Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cefuzonam (L-105, CZON), a new parenteral cephalosporin, was evaluated for its efficacy and safety in 22 children with bacterial infections (Table 1). The results obtained are summarized below. MICs of CZON to 26 strains of isolated organisms are shown in Table 2. MICs to all 14 strains of Haemophilus influenzae and 6 strains of Streptococcus pneumoniae were less than 0.05 microgram/ml. The MIC to 2 strains of Staphylococcus aureus was 0.39 microgram/ml and that to another was 0.78 microgram/ml. Two strains of Escherichia coli showed MICs of less than 0.05 and 0.10 microgram/ml, respectively. The MIC to 1 strain of Enterococcus faecalis was 6.25 micrograms/ml. The CZON was administered in 3 or 4 divided doses at a daily dosage ranging from 58.5 to 85.7 mg/kg by 30-minute drip infusion or intravenous injection to 22 patients (9 cases of pneumonia, 9 cases of tonsillitis, 2 cases of bronchitis, 1 case each of suppurative parotitis and acute pyelonephritis) and the following clinical results were obtained; excellent: 12 cases; good: 7 cases; fair: 3 cases. The overall efficacy rate was 86% (Table 4). Diarrhea was observed in four patients, and was resolved with or without discontinuation of the medication within a week. Anemia was noted in 2 cases. Leucopenia and neutropenia was observed in 1 case. There were a moderate rises in S-GOT and S-GPT activities in 1 patient (Table 4), and they necessitated the cessation of the CZON therapy. The S-GOT and S-GPT activities became normal after the drug treatment was stopped.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Clinical evaluation of cefuzonam in children]. 359 88

Studies were carried out on the penetration of cefuzonam (L-105, CZON), a new synthetic cephalosporin antibiotic, into cerebrospinal fluid, and on the clinical efficacy against bacterial infections. The results are summarized as follows: Concentrations of CZON in cerebrospinal fluid at 1 hour after intravenous administration of 100 mg/kg in cases of furunculosis of the external canal, encephalitis and mumps meningitis were 0.56 micrograms/ml, 1.44 micrograms/ml and 0.33 micrograms/ml, respectively. Concentrations of CZON in cerebrospinal fluid at 1 hour after intravenous administration of 100 mg/kg in 3 cases of purulent meningitis were 2.80-6.40 micrograms/ml at the acute stage and 0.56-1.45 micrograms/ml even at the recovering stage. Sensitivities of clinically isolated strains to CZON were determined and expressed as MIC. MICs of CZON on Haemophilus influenzae, Escherichia coli, Proteus mirabilis and Klebsiella pneumoniae were similar to MIC's of cefmenoxime (CMX), and lower than those of cefoperazone (CPZ), cefmetazole (CMZ), cefatiam (CTM) and Cefazolin (CEZ). The MIC of CZON on Staphylococcus aureus was similar to those of CEZ, CMZ and CTM, and lower than those of CMX and CPZ. Clinical responses of CZON were good in 2 cases of purulent meningitis, good in 2 cases of pyothorax, excellent in 1 case of septicemia, excellent in 3 cases of urinary tract infections, excellent in 7 cases and good in 3 cases out of 10 cases of pneumonia. Clinical responses of other diseases were excellent in 4 cases of bronchitis, good in 1 case of furunculosis of the external canal, excellent in 1 case of tonsillitis. No side effects nor abnormal laboratory findings were observed except 2 cases of mild diarrhea out of 24 cases.
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PMID:[Clinical evaluation of cefuzonam in pediatrics and a study on the penetration into cerebrospinal fluid]. 361 85

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

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

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

Microbiological, pharmacokinetic and clinical studies on sulbactam/cefoperazone (SBT/CPZ) were carried out in the field of pediatrics. Antimicrobial activity The MIC80 of SBT/CPZ was 6.25 micrograms/ml for clinically isolated 24 strains of S. aureus (24 beta-lactamase producing strains), 0.39 micrograms/ml for 17 strains of S. pyogenes, 3.13 micrograms/ml for 24 strains of E. coli (22 beta-lactamase producing strains), 3.13 micrograms/ml for 22 strains of K. pneumoniae (22 beta-lactamase producing strains), 1.56 micrograms/ml for 22 strains of P. mirabilis and 0.20 microgram/ml for 15 strains of H. influenzae (13 beta-lactamase producing strains). In comparison with CPZ in respect to the MIC, SBT/CPZ exhibited synergistic effect on 31 strains out of 81 beta-lactamase producing strains (included 6 strains of S. aureus, 9 of E. coli, 5 of K. pneumoniae and 11 of H. influenzae) which was scarcely observed against 43 non-beta-lactamase producing strains. Absorption and excretion Serum levels and urinary excretion of SBT/CPZ were studied in 7 children aged 5 to 12 years. The mean serum concentration of SBT at 15 minutes following a single intravenous injection of 10 mg/kg of SBT/CPZ was 14.2 micrograms/ml and that of CPZ was 30.4 micrograms/ml. The mean urinary recovery rates at 6 hours following the intravenous injection were 57.8% and 18.3%, respectively. The mean serum concentrations of SBT and CPZ after 1-hour infusion of 10 mg/kg of SBT/CPZ were 10.9 micrograms/ml and 17.6 micrograms/ml, respectively. The urinary recovery rates of SBT and CPZ at 7 hours after the infusion were 100.0% and 27.7% on average, respectively. The mean serum levels of SBT and CPZ at 15 minutes after a single intravenous injection of 20 mg/kg of SBT/CPZ were 25.6 micrograms/ml and 66.0 micrograms/ml, respectively and urinary elimination until up to 6 hours were 72.5% on average for SBT and 21.1% for CPZ. Clinical study SBT/CPZ was used for the treatment of a total of 20 pediatric patients aged 1 month to 14 years to evaluate its clinical effectiveness, bacteriological efficacy and adverse effects. The clinical efficacy in 6 patients with acute pneumonia, 3 with staphylococcal scalded skin syndrome, 2 each with acute purulent tonsillitis and acute pyelonephritis, 1 each with acute purulent lymphadenitis, acute sinusitis, acute bronchitis, peritonitis and acute enteritis was judged to be excellent in 15 cases and good in 3 cases with an efficacy ratio of 100%. The clinical efficacy in 6 patients whose infections were caused by beta-lactamase producing strains was judged to be excellent in all the cases.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Studies on sulbactam/cefoperazone in the field of pediatrics]. 609 65

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

To evaluate the antibacterial potency of cefotiam (CTM) clinical and laboratory studies were carried out and the results were as follows. Clinical evaluation and adverse reaction CTM was given to total of 23 patients, 10 with bronchopneumonia, 10 with bronchitis and one each with cystitis, enteritis and suspected sepsis. Overall efficacy rate was 78.3% (18/23) (excellent 9, good 9, fair 3, poor 2). Only 1 case showed a side effect of slightly elevated GOT and GPT. Antibacterial activities MIC of CTM against isolates from sputum was investigated on those patients mentioned above and was compared with MIC of CEZ and CMZ. CTM showed superior antibacterial activity against almost all strains. Especially on Haemophilus and Klebsiella antibacterial activity of CTM was impressive. Organisms in sputum Four out of 8 causative bacteria disappeared and 1 out of 8 decreased after administration of CTM. Thus CTM is considered to be the useful drug for the treatment of respiratory infection.
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PMID:[Antibacterial potency of cefotiam based on the clinical effect, MIC and decrement of organisms in the sputum]. 631 12

Experimental and clinical studies on cefoperazone (CPZ), a new synthetic cephalosporin, were performed in the field of pediatrics. 1) The MICs of CPZ against 26 strains of S. aureus, 21 strains of E. coli, 20 strains of K. pneumoniae and 15 strains of H. influenzae which were clinically isolated were estimated and compared with those of CEZ and ABPC. Some strains were found to be high in the MIC of CPZ against S. aureus, E. coli and K. pneumoniae by original inoculation but 88% of S. aureus, 95% of E. coli, 95% of K. pneumoniae and 100% of H. influenzae were under 6.25 mcg/ml by 100 times dilution inoculation. The MIC of CPZ against S. aureus was inferior to CEZ and superior to ABPC, and that against E. coli, K. pneumoniae and H. influenzae was superior to CEZ and ABPC. 2) The serum concentration, urinary concentration and recovery rate from urine were measured in two healthy infants and one infant in the stage of convalescence from cholangiohepatitis after a single intravenous administration of 25 mg/kg of CPZ. The mean serum concentration in the two healthy infants was 88.0 mcg/ml at 30 minutes, 63.0 at 1 hour, 31.4 at 2 hours, 12.2 at 4 hours and 4.2 at 6 hours; the half-life was 1.29 hours, and the recovery rate from urine was 14.5%. 3) The clinical effect of CPZ was examined in 16 cases of acute lobar pneumonia or acute bronchopneumonia, 1 case of acute bronchitis and 4 cases of acute urinary tract infections. All of the cases responded effectively or markedly effectively. Among the causative bacteria in those cases, 2 strains of S. pneumoniae, 1 strain of S. faecalis, 1 strain of H. influenzae and 2 strains of E. coli and 1 strain of K. pneumoniae disappeared following the administration of CPZ. The bacteriological effect against 1 strain of P. aeruginosa was unknown, but clinical effectiveness was observed in this case. No clinical side effects were observed. Laboratory examination carried out before and after the administration revealed a rise of GOT and eosinophilia in each one case, but in both abnormality returned to normal after termination of therapy.
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PMID:[Laboratory and clinical studies of cefoperazone in children (author's transl)]. 645 36

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.
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PMID:[Laboratory and clinical studies of 9,3"-diacetylmidecamycin in the pediatric field]. 698 50


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