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)

Sulbactam/Ampicillin (SBT/ABPC), a combination at a fixed ratio of ABPC and SBT which is an irreversible inhibitor of beta-lactamase in a 2:1 ratio, was clinically evaluated for its efficacy and safety in 24 patients with ages from 5 month-old to 12 years old with bacterial infection. The results obtained are summarized as follows. 1. A pharmacokinetic study following 30 mg/kg SBT/ABPC administration by 30 minutes drip infusion or intravenous bolus injection showed that mean half-lives of SBT and ABPC were 48.9 minutes and 40.2 minutes, respectively, and mean urinary excretion rates of SBT and ABPC in the first 6 hours were 67.1% and 48.3%, respectively. 2. SBT/ABPC was administered to 14 patients with bronchopneumonia, 4 patients with tonsillitis, a patient each with acute upper respiratory infection, with submandibular lymphadenitis, with phlegmon, with enterocolitis, with pyelonephritis and with cystitis at a daily dosage of 88.2-133.3 mg/kg, divided into 3 or 4, by intravenous bolus injection or by 30 minutes drip infusion. Clinical responses of the 24 patients were as follows: excellent: 17 patients, good: 7 patients. The efficacy rate was 100%. 3. Neither clinical adverse reactions nor abnormal laboratory test values, except slight eosinophilia in a patient and an elevation of GOT, GPT in another were observed. 4. MICs of SBT/ABPC against 7 strong beta-lactamase producing strains isolated from some of the patients were as follows. MIC against a strain of Staphylococcus aureus was 3.13 micrograms/ml, MICs against 2 out of 5 strains of Branhamella catarrhalis were 0.10 microgram/ml and those of the remaining 3 strains were 0.20 microgram/ml. MIC against a strain of Haemophilus parainfluenzae was 3.13 micrograms/ml. 5. These data described above show that SBT/ABPC has excellent bactericidal capacity against beta-lactamase producing bacteria as well as beta-lactamase non-producing Gram-positive and negative bacteria and suggest that SBT/ABPC is a very useful antibiotic for pediatric patients.
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PMID:[Clinical evaluation of sulbactam/ampicillin in children]. 266 51

Fundamental and clinical studies were carried out with aztreonam (AZT), a new monocyclic beta-lactam antibiotic, in pediatric infections. Results were as follows. The mean half-lives in the vein blood were 1.09 hours, 1.18 hours, 1.22 hours after injection, when the doses were 10, 20 and 40 mg/kg, respectively. Dose response was observed. The average recovery rates in the urine between 0 and 6 hours were 40.2%, 42.3%, 50.8% when the doses were 10, 20 and 40 mg/kg, respectively. The antibacterial activity of AZT against 16 clinical isolates were determined in comparison with those of ABPC, CPZ, LMOX and CTX. Against 8 clinical isolates of E. coli and 3 of H. influenzae, the activity of AZT was equal or superior to that of CPZ, LMOX and CTX, and way by far superior to that of ABPC. Twenty-three pediatric patients received AZT in doses ranging from 48 to 79 mg/kg divided 3 times a day; 12 cases of urinary tract infection, 9 cases of respiratory tract infection and 2 cases of bacterial enterocolitis. The rate of clinical effectiveness was 100%. No side effect was observed. Slight elevation of GOT and GPT were observed in 2 cases, increase of platelet count in 2. All were considered to be transient and mild.
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PMID:[Fundamental and clinical studies of aztreonam in pediatric infections]. 409 58

Clinical trials were carried out with sulbactam/cefoperazone (SBT/CPZ) (combination ratio of 1:1) in pediatric infections. Results were as follows. The mean half-lives of SBT and CPZ in the serum following intravenous injection of SBT/CPZ were about 0.7 and 1.2 hours, respectively. Urinary excretions of SBT and CPZ within 6 hours after intravenous injection of SBT/CPZ were 81.9% and 28.1%, respectively. SBT/CPZ was administered to 33 pediatric patients with various infection; 18 respiratory tract infections, 12 urinary tract infections and 3 Salmonella enterocolitis. The overall efficacy rate was 87.9%. In particular, 7 of 8 urinary tract infections caused by beta-lactamase producing organisms were improved after administration of SBT/CPZ. Diarrhea in 8 and soft stool in 3 of 33 patients occurred, and slight elevation of GOT/GPT was observed in 2 patients.
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PMID:[Experimental and clinical studies of sulbactam/cefoperazone in pediatric field]. 609 64

Cefotiam (CTM) was evaluated for its safety and efficacy in children. Twenty-six patients were treated with 40 to 200 mg/kg per day of CTM by intravenous administrations. The diagnosis of the patients were acute pharyngitis (2), acute bronchitis (1), pneumonia (4), empyema (2), urinary tract infection (2), typhoid fever (1), acute enterocolitis (2), partially-treated purulent meningitis (1), and suspected septicemia in neuroblastoma (1); and the remaining ten patients were considered to have nonbacterial infections. The pathogens recovered were Streptococcus pyogenes (1), Streptococcus pneumoniae (1), Staphylococcus aureus (4), Haemophilus influenzae (4), Escherichia coli (1), enteropathogenic Escherichia coli (1), Salmonella typhi (1), and Campylobacter jejuni (1). All but two patients of bacterial infections were cured after the CTM therapy, and the rate of efficacy was 87.5%. Diarrhea (3), urticaria (1), transient elevation of GOT and GPT (1), and transient eosinophilia (3) were found to be associated with the CTM therapy. However, no severe adverse reactions were encountered. Half life of the serum CTM level was 0.93 +/- 0.13 hours, and excretion into the urine was rapid. CSF concentration obtained 1 hour after an intravenous injection of 21 mg/kg of CTM in a case with inflamed meninges was 1.5 mcg/ml, and the CSF/serum ratio was 9.0%. From these data, CTM appears to be a safe and effective antibiotic when used in children with susceptible bacterial infections.
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PMID:[Clinical evaluation of cefotiam therapy in children (author's transl)]. 627 Apr 13

Fundamental and clinical studies of ceftizoxime, a new cephalosporin antibiotic, in children led to the following results. 1. Ceftizoxime compared favorably with cefazolin (CEZ) and cefmetazole (CMZ) for in vitro activity against clinically isolated strains of Staphylococcus aureus (31 strains), Escherichia coli (29), Klebsiella pneumoniae (30) and Pseudomonas aeruginosa (16). While somewhat less active against S. aureus than CEZ and CMZ, ceftizoxime was far more active than these 2 cephalosporin antibiotics against the test strains of E. coli and K. pneumoniae, which included strains resistant to the 2 drugs. Ceftizoxime was not particularly active against Ps. aeruginosa, but this seeming disadvantage was offset by the absolute ineffectiveness of the 2 reference drugs on this obstinate organism. 2. The time course of mean serum ceftizoxime levels in 3 pediatric patients of 5--10 years old given a single intravenous dose of 20 mg/kg was as follows: 45.4 micrograms/ml at 15 minutes, 40.4 micrograms/ml at 30 minutes, 22.1 micrograms/ml at 1 hour, 10.4 micrograms/ml at 2 hours, 2.9 micrograms/ml at 4 hours and 0.9 microgram/ml at 6 hours. The mean serum half life was 1.12 hours. The mean urinary levels of ceftizoxime at serial 2-hour collection intervals were as follows: 2,477 micrograms/ml for 1--2 hours, 1,235 micrograms/ml for 2--4 hours and 462 micrograms/ml for 4--6 hours. The mean urinary recovery up to 6 hours was 61.0%. 3. The clinical response of 28 children with infection to ceftizoxime treatment was 'excellent' in 22 children, 'good' in 4, and 'poor' in 2. These children comprised 11 with acute pneumonia, 3 with acute bronchitis, 4 with acute pyelonephritis, 2 each with acute purulent arthritis and acute enterocolitis, and 1 each with acute purulent tonsillitis, acute purulent lymphadenitis, furunculosis, subcutaneous abscess, subdural abscess and sepsis. The overall rate of effectiveness was 92.9%. Successfully eradicated strains in the bacteriological sense consisted of 4 strains each of H. influenzae and E. coli, 1 strain each of P. morganii, S. pneumoniae and S. pyogenes, 1 of the 2 strains of S. enteritidis, and 1 of the 3 strains of S. aureus. The overall rate of bacteriological effectiveness was 81.3%. No clinical side effects were observed. Changes in laboratory test findings included slightly and transiently elevated GOT and GPT in 1 child and GOT alone in another child.
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PMID:[Fundamental and clinical studies on ceftizoxime in pediatric field (author's transl)]. 627 13

Laboratory and clinical studies on ceftazidime ( CAZ ), a new cephem antibiotic, were carried out in the field of pediatrics. The results were as follows: Antibacterial activities of CAZ against clinically isolated strains of S. pneumoniae, H. influenzae, E. coli and P. aeruginosa were compared with those of cefotaxime (CTX), ceftizoxime (CZX), latamoxef ( LMOX ), cefoperazone (CPZ) and cefmetazole (CMZ), and also with cefsulodin (CFS) and gentamicin (GM) against P. aeruginosa. Against S. pneumoniae and H. influenzae, CAZ was almost as active as CTX, CZX and CPZ. Against E. coli, it was almost as active as CTX, CZX and LMOX . Against P. aeruginosa, it was almost as active as CFS and GM. Serum concentrations and urinary excretion rates after intravenous bolus injection of CAZ at doses of 20 mg/kg and 10 mg/kg for 5 minutes in each 2 cases (4 cases in total) were determined. The mean serum concentrations of CAZ were 78.9 and 52.0 micrograms/ml at 15 minutes, 38.5 and 27.4 micrograms/ml at 1 hour, and 6.5 and 4.8 micrograms/ml at 4 hours, with serum half-lives (T 1/2) of 1.39 and 1.80 hours respectively. Mean cumulative urinary excretion rate within 6 hours after administration was 84.6%. In a patient with chronic renal failure, serum half-life was 3.22 hours and urinary excretion rate within 6 hours was 22.8% (after intravenous bolus injection of CAZ at a dose of 10 mg/kg). CAZ was administered at a dose of 55.5 mg/kg by intravenous bolus injection to a child with purulent meningitis. The levels of CAZ in the cerebrospinal fluid (CSF) at 1 hour after administration were 2.7-38.9 micrograms/ml with CSF/Serum ratios of 3.2-28.8%. Forty-two pediatric patients with various bacterial infections (pyelonephritis 14, tonsillitis 1, bronchopneumonia 3, pneumonia 17, purulent meningitis 1, bacteremia 2, SSSS 1, enterocolitis 3) were treated with CAZ at a daily dose of 49-222 mg/kg t.i.d. or q.i.d. (as a rule 60 mg/kg t.i.d.). The efficacy rate was 97.6% clinically and 97.8% bacteriologically. No adverse reactions were observed except 1 case with mild diarrhea. Abnormal laboratory findings were also only mild; eosinophilia in 1, slight elevation of GOT in 5 and that of GOT & GPT in 3 cases. These results indicate the usefulness of CAZ in the treatment of bacterial infections in children.
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PMID:[Laboratory and clinical studies on ceftazidime in the field of pediatrics]. 637 56

A new semisynthetic 1-oxa-beta-lactam derivative, 6059-S, was evaluated for its safety and efficacy in children. Twenty-five patients were treated with 10 to 274 mg/kg per day of 6059-S by intravenous administrations. The diagnosis of the patients were acute pharyngitis (2), acute bronchitis (2), pneumonia (4), pertussis (4), acute enterocolitis (2), recurrent urinary tract infection (2), suspected septicemia (3), and acute purulent meningitis (1); and the remaining 5 patients were considered to have nonbacterial infections. The pathogens recovered were Streptococcus pneumoniae (1), Haemophilus influenzae (4), Haemophilus parainfluenzae (1), Enterobacter cloacae (1), Enterobacter aerogenes (1), Proteus morganii (1), Psuedomonas aeruginosa (2) and Salmonella typhimurium (1). All the patients of bacterial infections were cured after the 6059-S therapy. However, Pseudomonas aeruginosa and Salmonella typhimurium were not eradicated after the 6059-S therapy, and the rate of bacterial disappearance was 75%. Diarrhea (3), precordial pain (2, only in cases with high-dose therapy), transient elevation of GOT and GPT (2), and transient eosinophilia (2) were found to be associated with the 6059-S therapy. However, no severe adverse reactions were encountered. Half life of the serum 6059-S level was 1.34 +/- 0.16 hours. CSF concentrations in a case with Haemophilus influenzae meningitis ranged 4.0 to 9.7 mcg/ml after an intravenous injection of 34.3 to 75 mg/kg of 6059-S. From the present study, 6059-S appears to be a safe and effective antibiotic when used in children with susceptible bacterial infections. It remains to be further determined whether 6059-S is superior to ABPC in the treatment of Haemophilus influenzae meningitis.
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PMID:[Clinical evaluation of 6059-S therapy in children (author's transl)]. 645 68

Cefotetan (CTT), a new cephamycin antibiotic having a long serum half-life (2.93 +/- 0.78 hours), was evaluated for its safety and efficacy in children. Twenty-four patients were treated with a daily dose of 30 to 100 mg/kg of CTT by intravenous administrations mostly in 2 divided doses. The diagnoses of the effective patients were acute bronchitis (5), pneumonia (4), acute urinary tract infections (4), acute enterocolitis (2), presumed septicemia (1), and phlegmon (1); and the effectiveness was 77.3%. The pathogens recovered from these patients were S. pneumoniae (1), H. influenzae (3), S. marcescens (1), E. coli (2), and K. oxytoca (1). CTT was not effective in staphylococcal pneumonia and empyema (each 1 case), in Pseudomonas pneumonia (2), and in a case of brain abscess and mastoiditis of unknown etiology. Diarrhea (2), and transient elevations of the serum GOT, GPT, and LDH (1) were associated with the CTT therapy, but no severe adverse reaction was encountered. The CSF level of CTT seemed to be lower among several new cephalosporins. From the present study, CTT appears to be a safe and effective antibiotic when used in children with susceptible bacterial infections. A twice-a-day schedule was recommended from its long serum half-life.
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PMID:[Clinical evaluation of cefotetan in pediatrics]. 658 31

We conducted clinical studies on cefozopran (CZOP), a newly developed parenteral cephalosporin, for its clinical application in the field of pediatrics. 1. A clinical study was performed on 16 children with infections, including 9 with pneumonia, 1 each with acute bronchitis, enterocolitis, purulent lymphadenitis, 4 with skin and soft tissue infections. CZOP was administered by 30 minutes intravenous drip infusion. Doses varying from 20 to 35 mg/kg body weight were given t.i.d. Lengths of treatment ranged from 4 to 14 days. 2. Clinical efficacies were excellent in 10 and good in 6 cases, with an efficacy rate of 100%. The overall bacterial eradication rate for the pathogenic bacteria was also 100%. 3. Side effect was noted in 1 case with skin rash. Abnormal laboratory test data were found in 5 cases including slight elevations of GPT in 4 cases and GOT in 2 cases.
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PMID:[Clinical studies on cefozopran in pediatrics]. 785 88

Helicobacter hepaticus has been associated with naturally occurring hepatitis in certain inbred strains of mice, and in A/JCr mice it has been linked to the development of hepatic adenomas and adenocarcinomas. H. hepaticus was orally inoculated into 30 axenic, outbred female mice, and the mice were studied longitudinally to fulfill Koch's postulates and to ascertain the pathogenic potential of the organism under defined germfree conditions. Ten cage contact mice were also housed in the same germfree isolator to study transmission patterns, and 10 germfree mice were maintained in separate isolators as controls. Mice serially euthanized from 3 weeks through 24 months postinoculation (p.i.) were surveyed by culture and PCR for H. hepaticus in liver and intestinal tissues. Tissues were analyzed for histopathological changes, and sera were assayed for the presence of immunoglobulin G antibody to H. hepaticus and changes in the liver enzyme alanine aminotransferase. Inoculated mice and cage contact mice were persistently infected with H. hepaticus as identified by culture and PCR, in both the intestine and, less frequently, the liver, for the duration of the 2-year study. Animals developed persistent chronic hepatitis, and in some animals enterocolitis was noted. Hepatocellular carcinoma was diagnosed in one H. hepaticus-infected mouse. The level of H. hepaticus serum antibody was highest in experimentally infected mice at 12 to 18 months p.i.; this corresponded in general to the time interval when the highest levels of alanine aminotransferase were recorded. Although cage contact mice became persistently infected with H. hepaticus, lesions were less severe and the levels of serological biomarkers utilized in the study were lower. The H. hepaticus-infected mouse will provide an ideal model to study putative bacterial virulence determinants and how they interact with the host to induce chronic inflammation and tumorigenesis.
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PMID:Persistent hepatitis and enterocolitis in germfree mice infected with Helicobacter hepaticus. 875 16


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