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Caroline M. Perry - One of the best experts on this subject based on the ideXlab platform.

  • Cefpodoxime Proxetil
    Paediatric Drugs, 2001
    Co-Authors: Bret Fulton, Caroline M. Perry
    Abstract:

    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. Antibacterial Activity Cefpodoxime is active against a broad range of Gram-positive and Gram-negative bacteria, including those that are frequently associated with common paediatric infections, such as acute otitis media, pharyngitis and lower respiratory tract infections e.g. bronchitis and pneumonia. The drug is active against penicillin-susceptible strains of Streptococcus pneumoniae and has modest activity against strains that are intermediately susceptible to penicillin. In a US study that evaluated the activity of various antibacterial agents against S. pneumoniae isolates (n = 4489, including 2849 penicillin-susceptible, 1059 intermediately susceptible and 581 penicillin-resistant strains), the overall activity of Cefpodoxime was less than that of amoxicillin or amoxicillin/clavulanic acid but greater than that of cefaclor, cefuroxime, cefprozil, cefixime and loracarbef. Cefpodoxime shows good in vitro activity against S. pyogenes and S. agalactiae but only modest activity against Staphylococcus aureus (methicillin-susceptible strains). The drug also has good in vitro activity against a number of Gram-negative pathogens, such as Haemophilus influenzae (including β-lactamase-producing strains), Moraxella catarrhalis and Enterobacteriaceae ( Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis ). Cefpodoxime shows good stability towards common plasmid-mediated β-lactamases, including the TEM-1 enzyme that is frequently found in H. influenzae. However, the drug appears to be susceptible to hydrolysis by most chromosomally-mediated β-lactamases. Pharmacokinetic Properties After oral administration of Cefpodoxime Proxetil, the drug is absorbed and deesterified, releasing Cefpodoxime, the active moiety, into the plasma. In paediatric patients with bacterial infections, peak plasma Cefpodoxime concentrations range from 3.7 to 5.5 mg/L and are achieved approximately 2 hours after single oral doses of Cefpodoxime Proxetil 6 mg/kg; plasma Cefpodoxime concentrations remain above 0.5 mg/L for at least 8 hours after administration of the dose. Food has no effect on the extent of absorption of orally administered Cefpodoxime Proxetil. However, coadministration of Cefpodoxime Proxetil with agents that increase gastric pH significantly decreases Cefpodoxime absorption. Cefpodoxime is generally well distributed to relevant tissues and fluids. In adults, therapeutic Cefpodoxime concentrations have been observed in lung, head and neck, tonsillar, and skin tissues, bronchial mucosa, and pleural and skin blister fluids. In children, single doses of Cefpodoxime Proxetil produced drug concentrations above the MIC_90 in tonsillar tissue and in middle ear fluid. Mean concentrations of Cefpodoxime in middle ear fluid were 0.87 mg/L at 2 hours, and 0.52 mg/L hours after administration of a single 4 mg/kg dose of Cefpodoxime Proxetil. Excretion of unchanged Cefpodoxime in the urine is the primary route of elimination of the drug. Clearance of Cefpodoxime appears to be age-dependent, with mean clearance values higher (0.57 L/h/kg) in children less than 5 years of age than in older children (0.36 L/h/kg). The mean plasma elimination half-life of Cefpodoxime ranges from 1.7 to 3.3 hours in paediatric patients. Therapeutic Efficacy Cefpodoxime Proxetil is an effective treatment for a variety of bacterial infections in paediatric patients. In children with acute otitis media, randomised controlled trials have shown 5- to 10-day regimens of Cefpodoxime Proxetil 8 to 10 mg/kg/day to be at least as effective as 5 to 10 days’ treatment with comparator β-lactam antibacterials (amoxicillin/clavulanic acid, cefixime, cefuroxime axetil or cefaclor) as assessed by either clinical or bacteriological criteria. Cefpodoxime produced a significantly higher clinical cure rate than amoxicillin/clavulanic acid both at the end of 8 days’ therapy and after follow-up (20 to 30 days after the completion of therapy) in a single trial. In children with pharyngitis and/or tonsillitis caused by S. pyogenes , treatment with Cefpodoxime Proxetil 10 mg/kg/day for 10 days produced clinical cure rates (83 to 100%) broadly similar to those achieved with penicillin V 40 mg/kg/day for 10 days (76 to 100%). A statistically significant difference in favour of Cefpodoxime Proxetil in terms of clinical end-points was demonstrated in 1 study. In 2 other investigations, Cefpodoxime Proxetil produced significantly higher bacteriological response rates than penicillin V when assessed by bacteriological criteria. In 1 study, a 5-day course of Cefpodoxime Proxetil was at least as effective as a 10-day course of penicillin V. In the treatment of lower respiratory tract infections (e.g. pneumonia, bronchitis) in children, Cefpodoxime Proxetil has demonstrated significant efficacy in a number of controlled trials. In comparative trials, Cefpodoxime Proxetil 8 mg/kg/day for 10 days produced rates of clinical cure or improvement (93 and 95%) that were similar to those obtained after 10 days of therapy with either cefuroxime axetil 30 mg/kg/day (93%) or amoxicillin/clavulanic acid 40/10 mg/kg/day (97%). Cefpodoxime Proxetil also appears to be an effective treatment for children with skin and soft tissue infections. In 2 controlled trials that included both children and adults with a variety of infections (abscess, atheroma, furuncle and carbuncle, infected wounds, cellulitis), Cefpodoxime Proxetil and comparators (cefuroxime axetil, cefaclor) produced similar rates of clinical cure (>80%) and bacteriological eradication (>90%). Tolerability Cefpodoxime Proxetil has a tolerability profile similar to that of other oral cephalosporins, with gastrointestinal symptoms (e.g. diarrhoea, loose stools, nausea/vomiting, abdominal pain) and skin rashes being the most frequently reported adverse events. The incidence of diarrhoea is age-dependent, occurring more frequently in children aged 1 month to 2 years (12.8%) than in older children (6%). In clinical trials involving paediatric patients, the tolerability of Cefpodoxime Proxetil was similar to that of comparator antibacterial drugs in terms of incidences of adverse events, severe adverse events, laboratory abnormalities and treatment discontinuations. Administration of multiple doses of the drug to adults resulted in significant decreases in the number of streptococci, E. coli, Klebsiella spp., and Gram-positive anaerobic bacteria, an increase in the growth of yeasts and enterococci, and the colonisation of Clostridium difficile in the gastrointestinal tract. Dosage and Administration The recommended dosage of Cefpodoxime Proxetil oral suspension is 8 mg/kg/day in the UK and 10 mg/kg/day in the US, administered in 2 divided doses; in the US, recommended durations of treatment are 5 days for acute otitis media and 5 to 10 days for pharyngitis and/or tonsillitis. In Japan, the normal dosage of the ‘dry syrup’ formulation is 3 mg/kg (administered as a suspension) 2 to 3 times daily; recommended indications include lower respiratory tract infections, skin and soft tissue infections, and otitis media. Although Cefpodoxime Proxetil tablets are better absorbed on a full than on an empty stomach, the absorption of the oral suspension and ‘dry syrup’ formulations is not affected by food; thus, these formulations can be administered without regard to meals. The dosage interval should be increased to 24 hours in patients with moderate renal impairment (creatinine clearance

  • Cefpodoxime Proxetil: a review of its use in the management of bacterial infections in paediatric patients.
    Paediatric drugs, 2001
    Co-Authors: Bret Fulton, Caroline M. Perry
    Abstract:

    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.

Marie T. Borin - One of the best experts on this subject based on the ideXlab platform.

  • The bioavailability of Cefpodoxime Proxetil tablets relative to an oral solution
    Biopharmaceutics & drug disposition, 1995
    Co-Authors: Marie T. Borin, Kristi K. Forbes, George S. Hughes
    Abstract:

    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.

  • Effect of timing of food on absorption of Cefpodoxime Proxetil.
    Journal of clinical pharmacology, 1995
    Co-Authors: Marie T. Borin, Mary R. Driver, Kristi K. Forbes
    Abstract:

    The effect of a high-fat meal and the timing of this meal on the absorption of a 400-mg oral dose of Cefpodoxime Proxetil was evaluated in 20 healthy, adult, male volunteers in a four-way crossover study. The area under the plasma concentration-time curve, peak plasma concentration, and urinary recovery were significantly greater (P = .0001) after administration of Cefpodoxime Proxetil tablets with and 2 hours after a meal relative to dosing under fasted conditions or 1 hour before a meal. The time to peak concentration did not differ significantly among treatments, which suggests that food did not affect the rate of drug absorption. These results indicate that absorption of Cefpodoxime Proxetil is enhanced when tablets are taken with food or shortly after a meal.

  • Effect of food on absorption of Cefpodoxime Proxetil oral suspension in adults.
    Antimicrobial agents and chemotherapy, 1995
    Co-Authors: Marie T. Borin, Kristi K. Forbes
    Abstract:

    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.

  • A Review of the Pharmacokinetics of Cefpodoxime Proxetil
    Drugs, 1991
    Co-Authors: Marie T. Borin
    Abstract:

    Cefpodoxime Proxetil is an orally absorbed broad spectrum third generation cephalosporin antibacterial. It is a prodrug that is de-esterified in vivo to its active metabolite, Cefpodoxime. After single- and multiple-dose (12-hourly) administration of Cefpodoxime Proxetil in the therapeutic dose range of 100 to 400mg of Cefpodoxime equivalents, average peak plasma concentrations of Cefpodoxime range from 1.0 to 4.5 mg/L and occur between 1.9 and 3.1 hours after administration. The half-life of Cefpodoxime ranges from 1.9 to 2.8 hours. The absolute bioavailability of Cefpodoxime Proxetil tablets is 50%, and absorption is enhanced by concomitant administration of food. Raising gastric pH by pretreatment with antacids or H_2-receptor antagonists results in reduced absorption. Binding of Cefpodoxime to human plasma or serum protein is low ( 18 to 23%), suggesting that Cefpodoxime should readily transfer across the capillary lining into tissues. Cefpodoxime undergoes minimal metabolism in humans. Drug not absorbed is degraded in the gastrointestinal tract and excreted in the faeces. As expected for a drug eliminated primarily by renal excretion, the disposition of Cefpodoxime is altered in patients with impaired renal function; the half-life increases, while apparent plasma clearance and renal clearance decrease. The pharmacokinetics of Cefpodoxime after oral administration of Cefpodoxime Proxetil are not affected by age.

Wesley Mark Todd - One of the best experts on this subject based on the ideXlab platform.

  • Cefpodoxime Proxetil a comprehensive review
    International Journal of Antimicrobial Agents, 1994
    Co-Authors: Wesley Mark Todd
    Abstract:

    Abstract Cefpodoxime Proxetil, a relatively new broad-spectrum third-generaation cephalosporin, has very good in vitro activity against Enterobacteriaceae, Hemophilus spp. and Moraxella spp., including β-lactamase producers and many strains resistant to other oral agents. It also has activity against Gram-positive bacteria, especially against streptococci. Cefpodoxime has no activity against enterococci. It is well tolerated and is one of the first third-generation cephalosporins to be available in oral form. While the compound has been used most widely in the treatment of respiratory and urinary tract infections, its utility has also been demonstrated in the treatment of skin structure infections, acute otitis media, pharyngitis, tonsillitis, and sexually transmitted diseases.

Bret Fulton - One of the best experts on this subject based on the ideXlab platform.

  • Cefpodoxime Proxetil
    Paediatric Drugs, 2001
    Co-Authors: Bret Fulton, Caroline M. Perry
    Abstract:

    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. Antibacterial Activity Cefpodoxime is active against a broad range of Gram-positive and Gram-negative bacteria, including those that are frequently associated with common paediatric infections, such as acute otitis media, pharyngitis and lower respiratory tract infections e.g. bronchitis and pneumonia. The drug is active against penicillin-susceptible strains of Streptococcus pneumoniae and has modest activity against strains that are intermediately susceptible to penicillin. In a US study that evaluated the activity of various antibacterial agents against S. pneumoniae isolates (n = 4489, including 2849 penicillin-susceptible, 1059 intermediately susceptible and 581 penicillin-resistant strains), the overall activity of Cefpodoxime was less than that of amoxicillin or amoxicillin/clavulanic acid but greater than that of cefaclor, cefuroxime, cefprozil, cefixime and loracarbef. Cefpodoxime shows good in vitro activity against S. pyogenes and S. agalactiae but only modest activity against Staphylococcus aureus (methicillin-susceptible strains). The drug also has good in vitro activity against a number of Gram-negative pathogens, such as Haemophilus influenzae (including β-lactamase-producing strains), Moraxella catarrhalis and Enterobacteriaceae ( Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis ). Cefpodoxime shows good stability towards common plasmid-mediated β-lactamases, including the TEM-1 enzyme that is frequently found in H. influenzae. However, the drug appears to be susceptible to hydrolysis by most chromosomally-mediated β-lactamases. Pharmacokinetic Properties After oral administration of Cefpodoxime Proxetil, the drug is absorbed and deesterified, releasing Cefpodoxime, the active moiety, into the plasma. In paediatric patients with bacterial infections, peak plasma Cefpodoxime concentrations range from 3.7 to 5.5 mg/L and are achieved approximately 2 hours after single oral doses of Cefpodoxime Proxetil 6 mg/kg; plasma Cefpodoxime concentrations remain above 0.5 mg/L for at least 8 hours after administration of the dose. Food has no effect on the extent of absorption of orally administered Cefpodoxime Proxetil. However, coadministration of Cefpodoxime Proxetil with agents that increase gastric pH significantly decreases Cefpodoxime absorption. Cefpodoxime is generally well distributed to relevant tissues and fluids. In adults, therapeutic Cefpodoxime concentrations have been observed in lung, head and neck, tonsillar, and skin tissues, bronchial mucosa, and pleural and skin blister fluids. In children, single doses of Cefpodoxime Proxetil produced drug concentrations above the MIC_90 in tonsillar tissue and in middle ear fluid. Mean concentrations of Cefpodoxime in middle ear fluid were 0.87 mg/L at 2 hours, and 0.52 mg/L hours after administration of a single 4 mg/kg dose of Cefpodoxime Proxetil. Excretion of unchanged Cefpodoxime in the urine is the primary route of elimination of the drug. Clearance of Cefpodoxime appears to be age-dependent, with mean clearance values higher (0.57 L/h/kg) in children less than 5 years of age than in older children (0.36 L/h/kg). The mean plasma elimination half-life of Cefpodoxime ranges from 1.7 to 3.3 hours in paediatric patients. Therapeutic Efficacy Cefpodoxime Proxetil is an effective treatment for a variety of bacterial infections in paediatric patients. In children with acute otitis media, randomised controlled trials have shown 5- to 10-day regimens of Cefpodoxime Proxetil 8 to 10 mg/kg/day to be at least as effective as 5 to 10 days’ treatment with comparator β-lactam antibacterials (amoxicillin/clavulanic acid, cefixime, cefuroxime axetil or cefaclor) as assessed by either clinical or bacteriological criteria. Cefpodoxime produced a significantly higher clinical cure rate than amoxicillin/clavulanic acid both at the end of 8 days’ therapy and after follow-up (20 to 30 days after the completion of therapy) in a single trial. In children with pharyngitis and/or tonsillitis caused by S. pyogenes , treatment with Cefpodoxime Proxetil 10 mg/kg/day for 10 days produced clinical cure rates (83 to 100%) broadly similar to those achieved with penicillin V 40 mg/kg/day for 10 days (76 to 100%). A statistically significant difference in favour of Cefpodoxime Proxetil in terms of clinical end-points was demonstrated in 1 study. In 2 other investigations, Cefpodoxime Proxetil produced significantly higher bacteriological response rates than penicillin V when assessed by bacteriological criteria. In 1 study, a 5-day course of Cefpodoxime Proxetil was at least as effective as a 10-day course of penicillin V. In the treatment of lower respiratory tract infections (e.g. pneumonia, bronchitis) in children, Cefpodoxime Proxetil has demonstrated significant efficacy in a number of controlled trials. In comparative trials, Cefpodoxime Proxetil 8 mg/kg/day for 10 days produced rates of clinical cure or improvement (93 and 95%) that were similar to those obtained after 10 days of therapy with either cefuroxime axetil 30 mg/kg/day (93%) or amoxicillin/clavulanic acid 40/10 mg/kg/day (97%). Cefpodoxime Proxetil also appears to be an effective treatment for children with skin and soft tissue infections. In 2 controlled trials that included both children and adults with a variety of infections (abscess, atheroma, furuncle and carbuncle, infected wounds, cellulitis), Cefpodoxime Proxetil and comparators (cefuroxime axetil, cefaclor) produced similar rates of clinical cure (>80%) and bacteriological eradication (>90%). Tolerability Cefpodoxime Proxetil has a tolerability profile similar to that of other oral cephalosporins, with gastrointestinal symptoms (e.g. diarrhoea, loose stools, nausea/vomiting, abdominal pain) and skin rashes being the most frequently reported adverse events. The incidence of diarrhoea is age-dependent, occurring more frequently in children aged 1 month to 2 years (12.8%) than in older children (6%). In clinical trials involving paediatric patients, the tolerability of Cefpodoxime Proxetil was similar to that of comparator antibacterial drugs in terms of incidences of adverse events, severe adverse events, laboratory abnormalities and treatment discontinuations. Administration of multiple doses of the drug to adults resulted in significant decreases in the number of streptococci, E. coli, Klebsiella spp., and Gram-positive anaerobic bacteria, an increase in the growth of yeasts and enterococci, and the colonisation of Clostridium difficile in the gastrointestinal tract. Dosage and Administration The recommended dosage of Cefpodoxime Proxetil oral suspension is 8 mg/kg/day in the UK and 10 mg/kg/day in the US, administered in 2 divided doses; in the US, recommended durations of treatment are 5 days for acute otitis media and 5 to 10 days for pharyngitis and/or tonsillitis. In Japan, the normal dosage of the ‘dry syrup’ formulation is 3 mg/kg (administered as a suspension) 2 to 3 times daily; recommended indications include lower respiratory tract infections, skin and soft tissue infections, and otitis media. Although Cefpodoxime Proxetil tablets are better absorbed on a full than on an empty stomach, the absorption of the oral suspension and ‘dry syrup’ formulations is not affected by food; thus, these formulations can be administered without regard to meals. The dosage interval should be increased to 24 hours in patients with moderate renal impairment (creatinine clearance

  • Cefpodoxime Proxetil: a review of its use in the management of bacterial infections in paediatric patients.
    Paediatric drugs, 2001
    Co-Authors: Bret Fulton, Caroline M. Perry
    Abstract:

    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.

Kristi K. Forbes - One of the best experts on this subject based on the ideXlab platform.

  • The bioavailability of Cefpodoxime Proxetil tablets relative to an oral solution
    Biopharmaceutics & drug disposition, 1995
    Co-Authors: Marie T. Borin, Kristi K. Forbes, George S. Hughes
    Abstract:

    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.

  • Effect of timing of food on absorption of Cefpodoxime Proxetil.
    Journal of clinical pharmacology, 1995
    Co-Authors: Marie T. Borin, Mary R. Driver, Kristi K. Forbes
    Abstract:

    The effect of a high-fat meal and the timing of this meal on the absorption of a 400-mg oral dose of Cefpodoxime Proxetil was evaluated in 20 healthy, adult, male volunteers in a four-way crossover study. The area under the plasma concentration-time curve, peak plasma concentration, and urinary recovery were significantly greater (P = .0001) after administration of Cefpodoxime Proxetil tablets with and 2 hours after a meal relative to dosing under fasted conditions or 1 hour before a meal. The time to peak concentration did not differ significantly among treatments, which suggests that food did not affect the rate of drug absorption. These results indicate that absorption of Cefpodoxime Proxetil is enhanced when tablets are taken with food or shortly after a meal.

  • Effect of food on absorption of Cefpodoxime Proxetil oral suspension in adults.
    Antimicrobial agents and chemotherapy, 1995
    Co-Authors: Marie T. Borin, Kristi K. Forbes
    Abstract:

    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.