Ceftazidime-Acos, vials, 1g

Composition

1 bottle of powder for the preparation of a solution for injection contains:

Active ingredient:

1.0 g ceftazidime sodium carbonate pentahydrate (based on ceftazidime)

Pharmacological action

The drug Ceftazidim is an antibacterial drug from the group of cephalosporins of the third generation, has a wide spectrum and acts bactericidal, disrupts the synthesis of the cell wall of microorganisms, and is resistant to the action of most beta-lactamases. The drug is active against gram-negative microorganisms: Haemophilus influenzae, Neisseria gonorrhoeae and other Neisseria spp. and most representatives of the Enterobacteriaceae family (Citrobacter spp., Enterobacter spp., Escherichia coli, Klebsiella pneumoniae and others Klebsiella spp., Morganella morganii and others Morganella spp., Proteus mirabilis (including indole positive), Proteus vulgaris and others Proteus spp., Providensia rettgeri and others Providencia spp. and Serratia spp. ), Acinetobacter spp., Haemophilus parainfluenzae (including ampicillin-resistant strains), Pasteurella multocida. Salmonella spp., Shigella spp. and Yersinia enterocolitica.

Ceftazidime has the highest activity among third-generation cephalosporins against Pseudomonas aeruginosa and intrahospital infection. The drug is active against gram-positive bacteria: Micrococcus spp., Streptococcus aureus, Streptococcus mitis, Streptococcus pneumoniae, Streptococcus pyogenes group A, Streptococcus viridans and other Streptococcus spp. (excluding Streptococcus faecalis); strains sensitive to methicillin: Staphylococcus aureus, Staphylococcus epidermidis.

Ceftazidime is active against anaerobic bacteria: Bacteroides spp. (most strains of Bacteroides fragilis are resistant), Clostridium perfringens, Peptococcus spp., Peplostreptococcus spp. and Propionobacterium spp. The drug is not active against methicillin-resistant strains of CamPylobacter spp., Chlamydia spp., Clostridium difficile, Enterococcus spp., Listeria monocytogenes and other Listeria spp., Staphylococcus aureus and Staphylococcus epidermidis; Streptococcus faecalis.

Pharmacokinetics

After use, the drug is rapidly distributed in the human body and reaches therapeutic concentrations in most tissues and fluids, including synovial, pericardial and peritoneal fluids, as well as in bile, sputum and urine. Distribution also occurs in the bones, myocardium, gallbladder, skin and soft tissues in concentrations sufficient for the treatment of infectious diseases, especially in inflammatory processes that increase the diffusion of the drug. Poorly penetrates the intact blood-brain barrier, but the therapeutic level achieved by the drug in the cerebrospinal fluid is sufficient for the treatment of meningitis.

Reversibly binds to plasma proteins (less than 15%), and has a bactericidal effect only in free form. The degree of protein binding is independent of concentration. The maximum concentration with intramuscular use of 0.5 g or 1 g after an hour, respectively, is 17 mcg/ml and 39 mcg/ml, with intravenous use, respectively,42 mcg/ml and 69 mcg/ml. The time to reach the maximum concentration with intramuscular use is 1 hour, with intravenous use-by the end of the infusion. The concentration of the drug, equal to 4 micrograms / ml, is maintained for 6-8 hours. The therapeutic concentration in the blood plasma is maintained for 8-12 hours.

The elimination half-life is 1.8 hours for normal renal function and 2.2 hours for impaired renal function. The drug is not metabolized in the liver, and impaired liver function does not affect the Pharmacodynamics and pharmacokinetics of the drug. The dose in such patients remains normal. It is excreted unchanged by the kidneys up to 80-90% (70% of the administered dose is excreted in the first 4 hours) during the day by glomerular filtration and tubular secretion equally.

If renal function is impaired, a dose reduction is recommended. The volume of distribution is 0.21-0.28 l / kg. The drug accumulates in soft tissues, kidneys, lungs, bones and joints, serous cavities.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• severe infections, including nosocomial (septicemia, bacteremia, peritonitis, meningitis, infections in patients with reduced immunity, infected burns);
• urinary tract infections (acute and chronic pyelonephritis, pyelitis, prostatitis, cystitis, urethritis /only bacterial/, abscess of the kidney);
• infections of the lower respiratory tract (acute and chronic bronchitis, infected bronchiectasis, pneumonia caused by gram-negative bacteria, lung abscess, empyema, lung infection in cystic fibrosis patients);
• infections of skin and soft tissue (mastitis, wound infections, skin ulcers, cellulitis, erysipelas);
• infections of bones and joints (septic arthritis, osteomyelitis, bacterial bursitis);
• infections of the gastrointestinal tract, abdominal cavity and the biliary tract (enterocolitis, retroperitoneal abscess, diverticulitis, inflammation of the pelvic organs, cholecystitis, cholangitis, empyema of the gall bladder);
• infection of the pelvic organs and female reproductive organs;
• gonorrhea (especially if you are sensitive to antibiotics of penicillin group);
• infections of ear, throat, nose (otitis media, sinusitis, mastoiditis).

Use during pregnancy and lactation

During pregnancy, the drug is used only if the intended benefit to the mother exceeds the potential risk to the fetus and child. When using the drug during lactation, breast-feeding should be discontinued.

Contraindications

• hypersensitivity to the components of the drug Ceftazidime-AKOS;
• hypersensitivity to cephalosporins and penicillins.

With caution: renal failure, a history of colitis, malabsorption syndrome (increased risk of decreased prothrombin activity, especially in patients with severe renal and/or hepatic insufficiency), simultaneous use with a loop diuretic and aminoglycoside, as well as newborns.

Side effects

Allergic reactions: urticaria, chills or fever, rash, pruritus, bronchospasm, eosinophilia, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), angioedema, anaphylactic shock.

From 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.

From the hematopoietic system: eosinophilia, leukopenia, neutropenia, agranulocytosis, granulocytopenia, thrombocytopenia, hemolytic anemia, lymphocytosis, hemorrhages.

From the genital system: candida vaginitis.

From the urinary system: impaired renal function, toxic nephropathy.

From the central nervous system: headache, dizziness, paresthesia, dizziness, convulsive seizures, encephalopathy, “fluttering tremor”.

Laboratory parameters: hypercreatininemia, increased urea concentration, false positive urine glucose response, false positive direct Coombs reaction, increased prothrombin time.

Local reactions: with intravenous use-phlebitis; with intramuscular use-soreness, burning, compaction at the injection site.

Other services: nosebleeds, superinfection.

Interaction

Pharmacologically incompatible with aminoglycosides, heparin, and vancomycin. Do not use sodium bicarbonate solution as a solvent. Loop diuretics, aminoglycosides, vancomycin, and clindamycin reduce the clearance of ceftazidime, which increases the risk of nephrotoxic effects.

Pharmaceutically compatible with the following solutions: at a concentration of 1 to 40 mg/ml / sodium chloride 0,9% sodium lactate, Hartmann’s solution, dextrose 5%, sodium chloride 0,225% and dextrose 5%, sodium chloride 0.45% and dextrose 5%, sodium chloride 0.9% and dextrose 5%, sodium chloride 0.18% and dextrose 4%, dextrose 10%, dextran 40: a 10% solution of sodium chloride 0,9%, dextran 40: 10% in dextrose 5%, dextran 70: 6% in the solution of sodium chloride 0,9%, dextran 70: 6% in dextrose 5%. At concentrations from 0.05 to 0.25 mg/ml, ceftazidime is compatible with intraperitoneal dialysis solution (lactate).

For intravenous use, ceftazidime can be diluted with a 0.5% or 1% lidocaine hydrochloride solution. Both components remain active if ceftazidime is added to the following solutions (ceftazidime concentration is 4 mg/ml): hydrocortisone (hydrocortisone sodium phosphate) 1 mg/ml in 0.9% sodium chloride solution or 5% dextrose solution, cefuroxime (cefuroxime sodium) 3 mg/ml in 0.9% sodium chloride solution, cloxacillin (cloxacillin sodium) 4 mg/ml in 0.9% sodium chloride solution, heparin 10 IU/ml or 50 IU/ml in 0.9% sodium chloride solution,10 mEk/L potassium chloride or 40 mEk/L in 0.9% sodium chloride solution. When mixing a solution of ceftazidime (500 mg in 1.5 ml of water for injection) and metronidazole (500 mg/100 ml), both components retain their activity.

How to take it, course of use and dosage

Ceftazidime-AKOS is used only parenterally: intravenously (jet or drip) or intramuscularly. The dose of the drug is determined individually, taking into account the severity of the disease, the location of the infection, the type and sensitivity of the pathogen, age and kidney function.

The drug is administered intravenously (jet or drip) or deep intramuscularly in the upper outer quadrant of the gluteus maximus muscle or in the lateral part of the thigh. Ceftazidime solution 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 of age is 1 g intramuscularly or intravenously every 8-12 hours.

For uncomplicated urinary tract infections-intramuscularly or intravenously 250 mg every 12 hours.

For complicated urinary tract infections-iv or intravenously 0.5-1 g every 8-12 hours.

For uncomplicated pneumonia, skin and soft tissue infections-intramuscularly or intravenously 0.5-1 g every 8 hours.

In cystic fibrosis, respiratory tract infections caused by Pseudomonas spp. – intravenously at a dose of 100-150 mg / kg / day, the frequency of use is 3 times/day (the use of a dose of up to 9 g / day in such patients did not cause complications).

For infections of bones and joints-intravenously 2 g every 12 hours.

For severe infections, including nosocomial infections-2 g intravenously every 8 hours.

For extremely severe or life-threatening infections-intravenously 2 g every 8 hours.

In elderly patients, the maximum daily dose should not exceed 3 g.

Patients with renal insufficiency need to reduce the dose, because ceftazidime is excreted unchanged by the kidneys. The initial dose is 1 g. The maintenance dose is selected depending on the glomerular filtration rate.

Creatinine clearance > 50 ml / min (>>0.83 ml / sec)The usual dose for adults and children over 12 years of age is 35-50 ml / min (0.52-0.83 ml / sec).1 g every 12 hours 16-30 ml / min(0.27-0.5 ml / sec)1 g every 24 hours 6-15 ml / min(0.1-0.25 ml / sec)500 mg every 24 hours<5 ml / min (<0.08 ml / sec)500 mg every 48 hours Patients on hemodialysis 1 g after each session of hemodialysis Patients on peritoneal dialysis 500 mg every 24 hours

Patients with severe infections can increase the maintenance dose by 50% or increase the frequency of drug use. In this case, the level of ceftazidime in the blood serum should be monitored, while the serum concentration of ceftazidime should not exceed 40 mg/l.

For children, creatinine clearance is calculated according to the ideal body weight or surface area.

T1 / 2 of the drug during hemodialysis is 3-5 hours. The appropriate dose of the drug should be repeated after each dialysis period.

In 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 undergoing continuous hemodialysis using an arteriovenous shunt, and in patients undergoing high-speed hemofiltration in the intensive care unit, the recommended dose is 1 g / day daily (in 1 or several injections).

In patients who are on low-rate hemofiltration, the recommended doses are prescribed for impaired renal function.

Children under 2 months of age 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. For infections caused by Pseudomonas aeruginosa (pneumonia, cystic fibrosis, meningitis), the course of treatment can be extended to 21 days.

Rules for preparing solutions

When the powder is dissolved, carbon dioxide (carbon dioxide) is released. After use of the solvent, the vial must be shaken to obtain a clear solution. Small bubbles of carbon dioxide (carbon dioxide) may be present in the resulting ready-made solution of the drug.

The resulting solution can have a color from light yellow to dark yellow. If all the recommended rules for dilution of the drug are followed, then its effectiveness does not depend on the shade.

Primary breeding

Dosage Volume of blood vessels for intramuscular use Volume of blood vessels for intravenous use 500 mg 1.5 ml of water for injection or 0.5% or 1% lidocaine hydrochloride solution 5 ml of water for injection 1 g or 2 g 3 ml of water for injection or 0.5% or 1% lidocaine hydrochloride solution 10 ml of water for injection

Secondary breeding

For intravenous drip use, the solution of Ceftazidim-AKOS obtained by the method described above is additionally diluted in 50-100 ml of one of the following solvents intended for intravenous use (0.9% sodium chloride solution, Ringer’s solution,5% or 10% dextrose (glucose) solution,5% dextrose (glucose) solution with 0.9% sodium chloride solution. For secondary dilution, only a freshly prepared solution should be used.

Overdose

Symptoms: pain, inflammation, phlebitis at the injection site, dizziness, paresthesia, headache, convulsions in patients with renal insufficiency, hypercreatininemia, hyperbilirubinemia, thrombocytosis, thrombocytopenia, eosinophilia, leukopenia, prolongation of prothrombin time.

Treatment: carry out symptomatic therapy, in case of renal failure – peritoneal dialysis or hemodialysis.

Special instructions

Patients with a history of allergic reactions to penicillins may be hypersensitive to cephalosporin antibiotics.

Do not use ethanol during treatment.

When using the drug and 2-3 weeks after stopping treatment, diarrhea caused by Clostridium difficile may develop.

In mild cases, it is sufficient to cancel treatment and use ion exchange resins (colestyramine, colestipol), in severe cases, compensation for fluid, electrolyte and protein loss is indicated, and the appointment of vancomycin, bacitracin or metronidazole is indicated. Do not use medications that inhibit intestinal motility.

Influence on the ability to drive motor vehicles and manage mechanisms

During treatment, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions due to the risk of dizziness.

Form of production

Powder for preparation of solution for injection

Storage conditions

Store in a dry place, protected from light, at temperatures below 25 °C

Shelf life

2 years

Active ingredient

Ceftazidime

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

For adults as directed by your doctor

Indications

Prostatitis, Skin Infections, Urethritis, Urinary Tract Infections, Pneumonia, Infectious Diseases, Respiratory Tract Infections, Sinusitis, Biliary Tract Infections, Osteomyelitis, Bronchitis, Otitis