ANTIMICROBIAL ACTION:
Cefuroxime is bactericidal and has a similar spectrum of antimicrobial action and pattern of resistance to those of cefamandole. It is more resistant to hydrolysis by beta-lactamases than cefamandole, and therefore may be more active against beta-lactamase-producing strains of, for example, Haemophilus influenzae and Neisseria gonorrhoeae. However, treatment failures have occurred in patients with H. influenzae meningitis given Cefuroxime and might be associated with a relatively high minimum bactericidal concentration when compared with the minimum inhibitory concentration or with a significant inoculum effect. Reduced affinity of penicillin-binding proteins for Cefuroxime has also been reported to be responsible for resistance in a beta-lactamase-negative strain of H. influenzae.
PHARMACOKINETICS:
Cefuroxime axetil is absorbed from the gastrointestinal tract and is rapidly hydrolysed in the intestinal mucosa and blood to 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. Following injection, most of a 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.
INDICATIONS:
Cefuroxime is a second-generation cephalosporin antibacterial used in the treatment of susceptible infections. These have included bone and joint infections, bronchitis (and other lower respiratory-tract infections), gonorrhoea, 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.
DOSAGE and ADMINISTRATION:
Adults – 750 mg to 1.5 g every 8 hours, for 5 to 10 days
Uncomplicated UTI’s, gonococcal infections, uncomplicated pneumonia
- 750 mg dose every 8 hours
In severe or complicated infections
- 1.5 g dose every 8 hours
Bacterial meningitis
- Not to exceed 3 g every 8 hours
Bone and joint infections
- 1.5 g every 8 hours
Preventive use for potentially contaminated surgical procedures
- 1.5 g IV prior to surgery followed by 750 mg every 8 hours when procedure is prolonged
Impaired Renal Function: A reduced dosage must be employed when renal function is impaired. Dosage should be determined by the degree of renal impairment and the susceptibility of the causative organism.
- CC 10 to 20 mL/minute: 750 mg twice daily
- CC less than 10 mL/minute: 750 mg once daily
Patients undergoing haemodialysis should receive an additional 750-mg dose following each dialysis; those undergoing continuous peritoneal dialysis may be given 750 mg twice daily.
Infants and Children above 3 months of age:
Most infections
50 to 100 mg/kg/day in equally divided doses every 6 to 8 hours
Severe or serious infections
100 mg/kg/day in equally divided doses every 6 to hours
Or as prescribed by the physician.
Direction for Reconstitution:
Dissolve completely 750 mg cefuroxime in 6 mL Sterile Water for Injection. Solution should be used within 5 hours of preparation if stored at a temperature not exceeding 25 ° C or within 48 hours if stored between 2 ° C and 8 ° C.
PRECAUTIONS:
Hypersensitivity to beta-lactam antibiotics, pregnancy and lactation
Mild to moderate hearing loss has been reported in some children given Cefuroxime for the treatment of meningitis.
CONTRAINDICATIONS:
Cefuroxime is contraindicated if there is a history of hypersensitivity to cephalexin or other cephalosporins.
SIDE EFFECTS / ADVERSE DRUG REACTIONS:
Hypersensitivity reactions, gastrointestinal disturbances, rarely pain at injection site, candidiosis, eosinophilia, neutropenia, leucopenia, thrombocytopenia, transient rise in liver enzymes, and positive Combo’s test.
INTERACTIONS:
Probenecid reduces the renal clearance of Cefuroxime.
AVAILABILITY:
Cefuroxime Sodium 750 mg Inj. X 1 vial plus diluent per box
STORAGE CONDITION:
Store at temperature not exceeding 25ºC. Protect from light.
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