Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:2.6.1.2 (alanine aminotransferase)
 26,722 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In order to objectively evaluate the efficacy and the safety of ceftriaxone (CTRX) using once daily administration of 1 g to cases of acute suppurative otitis media and acute exacerbation of chronic suppurative otitis media, a group comparison study by the envelope method was conducted using cefotiam (CTM) as the control drug (2 g twice daily). The results obtained are summarized as follows. 1. Clinical efficacies evaluated by the committee were 71% in the CTRX group and 86% in the CTM group for acute suppurative otitis media, and 63% and 60%, respectively, for chronic suppurative otitis media. When all cases were considered both groups evidenced a clinical efficacy of 64%, and no significant difference was observed between the 2 groups. 2. Clinical efficacies evaluated by the physician in charge were 65% in the CTRX group and 86% in the CTM group for acute suppurative otitis media, and 72% and 60%, respectively, for chronic suppurative otitis media. When all cases were considered efficacies were, respectively, 70% and 64%, showing no significant difference between the 2 groups. 3. Bacteriological efficacies were 88% in the CTRX group and 86% in the CTM group for acute suppurative otitis media, and 74% and 62%, respectively, for chronic suppurative otitis media. With all cases bacterial eradication rates were, respectively, 76% and 67%. Bacterial eradication rates were always higher for the CTRX group than for the CTM group, but the difference was not significant between the 2 groups. 4. Against infections caused by Staphylococcus aureus alone, CTRX showed equal clinical and bacteriological efficacies to CTM. 5. As side effects, dermatitis, vomiting, and malaise were observed in 5 cases (4%) of the CTRX group and 3 cases (3%) of the CTM group. As clinical testing abnormalities, elevations of GOT, GPT, and Al-P, and thrombocytopenia were noted only in 3 cases (5%) of the CTRX group. Furthermore, all of these abnormalities were temporary and of moderate degree or mild, thus the safety of either drug was considered high. 6. Clinical utilities were 71% in the CTRX group and 86% in the CTM group for acute suppurative otitis media, and 72% and 62%, respectively, for chronic suppurative otitis media. When all cases were included, they were 72% and 66%, respectively, and there was no significant difference between the 2 groups. It is concluded from the above results that CTRX is a highly useful drug with once daily administration of 1 g in the treatment of suppurative otitis media.
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PMID:[Evaluation of the efficacy of ceftriaxone in acute suppurative otitis media and acute exacerbation of chronic suppurative otitis media. A comparative study with cefotiam as the control]. 252 93

Bacteriological, pharmacokinetic and clinical studies on cefpodoxime proxetil (CPDX-PR, CS-807), a new oral cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows. 1. Antibacterial activities of R-3746 (Na-salt of cefpodoxime (CPDX] against clinically isolated strains of Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, Branhamella catarrhalis, Escherichia coli, Proteus mirabilis and Haemophilus influenzae were compared with those of cefaclor, cephalexin and cefadroxil. R-3746 is superior to other antibiotics against S. pneumoniae, S. pyogenes, B. catarrhalis and Gram-negative rods. 2. Serum concentrations of CPDX after administration of CPDX-PR at doses of 3 mg/kg (fasting), 6 mg/kg (non-fasting) and 6 mg/kg (fasting) were determined. Mean AUC (area under curve)'s of CPDX obtained were 9.60, 31.35 and 17.89 micrograms.hr/ml, respectively for the 3 dosages. The mean half-lives of CPDX were 3.35, 1.88 and 1.76 hours, respectively. The mean urinary recovery rate within 8 hours after administration of CPDX-PR at a dose of 3 mg/kg (fasting) was 39.2%. 3. CPDX-PR was administered to 37 pediatric patients with various bacterial infections (pyelonephritis 9, cystitis 4, pneumonia 7, acute bronchitis 3, otitis media 2, tonsillitis 10, subcutaneous abscess 1 and purulent lymphadenitis 1). The overall clinical efficacy rate was 91.9% and the overall bacteriological eradication rate was also 91.9%. 4. No adverse reactions were observed. Abnormal laboratory findings were moderate, eosinophilia in 2 and slight elevation of GOT and GPT in 1. The taste and the odor of the CPDX-PR preparation was sufficiently tolerable. From the above results we have concluded that CPDX-PR is a useful oral antibiotic in the treatment of bacterial infections in children.
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PMID:[Bacteriological, pharmacokinetic and clinical studies on cefpodoxime proxetil in the pediatric field]. 256 89

1. Absorption and elimination Serum and urinary levels of cefodizime (CDZM, THR-221) were determined in 7 children with ages ranging from 3 to 12 years after a intravenous bolus injection of the drug at 20 mg/kg. The average serum level of the drug was 119.27 +/- 13.83 micrograms/ml at 30 minutes, then decreased gradually with a half-life of 2.01 +/- 0.25 hours to 10.56 +/- 2.93 micrograms/ml at 6 hours. The average urinary elimination rate was 77.34 +/- 12.60%. 2. Clinical study CDZM was given to the following 39 patients with ages ranging from 2 months to 15 years and clinical efficacy, bacteriological response and adverse reactions were evaluated. The treated cases were 2 cases of acute purulent tonsillitis, 30 cases of acute pneumonia, 1 case of acute purulent otitis media and 2 cases of acute urinary tract infections. Clinical efficacies were excellent in 29 cases, good in 5 cases and poor in 1 with an efficacy rate of 97.1%. Organisms presumed to be pathogens included 3 strains of Streptococcus pneumoniae, 1 beta-Streptococcus, 1 Staphylococcus epidermidis, 9 Haemophilus influenzae (1 beta-lactamase producing strain and 8 non-producing strains) and 1 Enterococcus faecalis. The last one was decreased and the others were eradicated with an eradication rate of 93.3% for all strains. Adverse reactions occurred in no patients. Abnormal changes in laboratory test values involved only 1 case each of elevated GOT, elevated GOT and GPT, eosinophilia and thrombocytosis. Based on the above-mentioned result and features of this drug, it was confirmed that this drug showed an excellent usefulness in the treatment of infections in childhood. It may be also effective in the management of infections under immunosuppression.
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PMID:[Experimental and clinical studies on cefodizime in pediatrics]. 279 56

Twenty nine children were treated with cefpodoxime proxetil (CPDX-PR, CS-807) and the clinical efficacy and side effects were evaluated. Ages of the patients ranged from 2 months to 10 years. Dose levels of CPDX-PR ranged from 7.5 to 12.0 mg/kg/day for 5 to 12.7 days. The 29 patients included 9 tonsillitis, 2 otitis media, 5 scarlet fever, 3 bronchopneumonia, 1 lymphadenitis, 8 urinary tract infections and 1 staphylococcal scalded skin syndrome, and they were evaluated for the clinical efficacy of CPDX-PR. Results were excellent in 21 and good in 8 patients. Out of the 29 patients, 3 cases showed diarrhea and 2 cases showed elevated GOT and GPT. The pharmacokinetics of CPDX-PR was studied in 9 patients whose ages ranged from 1 to 9 years. The serum peak concentrations of CPDX in 5 patients were between 1.37 and 4.10 micrograms/ml (mean: 2.53 micrograms/ml) at 1 to 6 hours after dosing 3 mg/kg before meals. Those of 4 patients ranged 3.29 to 4.88 micrograms/ml (mean: 4.36 micrograms/ml) at 2 hours after administering 6 mg/kg before meals. Portions of CPDX excreted into urine within 6 hours ranged from 20.3 to 34.3% (mean 27.1%) in 5 patients who were given 3 mg/kg, and ranged from 24.1 to 65.7% (mean 41.1%) in 4 patients given 6 mg/kg.
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PMID:[Clinical and pharmacokinetic evaluation of cefpodoxime proxetil in children]. 281 Jul 21

Pharmacokinetic, bacteriological and clinical studies on cefpodoxime proxetil (CPDX-PR, CS-807), a newly developed oral cephem, were carried out in the treatment of infectious diseases in the field of pediatrics. 1. Since CPDX demonstrates very powerful antimicrobial actions against such Gram-negative bacilli as Escherichia coli, Salmonella sp., Klebsiella pneumoniae and Serratia sp., such Gram-positive cocci as Streptococcus pyogenes and Streptococcus pneumoniae, and beta-lactamase producing Branhamella catarrhalis and Haemophilus influenzae, this drug was thought to be useful for the treatment of pediatric infectious diseases when main causative bacteria in the field of pediatrics were taken into account. 2. When changes in blood and urine concentrations of CPDX following the administration of this drug at 3.7 mg/kg before meal were determined, Cmax and T1/2 were found to be 2.98 micrograms/ml at 2-hour and 1.73 hours, respectively; an urinary excretion rate in the first 6 hours and a maximum urine concentration were 32.5% and 52 micrograms/ml, respectively. 3. Clinically, 8 of 8 patients with the upper respiratory tract infections (100%), 28 of 29 patients with bronchitis and/or pneumonia (96.6%), 3 of 4 patients with otitis media (75%), 2 of 2 patients with sinusitis (100%), 3 of 3 patients with the skin soft tissue infections (100%), 1 of 1 patient with bacterial enteritis (100%) and 11 of 14 patients with urinary tract infections (78.6%) responded well to the treatment with CPDX-PR, showing a 91.8% efficacy rate in all the patients treated. 4. Bacteriologically, Staphylococcus aureus, Staphylococcus epidermidis, S. pyogenes, S. pneumoniae, E. faecalis, B. catarrhalis, H. influenzae, E. coli and Salmonella typhimurium were all eradicated from 5, 1, 4, 6, 1, 5, 5, 11 and 1 patient, respectively. An eradication rate in all the patients examined was 97.5% (39/40). 5. Gastrointestinal symptoms appeared as side effects in 2 of 71 patients (vomiting in 1 and diarrhea in 1), hence, an incidence of side effects was 2.8% (2/71). As for abnormal laboratory findings, eosinophilia, thrombocytosis and increases in GOT and GPT were observed in 3 of 39 patients examined (7.7%), 1 of 39 patients (2.6%) and 2 of 34 patients (5.9%), respectively. In addition, we also examined the effect of the drug on the hemostatic system, but found no changes upon the treatment. Based on these results, it appeared that CPDX-PR was a useful and safe drug in treatment of infectious diseases in the field of pediatrics when administered 2-3 times a day at a dose of 3-6 mg/kg.
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PMID:[Pharmacokinetic, bacteriological and clinical studies on cefpodoxime proxetil in the field of pediatrics]. 281 Jul 29

Twenty-six children were treated with cefteram pivoxil (CFTM-PI) and the clinical efficacy and side effects were evaluated. Ages of the patients ranged from 8 months to 9 years. Doses of CFTM-PI ranged 7.5-20.1 mg/kg/day for 4 to 19 days. The twenty-six patients including 10 patients with tonsillitis, 1 pharyngitis, 3 otitis media, 2 scarlet fever, 1 bronchopneumonia, 1 lymphadenitis, 6 urinary tract infections, 1 vaginitis and 1 staphylococcal scalded skin syndrome were evaluated for clinical efficacy. Results were excellent in 11, good in 13, and fair in 2 patients. Out of the 26 patients, one case showed elevated GOT and GPT, and another case showed elevated GOT. The pharmacokinetic study of CFTM-PI was performed in 9 fasting patients whose ages ranged from 2 to 11 years. Serum peak concentrations of CFTM were 0.92 to 1.05 micrograms/ml (mean 0.99 microgram/ml) at 1 to 2 hours after a dose of 1.5 mg/kg each to 3 patients, 1.12 to 1.38 micrograms/ml (mean 1.25 micrograms/ml) after a dose of 3 mg/kg each to 3 patients and 0.66 to 2.1 micrograms/ml (mean 1.17 micrograms/ml) after a dose of 6 mg/kg each to 3 patients. The portions of the drug excreted into urine within 8 hours were 8.9% and 14.7% in 2 patients, each given a dose of 1.5 mg/kg, from 13.0 to 23.1% (mean 18.4%) in 3 patients, each given a dose of 3 mg/kg, and 6.3% and 8.7% in 2 patients, each given a dose of 6 mg/kg.
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PMID:[Clinical and pharmacokinetic evaluation of cefteram pivoxil in children]. 281 Jul 36

Bacteriological, pharmacokinetic and clinical studies were done on the effect of cefteram pivoxil (CFTM-PI, T-2588) (10% granules), a new oral cephalosporin, in the field of pediatrics. The results are summarized below. 1. Antibacterial activities Antibacterial activities of CFTM against Staphylococcus aureus and Streptococcus pyogenes were studied comparatively with activities of cefaclor (CCL), cephalexin (CEX) and ampicillin (ABPC). MICs of CFTM against S. aureus were distributed in a range between 0.78 and 12.5 micrograms/ml, with a peak value of 3.13 micrograms/ml, which were similar to MIC ranges of CEX and CCL. MICs of CFTM against all strains of S. pyogenes were less than or equal to 0.025 microgram/ml, which were similar to MIC of ABPC. CFTM was approximately 2 to 3 folds more effective than CCL or CEX. 2. Absorption and excretion. Serum concentrations and urinary excretions of CFTM were determined in doses of 3 mg/kg (non-fasting) and 6 mg/kg (non-fasting and fasting). In non-fasting subjects, peak concentrations of CFTM in serum were dose-dependent and were 1.15-2.3 micrograms/ml and 1.8-3.6 micrograms/ml at 2-3 hours, 0.125-0.78 micrograms/ml and 0.245-0.97 micrograms/ml at 6 hours, respectively, for the 2 dose levels. Serum half-lives were 1.03-2.65 hours for the dose of 3 mg/kg and 1.07-1.83 hours for 6 mg/kg. In fasting subjects, the mean peak serum concentrations were 1.73 micrograms/ml at 2 hours and 1.13 micrograms/ml at 6 hours for the dose of 6 mg/kg. Urinary recovery rates in the first 6 hours varied 5.3-19.2%. 3. Clinical study Clinical efficacies were examined in a total of 41 cases including 9 cases of bacterial pneumonia, 10 cases of bronchitis, 11 cases of tonsillitis, 7 cases of urinary tract infections, 3 cases of scarlet fever and 1 case of otitis media. Clinical efficacies were excellent in 30 cases, good in 10 cases, poor in 1 case, hence the efficacy rate was 97.6%. All of the 28 bacteria identified in these cases were eradicated after CFTM-PI treatments. No noticeable abnormalities were found as side effects. An elevation of eosinophil, an increase of platelet count and elevations of GOT and GPT were observed in 3 patients.
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PMID:[Bacteriological, pharmacokinetic and clinical studies on cefteram pivoxil in the pediatric field]. 281 Jul 43

Twenty five children were treated with rokitamycin (RKM) and its clinical efficacy and side effects were evaluated. Ages of the patients ranged from 13 days to 10 years. Doses of RKM ranged 17.1-39.3 mg/kg/day for 2.3 to 17.7 days. Twenty four patients including 8 Mycoplasma pneumonia, 5 bronchopneumonia, 6 bronchitis, 2 streptococcosis, 1 otitis media, 1 tonsillitis and 1 Chlamydia conjunctivitis were evaluated for clinical efficacy. Results were excellent in 7, good in 12, fair in 4, and poor in 1 patient. One patient was excluded from the evaluation, because the patient was treated with erythromycin before entering this study. Out of the 25 patients, 3 cases showed eosinophilia, 2 cases showed elevated GOT and GPT but no adverse clinical signs due to RKM were observed. The pharmacokinetics of RKM was studied in 5 patients whose ages ranged from 8 to 12 years. Plasma peak concentrations of RKM in 2 patients were 0.14 and 0.16 micrograms/ml at 30 minutes after doses of 5 mg/kg. Peak concentrations in 3 patients ranged from 0.32 to 1.02 micrograms/ml after doses of 10 mg/kg. Portions of the drug excreted into urine within 6 hours were 0.49 and 1.03% in 2 patients each of whom was given doses of 5 mg/kg, and ranged from 1.16 to 1.30% in 3 patients, each given 10 mg/kg. Metabolic products in urine within 4 hours after doses of 5 to 10 mg/kg were studied in 4 patients. Leucomycin A7 and leucomycin V accounted for almost 90% of all the related compounds excreted.
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PMID:[Clinical and pharmacokinetic evaluation of a +rokitamycin dry syrup in children]. 322 31

Preclinical and clinical studies were performed to evaluate usefulness and safety of aztreonam (AZT) in the treatment of acute otitis media, acute exacerbation of chronic otitis media and chronic otitis media and the following results were obtained. MICs for P. aeruginosa, P. mirabilis and P. inconstans isolated from the patients with suppurative otitis media were 1.56 micrograms/ml, less than or equal to 0.025 micrograms/ml and less than or equal to 0.025 micrograms/ml respectively in their peaks. In the intravenous injection of 1 g, AZT concentration in the mastoid cell mucosa was 7.52 micrograms/g on average and serum concentration 51.6 micrograms/ml sufficiently suggesting clinical efficacy of AZT. In the clinical trial by administering AZT 1-2 g/day for the patients with suppurative otitis media, effective rates were 2/3 (66.7%) for acute otitis media, 16/22 (72.7%) for acute exacerbation of chronic otitis media, 21/34 (61.8%) for chronic otitis media and 6/7 (85.7%) for cholesteatoma of the middle ear. Elimination rate of single Gram-negative pathogens was 82.1% in the bacteriological studies of AZT. As for abnormal laboratory findings, 7 cases showed GOT, GPT elevations. However, they were in minor degree and transient. Side effect was not noted except 1 case of flushing with itching. It was considered from the above results that AZT is a highly useful antibiotic for suppurative otitis media.
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PMID:[Efficacy evaluation of aztreonam for suppurative otitis media]. 351 6

Fundamental and clinical studies of cefixime (CFIX) granules, a new oral cephalosporin, were carried out with the following results: The MICs of CFIX against 234 clinical isolates were determined. Antibacterial activities of the drug against S. aureus, S. epidermidis and E. faecalis were weaker than those of conventional oral cephalosporins but antibacterial activities against Gram-negative bacteria were almost the same as those of cephem antibiotics of the Fujii's group 5. Peak serum concentrations of CFIX after oral doses of 3 and 6 mg/kg were, respectively, 1.51-4.86 micrograms/ml at 2-6 hours and 3.22-7.76 micrograms/ml at 4-8 hours. Serum concentrations of CFIX were dose-dependent in a patient given 3 and 6 mg/kg in a cross-over study. CFIX granules were administered mainly to children suffering from respiratory tract infection, otitis media and urinary tract infection at a dose of 3 mg/kg b.i.d. or t.i.d. for 3-27 days. The clinical responses to CFIX were excellent to good in 44 of the 50 children with infections, with an effectiveness rate of 88%. Thirty-five strains of the 40 clinical isolates were eradicated by the treatment with CFIX. The bacteriological eradication rate was 87.5%. Side effects observed were diarrhea and soft stool in 2 patients each, and elevated GOT X GPT and eosinophilia in 1 patient each. These symptoms and laboratory abnormalities disappeared on the day after the completion of therapy with CFIX. From the above results it has been concluded that CFIX is a useful and safe antibiotic for treating various bacterial infections in children.
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PMID:[Fundamental and clinical studies of cefixime granules in pediatrics]. 376 36


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