Cefpodoxime Research Articles

Study of efficacy, safety and dosage on cefpodoxime proxetil in pediatric infections

Cefpodoxime proxetil (CS-807, CPDX-PR), a new cephalosporin antibiotic, was investigated for its usefulness in pediatrics. 1. The total number of patients treated were 21 with their ages ranging from 3 months to 9 years and 1 month, consisting of 5 male and 16 female infants. 2. Single dosages of the drug ranged between 4.4 mg and 5.8 mg/kg with oral administration for 3 times daily in fasting. A total aggregated dosage was between 46.4 mg/kg and 200.0 mg/kg. The length of administration was 3 to 12 days. 3. The breakdown of symptoms were 9 cases of acute pharyngitis, 5 cases of acute tonsillitis, 3 cases of acute bronchitis, and 1 case each of impetigo + purulent rhinitis, cervical lymphadenitis, scarlet fever, and urinary tract infection. 4. The clinical efficacy rate was 100% with 18 excellent responses and 3 good responses. 5. The bacteriological efficacy rate was 90.9% in eradication rate, based on results on 17 strains of suspected causative microorganism among which 10 strains were eradicated, 1 strain was decreased, and 6 strains were unknown. 6. There was no side effect during the treatment and after the discontinuation, while, in clinical laboratory tests, GOT and GPT were elevated in 1 case which was judged as abnormal. No patient refused the drug. CPDX-PR was considered to be very useful drug because of its excellent efficacy and safety in pediatrics in treating infectious diseases.

Pharmacokinetic, bacteriological and clinical studies on cefpodoxime proxetil in the field of pediatrics

Pharmacokinetic, bacteriological and clinical studies on cefpodoxime proxetil (CPDX-PR, CS-807), a newly developed oral cephem, were carried out in the treatment of infectious diseases in the field of pediatrics. 1. Since CPDX demonstrates very powerful antimicrobial actions against such Gram-negative bacilli as Escherichia coli, Salmonella sp., Klebsiella pneumoniae and Serratia sp., such Gram-positive cocci as Streptococcus pyogenes and Streptococcus pneumoniae, and beta-lactamase producing Branhamella catarrhalis and Haemophilus influenzae, this drug was thought to be useful for the treatment of pediatric infectious diseases when main causative bacteria in the field of pediatrics were taken into account. 2. When changes in blood and urine concentrations of CPDX following the administration of this drug at 3.7 mg/kg before meal were determined, Cmax and T1/2 were found to be 2.98 micrograms/ml at 2-hour and 1.73 hours, respectively; an urinary excretion rate in the first 6 hours and a maximum urine concentration were 32.5% and 52 micrograms/ml, respectively. 3. Clinically, 8 of 8 patients with the upper respiratory tract infections (100%), 28 of 29 patients with bronchitis and/or pneumonia (96.6%), 3 of 4 patients with otitis media (75%), 2 of 2 patients with sinusitis (100%), 3 of 3 patients with the skin soft tissue infections (100%), 1 of 1 patient with bacterial enteritis (100%) and 11 of 14 patients with urinary tract infections (78.6%) responded well to the treatment with CPDX-PR, showing a 91.8% efficacy rate in all the patients treated. 4. Bacteriologically, Staphylococcus aureus, Staphylococcus epidermidis, S. pyogenes, S. pneumoniae, E. faecalis, B. catarrhalis, H. influenzae, E. coli and Salmonella typhimurium were all eradicated from 5, 1, 4, 6, 1, 5, 5, 11 and 1 patient, respectively. An eradication rate in all the patients examined was 97.5% (39/40). 5. Gastrointestinal symptoms appeared as side effects in 2 of 71 patients (vomiting in 1 and diarrhea in 1), hence, an incidence of side effects was 2.8% (2/71). As for abnormal laboratory findings, eosinophilia, thrombocytosis and increases in GOT and GPT were observed in 3 of 39 patients examined (7.7%), 1 of 39 patients (2.6%) and 2 of 34 patients (5.9%), respectively. In addition, we also examined the effect of the drug on the hemostatic system, but found no changes upon the treatment. Based on these results, it appeared that CPDX-PR was a useful and safe drug in treatment of infectious diseases in the field of pediatrics when administered 2-3 times a day at a dose of 3-6 mg/kg.

In vitro activity of cefpodoxime proxetil (U-76,252; CS-807) against clinical isolates of Branhamella catarrhalis

Cefpodoxime proxetil (U-76,252; CS-807) is a new esterified oral cephem antibiotic with a broad antibacterial spectrum. Since data regarding the activity of cefpodoxime against Branhamella catarrhalis are limited, we tested its activity against 200 B. catarrhalis isolates. The drug was highly active against beta-lactamase-negative and -positive isolates; 99% of all strains tested showed a cefpodoxime proxetil MIC of less than or equal to 2.0 micrograms/ml.

Effects of ranitidine, metoclopromide, and anisotropine methylbromide on the availability of cefpodoxime proxetil (CS-807) in Japanese Healthy subjects.

The effects of ranitidine, metoclopromide, and anisotropine methylbromide on the absorption of cefpodoxime proxetil (CS-807) were examined in two studies. Pharmacokinetic parameters of R-3763, an active metabolite of CS-807 by non-specific esterases in the intestinal wall, were calculated and compared.1) A single dose of ranitidine (150 mg) was administered orally to six healthy male subjects 1. 5 hr before the dose of CS-807 (100 mg). Intragastric pH was monitored through a micro-pH-electrode for 6.5 hr after ranitidine treatment (two-way crossover).2) Nine healthy volunteers were studied for the effect of metoclopromide (MCP) and anisotropine methylbromide (ATMB) (three-way crossover).Ranitidine treatment resulted in a significant decrease in the parameters: ka (from 0.957±0.052l/hr to 0.612±0.030l/hr; P<0.05); Cmax (from 1.44±0.05μg/ml to 0.67±0.04μg/ml; P<0.01); AUC (from 7.33±0.40μghr/ml to 4.10±0.13μg hr/ ml; P<0.01); the amount of urinary excretion (37.75±0.72% to 21.07±1.82%: P< 0. 01). This indicates that the absorption of CS-807 is affected probably by the increased gastric pH and by the decrease of the dissolution of CS-807 in the stomach.In contrast to the effect of ranitidine, no significant difference was found for the pharmacokinetic parameters of R-3763 among the groups of MCP, ATMB, and the control, except for the amount excreted into the urine between MCP (31.32±1.84%) and ATMB groups (39.80±3.18%) (P<0.05).From these results, a sufficient low gastric pH and delayed gastric emptying time should be required for better absorption of CS-807 in man.