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 6,902 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Bacteriological, pharmacokinetic, and clinical studies of cefixime (CFIX), a newly developed oral cephalosporin, was conducted in our pediatric department as outlined below. Bacteriology The prevalent MICs of CFIX by microbiological species, compared with those of the reference drugs, were detailed below. Against 16 strains of S. aureus, the MICs averaged 6.25 micrograms/ml, and were found to be nearly the same as the MICs of amoxicillin (AMPC) but higher than those of cephalexin (CEX) and cefaclor (CCL). For 4 strains of S. pyogenes, the MICs averaged 0.05 microgram/ml, and were higher than the MICs of AMPC but lower than those of CEX and CCL. Mean MICs of CFIX against other clinical isolates were lower than those of CEX, CCL, or AMPC; E. coli (20 strains), 3.13 micrograms/ml; K. pneumoniae (9), 0.10 microgram/ml; P. mirabilis (16), 0.025 microgram/ml; P. vulgaris (5), 0.10 microgram/ml; H. influenzae (11), 0.05 microgram/ml; and S. typhimurium (4), 0.10 microgram/ml. The MICs of CFIX against 10 strains of P. aeruginosa were distributed at and above 25 micrograms/ml, a range much lower than greater than or equal to 100 micrograms/ml for CEX, CCL, or AMPC. Pharmacokinetics The serum concentrations and urinary recovery were studied in 3 children ranging from age 7 to 13. They were given CFIX on empty stomach in 2 different single doses of 3 and 6 mg/kg in a cross-over design. Average serum CFIX concentrations were dose-dependent, as evidenced by the respective peak concentrations of 1.70 microgram/ml for a 3 mg/kg dosage and 2.72 micrograms/ml for 6 mg/kg, which were attained 4 hours after the administration of the drug. The average half-lives of CFIX in the serum were 3.09 hours and 3.11 hours, respectively, and the 12-hour serum concentrations were 0.32 microgram/ml and 0.77 microgram/ml, respectively, for the 2 different dose levels. The average 12-hour urinary recovery was 25.2% and 22.3%, respectively. Clinical study Clinical effectiveness, bacteriological effectiveness, and side effects were studied in 27 children with infection including 4 patients with acute pharyngitis, 13 with acute purulent tonsillitis, 5 with acute pneumonia, 3 with urinary tract infection, and 1 each with acute rhinitis and acute bronchitis. One child with acute pneumonia (Mycoplasma pneumonia) was excluded from the study. The therapeutic effectiveness was "excellent" in 21, "good" in 3, "fair" in 1, and "poor" in 1, with an effectiveness rate of 92.3%.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies on cefixime in pediatrics]. 376 39

T-2588 was used on 55 patients with respiratory tract infections and 44 cases were evaluated; 23 patients with pneumonia, 12 patients with acute bronchitis, 2 patients with chronic bronchitis, 1 patient with diffuse panbronchiolitis and 6 patients with bronchiectasis with infection. Clinical effects of T-2588 were as follows; excellent in 6 and good in 28 patients. The efficacy rate was 77.3% (34/44). Bacteriological effects of T-2588 were prominent in 8 patients infected with B. catarrhalis, H. influenzae, K. pneumoniae and E. coli, but not in a patient infected with P. putida. The elimination rate was 90.0% (9/10 strains). As side effects, stomatitis, anorexia, diarrhea X vomiting and pruritus were observed in one patient each. Abnormal laboratory findings were observed in 4 patients with elevated GOT and/or GPT. These side effects and abnormal laboratory findings were not serious. The usefulness of T-2588 was 68.2% (30/44). Therefore, T-2588 is a useful drug and its effects are promising in clinical management of respiratory tract infections.
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PMID:[Evaluation of T-2588 in the treatment of respiratory tract infection]. 382 May 69

Fundamental and clinical studies on BRL 25000 granules were carried out in the pediatric field. BRL 25000 is a formulation comprising 1 part of clavulanic acid (CVA) and 2 parts of amoxicillin (AMPC). The MICs of BRL 25000 and AMPC were assessed against 24 clinically isolated strains of S. aureus (including 23 beta-lactamase producing strains), 22 S. pyogenes, 20 E. coli (8 beta-lactamase producing strains), 24 K. pneumoniae (24 beta-lactamase producing strains), 20 H. influenzae (6 beta-lactamase producing strains). BRL 25000 showed MIC80 (cumulatively 80% of strains were inhibited) at 6.25 micrograms/ml against S. aureus, less than or equal to 0.10 micrograms/ml against inst S. pyogenes, 12.5 micrograms/ml against E. coli, 6.25 micrograms/ml against K. pneumoniae and 0.39 micrograms/ml against H. influenzae. BRL 25000 showed no improvement in MIC terms against beta-lactamase nonproducing strains compared with AMPC. However, BRL 25000 was markedly more effective against beta-lactamase producing strains. Thus BRL 25000 was up to 8 fold more active against S. aureus, 2 to 64 fold against E. coli, 4 to 128 fold against K. pneumoniae, 4 to 16 fold against H. influenzae than AMPC. Following oral administration of BRL 25000 granules (at a dose level of 12.5 mg/kg) to 2 children aged 9 and 11 years, the mean peak serum concentrations of AMPC and CVA were 8.33 +/- 2.43 micrograms/ml and 4.44 +/- 1.65 micrograms/ml respectively 1 hour after dosing. The half-lives of AMPC and CVA were 1.35 +/- 0.42 hours and 0.91 +/- 0.05 hour, respectively. The urinary excretion was 48.21 +/- 3.83% for AMPC and 16.90 +/- 7.06% for CVA in the first 6 hours after administration. In clinical studies, 23 pediatric patients aged 2 months to 12 years with bacterial infections were treated with BRL 25000 granules and the clinical effectiveness, bacteriological response and side effects were evaluated. The clinical response was assessed in 23 cases, 3 with acute rhinitis, 6 with acute purulent tonsillitis, 5 with acute bronchitis, 4 with acute pneumonia, 3 with impetigo, 1 with furunculosis and 1 with periproctal abscess. Results were excellent in 13 cases, good in 7, fair in 3 and hence the efficacy rate (excellent and good cases) was 87.0% (20/23). In particular the clinical response in 9 cases with infections due to beta-lactamase producing organisms was excellent in 6, good in 2, fair in 1 and the efficacy rate was 88.9% (8/9).(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) in the pediatric field]. 384 22

Aspoxicillin (ASPC), a new penicillin for injection, was evaluated for its efficacy and safety in 29 children with bacterial infection (Table 1), and the following results were obtained. MICs of ASPC to 26 strains of isolated organisms are shown in Table 2. MICs to 4 out of 13 strains of H. influenzae were higher than 6.25 micrograms/ml. MICs to 5 strains of S. pneumoniae were lower than 0.78 microgram/ml and 1 out of 3 strains of S. aureus and 1 strain of E. coli showed higher MICs than 100 micrograms/ml. ASPC was administered in 3 or 4 divided doses at a daily dosage ranging from 21 to 98 mg/kg by 30 minutes drip infusion or intravenous injection to 29 patients (16 cases of pneumonia, 8 cases of tonsillitis, 3 cases of bronchitis, 1 case of urinary tract infection, 1 case of impetigo) and the following clinical results were obtained: excellent; 11 cases, good; 11 cases, fair; 3 cases, poor; 1 case. The overall efficacy rate was 85% (Table 3, 4). No clinical side-effects were observed in any of the patients. Leukopenia was noted in 1 case. Slight elevation of GOT and GPT was noted in 2 cases, and minimal elevation of GOT was observed in other 2 cases (Table 5). These data suggest that ASPC is an useful new antibiotic in the treatment of children with susceptible bacterial infection and may be used as the first choice antibiotic for the treatment of respiratory tract infection in children.
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PMID:[Clinical evaluation of aspoxicillin in children]. 385 58

Fundamental and clinical studies of aspoxicillin (ASPC, TA-058), a new penicillin antibiotic, were performed in pediatric field. Antimicrobial activity MIC of ASPC was compared with that of piperacillin (PIPC), ampicillin (ABPC) and carbenicillin (CBPC) for clinical isolates of S. aureus (24 strains), S. pyogenes (22 strains), H. influenzae (18 strains), E. coli (21 strains) and K. pneumoniae (23 strains). MIC of ASPC against S. pyogenes was distributed in less than 0.39 microgram/ml and this numerical value of MIC was very superior. MIC distributions of ASPC against S. aureus, H. influenzae and E. coli had 2 peaks respectively. It was presumed that the results are due to an existence of beta-lactamase producing strains. The sensitive strains in those were distributed in less than 1.56-12.5, less than or equal to 0.10 and 0.78-3.13 micrograms/ml, respectively, and those numerical value of MIC was superior. While against K. pneumoniae, all strains were distributed in more than 12.5 micrograms/ml and the antimicrobial activity of ASPC was very inferior. ASPC was as active as PIPC and ABPC against S. pyogenes, but more active then CBPC, ASPC was less active against S. aureus than PIPC and ABPC, but more active than CBPC. And ASPC was less active against H. influenzae and E. coli than PIPC, but more active than ABPC and CBPC. Against K. pneumoniae, strains that showed somewhat low numerical value of MIC at only PIPC were observed, but antimicrobial activities of ABPC and CBPC, as well as ASPC were very inferior. Absorption and excretion Serum level and urinary excretion of ASPC in 6 pediatric patients of 4 months to 12 years of age after one shot intravenous injection of 20 mg/kg were examined. The serum mean levels were 51.7 micrograms/ml at 1/4 hour, 38.2 micrograms/ml at 1/2 hour, 22.9 micrograms/ml at 1 hour, 3.0 micrograms/ml at 4 hours and 1.0 microgram/ml at 6 hours after injection, respectively. The mean half-life of serum level was 1.03 hours. The mean urinary levels were 4,646 micrograms/ml for 0-2 hours, 1,773 micrograms/ml for 2-4 hours and 299 micrograms/ml for 4-6 hours. The mean urinary recovery rate within 6 hours after injection was 64.7%. Clinical studies In order to evaluate clinical response, bacteriological response and side effects, ASPC was applied to 28 cases, i.e., 5 cases of acute purulent tonsillitis, 2 cases of acute purulent otitis media, 2 cases of acute bronchitis and 19 cases of acute pneumonia.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies on aspoxicillin in the pediatric field]. 385 60

A fundamental and clinical study of ceftizoxime (CZX) suppositories was performed in pre-school and school-age children. The average time courses of CZX serum and urinary concentrations after administration of CZX suppository 250 mg (i.e. per kg body weight doses of 8.3-10.9 mg) to 4 school-age children were as follows. Serum concentrations: 6.1 micrograms/ml at 15 minutes, 6.3 micrograms/ml at 30 minutes, 3.8 micrograms/ml at 1 hour, 1.7 microgram/ml at 2 hours, 0.5 microgram/ml at 4 hours and 0.2 microgram/ml at 6 hours with a biological half-life of 1.43 hours. Urinary concentrations: 885 micrograms/ml for 0-2 hours, 209 micrograms/ml for 2-4 hours and 112 micrograms/ml for 4-6 hours with an average 6-hour urinary recovery rate of 25.6%. The clinical and biological effectiveness and adverse reactions were studied in 11 infants and school-age children afflicted with various infections (acute purulent tonsillitis, 1; acute bronchitis, 3; acute pneumonia, 4; and UTI, 3). The clinical responsiveness was "excellent" in 8, "good" in 2, and "failure" was recorded in 1, with an overall efficacy of 90.9% inclusive of "excellent" and "good". The microbiological effectiveness of CZX suppositories on presumed pathogenic organisms comprising 4 strains of H. influenzae, 1 strain of H. parainfluenzae, and 3 strains of E. coli was satisfactory, as evidenced by the substantially high eradication rate of 87.5%. The only organism that survived CZX suppository treatment was 1 strain of H. influenzae which however was greatly decreased. The only side effect was diarrhea in 1 patient, which however did not necessitate withdrawal of the drug. The only laboratory test abnormality was GOT and GPT elevation in 1 patient which was normalized within 8 days. In conclusion, CZX suppositories were found to be efficacious and safe for treatment of bacterial infections in children.
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PMID:[Clinical studies of ceftizoxime suppositories in respiratory tract infections and urinary tract infections in children]. 386 84

MICs of BRL 25000, a combination of a newly developed beta-lactamase inhibitor CVA and AMPC in the ratio of 1 to 2, were determined against a number of bacterial strains and compared with those of AMPC, CVA, CEX and CCL. The 98 bacterial strains tested included 2-S. aureus, 23-H. influenzae, 25-E. coli, 22-K. pneumoniae and 26-P. mirabilis. In pharmacokinetic studies, BRL 25000 medium granules were administered to groups of 3 male subjects, aged between 7 years 8 months and 9 years 5 months, at doses of 10, 15 and 20 mg/kg, 2 hours after a meal. The resultant serum and urine concentrations and drug recoveries were measured. Furthermore, BRL 25000 was administered to a total 43 patients (2-pharyngitis, 8-tonsillitis, 3-bronchitis, 2-pneumonia and 28-urinary tract infection) whom clinically evaluable. An average daily dosage of 45.3 mg/kg was given, in 3 or 4 divided doses, for a period of 8 days on average. Clinical and bacteriological effects as well as side effects were studied. In the microbiological studies on 98 clinical strains, including beta-lactamase negative bacteria, BRL 25000 showed MICs against the Gram-positive cocci (2-S. aureus) superior to the other 4 drugs at inoculum sizes of 10(8) and 10(6) cells/ml. For the Gram-negative bacilli, against H. influenzae at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but superior in the large MIC range to AMPC, and was superior to the other 3 drugs. Against E. coli at an inoculum of 10(8) cells/ml, BRL 25000 showed antibacterial activity next to AMPC and CCL whilst at an inoculum of 10(6) cells/ml, it was inferior in the small MIC range but superior in the large MIC range to AMPC and CEX and was inferior to CCL but superior to CVA. Against K. pneumoniae at an inoculum of 10(8) cells/ml, BRL 25000 was equal to AMPC, CVA and CEX but inferior to CCL, whilst at an inoculum of 10(6) cells/ml, it was inferior to CCL but superior to the other 3 drugs. Against P. mirabilis at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but equal or superior in the large MIC range to AMPC, and was superior to CVA and CEX.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical trials of BRL 25000 (clavulanic acid-amoxicillin) granules in the field of pediatrics]. 389 76

Fundamental and clinical trials were carried out with cefminox (CMNX, MT-141) in pediatric infections. Results were as follows. The mean serum concentrations of CMNX following intravenous injection of 10, 20 and 40 mg/kg were 73.1, 112.5 and 181.4 micrograms/ml at 15 minutes after injection, respectively. The serum half-life times were 1.37, 1.20 and 1.53 hours, respectively. Average recovery rates in the urine until 6 hours from the start of injection were 91.4, 59.4 and 85.8%, respectively. The antimicrobial activity of CMNX against clinically isolated organisms was measured; CMNX was more active than CMZ and CEZ against H. influenzae. CMNX was equal to or more active than CMZ and CEZ against E. coli. CMNX was administered clinically to 32 pediatric patients with various infections; 19-pneumonia, 5-bronchopneumonia, 3-bronchitis and 5-pyelonephritis. Overall efficacy rate was 93.8%. Slight elevation of S-GOT and S-GPT was observed in 2 patients. No other serious side effect was observed.
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PMID:[Clinical evaluation of cefminox in pediatric field]. 389 3

A new antibiotic of cephamycin group, cefminox (CMNX, MT-141) was studied both fundamentally and clinically in the field of pediatrics. The minimum inhibitory concentrations (MIC) of CMNX for clinical isolates including 24 strains of S. aureus, 15 strains of S. pyogenes, 21 strains of H. influenzae, 24 strains of E. coli, 22 strains of K. pneumoniae and 22 strains of P. mirabilis were determined and compared to those of cefmetazole (CMZ), latamoxef (LMOX), cefotaxime (CTX), cefoperazone (CPZ) and cefazolin (CEZ). The MIC80 (80% MIC) values of CMNX for H. influenzae, E. coli, K. pneumoniae and P. mirabilis were 1.56, 1.56, 0.39 and 1.56 micrograms/ml, respectively. When compared to antibacterial activities of the control drugs, the activity of CMNX was inferior to those of CTX and LMOX but superior to those of CMZ and CEZ. On the other hand, MIC80 values of CMNX for S. pyogenes and S. aureus were 6.25 and 12.5 micrograms/ml, the activities being inferior to all of CMZ, CTX, LMOX, CPZ and CEZ used as the control drugs. In 3 pediatric patients of 9 to 12 years old, 20 mg/kg of CMNX was given intravenously as one shot and serum and urinary concentrations were determined. The mean serum concentrations in these 3 cases were 124 micrograms/ml, 102 micrograms/ml, 74.0 micrograms/ml, 47.9 micrograms/ml, 20.4 micrograms/ml, 9.2 micrograms/ml and 4.3 micrograms/ml at 1/4, 1/2, 1, 2, 4, 6 and 8 hours, respectively, with a half-life of 1.83 hours. The mean urinary concentrations were 1,968 micrograms/ml at 0 approximately 2 hours, 1,205 micrograms/ml at 2 approximately 4 hours, 761 micrograms/ml at 4 approximately 6 hours and 409 micrograms/ml at 6 approximately 8 hours, with 65.4% of the drug dosed recovered from the urine within the first 8 hours on an average. CMNX was used in the treatment of 22 clinical cases including 3 cases of acute purulent tonsillitis, 3 cases of acute bronchitis, 9 cases of acute pneumonia, 5 cases of acute pyelonephritis and 2 cases of acute enteritis. Clinical results in 20 cases excluded of 2 cases of Mycoplasma pneumonia were rated as excellent in 19 cases and as good in 1 case, with an efficacy rate being 100% taking excellent and good cases as effective cases. Bacteriological results for 5 strains of H. influenzae, 1 strain of H. parainfluenzae, 5 strains of E. coli, 2 strains of K. oxytoca and 1 strain of S. pneumoniae revealed that disappearance was obtained for all strains but 1 strain of P. aeruginosa which persisted.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies on cefminox in the field of pediatrics]. 389 4

Fundamental and clinical studies on S 6472 were carried out and following results were obtained. Serum concentrations after single oral administration showed 2 peaks at 1 or 2 hours and 5 or 6 hours in the cases with normal meal. Namely this drug has much more maintenance of serum concentration than normal cefaclor. In maintenance of serum concentrations after the administration, there were no obviously difference between normal and heavy meal. S 6472 was administered twice a day to 7 patients with various infections (bronchopneumonia 2 cases, acute bronchitis 1 case, purulent tonsillitis 4 cases) and clinical responses were all effective results. Pathogenic bacteria of S. aureus, S. pneumoniae, S. pyogenes and H. influenzae were completely eliminated in all cases. No significant side effects were observed. On the above results, this administration method of S 6472 twice a day was considered to be good response against mild or moderate bacterial infections in children.
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PMID:[Fundamental and clinical studies of S 6472 (sustained release preparation of cefaclor) in the pediatric field]. 390 36


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