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Laboratory and clinical studies were performed as follows on aztreonam (AZT), a new monobactam antibiotic. Pharmacokinetics Serum concentrations of AZT were measured in 1 patient given 20 mg/kg by intravenous bolus injection. The peak concentration was 100 micrograms/ml at 15 minutes, and T 1/2 was 1.85 hours. Clinical efficacy AZT was administrated intravenously to 10 patients in doses of 59.2-170.7 mg/kg (average 76.1 mg/kg) t.i.d. for 3-8 days (average 5.3 days); 5 with pneumonia, 1 with bronchitis, 1 with lymphadenitis, 1 with sepsis (suspected) and 2 with urinary tract infections. The overall efficacy rate was 80%, i.e., efficacy was excellent in 5, good in 3, fair in 1 and poor in 1. Bacteriological efficacy was excellent, i.e., 4 of 4 Gram-negative strains disappeared. Any clinical side effects and laboratory abnormalities were not observed. The above results suggest that AZT is a useful antibiotic for treating pediatric bacterial infections, especially due to Gram-negative bacteria.
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PMID:[Laboratory and clinical studies on aztreonam in the pediatric field]. 409 67

Fundamental and clinical studies in the pediatric field on ceftizoxime were carried out, and the following results were obtained. 1. In 4 children age from 3 years to 5 years, the serum concentrations and urinary excretion of ceftizoxime in a dose of 20 mg/kg by intravenous drip infusion over 60 minutes were measured. The peak serum levels were 22.0--84.0 microgram/ml (mean 45.0 microgram/ml) at the end of infusion. The mean serum levels after the end of infusion were 16.9 microgram/ml at 30 minutes, 12.1 microgram/ml at 1 hour, 6.2 microgram/ml at 2 hours, 1.6 microgram/ml at 4 hours and 0.6 microgram/ml at 6 hours, with mean serum half-life (T 1/2) of 1.03 hours, mean urinary recovery rate was 64.9% up to 6 hours. 2. Concentrations of the drug in the cerebrospinal fluid in 1 patient with purulent meningitis at 30 minutes after an intravenous drip infusion of about 33.3 mg/kg were 0.2 to 1.5 microgram/ml, which were 8 to 60 times higher than the MICs of the causative organisms. 3. Ceftizoxime was administered to 38 children with pneumonia, bronchitis, Salmonella enteritis, purulent meningitis, etc. in the daily dose of 44--200 mg/kg for 3--19 days. Clinical response was excellent in 24, good in 12, poor in 1 and unknown in 1. The drug was proved to be very effective in 1 case of purulent meningitis due to H. influenzae. As for side effect, eruption was observed in only 1 case.
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PMID:[Fundamental and clinical studies in pediatric field on ceftizoxime (author's transl)]. 627 12

Ceftizoxime, a new cephalosporin preparation, was evaluated for its antibacterial activity, absorption, excretion and clinical effectiveness, and the following results were obtained. The minimum inhibitory concentrations (MICs) of ceftizoxime against 211 clinical isolates were determined in comparison with those of cefazolin, cefmetazole, cefotiam and 6059 S. Against S. pyogenes (50 strains), ceftizoxime was 1 tube inferior to cefazolin inoculum size of 10(8) cells/ml, but was 2--3 tubes superior to cefmetazole and 6059-S. Against E. coli (50 strains), ceftizoxime and 6059-S were significantly more active than the other drugs. The susceptibility pattern of Klebsiella sp. (50 strains) to ceftizoxime was similar to that to cefotiam and 6059-S. Against Proteus sp. (50 strains), cefotiam and 6059-S were more active than the other drugs. Ceftizoxime was intermediate in activity, and cefazolin was the least active. Against H. influenzae (11 strains), ceftizoxime was the most active, with concentrations of 0.1 mcg/ml required to inhibit 100% of strains with an inoculum size of 10(8) cells/ml and 10(6) cells/ml. A dose of ceftizoxime 10 mg/kg or 20 mg/kg was administered to 15 patients aged from 5 years to 12 years, and serum levels and urinary excretion of the drug were measured. Intravenous bolus injection of the drug in dose of 10 mg/kg and 20 mg/kg yielded mean serum levels of 26.6 mcg/ml and 55.7 mcg/ml at 30 minutes, respectively. The serum levels of the drug, thereafter, declined gradually but still remained 1.3 mcg/ml and 2.7 mcg/ml at 6 hours. The serum half-lives (T 1/2) were estimated to be 1.17 hours in dose of 10 mg/kg and 1.31 hours in dose of 20 mg/kg. When a dose of 20 mg/kg was infused over a period of 30 minutes, the serum levels attained the peak of 72.4 mcg/ml to 82.4 mcg/ml (mean 79.4 mcg/ml) at the end of infusion. The levels, thereafter, tapered to mean levels of 45.3 mcg/ml at 30 minutes, 24.7 mcg/ml at 1 1/2 hours, and 3.6 mcg/ml at 5 1/2 hours, with a T 1/2 of 1.22 hours. Meanwhile, when the same dose was infused over 1 hour, the serum levels attained the peak of 59.4 mcg/ml to 68.5 mcg/ml (mean 64.2 mcg/ml). The mean serum levels after the end of infusion were 41.3 mcg/ml at 30 minutes, 21.6 mcg/ml at 1 hour and 1.9 mcg/ml at 5 hours, with a T 1/2 of 0.97 hours. Urinary recovery of the drug was 69.2% to 79.9% after intravenous injection and 62.3% to 79.9% after drip infusion, most of the given drug was excreted in the first 2 hours after administration. In our clinical study, 27 children with moderate or severe infections (12 cases of bronchopneumonia or bronchitis, 5 of pyelonephritis, 3 of purulent meningitis, etc.) were treated with ceftizoxime at the daily dose of 30--309 mg/kg for 3--23 days. Clinical response was excellent in 10, good in 9, fair in 5 and poor in 3. The drug was proved to be very effective against infections due to H. influenzae K. pneumoniae, E. coli and S. aureus. No serious side effects were observed in any case.
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PMID:[Laboratory and clinical studies on ceftizoxime in the field of pediatrics (author's transl)]. 627 16

Studies on T-1982 (cefbuperazone), a new cephamycin antibiotic, were carried out in the field of pediatrics, and the following results were obtained. 1. Peak MIC of T-1982 against S. pyogenes (group A) lately isolated was 0.39 micrograms/ml, and the drug was active even against highly resistant strains of macrolides, lincomycin, tetracycline and chloramphenicol. 2. Peak MICs of T-1982 were 0.78 microgram/ml against B. pertussis, 0.2 microgram/ml against E. coli and less than or equal to 0.05 microgram/ml against K. oxytoca, and the drug was also active against ampicillin-resistant bacteria. 3. Serum levels and urinary excretions of T-1982 were investigated in 6 cases. When given at a dose of 20-28 mg/kg by 1 hour intravenous drip infusion, serum concentrations of T-1982 attained the peak level of 63.5-75.9 micrograms/ml at the end of administration and sustained the level of 0.9-2.6 micrograms/ml at 6 hours, the serum half-life (T 1/2) ranging 70-82 minutes. Approximately 20-72% of the dose were excreted in the active form into urine within 6 hours. 4. Twenty-seven cases of acute pediatric infections were treated with T-1982 mainly by intravenous drip infusion, and satisfactory clinical results were obtained in all the cases of angina lacunaris, bronchitis, bronchopneumonia, pertussis, sepsis caused by Serratia and acute urinary tract infections caused by ampicillin-resistant E. coli. The efficacy rate was 96.3%. In this study the drug was administered chiefly at a daily dose of 50-70 mg/kg 2-3 times a day for 2-12 days. 5. Gram-positive cocci (S. aureus, S. pneumoniae, S. pyogenes) and Gram-negative rods (H. influenzae, H. parainfluenzae P. vulgaris, B. pertussis, S. marcescens, E. coli) were eradicated by the treatment with T-1982. 6. No noticeable side effects were observed, except for temporary increase of eosinophil in 2 cases and slight elevation of GOT in 1 case.
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PMID:[Fundamental and clinical studies on T-1982 (cefbuperzone), a new cephamycin antibiotic, in the field of pediatrics]. 630 96

Ceftazidime ( CAZ ), a new injectable cephem antibiotic, was used for treatment of infections in children, and the following results were obtained. After an intravenous injection of CAZ at a dose of 20 mg/kg, the mean blood levels in 2 patients were 41.5 micrograms/ml at 30 minutes, 18.1 micrograms/ml at 2 hours and 2.55 micrograms/ml at 6 hours, with the half-life (T 1/2) of 1.37 hours. In a 22-day-old baby with meningitis given CAZ intravenously at a dose of 43.5 mg/kg, the blood levels were 100 micrograms/ml at 30 minutes, 68 micrograms/ml at 2 hours and 25 micrograms/ml at 6 hours, with the half-life (T 1/2) of 2.96 hours. After intravenous administration of CAZ in doses ranging from 35.7 to 50 mg/kg, CSF concentrations ranged from N.D. to 6.3 micrograms/ml in 3 patients with purulent meningitis, although 19 micrograms/ml at 1 hour and 13 micrograms/ml at 2 hours in 1 patient after intravenous administration of 46.7 mg/kg. In patient with mumps meningitis, CSF concentrations were undetectable after intravenous administration of 35.7 mg/kg. Seventeen patients (each 1 patient with lymphadenitis, tonsillitis and septicemia, each 2 patients with pneumonia, bronchiectatic bronchitis, pyothorax and purulent meningitis, each 3 patients with pyelonephritis and enteritis) were treated with CAZ intravenously, at the daily doses of 178.2 mg/kg and 200 mg/kg in 4 divided doses in patients with meningitis and 44.1 to 103.4 mg/kg in 3 divided doses in patients with other infections (two of them were given by intravenous drip infusion for 30 minutes). The clinical responses were excellent or good in all the patients except for 1 case of Salmonella enteritis (poor) and 1 case of Campylobacter enteritis (poor). The efficacy rate was 88.2%. It was noteworthy that the clinical response was excellent in 1 case of septicemia with P. aeruginosa with leukemic stage of malignant lymphoma and in 2 cases of purulent meningitis. As side effects, fever, eruption, leukocytopenia, elevation in GOT and positive CRP considered to be allergic, were observed on day 16 of administration in 1 case of pyothorax. These symptoms disappeared by discontinuance of administration. In addition, there were elevation in GOT and GPT in 2 cases and elevation in GOT in 2 cases and elevation in GPT in 1 case; they were all mild or transient, and there was nothing to be worried about.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Clinical evaluation of ceftazidime in paediatrics]. 637 60

Laboratory and clinical studies were performed on 6059-S in the field of pediatrics, a new semi-synthetic 1-oxacephem antibiotic, and results were as follows. 1. MICs of 6059-S were compared with those of cefazolin (CEZ) and cefmetazole (CMZ) on 31 strains of S. aureus, 29 strains of E. coli, 30 strains of K. pneumoniae and 16 strains of P. aeruginosa. With the inoculum size of 10(8) cells/ml an 10(6) cells/ml, the peak of distribution of MICs were S. aureus 6.25, 3.13 micrograms/ml, E. coli 0.2, 0.1 micrograms/ml, K. pneumoniae 0.2, 0.05 micrograms/ml and P. aeruginosa 12.5, 6.25 micrograms/ml, respectively. MICs 6059-S against S. aureus was more less 2 to 3 tubes than CEZ and CMZ, but against E. coli and K. pneunoniae were more higher than 3 to 4 tubes than CEZ and CMZ. 2. The serum concentrations and urinary recovery rate of 6059-S were measured in 5 pediatric patients. 6059-S was given 20 mg/kg by an intravenous injection to 2 cases or a 30 minutes intravenous drip infusion to 3 cases. The mean concentration of the former were 64.3, 44.3, 26.8, 11.7 and 5.0 micrograms/ml at 0.5, 1, 2, 4 and 6 hours, and T 1/2 was 1.51 hours. The urinary recovery rates was 75.0% within 6 hours after the injections. The mean concentration of the latter were 65.3, 86.3, 63.0, 40.3, 17.8 and 8.9 micrograms/ml at 0.25, 0.5, 1, 2, 4 and 6 hours, and T 1/2 was 1.63 hours. The urinary recovery rates was 52.1% within 6 hours after the injection. 3. Eleven cases with acute pneumonia, 1 case with acute bronchitis, 3 cases with acute purulent tonsillitis, 1 case with acute purulent parotitis and 1 case subcutaneous abscess were treated with 6059-S by intravenous injection. All cases were above effective clinically. Five strains of H. influenzae, 3 strains of S. pneumoniae, 2 strains of S. pyogenes and 1 strain of S. aureus were eradicated in all strains. No clinical adverse reaction and abnormal laboratory findings were noted.
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PMID:[Laboratory and clinical studies on 6059-S in children (author's transl)]. 645 76

Laboratory and clinical investigations were performed in the field of pediatrics with cefadroxil dry syrup, a new semi-synthetic cephalosporin antibiotic. (1) MIC of cefadroxil was measured, to compare with that of cephalexin (CEX), on 30 strains of S. aureus, 30 strains of S. pyogenes and 26 strains of E. coli, all of which were isolated clinically in the field of pediatrics. Two strains of S. aureus showed more than 100 microgram/ml with inoculum size of 10(8) cells/ml, and remaining 28 strains were distributed between 1.56 similar to or approximately 12.5 microgram/ml, while at inoculum size of 10(6) cells/ml, each 1 strain showed 25 microgram/ml and 50 microgram/ml, and the remaining strains were distributed between 1.56 similar to or approximately 3.13 microgram/ml. All 30 strains of S. pyogenes were inhibited the growth by less than 0.2 microgram/ml with inoculum size of both 10(8) cells/ml and 10(6) cells/ml. Three strains of E. coli showed MIC of more than 100 microgram/ml with inoculum size of 10(8) cells/ml, and the remaining 23 strains were distributed between 12.5 similar to or approximately 25 microgram/ml, while with inoculum size of 10(6) cells/ml, 3 strains showed more than 100 microgram/ml, and the remaining strains were distributed between 6.25 similar to or approximately 12.5 microgram/ml. In comparison with the results of CEX, cefadroxil was nearly equal to S. aureus and E. coli, whereas it was 2 grades superior to S. pyogenes. (2) A dose of 10 mg/kg of cefadroxil dry syrup was administered before 30 minutes of breakfast in 3 cases of children, and serum level, urinary level and recovery rate in urine were investigated. Average serum level was 15.2 +/- 2.39 microgram/ml in 1/2 hour, 16.4 +/- 2.3 microgram/ml in 1 hours. 10.1 +/- 2.8 microgram/ml in 2 hours, 3.8 +/- 1.5 microgram/ml in 4 hours and 1.0 +/- 0.4 microgram/ml in 6 hours, and average T 1/2 was 1.24 +/- 0.22 hours. Average urinary level was 857 +/0 232 microgram/ml in 0 similar to or approximately 2 hours, 690 +/- 180 microgram/ml in 2 similar to or approximately 4 hours and 249 +/- 55 microgram/ml in 4 similar to or approximately 6 hours, and average recovery ratio in urine was 86.3 +/- 17.5% within 0 similar to or approximately 6 hours. (3) Cefadroxil dry syrup was administered clinically in 20 cases of acute purulent tonsillitis, 5 cases of acute bronchitis, 14 cases of acute pharyngitis, 5 cases of acute purulent cervical lymphadenitis and 2 cases of acute urinary tract infection. Clinical efficacy, bacteriological effect and its side effect were investigated in total 46 cases of bacterial infection. A dose of 21.1 similar to or approximately 57.1 mg/kg of cefadroxil was administered daily, divided into 3, after each meal for 1 similar to or approximately 10 days, total dose being 0.5 similar to or approximately 11.0 g. Efficacy rate of cefadroxil, including excellent and effective effects, was 90.0% in acute purulent tonsillitis, 60.0% in acute bronchitis, 100.0% in acute pharyngitis, 80...
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PMID:[Laboratory and clinical studies on cefadroxil in the field of pediatrics (author's transl)]. 724 9

Bacteriological, pharmacokinetic and clinical studies on cefditoren pivoxil (CDTR-PI, ME 1207) in granules, a new oral cephalosporin, were performed in the field of pediatrics. The results are summarized below. 1. Antibacterial activities: Antibacterial activities of CDTR were studied against Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae, Haemophilus parainfluenzae and Branhamella catarrhalis in comparison with those of cefteram (CFTM), cefixime (CFIX), cefaclor (CCL), cefpodoxime (CPDX) and cefotiam (CTM). MIC80's of CDTR against S. aureus, S. pneumoniae, S. pyogenes, H. influenzae, H. parainfluenzae and B. catarrhalis were 1.56, 0.39, < or = 0.025, < or = 0.025, 0.05 and 0.20 micrograms/ml, respectively. These results showed that CDTR has high antibacterial activities against these organisms. 2. Absorption and excretion: Serum concentrations and urinary recovery rates of CDTR-PI (administered in granules) were determined. Upon single oral doses of 3 mg/kg and 6 mg/kg, the peak serum concentrations were 0.5-2.45 micrograms/ml at 2 to 4 hours and 1.79-4.05 micrograms/ml at 1 to 4 hours, respectively, and T 1/2 was 1.07-9.67 hours and 0.99-3.00 hours, respectively. At 8 hours after dosing, serum concentrations were 0-0.87 micrograms/ml with a dose of 3 mg/kg and 0.27-0.73 micrograms/ml with 6 mg/kg. These values indicated that the drug has a dose-dependent pharmacokinetic behavior. Urinary recovery rates in the first 8 hours were 12.9-34.2% with a dose of 3 mg/kg and 11.8-26.9% with 6 mg/kg. 3. Clinical study: Clinical efficacies were examined in a total of 81 cases consisting of 20 cases of acute bronchitis, 13 of acute pneumonia, 21 of tonsillitis, 5 of pharyngitis, 7 of scarlet fever, 2 each of impetigo, otitis media and purulent cervical lymphadenitis, 1 of pertussis and 8 of UTI. The clinical efficacy rate was 97.5% (79/81), and bacteriological eradication rate was 100% (76/76). As for side effects, 2 cases of watery stools and 1 case of minor elevation of GPT were observed.
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PMID:[Bacteriological, pharmacokinetic and clinical studies of cefditoren pivoxil in the pediatric field]. 837 96

Azithromycin (AZM) preparations in fine granules and capsules were evaluated in 36 pediatric patients with various infections. In patients with pneumonia caused by Moraxella catarrhalis, Haemophilus influenzae or Mycoplasma pneumoniae, bronchitis, pharyngitis, scarlet fever, whooping cough, or campylobacter enteritis, AZM was found effective in 94.4% (34/36). As for the bacteriological efficacy of AZM, all of 12 strains identified were found eradicated by the treatment. Plasma T 1/2(24 approximately 48 hrs.) of AZM in fine granules, given two patients at 10 mg/kg body weight once daily for 3 days, were 41.5 and 51.4 hours, while AUC0 approximately infinity was 7.45 and 13.44 mg.hr/ml. The rates of AZM recovered in the urine samples from two pediatrics patients in the first 81 hours of treatment, when it is given in fine granules at 10 mg/kg body weight once daily for 3 days, were 6.27% and 11.0%. Data from 43 patients were included for drug safety evaluation. Neither adverse reactions nor abnormal laboratory changes were observed. In conclusion, AZM was found useful in treatment of pediatric infections.
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PMID:[Clinical evaluation of a new macrolide antibiotic, azithromycin, in the pediatric field]. 957 55


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