Cefpodoxime Proxetil is an orally administered, extended-spectrum, semi-synthetic antibiotic of the cephalosporin class (third generation). Cefpodoxime Proxetil is a prodrug; its active metabolite is cefpodoxime. Cefpodoxime is stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and cephalosporins, due to their production of beta-lactamase, may be susceptible to cefpodoxime. Cefpodoxime is inactivated by certain extended-spectrum beta-lactamases. The bactericidal activity of cefpodoxime results from its inhibition of cell wall synthesis.
Cefpodoxime is active against a wide-spectrum of Gram-positive and Gram-negative bacteria. Cefpodoxime has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections:
Staphylococcus aureus (methicillin-susceptible strains, including those penicillinase-producing strains)
NOTE: Cefpodoxime is inactive against methicillin-resistant staphylococci.
Staphylococcus saprophyticus
Streptococcus pneumoniae (excluding penicillin-resistant strains)
Streptococcus pyogenes
scherichia coli
Klebsiella pneumoniae
Proteus mirabilis
Haemophilus influenzae (including beta-lactamase-producing strains)
Moraxella catarrhalis
Neisseria gonorrhoeae (including penicillinase-producing strains)
The following in vitro data are available, but their clinical significance is unknown. At least 90% of the following microorganisms exhibit an in vitro minimum inhibitory concentration (MIC) less than or equal to the susceptible breakpoint for Cefpodoxime. However, the safety and efficacy of cefpodoxime in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials.
treptococcus agalactiae
Streptococcus spp. (Groups C, F, G)
NOTE: Cefpodoxime is inactive against enterococci.
itrobacter diversus
Klebsiella oxytoca
Proteus vulgaris
Providencia rettgeri
Haemophilus parainfluenzae
NOTE: Cefpodoxime is inactive against most strains of Pseudomonas and Enterobacter.

Eptostreptococcus magnus
Cefpodoxime proxetil is a prodrug that is absorbed from the gastrointestinal tract and de-esterified to its active metabolite, cefpodoxime.
Cefpodoxime is taken up in the intestine and is hydrolysed to the active metabolite, cefpodoxime. The maximum plasma concentration is 2.5 mg/l after a dose of 200 mg respectively. Following administration of 200 mg twice daily over 14.5 days, the plasma pharmacokinetic parameters of cefpodoxime remain unchanged.
The extent of absorption (mean AUC) and the mean peak plasma concentration were increased when the film-coated tablets were administered with food. Following a 200 mg tablet dose taken with food, the AUC was 21-33% higher than under fasting conditions, and the peak plasma concentration averaged 3.1 μg/mL in fed subjects versus 2.6 μg/mL in fasted subjects. Time-to-peak concentration was not significantly different between fed and fasted subjects.
Over the recommended dosing range (100-400 mg), the rate and extent of cefpodoxime absorption exhibited dose-dependency; the dose-normalized Cmax and AUC decreased by up to 32% with increasing dose. Over the recommended dosing range, the Tmax was approximately 2-3 hours and the T1/2 ranged from 2.09 hours to 2.84 hours. Mean Cmax was 2.3 μg/mL for the 200 mg dose, and 3.9 μg/mL for the 400 mg dose. In patients with normal renal function, neither accumulation nor significant changes in other pharmacokinetic parameters were noted following multiple oral doses of up to 400 mg q12hours.
Protein binding of cefpodoxime ranges from 22% to 33% in serum, principally to albumin and from 21% to 29% in plasma.
Concentrations of cefpodoxime in excess of the MICs for common pathogens can be achieved in lung parenchyma, bronchial mucosa, pleural fluid, tonsils, interstitial fluid and prostate tissue. Skin Blister: Following multiple-dose administration, every 12 hours for 5 days, of 200 mg or 400 mg cefpodoxime proxetil, the mean maximum cefpodoxime concentration in skin blister fluid averaged 1.6 and 2.6 μg/ml, respectively. Skin blister fluid cefpodoxime levels at 12 hours after dosing averaged 0.2 and 0.4 μg/mL for the 200 mg and 400 mg multiple-dose regimens, respectively.V Lung Tissue: Following a single oral dose of 200 mg cefpodoxime proxetil, the mean maximum cefpodoxime concentration in lung tissue averaged 0.63 μg/g at 3 hours post-dosing, 0.52 μg/g at 6 hours post-dosing, and 0.19 μg/g at 12 hours post-dosing. The results of this study indicated that cefpodoxime penetrated into lung tissue and produced sustained drug concentrations for at least 12 hours after dosing at levels that exceeded the MIC90 for Streptococcus pneumoniae and Haemophilus influenzae.
Tonsil Tissue: Following a single, oral 100 mg cefpodoxime proxetil film-coated tablet, the mean maximum cefpodoxime concentration in tonsil tissue averaged 0.24 mcg/g at 4 hours post-dosing and 0.09 mcg/g at 7 hours post-dosing. Equilibrium was achieved between plasma and tonsil tissue within 4 hours of dosing. No detection of cefpodoxime in tonsillar tissue was reported 12 hours after dosing. These results demonstrated that concentrations of cefpodoxime exceeded the MIC90 of S. pyogenes for at least 7 hours after dosing of 100 mg of cefpodoxime proxetil. Cerebrospinal Fluid (CSF): Adequate data on CSF levels of cefpodoxime are not available.
As the majority of cefpodoxime is eliminated in the urine, the concentration is high. (Concentrations in fractions of 0-4, 4-8, 8-12 hours after a single dose exceed the MIC90 of common urinary pathogens). Good diffusion of cefpodoxime is also seen into renal tissue, with concentrations above MIC90 of the common urinary pathogens, 3-12 hours after an administration of a single 200 mg dose (1.6-3.1μG/G). Concentrations of cefpodoxime in the medullary and cortical tissues are similar.
The main route of excretion is renal; 80% is excreted unchanged in the urine, with an elimination half-life of approximately 2.4 hours.
The pharmacokinetics of cefpodoxime was investigated in 29 patients aged 1 to 17 years. Each patient received a single, oral, 5 mg/kg dose of cefpodoxime oral suspension. Plasma and urine samples were collected for 12 hours after dosing. The plasma levels reported from this study are as follows: