Ceftizoxime A Review of its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Use

Abstract

Ceftizoxime is a 'third generation' cephalosporin administered intravenously or intramuscularly. Like other third generation cephalosporins it has a wide spectrum of in vitro activity against Gram-positive and Gram-negative bacteria, is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains), and is resistant to hydrolysis by beta-lactamases. However, the third generation cephalosporins are less active than earlier cephalosporins against staphylococci and so could not be considered the drugs of choice. Like many currently available third generation cephalosporins, ceftizoxime has limited activity against Pseudomonas aeruginosa, and thus cannot be recommended as sole treatment of known or suspected non-urinary tract pseudomonal infections. Similarly, although favourable clinical results have been obtained in patients treated with ceftizoxime for infections caused by mixed aerobic/anaerobic organisms (such as intra-abdominal, and obstetric and gynaecological infections), the relatively low in vitro activity of ceftizoxime (in common with most other third generation cephalosporins) against Bacteroides fragilis and enterococci may restrict its usage in situations where these organisms are the suspected or proven pathogens. Ceftizoxime appears to be similar in efficacy to several other cephalosporins in lower respiratory tract infections in elderly and/or debilitated patients, and in chronic and/or complicated urinary tract infections, 2 clinical situations in which third generation cephalosporins may have a major role. Ceftizoxime is also effective clinically and bacteriologically in skin, soft tissue, bone and joint infections, septicaemia/bacteraemia, meningitis and neonatal infections. However, a few large, well designed clinical comparisons of efficacy with aminoglycosides are needed before ceftizoxime can be recommended as an alternative in patients in whom potential aminoglycoside toxicity is a concern. Single intramuscular doses of ceftizoxime appear similar in efficacy to aqueous procaine penicillin G in gonorrhoeae due to nonpenicillinase-producing Neisseria gonorrhoea, and ceftizoxime is also highly effective against penicillinase-producing strains. Although only a few infections have been treated to date, ceftizoxime may be useful in the treatment of gonorrhoea in places where penicillinase-producing strains are common. Thus, ceftizoxime appears to be an effective addition to the growing number of third generation cephalosporins. However, further studies are needed to confirm its relative efficacy compared with other new cephalosporins, in particular cefotaxime.(ABSTRACT TRUNCATED AT 400 WORDS)

Pharmacokinetics of cefepime after single and multiple intravenous administrations in healthy subjects

“…The levels of cefepime in plasma increase in a dose-proportional manner, and dose-independent parameters such as MRTiV, t112, CL., CLE, and Vs remained constant from the 250-to the 2,000-mg dose. These findings are consistent with those reported for other cephalosporins such as ceftazidime (16,26), cefpirome (21,22), cefpiramide (23), and cefotetan (24). The Cm.…”

“…It is likely that the CLR of cefepime, like that of ceftazidime (16,26), occurs by glomerular filtration, with negligible tubular secretion (1,3,5). A drug disposition study using radiolabeled cefepime clearly indicated that this cephalosporin undergoes minimal metabolism and is excreted primarily as an unchanged drug in urine in humans with normal kidney functions (4).…”

Postantibiotic effect of beta-lactam antibiotics on Escherichia coli evaluated by bioluminescence assay of bacterial ATP

“…Ceftazidime has its primary affinity for PBP 3 at low concentrations (14). We found short PAEs and mainly filaments for ceftazidime at up to 16 times the MIC.…”

“…We found short PAEs and mainly filaments for ceftazidime at up to 16 times the MIC. At higher concentrations of the drug, it also has affinities for PBP la and PBP lb (14). At 64 times the MIC and at higher concentrations, we observed PAEs of at least 2 h and a morphology of predominantly spheroplasts.…”

Ceftazidime/Avibactam: Who Says You Can’t Teach an Old Drug New Tricks?

“…It is well-described that ceftazidime displays timedependent pharmacodynamic activity requiring approximately 60% time above MIC for efficacy (33,34). However, the question of avibactam dosing frequency needed further elucidation.…”