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

Pharmacokinetics and clinical studies of imipenem/cilastatin sodium (IPM/CS), a combined preparation of a new carbapenem antibiotic and a dehydropeptidase-I inhibitor, respectively, were carried out in neonates and premature infants in a joint study by a co-research group. 1. Peak blood levels of IPM/CS when administered at 10 mg/10 mg/kg or 20 mg/20 mg/kg by 30- or 60-minute intravenous drip infusion were achieved at the end of infusion. A dose response was clearly observed between the doses and the peak levels achieved. 2. The areas under the blood concentration time curve (AUC) of CS were greater than those of IPM in most patients. Blood half-lives of IPM and CS tended to be longer in younger neonates and premature infants than in older subjects. The blood half-life of CS tended to be longer than that of IPM. 3. Cumulative urinary recovery rates of CS were greater than those of IPM, cumulative urinary recovery rates tended to be greater in older neonates and premature infants than younger subjects. 4. One hundred and thirteen patients were treated for bacterial infections with IPM/CS and 32 patients were treated prophylactically. Daily doses of IPM/CS ranged from 9 mg/9 mg/kg to 150 mg/150 mg/kg. 5. Clinical efficacies of IPM/CS were evaluated in a total of 56 patients with identified etiologic pathogens. The efficacy rate was 98.2% with 33 patients rated as excellent, 22 patients as good and 1 patient as fairly good. (Diagnoses were sepsis in 10 patients and meningitis in 2 patients, etc.) Fifty-seven patients with no identified etiologic pathogens were rated as excellent for 22 patients, good for 34 patients and fairly good for 1. The efficacy rate in these patients was 98.2%. Thirty-two patients were treated prophylactically and the results obtained were satisfactory. 6. Bacteriologically, the eradication rate was 94.5% in 56 patients; i.e., 52 were eradicated, 2 were decreased, 1 persisted and 1 was unknown. 7. Adverse effects were observed in 7 (4.4%) of 160 patients, i.e., 2 patients had diarrhea and 2 patients had rash, etc. Abnormal laboratory data considered related to the therapy occurred in 28 (17.6%) of 159 patients, with 10 patients with eosinophilia (6.3%) and elevation of GOT and/or GPT, etc. All these were non serious, and all values returned to normal after discontinuance of therapy. An abnormal prothrombin (PIVKA II) was observed in 1 of 10 patients tested.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Pharmacokinetic and clinical evaluation of imipenem/cilastatin sodium in neonates and premature infants. A study of imipenem/cilastatin sodium by a perinatal co-research group]. 267 29

Imipenem-cilastatin was evaluated for tolerability and efficacy in a multicenter open, noncomparative trial involving 178 infants and children with bacterial infections. Imipenemcilastatin was administered in total daily dosages of 100 mg/kg for patients up to 3 years of age and 60 mg/kg for those more than 3 years of age. Favorable clinical response was achieved in 98 of 100 patients judged evaluable for efficacy. Adverse effects were generally mild and reversible and included diarrhea alone or with vomiting (5.1%), irritation of intravenous infusion site (3.3%) and rash (2.2%). Changes in laboratory test values reported most frequently were thrombocytosis (8.9%), elevations in aspartate aminotransferase (7.9%) and alanine aminotransferase (5.6%) and eosinophilia (8.4%). This safety profile appears to be comparable to that of other beta-lactam antibiotics. Moreover imipenem-cilastatin was effective in infections caused by a broad spectrum of pathogens that include Haemophilus influenzae, Staphylococcus aureus, P. aeruginosa and anaerobes. These attributes suggest that imipenem-cilastatin should be safe and effective in selected pediatric patients.
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PMID:Imipenem-cilastatin in pediatric patients: an overview of safety and efficacy in studies conducted in the United States. 268 88

Intravenous administration of sulbactam/ampicillin (SBT/ABPC) was evaluated in pediatric patients. The serum half-lives of both ABPC and SBT were approximately 1 hour following the intravenous injection or intravenous drip infusion of 20-35 mg/kg, and 30-50% of ABPC and 30-70% of SBT were recovered in the urine 6 hours. Cerebrospinal fluid concentrations of ABPC and SBT were 0.76 and 0.68 micrograms/ml, respectively, at 1 hour after intravenous drip infusion of the 58 mg/kg, and concentration ratios of the drugs in cerebrospinal fluid/serum were 6.39 and 5.71%, respectively. Thirty-four pediatric patients were treated with intravenous drip infusion of SBT/ABPC in doses ranging from 54 to 150 mg/kg divided into 3 times a day. The rate of clinical efficacy was 93.5% and the bacterial elimination rate was 92.3%. The synergistic activity of sulbactam with ampicillin was demonstrated against beta-lactamase-producing Staphylococcus aureus and Haemophilus influenzae isolated from patients in the present study. The side effects of SBT/ABPC were observed in 6 patients (5 diarrheas; 1 diarrhea with vomiting) out of 34 patients administered. Eosinophilia (2 patients) and a slight elevation of GOT (1 patient), GPT and LDH (1 patient) were observed. The tolerance to the therapy, however, was good.
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PMID:[Clinical and pharmacokinetic studies on intravenous administration of sulbactam/ampicillin in pediatrics]. 274 46

Laboratory and clinical studies of sulbactam/ampicillin (SBT/ABPC) in children have been carried out, and the following results were obtained. 1. Antibacterial effect MICs of SBT/ABPC were only one-tube less than or similar to those of ABPC against susceptible organisms. Against ABPC-resistant organisms at the inoculum size of 10(8) cells/ml however, SBT/ABPC was superior to ABPC when evaluated in terms of their MIC values. When MICs of SBT/ABPC were compared to those of ABPC against organisms with high beta-lactamase producing activities, it was found that many of ABPC-resistant organisms were much susceptible to SBT/ABPC. 2. Absorption and urinary excretion In 2 cases to which 50 mg/kg and 20 mg/kg SBT/ABPC were respectively given over 30 minutes by drip infusion, peak serum levels were obtained at the end of the drip infusion with peak levels of SBT of 45.5 micrograms/ml, 12.5 micrograms/ml, respectively and those of ABPC of 83.0 micrograms/ml, 22.9 micrograms/ml, respectively. The half-lives of SBT and ABPC were 0.94 hour and 0.98 hour, respectively. The mean urinary excretion rates in the first 6 hours after the end of administration were 84.4% for SBT and 63.1% for ABPC. 3. Clinical results Clinical efficacies were evaluated in 24 cases including 9 cases of pneumonia, 2 cases of upper respiratory infection, 7 cases of urinary tract infection and 1 case each of bronchopneumonia, pyothorax, tonsillitis, streptococcal infection, ++ phlegmon and staphylococcal scalded skin syndrome. Clinical efficacies were excellent or good in 19 cases with an overall efficacy rate of 86.4%. Adverse effect was found in 1 case with nausea and vomiting, and abnormal laboratory test values observed were 2 cases each of eosinophilia, slight elevation of GOT and GPT and elevation of LDH, but they were not serious.
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PMID:[Pharmacokinetic and clinical studies on sulbactam/ampicillin in children]. 274 50

The usefulness of sulbactam/ampicillin (SBT/ABPC) in the treatment of pediatric infections was evaluated. 1. Twenty pediatric patients with infection were treated with SBT/ABPC and an intravenous dosage of 27.8-47.4 mg/kg, 3 to 4 times a day. Clinical efficacies in 18 patients excluding 2 patients of Mycoplasma pneumonia (9 cases of pneumonia, 6 urinary tract infection, 1 tonsillitis, 1 maxillary sinusitis and 1 osteomyelitis) were judged to be excellent in 13 patients and good in 5. There was no case of failure. 2. Bacteriological efficacies against 16 strains (1 Staphylococcus aureus, 3 Enterococcus faecalis, 4 Haemophilus influenzae, 2 Haemophilus parainfluenzae, 5 Escherichia coli and 1 Serratia sp.) isolated from 13 of the 18 patients were rated as "eradicated" for 13 strains, "decreased" for 1 and "unchanged" for 2 with an eradication rate of 81.3%. Of 13 strains eradicated, 3 were those with high beta-lactamase productivity. 3. Rash as a side effect developed in 1 patient and eosinophilia and elevated GOT and GPT were observed in 7 patients but none of them were serious. 4. Blood levels of the drug following an intravenous dose of 30 mg/kg were determined in 2 pediatric patients. Blood levels of SBT and ABPC at 30 minutes after intravenous administration were 19.0 and 29.2 micrograms/ml in one patient and 21.0 and 31.6 micrograms/ml in another, respectively, and those at 4 hours were 0.48 and 0.62 microgram/ml in one patient and 0.59 and 0.89 microgram/ml in another, respectively. The half-lives of SBT were 0.67 and 0.70 hour and those of ABPC were 0.64 and 0.69 hour in the 2 patients, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Bacteriological, pharmacokinetic and clinical studies of sulbactam/ampicillin in the pediatric field]. 274 51

A combination drug of sulbactam/ampicillin (SBT/ABPC) was intravenously administrated to 18 patients with ages 3 months to 10 years 10 months with various acute infections including 14 cases of pneumonia, 1 case each of tonsillitis, subacute bacterial endocarditis, empyema and suspected sepsis. Clinical responses were excellent in 14 cases and good in 4 cases. Bacteriological responses of 8 isolated strains were: 7 strains were eradicated and 1 strain was decreased. No side effect was observed in any case. Eosinophilia was observed in 2 cases, thrombocytosis in 2 cases, elevation of GOT in 1 case and elevations of GOT and GPT in 1 case. From the above results, it seemed that SBT/ABPC was a useful drug for the treatment of bacterial infections in the pediatric field.
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PMID:[Clinical study on sulbactam/ampicillin in the pediatric field]. 274 52

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

Clinical trials of cefodizime (CDZM, THR-221) were carried out in pediatric infection. Results are summarized as follows. 1. The mean half-life of CDZM in the serum following intravenous injection of CDZM (20 mg/kg) was about 2.06 hours. 2. The mean urinary excretion rate of CDZM within 8 hours after intravenous injection of CDZM was 60.1%. 3. CDZM was administrated to 19 pediatric patients with various infections; 9 cases of pneumonia, 3 bronchitis, 1 cervical lymphadenitis, 2 tonsillitis and 4 urinary tract infections. The overall efficacy rate was 94.7%. 4. No adverse reactions were observed. Abnormal laboratory test values found were thrombocytosis in 2, slight elevation of GOT and GPT in 1 and eosinophilia in 1 patient.
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PMID:[Laboratory and clinical studies of cefodizime in pediatric field]. 279 57

Cefodizime (THR-221, CDZM), a new parenteral cephalosporin, was evaluated for its efficacy and safety in 20 children with bacterial infections (Table 1), and the following results were obtained. 1. CDZM was administered in 3 or 4 divided doses at daily dosages ranging from 54.5 to 84.2 mg/kg administered by 30 minutes drip infusion or intravenous injection to 20 patients (7 cases of acute tonsillitis, 6 cases of pneumonia, 2 cases each of bronchitis and suppurative cervical lymphadenitis, and 1 case each of acute pharyngitis, acute enteritis and furunculosis) and the following clinical results were obtained: excellent, 7 cases; good, 11 cases; fair, 2 cases. The overall efficacy rate was 90% (Table 4). 2. MICs of CDZM against 15 strains of isolated organisms are shown in Table 2. MICs against all 7 strains of Haemophilus influenzae were less than 0.025 micrograms/ml. MIC against 1 out of 5 strains of Streptococcus pneumoniae was 0.05 micrograms/ml and those against 2 strains were 0.10 micrograms/ml and against the other 2 were 0.20 micrograms/ml. MICs against 3 strains of Staphylococcus aureus were 1.56, 25 and higher than 100 micrograms/ml, respectively. 3. No clinical adverse reaction was observed in any of the 20 patients. Eosinophilia was observed in 2 cases. A slight elevation of S-GOT was found in 1 patient (case No. 8) and moderate elevation of S-GOT and S-GPT in another (case No. 18) (Table 4). In case No. 18, the S-GOT and S-GPT activity improved after the administration of the drug was stopped.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Clinical evaluation of cefodizime in children]. 279 59


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