Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:2.6.1.2 (alanine aminotransferase)
26,722 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

PC-904 was administered to 16 pediatric patients and the following basic and clinical results were obtained. (1) PC-904 was administered 20 approximately 30 mg/kg. The serum peak level of PC-904 after drip intravenous infusion over 1 hour was 66.7 microgram/ml at 1 hour and T 1/2 of PC-904 was 67.8 minutes. PC-904 was administered 25 approximately 30 mg/kg intravenous one shot injection was 49.4 microgram/ml at 1 hour and T 1/2 of PC-904 was 52.2 minutes. (2) Urinary excretion rate was about 20% up to 6 hours after drip intravenous infusion of 20 mg/kg. In a case of intravenous one shot injection of 25 approximately 30 mg/kg, the excretion rate was 11.9 approximately 19.9%. (3) PC-904 was administered 60 approximately 120 mg/kg/day for 3 approximately 48 days to 5 cases of sepsis and bacterial endocarditis, 6 of pneumonia, 2 of sss syndrome (staphylococcal scald skin syndrome) and 3 of pyelonephritis. Clinical effects were excellent in 11 cases and good in 5 cases, effective ratio being 100%. (4) Pseudomonas aeruginosa, Staphylococcus epidermidis, Streptococcus viridans, Acinetobacter anitratus and Hemophilus influenzae isolated from clinical specimens disappeared by the treatment of PC-904, and Hemophilus influenzae isolated from clinical specimens disappeared by the treatment of PC-904. Escherichia coli and Klebsiella pneumoniae reduced. (5) As to the side effect by PC-904, s-GOT and s-GPT were elevated in 2 cases. Anemia, rash and fever were observed in each 1 case out of 16 patients though the causal relation with the agent was unknown.
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PMID:[Basic and clinical studies on new semisynthetic penicillin, PC-904, in pediatric field (author's transl)]. 69 Dec 65

Incubation of rat brain 4-aminobutyrate aminotransferase with 4-amino-hex-5-enoic acid, a substrate analog of 4-aminobutyric acid, results in a time-dependent irreversible loss of enzymatic activity. In the presence of 0.1 mM inhibitor the half-life of the inactivation process is approximately 6 min. Low concentrations of L-glutamic acid or 4-aminobutyric acid protect against this inactivation, while 2-oxoglutarate prevents this protection, suggesting that only the pyridoxal form of the enzyme is susceptible to inhibition by 4-amino-hex-5-enoic acid. The irreversible inhibition of mammalian 4-aminobutyrate aminotransferase by 4-amino-hex-5-enoic acid is selective. There is no inhibition of this enzyme from Pseudomonas fluorescens with the inhibitor at mM concentrations. Even at 10 mM there is no irreversible inhibition of mammalian glutamate decarboxylase or of aspartate aminotransferase, while alanine aminotransferase is inhibited over 500 times more slowly than rat brain 4-aminobutyrate transaminase.
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PMID:4-amino-hex-5-enoic acid, a selective catalytic inhibitor of 4-aminobutyric-acid aminotransferase in mammalian brain. 85 82

Sublethal doses of vincristine (VNC) and bacterial lipopolysaccharide (LPS) administered simultaneously to adult male mice resulted in markedly enhanced mortality. All of 10 strains of Pseudomonas aeruginosa tested, 4 of 7 strains of Bacteroides, and 6 of 10 strains of Listeria monocytogenes were able to substitute for purified LPS in enhancing mortality in VNC-treated mice. Inoculation of mice with each of 10 strains of Pseudomonas, each of 7 strains of Bacteroides, and about half of the 10 strains of Listeria tested elicited increased resistance to the lethal action of purified LPS. The patterns of responses of mice receiving a lethal combination of 2 mg of LPS/kg and 1 mg of VNC/kg resembled those of mice receiving a lethal dose of 10 mg of VNC/kg alone or 15 mg of LPS/kg alone with respect to (i) serum glutamic pyruvate transaminase activity, (ii) hematocrit values, and (iii) thrombocytopenia. The patterns of responses of mice receiving a lethal combination of LPS and VNC resembled those of mice receiving a lethal dose of LPS alone with respect to (i) hypothermia, (ii) retention of sulfobromophthalein, (iii) fibrinogen level, (iv) prothrombin activity, (v) blood urea nitrogen levels, and (vi) time of death. These data are consistent with the proposition that the combination of VNC and LPS produces a fatal renal failure. Histological studies confirmed that there was extensive renal damage in mice treated with lethal doses of LPS alone or a lethal combination of LPS and VNC.
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PMID:Enhanced toxicity for mice of combinations of bacterial lipopolysaccharide and vincristine. 94 80

Gentamicin (GM), one of the amino-glucosides, was administered intramuscularly to 27 patients with Pseudomonas and/or other antibiotics resistant infections. The clinical evaluation of the results obtained was classified excellent in 1 case good 6, fair 8, none 11 and indeterminate 1, the effectiveness accounting for 57.7 percent. Satisfactory results were noted in wound infections, peritonitis and urinary tract infections. Among untoward side effects, an elevation in GOT and GPT values was observed in 6 cases, an elevation of BUN value in 1, proteinuria in 1 and hematuria in 1. However, it is difficult to conclude that those side effects were attributable to GM itself because blood transfusion or combined therapy with anti-cancer agents was conducted in these cases during the GM therapy.
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PMID:[A clinical study on gentamicin in the field of surgery]. 127 81

Eighteen immuno-compromised children (malignancies, hematological diseases, collagen diseases) with neutropenia and infections were treated with imipenem/cilastatin sodium (IPM/CS), and the efficacy and the safety of the drug were evaluated. 1. Responses to IPM/CS were excellent in 13 patients, good in 1, and fair in 4. None of the patients displayed a poor response to the treatment thus the efficacy rate was 77.8%. 2. Of 5 patients with sepsis, 4 had excellent or good responses. IPM/CS was effective against sepsis caused by Enterococcus faecalis and Pseudomonas aeruginosa. 3. In patients with severe neutropenia (WBC less than 100/mm3), the efficacy rate was 70%. 4. As for side effects, elevations of GOT and GPT were observed in 1 patient with liver cirrhosis. These results indicate that IPM/CS is safe and effective in immuno-compromised children with neutropenia and infections.
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PMID:[Clinical evaluation of imipenem/cilastatin sodium against infections in compromised children (malignancy, hematological disease, collagen disease)]. 143 90

Panipenem/betamipron (PAPM/BP) is a combination drug of PAPM, a new parenteral carbapenem antibiotic and BP, an amino acid derivative at a weight ratio of 1:1. Its in vitro antibacterial activities against clinically isolated respiratory pathogenic bacteria were determined. It was superior to imipenem (IPM) in the in vitro antibacterial activities against Haemophilus influenzae, Haemophilus parainfluenzae, Branhamella catarrhalis, Staphylococcus aureus including MRSA, Klebsiella pneumoniae, Serratia marcescens and Escherichia coli. PAPM had antibacterial activities almost equal to those of IPM against Streptococcus pneumoniae and Enterococcus spp. Against Pseudomonas aeruginosa, however, its antibacterial activity was about 1/4 that of IPM. The clinical usefulness of PAPM/BP was studied by dissolving it in a solution containing lactate and administering the solution by intravenous drip infusion to 12 cases of respiratory tract infections. Out of 11 cases with respiratory tract infections excluding cytomegalovirus pneumonia, the efficacy rate was 90.9%, with 4 cases of excellent and 6 cases of good responses. In terms of its bacteriological efficacies, eradication of pathogenic bacteria including super-infection were observed in 2 out of 4 strains, but 2 strains of P. aeruginosa remained unchanged. Six strains appeared as superinfected bacteria during and after administration of this preparation substituting original pathogens. Side-effects were not observed in the 12 cases, and in laboratory tests, slight transient increases of S-GOT and S-GPT were found in 1 case. In conclusion, PAPM/BP is a very useful parenteral antibiotic against respiratory tract infections and can be one of the drugs of the first choice.
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PMID:[A study on in vitro antibacterial activity and clinical usefulness in respiratory tract infections of panipenem/betamipron, a newly synthesized carbapenem antibiotic]. 161 67

Cefpirome (CPR, HR 810) was clinically evaluated for its efficacy and safety in 11 patients with ages from 4 months to 11 years with bacterial infection. The results obtained are summarized as follows. 1. CPR was administered to 6 patients with bronchopneumonia, a patient with pneumonia, a patient with tonsillitis, 2 patients with acute pharyngitis and a patient with suppurative parotitis at daily dosage levels ranging 55.5-91.7 mg/kg, divided into 3 using intravenous bolus injection or 30 minutes drip infusion. Clinical responses of the 11 patients were as follows: excellent; 8 patients, good; 2 patients, poor; 1 patient, hence the efficacy rate was 90.9%. 2. Neither clinical adverse reaction nor abnormal laboratory test value was observed except slight elevation of GOT and GPT in a patient and leukopenia in another. 3. MICs of CPR against 18 beta-lactamase producing strains isolated from patients were as follows. MIC against a strain of Staphylococcus aureus was 1.56 micrograms/ml, MICs against 3 strains of Klebsiella pneumoniae were less than 0.025 microgram/ml, those against 3 out of 5 strains of Enterobacter cloacae were less than 0.025 microgram/ml and those against the remaining 2 strains were 0.05 and 0.20 micrograms/ml. MICs against 2 out of 3 strains Acinetobacter lwoffi were 1.56 micrograms/ml, and that of the remaining 1 strain was 0.39 microgram/ml. MICs against 2 strains of Pseudomonas cepacia were 1.56 micrograms/ml. MICs against a strain of Pseudomonas putida and a strain of Citrobacter diversus were 0.78 and less than 0.025 microgram/ml, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Clinical evaluation of cefpirome in children]. 188 Sep 23

Cefpirome (CPR, HR 810), a new parenteral cephalosporin antibiotic, was studied for its pharmacokinetics, bacteriological and clinical effects in the field of pediatrics. 1. CPR was very active against Staphylococcus aureus, Staphylococcus epidermidis, Coagulase-negative staphylococci, Streptococcus pneumoniae among Gram-positive cocci. Antibacterial activities of CPR were also strong against Branhamella catarrhalis, Haemophilus influenzae, Escherichia coli, Salmonella sp., Klebsiella oxytoca, Enterobacter cloacae, Pseudomonas aeruginosa among Gram-negative rods. 2. The plasma concentration 15 minutes after a bolus intravenous injection of 20 mg/kg was 80.4 micrograms/ml, and the T 1/2 (beta) was 1.03 hours. Plasma concentrations after intravenous drip infusion over 30 minutes of 20 mg/kg and 25 mg/kg were 48.3 and 117 micrograms/ml at the end of infusion, and T 1/2 (beta) for these dosage were 1.14 and 1.45 hours. 3. The urinary recovery rates over 6 hours after administration were 45.2-63.9% for CPR. 4. Clinical efficacies of CPR were excellent in 31 patients and good in 30 patients with an efficacy rate of 98.4%. In bacteriological examinations, causative organisms were eradicated with an eradication rate of 95.7%. 5. As side effects, diarrhea was observed in 5 patients and loose stool in 1 patient with an incidence of 8.2%. Abnormal values were found in some patients in clinical laboratory tests for eosinophilia, thrombocytosis and an elevation of GOT, GPT and triglyceride. These findings indicate that CPR will be useful against bacterial infections in pediatrics.
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PMID:[Pharmacokinetic and clinical studies on cefpirome in pediatrics]. 204 Nov 58

Decamethoxin is shown to be able to increase membrane permeability of Pseudomonas aeruginosa, Escherichia coli and Micrococcus lysodeikticus, that is confirmed by a loss of compounds with the absorption maximum at 260 nm by cells. Parallel with this the number of viable individuals has fallen and activity of dehydrogenases has been inhibited. The aspartate and alanine aminotransferase activity was not inhibited by decamethoxin and even increased. Decamethoxin lysed the protoplasts of the tested microorganisms. At high decamethoxin concentrations (over 500 micrograms/ml for P. aeruginosa and over 200 mu/ml--for E. coli) the outflow of components from the cells of gram-negative bacteria ceased, that may be associated with the coagulation changes in the cytoplasm. A loss of the low-molecular components by M. lysodeikticus cells and lysis of protoplasts proceeded less intensely than the same processes in the gram-negative microorganisms, that is explained by a less resistance of M. lysodeikticus to decamethoxin and earlier coagulation of the cytoplasm preventing lysis.
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PMID:[The effect of dexamethoxin on the integrity of cytoplasmic membrane in gram-positive and gram-negative microorganisms]. 212 May 53

Clinical evaluation, safety and kinetics in serum of sulbactam/cefoperazone (SBT/CPZ) in patients with lower respiratory tract infections have been studied in a multicenter trial participated by 28 institutions in Kyushu area during a period of 13 months from March 1987 to March 1988. 1. Mean peak serum levels of SBT and CPZ in 35 patients up to 4 hours after intravenous infusion of 2 g of SBT/CPZ were 38.2 +/- 17.3 micrograms/ml for SBT and 104.3 +/- 31.4 micrograms/ml for CPZ. Serum half-lives of SBT and CPZ were 0.76 hour and 1.53 hours, respectively. These results were in similar ranges to those reported elsewhere for SBT/CPZ. 2. Serum half-lives of SBT and CPZ after intravenous infusion of 2 g of SBT/CPZ were not significantly prolonged in patients with moderate liver or kidney dysfunctions. 3. Clinical efficacy rates of SBT/CPZ in 217 patients were 93.1% (81/87) for pneumonia, 93.3% (14/15) for lung abscess, 78.9% (15/19) for acute exacerbation of chronic bronchitis, 57.1% (4/7) for diffuse panbronchiolitis, 72.4% (21/29), 74.4% (32/43) and 100% (9/9) for infections concurrent to bronchiectasis, chronic respiratory disease and pulmonary emphysema, respectively. Those were 50% (1/2) for bronchitis associated with lung cancer and 66.7% (4/6) for empyema. The overall efficacy rate was 83.4% (181/217). 4. Clinical efficacy rate of SBT/CPZ for pneumonia in patients with underlying diseases such as lung cancer, pulmonary tuberculosis and pneumoconiosis, etc, was 85.3% (29/34) and was not significantly different from the efficacy rate of 98.1% (52/53) in patients without these underlying diseases. 5. Of 30 patients who failed to respond of previous antibiotic treatments, 21 were effectively treated by SBT/CPZ. 6. Bacteriological eradication rates against Pseudomonas aeruginosa, Haemophilus influenzae and Streptococcus pneumoniae were 42.9% (9/21), 87.5% (14/16) and 100% (5/5), respectively. The overall eradication rate in all cases including polymicrobial infections was 72.8% (67/92). 7. The high levels of peak serum concentration of CPZ, and the difference between serum levels of SBT and of CPZ seemed to contribute to the high clinical efficacy. 8. Adverse reactions occurred in 2.8% (6/217) of the patients, and consisted primarily of rash and diarrhea. Laboratory abnormalities were observed in 8 patients during the study. These were elevations of S-GOT and S-GPT, and eosinophilia. 9. SBT/CPZ is a very useful drug in the treatment of lower respiratory tract infections as it has become available just in time when increase in resistant organisms to beta-lactams is notable.
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PMID:[Clinical evaluation of sulbactam/cefoperazone in lower respiratory tract infections]. 219 54


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