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Cefpodoxime Proxetil

A Review of its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Potential

Abstract

Synopsis

Cefpodoxime proxetil is an orally administered prodrug which is absorbed and de-esterifled by the intestinal mucosa to release the third generation cephalosporin, cefpodoxime.

Cefpodoxime is stable towards the most commonly found plasmid-mediated β-lactamases and the drug has a broad spectrum of antibacterial activity encompassing both Gram-negative and Gram-positive bacteria, rendering it a possible option for empirical use in a wide range of community acquired infections in both adult and paediatric patinets. The extended plasma half-life of cefpodoxime (1.9 to 3.7h) permits twice daily administration.

In comparative trials, twice daily cefpodoxime proxetil (dose equivalent cefpodoxime 100 to 400mg) was as effective as a 3- to 4-times daily regimen of phenoxymethylpenicillin in pharyngotonsillitis, as well as thrice daily amoxicillin (with or without clavulanic acid) or cefaclor against infections of the ear, the upper and lower respiratory tract, the urinary tract and those of the skin and soft tissues. The latter reflects the enhanced antistaphylococcal activity of cefpodoxime, which distinguishes it from other orally active third generation cephalosporins such as cefixime. Most notably, an oral regimen of cefpodoxime proxetil was as efficacious as parenterally administered ceftriaxone for the treatment of bronchopneumonia in hospitalised patients at risk due to the presence of underlying diseases, addictions or advancing age. A single oral dose of cefpodoxime was also as efficacious as ceftriaxone in uncomplicated anogenital gonococcal infections.

Cefpodoxime proxetil is generally well tolerated, with mild to moderate gastrointestinal disturbances occurring in 4 to 15% of patients treated with therapeutic doses.

Thus, a convenient twice daily oral regimen of cefpodoxime proxetil can be prescribed as an effective alternative to established β-lactam therapies in the empirical outpatient treatment of infections of the respiratory and urinary tracts as well as those of the skin and soft tissues.

Antibacterial Activity

Cefpodoxime is highly active against both Haemophilus influenzae and Moraxella catarrhalis including β-lactamase producing strains, with a minimum inhibitory concentration for 90% of tested strains (MIC90) ⩽ 1 mg/L; cefpodoxime had a similar potency to that of cefixime but greater than that of cefuroxime, cefaclor and cephalexin against these microorganisms. Moreover, cefpodoxime was more active against H. influenzae including β-lactamase producing strains than amoxicillin/clavulanic acid, although these drugs shared a similar potency against M. catarrhalis.

Cefpodoxime is particularly active against Neisseria spp., including N. gonorrhoeae (MIC90 ⩽ 0.06 mg/L), against which it was only slightly less potent than ceftriaxone.

Most tested strains of Enterobacteriaceae including Escherichia coli, Proteus mirabilis, Klebsiella (pneumoniae and oxytoca) and Providencia (rettgeri and stuartii) are susceptible to cefpodoxime (MIC90 < 2 mg/L). In general, cefpodoxime shows a greater inhibitory activity against Enterobacteriaceae compared with cefaclor, cephalexin and cefuroxime, but it is less potent than cefixime. However, cefpodoxime shows a weak inhibitory activity against Citrobacter freundii, Serratia marcescens, Morganella morganii, and Enterobacter cloacae (MIC50 and/or MIC90 ⩾ 4 mg/L), reflecting the presence of inducible cephalosporinases within these species. Pseudomonas aeruginosa is resistant to cefpodoxime.

Cefpodoxime is very active against Streptococcus pyogenes and penicillin-susceptible strains of Streptococcus pneumoniae (MIC90 ⩽ 0.06 mg/L). Moreover, penicillin-resistant strains of S. pneumoniae are moderately susceptible to cefpodoxime, though resistant to cefixime and cefaclor. The activity of cefpodoxime against these streptococci is similar to that reported for cefuroxime and amoxicillin with or without clavulanic acid, but greater than that of cefixime or cefaclor. In common with other orally active cephalosporins, cefpodoxime was inactive against Enterococcus faecalis.

Most penicillin and methicillin-susceptible strains of Staphylococcus epidermidis and Staphylococcus aureus are moderately susceptible to cefpodoxime (MIC90 ⩽ 3 mg/L), although the drug is less active against Staphylococcus saprophyticus. Against these staphylococci, cefpodoxime is much more active than cefixime, but slightly less potent than cefuroxime. Cefpodoxime is inactive against methicillin-resistant strains of S. aureus.

Helicobacter pylori is moderately susceptible to cefpodoxime.

The inhibitory activity of cefpodoxime against a range of anaerobic respiratory tract pathogens including Prevotella, Peptostreptococcus and Fusobacterium spp. is similar to that of cefaclor, cefuroxime and amoxicillin, although less than that of amoxicillin with clavulanic acid.

The in vitro inhibitory activity of cefpodoxime is little affected by the addition of plasma serum or the type of testing medium used, although increasing the inocula size >106 cfu/ml reduced the potency of the drug against β-lactamase producing strains of Enterobacteriaceae.

Cefpodoxime appears to be a low activator of β-lactamase activity and is stable towards the most commonly found plasmid-mediated β-lactamases (TEM-1,2; SHV-1; OXA-1); the drug shows a similar stability to that of cefixime, cefuroxime and cephalexin, but is generally superior to cefaclor.

The antibacterial effect of cefpodoxime is based on inhibition of cell wall synthesis and the drug is bactericidal against most tested strains at a concentration equal to or 4-fold greater than the respective MIC. The bactericidal activity against tested β-lactamase producing strains of Enterobacteriaceae is comparable to that of cefixime and cefuroxime, but superior to that of cefaclor. Cefpodoxime proxetil demonstrated a postantibiotic effect of up to 2 hours against Gram-positive species, although it was without effect against Gram-negative species.

Cefpodoxime proxetil demonstrates a potent protective effect against death in mice caused by septicaemia induced with a range of Gram-positive and Gram-negative bacteria; the drug demonstrates an effect which is equivalent to or greater than that of cefaclor and amoxicillin, although it is somewhat less active against S. aureus infections. Cefpodoxime proxetil is comparable or less active than cefixime against Gram-negative infections, but is superior against Gram-positive infections.

Pharmacokinetic Properties

The pharmacokinetics of cefpodoxime have been investigated in healthy young and elderly volunteers as well as in paediatric and adult patients, including those with renal failure. Cefpodoxime proxetil is absorbed and de-esterified in vivo to release its active metabolite, cefpodoxime, which has ≈ 50% systemic availability. Peak plasma concentrations (Cmax) of cefpodoxime were achieved approximately 2 to 3 hours after oral administration of cefpodoxime proxetil to healthy volunteers; Cmax appears to be slightly higher in patients with renal failure or elderly patients with respiratory disease. The pharmacokinetics of cefpodoxime are linear with single doses within the therapeutic range (100 to 400mg) and the drug does not accumulate following twice daily administration for 15 days. The bioavailability of cefpodoxime is significantly increased by food, whereas it is significantly reduced by agents which elevate gastric pH.

Cefpodoxime is extensively distributed throughout tissues and fluids of the respiratory tract; for 7 to 12 hours after a single oral dose of cefpodoxime 100 or 200mg, the concentrations of the drug achieved in upper (tonsils) or lower respiratory tract tissues (bronchial mucosa, lung parenchyma, pleural fluid), were greater than or equivalent to the MIC90 for common respiratory tract pathogens. Similarly, a therapeutic concentration of cefpodoxime is achieved in the nasal mucosa and concha after administration of a single dose (200mg). Cefpodoxime 400mg penetrates well into the interstitial fluid and inflammatory exudate associated with skin damage to achieve a peak concentration greater than or equivalent to the mean MIC90 for common skin pathogens including some Staphylococcus spp. (methicillin-sensitive S. aureus and S. epidermidis). Lower, but still clinically relevant, concentrations of cefpodoxime are found in the myometrium and prostate. Small amounts of cefpodoxime are excreted into breast milk.

Once cefpodoxime reaches the systemic circulation little further metabolism occurs (80% of an intravenous dose of cefpodoxime is recovered in the urine as cefpodoxime) and the drug is eliminated primarily by renal excretion. The extended plasma half-life of cefpodoxime (2.1 to 3.6h) combined with the potent antibacterial activity of the drug, enables once or twice daily administration.

The pharmacokinetic properties of cefpodoxime do not appear to be altered to a clinically significant extent by age. However, clearance of cefpodoxime is reduced in proportion to creatinine clearance (CLCr) and dosage restrictions may be necessary in patients with CLCr values below 3.0 L/h.

Clinical Efficacy

Dosages of cefpodoxime proxetil refer to the cefpodoxime equivalent.

In adult patients, cefpodoxime proxetil has demonstrated a comparable efficacy to that of standard β-lactams in upper and lower respiratory tract infections due predominantly to S. pyogenes, H. influenzae, H. parainfluenzae, S. pneumoniae, M. catarrhalis and S. aureus.

The clinical and bacteriological efficacy of a 5- to 10-day regimen of cefpodoxime proxetil 100mg twice daily was equivalent to that of a 3 or 4 times daily regimen of phenoxymethyl-penicillin 250 to 600mg, amoxicillin 500mg or cefaclor 250mg as well as twice daily cefuroxime axetil 250mg in acute pharyngitis/tonsillitis. Although cefpodoxime proxetil 200mg twice daily resulted in a sigificantly higher clinical cure rate than cefaclor 500mg thrice daily in acute sinusitis (84 vs 68%, p < 0.01), the overall clinical efficacy (cure + improvement) and bacterial eradication rates were similar for each drug.

Cefpodoxime proxetil 100 or 200mg twice daily for 7 to 14 days (mean 10 days) proved as efficacious as thrice daily amoxicillin 500mg, amoxicillin/clavulanic 625mg or cefuroxime axetil 250mg for the treatment of acute bronchitis and/or acute exacerbations of chronic bronchitis. Similarly, cefpodoxime proxetil 200mg twice daily was also as efficacious as thrice daily administration of amoxicillin 500mg or cefaclor 500mg in community-acquired pneumonia.

Most notably, however, in a single trial cefpodoxime proxetil 200mg twice daily was as effective as parenterally administered ceftriaxone 1g per day in the treatment of community-acquired bronchopneumonia in hospitalised patients with additional ‘risk’ factors such as advanced age (⩾65 years), respiratory failure, cardiovascular disease or smoking.

Cefpodoxime proxetil 200 to 400mg twice daily for 7 to ≈ 14 days resulted in a complete clinical cure or improvement in all patients treated for mild to severe skin and soft tissue infections (SSTI), caused primarily by S. aureus, S. epidermidis, S. pyogenes, P. mirabilis and E. coli; the pathogen eradication rate was 98%. In comparative trials involving American patients, cefpodoxime proxetil 400mg twice daily was as effective as cefaclor 500mg thrice daily and ciprofloxacin 500mg twice daily in SSTI.

Cefpodoxime proxetil 100 to 300mg twice daily for 7 to 14 days is also effective in the treatment of patients with uncomplicated and complicated urinary tract infections (UTIs) caused primarily by E. coli, Klebsiella, Proteus or Staphylococcus spp. In comparative trials, cefpodoxime proxetil 100mg twice daily was as effective as thrice daily regimens of cefaclor 250mg or amoxicillin 250mg in the treatment of UTIs, achieving a clinical cure and bacteriological eradication rate of 79 and 80%, respectively.

Cefpodoxime is particularly effective against uncomplicated anogenital gonococcal infections, with a single oral dose (200mg) proving as effective as a single intramuscular injection of ceftriaxone 250mg. The presence of Chlamydia trachomatis infection in addition to N. gonorrhoeae infection before treatment did not appear to affect the overall clinical efficacy of cefpodoxime proxetil.

In Japanese paediatric patients aged ⩽ 16 years of age, cefpodoxime proxetil (standard dose 10 mg/kg/day administered in 2 to 3 daily doses for 10 days) is effective in pharyngitis/tonsillitis, lower respiratory tract and urinary tract infections as well as those of the skin and soft tissues, including impetigo, achieving a good to excellent clinical response in ⩾ 92% of treated patients.

In two large scale comparative trials (n ⩾ 229) involving American paediatric patients aged >2 months to 18 years, the clinical efficacy of cefpodoxime proxetil given twice daily was equivalent to that of thrice daily amoxicillin/clavulanic acid 50 mg/kg/day in otitis media (92 vs 88%, respectively) and phenoxymethylpenicillin 40 mg/kg/day in streptococcal pharyngitis (92 vs 87%, respectively). Moreover, a significantly higher (p < 0.01) S. pyogenes elimination rate was reported for cefpodoxime proxetil (93%) than phenoxymethylpenicillin (81%) in the latter study.

Tolerability

A 7- to 14-day regimen of cefpodoxime proxetil 100 to 400mg twice daily appears to be generally well tolerated, with adverse events reported in ≈8 to 19% of patients. The majority of these adverse events were judged to be of ‘mild to moderate’ severity, and the number of adult patients withdrawing from treatment with cefpodoxime proxetil 100 to 200mg twice daily was small (≈ 2%), although this rate may increase to 5% with a higher dosage (400mg twice daily); diarrhoea, nausea and dermatologic rash were cited as the main reasons for discontinuation.

As for other broad spectrum cephalosporins, gastrointestinal-related complaints were the most frequently reported adverse events, with diarrhoea and/or soft/loose stools occurring in ≈ 3 to 5% of adult patients treated with cefpodoxime proxetil (100 or 200mg twice daily). Disturbances of the skin and mucosa (rash, pruritus, candidiasis and vaginitis) have also been reported with this regimen, occurring in ⩽ 2% of patients. Similarly, gastrointestinal disturbances were the most frequently reported adverse events in paediatric patients treated with cefpodoxime proxetil 10 mg/kg/day, followed by adverse dermatological events (rash, urticaria, pruritus).

In both adult and paediatric studies, the overall tolerability of cefpodoxime proxetil was similar to that of phenoxymethylpenicillin, amoxicillin with or without clavulanic acid and cefaclor, although the latter tended to be associated with a slightly lower incidence of adverse gastrointestinal-related events in adult patients.

Reports of pseudomembranous colitis have been recorded during phase IV studies, despite the fact that this condition was not observed in over 7300 patients treated with cefpodoxime proxetil during pre-marketing studies. Clostridium difficile has been identified in 3 patients during diarrhoeal episodes associated with cefpodoxime proxetil therapy, although diarrhoea was infrequently associated with C. difficile colonisation in healthy volunteers receiving the drug.

Cefpodoxime proxetil does not appear to have a clinically significant effect on standard laboratory blood assays, although post-treatment eosinophilia is typically reported in a small proportion (⩽ 4%) of both adult and paediatric patients receiving the recommended regimen.

Dosage and Administration

A 5- to 16-day regimen of cefpodoxime proxetil therapy has demonstrated efficacy in a wide variety of community-acquired bacterial infections. The stated cefpodoxime proxetil doses refer to the cefpodoxime equivalent.

Adults: Cefpodoxime proxetil 200mg twice daily is recommended for the treatment of sinusitis, otitis media and lower respiratory tract infections including pneumonia, acute bronchitis and bronchitis as well as complicated urinary tract infections. A treatment duration of 7 to 14 days (mean 10 days) is typical for sinusitis, lower respiratory tract and complicated urinary tract infections, but therapy of otitis media should be continued for at least 10 days. A lower dose of cefpodoxime proxetil 100mg twice daily is effective in the treatment of tonsillitis/pharyngitis (10 days) as well as uncomplicated urinary tract infections (7 days). A single dose of cefpodoxime proxetil 200mg is recommended for the treatment of uncomplicated gonorrheal infections.

Cefpodoxime proxetil 200 to 400mg twice daily for 7 to 14 days is effective against infections of skin and soft tissues, with the higher dosage recommended for more severe infections or infections caused by less susceptible organisms.

Dosage adjustment may be required in patients with renal impairment or age-related decline in renal function which results in a creatinine clearance below 3 L/h.

Postprandial administration is recommended, particularly in patients receiving concomitant H2-antagonist or antacid therapy.

Children (aged 2 months to 18 years): Twice daily administration of cefpodoxime proxetil flavoured granules (suspension) 10 mg/kg/day for 10 days is recommended for the treatment of infections in paediatric subjects, including otitis media and infections of the respiratory and urinary tracts as well as those of the skin and soft tissues.

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References

  • Appelbaum PC, Spangler SK, Crotty E, Jacobs MR. Susceptibility of penicillin-sensitive and -resistant strains of Streptococcus pneumoniae to new antimicrobial agents, including daptomycin, teicoplanin, cefpodoxime and quinolones. Journal of Antimicrobial Chemotherapy 23: 509–516, 1989

    PubMed  Article  CAS  Google Scholar 

  • Baba S, Mori Y, Suzuki K, Shimada J, Seyano K, et al. Evaluation of CS-807 in acute lacunar tonsillitis: a comparative double-blind study with cefaclor. Jibi to Rinsho 34: 1274–1296, 1988

    Google Scholar 

  • Backhouse C, Wade A, Williamson P, Tremblay D, Lenfant B. Multiple dose pharmacokinetics of cefpodoxime in young adult and elderly patients. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 29–34, 1990

    PubMed  Google Scholar 

  • Baldwin DR, Honeybourne D, Andrews JM, Wise R. Penetration of cefpodoxime into bronchial mucosa. Poster presentation at the International Congress of Infectious Diseases, Montreal, July 15–19, 1990

    Google Scholar 

  • Bauernfeind A, Jungwirth R. Antibacterial activity of cefpodoxime in comparison with cefixime, cefdinir, cefetamet, ceftibuten, lorcarbef, cefprozil, BAY 3522, cefuroxime, cefaclor and cefadroxil. Infection 19: 353–362, 1991

    PubMed  Article  CAS  Google Scholar 

  • Bille J, Kaehler D, Glauser MP. In vitro activity against staphylococci and streptococci of cefpodoxime proxetil (RU 51807). Poster. International Conference on Chemotherapy Jerusalem, June 11–16, 1989

  • Bombardt PA, Cathcart KS, Bothwell BE, Closson SK. Determination of cefpodoxime levels and cefpodoxime stability in human urine by direct injection HPLC with column-switching. Journal of Liquid Chromatography 14: 1729–1746, 1991

    Article  CAS  Google Scholar 

  • Bonwell L, O’Keefe P, Libertin C. Comparison of cefpodoxime and ceftriaxone in uncomplicated gonococcal infections. Abstract. 90th Annual Meeting of the American Society for Microbiology Anaheim, May 13–17, 1990

  • Borin MT. A review of the pharmacokinetics of cefpodoxime proxetil. Drugs 42 (Suppl. 3): 13–21, 1991

    PubMed  Article  CAS  Google Scholar 

  • Borin MT, Hughes GS, Patel RK, Royer ME, Cathcart KS. Pharmacokinetic and tolerance studies of cefpodoxime after single- and multiple-dose oral administration of cefpodoxime proxetil. Journal of Clinical Pharmacology 31: 1137–1145, 1991

    PubMed  CAS  Google Scholar 

  • Borin MT, Hughes GS, Spillers CR, Patel RK. Pharmacokinetics of cefpodoxime in plasma and skin blister fluid following oral dosing of cefpodoxime proxetil. Antimicrobial Agents and Chemotherapy 34: 1094–1099, 1990

    PubMed  Article  CAS  Google Scholar 

  • Brown RJ, Batts DH, Hughes GS, Greenwald CA. Cefpodoxime Pharyngitis study Group. Comparison of oral cefpodoxime proxetil and penicillin V potassium in the treatment of group A streptococcal pharyngitis/tonsillitis. Clinical Therapeutics 13: 579–588, 1991

    PubMed  CAS  Google Scholar 

  • Callaway CK, Weidenbach CP. A comparison of cefpodoxime proxetil and cefaclor in the treatment of acute community acquired pneumonia. Submitted to Antimicrobial Agents and Chemotherapy, 1992

  • Casin I, Perrenet F, Perol Y. In vitro activity of cefpodoxime proxetil (RU 51807), a new oral cephalosporin against Neisseria gonorrhoeae (NG). International Congress of Infectious Diseases: Montreal, Canada July 15–19, 1990

  • Chantot JF, Mauvais P. RU 51807 (cefpodoxime proxetil). In vitro and in vivo antibacterial activity of a new orally active cephalosporin. (In French). Pathologie Biologie 39: 17–27, 1991

    PubMed  CAS  Google Scholar 

  • Chin N-X, Neu HC. In vitro activity of an oral iminomethoxy aminothiazolyl cephalosporin, R-3746. Antimicrobial Agents and Chemotherapy 32: 671–677, 1988

    PubMed  Article  CAS  Google Scholar 

  • Cho N, Fukunaga K, Kunii K, Kimura T, Suzuki A. Basic and clinical studies on CS-807 in the obstetric and gynecologic field. Chemotherapy 36 (Suppl. 1): 923–940, 1988

    Google Scholar 

  • Cogo R, Bonfiglio G, Monzani GP, Mattavelli M, Anelli M. Efficacy and tolerance of cefpodoxime proxetil 100mg bid in the treatment of hospitalized patients with pneumonias. Poster presentation at the International Congress of Infectious Diseases, p. 27, Montreal, July 15–19, 1990

    Google Scholar 

  • Collins GV. Comparison of cefpodoxime proxetil and ciprofloxacin hydrochloride in the treatment of skin and soft tissue infections. Submitted to Annals of Emergency Medicine, 1992

  • Couraud L, Andrews JM, Lecoeur H, Sultan E, Lenfant B. Concentrations of cefpodoxime in plasma and lung tissue after a single oral dose of cefpodoxime proxetil. Journal of Antimicrobial Chemotherapy 26 (Suppl. 1): 35–40, 1990

    PubMed  Google Scholar 

  • Cox CE, Graveline JF, Luongo JM. Review of clinical experience in the United States with cefpodoxime proxetil in adults with uncomplicated urinary tract infections. Drugs 42 (Suppl. 3): 41–50, 1991

    PubMed  Article  Google Scholar 

  • Dabernat H, Avril JL, Boussougant Y. In-vitro activity of cefpodoxime against pathogens responsible for community-acquired respiratory tract infections. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 1–6, 1990

    PubMed  CAS  Google Scholar 

  • Dajani AS, Kessler S, Mendelson R, Uden DL, Todd WM. Cefpodoxime proxetil verses Penicillin V in paediatric Pharyngitis/ Tonsillitis. Submitted to American Journal of Disease of Children, 1992

  • Depitre C, Chachaty E, Corthier G, Andremont A. Comparison of intestinal colonisation by Clostridium difficile in healthy volunteers treated with oral cefixime, oral cefpodoxime proxetil or placebo. Poster. International Congress on Chemotherapy, Berlin, June 23–28, 1991

    Google Scholar 

  • Drehobl M, Schultz C. Cefpodoxime proxetil verses penecillin V potassium in the treatment of adults with pharyngitis or tonsillitis due to Streptococcus pyogenes. Submitted to Journal of Family Practice, 1992

  • Dubreuill L, Derriennic M, Sedallian A. Antibacterial activity of cefpodoxime, cefuroxime and cefaclor against strict anaerobic bacteria. (In French). Pathologie Biologie 38: 343–346, 1990

    Google Scholar 

  • Dumont R, Guetat F, Andrews JM, Sultan E, Lenfant B. Concentrations of cefpodoxime in plasma and pleural fluid after a single oral dose of cefpodoxime proxetil. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 41–46, 1990

    PubMed  Google Scholar 

  • Fass RJ. Helsel VL. In vitro activity of U-76,252 (CS-807), a new oral cephalosporin. Antimicrobial Agents and Chemotherapy 32: 1082–1085, 1988

    PubMed  Article  CAS  Google Scholar 

  • Fekete T, Woodwell J, Cundy KR. Susceptibility of Neisseria gonorrhoeae to cefpodoxime: determination of MICs and disk diffusion zone diameters. Antimicrobial Agents and Chemotherapy 35: 497–499, 1991

    PubMed  Article  CAS  Google Scholar 

  • Fujii R. Clinical trials of cefpodoxime proxetil suspension in paediatrics. Drugs 42 (Suppl. 3): 57–60, 1991

    PubMed  Article  Google Scholar 

  • Fujii R, Meguro H, Arimasu O, Shiraishi H, Abe T. Overall clinical evaluation of cefpodoxime proxetil against infections in pediatric fields. Japanese Journal of Antibiotics 42: 1439–1453, 1989

    PubMed  CAS  Google Scholar 

  • Gehanno P, Andrews JM, Ichou F, Sultan E, Lenfant. Concentrations of cefpodoxime in plasma and tonsillar tissue after a single oral dose of cefpodoxime proxetil. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 47–51, 1990a

    PubMed  Google Scholar 

  • Gehanno P, Depondt J, Barry B, Simonet M, Dewever H. Comparison of cefpodoxime proxetil with cefaclor in the treatment of sinusitis. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 87–91, 1990b

    PubMed  Google Scholar 

  • Green J, Butler T, Todd WM. Comparative efficacy and safety of cefpodoxime proxetil verses cefaclor for acute Community-Acquired Pneumonia in a randomised double-blind trial. Submitted to American Review of Respiratory Disease, 1992

  • Grimm H. In vitro activity and cross resistance studies with cefpodoxime. Zbl. Bakt 276: 54–62, 1991

    CAS  Google Scholar 

  • Höffler D, Koeppe P, Corcilius M, Przyklinik A. Cefpodoxime proxetil in patients with enstage renal failure on hemodialysis. Infection 18: 157–163, 1990

    PubMed  Article  Google Scholar 

  • Holt HA, Bywater MJ, Reeves DS. In-vitro activity of cefpodoxime against 1834 isolates from domiciliary infections at 20 UK centres. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 7–12, 1990

    PubMed  CAS  Google Scholar 

  • Hughes GS, Heald DL, Barker BK, Patel RK, Spillers CR, et al. The effects of gastric pH and food on the pharmacokinetics of a new oral cephalosporin, cefpodoxime proxetil. Clinical Pharmacology and Therapeutics 46: 674–685, 1989

    PubMed  Article  CAS  Google Scholar 

  • Hughes GS, Heald DL, Patel R, Spillers CR, Batts DH, et al. Gastric emptying and the pharmacokinetics of the cephalosporin antibiotic, cefpodoxime proxetil. Methods and Findings in Experimental and Clinical Pharmacology 12: 197–204, 1990

    PubMed  CAS  Google Scholar 

  • Iravani A, Cox C, Miller D, Schneider R, Sugawara S, et al. A multicentre, dose-response study of cefpodoxime proxetil in patients with urinary tract infections. Poster: International Congress of Infectious Diseases, Montreal, p. 31, 1990

    Google Scholar 

  • Jones RN, Barry AL. In vitro evaluations of U-76,252 (CS-807): antimicrobial spectrum, beta-lactamase stability, and enzyme inhibition. Diagnostic Microbiology and Infectious Diseases 8: 245–249, 1987

    Article  CAS  Google Scholar 

  • Jones RN, Barry AL. Antimicrobial activity and disk diffusion susceptibility testing of U-76,253A (R-3746), the active metabolite of the new cephalosporin ester, U-76,252 (CS-807). Antimicrobial Agents and Chemotherapy 32: 443–449, 1988

    PubMed  Article  CAS  Google Scholar 

  • Keck CW, Martin DH, Todd, WM. Safety and efficacy of a single oral dose of cefpodoxime proxetil verses a single injection dose of ceftriaxone for uncomplicated gonococcal infections. Submitted to Sexually Transmitted Diseases, 1992

  • Kiesel N, Adam F, Isert D, Limbert M, Markus A, et al. 29 246, the active compound of the cephalosporin prodrug ester HR 916. Journal of Antibiotics 45: 922–931, 1992

    Article  Google Scholar 

  • Kline NE, Kline MW. Cefpodoxime proxetil versus penicillin V in the treatment of streptococcal pharyngitis in children. Current Therapeutic Research 49: 807–813, 1991

    Google Scholar 

  • Knapp CC, Sierra-Madero J, Washington JA. Antibacterial activities of cefpodoxime, cefixime and ceftriaxone. Antimicrobial Agents and Chemotherapy 32: 1896–1898, 1988

    PubMed  Article  CAS  Google Scholar 

  • Knothe H, Shah PM, Eckardt O. Cefpodoxime: comparative antibacterial activity, influence of growth conditions and bactericidal activity. Infection 19: 370–376, 1991

    PubMed  Article  CAS  Google Scholar 

  • Kumazawa J. Summary of clinical experience with cefpodoxime proxetil in adults in Japan. Drugs 42 (Suppl. 3): 1–5, 1991

    PubMed  Article  Google Scholar 

  • Leigh DA, Fraser S, Hannington J, Mason T. Comparative trial of the efficacy and tolerance of cefpodoxime proxetil and amoxicillin in the treatment of acute and acute-on-chronic bronchitis. Poster. International Conference on Chemotherapy, Berlin, June 23–28, 1991

  • Leophonte P, Rouquet RM, Gustin M, Robience Y, Balzer PD, et al. Cefpodoxime proxetil vs amoxicillin in the treatment of community-acquired pneumonia in adult patients. Poster. International Congress of Infectious Diseases, Montreal, p. 32, July 15–19, 1990

    Google Scholar 

  • Mellado E, Martin-Luengo F. In-vitro activity of the new oral third generation cephalosporins against different clinical isolates. Poster. International Congress on Chemotherapy, Berlin, June 23–28, 1991

    Google Scholar 

  • Mendelman PM, Del Becarro MA, McLinn SE, Todd WM. Cefpodoxime proxetil compared with amoxicillin/clavulanate for the treatment of otitis media. Journal of Paediatrics, in press, 1992

  • Mistretta A, Mirabella S, Cocuzza GE, Cogo R, Catena E, et al. Efficacy and tolerance of cefpodoxime proxetil (100mg bid) in the treatment of patients with acute exacerbations on chronic bronchitis: a multicentre study. Poster. International Congress of Infectious Diseases, Montreal, p. 33, July 15–19, 1990

    Google Scholar 

  • Miyazaki S, Miyazaki Y, Tsuji A, Nishida M, Goto S. In vitro antibacterial activity of ME1207, a new oral cephalosporin. Antimicrobial Agents and Chemotherapy 35: 1691–1694, 1991

    PubMed  Article  CAS  Google Scholar 

  • Montane F, Piolat V, Study Group. Comparison of efficacy and tolerance of cefpodoxime proxetil and cefuroxime axetil in the treatment of acute bronchitis. Poster presentation at the International Congress of Infectious Diseases, Montreal, p. 34, July 15–19, 1990

    Google Scholar 

  • Monteil H, Piemont Y. Staphylococcus aureus, S. epidermidis, S. saprophyticus, in vitro susceptibilities to the new orally active cephem antibiotic: cefpodoxime proxetil. Poster. International Conference on Chemotherapy, Jerusalem, pp. 20–21, June 11–16, 1989

  • Naber KG, Kinzig M, Adam D, Sörgel F, Bajorski AH, et al. Concentrations of cefpodoxime in plasma, ejaculate and in prostatic fluid and adenoma tissue. Infection 19: 30–34, 1991

    PubMed  Article  CAS  Google Scholar 

  • NCCLS (various Eds). Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically: approved standard. National Committee for Clinical Laboratory Standards publication, in press, 1992

  • Novak E, Paxton LM, Tubbs HJ, Turner LF, Keck CW, et al. Orally administered cefpodoxime proxetil for treatment of uncomplicated gonococcal urethritis in males: a dose response study. Antimicrobial Agents and Chemotherapy 36: 1764–1765, 1992

    PubMed  Article  CAS  Google Scholar 

  • Ogata N, Kumazawa J, Kushimoto T, Sakamoto K, Ueda S. et al. A double-blind study to compare CS-807 and L-cephalexin for the treatment of complicated urinary tract infections. The Nishinihon Journal of Urology 50: 2077–2098, 1988

    Google Scholar 

  • O’Neill P, Nye K, Douce G, Andrews J, Wise R. Pharmacokinetics and inflammatory fluid penetration of cefpodoxime proxetil in volunteers. Antimicrobial Agents and Chemotherapy 34: 232–234, 1990

    PubMed  Article  Google Scholar 

  • Periti P, Novelli A, Mini E, Mazzei T, Cassetta MI. Clinical pharmacokinetics of cefpodoxime proxetil in older patients. Poster. International Conference of Chemotherapy, Berlin, June 23–28, 1991

  • Periti P, Novelli A, Schildwachter G, SchmidtrGayk H, Ryo Y, et al. Efficacy and tolerance of cefpodoxime proxetil compared with co-amoxiclav in the treatment of exacerbations of chronic bronchitis. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 63–69, 1990

    PubMed  Google Scholar 

  • Portier H, Chavanet P, Gouyon JB, Guetat F. Five day treatment of pharyngotonsillitis with cefpodoxime proxetil. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 79–85, 1990b

    PubMed  Google Scholar 

  • Portier H, Chavanet P, Ichou F, Multicentre Group. Five-day antibiotherapy in presumed bacterial acute tonsillitis: a comparative study of cefpodoxime proxetil vs cefuroxime axetil. Poster. International Congress of Infectious Diseases, Montreal, p. 37, July 15–19, 1990a

    Google Scholar 

  • Portier H, Waldner, Combernoux A, Clarysse C, Kurzeja AH, Rostand A. Cefpodoxime proxetil vs amoxicillin in the treatment of pharyngitis or tonsillitis in adult out-patients. Poster. International Congress of Infectious Diseases, Montreal, p. 38], July 15–19, 1990

  • Raso F, Pintucci JP, Gulisano G, Bonfiglio G, Mattina R, et al. Efficacy and tolerance of cefpodoxime proxetil in the treatment of pharyngotonsillitis: a multicentre study. Poster. International Congress of Infectious Diseases, Montreal, p. 26, July 15–19, 1990

    Google Scholar 

  • Rodriguez A, Rivera-Castano R, Garcia H, Garcia M, Galindez SI et al. Oral cefpodoxime verses ceftriaxone in the treatment of uncomplicated gonorrhoea. 13th Interscience Conference on Antimicrobial Agents and Chemotherapy Atlanta, 21–24 October, 1990

  • St Peter JV, Borin MT, Hughes GS, Kelloway JS, Shapiro BE, et al. Disposition of cefpodoxime proxetil in healthy volunteers and patients with impaired renal function. Antimicrobial Agents and Chemotherapy 36: 126–131, 1992

    PubMed  Article  CAS  Google Scholar 

  • Saathoff N, Lode H, Neider K, Depperman KM, Borner K, et al. Pharmacokinetics of cefpodoxime proxetil and interactions with an antacid and an H2 receptor antagonist. Antimicrobial Agents and Chemotherapy 36: 796–800, 1992

    PubMed  Article  CAS  Google Scholar 

  • Safran C. Cefpodoxime proxetil: dosage, efficacy and tolerance in adults suffering from respiratory tract infections. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 93–101, 1990

    PubMed  Google Scholar 

  • Sarubbi FA, Verghese A, Caggiano C, Holtsclaw-Berk S, Berk SL. In vitro activity of cefpodoxime proxetil (U-76,252; CS-807) against clinical isolates of Branhamella catarrhalis. Antimicrobial Agents and Chemotherapy 33: 113–114, 1989

    PubMed  Article  CAS  Google Scholar 

  • Schaadt RD, Yagi BH, Zurenko GE. In vitro activity of cefpodoxime proxetil (U-76,252; CS-807) against Neisseria gonorrhoeae. Antimicrobial Agents and Chemotherapy 34: 371–372, 1990

    PubMed  Article  CAS  Google Scholar 

  • Schumacher-Perdreau F, Jansen B, Peters G. In vitro activity of cefpodoxime against staphylococci in comparison to other cephalosporins. European Journal of Clinical Microbiology and Infectious Diseases 10: 585–587, 1991

    Article  CAS  Google Scholar 

  • Sheppard M, King A, Phillips I. In vitro activity of cefpodoxime, a new oral cephalosporin, compared with that of nine other antimicrobial agents. European Journal of Clinical Microbiology and Infectious Diseases 10: 573–581, 1991

    Article  CAS  Google Scholar 

  • Siebor E, Cordin X, Merzouki-Idrissi B, Safran C, Kazmierczak A. The post-antibiotic effect of cefpodoxime. Poster. International Congress of Infectious Diseases, Montreal, July 15–19, 1990

    Google Scholar 

  • Sieling WS, Calver A, Dansey R, Davies T, Pope A et al. Cefpodoxime proxetil (RU 51807) in the treatment of adult community-acquired pneumonias: a multicentre study. Poster. International Chemotherapy Congress, Jerusalem, pp. 31–32, June 11–16, 1989

    Google Scholar 

  • Steenwyk RC, Brewer JE, Royer ME, Cathcart JS. Reversed-phase liquid Chromatographic determination of cefpodoxime in human plasma. Journal of Liquid Chromatograpy 14: 3641–3656, 1991

    Article  CAS  Google Scholar 

  • Stevens DL, Pien F, Drehobl M. Comparison of cefpodoxime proxetil and cefaclor in the treatment of skin and soft tissue infections. Submitted to Infectious Diseases in Clinical Practise, 1992

  • Stobberingh EE, Houben AW, Philips JH. In vitro activity of cefpodoxime, a new oral cephalosporin. European Journal of Clinical Microbiology and Infectious Diseases 8: 656–657, 1989

    Article  CAS  Google Scholar 

  • Tack KJ, Wilks NE, Semerdjian G, Frazier CH, Shirin K et al. Cefpodoxime proxetil in the treatment of skin and soft tissue infections. Drugs 42 (suppl. 3): 51–56, 1991

    PubMed  Article  Google Scholar 

  • Takenouchi T, Nishino T. Antibacterial activity of cefpodoxime against Branhamella catarrhalis. Microbiology and Immunology 35: 1059–1071, 1991

    PubMed  CAS  Google Scholar 

  • Thabaut A, Meyran TA. Comparative bactericidal activity of cefpodoxime and other antibiotics. Poster. International Conference on Chemotherapy, Jerusalem, p. 25, June 11–16, 1989

  • Then RL. Ability of newer Beta-lactam antibiotics to induce Betalactamase production in Enterobacter cloacae. European Journal of Clinical Microbiology 6: 451–455, 1987

    PubMed  Article  CAS  Google Scholar 

  • Theopold HM, Matthias Ch, Adam D. Cefpodoxime proxetil concentrations in head and neck tissues. European Journal for the Clinical Study and Treatment of Infections 19: 41–43, 1991

    CAS  Google Scholar 

  • Tremblay D, Dupront A, Ho C, Coussediere D, Lenfant B. Pharmacokinetics of cefpodoxime in young and elderly volunteers after single doses. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 21–28, 1990

    PubMed  CAS  Google Scholar 

  • Uchida E, Oguchi K, Hisaoka M, Kobayashi S, Kai K, et al. Effects of ranitidine, metoclopramide, and anisotropine methylbromide on the availability of cefpodoxime proxetil CS-807 in Japanese healthy subjects. Rinsho Yakuri 19: 573–579, 1988

    Article  CAS  Google Scholar 

  • Utsui Y, Inoue M, Mitsuhashi S. In vitro and in vivo antibacterial activities of CS-807, a new oral cephalosporin. Antimicrobial Agents and Chemotherapy 31: 1085–1092, 1987

    PubMed  Article  CAS  Google Scholar 

  • Wiedemanh B, Kliebe C, Kresken M. The epidemiology of β-lactamases. Journal of Antimicrobial Chemotherapy 24 (suppl. B): 1–22, 1989

    Google Scholar 

  • Wiedemann B, Luhmer E, Zuhlsdorf MT. Microbiological evaluation of cefpodoxime proxetil. Drugs 42 (suppl 3): 6–12, 1991a

    PubMed  Article  CAS  Google Scholar 

  • Wiedemann B, Luhmer E, Zühlsdorf MT. In vitro activity of cefpodoxime and ten other cephalosporins against Gram-positive Cocci, Enterobacteriaceae and Pseudomonas aeruginosa, including β-lactamase producers. Infection 19: 363–369, 1991b.

    PubMed  Article  CAS  Google Scholar 

  • Werner H, Heizmann WR, Höflsauer M. Comparative in vitro activity of cefpodoxime against anaerobes other than Bacteroides fragilis. Infection 19: 377–379, 1991.

    PubMed  Article  CAS  Google Scholar 

  • Westblom TU, Gudipati S, Midkiff BR. In vitro susceptibility of Helicobacter pylori to the new oral cephalosporins cefpodoxime, ceftibuten and cefixime. European Journal of Clinical Microbiology and Infectious Diseases 9: 691–693, 1990

    Article  CAS  Google Scholar 

  • Wise R. The pharmacokinetics of the oral cephalosporins — a review. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 13–20, 1990

    PubMed  CAS  Google Scholar 

  • Wise R, Andrews JM, Ashby JP, Thornber D. The in-vitro activity of cefpodoxime: a comparison with other oral cephalosporins. Journal of Antimicrobial Chemotherapy 25: 541–550, 1990

    PubMed  Article  CAS  Google Scholar 

  • Yamamoto T, Yasuda J, Kanao M, Okada H. CS-807 in the field of obstetrics and gynecology. Chemotherapy 36 (Suppl. 1): 967–978, 1988

    Google Scholar 

  • Yokota T, Suzuki E, Arai K. Cefpodoxime proxetil, its in vitro antibacterial activity, affinity to bacterial penicillin-binding proteins, and synergy of bactericidal activity with serum complement and mouse-cultured macrophages. Drugs in Experimental Clinical Research 14: 495–500, 1988

    CAS  Google Scholar 

  • Yura J, Shinagawa N, Mizuno A, Mashita K, Taniguchi M, et al. CS-807 in surgery. Chemotherapy 36 (Suppl. 1): 664–676, 1988a

    Google Scholar 

  • Yura J, Shinagawa N, Mizuno A, Watanabe S, Ando M, et al. Clinical evaluation of cefpodoxime proxetil in the treatment of skin and soft tissue infections. A double blind comparison of cefpodoxime proxetil and cefaclor. Japanese Journal of Antibiotics 41: 1517–1537, 1988b

    PubMed  CAS  Google Scholar 

  • Zuck P, Rio Y, Ichou F. Efficacy and tolerance of cefpodoxime proxetil compared with ceftriaxone in vulnerable patients with bronchopneumonia. Journal of Antimicrobial Chemotherapy 26 (Suppl. E): 71–77, 1990

    PubMed  Google Scholar 

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Various sections of the manuscript reviewed by E. Bergogne-Berezin, Department of Microbiology, Bichat Hospital, Paris, France, R.W. Bury, Department of Clinical Pharmacology and Therapeutics, Maelbourne, Victoria, Australia: C. Fernandez, Microbiology Department, Royal North Shore Hospital, St Leonards, New South Wales, Australia; H. Dabernat, Laboratoire de Bactériologie, Toulouse, France; R. Fujii, Department of Pediatrics, Teikyo University, Tokyo, Japan; A.M. Geddes, Department of Infection, Universty of Brimingham, Brimingham, England; P. Gehanno, Ear, Nose and Throat Department, Hôpital Bichat-Claude, Paris, France: R.N. Jones, Department of Pathology, University of Iowa College of Medcine, Iowa City, Iowa, USA; J. Kumazawa, Department of Urology, Faculty of Medicine, Kyushu University, Fukuoka, Japan.

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Frampton, J.E., Brogden, R.N., Langtry, H.D. et al. Cefpodoxime Proxetil. Drugs 44, 889–917 (1992). https://doi.org/10.2165/00003495-199244050-00011

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Keywords

  • Cefaclor
  • Cefixime
  • Cefpodoxime
  • Cefuroxime Axetil
  • Complicated Urinary Tract Infection