Cefuroxime is distributed throughout the body. It penetrates inflamed meninges in high enough concentrations to be effective in meningitis caused by susceptible organisms. Three-times-daily dosing is required to maintain effective plasma levels for most sensitive organisms, such as Neisseria meningitidis, Streptococcus pneumoniae, and H. influenzae. It has a plasma half-life of 1.4 hours.
Cefuroxime axetil (Ceftin) is the 1-acetyoxyethyl ester of cefuroxime. During absorption, this acid-stable, lipophilic, oral prodrug derivative of cefuroxime is hydrolyzed to cefuroxime by intestinal and/or plasma enzymes. The axetil ester provides an oral bioavailability of 35% to 50% of cefuroxime, depending on conditions. Oral absorption of the ester is increased by food but decreased by antacids and histamine H2-antagonists. The latter effect may be because of spontaneous hydrolysis of the ester in the intestine because of the higher pH created by these drugs. Axetil is used for the oral treatment of non-life-threatening infections caused by bacteria that are susceptible to cefuroxime. The prodrug form permits twice-a-day dosing for such infections.
Cefpodoxime proxetil (Vantin) is the isopropyloxycar-bonylethyl ester of the third-generation cephalosporin cefpodoxime. This orally active prodrug derivative is hydrolyzed by esterases in the intestinal wall and in the plasma to provide cefpodoxime. Tablets and a powder for the preparation of an aqueous suspension for oral pediatric administration are available. The oral bioavailability of cefpodoxime from the proxetil is estimated to be about 50%. Administration of the prodrug with food enhances its absorption. The plasma half-life is 2.2 hours, which permits administration on a twice-daily schedule.
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