Levexime-500

White, elongated, biconvex, on one side scored and plain on the other side film-coated tablets.
Each film-coated tablet contains: Cefuroxime Axetil eq. to Cefuroxime 500 mg.

Pharmacotherapeutic group: antibacterials for systemic use, second-generation cephalosporins.
Pharmacology: In vivo bactericidal activity of Cefuroxime axetil is due to Cefuroxime's binding to essential target proteins and the resultant inhibition of cell wall synthesis. Cefuroxime has bactericidal activity against a wide range of common pathogens, including many beta-lactamase-producing strains.
Cefuroxime is stable to many bacterial beta-lactamases, especially plasmid-mediated enzymes that are commonly found in enterobacteriaceae.
Mechanism of action: Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound Cefuroxime. Cefuroxime is a well characterised and effective antibacterial agent which has bactericidal activity against a wide range of common pathogens, including beta-lactamase producing strains.
Cefuroxime has good stability to bacterial beta-lactamase, and consequently is active against many ampicillin-resistant or amoxicillin-resistant strains.
The bactericidal action of Cefuroxime results from inhibition of cell wall synthesis by binding to essential target proteins.
Pharmacokinetics: Cefuroxime axetil is absorbed from the gastrointestinal tract and is rapidly hydrolysed in the intestinal mucosa and blood to release Cefuroxime; absorption is enhanced in the presence of food. Peak plasma concentrations are reported about 2 to 3 hours after an oral dose. The sodium salt is given by intramuscular or intravenous injection. Peak plasma concentrations of about 27 micrograms/mL have been achieved 45 minutes after an intramuscular dose of 750 mg with measurable amounts present 8 hours after a dose. Up to 50% of Cefuroxime in the circulation is bound to plasma proteins.
The plasma half-life is about 70 minutes and is prolonged in patients with renal impairment and in neonates. Cefuroxime is widely distributed in the body including pleural fluid, sputum, bone, synovial fluid, and aqueous humour, but only achieves therapeutic concentrations in the CSF when the meninges are inflamed. It crosses the placenta and has been detected in breast milk.
Cefuroxime is excreted unchanged, by glomerular filtration and renal tubular secretion, and high concentrations are achieved in the urine. On injection, most dose of Cefuroxime is excreted within 24 hours, the majority within 6 hours. Probenecid competes for renal tubular secretion with Cefuroxime resulting in higher and more prolonged plasma concentrations of Cefuroxime. Small amounts of Cefuroxime are excreted in bile.
Plasma concentrations are reduced by dialysis.

For the treatment of susceptible infections. Cefuroxime is used in bone and joint infections, bronchitis (and other lower respiratory tract infections), gonorrhea, meningitis (although treatment failures have been reported in H. influenzae meningitis), otitis media, peritonitis, pharyngitis, sinusitis, skin infections (including soft tissue infections), and urinary tract infections. It is also used for surgical infection prophylaxis.

For Uncomplicated Urinary Tract Infections: 125 mg twice daily.
For Respiratory Tract Infections: 250 to 500 mg twice daily.
A dose for children more than 3 months of age: 125 mg twice daily or 10 mg/kg twice daily to a maximum of 250 mg daily.
Children over 2 years of age with otitis media: 250 mg twice daily or 15 mg/kg twice daily to a maximum of 500 mg daily.
Adults with Pneumonia or with Acute Exacerbations of Chronic Bronchitis: 1.5 g twice daily or 750 mg twice daily, respectively, in parenteral route followed by oral Cefuroxime 500 mg twice daily in each case.
For Lyme disease in adults: 500 mg is given twice daily for 20 days.
For Uncomplicated Gonorrhea: A single 1 g oral dose of Cefuroxime can be given. In each case an oral dose of Probenecid 1 g may be given with Cefuroxime.
Or as prescribed by the physician.

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.

Hypersensitivity to cephalosporin antibiotics.

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. Before beginning treatment, it should be established whether the patient has a history of severe hypersensitivity reactions to Cefuroxime, to other cephalosporins or to any other type of beta-lactam agent. Caution should be used if Cefuroxime is given to patients with a history of non-severe hypersensitivity to other beta-lactam agents.
Jarisch-Herxheimer reaction: The Jarisch-Herxheimer reaction has been seen following Cefuroxime axetil treatment of Lyme disease. It results directly from the bactericidal activity of Cefuroxime axetil on the causative bacteria of Lyme disease, the spirochaete Borrelia burgdorferi. Patients should be reassured that this is a common and usually self-limiting consequence of antibiotic treatment of Lyme disease.
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 diarrhea 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. Medicinal products that inhibit peristalsis should not be given.
Interference with diagnostic tests: The development of a positive Coomb's Test associated with the use of Cefuroxime may interfere with crossmatching of blood. 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.
Cefuroxime Axetil should be given with caution to patients with renal impairment, dosage reduction may be necessary.
Renal and haematological status should be monitored especially during prolonged and high dose therapy.
Pseudomembranous colitis has been reported with the use of broad-spectrum antibiotics, therefore, it is important to consider its diagnosis in patients who develop serious diarrhea during or after antibiotic use.

Pregnancy: Cefuroxime Axetil should be administered with caution during the early months of pregnancy. This drug should be used during pregnancy only if clearly needed.
Lactation: Cefuroxime is excreted in human milk, and consequently caution should be exercised when Cefuroxime axetil is administered to a nursing mother.

Gastrointestinal disturbances, including diarrhea, nausea, and vomiting, have occurred in some patients receiving Cefuroxime Axetil. There have been rare reports of erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Mild to moderate hearing loss has been reported in some children given Cefuroxime for the treatment of meningitis.

Probenecid reduces the renal clearance of Cefuroxime.

Store at temperatures not exceeding 30°C.

Cephalosporins

J01DC02 - cefuroxime ; Belongs to the class of second-generation cephalosporins. Used in the systemic treatment of infections.

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