Auroxetil tablets 500 mg blister No. 10

Instructions for use: Auroxetil tablets 500 mg blister pack No. 10

Composition

active ingredient: cefuroxime axetil;

1 film-coated tablet contains cefuroxime axetil (equivalent to cefuroxime) 250 mg or 500 mg;

excipients: microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, colloidal anhydrous silicon dioxide, hydrogenated vegetable oil, hypromellose, polyethylene glycol, titanium dioxide (E 171).

Dosage form

Film-coated tablets.

Main physicochemical properties: off-white to white, capsule-shaped, film-coated tablets, debossed with "AZ3" on one side and plain on the other side for the 250 mg dosage and off-white to white, capsule-shaped, film-coated tablets, debossed with "AZ4" on one side and plain on the other side for the 500 mg dosage.

Pharmacotherapeutic group

Antimicrobials for systemic use. Beta-lactam antibiotics. 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:

*All methicillin-resistant Staphylococcus 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.

Serum cefuroxime levels are reduced by dialysis.

Indication

Auroxetil 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.

The drug should be prescribed in accordance with existing official recommendations for the prescription of antibacterial agents.

Contraindication

Hypersensitivity to cephalosporin antibiotics, cefuroxime or to any of the components of the drug. History of severe hypersensitivity reactions (e.g. anaphylactic reactions) to any other type of beta-lactam antibiotics (penicillins, monobactams and carbapenems).

Interaction with other medicinal products and other types of interactions

Drugs that reduce gastric acidity may reduce the bioavailability of Auroxetil and have the property of eliminating the effect of improved absorption after eating.

Since the ferrocyanide test may give a false-negative result, it is recommended that glucose oxidase or hexokinase methods be used to determine blood and plasma glucose levels in patients treated with cefuroxime axetil. Cefuroxime does not interfere with the alkaline picrate assay for creatinine.

Concomitant use with probenecid is not recommended, as it significantly increases the peak concentration, area under the serum concentration-time curve (AUC), and half-life of cefuroxime.

Concomitant use with oral anticoagulants may lead to an increase in the INR (international normalized ratio).

Serum cefuroxime levels are reduced by dialysis.

Cefuroxime in high doses should be administered with caution to patients taking strong diuretics, aminoglycosides, or amphotericin, as such combinations increase the risk of nephrotoxicity.

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 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 may occur with antibiotics and may range from mild to life-threatening. Therefore, it is important to keep this in mind if a patient develops 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. Drugs that inhibit peristalsis should not be prescribed.

During treatment of Lyme disease with cefuroxime axetil, a Jarisch-Herxheimer reaction has been observed, which is a direct result of the bactericidal action of cefuroxime axetil on the causative organism of Lyme disease, the spirochete Borrelia burgdorferi. Patients should be advised 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 Summary of Product Characteristics for cefuroxime sodium should be consulted.

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. Cefuroxime axetil should be used in pregnant women only if the potential benefit outweighs the potential risk.

Breastfeeding period

Cefuroxime passes into breast milk in small quantities. 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 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 effects of cefuroxime axetil on fertility in humans. Animal reproduction studies have not shown any effect of this medicinal product on fertility.

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.

Method of administration and doses

Antibiotic susceptibility varies by region and may change over time. 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 tables 1, 2.

Table 1

Adults and children (≥ 40 kg)

Table 2

Children (< 40 kg)

There is no experience with the use of cefuroxime axetil in children under 3 months of age.

Auroxetil tablets cannot be broken, so they are not prescribed to patients who cannot swallow tablets. It is recommended to prescribe the drug in the form of a suspension to children.

Cefuroxime axetil tablets are not bioequivalent to cefuroxime axetil oral suspension, therefore these products are not interchangeable on a milligram-for-milligram basis.

Patients with renal insufficiency

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 3).

Table 3

Patients with hepatic insufficiency

There are no data on the use of this medicinal product in patients with hepatic impairment. Cefuroxime is excreted primarily by the kidneys, therefore, 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. Auroxetil tablets cannot be broken and are therefore not recommended for patients who cannot swallow tablets. It is recommended that children be given the suspension.

Overdose

Overdose of cephalosporins may cause brain irritation and 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 (see sections "Method of administration and dosage" and "Special instructions for use").

Serum levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis.

Side effects

Side effects of cefuroxime axetil are mild and mostly reversible.

Adverse reactions, information about which is given below, are classified by organ system and by frequency of occurrence. By frequency of occurrence, they are divided into the following categories:

very common (≥ 1/10), common (≥ 1/100 and < 1/10), uncommon (≥ 1/1000 and < 1/100), rare (≥ 1/10000 and < 1/1000), very rare (< 1/10000).

Children.

The safety profile of cefuroxime in children is similar to that in adult patients.

Reporting of suspected adverse reactions. It is important to report suspected adverse reactions after the marketing authorisation of a medicinal product. This will allow for continued monitoring of the benefit/risk balance. Please report suspected adverse reactions via the national reporting system.

Expiration date

3 years.

Storage conditions

Store out of the reach of children at a temperature not exceeding 30 °C.

Packaging

10 tablets in a blister, 1 blister in a cardboard box.

Vacation category

According to the recipe.

Producer

Aurobindo Pharma Ltd. Unit VI, Block D/Aurobindo Pharma Ltd. Unit V Block D.

Address

Sy. No. 329/39 and 329/47, Chitkul Village, Patancheru Mandal, Medak District, Telangana state, 502307 India/Sy. No. 329/39 & 329/47, Chitkul Village, Patancheru Mandal, Medak District, Telangana state, 502307 India.