Instructions for Cefuroxime Sandoz film-coated tablets 500 mg No. 14
Composition
active ingredient: cefuroxime;
1 tablet contains cefuroxime axetil equivalent to 500 mg of cefuroxime;
excipients: sodium lauryl sulfate, copovidone, croscarmellose sodium, magnesium stearate, colloidal anhydrous silicon dioxide, mannitol (E 421), microcrystalline cellulose, crospovidone, talc;
shell: mannitol (E 421), soluble starch, talc, titanium dioxide (E 171), aspartame (E 951).
Dosage form
Film-coated tablets.
Main physicochemical properties: oblong biconvex, white to light yellow in color.
Pharmacotherapeutic group
Antimicrobials for systemic use. Second-generation cephalosporins.
ATX code J01D C02.
Pharmacological properties
Pharmacodynamics
Cefuroxime axetil is an oral form of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most beta-lactamases and is active against a broad spectrum of gram-positive and gram-negative microorganisms.
The bactericidal effect of cefuroxime is the result of inhibition of the synthesis of the cell membrane of microorganisms.
Acquired antibiotic resistance varies between regions and can change over time, and may vary significantly for individual strains. It is advisable to consult local antibiotic susceptibility data, if available, especially when treating severe infections.
Cefuroxime is generally active against the following microorganisms in vitro:
| Sensitive microorganisms |
| Gram-positive aerobes: Staphylococcus aureus (methicillin-susceptible)*, coagulase-negative staphylococcus (methicillin-susceptible), Streptococcus pyogenes, Streptococcus agalactiae |
| Gram-negative aerobes: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis |
| Spirochetes: Borrelia burgdorferi |
| Microorganisms for which acquired resistance may be a problem |
| Gram-positive aerobes: Streptococcus pneumoniae |
| Gram-negative aerobes: Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Proteus strains (other than P. vulgaris), Providencia strains |
| Gram-positive anaerobes: Peptostreptococcus strains, Propionibacterium strains |
| Gram-negative anaerobes: Fusobacterium strains, Bacteroides strains |
| Resistant microorganisms |
| Gram-positive aerobes: Enterococcus faecalis, Enterococcus faecium |
| Gram-negative aerobes: Acinetobacter strains, Campylobacter strains, Morganella morganii, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens |
| Gram-negative anaerobes: Bacteroides fragilis |
| Others: Chlamydia strains, Mycoplasma strains, Legionella strains |
(*) All methicillin-resistant S. aureus are insensitive to cefuroxime.
Pharmacokinetics
After oral administration of cefuroxime axetil is absorbed in the intestine, hydrolyzed on the intestinal mucosa and enters the bloodstream as cefuroxime.
The optimal level of absorption is observed immediately after eating. The maximum level of cefuroxime in the blood serum is observed approximately 2-3 hours after taking the drug. The half-life of the drug is approximately 1-1.5 hours. The level of protein binding is 33-55% depending on the method of determination. Cefuroxime is excreted by the kidneys in an unchanged state by tubular secretion and glomerular filtration.
Concomitant use of probenecid increases the area under the concentration-time curve (AUC) by 50%.
Serum cefuroxime levels are reduced by dialysis.
Indication
Cefuroxime Sandoz is indicated for the treatment of the following infections in adults and children aged 3 months and over:
Acute streptococcal tonsillitis and pharyngitis; Acute bacterial sinusitis; Acute otitis media; Exacerbation of chronic bronchitis caused by pathogens sensitive to cefuroxime axetil; Cystitis; Pyelonephritis; Uncomplicated skin and soft tissue infections; Early manifestations of Lyme disease.
Contraindication
Hypersensitivity to cephalosporin antibiotics, cefuroxime or to any of the excipients. History of severe hypersensitivity reactions (e.g. anaphylactic reactions) to any other type of beta-lactam antibiotic (penicillins, monobactams and carbapenems).
Interaction with other medicinal products and other types of interactions
Drugs that reduce gastric acidity may reduce the bioavailability of cefuroxime and have the property of eliminating the effect of improved absorption after eating.
Like other antibiotics, cefuroxime axetil may have an effect on the intestinal flora, which may lead to a decrease in the reabsorption of estrogens and a decrease in the effectiveness of combined oral contraceptives.
Since the ferrocyanide test may give a false-negative result, it is recommended that glucose oxidase or hexokinase methods be used to determine plasma glucose levels in patients treated with cefuroxime. Cefuroxime does not interfere with the alkaline picrate assay for creatinine.
Concomitant use with oral anticoagulants may lead to an increase in the international normalized ratio (INR).
Serum cefuroxime levels are reduced by dialysis.
There have been reports of positive Coombs' tests with cephalosporins. This phenomenon may interfere with cross-matching of blood.
Application features
Hypersensitivity reactions. Special caution should be exercised in patients with a history of allergic reactions to penicillins or other beta-lactam antibiotics, as there is a risk of cross-sensitivity. As with all beta-lactam antimicrobials, serious and occasionally fatal cases of hypersensitivity reactions have been reported. In the event of a severe hypersensitivity reaction, cefuroxime should be discontinued immediately and the patient should receive appropriate emergency medical care.
Before initiating therapy, it is necessary to determine whether the patient has had a previous severe hypersensitivity reaction to cefuroxime, other cephalosporins or other types of beta-lactam drugs. Cefuroxime should be administered with caution to patients with a history of non-severe hypersensitivity reactions to other beta-lactam drugs.
The use of cefuroxime axetil (as with other antibiotics) may result in overgrowth of Candida. Prolonged treatment may also result in overgrowth of other non-susceptible organisms (e.g. Enterococci, Clostridium difficile), which may necessitate discontinuation of treatment.
Pseudomembranous colitis can occur with antibiotics, ranging from mild to life-threatening. Therefore, it is important to keep this in mind if patients develop severe diarrhea during or after antibiotic therapy. If prolonged or severe diarrhea occurs or the patient experiences severe cramping abdominal pain, treatment should be discontinued immediately and the patient should be carefully examined.
During the treatment of Lyme disease, a Jarisch-Herxheimer reaction has been observed, which occurs directly due to the bactericidal effect of cefuroxime on the microorganism that causes Lyme disease, the spirochete Borrelia burgdorferi. Patients should be explained that this is a normal consequence of antibiotic therapy for Lyme disease and resolves without treatment.
When sequential therapy is used, the timing of the transition from parenteral to oral therapy is determined by the severity of the infection, the clinical condition of the patient, and the susceptibility of the pathogen. If there is no clinical improvement within 72 hours, parenteral therapy should be continued. Before starting sequential therapy, the appropriate instructions for medical use of cefuroxime sodium should be consulted.
Cefuroxime should be used with extreme caution in patients with phenylketonuria, as the tablet coating contains aspartame (E 951).
Ability to influence reaction speed when driving vehicles or other mechanisms
Since the drug may cause dizziness, patients should be warned to drive and operate other machinery with caution.
Use during pregnancy or breastfeeding
Pregnancy. There are limited data on the use of cefuroxime in pregnant women. Animal studies have not shown any adverse effects of cefuroxime axetil on pregnancy, embryonal and foetal development, parturition or postnatal development. The drug should be used in pregnant women only if the potential benefit outweighs the potential risk.
Breastfeeding. Cefuroxime passes into breast milk in small amounts. When using therapeutic doses of the drug, the development of adverse reactions is not expected, but the risk of diarrhea or fungal infection of the mucous membranes in the child cannot be excluded. Therefore, in connection with these reactions, it may be necessary to discontinue breastfeeding. The possibility of a sensitizing effect of the drug should also be taken into account. Cefuroxime is prescribed during breastfeeding only after a doctor has assessed the benefit-risk ratio of its use.
Fertility: There are no data on the effect of cefuroxime axetil on fertility in humans. Animal reproduction studies have not shown any effect of this medicinal product on fertility.
Method of administration and doses
Antibiotic susceptibility may vary over time and by region. Local antibiotic susceptibility data should be consulted if necessary.
Usually the duration of treatment is 7 days (can be from 5 to 10 days).
For better absorption, it is recommended to take the drug after meals.
The dosage of the drug for adults and children depending on the infection is given in the tables.
Adults and children (≥ 40 kg):
| Indications for use | Dose |
| Acute tonsillitis and pharyngitis, acute bacterial sinusitis | 250 mg 2 times a day |
| Acute otitis media | 500 mg 2 times a day |
| Exacerbation of chronic bronchitis | 500 mg 2 times a day |
| Cystitis | 250 mg 2 times a day |
| Pyelonephritis | 250 mg 2 times a day |
| Uncomplicated skin and soft tissue infections | 250 mg 2 times a day |
| Lyme disease | 500 mg 2 times a day for 14 days (therapy may last from 10 to 21 days) |
Children (< 40 kg):
| Indications for use | Dose |
| Acute tonsillitis and pharyngitis, acute bacterial sinusitis | 10 mg/kg 2 times a day, maximum dose – 125 mg 2 times a day |
| Children aged 2 years and older with otitis media or, if necessary, for more serious infections | 15 mg/kg 2 times a day, maximum dose – 250 mg 2 times a day |
| Cystitis | 15 mg/kg 2 times a day, maximum dose – 250 mg 2 times a day |
| Pyelonephritis | 15 mg/kg 2 times a day, maximum dose – 250 mg 2 times a day for 10-14 days |
| Uncomplicated skin and soft tissue infections | 15 mg/kg 2 times a day, maximum dose – 250 mg 2 times a day |
| Lyme disease | 15 mg/kg 2 times a day, maximum dose – 250 mg 2 times a day for 14 days (from 10 to 21 days) |
The 250 mg tablets are scored on both sides and can be divided into equal doses of 125 mg.
There is no experience with the use of cefuroxime axetil in children under 3 months of age. It is recommended that children be given the drug in suspension form.
Cefuroxime acetyl tablets and cefuroxime acetyl granules for suspension are not bioequivalent, so these dosage forms are not interchangeable on a milligram basis.
Cefuroxime axetil is also available as a sodium salt for parenteral use. This allows sequential therapy with a single antibiotic when switching from parenteral to oral administration, if clinically indicated.
Sequential therapy.
Exacerbation of chronic bronchitis: 750 mg of cefuroxime sodium 2-3 times a day (intravenously or intramuscularly) for 48-72 hours, followed by cefuroxime axetil 500 mg 2 times a day orally for 5-10 days.
The duration of both parenteral and oral treatment should be determined taking into account the severity of the infection and the patient's condition.
Patients with renal failure.
Cefuroxime is excreted primarily by the kidneys. In patients with severe renal impairment, a reduced dose of cefuroxime is recommended to compensate for its slower excretion (see table below).
| Creatinine clearance (ml/min) | T½ (hours) | Recommended dosage |
| ≥ 30 | 1.4-2.4 | No dose adjustment is required (use standard dose of 125 mg to 500 mg 2 times a day) |
| 10-29 | 4.6 | Standard individual dose every 24 hours |
| < 10 | 16.8 | Standard individual dose every 48 hours |
| During hemodialysis | 2-4 | One additional standard dose should be administered after each dialysis. |
Patients with liver failure.
There are no data on the use of this medicinal product in patients with hepatic impairment. Since cefuroxime is excreted primarily by the kidneys, it is expected that pre-existing hepatic impairment will not affect the pharmacokinetics of cefuroxime.
Children
There is no experience with the use of cefuroxime axetil in children under 3 months of age. It is recommended that children be given the drug in suspension form.
Overdose
Overdose of cephalosporins may cause neurological complications, including encephalopathy, convulsions, and coma. Symptoms of overdose may occur if the dose of the drug has not been appropriately adjusted for patients with impaired renal function. Serum cefuroxime levels can be reduced by hemodialysis and peritoneal dialysis.
Adverse reactions
Adverse reactions with cefuroxime axetil are mild and generally reversible. The adverse reactions listed below are classified by system organ class and frequency. The frequency of occurrence is defined as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), not known (frequency cannot be estimated from the lack of data).
Infections and infestations: common: Candida overgrowth; not known: Clostridium difficile overgrowth.
From the blood and lymphatic system: often - eosinophilia; infrequently - positive Coombs test, thrombocytopenia, leukopenia (sometimes profound); very rarely - hemolytic anemia.
Cephalosporins as a class have the property of being absorbed on the surface of the erythrocyte membrane and interacting with antibodies there, which can lead to a positive Coombs test (impact on blood compatibility) and (very rarely) to hemolytic anemia.
On the part of the immune system: hypersensitivity reactions, including infrequently - skin rashes; rarely - urticaria, itching; very rarely - drug fever, serum sickness, anaphylaxis; unknown - Jarisch-Herxheimer reaction.
From the nervous system: often - headache, dizziness.
On the part of the digestive tract: often - gastroenterological disorders, including diarrhea, nausea, abdominal pain; infrequently - vomiting; rarely - pseudomembranous colitis (see section "Special instructions").
Skin and subcutaneous tissue disorders: very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematous necrolysis); not known - angioedema.
Children.
The safety profile of cefuroxime in children is similar to that in adult patients.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
7 tablets in a blister, 2 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Sandoz GmbH – TechOps.
Location of the manufacturer and its business address
Biochemiststrasse 10, 6250 Kundl, Austria.
