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PubMed1992

Cefpodoxime proxetil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic potential.

Cefpodoxime proxetil is an orally administered prodrug which is absorbed and de-esterified by the intestinal mucosa to release the third generation cephalosporin, cefpodoxime. Cefpodoxime is stable towards the most commonly found plasmid-mediated beta-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 patients. The extended plasma half-life of cefpodoxime (1.9 to 3.7 h) permits twice daily administration. In comparative trials, twice daily cefpodoxime proxetil (dose equivalent cefpodoxime 100 to 400 mg) 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 beta-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.

Animals↗
PubMed2001

Cefpodoxime proxetil: a review of its use in the management of bacterial infections in paediatric patients.

UNLABELLED: Cefpodoxime proxetil is an oral third generation cephalosporin with a broad spectrum of antibacterial activity. The drug has in vitro activity against many common Gram-positive and Gram-negative pathogens associated with common paediatric infections, making the drug a useful option for empirical therapy. In randomised controlled trials conducted in children with acute otitis media, oral cefpodoxime proxetil 8 to 10 mg/kg/day (usually administered in 2 divided doses) for 5 to 10 days was at least as effective as standard regimens of amoxicillin/ clavulanic acid, cefixime, cefuroxime axetil or cefaclor as assessed by either clinical or bacteriological criteria. Cefpodoxime 8 to 10 mg/kg/day (administered in 2 divided doses) for 5 to 10 days was at least as effective as standard 10-day regimens of penicillin V in the treatment of children with pharyngitis and/or tonsillitis. Significant differences in favour of cefpodoxime proxetil were demonstrated in terms of clinical (1 study) and bacteriological (2 studies) criteria. The clinical efficacy of 5 days of treatment with cefpodoxime proxetil is similar to that of 10 days of treatment with penicillin V. In children with lower respiratory tract infections (primarily pneumonia), clinical and bacteriological efficacy rates achieved with cefpodoxime proxetil treatment were similar to those produced by cefuroxime axetil or amoxicillin/clavulanic acid in randomised controlled trials. Cefpodoxime proxetil also demonstrated clinical efficacy in paediatric patients with skin and soft tissue infections. In randomised studies that included both adults and children with a variety of infections (e.g. abscess, atheroma, furuncle and carbuncle, infected wounds, cellulitis), cefpodoxime proxetil showed efficacy similar to that of cefuroxime axetil or cefaclor. Cefpodoxime proxetil is well tolerated by paediatric patients, with adverse events (primarily gastrointestinal tract disturbances and skin rashes) that are consistent with those reported for other oral cephalosporins. CONCLUSION: Cefpodoxime proxetil is a third generation cephalosporin with a broad spectrum of antibacterial activity and a favourable pharmacokinetic profile which allows twice-daily administration. It is generally well tolerated and demonstrates good bacteriological and clinical efficacy in paediatric patients with various infectious diseases, including acute otitis media, tonsillitis and/or pharyngitis. Based on these characteristics, cefpodoxime proxetil is a suitable option for the treatment of paediatric patients with various common bacterial infections.

Acute Disease↗
PubMed1991

Cefpodoxime proxetil in the treatment of lower respiratory tract infections.

Cefpodoxime proxetil is the orally absorbed ester of cefpodoxime, a new third generation cephalosporin. In the gastrointestinal tract, cefpodoxime proxetil is hydrolysed to cefpodoxime, which has potent antibacterial activity against the major bacterial pathogens involved in lower respiratory tract infections: Haemophilus influenzae, Moraxella (Branhamella) catarrhalis (including beta-lactamase-producing strains), and Streptococcus pneumoniae (including amoxicillin-resistant strains). Six randomised comparative studies in patients with lower respiratory tract infections, 5 of which were large (enrollment of more than 200 patients) and double-blind, examined the efficacy and safety of cefpodoxime proxetil. Cefpodoxime proxetil (at a dosage equivalent to 200mg of cefpodoxime) administered twice daily for 5 to 10 days was similar in clinical and bacteriological efficacy to the following: amoxicillin 500mg 3 times daily in the treatment of community-acquired pneumonia; intramuscular ceftriaxone Ig once daily in the treatment of pulmonary infections in hospitalised patients; and to amoxicillin/clavulanic acid 500/125mg 3 times daily in the treatment of acute exacerbations of chronic bronchitis (AECB). Additionally, a dosage equivalent to 100mg or 200mg of cefpodoxime twice daily was similar in clinical and bacteriological efficacy to amoxicillin 250mg 3 times daily in the treatment of bronchitis (acute or AECB). The adverse events noted with cefpodoxime proxetil administration were similar to those associated with other beta-lactam antibacterials and most commonly involved the gastrointestinal tract and skin or mucous membranes. Thus, cefpodoxime proxetil is a useful addition to the antibacterials available for the treatment of infections of the lower respiratory tract.

Aged↗
PubMed1990

Pharmacokinetics of cefpodoxime in young and elderly volunteers after single doses.

Three pharmacokinetic studies involving single oral doses of cefpodoxime proxetil in healthy volunteers are reported. The first study was to determine the absolute bioavailability of cefpodoxime, the second was to study the relationship between the oral dose of cefpodoxime proxetil and pharmacokinetic parameters of cefpodoxime, and the third was to compare the pharmacokinetics of cefpodoxime in healthy young and elderly volunteers. Half the dose of cefpodoxime orally administered as cefpodoxime proxetil in tablet form reaches the systemic circulation, while 80% of the cefpodoxime absorbed is excreted unchanged in urine. The volume of distribution is large (32.3 l). The pharmacokinetics of cefpodoxime were linear in young and elderly subjects after 100 and 200 mg oral doses, which are those used therapeutically. The Cmax was about 1.4 mg/l (after 100 mg) and 2.6 mg/l (after 200 mg). Deviation from linearity appeared at 400 mg and the effect was confirmed at 800 mg. The differences between young and elderly subjects were negligible, with the exception of the half-life which increased by only 14%, from 2.67 to 3 h. Dosage adjustment is therefore not necessary in the elderly.

Administration, Oral↗
PubMed1995

The bioavailability of cefpodoxime proxetil tablets relative to an oral solution.

The bioavailability of cefpodoxime proxetil tablets relative to an oral solution of cefpodoxime proxetil in a sucrose/alcohol/citric acid vehicle was studied in 11 healthy volunteers in a randomized, crossover study. Fasted subjects took one cefpodoxime proxetil 100 mg tablet or 50 mL of a 2 mg mL-1 cefpodoxime proxetil oral solution on two separate occasions. In a third study period, all subjects took a 100 mg dose of the oral solution with a high-fat meal to investigate the effect of food on cefpodoxime proxetil absorption from the oral solution. Serial blood samples were obtained over a 24 h period, and urine was collected for 48 h after dosing. Cefpodoxime concentrations in plasma and in urine were determined using HPLC methods. The bioavailability of cefpodoxime proxetil tablets relative to the oral solution was 82%, as determined from AUC ratios. There was no difference in the rate of cefpodoxime absorption between dosage forms. Food had no effect on the extent of drug absorption from the oral solution but did result in delayed absorption. These results suggest that complete dissolution of cefpodoxime proxetil is critical for optimal bioavailability.

Administration, Oral↗
PubMedDate not supplied

Cefpodoxime: comparative antibacterial activity, influence of growth conditions, and bactericidal activity.

The antimicrobial activity of cefpodoxime, the active metabolite of the new cephalosporin ester cefpodoxime proxetil, in comparison to cefixime, cefotiam, cefuroxime, and cefotaxime was determined against a broad spectrum of freshly isolated gram-positive and gram-negative bacterial strains. Cefpodoxime was demonstrated to be inhibitory at concentrations of less than or equal to 1 mg/l against 90% of strains of Moraxella catarrhalis, Haemophilus influenzae, Escherichia coli (beta-lactamase- negative strains), Klebsiella spp., Serratia spp., Proteus mirabilis, Proteus vulgaris, Providencia spp., and Salmonella spp. This antimicrobial activity of cefpodoxime was generally superior to that of cefuroxime and similar to that of cefixime. Cefpodoxime was active at less than or equal to 1 mg/l against 50% of the members of beta-lactamase-producing Escherichia coli, Enterobacter cloacae, Enterobacter aerogenes, Citrobacter spp., and Morganella morganii. Cefpodoxime proved to be highly inhibitory against group A, B, and G streptococci and Streptococcus pneumoniae (MIC90 less than 0.015 mg/l). The MICs of cefpodoxime and those of the other cephalosporins were less than 2 mg/l for greater than or equal to 90% of the strains of Staphylococcus aureus and Staphylococcus epidermidis, with the exception of cefixime which had no activity with MICs below 8 mg/l against these bacteria. Pseudomonas spp., Acinetobacter spp., and Enterococcus spp. were resistant to cefpodoxime. The antibacterial activity of cefpodoxime was only to a minor degree influenced by different growth conditions with the exception of high inoculum sizes against some beta-lactamase producing strains of gram-negative bacilli.(ABSTRACT TRUNCATED AT 250 WORDS)

Anti-Infective Agents, Urinary↗
PubMed1992

Disposition of cefpodoxime proxetil in healthy volunteers and patients with impaired renal function.

The disposition of cefpodoxime in 24 subjects with various degrees of renal function after administration of a single oral dose of 200 mg of cefpodoxime proxetil (equivalent to 200 mg of cefpodoxime activity) was studied. Subjects were assigned to one of four groups (six per group): group I, normal renal function (creatinine clearance [CLCR], greater than ml/min); group II, mild renal impairment (CLCR, 50 to 80 ml/min); group III, moderate renal impairment (CLCR, 30 to 49 ml/min); or group IV, severe renal impairment (CLCR, 5 to 29 ml/min). Although cefpodoxime terminal elimination half-life in group I (2.55 +/- 0.25 h [mean +/- standard deviation]) was not significantly different from that in group II (3.53 +/- 0.74 h), the half-life values for group III (5.90 +/- 1.67 h) and group IV (9.80 +/- 1.21 h) were significantly prolonged compared with those of group I. The mean absorption rate constant was similar among groups and ranged from 0.68 to 0.85 h-1. All groups exhibited absorption lag-times which were comparable (0.30 to 0.41 h), and the apparent volume of distribution was similar among groups. Cefpodoxime apparent total body clearance (CLP/F) values in groups II, III, and IV (132 +/- 29, 112 +/- 41, and 55.7 +/- 9.9 ml/min, respectively) were significantly lower than that in group I (238 +/- 44 ml/min). Cefpodoxime CLP/F was positively correlated with CLCR (r2 = 0.79; P less than 0.05): CLP/F = (1.9 CLCR) + 18.4. Renal clearance also declined with decreasing renal function. Adjustments in cefpodoxime organism and on the site and severity of infection. Simulated plasma concentration-time data from this study suggest that 200 mg of cefpodoxime proxetil administered every 12 to 24 h to subjects with CLcr between 30 and 49 ml/min and 200-mg dose taken every 24 h by subjects with CLcr between 5 and 29 ml/min will maintain cefpodoxime concentration in plasma similar to those in subjects with normal renal function who receive a standard dosage mg every 12 h.

Acute Kidney Injury↗
PubMed1995

Subinhibitory concentrations of cefpodoxime alter membrane protein expression of Actinobacillus actinomycetemcomitans and enhance its susceptibility to killing by neutrophils.

The aim of the present study was to determine the effect of the antibiotic cefpodoxime on the gram-negative periodontopathic microorganism Actinobacillus actinomycetemcomitans and its interaction with elements of the host immune system. Growth of A. actinomycetemcomitans in subinhibitory concentrations of cefpodoxime induced morphological changes in the bacteria, causing the organisms to grow as filaments rather than coccobacilli. Growth in cefpodoxime did not render these bacteria susceptible to killing by serum, nor did it abrogate the requirement for serum opsonins to support the bactericidal activity of neutrophils. Cefpodoxime enhanced the susceptibility of A. actinomycetemcomitans to the bactericidal activity of neutrophils. In the presence of suitable opsonins, neutrophils were able to kill four times as many cefpodoxime-induced A. actinomycetemcomitans filaments as untreated A. actinomycetemcomitans CFU. This effect was due to antibiotic actions on the bacterium and not on the neutrophil. At inhibitory concentrations, the bactericidal activities of cefpodoxime and neutrophils were additive, and cefpodoxime did not interfere with the normal functioning of the neutrophils. Concomitant with these morphological and functional changes, the expression of two outer membrane proteins (66 and 29 kDa) and one inner membrane protein (57 kDa) was decreased in A. actinomycetemcomitans grown in cefpodoxime. The concentration range over which cefpodoxime is effective against A. actinomycetemcomitans in vivo may be extended by the ability of subinhibitory concentrations to enhance the susceptibility of this organism to host immune defenses.

Adult↗
PubMed1998

Comparison of once daily cefpodoxime proxetil suspension and thrice daily cefaclor suspension in the treatment of acute otitis media in children.

An open-labeled and randomized trial was conducted to compare the efficacy and safety of once daily cefpodoxime proxetil suspension (10mg/kg/day) and thrice daily cefaclor (45mg/kg/day) in the treatment of acute otitis media in children. A total of 57 children aged from 6 months to 9 years were enrolled; 23 were treated with cefpodoxime and 34 with cefaclor. Satisfactory clinical outcome, either cure or improvement, was achieved at the end of treatment in 90% of patients in the cefaclor group and 95% of patients in the cefpodoxime group (p > 0.05). Clinical recurrence was identified at the follow-up visits in one case of the cefaclor group (3%), and none in the cefpodoxime group (p > 0.05). These drugs were well tolerated by 14/21 (67%) in the cefpodoxime-treated group and 27/32 (84%) in the cefaclor-treated group. The incidence of adverse events was slightly higher in the cefpodoxime group than in the cefaclor group, however the difference did not reach statistical significance (p > 0.05). The daily cost of once-daily cefpodoxime was lower than that of thrice-daily cefaclor. We conclude that cefpodoxime administered once daily is as effective and safe as cefaclor administered thrice daily in the treatment of acute otitis media in children. The less dosing frequency and lower daily price of cefpodoxime provide additional benefits.

Acute Disease↗
PubMed1994

Comparison of cefpodoxime proxetil and cefixime in the treatment of acute otitis media in infants and children. Otitis Study Group.

OBJECTIVE: To compare the use of once-a-day cefpodoxime proxetil to once-a-day cefixime in the treatment of acute suppurative otitis media. DESIGN: Randomized, multicenter, investigator-blinded. SETTING: Outpatient. PATIENTS: A total of 368 patients (age 2 months to 17 years) were randomized to receive either cefpodoxime or cefixime in a 2:1 ratio (245 cefpodoxime, 123 cefixime); 236 patients (155 cefpodoxime, 81 cefixime) were evaluable for drug efficacy. INTERVENTIONS: Patients received either cefpodoxime proxetil oral suspension (10 mg/kg/day, once daily for 10 days) or cefixime oral suspension (8 mg/kg/day, once daily for 10 days). MAIN OUTCOME MEASURES: Clinical evaluations were performed before treatment (study day 1), at an interim visit (study day 3 through 6), at the end of therapy (study day 12 through 15), and at final follow-up (study day 25 through 38). Microbiologic evaluations were performed at enrollment and whenever appropriate thereafter. RESULTS: End-of-therapy clinical cure rates in evaluable patients were 56% for the cefpodoxime group and 54% for the cefixime group. Clinical improvement rates were 27% for both groups. Clinical response rates were not significantly different between treatment groups (P = .541; 95% confidence interval = -8.1%, 15.2%). At long-term follow-up, 17% of patients in the cefpodoxime group and 20% in the cefixime group had a recurrence of infection. Drug-related adverse events (eg, diarrhea, diaper rash, vomiting, rash) occurred in 23.3% of cefpodoxime-treated patients and 17.9% of cefixime-treated patients (P = .282). CONCLUSIONS: These findings suggest that cefpodoxime proxetil administered once daily is as effective and safe as cefixime given once daily in the treatment of acute suppurative otitis media in pediatric patients.

Acute Disease↗
PubMed1994

Pharmacokinetics of cefpodoxime proxetil in healthy young and elderly volunteers.

The influence of age on the pharmacokinetics of cefpodoxime was evaluated in 12 elderly (ages 65-85 years) and 12 weight- and sex-matched young (ages 20-33 years) subjects, each of whom received two cefpodoxime proxetil 200-mg tablets every 12 hours for 14.5 days. Serial blood samples and urine were collected after the first dose on day 1, after the morning dose on day 8, and after the last (morning) dose on day 15. Plasma and urine samples were assayed for cefpodoxime concentrations using HPLC methods. Within each age group, mean pharmacokinetic parameters determined on day 1 were similar to corresponding values on days 8 and 15, indicating that cefpodoxime does not accumulate after twice-daily dosing of cefpodoxime proxetil. Based on this result, parameters were pooled across days in each age group. No significant differences were observed between healthy and elderly volunteers in area under the plasma concentration-time curve for the 12-hour dosing interval, peak plasma concentration, or time to peak concentration. Mean urinary excretion and renal clearance of cefpodoxime were significantly lower in elderly subjects. Differences in renal clearance were attributed to the corresponding age-related reduction that was noted in creatinine clearance values, whereas the lower urinary excretion of cefpodoxime probably reflected slightly reduced systemic drug absorption in the elderly. Differences in these parameters between groups were less than 30%, and were unlikely to be of clinical importance. The data indicate that dose adjustment of cefpodoxime in elderly subjects having normal (age-adjusted) creatinine clearance values is not required.

Adolescent↗
PubMed1993

Comparison of oral cefpodoxime proxetil and cefaclor in the treatment of skin and soft tissue infections.

This multicenter, randomized, double-blind study was designed to compare the safety and efficacy of cefpodoxime proxetil and cefaclor in the treatment of skin and soft tissue infections. Patients were aged > or = 12 years with acute (< or = 7 days duration), single-site skin or skin-structure infections. The 7- to 10-day treatment regimens were cefpodoxime proxetil (400 mg cefpodoxime) orally with food twice a day with cefaclor-matched placebo (orally, fasting, three times a day); or cefaclor (Ceclor; 500 mg anhydrous equivalent) orally, fasting, three times a day, with cefpodoxime-matched placebo (orally with food twice a day). Clinical progress and cultures were evaluated upon admission to the study; on study days 7-10 and 15-18; and 2-3 weeks after treatment. Cefpodoxime had lower minimum inhibitory concentrations against the majority of Staphylococcus species than did cefaclor. Both treatments were highly effective (99% pathogen eradication and 86% cure rate). These high eradication rates were not unexpected in this study of minor infections in which patients with resistant pathogens were excluded. Cefaclor had a higher failure rate [2 (4%) of 57], than did cefpodoxime [2 (1%) of 139; p not significant]. Most patients in both groups completed treatment as planned: 185 (74%) of 249 cefpodoxime-treated patients and 91 (75%) of 122 cefaclor-treated patients. Both treatments were well tolerated and considered safe and effective in the treatment of skin and skin structure infections. However, the twice-a-day dosing regimen for cefpodoxime proxetil compared with the three-times-a-day regimen for cefaclor may result in better patient compliance.

Administration, Oral↗
PubMed1995

Clinical experience with cefpodoxime proxetil in acute otitis media.

Although it varies from country to country, there is a worrying worldwide increase in antibiotic resistance among pathogens causing otitis. This has led to a search for therapeutic alternatives to the reference treatment, which is still amoxicillin in many countries. Cefpodoxime proxetil is one such alternative. Six comparative randomized trials of cefpodoxime proxetil in childhood acute otitis media have been published or presented at international conferences. They involved a total of 1188 patients, 658 of whom received cefpodoxime proxetil and 530 of whom received the comparator drug (amoxicillin/clavulanic acid in 3 trials, cefaclor in 1, and cefixime in 2); duration of treatment varied from 5 days for cefpodoxime proxetil to 10 days for amoxicillin/clavulanic acid, and the age of the children included ranged from 2 months to 12 years. The clinical efficacy of cefpodoxime proxetil was at least equivalent to that of the comparators in 4 trials and significantly better in 2 trials. Firstly, in one study vs. amoxicillin/clavulanic acid, the superiority of cefpodoxime proxetil (8 mg/kg/day twice daily) in terms of healing at the end of treatment and in terms of the number of normal tympanograms at the follow-up visit was shown. Secondly, in a study performed by our group, vs. cefixime, cefpodoxime proxetil (8 mg/kg/day twice daily) showed a better healing rate at the end of treatment in febrile and painful acute otitis media. The microbiologic and pharmacokinetic data show that cefpodoxime proxetil is one of the most active compounds against Haemophilus influenzae and Streptococcus pneumoniae.(ABSTRACT TRUNCATED AT 250 WORDS)

Acute Disease↗
PubMed1993

Pharmacokinetics and ex vivo susceptibility of cefpodoxime proxetil in patients receiving continuous ambulatory peritoneal dialysis.

Pharmacokinetics of cefpodoxime, an extended-spectrum cephalosporin, were determined for eight noninfected patients on continuous ambulatory peritoneal dialysis (CAPD) and eight healthy volunteers. Subjects were matched for sex, age (+/- 6 years), and body weight (+/- 10 kg, except for one pair) and received a single 200-mg (cefpodoxime equivalents) oral dose of the prodrug cefpodoxime proxetil in an open-label, paired-design fashion. Dialysate (CAPD group only), plasma, and urine samples were collected and assayed for cefpodoxime by a microbiologic method. In addition, mean bactericidal titers of the effluent dialysate against selected bacterial strains often associated with CAPD-related peritonitis were determined at 6 and 24 h after the dose. There was a significant difference (P < 0.05) in all pharmacokinetic parameters between healthy and CAPD subjects, except for lag time to absorption. The mean peak plasma cefpodoxime concentration of 1.88 +/- 0.6 micrograms/ml occurred at 2.44 +/- 0.5 h for healthy volunteers, while the peak concentration of 3.25 +/- 1.4 micrograms/ml occurred at 12.0 +/- 4.2 h for patients on CAPD. The average elimination half-life in CAPD patients was approximately 12 times greater than that seen in healthy volunteers. Peritoneal dialysis had a minimal effect on cefpodoxime clearance. In healthy volunteers, 24.2% +/- 13% of the dose was recovered from the urine, in contrast to only 5.59% +/- 6.9% for CAPD patients. The mean bactericidal titers for all CAPD patients, at 6 and 24 h, were mostly less than 1:2 and did not exceed 1:4 for any of the isolates. Because of the decreased renal clearance and negligible dialysate clearance of cefpodoxime, and delayed drug absorption, the dosage interval for cefpodoxime proxetil may need to be extended in CAPD patients.

Administration, Oral↗
PubMed1991

Microbiological evaluation of cefpodoxime proxetil.

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.

Ceftizoxime↗
PubMed2005

[Activity of cefpodoxime against pathogens causing respiratory, urinary or soft tissue infections].

BACKGROUND: Cefpodoxime is a new antimicrobial in the Chilean market, recommended for treatment of respiratory and urinary tract infections. AIM: To study the susceptibility of common pathogens isolated from Chilean patients to cefpodoxime and other antimicrobials. MATERIAL AND METHODS: The in vitro activity of cefpodoxime, expressed as Minimal Inhibitory Concentration, was studied in 331 S pneumoniae, H influenzae, M catarrhalis, E coli, S aureus and S pyogenes strains, isolated between 2000 and 2004 from respiratory, urinary and soft tissue infections, respectively. RESULTS: Eleven percent of S pneumoniae isolates were resistant to penicillin, 11% were resistant to cefuroxime and 10% to cefpodoxime. All H influenzae isolates were susceptible to cefpodoxime. No H influenzae isolates were resistant to second or third generation cephalosporines. Four percent of H influenzae isolates were resistant to ampicillin by ss-lactamase production. In contrast 81% of M catarrhalis strains were resistant to ampicillin. Six percent of E coli isolates were resistant to cefpodoxime, 9% to cefuroxime, 11% to cefadroxile and 50% to ampicillin or trimethoprim/sulphamethoxazole. Cefpodoxime was the most active antimicrobial against S pyogenes. CONCLUSIONS: Cefpodoxime, recently introduced in Chile, is a good alternative for the treatment of common respiratory and urinary tract infections.

Anti-Bacterial Agents↗
PubMed1991

[Study of the bactericidal effect of cefpodoxime using an in vitro pharmacokinetic model].

Cefpodoxime is a new oral prodrug antibiotic. Following absorption from the proximal intestine, non-specific esterases hydrolyze this cleavable ester, releasing cefpodoxime, a new broad-spectrum third-generation cephalosporin with sustained plasma levels in humans. Cefpodoxime killing kinetics were studied using an in vitro model which simulates the pharmacokinetic profile obtained in healthy volunteers given a single oral dose of cefpodoxime proxetil providing 100, 200 or 400 mg active cefpodoxime. Cefpodoxime exhibited strong antibacterial activity against tested strains of Escherichia coli, Streptococcus pneumoniae and Staphylococcus aureus. These results suggest that use of two daily doses of 100 or 200 mg each are appropriate for the treatment of E. coli and S. pneumoniae infections in view of the pharmacokinetic properties of cefpodoxime. Less intensive therapy is probably adequate in uncomplicated community-acquired urinary tract infections. The bactericidal effect of cefpodoxime against S. aureus is prolonged due to a postantibiotic effect.

Ceftizoxime↗
PubMed1996

Bioavailability of cefpodoxime proxetil with co-administered acetylcysteine.

In a cross-over study on twelve healthy volunteers cefpodoxime proxetil (CAS 87239-81-4) and acetylcysteine (CAS 616-91-1) were evaluated for possible pharmacokinetic interactions. After a standardized breakfast, the subjects received p.o. either 200 mg cefpodoxime administered as cefpodoxime proxetil (reference) or 200 mg cefpodoxime and 200 mg acetylcysteine (test). To determine the pharmacokinetic profile of cefpodoxime the plasma concentrations were determined by HPLC. The plasma concentration-time curve of cefpodoxime was very similar after both regimens, and with respect to cefpodoxime bioequivalence has been proven. The narrow range of 90% confidence intervals for the quotient test/reference for Cmax and AUC indicate reliable bioavailability of cefpodoxime proxetil independent of co-administered acetylcysteine.

Acetylcysteine↗