Composition, form of production and packaging
Granules for the preparation of suspension for ingestion in the form of grains of irregular shape, of various sizes, but not more than 3 mm, white or almost white;When diluted, a suspension is formed from white to light yellow with a characteristic fruiting odor.
5 ml
cefuroxime axetil 150 mg,
which corresponds to the content of cefuroxime 125 mg
Auxiliary substances: stearic acid - 852 mg, sucrose - 3.062 g, flavoring "tutti-frutti" - 100 mg, acesulfame potassium - 21 mg, aspartame - 21 mg, povidone K30 - 13 mg, xanthan gum - 1 mg.
1.25 g - bottles of dark glass (1) complete with a dosage spoon and a measuring cup - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Cefuroxime axetil is a precursor of cefuroxime, which belongs to the second generation of cephalosporin antibiotics. Cefuroxime is active against a wide range of pathogens, including strains producing ОІ-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.
In vitro, cefuroxime is active against the following microorganisms: Gram-negative aerobes- Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae (including strains producing and not producing penicillinase), Escherichia coli, Klebsiella spp., Proteus mirabilis , Providencia spp., Providencia rettgeri; Gram-positive aerobes - Staphylococcus aureus (including strains producing penicillinase but excluding methicillin-resistant strains), Staphylococcus epidermidis (including strains producing penicillinase but excluding methicillin-resistant strains), Streptococcus pyogenes and other beta-hemolytic streptococci, Streptococcus pneumoniae, Streptococcus group B (Streptococcus agalactiae); anaerobes are Gram -positive and Gram-negative cocci (including Peptococcus spp. and Peptostreptococcus spp.), Gram-positive rods (including Clostridium spp., except Clostridium difficile, Propionibacterium spp.), Gram-negative rods (including Bacteroides spp. and Fusobacterium spp.), Gram-negative spirochaetes Borrelia burgdorferi).
The following microorganisms are not sensitive to cefuroxime: Clostridium difficile, Pseudomonas spp., Campylobacter spp., Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Legionella spp., Enterococcus faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp. , Citrobacter spp., Serratia spp., Bacteroides fragilis.
PHARMACOKINETICS
Suction
After oral administration of cefuroxime, the auxetil is slowly absorbed from the digestive tract and is rapidly hydrolyzed in the intestinal mucosa and blood with the release of cefuroxime. Cefuroxime axetil is optimally absorbed if the drug is taken immediately after a meal.
After taking a suspension of C max cefuroxime (2-3 mg / L for a dose of 125 mg and 4-6 mg / L for a dose of 250 mg) are observed approximately 2-3 hours after taking the drug after a meal.
Distribution
The binding of cefuroxime to plasma proteins is 33-50%.
Cefuroxime penetrates the BBB, penetrates the placenta and is excreted in breast milk.
Metabolism
Cefuroxime is not metabolized in the body.
Excretion
It is isolated by glomerular filtration and tubular secretion. Serum cefuroxime levels decrease with dialysis.
T 1/2 is 1-1.5 hours.
INDICATIONS
Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper respiratory tract, ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media);
- infections of the lower respiratory tract (acute bacterial bronchitis and exacerbation of chronic bronchitis, pneumonia);
- urinary tract infections (pyelonephritis, cystitis, urethritis);
- skin and soft tissue infections (furunculosis, pyoderma, impetigo);
- gonorrhea, acute uncomplicated gonorrhea urethritis and cervicitis;
- Treatment of 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. In the framework of the stepwise therapy, the transition from the parenteral form to the oral form of cefuroxime is recommended.
Stepwise therapy is indicated in the treatment of pneumonia and with exacerbation of chronic bronchitis.
DOSING MODE
The drug Zinnat В® in the form of a suspension for oral administration is recommended for use in children from 3 months . There is no experience of using Zinnat В®in children younger than 3 months.
If a fixed dose is preferred, then for most infections it is recommended to take 125 mg 2 times / day. Children aged 2 years and older with an average otitis or with more severe infections are prescribed 250 mg 2 times / day; the maximum daily dose is 500 mg.
When treating infants and children, it is necessary to calculate the dose depending on body weight and age. For most infections, the dose for infants and children aged 3 months to 12 years is 10 mg / kg 2 times / day, but not more than 250 mg / day. With average otitis and more severe infections, the recommended dose is 15 mg / kg 2 times / day, but not more than 500 mg / day.
The following tables show the dose, depending on the age and body weight of the child, for dispensing a suspension of Zinnat В® 125 mg / 5 ml with 5 ml spoonfuls attached to the package.
Dose at the rate of 10 mg / kg body weight, prescribed for most infections
Age Body weight (kg) (approximately) Single dose (mg) when taken 2 times / day Number of measuring spoons (5 ml) in a single dose
3-6 months 4-6 40-60 1/2
6 months-2 years 6-12 60-120 1 / 2-1
2-12 years from 12 and more 20 125 1
Dose at the rate of 15 mg / kg body weight, prescribed for otitis media and more serious infections
Age Body weight (kg) (approximate) Single dose (mg) when taking body weight Number of measuring spoons (5 ml) in a single dose
3-6 months 4-6 60-90 1/2
6 months-2 years 6-12 90-180 1-1.5
2-12 years from 12 and more 20 180-250 1.5-2
Stepwise therapy
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.
Pneumonia
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.
SIDE EFFECT
The undesirable phenomena presented below are listed depending on the anatomical and physiological classification 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.
Infections: often - superinfection with fungi of the genus Candida.
From the hematopoietic and lymphatic system: often - eosinophilia; infrequently, false-positive Coombs reaction (cephalosporins are absorbed on the surface of the cell membrane of erythrocytes, binding to antibodies to cephalosporins, which leads to a false positive result of Coombs test and in very rare cases to hemolytic anemia), thrombocytopenia, leukopenia (sometimes severe); very rarely - hemolytic anemia.
From the immune system: hypersensitivity reactions: infrequently - skin rash; rarely - hives, itching; very rarely - drug fever, serum sickness and anaphylaxis.
From the nervous system: often - headache, dizziness.
From the digestive system: often - diarrhea, nausea, abdominal pain; infrequently - vomiting; rarely - pseudomembranous colitis.
On the part of the liver and biliary tract: often - a transient increase in the level of liver enzymes ALT, ACT, LDH; very rarely - jaundice (mostly cholestatic), hepatitis.
From the skin and subcutaneous fat: very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
CONTRAINDICATIONS
- phenylketonuria;
- Children's age up to 3 months;
- Hypersensitivity to antibiotics group cephalosporins.
With caution
Caution should be exercised in appointing patients with impaired renal function; Gastrointestinal diseases (including in history, as well as ulcerative colitis); pregnant women, during lactation.
PREGNANCY AND LACTATION
The drug Zinnat В® should be used if the intended benefit to the mother exceeds the potential risk to the child.
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
SPECIAL INSTRUCTIONS
Caution should be shown when prescribing the drug to patients with an allergic reaction to beta-lactam antibiotics in the anamnesis.
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.
Pseudomembranous colitis was observed with the use of broad-spectrum antibiotics, therefore it is necessary to conduct differential diagnosis of pseudomembranous colitis in patients with severe diarrhea that occurred during or after a course of antibiotic treatment.
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.
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 onset of stepwise therapy, refer to the available reference books for the sodium salt of cefuroxime (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.
OVERDOSE
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.
DRUG INTERACTION
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 at a temperature of no higher than 30 В° C. Shelf life - 2 years.
The prepared suspension should be stored in the refrigerator at a temperature of 2-8 В° C for not more than 10 days.
Keep out of the reach of children.
