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
bottles (1) - packs of cardboard.
bottles (50) - cardboard boxes.
Powder for solution preparation for intravenous and intravenous administration 1 fl.
cefoperazone (in the form of the sodium salt) 2 g
bottles (1) - packs of cardboard.
bottles (50) - cardboard boxes.
Powder for solution preparation for intravenous and intravenous administration 1 fl.
cefoperazone (in the form of the sodium salt) 500 mg
bottles (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
Cephalosporin semisynthetic antibiotic III generation of a broad spectrum of action. Has a bactericidal effect by inhibiting the synthesis of the cell wall of microorganisms: acetylates membrane-bound transpeptidases, thereby violating the cross-linking of peptidoglycans necessary to ensure the strength and rigidity of the cell wall.
Active in relation to:
- Gram-positive microorganisms: Staphylococcus aureus (strains producing and non-producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococcus), Streptococcus agalactiae (group B beta-hemolytic streptococcus, Streptococcus faecalis;
- Gram-negative microorganisms: Esherichia coli, Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Citrobacter spp., Haemophilus influenzae (strains producing and non-producing beta-lactamases), Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii, Serratia marcescens, Salmonella spp. and Shigella spp., Pseudomonas spp., including Pseudomonas aeruginosa, some strains of Acinetobacter spp. Neisseria gonorrhoeae (strains producing and not producing beta-lactamases) and Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica;
- Anaerobic microorganisms: Gram-positive cocci (including Peptococcus spp., Peptostreptococcus spp.), gram-positive sporo- and non-spore-forming anaerobes (Clostridium difficile, Eubacterium spp., Lactobacillus spp.) and Gram-negative rods (including Fusobacterium spp., some strains of Bacteroides fragilis, and other Vasteroides spp.).
PHARMACOKINETICS
TC max after intramuscular injection - 1-2 hours; after intravenous administration - at the end of the infusion. C max in the blood serum after intramuscular injection of 0.25 g and 0.5 g of cefoperazone is 22 Ојg / ml and 33 Ојg / ml, respectively. C max for intravenous administration of 1 g and 2 g of the drug is 153 Ојg / ml and 252 Ојg / ml, respectively.
The connection with plasma proteins is 82-93%.
Cefoperazone reaches therapeutic concentrations in the tissues and body fluids: ascitic, peritoneal, synovial fluid, urine, bile and gallbladder walls, lungs, sputum, palatine tonsils, sinus mucosa, atria, kidneys, ureters, prostate, testicles, uterus, fallopian tubes, bones, cord blood, amniotic fluid, as well as in cerebrospinal fluid (with meningitis). In small concentrations, cefoperazone can be found in breast milk.
The volume of distribution is 0.14 - 2 l / kg. T 1/2 is an average of 2 hours, regardless of the mode of administration, 2.8 to 4.2 hours for hemodialysis, 2.2 hours for newborns and children from 2 months to 11 years. It is output in active form (meta-bolziruetsya less than 1%) 70-80% with bile, 20-30% - kidneys. In patients with impaired liver function and bile duct 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 is elongated only 2-4 times. In patients with renal-hepatic insufficiency can cumulate.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper and lower respiratory tract;
- urinary tract infections;
- skin and soft tissue infections;
- infections of bones and joints;
- Infectious inflammatory diseases of the pelvic organs (endometritis, gonorrhea);
- abdominal infections (peritonitis, cholecystitis, cholangitis);
- sepsis;
- Meningitis.
Prevention of infectious complications in abdominal, gynecological and traumatological operations, as well as in cardiovascular surgery.
DOSING MODE
Intravenous (drip, jet), intramuscularly.
Adults: an average daily dose of cefoperazone 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 - to 1 g or 2 g IV for 30-90 minutes before the operation. The dose can be repeated every 12 hours, however, in most cases, for no more than 24 hours.
In case of operations with an increased risk of infection (for example, operations in the rectal area), or if the infection is particularly dangerous (for example, in open-heart surgery or joint replacement), 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 a serum creatinine level above 3.5 mg / dL should not exceed a daily dose of 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 of 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. Efficacy and safety of use in children has not been established to date.
Intravenous administration
A solution for intravenous administration is prepared ex tempore.
As a solvent, -5% dextrose solution, 10% dextrose solution, 0.9% sodium chloride solution, 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 of droplets to facilitate dissolution, it is recommended to use 5 ml of solvent per 1 g of cefoperazone. The resulting solution is added to the infusion solution (Ringer's lactate solution, 5% dextrose solution, 0.9% sodium chloride solution) in a volume of 20-100 ml. The duration of administration depending on the volume of the solution can be from 10-30 minutes or more.
Intramuscular injection
To prepare solutions for intravenous injections, sterile water for injection or 0.9% 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 pain with intramuscular injections, when a solution with a concentration of 250 mg / ml or more is intended to be administered, a 2% solution of lidocaine is recommended for 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, maculopapular rash, fever, eosinophilia, erythema multiforme, itching, malignant exudative erythema (Stevens-Johnson syndrome), rarely - Quincke's edema, anaphylactic shock.
From the digestive tract: nausea, vomiting, diarrhea, pseudomembranous colitis.
Laboratory indices: hypoprothrombinemia, increased prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, transient hypercreatininemia, transient eosinophilia, decrease in hematocrit, positive Coombs reaction.
On the part of the organs of hematopoiesis: anemia, reversible neutropenia (with prolonged use), bleeding.
Local reactions: phlebitis (with intravenous administration), soreness at the injection site (with intramuscular injection).
Other: Candidiasis.
CONTRAINDICATIONS
- hypersensitivity to cephalosporins and other beta-lactam antibiotics.
With caution: renal and hepatic insufficiency, colitis in the anamnesis.
PREGNANCY AND LACTATION
Cefoperazone can be used during pregnancy if the intended benefit to the mother exceeds the potential risk to the fetus. When appointing cefoperazona during lactation it is necessary to stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: liver failure.
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.
Patients with hypersensitivity to penicillins may have cross-allergic reactions to cephalosporin antibiotics, including cefoperazone.
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 with cefoperazonom and within 5 days after it is completed, you should refrain from taking ethanol, because it is possible to develop a disulfiramylate reaction.
Patients with a malabsorption of food (for example, suffering from muco-viscidosis), as well as patients who have been on parenteral nutrition for a long time, may have vitamin K deficiency. Such patients should be monitored for prothrombin time and, if necessary, shows the appointment of exogenous vitamin K.
Long-term use can lead to the development of resistance of the pathogen. In case of obstruction of the bile duct, severe liver disease or concomitant renal dysfunction, it may be necessary to change the dosage regimen.
OVERDOSE
Symptoms: epileptic seizure.
Treatment: diazepam administration, symptomatic therapy.
DRUG INTERACTION
Do not mix cefoperazone solution in one syringe with aminoglycosides due to the chemical-physical incompatibility (if necessary, combination therapy with these drugs, cefoperazone and aminoglycoside is given as a sequential fractional intravenous injection, using two separate intravenous catheters).
Non-steroidal anti-inflammatory drugs (diclofenac, ibuprofen, indomethacin, ketorolac, etc.), indirect anticoagulants, heparin, thrombolytics and antiaggregants (dipyridamole, alprostadil, etc.) increase the frequency of hypoprothrombinemia, increase the risk of bleeding.
Aminoglycosides and looped diuretics increase the risk of developing nephrotoxicity, especially in people with kidney failure.
When co-administration of cefoperazone with ethanol is co-administered, or if the interval between their administrations is less than 5 days, a disulfiram-like reaction may occur in the form of hyperemia, nausea, vomiting, headache, dyspnea, tachycardia, lowering of blood pressure, abdominal cramps.
Drugs that reduce tubular secretion, increase the concentration of the drug in the blood and slow its elimination.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dry, dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 3 years.
