Comparative microbiological activity and pharmacokinetics of cefprozil

Abstract

In vitro studies on the activity of cefprozil have been conducted in Europe and North America. Against gram-negative bacilli, cefprozil and cefaclor are at least two to four times more active than cephalexin. Cefixime is more active against these organisms. Against gram-positive cocci, cefprozil is at least two to four times more active than cefaclor and cephalexin; cefixime has limited gram-positive activity, and is particularly inactive against staphylococci (MIC90 32 mg/l). Cefprozil is highly active against Streptococcus pneumoniae (unlike cefixime). Those strains of this genus that display intermediate resistance to pneumococci are more susceptible to cefprozil than cefaclor. Neisseria species and Moraxella catarrhalis are susceptible to cefprozil (MIC90 0.06 and 1 mg/l). beta-lactamase-producing strains of Haemophilus influenzae appear to be susceptible to cefprozil, as the reported MIC90 is 2-4 mg/l. Enterococci, Pseudomonas aeruginosa, and those strains of the Enterobacteriaceae that commonly possess a chromosomal cephalosporinase (e.g., Providencia, Morganella and Enterobacter) are generally considered to be resistant to cefprozil as well as to other oral cephalosporins. Cefprozil appears to display enhanced stability to the commonly encountered Tem-1 and SHV-1 plasmid-mediated beta-lactamases, as found in Haemophilus influenzae, Neisseria gonorrhoeae and the Enterobacteriaceae. Cefprozil is rapidly absorbed, reaching a maximum concentration 0.9 to 1.2 h post-dose. Following oral doses of 250 and 500 mg, the Cmax is 6.2 and 10.0 mg/l respectively. Serum half-lives are generally reported as between 1.2 and 1.4 h, and urine recovery is high, 57-70%.(ABSTRACT TRUNCATED AT 250 WORDS)