Zinnat tablets 250mg, No. 10

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 mode is individual.

Film-coated tablets of white or almost white color, oval, biconvex, engraved on one side 'GX ES7'; in cross section, the core is white or almost white.

1 tab. 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, hydrogenated vegetable oil - 8.5 mg, colloidal silicon dioxide - 1.25 mg.

• Children under 3 years of age (for children from 3 months to 3 years, ZinnatЃ, granules for the preparation of a suspension for oral administration);

• hypersensitivity to beta-lactam antibiotics (in particular to cephalosporin antibiotics, penicillins and carbapenems in history).

  With care

• Caution should be exercised when used in patients with impaired renal function; 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 from region to 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 Commonly Sensitive 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 pneumoniae 1.

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., Excluding Clostridium difficile.

Gram-negative anaerobes: Bacteroides spp., With the exception of Bacteroides fragilis, Fusobacterium spp.

Bacteria that are 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.

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

Pharmacokinetics

Suction

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. Optimal absorption of cefuroxime axetil in the form of film-coated tablets is achieved if the drug is taken immediately after a meal. Cmax of cefuroxime (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) are observed after approximately 2-3 hours when taking the drug with meals.

Distribution

Plasma protein binding is approximately 33-50% and depends on the determination method.

Metabolism

Cefuroxime is not metabolized.

Withdrawal

T1 / 2 is 1-1.5 hours. Cefuroxime is excreted 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 - positive Coombs' test, thrombocytopenia, leukopenia (sometimes severe); 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 reaction (which can affect cross-compatibility) and, in very rare cases, to hemolytic anemia.

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

From the nervous system: often - headache, dizziness.

From the digestive system: often - gastrointestinal disorders, including diarrhea, nausea, abdominal pain, a transient increase in the activity of hepatic liver enzymes ALT, ACT, 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.

Application during pregnancy and lactation

ZinnatЃ should be used if the potential benefit to the mother outweighs the potential risk to the fetus and child.

There is no experimental evidence for the embryopathic or teratogenic effects of cefuroxime axetil, but as with other drugs, caution should be exercised when prescribing it in early pregnancy.

Care must be taken when prescribing the drug to nursing mothers, since the drug is excreted in breast milk.

Application for impaired renal function

Caution should be exercised when prescribing to patients with impaired renal function.

Application in children

Contraindicated in children under 3 years of age.

special instructions

Before use, it is necessary to carefully collect an allergic history.

During treatment, it is necessary to monitor kidney function, especially in patients receiving a high dose of the drug.

During the period of taking ZinnatЃ, a false-positive reaction of urine to glucose is possible.

As with other antibiotics, long-term use of ZinnatЃ can lead to overgrowth of Candida fungi. Long-term use can cause the growth of other resistant microorganisms (Enterococcus 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 Jarisch-Herxheimer reaction was observed in borreliosis (Lyme disease) when taking the drug ZinnatЃ and is due to the bactericidal activity of the drug against the causative agent of the disease of the spirochete Borrelia burgdorferi. Patients should be informed that these symptoms are typical consequences of the use of antibiotics for this disease.

With stepwise therapy, the time to switch 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 starting sequential therapy, you should carefully read the instructions for using cefuroxime sodium salt for parenteral administration (ZinacefЃ).

Influence on the ability to drive vehicles and 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 brain with the development of seizures.

Treatment: symptomatic therapy is performed. Serum cefuroxime concentrations can be decreased with hemodialysis and peritoneal dialysis.

Drug interactions

Drugs that reduce the acidity of gastric juice can reduce the bioavailability of cefuroxime axetil when compared with that observed after taking the drug on an empty stomach, and also neutralize the effect of increased absorption of the drug after a meal.

Like other antibiotics, ZinnatЃ can affect the intestinal microflora, which leads to a decrease in estrogen reabsorption and, as a consequence, to a decrease in the effectiveness of oral hormonal combined contraceptives.

When conducting a ferrocyanide test, a false negative result can be observed, therefore, it is recommended to use glucose oxidase or hexokinase methods to determine the level of glucose in the blood and / or plasma.

ZinnatЃ does not affect the quantitative determination of creatinine by the alkaline-picrate method.

Simultaneous administration with loop diuretics slows down tubular secretion, decreases 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.