertheless, Cefobide can also be used in combination therapy in combination with other antibiotics if such treatment is indicated. When combined with aminoglycosides, it is recommended to monitor kidney function.
Prior to the appointment of a patient with Cefobide, for the sake of precaution, it is necessary to establish whether he has previously had a heightened sensitivity to cephalosporins, penicillins and other drugs.
Patients with hypersensitivity to penicillin should be prescribed with great care. All patients who have a history of various allergic reactions and especially a drug allergy, antibiotics should be administered with caution.
If an allergic reaction occurs, the use of Cephobide should be discontinued and appropriate treatment initiated.
Serious anaphylactic reactions require the immediate introduction of epinephrine (adrenaline). If necessary, use oxygen, intravenous corticosteroids and ensure normal breathing (including intubation).
With severe blockage of the bile ducts, severe liver disease, T 1/2 of cefoperazone usually lengthens, and excretion of the drug with urine increases.

In some patients, treatment with Cefobide, as well as treatment with other antibiotics, can lead to a deficiency in the body of vitamin K. Most likely, this is due to the suppression of the intestinal flora that synthesizes this vitamin.
Such a risk is susceptible to patients who adhere to the reduction diet, which are for a long time on parenteral nutrition or with a violation of food intake (eg, patients with cystic fibrosis). Such patients should be monitored prothrombin time and, if necessary, they are assigned exogenous vitamin K.
Long-term use of cefoperazone can lead to increased growth of resistant microorganisms (as in the treatment with other antibiotics).
Therefore, during treatment, you need to carefully monitor patients.
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.

When drinking alcohol during or for 5 days after using Cephobide, disulfiram-like reactions were observed, manifested in the form of sudden hot flushes, increased sweating, headache and tachycardia.
Therefore, patients should refrain from drinking alcohol and taking ethanol-containing medications while treating Cefobed.
Use in Pediatrics

Cefobide is successfully used in the treatment of infants.
But until now no studies have been conducted on a large scale concerning the use in newborns and premature infants. Therefore, before prescribing it to premature and newborn children, both anticipated positive effects and the possible risks associated with treatment should be taken into account.
OVERDOSE

Information on the acute overdose of Cefobed is limited.

Symptoms: may increase the described side effects.
Cephalosporins in very high doses can cause epileptic seizures.
Treatment: sedative therapy with diazepam in case of epileptic seizures caused by overdose.
Cefoperazone is excreted in hemodialysis, therefore, it is possible to use this procedure for overdose in patients with impaired renal function.
DRUG INTERACTION

With the simultaneous use of probenecid does not affect the concentration of cefoperazone in the blood serum.

Pharmaceutical interaction .

Solutions of Cepobide and aminoglycoside should not be confused directly, because there is a physical incompatibility between them.

If combined therapy with cefoperazone and aminoglycoside is required, sequential fractional iv preparations are administered using two separate intravenous IV catheters, provided they are adequately washed with appropriate solvents between the administration of sequential doses of the drugs.
It is also proposed to administer cefoperazone before the administration of aminoglycoside.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of the reach of children at a temperature of not more than 30C.
Shelf life - 2 years.
Stability of ready solutions depends on the type of solvent, concentration, storage conditions.
The storage times are indicated in the table. At the end of these deadlines unused balance of solutions should be discarded.
Types solvent Sample concentration
at a temperature of 15-25 ° C for 24 h
5% solution of dextrose in lactate Ringer p-D d / inj. 2-50 mg / ml of
10% solution of dextrose d / inj. 2-50 mg / ml
at a temperature of 15-25 ° C for 24 hours or in a refrigerator (2-8 ° C) - within 5 days
Bacteriostatic water d / inj. 300 mg / ml of
5% solution of dextrose d / inj. 2-50 mg / ml of
5% solution of dextrose d / inj. and 0.9% solution of sodium chloride d / inj. 2-50 mg / ml of
5% solution of dextrose d / inj. and 0.2% solution of sodium chloride d / inj. 2-50 mg / mL
The lactate Ringer rr d / inj. 2 mg / ml
0.5% solution of lidocaine d / inj. 300 mg / ml
0.9% solution of sodium chloride d / inj. 2-300 mg / ml of
Normosol M 5% solution of dextrose in D d / inj. 2-50 mg / ml of
Normosol R 2-50 mg / ml
Sterile water q / inj. 300 mg / ml
reconstituted solutions stored in glass or plastic syringes, glass or flexible plastic containers intended for parenteral solutions.
Solvent Species Exemplary concentrations
in the freezer (from -10 ° to -20 ° C) - for 3 weeks
5% solution of dextrose d / inj. 50 mg / ml of
5% solution of dextrose d / inj. and 0.9% solution of sodium chloride d / inj. 2 mg / ml of
5% solution of dextrose d / inj. and 0.2% solution of sodium chloride d / inj. 2 mg / ml
in a freezer (from -10 ° to -20 ° C) - 5 weeks
0.9% solution of sodium chloride d / inj. 300 mg / ml
Sterile water q / inj. 300 mg / ml
in a freezer reconstituted solutions were stored in plastic syringes or flexible plastic containers intended for parenteral solutions.
Before use the frozen formulation solutions were thawed at room temperature. Unused frozen solution must be destroyed.
The solutions should not be frozen again.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!