Pharmacokinetic and clinical studies on cefuzonam in the pediatric field

A multi-center open study was conducted to investigate cefuzonam (L-105, CZON), a newly developed cephalosporin from pharmacokinetic, bacteriological and clinical aspects, in the pediatric field with the participation of 17 institutions and their related facilities. The results are summarized as follows. Serum concentrations and urinary excretion. The pharmacokinetics in pediatric patients was investigated with a dose of 20 mg/kg, via one shot intravenous injection or intravenous drip infusion over 1 hour. The results were nearly the same as those in adult patients. Mean serum concentrations 5 minutes after one shot intravenous injections were: 52.8 micrograms/ml with the dosage of 10 mg/kg, 135 micrograms/ml with 20 mg/kg, and 317 micrograms/ml with 40 mg/kg, and T1/2 beta's for the 3 dosages were 1.07 hours, 0.91 hour, and 1.01 hours, respectively. With 1-hour intravenous drip infusion, mean serum concentrations at the end of infusion were: 22.4 micrograms/ml with 10 mg/kg, 46.3 micrograms/ml with 20 mg/kg, 72.5 micrograms/ml with 40 mg/kg, and 69.2 micrograms/ml with 50 mg/kg, and T1/2 beta's for these dosages were 1.31 hours, 1.45 hours, 0.84 hour, and 0.66 hour, respectively. In 6 hours after administration of CZON, urinary excretion rates were 43.5-51.4% for one shot intravenous injections of 10-40 mg/kg, and 42.7-58.6% for 10-50 mg/kg drip infusions. Concentrations in cerebrospinal fluid Penetrations into cerebrospinal fluids in patients with purulent meningitis achieved levels of 2.80-6.40 micrograms/ml with the administration of CZON at 100 mg/kg in acute cases of within 6 days after onset. When the administration of the drug was done at the earlier stage, the greater penetration occurred. However, rates of penetration were 3.10% to 5.03% within 4 days after a drug administration, thus, the penetration was not thought to be as good as other beta-lactam agents which achieve higher penetration rates. Clinical results Of 407 cases treated with CZON, 18 cases were excluded from the statistical analysis. The remaining 389 cases plus 8 cases each of which had 2 complicated diseases, with a total of 397, were statistically analyzed for the clinical effectiveness of this drug against various infections. The efficacy was evaluated as "good" or "excellent" in 248 out of 266 cases from which pathogens were isolated, for an efficacy rate of 93.2%. The efficacy rate was 88.5% for 131 cases for which pathogens were unidentified, thus no statistically significant difference was noted between the 2 groups.(ABSTRACT TRUNCATED AT 400 WORDS)     

Clinical studies of cefuzonam in the pediatric field

Analysis on serum concentrations of cefuzonam (CZON, L-105) in 7 children who received different doses of CZON revealed a dose-response relationship. The half-life of the drug in blood was 0.90 hour. CZON was administered to 17 pediatric patients with bacterial infections. The clinical efficacy rate was 88% (15/17), and the eradication rate of pathogens was 80% (4/5). Only one case of mild diarrhea (1/17) was observed as a side effect associated with CZON.     

Laboratory and clinical studies of cefodizime in pediatric field

Clinical trials of cefodizime (CDZM, THR-221) were carried out in pediatric infection. Results are summarized as follows. 1. The mean half-life of CDZM in the serum following intravenous injection of CDZM (20 mg/kg) was about 2.06 hours. 2. The mean urinary excretion rate of CDZM within 8 hours after intravenous injection of CDZM was 60.1%. 3. CDZM was administrated to 19 pediatric patients with various infections; 9 cases of pneumonia, 3 bronchitis, 1 cervical lymphadenitis, 2 tonsillitis and 4 urinary tract infections. The overall efficacy rate was 94.7%. 4. No adverse reactions were observed. Abnormal laboratory test values found were thrombocytosis in 2, slight elevation of GOT and GPT in 1 and eosinophilia in 1 patient.     

Laboratory and clinical studies of sultamicillin in pediatric field

We have carried out laboratory and clinical studies on sultamicillin (SBTPC). The results are summarized as follows. SBTPC was given by oral administration to 2 children in a single dose at 5 mg/kg and to 3 children in a single dose at 10 mg/kg. After the oral administration, mean peak serum levels of ampicillin (ABPC) and sulbactam (SBT) obtained for the 2 dose levels were 1.91 +/- 1.34 and 2.06 +/- 1.06 micrograms/ml and 2.43 +/- 0.68 and 2.96 +/- 0.77 micrograms/ml at 1 hour, respectively, and mean half-lives were 0.80 +/- 0.10 and 0.98 +/- 0.46 hour and 1.57 +/- 0.57 and 2.01 +/- 0.70 hours, respectively. SBTPC was given to 2 children in a single dose at 15 mg/kg. After oral administration, the mean serum levels of ABPC and SBT at 30 minutes were 6.55 +/- 1.63 and 6.00 +/- 1.00 micrograms/ml, and the mean half-lives were 0.90 +/- 0.13 and 0.82 +/- 0.16 hour. SBTPC was given to 1 child at a single dose of 20 mg/kg. The peak serum levels of ABPC and SBT were 11.3 and 8.64 micrograms/ml, and the half-lives were 0.87 and 0.92 hour. Mean urinary excretion rates of ABPC and SBT were 38.4 +/- 2.7 and 34.6 +/- 4.7%, 43.0 +/- 3.6 and 41.6 +/- 5.8%, 47.7 +/- 5.2 and 51.6 +/- 3.5% in 6 hours and 66.1 and 59.2% in 8 hours after oral administration of 5 mg/kg, 10 mg/kg, 15 mg/kg and 20 mg/kg, respectively. Treatment with SBTPC was made in 34 cases of pediatric bacterial infections; 2 cases of pharyngitis, 19 cases of tonsillitis, 2 cases of bronchitis, 3 cases of impetigo, 2 cases of staphylococcal skalded skin syndrome, 4 cases of urinary tract infection and 1 case each of pneumonia and scarlet fever. Results obtained were excellent in 20 cases, good in 13 cases and poor in 1 case. No significant side effect due to the drug was observed in any cases.     

Laboratory and clinical studies of cefpirome in pediatric field

We have carried out laboratory and clinical studies on cefpirome (CPR, HR 810). The results are summarized as follows. CPR was given by 30-minute drip infusion to 3 children at a single dose of 20 mg/kg. After the 30-minute drip infusion, the mean peak serum level of CPR was 65.7 +/- 2.2 micrograms/ml at the end of infusion, and the mean half-life was 1.49 +/- 0.046 hours. The mean urinary excretion rate of CPR was 57.0 +/- 25.8% in the first 8 hours after the 30-minute drip infusion of 20 mg/kg. Treatment with CPR was made in 9 cases of pediatric bacterial infections; 1 case each of tonsillitis, pharyngitis, and bronchopneumonia, 4 cases of pneumonia, 2 cases of urinary tract infection. Results obtained were excellent in 6 cases, good in 3 cases. No significant side effects due to the drug were observed except one case of elevated GOT and GPT, and 3 cases of eosinophilia.     

Laboratory and clinical studies of cefodizime in pediatric field

We have carried our laboratory and clinical studies on cefodizime (CDZM, THR-221). The results were summarized as follows. CDZM was given by 30-minute drip infusion to 2 children at a single dose of 10 mg/kg and to 2 children at a single dose of 20 mg/kg and to 3 children at a single dose of 40 mg/kg. After the 30-minute drip infusion, mean serum levels of CDZM obtained for the 3 dose levels were 76.16 +/- 5.52 micrograms/ml, 170.49 +/- 16.70 micrograms/ml, 270.01 +/- 50.44 micrograms/ml at the end of injection, respectively, and serum half-lives were 2.03 +/- 0.78 hours, 2.03 +/- 0.38 hours, 2.28 +/- 0.30 hours, respectively. The mean urinary excretion rate of CDZM were 83.3 +/- 22.3%, 73.1 +/- 13.9%, 51.1 +/- 8.5% in the first 8 hours after the 30-minute drip infusion of 10 mg/kg, 20 mg/kg, 40 mg/kg, 40 mg/kg, respectively. Treatment with CDZM was made in 28 cases of pediatric bacterial infections; 5 cases of tonsillitis, 2 cases of bronchitis, 10 cases of pneumonia, 6 cases of enteritis, 3 cases of urinary tract infection and 1 case each of maxillary sinusitis and laryngitis. Results obtained were excellent in 13 cases, good in 7 cases, fair in 2 cases, poor in 6 cases. No significant side effect due to the drug was observed except one case of thrombocytosis and 2 cases each of elevated GOT and elevated GOT and GPT.     

Laboratory and clinical studies of norfloxacin in pediatric field

We have carried out laboratory and clinical studies on norfloxacin (NFLX, AM-715). The results are summarized as follows. NFLX was given through oral administration to one child each at dose levels of 1.7 mg/kg, 2.4 mg/kg and 3.2 mg/kg. After administration, peak serum levels of NFLX obtained for the 3 dose levels were 0.16 micrograms/ml at 1 hour, 0.69 micrograms/ml at 2 hours, 0.81 micrograms/ml at 1 hour, respectively, and half-lives were 2.5 hours, 1.8 hours and 2.7 hours, respectively. NFLX was given through oral administration to 2 children at a dose level of 4.4 mg/kg and to another child at a dose level of 4.8 mg/kg. After administration, mean peak serum levels of NFLX obtained were 1.17 +/- 0.48 micrograms/ml and half-lives were 3.0 +/- 0.5 hours. Urinary excretion rates of NFLX were 14.5% and 28.4% in the first 8 hours after administration of 1.7 mg/kg and 3.2 mg/kg, respectively, and 29.1% in the first 6 hours after administration of 2.4 mg/kg. Mean urinary excretion rates of NFLX were 38.5 +/- 13.0% in the first 8 hours after administration of 4.4 mg/kg and 4.8 mg/kg. Treatment with NFLX was made in 33 cases of pediatric bacterial infections including 5 cases of tonsillitis, 14 cases of enteritis, 10 cases of UTI and 1 case each of bronchitis, balanoposthitis, impetigo and pustulosis. Results obtained were excellent in 14 cases, good in 15 cases. No significant side effect due to the drug was observed in any cases.     

Laboratory and clinical studies on cefdinir in pediatric field

Clinical trials of cefdinir (CFDN) in pediatric infections were carried out. Results are summarized as follows. 1. Mean half-lives of CFDN in serum in children when administered on an empty stomach were 1.24 hours (3 mg/kg per os) and 1.85 hours (6 mg/kg per os). 2. Mean 8 hour urinary excretion rates of CFDN were 19.0% (3 mg/kg/per os) and 10.5% (6 mg/kg per os). 3. CFDN was administered to 28 children with various infections: 12 patients with tonsillitis, 8 with bronchitis, 2 with pneumonia, 4 with urinary tract infections, 1 staphylococcal scalded skin syndrome and 1 with impetigo. The overall efficacy rate was 89.3%. 4. Diarrhea was noted in 1 patient. Abnormal laboratory test values encountered were eosinophilia in 2 patients, thrombocytosis in 1.     

Laboratory and clinical studies of cefminox in the pediatric field

The authors have carried out the pharmacokinetic and clinical studies of cefminox (CMNX, MT-141). The results were as follows: CMNX was given by intravenous drip infusion for 1 hour at a dose of 20 mg/kg b.w. to 2 children. The serum levels of CMNX were 103.02 micrograms/ml and 77.73 micrograms/ml at 1 hour after drip infusion, and the levels at 7 hours were 4.39 micrograms/ml and 4.19 micrograms/ml, respectively. The half life times were 1.20 hours and 1.32 hours, respectively. CSF concentrations of CMNX at 1 hour after drip infusion of a dose of 50 mg/kg in 3 patients with aseptic meningitis were 1.68 micrograms/ml (d.i. for 30 minutes), less than or equal to 0.25 micrograms/ml (d.i. for 1 hour) and 0.51 micrograms/ml (d.i. for 1 hour), respectively. CSF/serum ratios were 1.1% and 0.6%. Clinical efficacy was evaluated in 10 cases with purulent tonsillitis (3 cases), pneumonia (3 cases), pyelonephritis (1 case) and enteritis (3 cases). Excellent and good responses were obtained in all cases. Bacteriological response in the form of eradication was noted 8 of 9 cases. No side effects were observed.     

Laboratory and clinical studies of cefmenoxime in the pediatric field

Laboratory and clinical studies were performed on cefmenoxime (CMX), a new cephalosporin antibiotic, and the following results were obtained. 1. Susceptibility of clinically isolated bacteria to CMX and cefotiam (CTM) or cefazolin (CEZ) Antimicrobial activity of CMX was compared with that of CTM and CEZ against S. aureus, S. epidermidis, S. pneumoniae, H. influenzae and E. coli. CEZ and CTM were more active than CMX against S. aureus, S. epidermidis and S. pneumoniae. But CMX was found to be more active by 1-10 tubes than CEZ and CTM against H. influenzae and E. coli. 2. Clinical efficacy. CMX was intravenously administered to 19 patients; 3 with lacunar tonsillitis, 2 with acute bronchitis, 8 with bronchopneumonia, 3 with UTI, 1 with septicemia, 1 with acute panperitonitis, 1 with S.S.S.S. at daily doses of 30-115 mg/kg (64.6 mg/kg on an average) t.i.d. or q.i.d. for 3-17 days (6.1 days on an average). The overall efficacy rate was 94.7%, i.e., efficacy was excellent in 10 cases (52.6%), good in 8 cases (42.1%), and poor in 1 case (5.3%). Bacteriological efficacy was good, i.e. 16 of the 19 strains disappeared. Transient eosinophilia was observed in 1 patient, but no other laboratory abnormality was observed during treatment. The above results suggest that CMX is 1 of the useful antibiotics in treatment of pediatric infections, especially due to Gram negative bacteria.     

Laboratory and clinical studies of flomoxef in the pediatric field

We have carried out laboratory and clinical studies on flomoxef (FMOX, 6315-S). The results were summarized as follows. FMOX was given by 5-minute intravenous administration to 3 children at a single dose of 20 mg/kg. After the intravenous administration, mean serum levels of FMOX were 110.1 +/- 30.95 micrograms/ml at the end of injection, 44.4 +/- 10.55 micrograms/ml at 15 minutes, 11.0 +/- 1.72 micrograms/ml at 1 hour and 0.42 +/- 0.17 microgram/ml at 6 hours. The mean half-life was 1.14 +/- 0.30 hours. The mean urinary excretion rate was 68.8 +/- 17.4% up to 6 hours after the intravenous administration. FMOX was given by 30-minute drip infusion to 2 children at a single dose of 20 mg/kg and to 3 children at a single dose of 40 mg/kg. After the 30-minute drip infusion, mean peak serum levels of FMOX obtained for the 2 dose levels were 45.5 +/- 0.45 micrograms/ml and 87.4 +/- 18.35 micrograms/ml at the end of injection, respectively, and mean half-lives were 0.63 +/- 0.23 hours and 0.70 +/- 0.27 hours, respectively. The mean urinary excretion rate was 53.4 +/- 6.1% up to 6 hours after the 30-minute drip infusion of 40 mg/kg FMOX. Treatment with FMOX was made in 24 cases of pediatric bacterial infections; 5 cases of purulent tonsillitis, 2 cases of bronchopneumonia, 12 cases of pneumonia, and 1 case each of lymphadenitis, pyothorax, purulent meningitis, cellulitis, and abscess. Results obtained were excellent in 15 cases and good in 9 cases. No significant side effect due to the drug was observed in any cases.     

Laboratory and clinical studies of aztreonam in the pediatric field

The authors have carried out the laboratory and clinical studies of aztreonam (AZT) and obtained the following results. The antibacterial activities of AZT against the clinical isolates of E. coli, K. pneumoniae and P. aeruginosa were measured by the agar dilution method with inoculum size of 10(6) cells/ml. The susceptibility distribution of E. coli to AZT ranged from 0.025 or lower to 1.56 microgram/ml, and the peak of distribution was 0.05 microgram/ml. The peak of susceptibility distribution of K. pneumoniae was 0.025 microgram/ml or lower, and the distribution of P. aeruginosa ranged from 0.1 to 100 micrograms/ml higher and the peak of distribution was 3.13 micrograms/ml. After intravenous bolus injection of 20 mg of AZT in 4 children, the mean peak serum level was 117 +/- 35.1 micrograms/ml at 15 minutes after injection, and half-life time was 1.42 hours. The mean urinary excretion rates was 63.2 +/- 30.6% up to 6 hours after bolus injection of 20 mg/kg of AZT. AZT was given 11 cases with bacterial injection. Daily doses of AZT were from 41.7 to 94.9 mg/kg. Clinical results obtained were excellent and good responses in 8 of 11 cases (72.7%). No side effect was observed.     

Laboratory and clinical studies of cefteram pivoxil in pediatric field

We have carried out laboratory and clinical studies on cefteram pivoxil (CFTM-PI, T-2588). The results are summarized as follows. CFTM-PI was given through oral administration to 2 children each at dose levels of 1.5 mg/kg, 3 mg/kg and 6 mg/kg. After administration, mean peak serum levels of CFTM obtained for the 3 dose levels were 0.66 +/- 0.01 microgram/ml, 1.26 +/- 1.05 micrograms/ml and 2.28 +/- 0.95 micrograms/ml at 2 hours, respectively, and mean half-lives were 1.07 +/- 0.52 hours, 1.32 +/- 0.76 hours and 2.53 +/- 1.70 hours, respectively. Mean urinary excretion rates of CFTM were 19.0 +/- 4.0%, 9.4 +/- 1.5% and 19.9 +/- 4.0% in the first 8 hours after administration of 1.5 mg/kg, 3 mg/kg, 6 mg/kg, respectively. Treatment with CFTM-PI was made in 36 cases of pediatric bacterial infections including 20 cases of tonsillitis, 3 cases of bronchitis, 6 cases of scarlet fever, 3 cases of UTI and 1 case each of bronchopneumonia, abscess, staphylococcal scalded skin syndrome and vaginitis. Results obtained were excellent in 22 cases, good in 14 cases. No significant side effect due to the drug was observed in any cases.     

Laboratory and clinical studies of cefpodoxime proxetil in pediatric field

We have carried out laboratory and clinical studies on cefpodoxime proxetil (CS-807, CPDX-PR). The results are summarized as follows. CPDX-PR was given via oral administration to each 2 children at a single dose of 3 mg/kg and to each of 3 children in a 100 mg tablet. After the oral administration, mean peak serum levels of CPDX obtained for the 2 dose levels were 1.86 +/- 0.35 micrograms/ml and 2.16 +/- 0.63 micrograms/ml at 2 hours, respectively, and mean half-lives were 1.31 +/- 0.02 hours and 1.47 +/- 0.18 hours, respectively. The mean urinary excretion rate of CPDX was 32.8 +/- 1.0% in the first 12 hours after the oral administration of 3 mg/kg. When a dose of 100 mg tablet was given to each of the 3 children, urinary excretion rates in the first 12 hours were 43.5%, 48.6% and 24.8%, respectively. Treatment with CPDX-PR was done in 38 cases of pediatric bacterial infections; 19 cases of tonsillitis, 3 cases of pharyngitis, 1 case of bronchitis, 3 cases of pneumonia, 3 cases of scarlet fever, 2 cases of impetigo, 4 cases of UTI and 1 case each of phlegmone, subcutaneous abscess and balanitis. Results obtained were excellent in 23 cases, good in 15 cases. No significant side effect due to the drug was observed in any cases.     

Laboratory and clinical studies of cefprozil in pediatric field]

Laboratory and clinical studies were done on cefprozil (CFPZ, BMY-28100). The results are summarized as follows. CFPZ was administered through the oral route to 2 children at a single dose of 7.5 mg/kg. After administration, peak serum levels of CFPZ obtained in the 2 cases were 6.71 micrograms/ml at 1 hour and 6.45 micrograms/ml at 2 hours, respectively and half-lives were 1.28 hours and 0.92 hour, respectively. The urinary excretion rates of CFPZ were 58.9% and 59.4%, respectively. Treatment with CFPZ was made in 37 cases of pediatric bacterial infections: 1 case of pharyngitis, 16 cases of tonsillitis, 16 cases of scarlet fever, 3 cases of impetigo, 1 case of UTI. Results obtained were excellent in 24 cases, good in 13 cases. No significant side effects due to the drug were observed, except 1 case of loose stool, 3 cases of eosinophilia, and 1 case each of elevated GOT and GPT.     

Laboratory and clinical studies of ceftazidime in the pediatric field

The authors have carried out the laboratory and clinical studies of ceftazidime ( CAZ ) and obtained the following results. The antibacterial activities of CAZ against the clinical isolates of S. aureus, E. coli, K. pneumoniae, E. cloacae, E. aerogenes, S. marcescens, C. freundii and P. aeruginosa were measured by the plate dilution method with inoculum size of 10(6) cells/ml. The susceptibility distribution of S. aureus to CAZ ranged from 3.13 to 100 micrograms/ml, and the peak of distribution was 12.5 micrograms/ml. The peak of susceptibility distribution of E. coli, K. pneumoniae and E. cloacae was 0.2 micrograms/ml, and the distribution of E. aerogenes ranged from 0.1 to 100 micrograms/ml and that of S. marcescens, from 0.05 to 3.13 micrograms /ml. The growth of 92% of P. aeruginosa was inhibited at the concentration of 3.13 micrograms/ml or lower. For pharmacokinetic study, CAZ was given in a single dose of 10 mg/kg by intravenous administration for 5 minutes in 1 child and by drip infusion for 30 minutes in 2 children. After intravenous administration of CAZ , the serum level got to the peak of 41.0 micrograms/ml at 15 minutes, and was 1.0 micrograms /ml at 6 hours. Half-life time was 1.30 hours. With drip infusion of CAZ , the mean peak serum level was 52.45 +/- 2.05 micrograms/ml on completion of the infusion, and 1.05 +/- 0.05 micrograms/ml at 6 hours. Half-life time was 1.30 hours. CAZ was effective in 9 cases out of 11 cases with bacterial infection. No side effect was observed except for elevation of serum GOT and GPT in 1 case and eosinophilia in 1 case.     

Laboratory and clinical studies on norfloxacin in the pediatric field

In bacteriological, pharmacokinetic and clinical studies on norfloxacin (NFLX, AM-715), the following results were obtained: 1. Antibacterial activity of NFLX, nalidixic acid (NA), amoxicillin (AMPC), cefaclor (CCL), erythromycin (EM) and fosfomycin (FOM) against clinically isolated bacteria was examined, and it was found that MIC80 of NFLX against Staphylococcus aureus was 3.13 micrograms/ml, thus NFLX exhibited stronger antimicrobial activity than NA, AMPC, CCL, EM and FOM. NFLX also showed good activities to those strains of S. aureus which were resistance to NA, AMPC, CCL, EM and FOM. 2. MIC80 of NFLX against Escherichia coli was 0.05 micrograms/ml or lower, thus NFLX showed better activity than NA, AMPC, CCL, EM and FOM. 3. In single oral administration at fasting of NFLX at dose levels of 1.5-2.4 and 2.5-3.4 mg/kg in tablet form mean peak values of serum concentration were 0.32 micrograms/ml reached in 1 hour and 0.38 micrograms/ml in 2 hours, T1/2's obtained were 1.7-4.0 and 2.2-2.9 hours and AUC's were 1.54 +/- 0.52 and 2.02 +/- 0.93 micrograms.hr/ml, respectively. Urinary recovery rates of 11.6-46.9%, 13.8-35.4% in 6-8 hours were demonstrated with the 2 ranges of dose levels, respectively. 4. NFLX was administrated to 34 patients consisting of 8 cases of acute pneumonia, 3 cases of acute tonsillitis, 3 cases of bacterial colitis, 19 cases of urinary tract infections and 1 case of purulent parotitis. The clinical efficacy rate was 97.1% including 34 cases with excellent results in 28, good in 5 and fair in 1. 5. The bacterial eradication rate was 96.8% (30/31) with one exception of a Campylobacter jejuni strain. 6. NFLX was given to patients according to a dosing regimen with 4.5-21.4 mg/kg/day dose levels for 3 doses daily except 1 case of UTI where 2 daily doses were given daily. 7. No adverse reactions were observed. Abnormal laboratory test value was obtained in 1 case where eosinophilia was found. The above results have suggested that NFLX is a useful and safe antimicrobial agent against bacterial infections in children.     

Laboratory and clinical studies on cefteram pivoxil in pediatric field

Pharmacokinetic and clinical studies of cefteram pivoxil (CFTM-PI, T-2588) fine granules in children were performed and the following results were obtained. 1. Peak serum concentrations in 4 children given orally a dose of 3 mg/kg and 2 children given orally a dose of 6 mg/kg after meal were reached in 3 to 4 hours and the concentration curves were dependent on dosage levels. The urinary recovery rates up to 8 hours were 29.7% in children given a dose of 3 mg/kg and 29.7% in children given a dose of 6 mg/kg. 2. Clinical efficacies were evaluated in 38 patients with bacterial infections. Twenty seven patients were given each doses of 3 mg/kg in 3 times a day and other 11 patients each doses of 6 mg/kg in 3 times. Clinical effects of CFTM-PI were excellent in 18, good in 19, fair in 1 case, hence the overall clinical efficacy rate was 97.4%. 3. Bacteriologically, 24 strains of causative organisms were isolated. The overall bacteriological eradication rate was 81.8%. Antimicrobial activities were excellent especially against Streptococcus pyogenes, Streptococcus pneumoniae, and Haemophilus influenzae. 4. As for the side effects, slight loose stools were observed in 2 cases, and in laboratory tests, elevations of GOT and GPT were observed in 1 case and an elevation of eosinophil was observed in 1 case. But no one needed any treatment. 5. CFTM-PI is a useful and safe oral antibiotic for the treatment of bacterial infections in pediatrics.     

Laboratory and clinical studies on cefodizime in the pediatric field

Laboratory and clinical studies on cefodizime (CDZM, THR-221), a newly developed cephem antibiotic, were done. The results obtained are summarized as follows: 1. Absorption and elimination were examined in a total of 5 cases including a case of 10 mg/kg intravenous drip infusion for 30 minutes, 2 cases of 20 mg/kg rapid intravenous injection and 2 cases of 40 mg/kg drip infusion for 30 minutes. Maximum serum levels were attained immediately after drip infusion or rapid injection. Cmax's were 119.2 micrograms/ml for 10 mg/kg, 374.9 micrograms/ml or 255.7 micrograms/ml for 20 mg/kg, and 321.3 micrograms/ml or 431.8 micrograms/ml for 40 mg/kg. These values were determined using an high performance liquid chromatography (HPLC) method. In general, values using the bioassay were higher than those with the HPLC method. T 1/2 (beta)'s were between 1.74 and 1.93 hours using HPLC, and between 1.77 and 2.24 hours using bioassay. Urinary recovery rates were examined in 3 out of 5 cases. Cumulative urinary recovery rates were 57.9-90.6% with HPLC method and 50.4-88.0% with bioassay in a period of 0-8 hours after administration. 2. Clinical efficacy was evaluated in a total of 22 cases including 14 cases of respiratory tract infections, 5 cases of urinary tract infections and 3 cases of cellulitis. Clinical efficacy rate was 95.2%. Bacteriologically, pathogenic organisms were eradicated in 90.0%. As adverse reactions, 1 angular stomatitis, 1 diarrhea and 1 loose stool were noted. Abnormal laboratory test values detected were 1 case of increased GPT and 1 case of increased GOT and GPT.     

Laboratory and clinical studies on cefminox in the pediatric field

Laboratory and clinical studies were performed as follows on cefminox (CMNX, MT-141), a new cephamycin antibiotic. Pharmacokinetics Serum concentrations of CMNX were measured in 4 patients given CMNX for prophylactic purpose during cardiac catheterization. In 2 patients given 20 mg/kg of CMNX by intravenous bolus injection, the average of peak serum concentration was 178.9 micrograms/ml at 15 minutes. The mean urinary recoveries in these 2 cases was 66.9% within 6 hours after injection. In 2 patients given 20 mg/kg of this drug by 1 hour drip infusion, the peak serum concentration was obtained at the time drip was completed, and the average value was 68.3 micrograms/ml. Clinical efficacy CMNX was administrated intravenously to 13 patients in dose of 52.9 approximately 96.0 mg/kg t.i.d. or q.i.d. for 4 approximately 7 days; 3 with tonsillitis, 6 with bronchitis, 1 with bronchopneumonia, 1 with UTI, 1 with lymphadenitis and 1 with enterocolitis. The overall efficacy rate was 92.3%, i.e., efficacy was excellent in 12, and poor in 1. Bacteriological efficacy was excellent, i.e., 3 of 3 strains disappeared. Side effects were observed in 3 cases, i.e., 1 case of eruption, 1 case of diarrhea and 1 case of transient eosinophilia. The above results suggest that CMNX is a useful antibiotic for treating pediatric bacterial infections.