Cefpodoxime proxetil is a prodrug that is absorbed from and de-esterified in the gastrointestinal tract to its active metabolite, cefpodoxime. Following oral administration to fasting Beagles, oral bioavailability was 63.1 ± 5.3%.
Figure 1. Canine Plasma Concentration of Cefpodoxime After a Single Oral Dose of 10 mg/kg Cefpodoxime Proxetil Tablets
Cefpodoxime is distributed in the body with an apparent volume of distribution of 151 ± 27 mL/kg. Like other β-lactam antibiotics, cefpodoxime is eliminated from the body primarily in the urine, with an apparent elimination half-life of approximately 5-6 hours after oral administration. This is similar to the 4.7 hour apparent elimination half-life observed after intravenous dosing. Following intravenous administration of 10 mg/kg, the average total body clearance (ClB ) was 22.7 ± 4.19 mL/hr/kg.
|PK Parameter||Unit||Tablet (SD)|
|Maximum concentration (Cmax )||mcg/mL||16.4 (11.8)|
|Terminal plasma elimination half-life (t1/2,z )||hr||5.61 (1.15)|
|Time of maximum concentration (tmax )||hr||2.21 (0.542)|
|Mean residence time (MRT0-∞ )||hr||9.21 (1.97)|
Like other β-lactam antibiotics, cefpodoxime exerts its inhibitory effect by interfering with bacterial cell wall synthesis. This interference is primarily due to its covalently binding to the penicillin-binding proteins (PBPs) (i.e. transpeptidase and/or carboxypeptidase), which are essential for synthesis of the bacterial cell wall. Therefore, cefpodoxime is bactericidal. Cefpodoxime is stable in the presence of many common β-lactamase enzymes. As a result, many organisms resistant to other β-lactam antibiotics (penicillins and some cephalosporins) due to the production of β-lactamases may be susceptible to cefpodoxime.
Cefpodoxime has a broad spectrum of clinically useful antibacterial activity that includes staphylococci, streptococci, and Gram-negative species (including Pasteurella, Escherichia, and Proteus). The compound is not active against most obligate anaerobes, Pseudomonas spp., or enterococci. The minimum inhibitory concentrations (MICs) for cefpodoxime against Gram-positive and Gram-negative pathogens isolated from canine skin infections (wounds and abscesses) in a 2002 U.S. field study are presented in Table 5. All MICs were determined in accordance with the National Committee for Clinical Laboratory Standards (NCCLS). Appropriate quality control (QC) ranges for in vitro susceptibility testing are presented in Table 6.
|Organism *||# of Isolates||MIC50||MIC90||Range|
|Streptococcus canis (group G, β hemolytic)||33||≤0.03||≤0.03||≤0.03†|
|QC ATCC strain||KB Disk Diffusion Method||Broth Micro-dilution Method|
|Drug concentration||Zone diameter||MIC|
|Escherichia coli 25922||10 mcg||23-28 mm *||0.25-1 mcg/mL *|
|Staphylococcus aureus 25923||10 mcg||19-25 mm *|
|Staphylococcus aureus 29213||1-8 mcg/mL *|
|Streptococcus pneumoniae 49619||10 mcg||28-34 mm †||0.03-0.12 mcg/mL †|
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