Sign Out
Pharmacology: Pharmacokinetics: Zoltax: Cefuroxime axetil is absorbed from the GIT and is rapidly hydrolyzed in the intestinal mucosa and blood to cefuroxime; absorption is enhanced in the presence of food. Peak plasma concentrations are reported to about 2-3 hrs after an oral dose.
Up to 50% of cefuroxime in the circulation is bound to plasma proteins. The plasma t½ is about 70 min 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 adequate humor, but only achieves therapeutic concentrations in the cerebrospinal fluid (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.
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 concentration are reduced by dialysis.
Food Effect on Pharmacokinetics: Absorption of the tablet is greater when taken after food (absolute bioavailability of cefuroxime axetil tablet increases from 37-52%). Despite this difference in absorption, the clinical and bacteriologic responses of patients were independent of food intake at the time of tablet administration in 2 studies where this was assessed.
Renal Excretion: Cefuroxime is excreted unchanged in the urine. In adults, approximately 50% of the administered dose is recovered in the urine within 12 hrs. The pharmacokinetics of cefuroxime in the urine of pediatric patients have not been studied at this time. Until further data are available, the renal pharmacokinetic properties of cefuroxime axetil established in adults should not be extrapolated to pediatric patients.
Zoltax Injection: Cefuroxime sodium is given by IM or IV injection. Peak plasma concentrations of about 27 mcg/mL have been achieved 45 min after an IM dose of 750 mg with measurable amounts present 8 hrs after a dose.
Up to 50% of cefuroxime in the circulation is bound to plasma proteins. The plasma half-life (t½) is about 70 min 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 adequate humor, but only achieves therapeutic concentrations in the cerebrospinal fluid 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 the dose of cefuroxime is excreted within 24 hrs, the majority within 6 hrs.
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 concentration are reduced by dialysis.
Microbiology: Cefuroxime is a 2nd-generation cephalosporin antibiotic used in the treatment of susceptible infections. It is bactericidal and has a similar spectrum of antimicrobial action and pattern of resistance to those of cefamandole. Cefuroxime is more resistant to hydrolysis by β-lactamases than cefamandole and therefore, may be more active against β-lactamase-producing strains eg, 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 bacterial concentration when compared with minimum inhibitory concentration or with a significant inoculum effect. Reduced affinity of penicillin-binding proteins for cefuroxime has also been reported to be responsible in a β-lactamase-negative strain of H. influenzae.
Zoltax: Cefuroxime has been demonstrated to be active against most strains of the following organisms: Aerobic Gram-Positive Microorganisms: Staphylococcus aureus (including β-lactamase-producing strains), Streptococcus pneumoniae, Streptococcus pyogenes.
Aerobic Gram-Negative Microorganisms: Escherichia coli, H. influenzae (including β-lactamase-producing strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis and N. gonorrhoeae (including β-lactamase-producing strains).
Spirochetes: Borrelia burgdorferi.
Cefuroxime has been shown to be active in vitro against most strains of the following microorganisms; however, the clinical significance of these findings is unknown.
Cefuroxime exhibits in vitro minimum inhibitory concentrations (MICs) of ≤4 mcg/mL (systemic susceptible breakpoint) against most (≥90%) strains of the following microorganisms; however, the safety and effectiveness of cefuroxime in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled trials.
Aerobic Gram-Positive Microorganisms: Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae.
Note: Listeria monocytogenes and certain strains of enterococci eg, Enterococcus faecalis (formerly Streptococcus faecalis), are resistant to cefuroxime. Methicillin-resistant staphylococcus are resistant to cefuroxime.
Aerobic Gram-Negative Microorganisms: Morganella morganii, Proteus inconstans, Proteus mirabilis, Providencia retigen.
Note: Pseudomonas spp, Campylobacter spp, Acinetobacter calcoaceticus, Legionella spp and most strains of Serratia spp and Proteus vulgaris are resistant to most 1st- and 2nd-generation cephalosporins. Some strains of Morganella morganii, Enterobacter cloacae and Citrobacter spp have been shown by in vitro test to be resistant to cefuroxime and other cephalosporins.
Anaerobic Microorganism: Peptococcus niger.
Note: Most strains of Clostridium difficile and Bacteroides fragilis are resistant to cefuroxime.
Zoltax Injection: Cefuroxime for injection is indicated for the treatment of patients with infections caused by susceptible strains of the designated organism in the following diseases: Lower respiratory tract infections including pneumonia, caused by Streptococcus pneumoniae, Haemophilus influenzae (including ampicillin-resistant strains), Klebsiella spp, Staphylococcus aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes and Escherichia coli.
Urinary tract infections caused by Escherichia coli and Klebsiella spp.
Skin and skin structure infections caused by S. aureus (penicillinase- and non-penicillinase-producing strains), Streptococcus pyogenes, E. coli, Klebsiella and Enterobacter spp.
Septicemia caused by S. aureus (penicillinase- and non-penicillinase-producing strains), S. pneumoniae, E. coli, H. influenzae (including ampicillin-resistant strains) and Klebsiella spp.
Meningitis caused by S. pneumoniae, H. influenzae (including ampicillin-resistant strains), Neisseria meningitidis and S. aureus (penicillinase- and non-penicillinase-producing strains).
Gonorrhea: Uncomplicated and disseminated gonococcal infections due to Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains) in both males and females.
Bone and joint infections caused by S. aureus (penicillinase- and non-penicillinase-producing strains).
Clinical microbiological studies in skin and skin structure infection frequently reveal the growth of susceptible strains of both aerobic and anaerobic organisms. Cefuroxime has been used successfully in these mixed infections in which several organisms have been isolated.
In certain cases of confirmed or suspected gram-positive or gram-negative sepsis or in patients with other serious infections in which the causative organism has not been identified, cefuroxime may be used concomitantly with an aminoglycoside. The recommended doses of both antibiotics may be given depending on the severity of the infection and the patient's condition.
Prevention: Cefuroxime is also used for surgical infection prophylaxis. The preoperative prophylactic administration of cefuroxime may prevent the growth of susceptible disease-causing bacteria and thereby reduce the incidence of certain postoperative infections in patients undergoing surgical procedures (eg, vaginal hysterectomy) that are classified as clean-contaminated or potentially contaminated procedures. Effective prophylactic use of antibiotics in surgery depends on the time of administration. Cefuroxime should usually be given ½-1 hr before the operation to allow sufficient time to achieve effective antibiotic concentrations in the wound tissue during procedure. The dose should be repeated intraoperatively if the procedure is lengthy.
Prophylactic administration is usually not required after the surgical procedure ends and should be stopped within 24 hrs. In the majority of surgical procedures, continuing prophylactic administration of any antibiotic does not reduce the incidence of subsequent infections but will increase the possibility of adverse reactions and the development of bacterial resistance.
The preoperative use of cefuroxime has also been effective during open heart surgery for surgical patients in whom infections at the operative site would present a serious risk. For these patients, it is recommended that cefuroxime therapy be continued for at least 48 hrs after the surgical procedure ends. If an infection is present, specimens for culture should be obtained for the identification of the causative organism and appropriate antimicrobial therapy should be instituted.
