Gene/Protein Disease Symptom Drug Enzyme Compound
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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

The basic and clinical studies of cefotiam (CTM) in pediatric infections were carried out, and the following results were obtained: 1. The antibacterial activity of CTM against S. aureus was equal or slightly less than that of cefazolin (CEZ). Those of CTM against E. coli and K. pneumoniae were eight times more active than those of CEZ. 2. CTM 20 mg/kg was administered wither by 30 minutes or 1 hour intravenous drip infusion. The peak serum levels were obtained at the end of each drip infusion, with the mean peak levels being 44.8 and 41.4 mcg/ml respectively. The serum levels at 1.5 and 2 hours after drip infusion were 2.8 and 2.2 mcg/ml respectively, and at 3.5 and 4 hours after drip and 4 hours after drip infusion were 0.3 and 0.7 mcg/ml respectively. The half lives were 0.62 and 1.15 hours, respectively. The mean urinary excretion over 6 hours were 52.8% in ;the 30 minutes drip infusion group and 42.6% in the 1 hour drip infusion group. 3. Clinical efficacy was evaluated in sixteen cases suffering from tonsillitis (4 cases), pneumonia (4), bronchitis (2), cervical lymphadenitis (2), purulent meningitis (2), suppurative arthritis (1) and suspected sepsis (1). Good and excellent responses were obtained in 15 of 16 cases (93.8%). Bacteriological response in the form of eradication was noted in 4 of 6 cases. Side effect observed was rash in 1 case, and laboratory abnormalities were elevation of BUN in 1 case and elevation of GPT in 2 cases.
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PMID:[Basic and clinical studies of cefotiam in pediatric field (author's transl)]. 627 Apr 19

Pharmacokinetics of ceftizoxime (CZX), a new cephalosporin antibiotic, was investigated in 9 children with normal renal and hepatic function. In addition, the clinical effect of CZX was evaluated in 26 pediatric patients with various infections. In 4 of the 9 children with normal renal and hepatic function, intravenous bolus injection of CZX in a dose of 20 mg/kg yielded a mean peak serum level of 36.5 micrograms/ml at 1/2 hour after infusion, and mean serum levels of 12.5 micrograms/ml at 2 hours and 6.0 micrograms/ml at 4 hours after infusion. The biological half-lives of CZX were estimated to be 1.25--2.55 hours. In another child, serum levels of CZX at 1/2, 2 and 4 hours after intravenous bolus injection in a dose of 10 mg/kg were 19.60, 5.96 and 2.06 micrograms/ml, respectively. The clear difference in dose response between 20 mg/kg and 10 mg/kg reflected the doubled dose levels. In the remaining 4 children, drip infusion of CZX in a dose of 20 mg/kg (1 child 17 mg/kg) over 0.5--1.5 hours yielded peak serum levels at the end of infusion. The biological half-lives of CZX were estimated to be 0.95--1.50 hours. About 80% of CZX was excreted in the urine within 6 hours after infusion in the 4 children tested. Twenty-six pediatric patients with various infections were treated with CZX intravenous doses of 20 mg/kg to 118 mg/kg b.i.d.--q.i.d. for 3--14 days. Of the 12 patients with acute bronchitis and pneumonia, 5 showed excellent response, 6 good and 1 fair response. Of the 5 patients with urinary tract infection, 4 showed excellent response and 1 good response. One patient each with colitis, tonsillitis and facial cellulitis, pharyngitis showed excellent response and 1 patient each with purulent thyroiditis and gluteal abscess showed good response. The single patients with sepsis showed excellent response. One patient each with pyothorax, purulent arthritis and cerebral abscess showed poor response. Overall effectiveness rate was 84.6%. although 22 of all 26 patients treated had serious underlying diseases such as APL, AML. A mild increase in GOT and GPT was observed in 1 patient during treatment with CZX, and the values returned to normal after discontinuation of the drug. These results suggest that ceftizoxime is 1 of the most important antibiotics for treating a wide range of infections in children as well as in adults.
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PMID:[Pharmacokinetics and clinical evaluation of ceftizoxime (author's transl)]. 627 8

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

Clinical studies in the field of pediatrics have been carried out with cefmenoxime (CMX), a new cephalosporin antibiotic and the following results were obtained. 1. CMX was administered intravenously by drip infusion in 23 patients with infectious diseases. These diseases consist of 10 pneumonia, 1 bronchitis, 6 upper respiratory tract infections, 2 acute pyelitis, 3 other urinary tract infections and 1 Douglas abscess. CMX was effective in all cases except 1 case of pneumonia with pyothorax. 2. No side effects have been observed in all cases. As for abnormal laboratory findings, 2 cases of eosinophilia, slight elevations of GOT in 3 cases and GPT in 2 cases were seen.
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PMID:[Clinical studies on cefmenoxime in the pediatric field]. 630 36

Cefotaxime (CTX) was used for 129 cases in respiratory tract and other infections; 57 cases of pneumonia, 20 cases of bronchopneumonia, 20 cases of acute bronchitis, 14 cases of chronic bronchitis, 7 cases of acute exacerbation of bronchiectasia or pulmonary emphysema, 4 cases of suppurative diseases of the lung, 1 case of pyothorax, 1 case of retropharyngeal abscess, 3 cases of pleurisy and 1 case of urinary tract infection. (A case was excepted on clinical evaluation.) CTX was administered by intravenous injection or drip infusion at a daily dose ranging from 0.5 to 8 g, for a term of 2 to 61 days. The total dose patients received ranged from 3 to 226 g. The results obtained were as follows. Clinical effects; excellent in 45 cases, good in 63 cases, fair in 9 cases, poor in 7 cases and unevaluable in 4 cases. The efficacy rate was 87.1% (108/124). Bacteriological effects; eliminated in 30 cases, decreased in 8 cases, unchanged in 2 cases and replaced in 1 case. The elimination rate was 75.6% (31/41). Side effects and abnormal laboratory findings; general itching, fatigue in lower extremities and albuminuria in 1 case each, and anemia in 2 cases. Increased number of eosinophiles and elevated GOT in 1 case each, elevated GOT and GPT in 3 cases and elevated GOT, GPT and A1-P in 2 cases. These symptoms or abnormal laboratory findings disappeared after the discontinuation or termination of CTX therapy. In view of the above, CTX may be considered to be a clinically useful antibiotic against respiratory tract infections.
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PMID:[Clinical evaluation of cefotaxime in internal medicine]. 631 10

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

T-1982 (cefbuperazone), a new cephamycin antibiotic, was basically and clinically studied in the field of pediatrics, and the following results were obtained. 1. The antibacterial activity of T-1982 was compared with that of CEZ, CMZ and ABPC. T-1982 was more active than the other drugs against Gram-negative bacteria, the sensitivity of E. coli (22 strains), K. pneumoniae (18 strains), P. mirabilis (19 strains), P. vulgaris (4 strains), P. morganii (5 strains) and K. oxytoca (4 strains) distributing less than 0.39, 0.1, 1.56, 0.39, 6.25 and 0.2 microgram/ml, respectively. Two of 3 strains of C. freundii were inhibited by 12.5 micrograms/ml. Against Gram-positive bacteria, the activity of T-1982 was inferior to that of the other drugs. S. pyogenes (28 strains) were inhibited by 0.78 microgram/ml or less, but the sensitivity of S. aureus (34 strains distributed 12.5-100 micrograms/ml). 2. T-1982 was administered to each 3 children at a dose of 20 mg/kg by one shot intravenous injection or 1 hour drip infusion, or at dose of 40 mg/kg by 1 hour drip infusion. The mean serum levels at 0.25, 0.5, 1, 2, 4 and 6 hours after one shot intravenous injection of 20 mg/kg were respectively 74.3, 56.3, 42.3, 17.6, 5.7 and 1.2 micrograms/ml with the mean half-life of 1.01 hours. The values were 32.9, 50.0, 73.7, 27.5, 12.4 and 4.5 micrograms/ml and 1.31 hours by intravenous drip infusion of 20 mg/kg and 50.4, 104.7, 136.3, 62.3, 18.6 and 6.9 micrograms/ml and 1.16 hours by intravenous drip infusion of 40 mg/kg. The mean urinary recovery rates within 6 hours were 47.7, 67.6 and 60.9%, respectively. 3. Treatment with T-1982 was made in 28 cases of pediatric infections; 1 case of acute bronchitis, 19 cases of acute bronchopneumonia or lobar pneumonia, 2 cases of acute purulent cervical lymphadenitis, 4 cases of acute pyelonephritis and each 1 case of subcutaneous abscess and suspected bacterial endocarditis. The clinical responses assessed in 27 cases were excellent in 21 cases, good in 5 cases and poor in 1 case, the efficacy rate being 96.3%. Bacteriologically, 2 strains of S. aureus, 3 strains of S. pneumoniae, 4 strains of H. influenzae, 2 strains of E. coli and 1 strain of P. mirabilis were eradicated. One strain of S. faecalis was reduced. No side effects were observed in any cases. Slight elevation of GOT and GPT and that of GOT were noted in each 1 case.
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PMID:[Basic and clinical studies on T-1982 (cefbuperazone) in the field of pediatrics]. 634 36

T-1982 (cefbuperazone), a new injectable cephamycin antibiotic, was studied for its antibacterial activity, concentration in serum and urine, penetration into cerebrospinal fluid (CSF) as well as clinical application. The following results were obtained. 1. Antibacterial activity: The susceptibilities of clinically isolated K. pneumoniae, E. coli and E. cloacae to T-1982 were superior to those of CEZ CMZ, and ABPC. T-1982 seemed to be useful for various infections due to Gram-negative rods. 2. Concentration in serum and urine: Subjects were 10 children with congenital heart failure but no abnormal renal and liver functions. T-1982 was given intravenously to 3 groups at 200 mg/kg by one shot (4 cases), 20 mg/kg by 1 hour drip infusion (3 cases) and 10 mg/kg by 1 hour drip infusion (3 cases). The half-lives were 60, 78 and 85 minutes, respectively. 3. Penetration into cerebrospinal fluid: Three children with malignant tumor were injected 20 mg/kg intravenously. A small amount of T-1982 was penetrated into CSF. 4. Clinical efficacy: T-1982 was administered daily 40-116 mg/kg t.i.d. or q.i.d. for 2-14 days to 17 children comprising 1 bronchopneumonia, 1 bronchitis, 4 tonsillitis, 1 lymphadenitis, 1 sepsis, 1 pharyngitis, 1 impetigo, 1 acute sinusitis and 6 pyelonephritis. Clinical efficacy was excellent in 10, good in 2, fair and poor in 3, and the efficacy rate was 70.6%. Bacteriological effect was as follows; eradicated in 9 cases and unknown in 8 cases. As side effect, GOT and GPT elevations unrelated to the drug were observed in 2 cases. Other abnormal findings were not found. T-1982 seems to be safe antibiotic in the field of pediatrics.
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PMID:[Fundamental and clinical studies on T-1982 (cefbuperazone) in the field of pediatrics]. 634 37

Ceftazidime ( CAZ ) is a newly developed cephalosporin. Clinical studies on this drug was carried out and the results were as follows. Twenty-nine patients (acute purulent tonsillitis 2, acute bronchitis 1, pneumonia 15, acute purulent lymphadenitis 2, pyoderma 1, skin abscess 2 and urinary tract infection 6) were treated with CAZ in doses of 42-1 mg/kg (mean 59 mg/kg) divided 2-3 times per day for 3-10 days (mean 5.7 days) intravenously. The overall efficacy rate was 96.6%. As to adverse reaction, drug fever was observed in 1 patient. Abnormal laboratory data were noted in 4 cases (elevation of serum GOT, GPT and BUN in 1, elevation of serum GOT and GPT in 1, elevation of BUN in 1 and leukopenia in 1).
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PMID:[Clinical studies on ceftazidime in the pediatric field]. 637 48


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