Composition, form of production and packaging
Powder for solution for injection from white to light yellow color.
1 f.
cefuroxime (in the form of the sodium salt) 250 mg
- "- 750 mg
- "- 1.5 g
Vials (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Cephalosporin II generation. Cefuroxime is active against a wide range of pathogens, including strains producing ОІ-lactamases. The bactericidal effect of cefuroxime is associated with the suppression of bacterial cell wall synthesis as a result of binding to the main target proteins.
Cefuroxime in vitro is active against gram-negative aerobes: Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Moraxella catarrhalis, Esherichia coli, Klebsiella spp., Proteus mirabilis, Providencia spp., Proteus rettgeri and Neisseria gonorrhoeae (including strains producing and non-producing penicillinase), Neisseria meningitidis, Salmonella spp .; Gram-positive aerobes: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes (and others? -hemolytic streptococci), Streptococcus group B (Streptococcus agalactiae), Streptococcus mitis (viridans group), Bordetella pertussis;anaerobes: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Fusobacterium spp., Propionibacterium spp .; other microorganisms:Borrelia burgdorferi.
Cefuroxime is not sensitive to: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Legionella spp.
PHARMACOKINETICS
Suction
C max of cefuroxime in the plasma after the / m administration, is observed in the period from 30 to 45 minutes, is 27 Ојg / ml and remains for 5.3 hours.
Distribution
Cefuroxime penetrates the GEB, the placental barrier and is excreted in breast milk. Therapeutic concentrations of cefuroxime are created in the bones, skin, soft tissues, synovial, pleural, intraocular fluid, bile, sputum and myocardium. Concentrations of cefuroxime exceeding the minimum inhibitory concentration for most microorganisms can be achieved in bone tissue, synovial and intraocular fluid.
Binding to plasma proteins - 33-50%.
Metabolism and excretion
Cefuroxime is not metabolized. T 1/2 of cefuroxime after parenteral administration is approximately 70 minutes. In newborn infants, T 1/2 cefuroxime may be 3-5 times longer than in adults.
It is excreted by the kidneys through glomerular filtration and tubular secretion. Within 24 hours after parenteral administration, cefuroxime is almost completely (85-90%) excreted unchanged in urine, with most of the drug in the first 6 hours. Serum cefuroxime levels decrease with dialysis.
INDICATIONS
Treatment of diseases caused by bacteria sensitive to cefuroxime:
- infections of the upper and lower respiratory tract (pneumonia, bronchitis, infected bronchiectasis, lung abscess, postoperative infectious diseases of the thorax);
- infections of the ENT organs (otitis media, sinusitis, tonsillitis, pharyngitis);
- urinary tract infections (pyelonephritis, cystitis, asymptomatic bacteriuria, gonorrhea);
- infections of the skin and soft tissues (furunculosis, erysipelas and wound infections);
- infections of bones and joints (osteomyelitis and septic arthritis);
- infection of the pelvic organs;
- septicemia;
- meningitis;
peritonitis.
Prevention of infectious complications in operations on the abdominal organs, pelvis, with orthopedic operations, operations on the heart, lungs, esophagus and vessels.
DOSING MODE
Adults prescribe in / m or / in 750 mg 3 times / day. In more severe cases, the drug is administered IV in a dose of 1.5 g 3 times / day. If necessary, Zinacef can be administered every 6 hours, and the daily dose can be from 3 to 6 g.
In some infections Zinatsef is effectively administered at a dose of 750 mg or 1.5 g 2 times / day (IM or IV) followed by Zinnat's ingestion.
Children prescribe the drug in a dose of 30-100 mg / kg / day in 3-4 divided doses. For most infections, the optimal dose is 60 mg / kg / day.
Newborns are prescribed 30-100 mg / kg / day in 2-3 doses.
To treat gonorrhea appoint 1.5 g once (two doses of 750 mg IM in different places, for example, in both gluteal muscles).
When meningitis, adults are prescribed 3 g IV every 8 hours; Children - 150-250 mg / kg / day iv in 3-4 doses; newborns - 100 mg / kg / day IV.
To prevent infectious complications during surgery on the abdominal cavity, pelvis and orthopedic interventions, Zinacef 1.5 g is given IV during intravenous anesthesia. After 8 h and 16 h after the operation, 750 mg of Zinatsef can additionally be injected in / m.
To prevent infectious complications in operations on the heart, lungs, esophagus and vessels during anesthesia, Zinaceft is administered IV in a dose of 1.5 g, and then for 24-48 hours 750 mg 3 times / day IM.
When the joint is completely replaced, 1.5 g of cefuroxime powder can be mixed with the polymer packet with methyl methacrylate cement before adding the liquid polymer.
Stepwise therapy
With pneumonia, Zinatsef is prescribed in a dose of 1.5 g 2-3 times / day (IV or IM) for 48-72 hours, followed by the appointment of Zinnat (inside) at a dose of 500 mg 2 times / day for 7-10 days .
With exacerbation of chronic bronchitis, Zinatsef is administered at a dose of 750 mg 2-3 times / day (IV or IM) for 48-72 hours, followed by the appointment of Zinnat (inside) 500 mg 2 times / day for 5-10 days .
The duration of each period (parenteral therapy and oral administration) is determined by the severity of the infection and the general condition of the patient.
Renal insufficiency
With renal failure , a dose reduction of Zinatsef is recommended. However, there is no need to reduce the standard dose of the drug (0.75-1.5 g 3 times / day) inpatients with QC more than 20 ml / min .
Correction of dose of Zinacef in renal failure in adults
Creatinine clearance Dose Zinacef
> 20 ml / min 0.75-1.5 g 3 times / day
10-20 ml / min 750 mg 2 times / day
<10 ml / min 750 mg / day
Patients on hemodialysis at the end of each hemodialysis session should be administered an additional dose of Zinatsef, equal to 750 mg.
Patients in the intensive care unit on continuous hemodialysis using an arteriovenous shunt or high-speed hemofiltration are recommended 750 mg twice daily. If hemofiltration is used at a low rate, then doses are used, as in renal failure.
Rules for the preparation of solution for injection
To prepare a solution for intravenous administration , add 1 ml of water for injection to 250 mg of Zinacef or 3 ml of water for injection to 750 mg of Zinacef. Gently shake until a slurry forms.
To prepare the solution for intravenous administration , 250 mg of Zinacef should be dissolved in 2 ml or more of water for injection, 750 mg of Zinacef in 6 ml or more of water for injection, 1.5 g of Zinaceph in 15 ml or more of water for injection.
To prepare a solution for short-term intravenous infusions (up to 30 min), 1.5 g of the drug is dissolved in 50 ml of water for injection. These solutions can be injected directly into the vein or into the tube of the infusion system.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea, spasms and pain in the abdominal cavity, pseudomembranous colitis, candidiasis of the oral cavity, increased activity of liver enzymes (ALT, AST, LDG, AF), hyperbilirubinemia.
On the part of the hematopoiesis system: eosinophilia, leukopenia, neutropenia, thrombocytopenia, agranulocytosis, hemolytic anemia.
From the side of the central nervous system and sensory organs: convulsions, hearing loss.
On the part of the genitourinary system: a violation of kidney function with an increase in the level of creatinine and / or urea nitrogen and decreased QC, itching in the perineum, vaginitis (with the development of candidiasis).
Allergic reactions: exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), skin rash (including urticaria), itching, drug fever, bronchospasm, serum sickness; very rarely - anaphylactic shock.
Laboratory indicators: false-positive Coombs test.
Local reactions: with the / m introduction - pain, irritation and infiltration at the injection site, with iv injection - phlebitis, thrombophlebitis.
Long-term use of Zinatsef can be accompanied by excessive growth of insensitive microorganisms, incl. fungi of the genus Candida with the development of candidiasis of the oral cavity and vagina (itching, discharge).
CONTRAINDICATIONS
- Hypersensitivity to cephalosporin antibiotics, penicillins and carbapenems.
Caution should be applied to the drug in case of kidney failure, gastrointestinal diseases (including in anamnesis and ulcerative colitis), if necessary combined with "loop" diuretics and aminoglycosides, during pregnancy and lactation, as well as in newborns (especially in premature babies).
PREGNANCY AND LACTATION
The drug belongs to the category B. With caution should prescribe the drug during pregnancy.
Cefuroxime excreted in breast milk, so caution should be exercised when prescribing the drug to nursing mothers.
There is no evidence of the development of embryotoxic or teratogenic effects of cefuroxime.
APPLICATION FOR FUNCTIONS OF THE LIVER
Renal insufficiency
With renal failure , a dose reduction of Zinatsef is recommended. However, there is no need to reduce the standard dose of the drug (0.75-1.5 g 3 times / day) in patients with QC more than 20 ml / min.
Correction of dose of Zinacef in renal failure in adults
Creatinine clearance Dose Zinacef
> 20 ml / min 0.75-1.5 g 3 times / day
10-20 ml / min 750 mg 2 times / day
<10 ml / min 750 mg / day
Patients on hemodialysis at the end of each hemodialysis session should be administered an additional dose of Zinatsef, equal to 750 mg.
Patients in the intensive care unit on continuous hemodialysis using an arteriovenous shunt or high-speed hemofiltration are recommended 750 mg twice daily. If hemofiltration is used at a low rate, then doses are used, as in renal failure.
APPLICATION FOR CHILDREN
According to the indications and in doses that take into account the age of the patient.
SPECIAL INSTRUCTIONS
With caution should prescribe the drug to patients with an anaphylactic reaction to penicillins and other beta-lactam antibiotics in the anamnesis.
With simultaneous administration with aminoglycosides and diuretics, the risk of nephrotoxic effects increases, so it is necessary to monitor kidney function when using this combination of drugs, especially in elderly patients, with kidney disease and in those receiving the drug in high doses.
In the treatment of meningitis by Zinatsef, in some children there was a decrease in mild to moderate hearing, while in the cerebrospinal fluid positive cultures of Haemophilus influenzae were detected after 18-36 hours of therapy. Similar phenomena were also observed with the use of other antibiotics, their clinical significance is not known.
Pseudomembranous colitis is observed with a wide range of antibiotics, the possibility of its occurrence must be borne in mind in patients with severe diarrhea that occurred during or after a course of antibiotic treatment.
Cefuroxime is also available in the form of aksetila (Zinnat) in tablets, which allows you to assign the same antibiotic consistently, when you need to switch from parenteral to oral therapy.
For the treatment of pneumonia and exacerbation of chronic bronchitis, it is effective to prescribe a course of treatment with Zinatsef, an antibiotic for parenteral administration, before applying Zinnat orally (stepwise therapy).
With stepwise therapy, the time for switching to oral therapy is determined by the severity of the infection, the clinical condition of the patients and the sensitivity of the pathogen. If there is no clinical effect within 72 hours from the start of treatment, the parenteral course of therapy should be continued.
Before starting stepwise therapy, consult the available reference books for cefuroxime axetil.
Zinatsef does not affect the results of the determination of glucose in urine using enzyme methods. However, when using other methods (Benedikt, Feling, Klinist), there can be an interaction that does not lead to false positive results.
In patients receiving Zinacef, it is recommended that glucose oxidase or with hexokinase be used to determine the blood glucose / plasma level.
Zinatsef does not affect the quantitative determination of creatinine by an alkaline-picrate method.
Each 750 mg Zinatsef vial contains 42 mg of sodium.
Impact on the ability to drive vehicles and manage mechanisms
No messages.
OVERDOSE
Symptoms: increased excitability of the cerebral cortex with the development of seizures.
Treatment: conduct symptomatic therapy, hemodialysis, peritoneal dialysis.
DRUG INTERACTION
Simultaneous administration with "loop" diuretics (furosemide) and aminoglycosides slows tubular secretion, reduces renal clearance, increases plasma concentration and increases T 1/2 of cefuroxime, which increases the risk of nephrotoxic effects. Zincaph in combination with aminoglycosides act additively, but sometimes synergism of action can be observed.
Pharmaceutical interaction
When mixing a solution of cefuroxime (1.5 g in 15 ml of water for injection) and metronidazole (500 mg / 100 ml), both components remain active for up to 24 hours at a temperature of no higher than 25 В° C. Zinacef in a dose of 1.5 g is compatible with azolocillin solution (1 g in 15 ml or 5 g in 50 ml); both components retain their activity for up to 24 hours at a temperature of 4 В° C or up to 6 hours at a temperature of no higher than 25 В° C.
A solution of Zinacef (5 mg / ml) in a 5% or 10% xylitol solution can be stored for up to 24 hours at a temperature of no higher than 25 В° C.
Zinacef is compatible with aqueous solutions containing up to 1% lidocaine hydrochloride.
Zinacef is compatible with the most widely used infusion solutions.
When mixed with the following solutions, the preparation is stable up to 24 hours at room temperature: 0.9% sodium chloride solution; 5% dextrose solution for injection; 0.18% sodium chloride solution and 4% dextrose solution for injection; 5% dextrose solution and 0.9% sodium chloride solution; 5% dextrose solution and 0.45% sodium chloride solution; 5% dextrose solution and 0.225% sodium chloride solution; 10% dextrose solution for injection; Ringer's solution; Ringer's solution of lactate; Hartman solution.
Stability of cefuroxime in a 0.9% solution of sodium chloride and in a 5% solution of dextrose is not disturbed in the presence of hydrocortisone sodium phosphate.
With the following solutions, Zinacef is compatible and stable for 24 hours at room temperature: heparin (10 U / ml and 50 U / ml) in a 0.9% solution of sodium chloride; potassium chloride (10 mEq / L and 40 mEq / L) in a 0.9% solution of sodium chloride.
Zinatsef should not be mixed in one syringe with antibiotics from the aminoglycoside group.
Sodium bicarbonate solution 2.74% has a pH value that significantly affects the color of the cefuroxime solution, so it is not recommended to use it for diluting Zinatsef. However, if a patient is given a solution of sodium bicarbonate by infusion, then, if necessary, Zinatsef can be injected directly into the tube of the infusion system.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a place protected from light, inaccessible to children at a temperature of no higher than 25 В° C. Shelf life - 2 years.
After dilution, the solution is stored for 5 hours at a temperature of no higher than 25 В° C and 48 hours at 4 В° C (in the refrigerator).
