Zinnat granules d / prig.asp.d / pr. inside 125mg / 5ml, 50 ml

The drug is indicated for the treatment of infectious and inflammatory diseases caused by bacteria sensitive to cefuroxime:

- infections of the upper respiratory tract, ENT organs, such as otitis media, sinusitis, tonsillitis and pharyngitis;

-infections of the lower respiratory tract, such as pneumonia, acute bacterial bronchitis and exacerbation of chronic bronchitis;

- urinary tract infections such as pyelonephritis, cystitis and urethritis;

-infections of the skin and soft tissues, such as furunculosis, pyoderma and impetigo;

- gonorrhea: acute uncomplicated gonorrheal urethritis and cervicitis;

- treatment of borreliosis (Lyme disease) at an early stage and prevention of the later stages of this disease in adults and children over 12 years old.

The reception regimen depends on age and indications.

Granules for the preparation of a suspension for oral administration from white to almost white, irregular in shape, of various sizes, but not more than 3 mm; prepared suspension from white to light yellow, with a characteristic fruity odor.

cefuroxime 125 mg

Excipients: stearic acid - 852 mg, sucrose - 3.062 g, tutti-frutti flavor - 100 mg, acesulfame potassium - 21 mg, aspartame - 21 mg, povidone K30 - 13 mg, xanthan gum - 1 mg, purified water (absent in the finished product, is used as a granulating liquid and is removed during the production process).

• Phenylketonuria;

• children's age up to 3 months;

• hypersensitivity to cefuroxime, other cephalosporin antibiotics, aspartame and other excipients;

• a history of severe hypersensitivity reactions (including anaphylactic reactions) to other beta-lactam antibiotics (penicillins, monobactams and carbapenems).

  With care

• Caution should be exercised when prescribing to patients with mild allergic reactions to penicillins, monobactams and carbapenems in history; kidney failure; diseases of the gastrointestinal tract (including history, as well as ulcerative colitis); in pregnant women and during breastfeeding.

pharmachologic effect

Mechanism of action Cefuroxime axetil is a precursor of cefuroxime, an antibiotic of the second generation cephalosporin group with a bactericidal effect. Cefuroxime is active against a wide range of pathogens, including strains producing ?-lactamases. Cefuroxime is resistant to the action of bacterial ?-lactamases, therefore it is effective against ampicillin-resistant or amoxicillin-resistant strains. The bactericidal effect of cefuroxime is associated with the suppression of the synthesis of the bacterial cell wall as a result of binding to the main target proteins. Pharmacodynamic effects 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 in the treatment of severe infections. Cefuroxime is active in vitro against the microorganisms listed below. Bacteria usually susceptible to cefuroxime Gram-positive aerobes: Staphylococcus aureus (strains sensitive to methicillin) 1, coagulase-negative staphylococci (strains sensitive to methicillin), Streptococcus pyogenes1,? - hemolytic streptococci.

Gram-negative aerobes: Haemophilus influenzae1, including ampicillin-resistant strains, Haemophilus parainfluenzae1, Moraxella catarrhalis1, Neisseria gonorrhoeae1, including penicillinase-producing and non-producing strains.

Gram-positive anaerobes: Peptostreptococcus spp., Propionibacterium spp., Spirochetes, Borrelia burgdorferi 1. Bacteria for which acquired resistance to cefuroxime is possible Gram-positive aerobes: Streptococcus pneumoniae1. Gram-negative aerobes: Citrobacter spp., Excluding Citrobacter freundii, Enterobacter spp., Excluding Enterobacter aerogenes and Enterobacter cloacae, Escherichia coli1, Klebsiella spp., Including Klebsiella pneumoniae1, Proteus mirabills, Proteus spp., And excluding Proteus vulus spp., And excluding Proteus vulus spp. Providencia spp. Gram-positive anaerobes: Clostridium spp., With the exception of Clostridium difficile. Gram-negative anaerobes: Bacteroides spp., With the exception of Bacteroides fragills, Fusobacterium spp. Bacteria naturally resistant to cefuroxime Gram-positive aerobes: Enterococcus spp.,including Enterococcus faecalis and Enterococcus 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 malosa. Gram-positive anaerobes: Clostridium difficile. Gram-negative anaerobes: Bacteroides fragilis. Others: Chlamydia spp., Mycoplasma spp., Legionella spp.including Pseudomonas aeruginosa, Serratia spp., Stenotrophomonas maltophilia. Gram-positive anaerobes: Clostridium difficile. Gram-negative anaerobes: Bacteroides fragilis. Others: Chlamydia spp., Mycoplasma spp., Legionella spp.including Pseudomonas aeruginosa, Serratia spp., Stenotrophomonas maltophilia. Gram-positive anaerobes: Clostridium difficile. Gram-negative anaerobes: Bacteroides fragilis. Others: Chlamydia spp., Mycoplasma spp., Legionella spp.

1 For these bacteria, the clinical efficacy of cefuroxime has been demonstrated in clinical studies.

Pharmacokinetics

Suction

Optimal absorption is achieved when the drug is taken with meals. After oral administration of cefuroxime, axetil is absorbed from the gastrointestinal tract and is rapidly hydrolyzed in the mucous membrane of the small intestine and in the blood with the release of cefuroxime. Cmax of cefuroxime in serum (2.1 mg / L for a dosage of 125 mg, 4.1 mg / L for a dosage of 250 mg) are observed after approximately 2-3 hours when taking the drug in tablet dosage form with meals. The rate of absorption of cefuroxime from the suspension is lower than from the tablets, therefore the Cmax of the drug is lower, the systemic bioavailability is also reduced (by 4-17%).

Distribution 33-50% of the drug binds to plasma proteins, depending on the determination method. Metabolism Cefuroxime is not metabolized. Excretion of T1 / 2 cefuroxime is 1-1.5 hours. Cefuroxime is excreted from the body by glomerular filtration and tubular secretion.

Pharmacokinetics in special patient groups

The pharmacokinetics of cefuroxime was studied in patients with impaired renal function of varying severity. T1 / 2 cefuroxime increases with decreasing renal function, which is the basis for recommendations for adjusting the dosage regimen for this group of patients. In patients on hemodialysis, at least 60% of the total amount of cefuroxime present in the body at the time of dialysis initiation will be removed during the 4-hour dialysis period. Therefore, an additional single dose of cefuroxime should be given after completion of the hemodialysis procedure.

Side effect

Infectious and parasitic diseases: often - overgrowth of fungi of the genus Candida.

From the hematopoietic system: often - eosinophilia; infrequently - a positive Coombs test, thrombocytopenia, leukopenia (sometimes pronounced); very rarely - hemolytic anemia. Cephalosporins are absorbed on the surface of the cell membrane of erythrocytes, binding with antibodies to cephalosporins, which leads to a positive result of the Coombs test (which can affect cross-compatibility) and, in very rare cases, to hemolytic anemia.

From the nervous system: often - headache, dizziness.

From the digestive system: often - gastrointestinal disorders, including diarrhea, nausea, abdominal pain, a temporary increase in the activity of liver enzymes ALT, AST, LDH; infrequently - vomiting; rarely - pseudomembranous colitis; very rarely - jaundice (mainly cholestatic), hepatitis.

Skin and subcutaneous tissue disorders: very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematous necrolysis).

From the immune system: hypersensitivity reactions, incl. infrequently - skin rash; rarely - urticaria, itching; very rarely, drug fever, serum sickness, and anaphylaxis.

Application during pregnancy and lactation

There is no experimental evidence for the embryopathic and teratogenic effects of cefuroxime axetil, but as with other drugs, it should be carefully prescribed in the first months of pregnancy. Cefuroxime is excreted in breast milk, so care must be taken when prescribing it to lactating women.

Application for impaired renal function

Caution should be exercised when prescribing to patients with renal insufficiency.

special instructions

Caution should be exercised when used in patients with mild allergic reactions to penicillins, monobactams and carbapenems in history, since the possible risk of developing cross-hypersensitivity reactions must be taken into account.

Before starting treatment with ZinnatЃ, it is necessary to collect a detailed history of previous hypersensitivity reactions to penicillins, cephalosporins or other substances that cause allergic reactions in the patient. In the event of an allergic reaction, it is necessary to discontinue treatment with ZinnatЃ and begin an appropriate alternative therapy.

In severe anaphylactic reactions, epinephrine should be given promptly to the patient. Oxygen therapy, intravenous administration of corticosteroids and airway management, including intubation, may also be required. As with other antibiotics, taking cefuroxime axetil can lead to overgrowth of Candida. Long-term use can cause the growth of other resistant microorganisms (for example, enterococci and Clostridium difficile), which may require discontinuation of treatment.

Cases of pseudomembranous colitis with antibiotics have been described, the severity of which can vary from mild to life-threatening.

Therefore, it is necessary to carry out a differential diagnosis of pseudomembranous colitis in patients with diarrhea that occurred during or after a course of antibiotic treatment.

If the diarrhea is prolonged or has a pronounced character, or the patient experiences abdominal cramps, treatment with ZinnatЃ should be stopped immediately, the patient should be examined. The sucrose content of the preparation should be taken into account when treating patients with diabetes mellitus. Patients should be given appropriate advice.

5 ml of the prepared ZinnatЃ suspension contains 0.25 bread units (XE). The ZinnatЃ suspension contains aspartame, which is a source of phenylalanine. When treating Lyme disease with ZinnatЃ, the Jarisch-Herxheimer reaction may occur, which is due to the bactericidal activity of the drug against the causative agent of the spirochete Borrelia burgdorferi disease. Patients should be informed that these symptoms are typical consequences of the use of antibiotics for this disease, which resolves spontaneously.

Influence on the ability to drive vehicles and use mechanisms

Since cefuroxime axetil can cause dizziness, patients should be warned about precautions when driving or working with moving machinery.

Overdose

Symptoms: an overdose of cephalosporins can cause an increase in the excitability of the central nervous system with the development of seizures. Treatment: symptomatic therapy is performed. Serum cefuroxime concentrations can be reduced by hemodialysis and peritoneal dialysis.

Drug interactions

Drugs that lower the acidity of gastric juice can cause a decrease in the bioavailability of the ZinnatЃ suspension. Like many antibacterial drugs, ZinnatЃ can affect the intestinal microflora, which leads to a reduced reabsorption of estrogens and, accordingly, to a decrease in the effectiveness of combined oral contraceptives. Simultaneous reception with 'loop' diuretics slows down tubular secretion, reduces renal clearance, increases plasma concentration and increases T1 / 2 of cefuroxime. The simultaneous administration of cefuroxime and probenecid leads to an increase in the AUC of cefuroxime by 50%. When taken simultaneously with aminoglycosides and diuretics, the risk of nephrotoxic effects increases. In patients receiving cefuroxime axetil, a test with potassium ferrocyanide may give a false negative result.For such patients, it is recommended to use methods using glucose oxidase or hexokinase to determine blood glucose. Cefuroxime does not affect the results of determining the concentration of creatinine by the alkaline-picrate method.