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Azithromycin (AZM) was studied for its clinical efficacy in pediatric infections. The study on AZM was carried out in 43 patients whose diagnoses were given as follows: pharyngitis in five cases, tonsillitis in one, bronchitis in four, pneumonia in four, Mycoplasma pneumonia in 14, scarlet fever in nine, impetigo in four, pyodermia in one and Campylobacter enteritis in one. The patients received AZM once daily at 1.6 approximately 20.0 mg/kg body weight for three to five days. Effectiveness of AZM was evaluated in 39 cases and the drug was rated "excellent" in 15, "good" in 19, "fair" in one, "poor" in four, resulting in an efficacy rate of 87.2%. Twenty bacterial isolates were identified as causative isolates in 19 patients: Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae, Campylobacter jejuni and Mycoplasma pneumoniae. AZM eradicated 16 isolates but four persisted after therapy. One patient complained of loose stool, while two patients were found with decreases in white blood cell counts, and seven showed increases in eosinophils. However, no serious case of adverse event was reported.

Clinical studies were carried out on SY5555, a new oral penem, in the field of pediatrics. The results obtained are summarized below. The clinical efficacies were examined in a total 31 patients consisting of 4 patients with pharyngitis, 10 with purulent tonsillitis, 4 with scarlet fever, 7 with impetigo, one with balanitis, one with cellulitis and 4 with UTI. The clinical efficacy rate was 96.8% (30/31). Bacteriological efficacies of SY5555 were examined on identified pathogens including 7 strains of Staphylococcus aureus, 6 of Streptococcus pyogenes, 3 of Enterococcus faecalis, 3 of Haemophilus influenzae, one of Escherichia coli and one of Citrobacter freundii. The bacteriological eradication rate was 81.0%. As for side effects, loose stool in one patient was noted. Abnormal laboratory findings test results included eosinophilia in 2 patients, eosinophilia and elevation of serum transaminase in one patient, and thrombocytosis in another.

We carried out clinical studies on cefozopran (CZOP, SCE-2787). The results are summarized as follows. Treatment with CZOP was made in 17 cases of pediatric bacterial infections including 2 cases of purulent tonsillitis, 11 cases of acute pneumonia and 2 cases each of urinary tract infections and enteritis. Results obtained were excellent in 12 cases, good in 2 cases, fair in 2 cases and poor in 1 case. All of 9 isolated bacteria were eradicated by the treatment. As side effects and laboratory test results, rash was observed in one case and transient increase of platelets in one case, slight increase of eosinophil in 2 cases and transient elevation of GPT and GOT.GPT in one case.

We have carried out bacteriological and clinical studies on L-627. The results are summarized as follows. Treatment with L-627 was made in 14 cases of pediatric bacterial infections including 5 cases of pneumonia and 2 cases each of tonsillitis, urinary tract infection and one case each of colitis, and phlegmon. Results obtained were excellent in 11 cases, good in 2 cases and poor in one case. The bacteriological effect of L-627 was excellent, all causative organisms (Staphylococcus aureus one strain, Streptococcus pyogenes 2 strains, Streptococcus pneumoniae 3 strains, Escherichia coli 3 strains, Haemophilus influenzae one strain, Haemophilus parainfluenzae one strain) were eradicated. No significant side effects due to the drug were observed in any cases, except 2 cases each of elevated eosinophil counts and elevated platelet counts.

Nine pediatric patients with bacterial infections (5 cases of tonsillitis, 3 cases of impetigo and 1 case of UTI) were treated with S-1108, and the efficacy and the safety were evaluated. The clinical responses to S-1108 treatment were excellent in 7 cases and good in 2. The efficacy rate was 100%. Bacteriologically, the causative organisms (Streptococcus pyogenes, Staphylococcus aureus, Haemophilus parainfluenzae and Escherichia coli) were eradicated. No clinical side effects were observed. Elevation of CK in 2 cases and eosinophilia in 1 case were noted.

We have carried out clinical studies on cefditoren pivoxil (CDTR-PI, ME1207) in granules. The results are summarized as follows. Treatment with CDTR-PI was made for 14 cases of pediatric bacterial infections: 4 cases of tonsillitis, 2 cases of pneumonia, 3 cases of scarlet fever, 3 cases of impetigo, 1 case of subcutaneous abscess and 1 case of urinary tract infection. Results obtained were excellent in 12 cases, good in 1 case and poor in 1 case. No significant side effects due to the drug were observed.

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.

We have carried out clinical studies on meropenem (MEPM, SM-7338), the results are summarized as follows. Treatment with MEPM was made in 13 cases of pediatric bacterial infections including 9 cases of pneumonia and 2 cases of colitis and 1 case each of purulent tonsillitis, and pharyngitis. Results obtained were excellent in 10 cases, good in 3 cases. No significant side effects due to the drug were observed in any cases, except in 1 case each of eosinophilia, elevated gamma-GTP, elevated total bilirubin and elevated GPT.

We have carried out clinical studies on panipenem/betamipron (PAPM/BP, CS-976). The results are summarized as follows. Treatment with PAPM/BP was made in 21 cases of pediatric bacterial infections including 2 cases of tonsillitis, 15 cases of pneumonia and 1 case each of bronchitis, scarlet fever, urinary tract infection and otitis media. Results obtained were excellent in 15 cases, good in 6 cases. No significant side effects due to the drug were observed in any cases.

We have carried out laboratory and clinical studies on cefdinir (CFDN) 5% and 10% fine granule preparations. The results are summarized as follows. CFDN 5% fine granule preparation was given via oral route to each of 2 children in the fasting state at a single dose of 3 mg/kg. After administration, the mean peak plasma level of CFDN was 0.76 micrograms/ml at 4 hours and the mean half-life was 1.77 hours. The mean urinary excretion rate of CFDN was 31.5% in the first 12 hours after oral administration. CFDN 10% fine granule preparation and CFDN 100 mg capsule were given via oral route 3 children and to another child in the fasting state at single doses of 3 mg/kg and 2.63 mg/kg, respectively. After administration of 10% granules the mean peak plasma level of CFDN was 0.73 micrograms/ml at 2 hours and the mean half-life was 1.62 hours. The peak serum level obtained after administration of CFDN 100 mg capsule was 0.91 micrograms/ml at 2 hours and the half-life was 1.08 hours. The mean urinary excretion rate obtained with CFDN 10% fine granules was 26.2% in the first 8 hours after oral administration and the urinary excretion rate obtained with CFDN 100 mg capsule was 19.7% in the first 12 hours after oral administration. Treatment with CFDN 5% fine granules was made for a total of 48 cases of pediatric bacterial infections including 21 cases of tonsillitis, 12 cases of scarlet fever, 3 cases of pharyngitis, 5 cases of impetigo, 1 case of subcutaneous abscess, 1 case of furuncle, 5 cases of UTI. Results obtained were excellent in 30 cases, good in 18 cases. Treatment with CFDN 10% fine granules was made for a total of 16 cases of pediatric bacterial infections including 6 cases of tonsillitis, 3 cases of pneumonia, 4 cases of scarlet fever, 2 cases of impetigo, 1 case of UTI. Results obtained were excellent in 8 cases, good in 7 cases, poor in 1 case. No significant side effects due to the drugs were observed except 2 cases (1 case with 5% preparation and another with 10%) with eosinophilia, 3 cases (all with 5%) with diarrhea and 1 case each of elevated GOT & GPT (with 5%) and elevated GOT, GPT & Al-P (with 10%).

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.

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.

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.

The authors have carried out the laboratory and clinical studies of sulbactam/cefoperazone (SBT/CPZ) and obtained the following results. The antibacterial activities of SBT/CPZ against the clinical isolates of S. aureus, E. coli, K. pneumoniae, E. cloacae, E. aerogenes, S. marcescens, P. aeruginosa were measured by the plate dilution method with inoculum size of 10(6) cells/ml. The susceptibility distribution of S. aureus to SBT/CPZ ranged from 0.39 to 6.25 micrograms/ml, and the peak of distribution was 1.56 micrograms/ml. The peak of susceptibility distribution of K. pneumoniae was 0.20 microgram/ml, and the distribution of E. coli and E. aerogenes ranged from 0.10 to 12.5 micrograms/ml and that of S. marcescens, from 0.2 to 25 micrograms/ml. The growth of 80.8% of P. aeruginosa was inhibited at the concentration of 12.5 micrograms/ml. The distribution of E. cloacae ranged from 0.1 to 50 micrograms/ml. For pharmacokinetic study, SBT/CPZ was given in a single dose of 20 mg/kg by drip infusion for 1 hour in 2 children and 40 mg/kg by drip infusion for 1 hour in 1 children. With drip infusion of SBT/CPZ, the peak serum level were 17.8/43.9 micrograms/ml, 21.8/75.5 micrograms/ml on completion of the infusion, respectively. SBT/CPZ was effective in 14 cases out of 16 cases with clinical effect. No side effect was observed except for eosinophilia in 1 case.

Laboratory and clinical studies on imipenem/cilastatin sodium were carried out and the obtained results were summarized below. The antibacterial activity of imipenem against clinical isolates of S. aureus, E. coli, K. pneumoniae, Salmonella sp., S. marcescens and P. aeruginosa was measured by the plate dilution method with an inoculum size of 10(6) cells/ml. The growth of S. aureus was inhibited at an imipenem concentration of 0.025 microgram/ml or lower. The susceptibility distribution of E. coli to imipenem ranged from 0.1 to 1.56 micrograms/ml, and the peak of the distribution was at 0.1 microgram/ml. The peak of the susceptibility distribution of K. pneumoniae was 0.2 microgram/ml, and those of S. marcescens and Salmonella ranged from 0.2 to 1.56 micrograms/ml and from 0.1 to 0.39 microgram/ml, respectively. The growth of P. aeruginosa was inhibited at a concentration of imipenem at 6.25 micrograms/ml. For a pharmacokinetic study, imipenem/cilastatin sodium was given to 1 patient in a single dose of 10 mg/kg or 20 mg/kg by drip infusion over 1 hour. With drip infusion of imipenem/cilastatin sodium, the peak plasma levels obtained with the two doses (10 and 20 mg/kg) were 20.6/26.4 micrograms/ml and 19.4/36.5 micrograms/ml, respectively on completion of the infusion. Clinical responses to imipenem/cilastatin sodium were excellent in 6 patients and fairly good in 1 patient, and the clinical effectiveness ratio was 85.7%. No side effect was observed except for elevations of GOT and GPT in 1 patient.

The authors have carried out the laboratory and clinical studies of T-1982 (cefbuperazone). The results were as follows: The sensitivity was estimated by the plate dilution method on 28 strains of S. aureus 26 strains of E. coli, 27 strains of K. pneumoniae, 25 strains of S. marcescens and 14 strains of Proteus sp. isolated from patients. The distribution of susceptibility of S. aureus was 1.25-25 micrograms/ml and the peak of distribution was 12.5 micrograms/ml. The strains of 84.6% of E. coli were inhibited at concentration of less than 0.39 micrograms/ml. The strains of 77.8% of K. pneumoniae were inhibited at concentration of less than 0.2 microgram/ml. The strains of 96% of S. marcescens was inhibited at concentration of less than 3.13 micrograms/ml. The distribution of susceptibility of Proteus sp. was 0.39-25 micrograms/ml. T-1982 was given to intravenous administration for 5 minutes and drip infusion for 30 minutes a single dose of 20 mg/kg of T-1982 to 2 and 2 children respectively. After intravenous administration of T-1982, the mean serum level was peak 88.4 +/- 8.7 micrograms/ml at 15 minutes, 52.5 +/- 2.7 micrograms/ml at 1 hour, 4.6 +/- 0.15 micrograms/ml at 6 hours respectively. Half-life was 89 minutes. And after drip infusion of T-1982, the mean serum level was 75.5 +/- 3.5 micrograms/ml at 30 minutes and 3.1 +/- 0.6 micrograms/ml at 6.5 hours respectively. Half-life was 82 minutes. The mean urinary excretion rate was 94.7%, 57.4 +/- 11.0% up to 6 hours after intravenous administration and drip infusion respectively. T-1982 was effective in 13 cases out of 13 cases with bacterial infections. No side effects were observed except for 1 case with elevation of serum GOT, 1 case with elevation of serum GPT and 2 cases with eosinophilia.

Pharmacokinetic and clinical studies of cefixime (CFIX) in children were done and the following results were obtained. Serum and urinary concentrations of CFIX were determined in 6 children aged 5 to 14 years given single doses of 1.5 or 6.0 mg/kg. Mean serum concentrations peaked at 4 hours after the administration of either 1.5 or 6.0 mg/kg, and respective peak values were 0.71 and 4.46 micrograms/ml. Biological half-lives for the low and the high doses were 5.28 and 4.45 hours, respectively. The 12-hours urinary recovery ranged from 7.0 to 13.8% after administration of 1.5 mg/kg, and the 8-hours urinary recovery was 18.1% after administration of 6.0 mg/kg. Therapeutic responses were recorded as excellent or good in 43 (97.7%) of the children, comprising 13 with tonsillitis and 31 with scarlet fever. The microbiological effectiveness of CFIX on identified pathogens comprising 29 strains of S. pyogenes and 2 strains of S. aureus was satisfactory as evidence by a high eradication rate of 93.5%. No clinical side effects were observed. Abnormal laboratory findings were elevation of GOT and/or GPT in 4 patients and eosinophilia in 1 patient. In conclusion, CFIX was found to be efficacious and safe for the treatment of bacterial infections in children.

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.

Pharmacokinetic and clinical studies on ceftriaxone (CTRX) in mature and premature neonates were carried out. The results are summarized as follows. The mean serum peak level of CTRX after intravenous administration at a single dose of 10 mg/kg in 4 to 13 day-old-neonates was 34.1 +/- 11.4 micrograms/ml at 30 minutes. The mean serum level at 12 hours after dosage was 11.1 +/- 2.1 micrograms/ml. The mean half-life time was 11.6 +/- 1.4 hours. Mean serum peak levels of CTRX after intravenous administration at a single dose of 20 mg/kg were 64.6 +/- 15.4 micrograms/ml in 1 to 3 day-old-neonates, 44.6 +/- 1.1 micrograms/ml in 5 day-old-neonates at 30 minutes. Mean serum levels at 12 hours after dosage in these two groups of neonates were 16.4 +/- 4.8 micrograms/ml and 12.4 +/- 2.5 micrograms/ml, respectively. Mean half-life times were 13.7 +/- 3.7 hours in 1 to 3 day-old-neonates and 10.2 +/- 1.3 hours in 5 day-old-neonates. CTRX was clinically effective in a case of urinary tract infection. No side effect was observed except an elevation of GOT.

We have carried out laboratory and clinical studies on clarithromycin (TE-031, A-56268). The results are summarized as follows. Serum and urinary concentrations of TE-031 were determined in 5 children with ages between 6 and 11 years given single oral doses of 5, 6.7, 10 and 15 mg/kg. Serum concentrations peaked at 1 hour after administration of 5, 6.7 and 15 mg/kg, and respective peak values were 1.98 micrograms/ml, 2.21 micrograms/ml and 5.58 micrograms/ml. Biological half-lives for the drug at 5, 6.7 and 15 mg/kg dose were 2.99 hours, 2.08 hours and 2.09 hours, respectively. Mean serum concentrations peaked at 2 hours after administration of 10 mg/kg, and peak values were 3.91 +/- 1.64 micrograms/ml. Biological half-lives were 3.00 +/- 0.58 hours. The 6-hour urinary recovery rates ranged from 22.7% to 23.8% after administration of 10 mg/kg, and the 6-hour urinary recoveries were 30.1%, 20.5% and 39.1% after administration of 5 mg/kg, 6.7 mg/kg and 15 mg/kg, respectively. Therapeutic responses were recorded as excellent or good in 35(89.7%) of the children, comprising 5 with tonsillitis, 3 with pharyngitis, 7 with bronchitis, 5 with pneumonia, 15 with Mycoplasma pneumonia, 1 with whooping cough and 3 with Campylobacter enteritis. The microbiological effectiveness of TE-031 on identified pathogens comprising 2 strains of Streptococcus pneumoniae, 5 strains of Haemophilus influenzae, 2 strains of Haemophilus parainfluenzae, 5 strains of Mycoplasma pneumoniae and Campylobacter spp. was satisfactory as evidenced by an eradication rate of 82.4%. No significant side effect due to the drug was observed in any cases. In conclusion, TE-031 was found to be efficacious and safe for the treatment of bacterial infections in children.

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.

The authors have carried out laboratory and clinical studies on the BRL 25000 granule (containing 2 parts amoxicillin and 1 part clavulanic acid). The antibacterial activity of BRL 25000 against 29 clinically isolated strains of S. aureus, 30 E. coli and 30 K. pneumoniae were measured by the agar dilution method using an inoculum size of 10(6) cells/ml. beta-Lactamase production was detected by the Nitrocefin method. The MICs of BRL 25000 against S. aureus ranged from 0.2 approximately 12.5 micrograms/ml, with the majority of strains being inhibited by 1.56 micrograms/ml or less. Seven beta-lactamase producing strains of S. aureus were all inhibited by less than 12.5 micrograms/ml. The range against E. coli was 1.56 approximately 100 micrograms/ml, with the majority inhibited by 6.25 micrograms/ml or less. Fifteen beta-lactamase producing strains of E. coli were inhibited by 6.25 approximately 100 micrograms/ml and the majority by 25 micrograms/ml or less. All strains of K. pneumoniae were beta-lactamase producers and the MIC distribution against K. pneumoniae was 1.56 approximately 50 micrograms/ml, with a majority inhibited by 3.13 micrograms/ml or less, 96% of strains, were inhibited by less than 6.25 micrograms/ml. Against K. pneumoniae, BRL 25000 showed a 8 to 16-fold superiority when compared with AMPC. In a pharmacokinetic study, BRL 25000 granules were orally administered to children in the fasting state at single doses of 7.5 mg/kg and 20 mg/kg. The peak serum levels of AMPC were 6.13 and 6.94 micrograms/ml approximately 1 hour after administration and decreased with half-lives of 1.08 and 0.97 hours, respectively. The corresponding serum levels of CVA were 1.16 and 1.90 micrograms/ml at 1 hour after administration, with half-lives of 0.99 and 0.87 hour, respectively. In clinical studies, the BRL 25000 granule was effective in 39 cases of bacterial infection out of a total of 41 treated. Side effects were limited to 2 cases of diarrhea and minor changes in laboratory findings were elevation of serum GOT (1 case), elevation of serum GPT (1 case), and eosinophilia (2 cases).

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.

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.

We have carried out laboratory and clinical studies on sulbactam/ampicillin (SBT/ABPC). The results are summarized as follows. SBT/ABPC was given by 30-minute drip infusion to 1 child at a single dose of 15 mg/kg and to 2 children at a single dose of 30 mg/kg. After the 30-minute drip infusion, peak serum levels of ABPC(SBT) obtained for the 2 dose levels were 18.0 micrograms/ml (12.4 micrograms/ml) for the former dose level and 81.0 micrograms/ml (53.7 micrograms/ml) and 300 micrograms/ml (200 micrograms/ml) for the latter at the end of injection, and half-lives were 0.84 hour (0.82 hour) for the former and 0.96 hour (1.44 hours) and 0.93 hour (1.19 hours) for the latter. In another trial, SBT/ABPC was given to 1 child at a single dose of 60 mg/kg. After the 30-minute drip infusion, peak serum level of ABPC (SBT) was 82.3 micrograms/ml (45.9 micrograms/ml), and half-life was 1.20 hours (1.36 hours). The urinary excretion rates of ABPC (SBT) were 51.3% (49.5%), 55.8 +/- 10.4% (65.3 +/- 9.1%), 74.0% (76.1%) up to 6 hours after the 30-minute drip infusion of 15 mg/kg, 30 mg/kg and 60 mg/kg, respectively. Treatment with SBT/ABPC was made in 21 cases of pediatric bacterial infections: 8 cases of tonsillitis, 4 cases of bronchitis, 3 cases of pneumonia and 1 case each of pharyngitis, peritonsillar abscess, lymphadenitis, impetigo, abscess and urinary tract infection. Results obtained were excellent in 14 cases, good in 7 cases. No significant side effect due to the drug was observed in any cases except 1 case of fever and rash.

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.

The authors have carried out laboratory and clinical studies of 9,3"-diacetylmidecamycin (MOM) and obtained the following results. 1. Absorption and excretion of MOM. MOM was administered orally to 4 patients at a dose of 10 mg/kg in the fasting condition. The peak of serum levels was found at 30 minutes after administration. The mean values were 1.3 +/- 0.5 microgram/ml, and 1.1 +/- 0.9 microgram/ml after 30 minutes and 1 hour respectively. The serum levels were detectable in 2 cases after 2 hours (1.0 and 0.78 microgram/ml), in 1 case after 4 hours (0.78 microgram/ml) and were not detectable in all cases after 6 hours. Half-life was able to calculate in 2 cases (2.5 and 1.5 hours). The mean urinary recovery rate examined in 3 cases was 0.33% for initial 6 hours. 2. Clinical result. MOM was administered to 35 children at a daily dose of 16.7--51.1 mg/kg divided into 3 or 4 doses for 4 to 19 days: 18 cases with bacterial infection (9 cases with tonsillitis, 7 cases with scarlet fever and each 1 case with bronchitis and pneumonia) and 17 cases with Mycoplasma infection (5 cases with bronchitis and 12 cases with pneumonia). The overall clinical response was good in 28 cases (80.0%), fair in 6 cases and poor in 1 case. The efficacy rate in bacterial infections and Mycoplasma infections were 66.7 and 94.1% respectively. Eight strains of S. pyogenes and 1 strain of S. pneumoniae were isolated from 9 cases. One strain of S. pyrogenes was eradicated and the others were unchanged. The eradication rate was 11.1%. The MIC of MOM against S. pyogenes was above 50 micrograms/ml in 3 strains out of measured 5 isolated strains. 3. Side effect. Side effects were examined with all the 54 cases involving 19 drop-out cases. Although clinical side effects were not observed, a mild elevation in GOT and a mild rise in eosinophil were observed in 2 cases and 1 case respectively.

The authors have carried out the clinical and laboratory evaluation of aspoxicillin (ASPC, TA-058). The results were as follows: Antibacterial activities The susceptibility to ASPC was estimated by plate dilution method on 26 strains each of S. aureus, E. coli, Salmonella and P. aeruginosa and 19 strains of S. marcescens isolated from clinical specimens. Minimum inhibitory concentration (MIC) of ASPC against E. coli and Salmonella was about twice active to compare with ampicillin (ABPC), but MIC of ASPC against S. aureus was two-fold less active than that of ABPC. Antimicrobial activities of ASPC against S. marcescens were similar to that of ABPC, while against P. aeruginosa its activities were two-fold higher than that of carbenicillin. Serum levels and urinary excretions When ASPC was administered at 20 mg/kg by one shot intravenous injection, serum concentration was 75 micrograms/ml after 15 minutes and half-life (T 1/2 beta) was 1.65 hours. Urinary excretion within 6 hours after ASPC injection reached to 245.6 mg (26.1%). The reason of this law urinary excretion rate was due to the underlying disease (hydronephrosis). In case of 20 mg/kg administration of ASPC by intravenous drip infusion, peak serum level reached to 88 micrograms/ml at the end of injection, and half-life (T 1/2 beta) was 0.77 hour. Since ASPC degradation by beta-lactamase was proceeded, urinary excretion of this case was not measured by microbiological method. Penicillonic acid and its epimer were detected by HPLC method. It was found that beta-lactamase producing strain was S. marcescens which was isolated by urine culture.(ABSTRACT TRUNCATED AT 250 WORDS)

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.

The authors have carried out the laboratory and clinical studies of SM-4300 and obtained the following results. Serum level of IgG before and after administration of SM-4300 was observed in a case with agammaglobulinemia. The serum level reached the peak at 30 minutes after administration of SM-4300 and the half-life was about 25 days. SM-4300 enhanced the opsonic activity of human neutrophils to Pseudomonas aeruginosa in vitro. In substitution therapy against agammaglobulinemia, the clinical effect of SM-4300 was observed. Four patients with severe infections were treated with SM-4300 and antibiotics and evaluated. Clinical effects of SM-4300 in combination therapy with antibiotics were excellent in 2 cases, good in 1 case and poor in 1 case. The subjective and objective clinical side effects and abnormal laboratory findings were not noted.

The authors have carried out the laboratory and clinical studies of cefotetan (CTT), and obtained the following results. The antibacterial activities of CTT were measured by the plate dilution method against the clinical isolates of S. aureus, E. coli, K. pneumoniae, S. marcescens and Salmonella sp. The susceptibility distribution of S. aureus to CTT was at concentration of 6.25-12.5 micrograms/ml and the peak of that was obtained at 6.25 micrograms/ml with an inoculum size of 10(6) cells/ml. And the peaks of susceptibility distribution of E. coli and K. pneumoniae to CTT were obtained at less than 0.1 microgram/ml respectively, and that of S. marcescens was obtained at 6.25-12.5 micrograms/ml with an inoculum size of 10(6) cells/ml. The growth of all strains of Salmonella sp. was inhibited at concentration of less than 0.1 microgram/ml. As for pharmacokinetic study, CTT was given by intravenous bolus injection and drip infusion for 30 minutes at a single dose of 20 mg/kg. After intravenous bolus injection of 20 mg/kg of CTT, the mean peak serum level was 175.0 +/- 7.0 micrograms/ml at 15 minutes after injection, and half-life time was 3.53 hours. After 30 minutes drip infusion of 20 mg/kg of CTT, the mean serum concentration was 106.0 +/- 6.0 micrograms/ml at end of infusion, half-life time was 2.41 hours. The mean urinary excretion rates were 49.4% and 64.2% up to 8 hours after drip and bolus injection of 20 mg/kg of CTT, respectively. CTT was given 15 cases with bacterial infection. Daily doses of CTT were from 15.0 to 107.0 mg/kg. Clinical results obtained were excellent and good responses in 12 of 15 cases (80.0%). No side effects were obtained except for 2 cases with elevation of GOT and GPT, and 1 case with eosinophilia.

The authors have carried out the laboratory and clinical studies of ceftizoxime (CZX), and obtained the following results. 1. The antibacterial activities of CZX were measured by plate dilution method against clinical isolates of S. aureus, E. coli, K. pneumoniae and P. aeruginosa. CZX inhibited the growth of S. aureus at concentrations less than 12.5 micrograms/ml, and the peak of sensitivity distribution was obtained at 3.13 micrograms/ml with an inoculum size of 10(6) cells/ml. And the peak sensitivity distribution of E. coli and K. pneumoniae were obtained at less than 0.1 microgram/ml and that of P. aeruginosa was obtained at 6.25 micrograms/ml. 2. Phagocytosis was determined by Quie's method. Phagocytosis of E. coli and K. pneumoniae by human polymorphonuclear neutrophil was more enhanced in the presence of 1 MIC and 1/2 MIC of CZX than of CEZ at 4 and 6 hours after incubation. 3. As for pharmacokinetic study, CZX was given by intravenous injection and drip infusion for 1 hour at a single dose of 10 mg/kg and 30 mg/kg. After intravenous injection of 10 mg/kg and 30 mg/kg of CZX, the mean peak serum levels were 19.1 +/- 3.4 micrograms/ml and 69.1 micrograms/ml at 30 minutes, and half-life times were 1.20 hours and 1.35 hours, respectively. After 1 hour drip infusion of 10 mg/kg and 30 mg/kg of CZX, the mean peak serum levels were 28.8 +/- 3.6 micrograms/ml and 60.9 +/- 5.9 micrograms/ml at the end of infusion, and half-life times were 1.40 hours and 1.77 hours, respectively. The mean urinary excretion rates were between 75.3% and 101% up to 6 hours after intravenous injection and drip infusion. 4. CZX was given to 4 cases with tonsillitis, 3 with pneumonia, 1 with enteritis, 4 with U.T.I., totaling 21 cases. A daily dose of CZX between 350 mg and 2,000 mg was given for 3 to 5 days. Clinical results obtained were good in all cases. No side effects and abnormal laboratory findings were observed.

A bacteriological and clinical study of ceftizoxime suppositories (CZX-S) let to the following results. The CZX serum concentration 10 minutes after insertion of one 250 mg suppository (i.e. 5.7-15.2 mg CZX per kg body weight) ranged from 1.64 to 6.53 micrograms/ml (average: 4.41 micrograms/ml). In one child the concentration 7 minutes after insertion was 4.13 micrograms/ml. Therapeutic responsiveness was recorded as "effective" in 8 (88.9%) of the 9 children who were broken down into 6 with tonsillitis, 1 with pharyngitis, and 2 with UTI. Bacteriological studies conducted in 5 children have confirmed eradication in 4 children, one of whom showing appearance of another strain. The rate of discharge of the suppository within 10 minutes after insertion was 20.4%. Reddening and erosion of the anus were observed in 1 child.

We have carried out laboratory and clinical studies on rokitamycin (RKM, TMS-19-Q). The results are summarized as follows. Serum and urinary concentrations of RKM were determined in 6 children with ages between 6 and 12 years given single oral doses of 5, 10 and 15 mg/kg. Mean serum concentrations peaked at 30 minutes after administration of 5, 10 and 15 mg/kg, and respective peak values were 0.30 microgram/ml, 0.79 microgram/ml and 1.32 micrograms/ml. Biological half-lives for 5, 10 and 15 mg/kg were 2.0 hours, 1.65 hours and 1.36 hours. The 6-hour urinary recovery ranged from 1.11% to 2.58% after administration of 5 mg/kg, and the mean 6-hour urinary recoveries were 1.35% after administration of 10 mg/kg and 2.28% after administration of 15 mg/kg. Therapeutic responses were recorded as excellent or good in 22 (73.3%) of the children, comprising 6 with tonsillitis, 2 with pharyngitis, 4 with bronchitis, 1 with bronchopneumonia, 1 with Mycoplasma pneumonia, 2 with whooping cough, 5 with streptococcal infections, 5 with Campylobacter enteritis, 3 with impetigo and 1 with SSSS. The microbiological effectiveness of RKM on identified pathogens comprising 4 strains of Staphylococcus aureus, 1 strain of Streptococcus pneumoniae, 6 strains of Streptococcus pyogenes, 4 strains of Haemophilus influenzae and 5 strains of Campylobacter spp. was not so satisfactory as evidenced by a eradication rate of 50.0%. No significant side effect due to the drug was observed in any cases. In conclusion, RKM was found to be efficacious and safe for the treatment of bacterial infections in children.

The authors have carried out the laboratory and clinical studies of 6059-S. The results were as follows: The sensitivity was estimated by the plate dilution method on 27 strains of S. aureus, 26 strains of E. coli, K. pneumoniae and P. aeruginosa, 21 strains of Salmonella sp. and 9 strains of GM resistant P. aeruginosa isolated from patients. The distribution of sensitivity of S. aureus was 6.25-12.5 micrograms/ml and the peak of distribution was 6.25 micrograms/ml. The growth of 80.8% of E. coli was inhibited at concentration of less than 0.1 microgram/ml. The growth of 88.5% of K. pneumoniae was inhibited at concentration of less than 0.2 microgram/ml. The growth of 81.0% of Salmonella sp. was inhibited at concentration of less than 1.56 microgram/ml. The distribution of sensitivity of P. aeruginosa was 12.5- greater than 100 micrograms/ml and the peak of distribution was 25.0 micrograms/ml. The distribution of sensitivity of GM-resistance P. aeruginosa (greater than or equal to 25 micrograms/ml) was 12.5-50 microgram/ml and 5 of 8 strains were inhibited at concentration of less than 25 micrograms/ml. Phagocytosis was determined by Quie's method. Phagocytosis of E. coli, K. pneumoniae, Proteus vulgaris and Enterobacter cloacae by human polymorphonuclear neutrophil was more enhanced in the presence of 1 MIC and 1/2 MIC for 6059-S than for cefazolin at 4 and 6 hours after incubation. But phagocytosis of S. aureus did not enhanced in the presence of 6059-S. 6059-S was given by intravenous administration for 5 minutes and drip infusion for one hour at a single dose of 10 mg/kg of 6059-S to 3 and 4 children respectively. After intravenous administration of 6059-S, the mean peak serum level was 76.0 +/- 2.0 micrograms/ml at 15 minutes, 36.0 +/- 2.8 micrograms/ml at one hour, 1.5 +/- 0.4 micrograms/ml at 6 hours respectively. Half-life time was 1.3 hours. And after drip infusion of 6059-S was 39.9 +/- 9.7 micrograms/ml at one hour, 11.7 +/- 4.8 micrograms/ml at 3 hours and 1.8 +/- 1.4 micrograms/ml at 7 hours respectively. Half-life time was 1.4 hours. The mean urinary excretion rate was 90.4 +/- 6.1%, 76.5 +/- 16.0% up to 6 hours after intravenous administration and drip infusion respectively. 6059-S was effective in 17 cases out of 18 cases with bacterial infections. No side effects were observed except for 4 cases with elevation of serum transaminase, each on case of eosinophilia and of anemia.

The authors have carried out the laboratory and clinical studies of ceftriaxone (Ro 13-9904, CTRX) and obtained the following results. The antibacterial activities of CTRX against the clinical isolates of S. aureus, E. coli, K. pneumoniae, E. cloacae, E. aerogenes, S. marcescens, Citrobacter sp. and P. aeruginosa were measured by the agar dilution method with inoculum size of 10(6) cells/ml. The susceptibility distribution of S. aureus to CTRX ranged from 0.2 to 12.5 micrograms/ml, and the peak of distribution was 3.13 micrograms/ml. The peak of susceptibility distribution of E. coli and K. pneumoniae were 0.1 microgram/ml or lower, and the distribution of E. aerogenes and E. cloacae ranged from 0.1 to 100 micrograms/ml, Citrobacter sp. and S. marcescens, from 0.1 to 12.5 micrograms/ml and that of P. aeruginosa, from 0.39 to 100 micrograms/ml or more. For pharmacokinetic study, CTRX was given in a single dose of 10 mg/kg in 1 child and 20 mg/kg in 2 children by drip infusion for 1 hour. After drip infusion of CTRX in a single dose of 10 mg/kg, the peak serum level was 61.4 micrograms/ml on completion of the infusion, and 8.43 micrograms/ml at 12 hours. Half-life time was 4.6 hours. With drip infusion of CTRX in a single dose of 20 mg/kg, the peak serum level was 105.5 micrograms/ml on completion of the infusion, and 19.1 micrograms/ml at 12 hours. Half-life time was 8.7 hours. CTRX was effective all cases out of 8 cases with bacterial infection. No side effect was observed except for elevation of serum GOT in 2 cases and eosinophilia in 1 case.

The authors have carried out the laboratory and clinical studies of cefpiramide (CPM). The results were as follows; The sensitivity was estimated by plate dilution method on 27 strains of S. aureus and P. aeruginosa, 26 strains of E. coli, 25 strains of K. pneumoniae and 13 strains of Proteus sp. isolated from patients. The distribution of S. aureus was 0.78 approximately 6.25 micrograms/ml and the peak of distribution was 1.56 micrograms/ml. The distribution of E. coli was 0.78 approximately 50 micrograms/ml and the peak of distribution was 0.78 and 25 micrograms/ml. The growth of 24% of K. pneumoniae was not inhibited at concentration of more than 50 micrograms/ml. The distribution of Proteus sp. was 6.25 approximately 100 micrograms/ml. The growth of 77.8% of P. aeruginosa was inhibited at concentration of less than 3.13 micrograms/ml. CPM was given by intravenous administration for 5 minutes and drip infusion for 30 minutes at a single dose of 20 mg/kg of CPM to each 2 children respectively. After intravenous administration of CPM, the mean peak serum level was 200.5 +/- 37.5 micrograms/ml at 15 minutes, 44.3 +/- 0.9 micrograms/ml at 6 hours, 19.9 +/- 0.3 micrograms/ml at 12 hours respectively. Half-life time was 4.2 hours. After drip infusion of CPM, the mean peak serum level was 150.5 +/- 14.5 micrograms/ml at end of infusion, 23.6 +/- 3.3 micrograms/ml at 6 hours and 8.2 +/- 2.0 micrograms/ml at 12 hours respectively. Half-life time was 3.8 hours. The mean urinary excretion rate was 23.15%, 28.2% up to 12 hours after intravenous administration and drip infusion respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

We have carried out laboratory and clinical studies of cefuzonam. The results were summarized as follows: The effectiveness of cefuzonam was estimated by a plate dilution method on 26 strains each of S. aureus, E. coli, K. pneumoniae, Salmonella spp. and P. aeruginosa and 27 strains of S. marcescens isolated from patients. The distribution of MIC's of cefuzonam against S. aureus was 0.39 approximately 1.56 micrograms/ml and the peak of the distribution was 0.39 microgram/ml. Strains of 96.2% of E. coli and Salmonella spp. were inhibited at cefuzonam concentrations less than 0.39 microgram/ml. Strains of 92.3% of K. pneumoniae were inhibited at drug concentrations less than 0.20 microgram/ml. The distribution of MIC's of cefuzonam against S. marcescens was less than or equal to 0.025 approximately 12.5 micrograms/ml and the peak of the distribution was 0.2 microgram/ml and 1.56 microgram/ml. MIC's against P. aeruginosa was 12.5 approximately greater than 100 micrograms/ml. Cefuzonam was given by 5-minute intravenous administration to 4 children and 1-hour drip infusion to 1 child at a single dose of 20 mg/kg. After the intravenous administration, mean serum levels of cefuzonam were 30.8 +/- 4.55 microgram/ml at 30 minutes, 13.8 +/- 1.83 micrograms/ml at 1 hour, 0.4 +/- 0.159 microgram/ml at 6 hours. The half-life was 1.12 +/- 0.198 hours. After the drip infusion, the serum levels of the drug were 38.7 micrograms/ml at 1 hour, 5.25 micrograms/ml at 2 hours and 0.087 microgram/ml at 7 hours. The half-life was 0.93 hour. The mean urinary excretion rate was 58.1% and 33.4% up to 6 hours after the intravenous administration and the drip infusion, respectively. Cefuzoname was effective in 4 out of 5 cases with bacterial infections. No side effect due to the drug was observed in any case.

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.