Composition, form of production and packaging
Powder for solution for iv and in / m introduction white or white with a yellowish or yellowish brown tinge.
1 f.
ceftazidime (in the form of pentahydrate) 0.5 g
Excipients: sodium carbonate - 0.05 g.
Solvent: water d / and.
0.5 g - bottles (1) - packs of cardboard.
0.5 g - bottles (5) - packs of cardboard.
0.5 g - bottles (10) - packs of cardboard.
0.5 g - bottles (1) complete with a solvent of 5 ml amp. 1 PC. - packings of cellular contour (1) - packs cardboard.
0.5 g - bottles (1) complete with a solvent of 5 ml amp. 2 pcs. - packings of cellular contour (1) - packs cardboard.
0.5 g - bottles (1) complete with a solvent of 5 ml amp. 1 PC. - packs cardboard.
0.5 g - bottles (1) complete with a solvent of 5 ml amp. 2 pcs. - packs cardboard.
0.5 g - bottles (5) - packings of cellular contour (1) complete with a solvent of 5 ml amp. 5 pieces. in the packaging of the cellular contour (1 pc.) - packs of cardboard.
0.5 g - bottles (5) - packings of cellular contour (1) complete with a solvent of 5 ml amp. 5 pieces. in the package of a cellular contour (2 pieces) - packs cardboard.
0.5 g - bottles (50) - cardboard boxes (for hospitals).
Powder for solution for iv and in / m introduction white or white with a yellowish or yellowish brown tinge.
1 f.
ceftazidime (in the form of pentahydrate) 1 g
Excipients: sodium carbonate - 0.1 g.
Solvent: water d / and.
1 g - bottles (1) - packs of cardboard.
1 g - bottles (5) - packs of cardboard.
1 g - bottles (10) - packs of cardboard.
1 g - bottles (1) complete with a solvent of 5 ml amp. 1 PC. - packings of cellular contour (1) - packs cardboard.
1 g - bottles (1) complete with a solvent of 5 ml amp. 2 pcs. - packings of cellular contour (1) - packs cardboard.
1 g - bottles (1) complete with a solvent of 5 ml amp. 1 PC. - packs cardboard.
1 g - bottles (1) complete with a solvent of 5 ml amp. 2 pcs. - packs cardboard.
1 g - vials (5) - packings of cellular contour (1) complete with a solvent of 5 ml amp. 5 pieces. in the packaging of the cellular contour (1 pc.) - packs of cardboard.
1 g - vials (5) - packings of cellular contour (1) complete with a solvent of 5 ml amp. 5 pieces. in the package of a cellular contour (2 pieces) - packs cardboard.
1 g - bottles (1) - packs of cardboard.
1 g - bottles (50) - cardboard boxes (for hospitals).
Powder for solution for iv and in / m introduction white or white with a yellowish or yellowish brown tinge.
1 f.
ceftazidime (in the form of pentahydrate) 2 g
Excipients: sodium carbonate - 0.2 g.
Solvent: water d / and.
2 g - vials (1) - packs of cardboard.
2 g - bottles (5) - packs of cardboard.
2 g - bottles (10) - packs of cardboard.
2 g - vials (1) complete with a solvent of 5 ml amp. 1 PC. - packings of cellular contour (1) - packs cardboard.
2 g - vials (1) complete with a solvent of 5 ml amp. 2 pcs. - packings of cellular contour (1) - packs cardboard.
2 g - vials (1) complete with a solvent of 5 ml amp. 1 PC. - packs cardboard.
2 g - vials (1) complete with a solvent of 5 ml amp. 2 pcs. - packs cardboard.
2 g - vials (5) - packings of cellular contour (1) complete with a solvent of 5 ml amp. 5 pieces. in the packaging of the cellular contour (1 pc.) - packs of cardboard.
2 g - vials (5) - packings of cellular contour (1) complete with a solvent of 5 ml amp. 5 pieces. in the package of a cellular contour (2 pieces) - packs cardboard.
2 g - bottles (50) - cardboard boxes (for hospitals).
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
Antibiotic group cephalosporins III generation of a broad spectrum of action for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Resistant to the action of most ОІ-lactamases. Effects on many strains resistant to ampicillin and other cephalosporins.
The drug is active against gram-negative microorganisms: Pseudomonas spp. (including Pseudomonas aeruginosa), Klebsiella spp. (including Klebsiella pneumoniae), Proteus mirabilis, Proteus vulgaris, Escherichia coli, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter cloacae), Citrobacter spp. (including Citrobacter diversus, Citrobacter freundii), Pasteurella multocida, Neisseria meningitidis, Haemophilus influenzae (including strains resistant to ampicillin); Gram-positive microorganisms: Staphylococcus aureus (producing and not producing penicillinase strains sensitive to methicillin), Streptococcus pyogenes (group A beta-hemolytic streptococcus), Streptococcus agalactiae (group B), Streptococcus pneumoniae; anaerobic microorganisms: Bacteroides spp. (but many strains of Bacteroides fragilis are resistant).
It is active in vitro against most strains of the following microorganisms (the clinical significance of this activity is unknown): Clostridium perfringens, Acinetobacter spp., Haemophilus parainfluenzae, Morganella morganii, Neisseria gonorrhoeae, Peptococcus spp., Peptostreptococcus spp., Providencia spp., Incl. Providencia rettgeri, Salmonella spp., Shigella spp., Staphylococcus epidermidis, Yersinia enterocolitica.
Not active against methicillin-resistant Staphylococcus spp., Streptococcus faecalis, Enterococcus spp .; Listeria monocytogenes, Campylobacter spp. and Clostridium difficile.
PHARMACOKINETICS
Suction
After i / m administration of the drug in a dose of 0.5 g or 1 g of C max is achieved after 1 hour and is 17 Ојg / ml and 39 Ојg / ml, respectively; after iv bolus administration in doses of 0.5 g, 1 g or 2 g of C max is respectively 42 Ојg / ml, 69 Ојg / ml and 170 Ојg / ml.
Therapeutic effective serum concentrations after IM and IV administration are maintained for 8-12 hours.
Distribution
Binding to blood plasma proteins - 10%.
Concentrations of ceftazidime exceeding the MIC for the most common pathogens can be achieved in bone tissue, heart, bile, sputum, synovial fluid, intraocular, pleural and peritoneal fluids. It easily penetrates the placental barrier and is excreted in breast milk. In the absence of an inflammatory process in the meningeal membranes, ceftazidime poorly penetrates the BBB, the concentration of the drug in the cerebrospinal fluid is low. With meningitis in the cerebrospinal fluid, therapeutic concentrations of ceftazidime are achieved, which are 4-20 mg / l and higher.
Metabolism and excretion
Ceftazidime is not metabolized in the body. T 1/2 - about 2 hours, in newborns - 3-4 times more than in adults. Ceftazidime is excreted unchanged by kidneys by glomerular filtration. Approximately 80-90% of the dose is excreted by the kidneys within 24 hours. Less than 1% of the drug is excreted with bile.
Pharmacokinetics in special clinical cases
If the renal function is impaired, the rate of excretion of ceftazidime is reduced. With hemodialysis, T 1/2 is 3-5 hours.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- Severe infections, including nosocomial infections (septicemia, bacteremia, peritonitis, meningitis, infections in patients with reduced immunity, infected burns);
- Urinary tract infection (acute and chronic pyelonephritis, pyelitis, prostatitis, cystitis, urethritis (bacterial only), kidney abscess);
- Lower respiratory tract infections (acute and chronic bronchitis, infected bronchiectasis, pneumonia caused by gram-negative bacteria, lung abscess, pleural empyema, lung infections in patients with cystic fibrosis);
- infections of the skin and soft tissues (mastitis, wound infections, skin ulcers, phlegmon, erysipelas);
- infections of bones and joints (septic arthritis, osteomyelitis, bacterial bursitis);
- infections of the gastrointestinal tract, abdominal cavity and biliary tract (enterocolitis, retroperitoneal abscesses, diverticulitis, pelvic inflammatory disease, cholecystitis, cholangitis, empyema of the gallbladder);
- infections of the pelvic organs and female genital organs;
- gonorrhea (especially with increased sensitivity to antibacterial drugs from the penicillin group);
- infections of the ear, throat, nose (otitis media, sinusitis, mastoiditis).
DOSING MODE
The drug Ceftazidim-AKOS is used only parenterally: iv (jet or drip) or IM. The dose of the drug is set individually, taking into account the severity of the disease, the localization of infection, the type and sensitivity of the pathogen, age and function of the kidneys.
The drug is administered iv in (jet or drip) or deep in / m in the region of the upper outer quadrant of the gluteus maximus or in the region of the lateral part of the thigh. The solution of ceftazidime can be injected directly into the vein or into the tube of the infusion system.
The usual dose for adults and children over 12 years is 1 g IM or IV every 8-12 hours.
In uncomplicated infections of the urinary tract - in / m or / in the 250 mg every 12 hours.
With complicated infections of the urinary tract - in / m or / in the 0.5-1 g every 8-12 hours.
With uncomplicated pneumonia, infections of the skin and soft tissue - in / m or / in the 0.5-1 g every 8 hours.
In cystic fibrosis, respiratory infections caused by Pseudomonas spp. - IV in the dose of 100-150 mg / kg / day, the frequency of administration - 3 times / day (dose up to 9 g / day in such patients did not cause complications).
When infections of bones and joints - in / in 2 g every 12 hours.
In severe infections, including intrahospital - in / in 2 g every 8 hours.
In extremely severe or life-threatening infections - in / in 2 g every 8 h.
For elderly patients, the maximum daily dose should not exceed 3 g.
Patients with renal insufficiency require a dose reduction because ceftazidime is excreted by the kidneys unchanged. The initial dose is 1 g. The maintenance dose is selected depending on the rate of glomerular filtration.
Creatinine clearance
> 50 ml / min (> 0.83 ml / s) Usual dose for adults and children over 12 years of age
35-50 ml / min (0.52-0.83 ml / sec) 1 g every 12 h
16-30 ml / min (0.27-0.5 ml / sec) 1 g every 24 hours
6-15 ml / min (0.1-0.25 ml / s) for 500 mg every 24 hours
<5 ml / min (<0.08 ml / sec) of 500 mg every 48 hours
Patients on hemodialysis for 1 g after each hemodialysis session
Patients on peritoneal dialysis at 500 mg every 24 hours
Patients with severe infections can increase the maintenance dose by 50% or increase the frequency of administration of the drug. In this case, the level of ceftazidime should be monitored in serum, the serum concentration of ceftazidime should not exceed 40 mg / l.
For children, the clearance of creatinine is calculated according to the ideal mass or surface area of ​​the body.
T 1/2 of the drug during hemodialysis is 3-5 hours. The appropriate dose of the drug should be repeated after each period of dialysis.
With peritoneal dialysis, ceftazidime can be included in the dialysis solution at a dose of 125 mg to 250 mg per 2 liters of dialysis solution.
In patients with renal insufficiency, on continuous hemodialysis using an arteriovenous shunt, and in patients who are on high-speed haemofiltration in the intensive care unit , the recommended dose is 1 g / day daily (in 1 or more injections).
Patients on low-speed haemofiltration are prescribed doses recommended for renal dysfunction.
Children under 2 months are prescribed 25-60 mg / kg / day (in 2 injections).
Children from 2 months to 12 years are prescribed 30-100 mg / kg / day (in 2-3 injections).
Children with reduced immunity, cystic fibrosis and meningitis - 150 mg / kg / day (in 3 injections).
The maximum daily dose of ceftazidime for children is 6 g.
Duration of treatment
The duration of treatment with ceftazidime is 7-14 days. In infections caused by Pseudomonas aeruginosa (pneumonia, cystic fibrosis, meningitis), the course of treatment can be increased to 21 days.
Rules for the preparation of solutions
When the powder is dissolved, carbon dioxide (carbon dioxide) is released. After the introduction of the solvent, the vial must be shaken to obtain a clear solution. In the finished product solution prepared, small bubbles of carbon dioxide (carbon dioxide) may be present.
The resulting solution may have a color from light yellow to dark yellow. If all the recommended rules for dilution of the drug are observed, then its effectiveness does not depend on the shade.
Primary dilution
Dose Volume of the dissolver for the / m introduction Volume of the diluent for intravenous administration
500 mg 1.5 ml water for injection or 0.5% or 1% lidocaine hydrochloride solution 5 ml water for injection
1 g or 2 g 3 ml water for injection or 0.5% or 1% lidocaine hydrochloride solution 10 ml water for injection
Secondary breeding
For intravenous administration, the solution of the preparation Ceftazidime-AKOS obtained in the above described way is further diluted in 50-100 ml of one of the following solvents intended for intravenous administration (0.9% sodium chloride solution, Ringer's solution, 5% or 10% dextrose solution glucose), 5% dextrose (glucose) solution with 0.9% sodium chloride solution.For reconstitution only freshly prepared solution should be used.
SIDE EFFECT
Allergic reactions: urticaria, chills or fever, rash, itching, bronchospasm, eosinophilia, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), angioedema, anaphylactic shock.
On the part of the digestive system: nausea, vomiting, diarrhea, flatulence, abdominal pain, dysbiosis, increased activity of hepatic transaminases, alkaline phosphatase, hyperbilirubinemia, stomatitis, glossitis, pseudomembranous enterocolitis, oropharyngeal candidiasis, cholestasis.
On the part of the hematopoiesis system: eosinophilia, leukopenia, neutropenia, agranulocytosis, granulocytopenia, thrombocytopenia, hemolytic anemia, lymphocytosis, hemorrhages.
On the part of the reproductive system: candidiasis vaginitis.
From the urinary system: a violation of kidney function, toxic nephropathy.
From the side of the central nervous system: headache, dizziness, paresthesia, dizziness, convulsive seizures, encephalopathy, "fluttering tremor."
Laboratory indicators: hypercreatininaemia, increased urea concentration, false positive urine reaction to glucose, false positive Coombs' direct reaction, increase in prothrombin time.
Local reactions: with iv injection, phlebitis; with the / m introduction - soreness, burning, compaction at the injection site.
Other: nosebleeds, superinfection.
CONTRAINDICATIONS
- hypersensitivity to the components of the drug;
- Hypersensitivity to cephalosporins and penicillins.
With caution: renal failure, colitis in history, malabsorption syndrome (increased risk of decreased prothrombin activity, especially in persons with severe renal and / or liver failure), simultaneous administration with loop diuretic and aminoglycoside, as well as newborns.
PREGNANCY AND LACTATION
In pregnancy, the drug is used only if the intended benefit to the mother exceeds the potential risk to the fetus and the baby. When using the drug during lactation, breast-feeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal insufficiency require a dose reduction because ceftazidime is excreted by the kidneys in an unchanged form. The initial dose is 1 g. The maintenance dose is selected depending on the rate of glomerular filtration.
QC Dose
> 50 ml / min (> 0.83 ml / s) Usual dose for adults and children over 12 years of age
35-50 ml / min (0.52-0.83 ml / sec) 1 g every 12 h
16-30 ml / min (0.27-0.5 ml / sec) 1 g every 24 hours
6-15 ml / min (0.1-0.25 ml / s) for 500 mg every 24 hours
<5 ml / min (<0.08 ml / sec) of 500 mg every 48 hours
Patients on hemodialysis for 1 g after each hemodialysis session
Patients on peritoneal dialysis at 500 mg every 24 hours
Patients with severe infections can increase the maintenance dose by 50% or increase the frequency of administration of the drug. In this case, the level of ceftazidime should be monitored in serum, the serum concentration of ceftazidime should not exceed 40 mg / l.
For children, the clearance of creatinine is calculated according to the ideal mass or surface area of ​​the body.
T 1/2 of the drug during hemodialysis is 3-5 hours. The appropriate dose of the drug should be repeated after each period of dialysis.
With peritoneal dialysis, ceftazidime can be included in the dialysis solution at a dose of 125 mg to 250 mg per 2 liters of dialysis solution. In patients with renal insufficiency, on continuous hemodialysis using an arteriovenous shunt, and in patients who are on high-speed haemofiltration in the intensive care unit , the recommended dose is 1 g / day daily (for one or more injections).
Patients on low-speed haemofiltration are given doses recommended for kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug in patients with impaired liver function.
APPLICATION FOR CHILDREN
Children under 2 months are prescribed 25-60 mg / kg / day (in 2 injections).
Children from 2 months to 12 years are prescribed 30-100 mg / kg / day (in 2-3 injections).
Children with reduced immunity, cystic fibrosis and meningitis - 150 mg / kg / day (in 3 injections).
The maximum daily dose for children is 6 g.
APPLICATION IN ELDERLY PATIENTS
For elderly patients, the maximum daily dose should not exceed 3 g.
SPECIAL INSTRUCTIONS
Patients with a history of allergic reactions to penicillins may have increased sensitivity to cephalosporin antibiotics.
Do not use ethanol during treatment.
When using the drug and after 2-3 weeks after discontinuation of treatment, it is possible to develop diarrhea caused by Clostridium difficile. In mild cases, it is sufficient to cancel treatment and use ion-exchange resins (colestyramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole. Do not use drugs that inhibit the intestinal motility.
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions due to the risk of dizziness.
OVERDOSE
Symptoms: pain, inflammation, phlebitis at the injection site, dizziness, paresthesia, headache, convulsions in patients with renal insufficiency, hypercreatininaemia, hyperbilirubinemia, thrombocytosis, thrombocytopenia, eosinophilia, leukopenia, lengthening prothrombin time.
Treatment: conduct symptomatic therapy, in the case of renal failure - peritoneal dialysis or hemodialysis.
DRUG INTERACTION
Synergism of antibacterial action with simultaneous application with aminoglycosides is noted.
"Loopback" diuretics, aminoglycosides, vancomycin, clindamycin reduce the clearance of ceftazidime, which increases the risk of nephrotoxic action.
Bacteriostatic antibiotics (including chloramphenicol) reduce the effect of the drug.
Pharmaceutical interaction
Do not use sodium bicarbonate solution as a solvent (carbon dioxide is formed, this may require the gas to be discharged outside).
Pharmacologically incompatible with aminoglycosides (significant mutual inactivation: with simultaneous use these drugs should be administered to different parts of the body) and vancomycin (forms a precipitate depending on the concentration, if necessary, administer two drugs through a single tube, between their application of the IV system should be Rinse).
Pharmaceutically compatible with the following solutions: at a concentration of 1 to 40 mg / ml - sodium chloride 0.9%, sodium lactate, Hartman solution, dextrose (glucose) 5%, sodium chloride 0.225% and dextrose (glucose) 5%, sodium chloride 0.45% and dextrose (glucose) 5%, sodium chloride 0.9% and dextrose (glucose) 5%, sodium chloride 0.18% and dextrose (glucose) 4%, dextrose (glucose) 10%, dextran 40 (10%) in a solution of sodium chloride 0.9 %, dextran 40 (10%) in a solution of dextrose (glucose) 5%, dextran 70 (6%) in a solution of sodium chloride 0.9%, dextran 70 (6%) in a solution of dextrose (glucose) 5%.
At a concentration of 0.05 to 0.25 mg / ml, ceftazidime is compatible with the solution for intraperitoneal dialysis (lactate).
For the / m administration ceftazidime can be diluted with a solution of lidocaine hydrochloride 0.5% or 1%. Both components are active if ceftazidime is added to the following solutions (concentration of ceftazidime 4 mg / mL) hydrocortisone (hydrocortisone sodium phosphate) 1 mg / ml in sodium chloride 0.9% or dextrose (glucose) 5%, cefuroxime (cefuroxime sodium ) 3 mg / ml in chloride 0.9% solution of sodium, cloxacillin (cloxacillin sodium) 4 mg / ml in sodium chloride 0.9%, heparin 10 IU / ml in sodium chloride 0.9% potassium chloride, 10 meq / liter or 40 mEq / l sodium chloride 0.9%.
When mixing a solution of ceftazidime (500 mg in 1.5 ml of water for injection) and metronidazole (500 mg / 100 ml), both components remain active.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 3 years.
