In vitro antibacterial activity of pediatric Faropenem sodium against respiratory tract pathogens in children / 中华实用儿科临床杂志

Objective:To evaluate the antibacterial activity of pediatric Faropenem sodium against common pathogens isolated from children′s respiratory tract in vitro, and to provide reference for its clinical research and application. Methods:Retrospective analysis.The minimum inhibitory concentration (MIC) of Faropenem sodium, Merope-nem, Imipenem and other antibiotics was determined by the agar dilution method.A total of 156 strains of Streptococcus pneumoniae [including 32 strains of Penicillin-susceptible Streptococcus pneumoniae (PSSP), 28 strains of Penicillin-intermediate Streptococcus pneumoniae (PISP) and 96 strains of Penicillin-resistant Streptococcus pneumoniae (PRSP)], 98 strains of Haemophilus influenza, 173 strains of Klebsiella pneumoniae, and 55 strains of Moraxella catarrhali clinical isolates were used.MIC 50, MIC 90 and the accumulative inhibition of the bacteria were investigated. Results:The MIC of Faropenem sodium against all the Streptococcus pneumoniae strains ranged from 0.010-2.000 mg/L.There was no difference in the MIC distribution of Faropenem sodium against PSSP, PISP and PRSP, and the MIC 90 value was all 1.000 mg/L.Faropenem sodium inhibited all the Haemophilus influenza strains at concentrations ranging from 0.030-8.000 mg/L.There was no difference in the MIC distribution of Faropenem sodium against Haemophilus influenza with or without β-lactamase and Ampicillin resistance.The MIC 90 value was all 4.000 mg/L.Ho-wever, the MIC of Faropenem sodium against Klebsiella pneumoniae ranged from 0.250 to above 32.000 mg/L, and both MIC 50 and MIC 90 were greater than 32.000 mg/L.Faropenem sodium inhibited all the Moraxella catarrhalis strains at concentrations ranging from 0.030-2.000 mg/L, with MIC 50 being 0.500 mg/L and MIC 90 being 1.000 mg/L. Conclusions:Antimicrobial susceptibility testing results in vitro demonstrate that pediatric Faropenem sodium has satisfactory antibacterial activities against Streptococcus pneumoniae, Haemophilus influenza, and Moraxella catarrhalis, but comparatively weak antibacterial activities against Klebsiella pneumoniae.

Treatment of acute uncomplicated cystitis with faropenem for 3 days versus 7 days: multicentre, randomized, open-label, controlled trial.

OBJECTIVES: The increasing prevalence of resistant bacteria such as fluoroquinolone-resistant or extended-spectrum ß-lactamase-producing strains in pathogens causing acute uncomplicated cystitis has been of concern in Japan. Faropenem sodium is a penem antimicrobial that demonstrates a wide antimicrobial spectrum against both aerobic and anaerobic bacteria. It is stable against a number of ß-lactamases. METHODS: We compared 3 and 7 day administration regimens of faropenem in a multicentre, randomized, open-label, controlled study. RESULTS: In total, 200 female patients with cystitis were enrolled and randomized into 3 day (N = 97) or 7 day (N = 103) treatment groups. At the first visit, 161 bacterial strains were isolated from 154 participants, and Escherichia coli accounted for 73.9% (119/161) of bacterial strains. At 5-9 days after the completion of treatment, 73 and 81 patients from the 3 day and 7 day groups, respectively, were evaluated by intention-to-treat analysis; the microbiological efficacies were 58.9% eradication (43/73), 20.5% persistence (15/73) and 8.2% replaced (6/73), and 66.7% eradication (54/81), 6.2% persistence (5/81) and 7.4% replaced (6/81), respectively (P = 0.048). The clinical efficacies were 76.7% (56/73) and 80.2% (65/81), respectively (P = 0.695). Adverse events due to faropenem were reported in 9.5% of participants (19/200), and the most common adverse event was diarrhoea. CONCLUSIONS: The 7 day regimen showed a superior rate of microbiological response. E. coli strains were in general susceptible to faropenem, including fluoroquinolone- and cephalosporin-resistant strains.

Pharmacokinetics of faropenem sodium for injection after a single and multiple intravenous dose in healthy volunteers / 中国药理学通报

Aim To study the pharmacokinetics of faropenem sodium for injection after a single and multiple intravenous dose in 12 healthy volunteers.Methods Multiple-dose regiments used 12-hour dosing intervals for 5 doses.Plasma and urine faropenem sodium concentrations were measured using high-performance liquid chromatography.The concentration-time curves of faropenem sodium were fitted to a two-compartment open model.The excretion data in urine were disposed by the method of excretion rate in urine.Results The pharmacokinetic parameters obtained from the single-dose study were as follows: C_(max) =(45.20±8.73) mg·L ~(-1); T_(1/2α) =(0.401±0.096) h; T_(1/2β) =(1.419±0.267) h;AUC_(0-12) =(59.216±11.886) mg·h·L~(-1) .The steady-state pharmacokinetic parameters were: C ss min =(0.03±0.02) mg·L~(-1) ; C ss max =(44.60±9.08) mg·L~(-1) ; C_(av)=(4.939±1.048) mg·L~(-1) ; T_(1/2α) =(0.340±0.105) h; T_(1/2β) =(1.257±0.173) h;AUC~(ss)_(0-12) =(59.268±12.571) mg·h·L~(-1) .The amount of cumulative recovery of faropenem sodium in urine for single and multiple dose within 12 h was(30.48±12.77)% and (40.55±17.53)%, respectively.The pharmacokinetic parameters in urine of the single-dose study were: T_(1/2) =(0.993±0.088) h, K_e=(0.227±0.097) h~(-1) .The steady-state pharmacokinetic parameters in urine were: T_(1/2) =(1.085±0.069) h, K_e=(0.296±0.136) h~(-1) .Conclusions The distribution and elimination rates of faropenem sodium for injection are not changed after multiple intravenous administrations.Effective concentrations in vivo can be achieved after the repeated administration with 400 mg twice a day regiment.The dosing schedule can be recommended.