Source: Health Products Regulatory Authority (ZA) Publisher: sanofi-aventis south africa (pty) ltd., 2 Bond Street, Midrand, 1685, South Africa
A 20.1.1 Broad and medium spectrum antibiotics
Cefpodoxime proxetil is a semisynthetic β-lactam antibiotic belonging to the third generation oral cephalosporin group. Cefpodoxime proxetil is the prodrug of the bactericidal antibiotic cefpodoxime. Cefpodoxime possesses in vitro bactericidal activity against a broad spectrum of Grampositive and Gram-negative bacteria. In vitro sensitivity does not necessarily imply in vivo efficacy. Therefore sensitivity tests must be performed. The mechanism of action is bactericidal through inhibition of bacterial cell wall biosynthesis enhanced by a high affinity for proteins at the cytoplasmic membrane.
The following organisms are not sensitive: Group D streptococci, Methicillin-resistant staphylococci (S. aureus and S. epidermidis), Staphylococcus saprophyticus, Corynebacteria, groups J and K, Listeria monocytogenes, Pseudomonas aeruginosa and Pseudomonas spp., Acinetobacter baumanii, Clostridium difficile, Bacteroides fragilis and related species.
The bioavailability of cefpodoxime proxetil is increased when the product is administered with meals, or when there is a decrease in gastric pH. An increase in gastric pH results in decreased bioavailability.
After oral administration, cefpodoxime proxetil is absorbed in the gastrointestinal tract and rapidly hydrolysed by non-specific esterases in the gastrointestinal wall to cefpodoxime, the active acid.
After oral administration of a single dose of 100 mg of cefpodoxime, the maximum plasma concentration (Cmax) obtained is 1 to 1,2 mg/l and after administration of a dose of 200 mg of cefpodoxime, the maximum plasma concentration (Cmax) obtained is 2,2 to 2,5 mg/l. In both cases the time (Tmax) taken to reach the maximum concentration is 2 to 3 hours.
Following administration of 100 and 200 mg twice daily for 14,5 days, the pharmacokinetic parameters of cefpodoxime remain unchanged, indicating that there is no accumulation of the active principle. The binding of cefpodoxime to plasma proteins is about 40 %. This binding is principally to albumin and is of the non-saturable type.
After oral administration of a single 5 mg/kg dose (200 mg maximum) of cefpodoxime to subjects between 4 and 12 years of age, the maximum plasma concentration (Cmax) is on average 2,6 mg/l. The time taken to reach the maximum concentration (Tmax) is 2 to 4 hours. The average plasma concentrations observed 8 and 12 hours after administration (residual) are 0,39 and 0,08 mg/l respectively.
Cefpodoxime proxetil diffuses well in lung parenchyma, bronchial mucosa, pleural fluid and tonsils.
The main metabolite is cefpodoxime, resulting from the hydrolysis of cefpodoxime proxetil. The elimination half-life of cefpodoxime is 2,4 hours. 80% of unchanged cefpodoxime is excreted in the urine.
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