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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cefpodoxime, the active de-esterified molecule of the orally absorbable cephalosporin cefpodoxime proxetil, inhibits streptococci, Neisseria spp., and most Enterobacteriaceae, with MIC50 and/or MIC90 values of less than or equal to 2 mg/L; with regard to the latter family of bacteria, the MIC50 and/or MIC90 values of cefpodoxime are consistently greater than or equal to 4 mg/L for only Enterobacter cloacae, Citrobacter freundii, Serratia marcescens, and Morganella morganii. The MIC50 of cedpodoxime for coagulase-negative staphylococci is greater than 2 mg/L, while the MIC for Staphylococcus aureus strains is 4 mg/L. In comparison with other orally absorbable cephalosporins, cefpodoxime is slightly less active than cefixime, cefetamet, and cefotiam against Gram-negative bacteria, but more active than cefuroxime, cefaclor, and cefalexin. Against staphylococci, the activity of cefpodoxime is comparable to that of cefotiam and cefuroxime, and superior to that of cefaclor, while cefixime and cefetamet have insufficient activity against these species. In common with other cephalosporins, cefpodoxime has no activity against enterococci. In vitro models simulating human serum cefpodoxime concentrations demonstrate that a dosage regimen of 200mg is probably sufficient to treat most infections. However, further study is needed to clarify whether infections due to bacteria such as S. aureus, with higher cefpodoxime MICs, can be treated with this dose regimen.
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PMID:Microbiological evaluation of cefpodoxime proxetil. 172 4

On the basis of MIC determinations and appropriate MIC breakpoints, 370 pathogens showed complete cross resistance between cefpodoxime and cefuroxime axetil, cefotiam hexetil, cefixime and cefotaxime in 69.7%, 80.3%, 92.2% and 87% of the strains, respectively. Cefpodoxime was superior to cefuroxime axetil in 28.7%, to cefotiam hexetil in 17.6%, to cefixime in 7% of strains and to cefotaxime not at all. On the other hand, we found cefpodoxime to be inferior to the cephalosporins mentioned in 1.6%, 2.1%, 0.8% and 13%, respectively.
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PMID:In vitro activity and cross resistance studies with cefpodoxime. 178 1

Cefpodoxime, the deesterified part of the orally available cefpodoxime proxetil, is active against most Enterobacteriaceae with MIC50 of 0.06 to 2 mg/l. Only Enterobacter cloacae and Citrobacter freundii strains show MIC50 of 4 mg/l. Coagulase negative staphylococci have a MIC50 of 2, while Staphylococcus aureus strains have a MIC of 4 mg/l. In comparison to other orally available cephalosporins cefpodoxime is slightly less active than cefixime and cefotiam against gram-negative bacteria but more active than cefuroxime, cefaclor, and cephalexin. Against staphylococci the activity of cefpodoxime is comparable to that of cefotiam and cefuroxime and superior to cefaclor and cephalexin, while cefixime does not have sufficient activity against these species. Like all cephalosporins cefpodoxime has no activity against enterococci.
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PMID:In vitro activity of cefpodoxime and ten other cephalosporins against gram-positive cocci, Enterobacteriaceae and Pseudomonas aeruginosa, including beta-lactamase producers. 180 Mar 78

The antibacterial activity of cefpodoxime against Branhamella catarrhalis was studied. All of the 65 clinical isolates tested were inhibited at and below 1.56 micrograms/ml, both at 10(7) and at 10(5) CFUs. The following was further studied on B. catarrhalis N-5 which showed average susceptibility to each drug examined. Bactericidal activity was observed at and above the MIC. Scanning and transmission electron microscopy revealed morphological changes, such as cellular swelling, bleb formation, inhibition of septum formation, and lysis, of the cells exposed to cefpodoxime at concentrations around the MIC. Cefpodoxime was poorly hydrolyzed by the beta-lactamase and it showed affinity for two penicillin-binding proteins that had approximate molecular weights of 83 and 74 kilodaltons, with I50 values of 3.7 and 2.1 micrograms/ml, respectively.
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PMID:Antibacterial activity of cefpodoxime against Branhamella catarrhalis. 180 60

We studied the susceptibilities of 77 strains of Neisseria gonorrhoeae to four antibiotics: cefpodoxime, ceftriaxone, penicillin, and tetracycline. All strains were susceptible to ceftriaxone. Cefpodoxime MICs (range, 0.001 to 0.125 micrograms/ml) were parallel to and approximately four times those of ceftriaxone, and all strains will probably be considered susceptible to cefpodoxime. Disk diffusion zone diameters for cefpodoxime ranged from 35 to 57 mm. Of the strains, 32% were penicillin resistant and 51% were tetracycline resistant (MIC, greater than or equal to 2 micrograms/ml). Susceptibility measurements were consistent for disk diffusion zone diameter and MIC, with an overall agreement of 215 of 225 (96%) for ceftriaxone, penicillin, and tetracycline combined. On the basis of these in vitro data, cefpodoxime should be evaluated in the treatment of gonorrhea.
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PMID:Susceptibility of Neisseria gonorrhoeae to cefpodoxime: determination of MICs and disk diffusion zone diameters. 190 10

The antibacterial activity of cefpodoxime, a new orally active methoxy-imino cephalosporin was evaluated in 470 recent isolates of gram-positive cocci and gram-negative rods from clinical specimens and compared to that of other orally active beta-lactam compounds. Cefpodoxime was highly active against ampicillin-resistant enterobacteria producing the plasmid-mediated TEM-1, TEM-2 or OXA-1 enzymes, as was the case for the other newer compounds. However, it was poorly active against cefuroxime-resistant (MIC greater than or equal to 16 mg/l) E. coli isolates, thus resembling cefetamet and cefixime. It was inactive against isolates exhibiting a production of large amounts of class I beta-lactamase, as was the case with all other compounds studied. Cefpodoxime was highly active against beta-hemolytic streptococci and against Haemophilus influenzae, resembling the related agents. Moreover, its activity against Staphylococcus aureus was comparable to that of cefotaxime and exceeded that of cefetamet and cefixime. Cefpodoxime and the other methoxyimino cephalosporins exhibited a poor affinity to the plasmid-mediated TEM-2 and OXA-1 enzymes. The hydrolysis of cefpodoxime by class I beta-lactamases was barely detectable, whereas it served as a moderate substrate for the enzyme from Klebsiella oxytoca 3951. Cefpodoxime, cefetamet and cefixime were slowly inactivated by the enzyme from Proteus vulgaris 4917 (an enzyme with cefuroximase activity) and much poorer substrates than cefotaxime.
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PMID:Cefpodoxime: comparable evaluation with other orally available cephalosporins. With a note on the role of beta-lactamases. 224 85

The single-dose and steady-state pharmacokinetics of cefpodoxime were assessed in plasma and skin blister fluid (SBF) after oral dosing of 200 mg (n = 8) and 400 mg (n = 8) of cefpodoxime proxetil (doses are expressed as cefpodoxime equivalents) in healthy subjects in an open-label, parallel-design study. Skin blisters were formed by air suction on the midvolar forearm by a previously validated method. After single-dose administration, serial plasma and SBF samples were collected over 24 h for measurement of cefpodoxime by microbiological assays. After a 1-week washout, subjects received the same doses of antibiotic every 12 h for 5 days, with plasma and SBF sampling on day 5. After 200 mg of cefpodoxime proxetil, average peak concentrations (Cmax) in plasma and SBF were 2.18 +/- 0.52 and 1.55 +/- 0.59 micrograms/ml, respectively, after a single dose and 2.33 +/- 0.74 and 1.56 +/- 0.55 micrograms/ml, respectively, at steady state. After 400 mg of cefpodoxime proxetil, Cmax in plasma and SBF averaged 4.16 +/- 1.04 and 2.94 +/- 0.71 micrograms/ml, respectively, following a single dose and 4.10 +/- 0.95 and 2.84 +/- 0.88 micrograms/ml, respectively, at steady state. Cmax occurred 1.1 to 1.6 h later in SBF than in plasma. There was no accumulation of cefpodoxime in plasma or SBF when dosing was done every 12 h. Cefpodoxime blister fluid penetration was estimated to be 67 to 101%, consistent with the relatively low serum protein binding of the drug. Cefpodoxime levels exceeding the MIC for 90% of many skin pathogens, such as Streptococcus species (<1 microgram/ml) or Staphylococcus species (2 to 4 micrograms/ml), were achieved in plasma and SBF following the 200- and/or 400-mg dosing regimens.
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PMID:Pharmacokinetics of cefpodoxime in plasma and skin blister fluid following oral dosing of cefpodoxime proxetil. 239 68

One hundred and thirty seven consecutive isolates of Neisseria gonorrhoeae and a further 36 selected gonococci with either chromosomal (CMRNG) or plasmid mediated (PPNG) resistance to penicillin, all cultured in Sydney in 1993, were found to be sensitive to cefpodoxime, an oral third generation cephalosporin antibiotic (MIC range < 0.001-0.25 mg/L). All isolates were also sensitive to ceftriaxone and spectinomycin. Six gonococci showed high level resistance to tetracycline (TRNG, MIC = 32 mg/L) and 12 had decreased susceptibility to quinolone antibiotics (MIC range 0.06-0.5 mg/L). The MIC50 and MIC90 for both cefpodoxime and ceftriaxone were highest amongst CMRNG and ceftriaxone was 2 to 4 times as active as cefpodoxime weight for weight. Cefpodoxime may be a valuable additional oral agent for the treatment of gonorrhea in Australia. The sensitivity of gonococci to cefpodoxime can probably be inferred from values obtained for ceftriaxone.
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PMID:The sensitivity of 173 Sydney isolates of Neisseria gonorrhoeae to cefpodoxime and other antibiotics used to treat gonorrhea. 760 56

The effects of sub-minimum inhibitory concentrations (sub-MICs) of three antibiotics affecting the biosynthesis of peptidoglycan on the interactions of Staphylococcus aureus strains with collagenous substrata were evaluated. In a system measuring binding of 125I-labeled collagen, growth of bacteria in the presence of one-quarter MIC of cloxacillin and vancomycin reduced the number of collagen binding sites on the surface of bacteria. Growth in the presence of cefpodoxime reduced the number of collagen binding sites in one strain and increased it in another. Cefpodoxime also increased the dissociation constant of collagen binding to bacteria, 2- to 3-fold, while the other two antibiotics did not affect the affinity of the interaction. In a system measuring adhesion of 125I-labeled bacteria to collagen-coated surfaces or cartilage, bacteria grown in the presence of cloxacillin and vancomycin attached to varying degrees depending on the strain. In contrast, compared to untreated controls as well as to bacteria treated with the other two antibiotics, growth in the presence of cefpodoxime significantly reduced adhesion of the majority of strains tested. Sub-MICs of antibiotics appear to affect staphylococcal adhesion to collagenous substrata with cefpodoxime exhibiting the strongest effect. The critical factor in reducing bacterial adhesion seems not to be the number of bacterial binding sites for collagen, but the affinity of the interaction.
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PMID:Antibiotics alter interactions of Staphylococcus aureus with collagenous substrata. 813 33

Since resistance to several oral antimicrobials useful for the treatment of pediatric urinary tract infections (UTI) is overwhelming in Argentina, an in vitro investigation was performed testing 400 isolates obtained from urines of children suffering UTI's, 200 collected in 1990 and 200 in 1991. Their susceptibility against oral antimicrobials marketed in Argentina and appropriate for the treatment of UTI was determined by the agar dilution methods. An increase of the resistance to aminopenicillin combined with beta-lactamase inhibitors and to fluoroquinolones was observed comparing the two periods. Cefpodoxime (CPD), cefixime and fluoroquinolones except norfloxacin were the sole oral antimicrobials showing in vitro activity at the 90 per cent level. Unfortunately fluoroquinolones are not yet approved for pediatric use. Consequently we realized an in vitro and in vivo pharmacokinetic study in order to determine CPD activity against E. coli isolated in UTI cases. Five children (6-10 y) showing E. coli UTI infections received 10 mg/kg/d CPD in a single oral daily dose and were treated up to 10 days, 3 had lower UTI and 2 upper UTI. All patients were clinical and bacteriologically cured. Cultures obtained up to 4 weeks after treatment were negative. CPD serum levels at 2 hours after the first dose of treatment showed a median of 2.7 mg/l (2.3-3.4 range). Bactericidal serum titers at the same time against the patients own strain and an E. coli TEM-1 hyperproducer strain (MIC 4,096 mg/l for ampicillin and 0.5 mg/l for CPD) showed a median value of 1/8 against patients strains and 1/2 against the THP strain.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Serum and urinary cefpodoxime levels and time killing curves performed in the urine of children presenting urinary tract infections. 823 40


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