Axetine

Axetine

cefuroxime

Manufacturer:

Medochemie

Distributor:

Medochemie
Full Prescribing Info
Contents
Cefuroxime axetil.
Description
Each tablet also contains the following excipients: Microcrystaline cellulose 105, colloidal anhydrous silica, crosscarmellose sodium, sodium lauryl sulphate, hydrogenated vegetable oil, hydroxypropyl methylcellulose (methocel E5), propylene glycol, titanium dioxide and talc.
Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to most β-lactamases and is active against a wide range of gram-positive and gram-negative organisms.
Action
Pharmacotherapeutic Group: Second generation cephalosporins. ATC Code: J01DC02.
Pharmacology: Pharmacodynamics: Cefuroxime inhibits cell wall production and are selective inhibitors of peptidoglycan synthesis.
Breakpoints: According to the EUCAST clinical breakpoint table v. 2, valid from January 1, 2012, the following breakpoints have been defined for cefuroxime axetil: See table.

Click on icon to see table/diagram/image

Pharmacokinetics: After oral administration cefuroxime axetil is slowly absorbed from the gastrointestinal tract and rapidly hydrolysed in the intestinal mucosa and blood to release cefuroxime into the circulation.
Optimum absorption occurs when it is administered shortly after a meal.
Peak serum levels (2-3 mg/L for a 125 mg dose, 4-6 mg/L for a 250 mg dose, 5-8 mg/L for a 500 mg dose and 9-14 mg/L for a 1 g dose) occur approximately 2-3 hrs after dosing when taken after food, unlike IV dosing which peaks immediately.
The absorption of cefuroxime from the suspension is more prolonged compared with tablets, leading to later, lower peak serum levels and slightly reduced systemic bioavailability (4-17% less). Post peak levels, the serum half life (t½) is between 1 hr and 1.5 hrs. Protein-binding has been variously stated as 33-50% depending on the methodology used. Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion.
Concurrent administration of probenecid increases the area under the mean serum concentrations time curve by 50%. Serum levels of cefuroxime are reduced by dialysis.
Microbiology: Susceptibility: Cefuroxime is usually active against the following organisms in vitro.
Aerobes Gram Negative: Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains), Escherichia coli, Klebsiella spp, Proteus mirabilis, Providencia spp, Proteus rettgeri.
Aerobes Gram Positive: Staphylococcus aureus and Staphylococcus epidermidis (including penicillinase producing strains but excluding methicillin resistant strains), Streptococcus pyogenes (and other β-haemolytic streptococci), Streptococcus pneumoniae, Streptococcus Group B (Streptococcus agalactiae).
Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp), gram positive bacilli (including Clostridium spp), gram negative bacilli (including Bacteroides spp and Fusobacterium spp), Propionibacterium spp.
Other Organisms: Borrelia burgdorferi.
The Following Organisms are Not Susceptible to Cefuroxime: Clostridium difficile, Pseudomonas spp, Campylobacter spp, Acinetobacter calcoaceticus, Listeria monocytogenes, methicillin resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, Legionella spp.
Some Strains of the Following Genera are Not Susceptible to Cefuroxime: Enterococcus (Streptococcus) faecalis, Morganella morganii, Proteus vulgaris, Enterobacter spp, Citrobacter spp, Serratia spp, Bacteroides fragilis.
Indications/Uses
Treatment of infections caused by sensitive bacteria including: Upper respiratory tract infections eg, ear, nose and throat infections (eg, otitis media, sinusitis, tonsillitis and pharyngitis); lower respiratory tract infections eg, pneumonia, acute bronchitis and acute exacerbations of chronic bronchitis; genitourinary tract infections eg, pyelonephritis, cystitis and urethritis; skin and soft tissue infections eg, furunculosis, pyoderma and impetigo; gonorrhoea, acute uncomplicated gonococcal urethritis and cervicitis.
Cefuroxime is also available as the sodium salt for parenteral administration. This permits the use of sequential therapy with the same antibiotic, when a change from parenteral to oral therapy is clinically indicated. Where appropriate Axetine is effective when used following initial parenteral Axetine in the treatment of pneumonia and acute exacerbations of chronic bronchitis.
Consideration should be given to official guidance on the appropriate use of antibacterial agents.
Dosage/Direction for Use
The usual course of therapy is seven days (range 5-10 days).
Adults: Most Infections: 250 mg twice daily. Urinary Tract Infections: 125 mg twice daily. Mild to Moderate Lower Respiratory Tract Infections eg, Bronchitis: 250 mg twice daily. More Severe Lower Respiratory Tract Infections, or if Pneumonia is Suspected: 500 mg twice daily. Pyelonephritis: 250 mg twice daily. Uncomplicated Gonorhhoea: Single dose of 1g.
Sequential Therapy: Pneumonia: 1.5 g, 2 or 3 times a day (IV or IM) for 48-72 hrs, followed by 500 mg twice daily Axetine oral therapy for 7-10 days.
Acute Exacerbations of Chronic Bronchitis: 750 mg, 2 or 3 times a day (IV or IM) for 48-72 hrs, followed by 500 mg twice daily Axetine oral therapy for 5-10 days.
Duration of both parenteral and oral therapy is determined by the severity of the infection and the clinical status of the patient.
Children: Most Infections: 125 mg twice daily, to a maximum of 250 mg daily. ≥2 years: Otitis Media or, where Appropriate, with More Severe Infections: 250 mg (one 250 mg tablet or two 125 mg tablets) twice daily, to a maximum of 500 mg daily.
Administration: Cefuroxime axetil should be taken after food for optimum absorption.
Axetine tablets should not be crushed and are therefore unsuitable for treatment of patients eg, younger children, who cannot swallow tablets. In children cefuroxime oral suspension may be used.
Overdosage
Cephalosporins may cause cerebral irritancy leading to convulsions. In case of overdose cefuroxime serum levels can be reduced by haemodialysis and peritoneal dialysis.
Contraindications
Hypersensitivity to cefuroxime, other cephalosporins or to any of the excipients of Axetine.
Special Precautions
If after administration of cefuroxime axetil sensitivity reactions occur, the use should be discontinued immediately and an appropriate treatment should be established. Special care is indicated in patients who have experienced an allergic reaction to penicillins or other β-lactams.
As with other broad spectrum antibiotics, prolonged use of cefuroxime axetil may result in the overgrowth of non-susceptible organisms (eg, Candida, Enterococci and Clostridium difficile, which may require interruption of treatment.
In patients who develop severe diarrhoea during or after use of cefuroxime axetil, the risk of life-threatening pseudomembranous colitis should be taken into account. The use of cefuroxime axetil should be discontinued and the appropriate treatment established.
With a sequential therapy regime the timing of change to oral therapy is determined by severity of the infection, clinical status of the patient and susceptibility of the pathogens involved. If there is no clinical improvement within 72 hrs, then the parenteral course of treatment must be continued.
Please refer to the relevant prescribing information for cefuroxime sodium before initiating sequential therapy.
Effects on the Ability to Drive or Operate Machinery: As this medicine may cause dizziness, patients should be warned to be cautious when driving or operating machinery.
Use in pregnancy & lactation: There is no experimental evidence of embryopathic or teratogenic effects attributable to cefuroxime axetil but, as with all drugs, it should be administered with caution during the early months of pregnancy. Cefuroxime is excreted in human milk, and consequently caution should be exercised when cefuroxime axetil is administered to a nursing mother.
Use in children: There is no experience of using cefuroxime in children <3 months.
Adverse Reactions
Adverse drug reactions to cefuroxime axetil are generally mild and transient in nature. The frequency categories assigned to the adverse reactions below are estimates, as for most reactions suitable data (eg, from placebo-controlled studies) for calculating incidence were not available. In addition the incidence of adverse reactions associated with cefuroxime axetil may vary according to the indication.
Data from large clinical studies were used to determine the frequency of very common to rare undesirable effects. The frequencies assigned to all other undesirable effects (ie, those occurring at <1/10,000) were mainly determined using post-marketing data and refer to a reporting rate rather than true frequency. Placebo-controlled trial data were not available. Where incidences have been calculated from clinical trial data, these were based on drug-related (investigator assessed) data.
The following convention has been used for the classification of frequency: Very common ≥1/10; common ≥1/100 and <1/10; uncommon ≥1/1000 and <1/100; rare ≥1/10,000 and <1/1000; very rare <1/10,000.
Infections and Infestations: Common: Overgrowth of Candida.
Blood and Lymphatic System Disorders: Common: Eosinophilia. Uncommon: Positive Coombs' test, thrombocytopenia, leukopenia (sometimes profound). Very Rare: Haemolytic anaemia.
Cephalosporins as a class tend to be absorbed onto the surface of red cells membranes and react with antibodies directed against the drug to produce a positive Coombs' test (which can interfere with cross-matching of blood) and very rarely haemolytic anaemia.
Immune System Disorders: Hypersensitivity reactions including: Uncommon: Skin rashes. Rare: Urticaria, pruritus. Very Rare: Drug fever, serum sickness, anaphylaxis.
Nervous System Disorders: Common: Headache, dizziness.
Gastrointestinal Disorders: Common: Gastrointestinal disturbances including diarrhoea, nausea, abdominal pain. Uncommon: Vomiting. Rare: Pseudomembranous colitis.
Hepatobiliary Disorders: Common: Transient increases of hepatic enzyme levels, [ALT (SGPT), AST (SGOT), LDH]. Very Rare: Jaundice (predominantly cholestatic), hepatitis.
Skin and Subcutaneous Tissue Disorders: Very Rare: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematic necrolysis) (See Immune System Disorders as previously discussed.)
Drug Interactions
Drugs which reduce gastric acidity may result in a lower bioavailability of cefuroxime compared with that of the fasting state and tend to cancel the effect of enhanced postprandial absorption. In common with other antibiotics, cefuroxime may affect the gut flora, leading to lower oestrogen reabsorption and reduced efficacy of combined oral contraceptives.
As a false negative result may occur in the ferricyanide test, it is recommended that either the glucose oxidase or hexokinase methods are used to determine blood/plasma glucose levels in patients receiving cefuroxime axetil. This antibiotic does not interfere in the alkaline picrate assay for creatinine.
Incompatibilities: Not applicable.
Storage
Store below 30°C. Protect from light.
Shelf-Life: 36 months.
MIMS Class
ATC Classification
J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
Tab 250 mg (white, capsule-shaped tablet, scored on one side, having a nucleus diameter of 14 mm) 1 x 10's . 500 mg (white, capsule shaped tablet, scored on one side, having a nucleus diameter of 19 mm) 1 x 10's.
The scoreline is only to facilitate breaking for ease of swallowing and not to divide into equal doses.
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