Composition, form of production and packaging
Tablets covered with a film shell of white or almost white color, oval, biconcave, on one side engraved "GX ES5"; on the cross section - the core is white or almost white.
cefuroxime axetil * 150.36 mg,
which corresponds to the content of cefuroxime 125 mg
Excipients: microcrystalline cellulose ** - 47.51 mg, croscarmellose sodium - 20 mg, sodium lauryl sulfate - 2.25 mg, vegetable hydrogenated oil - 4.25 mg, silicon dioxide colloid - 0.63 mg.
The composition of the film membrane: hypromellose - 5.55 mg, propylene glycol 0.33 mg, methyl parahydroxybenzoate 0.06 mg, propyl parahydroxybenzoate 0.04 mg, dangerous color white 1.52 mg (hypromellose 3%, titanium dioxide 36%, sodium benzoate 0.1%).
10 pieces. - blisters (1) - packs of cardboard.
Tablets covered with a film shell of white or almost white color, oval, biconcave, on one side engraved "GX ES7"; on the cross section - the core is white or almost white.
cefuroxime axetil * 300.72 mg,
which corresponds to the content of cefuroxime 250 mg
Excipients: microcrystalline cellulose ** - 95.03 mg, croscarmellose sodium - 40 mg, sodium lauryl sulfate - 4.5 mg, vegetable hydrogenated oil - 8.5 mg, silicon dioxide colloid - 1.25 mg.
Composition of the film coat: hypromellose 7.4 mg, propylene glycol 0.44 mg, methyl parahydroxybenzoate 0.07 mg, propyl parahydroxybenzoate 0.06 mg, dangerous white dye 2.03 mg (hypromellose 3%, titanium dioxide 36%, sodium benzoate 0.1%).
10 pieces. - blisters (1) - packs of cardboard.
* The amount of cefuroxime axetil is correlated depending on the purity of the substance series used.
** The amount of microcrystalline cellulose is correlated to maintain the constant mass of the core.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
Cefuroxime axetil is a prodrug of cefuroxime, an antibiotic of the second generation of cephalosporins with bactericidal action. Cefuroxime is active against a wide range of pathogens, including strains producing beta-lactamases.
Cefuroxime has resistance to the action of bacterial ОІ-lactamases, and is therefore effective against ampicillin-resistant or amoxicillin-resistant strains.
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.
The prevalence of acquired bacterial resistance to cefuroxime varies depending on the region and over time, in certain types of microorganisms, resistance can be very high. It is preferable to have local sensitivity data, especially when treating severe infections.
Cefuroxime in vitro is usually active against the following microorganisms.
Bacteria, usually sensitive to cefuroxime:
Gram-positive aerobes - Staphylococcus aureus (strains sensitive to methicillin) 1 , coagulase-negative staphylococci (strains sensitive to methicillin), Streptococcus pyogenes 1 (beta-hemolytic streptococci);
gram-negative aerobes - Haemophilus influenzae 1 (including ampicillin-resistant strains), Haemophilus parainfluenzae 1 , Moraxella catarrhalis 1 , Neisseria gonorrhoeae 1 (including strains producing and not producing penicillinase);
Gram-positive anaerobes - Peptostreptococcus spp., Propionibacterium spp .; gram-negative spirochetes - Borrelia burgdorferi. 1
Bacteria for which acquired resistance to cefuroxime is likely:
Gram-positive aerobes - Streptococcus pneumoniae 1 ;
gram-negative aerobes - Citrobacter spp. (with the exception of C. freundii), Enterobacter spp. (with the exception of E. aerogenes and E. colaae), Escherichia coli 1 , Klebsiella spp. (including Klebsiella pneumonia 1 ), Proteus mirabilis, Proteus spp. (with the exception of P. penneri and P. vulgaris), Providencia spp .;
Gram-positive anaerobes - Clostridium spp. (with the exception of C. difficile), gram-negative aerobes - Bacteroides spp. (with the exception of B. fragilis), Fusobacterium spp.
Bacteria that have natural resistance to cefuroxime:
Gram-positive aerobes - Enterococcus spp. (including E. faecalis and E. faecium), Listeria monocytogenes;
Gram-negative aerobes - Acinetobacter spp., Burkholderia cepacia, Campylobacter spp., Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Morganella morganii, Proteus penneri, Proteus vulgaris, Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp., Stenotrophomonas maltophilia;
Gram-positive anaerobes - Clostridium difficile;
gram-negative aerobes - Bacteroides fragilis); other - Chlamydia spp., Mycoplasma spp., Legionella spp.
1 - for these bacteria, the clinical efficacy of cefuroxime has been demonstrated in clinical studies.
After ingestion of cefuroxime, the auxetil is absorbed from the digestive tract and is rapidly hydrolyzed in the mucosa of the small intestine and in the blood with the release of cefuroxime.
Optimum absorption of cefuroxime axetil in the form of tablets coated with a film membrane is achieved when
condition of taking the drug immediately after eating.
C max cefuroxime in serum (2.1 mg / L for a dosage of 125 mg, 4.1 mg / L for a dosage of 250 mg, 7.0 mg / L for a dosage of 500 mg) is observed after about 2-3 hours when taking the drug with meals.
Binding to blood plasma proteins is approximately 33-50% and depends on the technique of determination.
Cefuroxime is not metabolized.
T 1/2 is 1-1.5 hours. Cefuroxime is excreted by glomerular filtration and tubular secretion. With the simultaneous administration of probenecid AUC is increased by 50%.
Pharmacokinetics in special clinical cases
Patients with impaired renal function
The pharmacokinetics of cefuroxime were studied in patients with renal dysfunction of varying severity. T 1/2 of cefuroxime increases with decreasing renal function, which is the basis for recommendations for correcting the dosing regimen for this group of patients (see section "Dosage regimen"). In patients on hemodialysis, at least 60% of the total amount of cefuroxime present in the body at the time of onset of dialysis will be removed within a 4-hour dialysis period. Thus, an additional single dose of cefuroxime should be administered after completion of the hemodialysis procedure.
Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper respiratory tract, ENT organs (otitis media, sinusitis, tonsillitis, pharyngitis);
- infections of the lower respiratory tract (including pneumonia acute bacterial bronchitis and exacerbation of chronic bronchitis);
- Urinary tract infections (including pyelonephritis, cystitis, urethritis);
- infections of the skin and soft tissues (including furunculosis, pyoderma, impetigo);
- gonorrhea: acute uncomplicated gonorrhea urethritis and cervicitis;
- treatment of borreliosis (Lyme disease) at an early stage and prevention of late stages of the disease in adults and children over 12 years of age.
Cefuroxime is also available as a sodium salt (Zinacef В® preparation ) for parenteral administration. This allows for stepwise therapy, using a transition from the parenteral form to the oral form of cefuroxime, if there is a clinical indication for this.
If necessary, stepwise therapy is indicated in the treatment of pneumonia and exacerbation of chronic bronchitis.
The sensitivity of bacteria to cefuroxime varies depending on the region and over time. Where possible, local sensitivity data should be taken into account (see section "Pharmacological action").
The standard course of therapy is 7 days (can vary from 5 to 10 days). For optimal absorption, the drug should be taken after meals.
Most infections are 250 mg 2 times / day
Urinary tract infections (cystitis, urethritis) 125 mg 2 times / day
Pyelonephritis 250 mg 2 times / day
Light and moderate infections of the lower respiratory tract, for example, bronchitis 250 mg 2 times / day
Heavier infections of the lower respiratory tract or suspected pneumonia 500 mg 2 times / day
Uncomplicated gonorrhea 1 g once
Borreliosis (Lyme disease) in adults and children over 12 years of age 500 mg 2 times / day for 20 days
Cefuroxime is also available as a sodium salt (preparation Zinacef В® ) for parenteral administration, which allows you to assign the same antibiotic consistently, when you need to switch from parenteral to oral therapy. The drug Zinnat В® is effective after the parenteral use of the drug Zinacef В® for the treatment of pneumonia and exacerbation of chronic bronchitis.
The duration of parenteral and oral treatment is determined by the severity of the infection and the clinical picture.
The drug Zinacef В® (cefuroxime in the form of sodium salt) at a dose of 1.5 g 2-3 times / day (iv or IM) for 48-72 hours, then - Zinnat В® (cefuroxime axetil) inwards at a dose of 500 mg 2 times / day for 7-10 days.
Exacerbation of chronic bronchitis
The drug Zinacef В® (cefuroxime in the form of sodium salt) at a dose of 750 mg 2-3 times / day (iv or IM) for 48-72 hours, then - a course of treatment with Zinnat В®(cefuroxime axetil) orally in a dose 500 mg 2 times / day for 5-10 days.
Children from 3 years old
Most infections are 125 mg (1 tablet at 125 mg) 2 times / day. The maximum daily dose is 250 mg
The average otitis or more severe infections are 250 mg (1 tablets of 250 mg or 2 tablets of 125 mg) 2 times / day. The maximum daily dose is 500 mg
Tablets of Zinnat В® can not be broken and crushed.
Therefore, this dosage form is not used to treat patients with swallowing difficulties, incl. small children who can not swallow a whole pill. For children, a Zinnat В®preparation in the form of granules can be used to prepare a suspension for oral administration.
Patients with impaired renal function
The excretion of cefuroxime occurs mainly by the kidneys.
It is recommended to reduce the dose of cefuroxime in patients with severe renal dysfunction to compensate for delayed excretion (see table below).
Creatinine clearance T 1/2 (hours) Recommended dose
? 30 ml / min 1.4-2.4 No dose adjustment is required.
10-29 ml / min 4.6 The standard single dose every 24 hours.
<10 ml / min 16.8 The standard single dose every 48 hours.
During hemodialysis 2-4 At the end of each dialysis session, one additional standard single dose should be taken.
Undesired reactions with cefuroxime axetil are usually only slightly expressed, short-lived and reversible.
The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems and
frequency of occurrence. Frequency of occurrence is defined as follows: very often (? 1/10), often (? 1/100 and <1/10), infrequently (? 1/1 000 and <1/100), rarely (? 1/10 000 and <1/1 000), very rarely (<1/10 000, including individual cases). Frequency categories were formed on the basis of clinical studies of the drug and post-registration surveillance.
Infectious and parasitic diseases: often - excessive growth of fungi of the genus Candida.
From the hematopoietic and lymphatic system: often - eosinophilia; infrequently positive Coombs test, thrombocytopenia, leukopenia (sometimes severe); very rarely - hemolytic anemia. Cephalosporins are absorbed on the surface of the cell membrane of erythrocytes, binding to antibodies to cephalosporins, which leads to a positive result of the Coombs reaction (which may affect cross-compatibility) and, in very rare cases, hemolytic anemia.
From the side of the immune system: hypersensitivity reactions, incl. infrequent skin rash; rarely - hives, itching; very rarely - drug fever, serum sickness and anaphylaxis.
From the nervous system: often - headache, dizziness.
On the part of the digestive system: often - gastrointestinal disorders, including diarrhea, nausea, abdominal pain; infrequently - vomiting; rarely - pseudomembranous colitis (see section "Special instructions").
On the part of the liver and biliary tract: often - a transient increase in liver liver enzymes ALT, ACT, LDH; very rarely - jaundice (mostly cholestatic), hepatitis.
From the skin and subcutaneous tissues: very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. See also violations from the immune system .
- phenylketonuria (for suspension for oral administration);
- Children's age up to 3 months (for suspension for oral administration);
- for tablets - children under 3 years of age (for children from 3 months to 3 years, the drug Zinnat В® should be used in the form of a suspension);
- Hypersensitivity to antibiotics group cephalosporins.
Caution should be exercised when used in patients with impaired renal function; Gastrointestinal diseases (including in history, as well as ulcerative colitis); pregnant women, during breastfeeding.
PREGNANCY AND LACTATION
Zinnat В® should be used if the intended benefit to the mother exceeds the potential risk to the fetus and the baby.
There is no experimental evidence of embryopathic or teratogenic effects of cefuroxime axetil, but as with other medications, caution should be exercised when prescribing it in the early stages of pregnancy.
Care must be taken when prescribing it to nursing mothers, as the drug is determined in breast milk.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be exercised in appointing patients with impaired renal function.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 3 months (for suspension for oral administration); for tablets - children's age up to 3 years (for children from 3 months to 3 years, the drug Zinnat В® should be used in the form of a suspension).
Before use, you must carefully collect allergic history.
In the process of treatment, it is necessary to monitor kidney function, especially in patients receiving the drug in a high dose.
During the period of taking Zinnat В®, a false positive urine reaction to glucose is possible.
As with other antibiotics, prolonged use of Zinnat В® can lead to excessive growth of Candida fungi. Long-term use can cause the growth of other resistant microorganisms (Enterococcus and Clostridium difficile), which may require discontinuation of treatment.
There are cases of pseudomembranous colitis occurring when taking antibiotics, the severity of which can range from mild to life-threatening. Therefore, it is necessary to conduct differential diagnosis of pseudomembranous colitis in patients with diarrhea that occurred during or after a course of antibiotic treatment. If diarrhea is severe or severe, or the patient experiences abdominal cramps, treatment with Zinnat В® should be immediately discontinued and the patient should be examined.
The Yarisch-Gerxheimer reaction was observed in borreliosis (Lyme disease) with the administration of Zinnat В® and is due to the bactericidal activity of the drug against the causative agent of spirochaete Borrelia burgdorferi. Patients should be informed that these symptoms are a typical consequence of the use of antibiotics in this disease.
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 the clinical effect is not achieved within 72 hours from the start of treatment, the parenteral course of therapy should be continued.
Before the start of the stepwise therapy, you should carefully read the instruction for the use of the sodium salt of cefuroxime for parenteral administration (Zinacef В®preparation).
Tablets of Zinnat В® can not be broken and crushed. Therefore, this dosage form is not used to treat patients with swallowing difficulties, incl. small children who can not swallow a whole pill.
It is necessary to take into account the content of sucrose in a suspension of Zinnat В® in the treatment of patients with diabetes mellitus.
5 ml of the prepared suspension of Zinnat В® contains 0.25 bread units (XE).
Impact on the ability to drive vehicles and manage mechanisms
Since cefuroxime axetil may cause dizziness, it is necessary to warn patients about precautions when driving a vehicle or working with moving machinery.
Symptoms: an overdose of cephalosporins can cause an increase in the excitability of the brain with the development of seizures.
Treatment: conduct symptomatic therapy. Serum concentrations of cefuroxime decrease with hemodialysis and peritoneal dialysis.
Drugs that reduce the acidity of gastric juice can reduce the bioavailability of cefuroxime when compared with that observed after taking the drug on an empty stomach, and also level the effect of increased absorption of the drug after ingestion.
Like other antibiotics, Zinnat В® can affect the intestinal microflora, which leads to a decrease in the reabsorption of estrogens and, consequently, to a decrease in the effectiveness of oral hormonal combined contraceptives.
When conducting a ferrocyanide test, a false negative result can be observed, therefore glucose oxidase or hexokinase methods are recommended to determine the level of glucose in the blood and / or plasma.
The drug Zinnat В® does not affect the quantitative determination of creatinine by an alkaline-picrate method.
Simultaneous reception with "loop" diuretics slows tubular secretion, reduces renal clearance, increases plasma concentration and increases T 1/2 of cefuroxime.
Simultaneous administration of cefuroxime and probenecid results in an AUC increase of 50%.
With simultaneous administration with aminoglycosides and diuretics, the risk of nephrotoxic effects increases.
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 at a temperature of no higher than 30 В° C. Shelf life - 3 years.