- ANTI-INFECTIVE DRUGS
- BETA-LACTAM ANTIBIOTICS
- Pharmaceutical Form : Dry Powder for oral suspension
- Composition : Cefuroxime ( as axetil ) 125 mg / 5 ml Susp
- Active Substance : Cefuroxime
Cefuroxime axetil undergoes hydrolysis by esterase enzymes to the active antibiotic, cefuroxime. Cefuroxime inhibits bacterial cell wall synthesis following attachment to penicillin binding proteins (PBPs). This results in the interruption of cell wall (peptidoglycan) biosynthesis, which leads to bacterial cell lysis and death.
After oral administration cefuroxime axetil is 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.
The rate of absorption of cefuroxime from the suspension is reduced compared with the tablets, leading to later, lower peak serum levels and reduced systemic bioavailability (4 to 17% less). Cefuroxime axetil oral suspension is not bioequivalent to cefuroxime axetil tablets, and therefore is not substitutable on a milligram-per-milligram basis. Protein binding has been stated as 33 to 50% depending on the methodology used. Cefuroxime passes the blood-brain barrier when the meninges are inflamed. Cefuroxime is not metabolised. The serum half-life is between 1 and 1.5 hours. Cefuroxime is effectively removed by dialysis.
Cefuroxime is indicated for the treatment of the infections listed below in adults and children from the age of 3 months.
- Acute streptococcal tonsillitis and pharyngitis.
- Acute bacterial sinusitis.
- Acute otitis media.
- Acute exacerbations of chronic bronchitis.
- Uncomplicated skin and soft tissue infections.
- Treatment of early Lyme disease.
Cefuroxime is contraindicated in patients with a known allergy to the cephalosporin group of antibiotics.
It is also contraindicated in patients with a history of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
The most common adverse reactions are Candida overgrowth, eosinophilia, headache, dizziness, gastrointestinal disturbances and transient rise in liver enzymes.
WARNINGS & PRECAUTIONS:
Hypersensitivity reactions: Special care is indicated in patients who have experienced an allergic reaction to penicillins or other beta-lactam antibiotics because there is a risk of cross-sensitivity. As with all beta-lactam antibacterial agents, serious and occasionally fatal hypersensitivity reactions have been reported. In case of severe hypersensitivity reactions, treatment with cefuroxime must be discontinued immediately and adequate emergency measures must be initiated.
Overgrowth of non-susceptible microorganisms: As with other antibiotics, use of cefuroxime axetil may result in the overgrowth of Candida. Prolonged use may also result in the overgrowth of other non-susceptible microorganisms (e.g. enterococci and Clostridium difficile), which may require interruption of treatment. Antibacterial agent–associated pseudomembranous colitis have been reported with nearly all antibacterial agents, including cefuroxime and may range in severity from mild to life threatening. This diagnosis should be considered in patients with diarrhoea during or subsequent to the administration of cefuroxime. Discontinuation of therapy with cefuroxime and the administration of specific treatment for Clostridium difficile should be considered.
Interference with diagnostic tests: It is recommended that either the glucose oxidase or hexokinase methods are used to determine blood/plasma glucose levels in patients receiving cefuroxime axetil.
There are limited data from the use of cefuroxime in pregnant women. Cefuroxime-MP should be prescribed to pregnant women only if the benefit outweighs the risk.
Cefuroxime is excreted in human milk in small quantities. Adverse effects at therapeutic doses are not expected, although a risk of diarrhoea and fungus infection of the mucous membranes cannot be excluded. Breastfeeding might have to be discontinued due to these effects. Cefuroxime should only be used during breastfeeding after benefit/risk assessment by the physician.
Effect on driving and operating machines:
As this medicine may cause dizziness, patients should be warned to be cautious when driving or operating machinery.
Drugs which reduce gastric acidity may result in a lower bioavailability of cefuroxime axetil compared with that of the fasting state and tend to cancel the effect of enhanced absorption after food.
Cefuroxime axetil may affect the gut flora, leading to lower oestrogen reabsorption and reduced efficacy of combined oral contraceptives.
Concomitant use with oral anticoagulants may give rise to increased INR.
DOSAGE AND METHOD OF ADMINISTRATION:
For optimal absorption cefuroxime axetil suspension should be taken with food.
The usual course of therapy is seven days (may range from five to ten days).
Adults and children ( ≥ 40 kg )
|Acute tonsillitis and pharyngitis, acute bacterial sinusitis||250 mg twice daily|
|Acute otitis media||500 mg twice daily|
|Acute exacerbations of chronic bronchitis||500 mg twice daily|
|Cystitis||250 mg twice daily|
|Pyelonephritis||250 mg twice daily|
|Uncomplicated skin and soft tissue infections||250 mg twice daily|
|Lyme disease||500 mg twice daily for 14 days (range of 10 to 21 days)|
Children (<40 kg)
|Acute tonsillitis and pharyngitis, acute bacterial sinusitis||10 mg/kg twice daily to a maximum of 125 mg twice daily|
|Children aged two years or older with otitis media or, where appropriate, with more severe infections||15 mg/kg twice daily to a maximum of 250 mg twice daily|
|Cystitis||15 mg/kg twice daily to a maximum of 250 mg twice daily|
|Pyelonephritis||15 mg/kg twice daily to a maximum of 250 mg twice daily for 10 to 14 days|
|Uncomplicated skin and soft tissue infections||15 mg/kg twice daily to a maximum of 250 mg twice daily|
|Lyme disease||15 mg/kg twice daily to a maximum of 250 mg twice daily for 14 days (10 to 21 days)|
There is no experience of using Cefuroxime in children under the age of 3 months.
In infants (from the age of 3 months) and children with a body mass of less than 40 kg, it may be preferable to adjust dosage according to weight or age. The dose in infants and children 3 months to 18 years is 10 mg/kg twice daily for most infections, to a maximum of 250 mg daily. In otitis media or more severe infections the recommended dose is 15 mg/kg twice daily to a maximum of 500 mg daily.
Cefuroxime is primarily excreted by the kidneys. In patients with markedly impaired renal function it is recommended that the dosage of cefuroxime should be reduced to compensate for its slower excretion. Elderly patients are more likely to have decreased renal function; therefore, the dose should be adjusted in accordance with the renal function in the elderly. Cefuroxime is effectively removed by dialysis.
Recommended doses for Cefuroxime Granules for Oral Suspension in renal impairment
|Creatinine clearance||T1/2 (hrs)||Recommended dosage|
|≥ 30 ml/min/1.73 m2||1.4 – 2.4||no dose adjustment necessary (standard dose of 125 mg to 500 mg given twice daily)|
|10 – 29 ml/min/1.73 m2||4.6||standard individual dose given every 24 hours|
|<10 ml/min/1.73 m2||16.8||standard individual dose given every 48 hours|
|Patients on haemodialysis||2 – 4||a further standard individual dose should be given at the end of each dialysis|
Directions for Mixing Cefuroxime Granules for Oral Suspension:
Prepare a suspension at the time of dispensing as follows: Shake the bottle to loosen the powder, add water for reconstitution (37 ml for CEFUROXIME 125 mg, and 19 ml for CEFUROXIME 250 mg) and replace the cap. Invert the bottle and vigorously shake the bottle.
Overdose can lead to neurological sequelae including encephalopathy, convulsions and coma. Symptoms of overdose can occur if the dose is not reduced appropriately in patients with renal impairment. Serum levels of cefuroxime can be reduced by haemodialysis and peritoneal dialysis.
The constituted suspension should be stored in a refrigerator (4-8) °C and used within 10 days.
PACKAGING: Granules for Oral Suspension in bottle 60 mL.