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PubMed2004

[Comparison of pharmacokinetics/pharmacodynamics of cefdinir, cefpodoxime proxetil and cefaclor against common bacteria of community acquired infections].

OBJECTIVE: To compare the pharmacokinetics/pharmacodynamics property of cefdinir, cefpodoxime proxetil and cefaclor against common bacteria of community acquired infections and evaluate the recommended regimens. METHODS: The antibacterial activities of 3 agents against 238 clinical isolates were determined by standard agar dilution test and the pharmacokinetics of these antibiotics in male healthy volunteers were conducted in Latin-square manner. The time over MIC (T > MIC) of serum antibiotic concentrations were calculated with pharmacokinetic equation and MIC. RESULTS: The value of MIC90 s cefdinir against these bacterial strains except penicillin non-sensitive pneumococci were 0.031-1 mg/L. Cefpodoxime held similar antibacterial activity with cefdinir, but was less potent against staphylococci. Cefaclor had much higher MIC values than other two drugs. After oral administration of 250 mg cefaclor, the drug concentration quickly reached peak concentration of 4.95 mg/L +/- 2.41 mg/L and the eliminative half time was 0.69 h +/- 0.6 h; the Tmax, Cmax and T1/2beta of cefdinir and cefpodoxime after oral administration of 100 mg were 2.5 h +/- 0.48 h, 0.81 mg/L +/- 0.19 mg/L, 1.73 h +/- 0.3 h and 2.38 h +/- 0.43 h, 1.12 mg/L +/- 0.28 mg/L, 1.92 h +/- 0.55 h, respectively. T > MIC of cefdinir in thrice daily administration were longer than 40% of medication interval against most of the tested isolates; no T > MIC period was found in cefpodoxime against staphylococci and the T > MICs of cefaclor after 250 mg oral administration were shorter than expected values against most bacteria. CONCLUSION: With powerful antibacterial activity, the T > MICs of cefdinir after 100 mg oral administration can meet with the clinical requirement in most infections; PK/PD value of cefpodoxime proxetil against staphylococci is lower than expectancy and 250 mg cefaclor 3 times daily is not enough to the treatment of common community acquired infections, the regimens of cefpodoxime proxetil and cefclor should be furtherly optimized.

Anti-Bacterial Agents↗
PubMed1991

[RU 51807 (cefpodoxime proxetil). In vitro and in vivo antibacterial activity of a new orally administered active cephalosporin].

Cefpodoxime proxetil (RU 51807) is an enterally absorbed ester prodrug which is rapidly cleaved in vivo after oral administration, with release of the active free acid metabolite cefpodoxime. The in vitro antibacterial activity of the sodium salt of cefpodoxime (RU 51746) against approximately 800 clinical isolates was evaluated comparatively with other orally active beta-lactams. RU 51746 was found to be active against enterobacteria normally susceptible to third generation cephalosporins, with MIC50 values ranging from 0.02 mg/l (Providencia sp) to 5 mg/l (C. freundii). RU 51746 was also active against H. influenzae, including beta-lactamase producing strains (MIC50 0.04 mg/l), oxa-S S. aureus (2,5), beta-hemolytic streptococci (0.05) and S. pneumoniae (0.002). Oxa-R staphylococci and P. aeruginosa were resistant to RU 51746 (MIC50 greater than 40 mg/l for both organisms). The antibacterial activity of RU 51746 was bactericidal in nature and independent from test conditions. The molecule was stable to all the beta-lactamases studied, with the exception of cefuroximase (type Ic). RU 51746 exhibited no strong inhibitory effects on these enzymes, except with Enterobacter P99 (type Ia). A good correlation was found between in vivo activity of RU 51807 and in vitro activity of RU 51746. Cefpodoxime proxetil was found to be more effective than cefaclor in mice with experimental septicemia caused by various streptococci, with a DP50 ratio in the 10-100 range. This advantage was again evidenced for septicemias due to various enterobacteria. In contrast, cefaclor proved more effective in experimental staphylococcus infections. In mice with experimental pneumonia, cefpodoxime proxetil caused sharp falls in K. pneumoniae lung counts. Six days after induction of the infection, 60% of animals under cefpodoxime proxetil had sterile lungs, versus 25% of animals under amoxicillin.

Animals↗
PubMed1990

Pharmacokinetics and inflammatory fluid penetration of cefpodoxime proxetil in volunteers.

The pharmacokinetics of cefpodoxime were determined after a single oral dose of 261 mg of cefpodoxime proxetil, equivalent to 200 mg of cefpodoxime, was given to each of six healthy male volunteers. Concentrations in serum, urine, and cantharidin-induced inflammatory fluid were measured by a microbiological assay. The mean peak level in plasma was 2.1 micrograms/ml, attained at a mean time of 2.9 h. The mean half-life of elimination from serum was 2.2 h. The inflammatory exudate was penetrated moderately rapidly, the mean peak level being 1.7 micrograms/ml at 3.5 h. The mean percent penetration of the inflammatory exudate was 103.7. The mean 24-h urine recovery of cefpodoxime was 32.2%. This study suggests that cefpodoxime proxetil taken once or twice daily will be sufficient to treat urinary or systemic infections caused by susceptible pathogens.

Adult↗
PubMedDate not supplied

In vitro activity of cefpodoxime and ten other cephalosporins against gram-positive cocci, Enterobacteriaceae and Pseudomonas aeruginosa, including beta-lactamase producers.

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.

Bacteria↗
PubMedDate not supplied

Tissue penetration of cefpodoxime into the skeletal muscle and lung in rats.

PURPOSE: The aim of this study was to investigate the pharmacokinetics of cefpodoxime in interstitial tissue fluids (skeletal muscle and lung) in rats by microdialysis, and to examine the relationship between free drug levels in plasma and in tissues. METHODS: Cefpodoxime was administered to anesthetized male Wistar rats as single intravenous bolus of 10 or 20 mg/kg and constant infusion of 260 microg/h with a loading dose. The protein binding of cefpodoxime in rat plasma was determined using ultrafiltration. RESULTS: The average protein binding of cefpodoxime in rat plasma was 38%. The half-lives in plasma, muscle and lung were similar (approximately 5 h). After constant rate infusion, the free concentrations in the muscle and the lung were almost identical, but lower than total and free plasma concentrations. The data were modeled simultaneously using a two-compartmental body model. CONCLUSIONS: Free interstitial levels of cefpodoxime in muscle and lung tissue are very similar. Since muscle is more accessible than lung, free muscle concentrations may serve as a good surrogate for unbound concentrations in lung.

Animals↗
PubMed2005

Pharmacokinetic-pharmacodynamic modelling of antibacterial activity of cefpodoxime and cefixime in in vitro kinetic models.

The bacterial time-kill curves of cefpodoxime and cefixime against four bacterial strains (Haemophilus influenzae, Moraxella catarrhalis, Streptococcus pneumoniae/penicillin sensitive and S. pneumoniae/penicillin intermediate) were compared in in vitro infection models in which various human pharmacokinetic profiles of unbound antibiotic were simulated. This approach offers more detailed information than the minimum inhibitory concentration (MIC) does about the time course of antibacterial efficacy of an antibiotic. A pharmacokinetic-pharmacodynamic (PK-PD) model based on unbound antibiotic concentrations at the site of infection, and a sigmoid Emax-relationship with EC50 as the antibiotic concentration necessary to produce 50% of the maximum effect, effectively described the antimicrobial efficacy of both cefpodoxime and cefixime. The EC50 values of cefpodoxime and cefixime were consistent with their respective MIC values. Both antibiotics had similar high potency against H. influenzae (EC50: 0.04 mg/L) and M. catarrhalis (EC50: 0.12 mg/L), while the potency of cefpodoxime against S. pneumoniae strains was about 10-fold higher than that of cefixime (EC50s/sensitive strain: 0.02 mg/L versus 0.27 mg/L; EC50s/intermediate strain: 0.09 mg/L versus 0.69 mg/L). Applications of this model and unbound tissue PK profiles obtained from a previous clinical study performed in our group, showed that cefpodoxime has higher bacteriological potency than cefixime against S. pneumoniae. Simulations based on this model allow the comparison of antibacterial efficacy of different antibiotics and dosing regimens.

Anti-Bacterial Agents↗
PubMed1995

The sensitivity of 173 Sydney isolates of Neisseria gonorrhoeae to cefpodoxime and other antibiotics used to treat gonorrhea.

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.

Anti-Bacterial Agents↗
PubMed1990

Efficacy and tolerance of cefpodoxime proxetil compared with co-amoxiclav in the treatment of exacerbations of chronic bronchitis.

This European, multicentre trial evaluated the efficacy and tolerance of cefpodoxime proxetil in comparison with co-amoxiclav (amoxycillin plus clavulanic acid) in the treatment of acute exacerbations of chronic bronchitis. The study design was double-blind and double-placebo controlled. Doses of either 200 mg bd of cefpodoxime proxetil or 500 mg/125 mg tds amoxycillin plus clavulanic acid were given orally for 9.6 +/- 1.8 days. Two hundred and fifty-one patients were enrolled in 27 centres in West Germany, France, and Italy. The overall clinical efficacy was 97.2% in the cefpodoxime proxetil group compared with 94.7% in the co-amoxiclav group. Fifty-eight adverse events, mainly gastrointestinal, occurred in 42 patients with no significant difference between the groups. A significant difference in the number of resistant pathogens on pre-treatment culture to the advantage of cefpodoxime was noted. In our experience, both drugs were of similar value in the treatment of respiratory tract infections. Thus, cefpodoxime proxetil should be an effective antibiotic for the treatment of acute exacerbations of chronic bronchitis.

Adult↗
PubMed1990

Efficacy and tolerance of cefpodoxime proxetil compared with ceftriaxone in vulnerable patients with bronchopneumonia.

This multicentre, randomized study compared the efficacy and tolerance of cefpodoxime proxetil and ceftriaxone in vulnerable patients with bronchopneumonia. Patients received cefpodoxime proxetil 200 mg bd orally or ceftriaxone 1 g daily im for a ten-day period. They were evaluated at days 10 and 30. Ninety-six patients were evaluated for tolerance, 85 for clinical efficacy and 65 for bacteriological efficacy. At entry all patients had radiographic evidence of pneumonia and 74% of bacteriological samples were positive. The percentage of overall success (cured or improved) was 97.7% (43/44) in the cefpodoxime proxetil group and 95.1% (39/41) in the ceftriaxone group. The bacteriological efficacy was 94.3% in the cefpodoxime proxetil group and 97.4% in the ceftriaxone group. Clinical tolerance was satisfactory in both groups. In this study, the clinical and bacteriological results obtained with cefpodoxime proxetil were comparable with those obtained with ceftriaxone in the treatment of community-acquired bronchopneumonia in patients with additional risk factors.

Adult↗
PubMed1990

Cefpodoxime proxetil: dosage, efficacy and tolerance in adults suffering from respiratory tract infections.

The efficacy of cefpodoxime proxetil has been studied in ten clinical trials conducted in adults suffering from lower respiratory tract infections (pneumonia, acute bronchitis or acute on chronic bronchitis) and upper respiratory tract infections (tonsillitis/pharyngitis or sinusitis). All the trials were controlled, randomized, multicentre and international and seven were double-blind, double-dummy designed. Over a period of 18 months from July 1988 to December 1989, 2448 patients were included. Among them, 2429 (99%) were evaluated for tolerance, 2101 (86%) for tolerance and clinical efficacy and 1018 (42%) for tolerance and clinical and bacteriological efficacy. The clinical response was judged satisfactory in 1205/1263 (95.4%) patients treated with cefpodoxime proxetil and in 788/838 (94%) patients treated with comparative antibiotics. The bacteriological response was judged satisfactory for 662/699 (95%) pathogens for cefpodoxime proxetil treatment versus 427/463 (92, 2%) for comparators. Cefpodoxime proxetil has been given to 7351 patients in the course of its international development with no severe side-effect being observed. Common reactions have been noted with a similar frequency to that seen with the other beta-lactams. No pseudomembranous colitis has been observed during clinical trials. On this basis, cefpodoxime proxetil appears to be efficacious and well tolerated and could be an antibiotic of first choice in the treatment of lower and upper respiratory tract infections in adults and adolescents.

Adult↗
PubMed1994

In-vitro evaluation of cefpodoxime.

In-vitro antimicrobial activity of cefpodoxime was evaluated against several microbial species by both conventional tests and additional parameters which take into consideration some of the conditions likely to be encountered in infected tissues. MICs for 414 recent clinical isolates, including staphylococci, streptococci, Haemophilus influenzae, Moraxella catarrhalis, several Enterobacteriaceae, Aeromonas hydrophila and Campylobacter jejuni were determined. MIC values overall were similar to those observed for strains from other geographical areas. Inhibition of growth by cefpodoxime was virtually unaffected by the inoculum size, even using bacterial populations as large as 10(9) cfu of Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, H. influenzae, beta-lactamase-negative M. catarrhalis, Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis. Growth in the presence of human serum as the only source of nutrients did not significantly affect the inhibition exerted by cefpodoxime, even against large bacterial populations of S. aureus, S. pneumoniae, E. coli, and K. pneumoniae. For K. pneumoniae, E. coli, P. mirabilis and beta-lactamase-negative M. catarrhalis it was also found that sub-MIC concentrations of cefpodoxime were still able to inhibit the majority of cells in microbial populations as large as 10(9) cfu. Evaluation of bactericidal activity demonstrated that cefpodoxime concentrations comparable to those achievable in plasma or in the respiratory tract were able to kill rapidly large bacterial populations of S. pneumoniae and S. pyogenes. The bactericidal activity was apparently lower against M. catarrhalis, H. influenzae, S. aureus, E. coli, and K. pneumoniae.

Bacteria↗
PubMed1993

Cefpodoxime proxetil vs. penicillin V in pediatric streptococcal pharyngitis/tonsillitis.

This multicenter, randomized, parallel treatment, observer-blinded study was designed to evaluate the safety and efficacy of cefpodoxime proxetil (5 mg/kg twice daily for 10 days) compared with penicillin V (13.4 mg/kg three times daily for 10 days) for treatment of Group A streptococcal pharyngitis and tonsillitis in pediatric patients. Clinical and microbiologic results were evaluated before therapy, during therapy (Study Days 3 to 5), at the end of therapy (Study Days 14 to 18) and at long term follow-up (Study Days 30 to 32). Both drugs were well-tolerated in 578 patients evaluable for safety. Mild gastrointestinal complaints were noted in 6.7% of 386 cefpodoxime-treated patients and in 5.2% of 192 penicillin-treated patients. In 413 patients evaluable for efficacy, both treatment regimens resulted in comparably favorable clinical outcome; cure rates were 83.8% for 275 cefpodoxime-treated patients and 77.5% for 138 penicillin-treated patients. However, eradication of S. pyogenes at end of therapy was significantly higher with cefpodoxime (93.1%) than with penicillin (81.2%) (P < 0.01). Cefpodoxime proxetil provides an effective alternative to penicillin V for the treatment of streptococcal pharyngitis and tonsillitis.

Adolescent↗
PubMed1990

In vitro activity of cefpodoxime proxetil (U-76,252; CS-807) against Neisseria gonorrhoeae.

Cefpodoxime proxetil is an oral cephalosporin antibiotic. The in vitro activities of cefpodoxime (the active metabolite of cefpodoxime proxetil), ceftriaxone, and cefuroxime against both antibiotic-susceptible and antibiotic-resistant clinical isolates of Neisseria gonorrhoeae were determined. Cefpodoxime inhibited all penicillin-susceptible strains and penicillinase-producing strains at less than or equal to 0.015 microgram/ml; chromosomally resistant strains were inhibited by cefpodoxime at less than or equal to 0.125 microgram/ml.

Ceftizoxime↗
PubMed1991

Susceptibility of Neisseria gonorrhoeae to cefpodoxime: determination of MICs and disk diffusion zone diameters.

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.

Ceftizoxime↗
PubMed1995

Effect of food on absorption of cefpodoxime proxetil oral suspension in adults.

The effect of a high-fat meal on absorption of a 200-mg dose of cefpodoxime proxetil oral suspension was evaluated in 20 healthy, male volunteers in a randomized, two-way crossover study. The concentrations of cefpodoxime in plasma and in urine were determined by sensitive and specific high-performance liquid chromatography methods. The area under the plasma drug concentration-time curve, time to peak concentration, and urinary excretion of cefpodoxime were significantly greater (P < or = 0.05) after administration of cefpodoxime proxetil oral suspension with food than under fasting conditions. However, the difference in the areas under the curve between fed and fasted treatments was only 11%, and application of the two one-sided tests procedure showed bioequivalence between treatments for this parameter. The slight increase in the extent of drug absorption and the slower rate of absorption which results when cefpodoxime proxetil is given with food are unlikely to be of clinical importance.

Administration, Oral↗
PubMed2005

Tissue penetration of cefpodoxime and cefixime in healthy subjects.

Microdialysis is a technique that allows the measurement of free antibiotic concentrations in different tissues, which are responsible for the antibacterial activity at the infection site. In an open, randomized, 2-way crossover study in healthy volunteers, the muscle penetration of orally administered cefpodoxime (400 mg) and cefixime (400 mg) was compared using microdialysis. The results show that the total plasma concentration-time profiles of each antibiotic were similar; the area under the curve for cefpodoxime was 22.4 +/- 8.7 versus 25.6 +/- 8.5 mg/L*h for cefixime. However, tissue penetration was twice as high for cefpodoxime (area under the curve 15.4 +/- 5.1 mg/L*h) as for cefixime (area under the curve 7.3 mg/L*h). This degree of tissue distribution is consistent with their protein binding of 21% for cefpodoxime and 65% for cefixime. After equilibration, the unbound tissue concentrations of both antibiotics were similar to their unbound plasma concentrations. Pharmacokinetic modeling was applied to describe the pharmacokinetic profiles in plasma and muscle. The study demonstrates that cefpodoxime shows greater tissue penetration than cefixime.

Anti-Bacterial Agents↗
PubMed1991

Cefpodoxime proxetil in upper respiratory tract infections.

Cefpodoxime proxetil is a new third generation oral cephalosporin, which shows potent antibacterial activity against both Gram-positive and Gram-negative bacteria, and high stability in the presence of beta-lactamases. Low concentrations of cefpodoxime inhibit most respiratory pathogens, including Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella (Branhamella) catarrhalis. Cefpodoxime reaches concentrations of 0.24 +/- 0.06 mg/kg in tonsils, 0.89 +/- 0.80 mg/kg in lung parenchyma, and 0.91 +/- 0.01 mg/kg in bronchial mucosa; these values exceed by far the minimum inhibitory concentrations (MICs) of cefpodoxime for respiratory pathogens. Preliminary clinical studies were carried out in 181 patients with upper respiratory tract infections: the results indicated an overall clinical response in 88.4% of patients; in 30% the clinical efficacy was excellent and in 58.5% it was good. Further studies showed clinical cure in 90.3% of patients with pharyngotonsillitis, and clinical efficacy (cure plus improvement) in 95% of those with acute sinusitis. Moreover, bacterial eradication was obtained in 78 to 96.7% of cases, most of which involved H. influenzae, streptococci, or M. catarrhalis. Cefpodoxime appears to be an effective new antibacterial that can be recommended as a drug of first choice in the treatment of most upper respiratory tract infections.

Ceftizoxime↗
PubMed2005

Disposition of orally administered cefpodoxime proxetil in foals and adult horses and minimum inhibitory concentration of the drug against common bacterial pathogens of horses.

OBJECTIVES: To determine the disposition of orally administered cefpodoxime proxetil in foals and adult horses and measure the minimum inhibitory concentrations (MICs) of the drug against common bacterial pathogens of horses. ANIMALS: 6 healthy adult horses and 6 healthy foals at 7 to 14 days of age and again at 3 to 4 months of age. PROCEDURE: A single dose of cefpodoxime proxetil oral suspension was administered (10 mg/kg) to each horse by use of a nasogastric tube. In 7- to 14-day-old foals, 5 additional doses were administered intragastrically at 12-hour intervals. The MIC of cefpodoxime for each of 173 bacterial isolates was determined by use of a commercially available test. RESULTS: In 7- to 14-day-old foals, mean +/- SD time to peak serum concentration (Tmax) was 1.7 +/- 0.7 hours, maximum serum concentration (Cmax) was 0.81 +/- 0.22 microg/mL, and elimination half-life (harmonic mean) was 7.2 hours. Disposition of cefpodoxime in 3- to 4-month-old foals was not significantly different from that of neonates. Adult horses had significantly higher Cmax and significantly lower Tmax, compared with values for foals. The MIC of cefpodoxime required to inhibit growth of 90% of isolates for Salmonella enterica, Escherichia coli, Pasteurella spp, Klebsiella spp, and beta-hemolytic streptococci was 0.38, 1.00, 0.16, 0.19, and 0.09 microg/mL, respectively. CONCLUSIONS AND CLINICAL RELEVANCE: Oral administration at a dosage of 10 mg/kg every 6 to 12 hours would appear appropriate for the treatment of equine neonates with bacterial infections.

Administration, Oral↗