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)

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

For the purpose of evaluation of clinical efficacy, safety and usefulness on Salmonella enteritis, T-3262 (Tosufloxacin tosilate), a newly developed pyridone-carboxylic acid derivative, was administered to a total of 103 patients and carriers. In addition, in vitro antibacterial activity of T-3262 was determined against the clinical isolates, and compared with those of nalidixic acid (NA), pipemidic acid (PPA), enoxacin (ENX), norfloxacin (NFLX) and ofloxacin (OFLX). And when T-3262 was administered to the patients of acute infectious enteritis, fecal drug concentration and their correlation to the changes in the fecal microflora were investigated. The daily dose of 450 mg T-3262 was administered orally three times after meal for 7 days. A total of 63 cases were evaluated (one case of mixed infection caused by Shigella flexneri and Salmonella sp. was included). The clinical efficacy was good in all the enteritis (N = 6). As the bacteriological effect, 60 out of 61 were eradicated, and eradication rate was 98.4%. Adverse effects were observed in four of 102 cases (3.9%), consisting of one with skin rash, one with nausea, headache and stomatitis and two with soft stools. Deteriorations in laboratory findings were seen in 5 of 23 cases (17.4%), consisting of one with elevated GOT, two with elevated GOT and GPT, one with elevated BUN and one with increased eosinophiles count, although they were all slight in degree. MICs of T-3262 which inhibited 90% of the isolates of Salmonella spp. was 0.05 microgram/ml, which was the lowest among the quinolone derivatives tested. The values of the fecal drug concentration of 7 cases of acute infectious enteritis, to which T-3262 administered, were higher than that of MIC90 and recovery rates of T-3262 were distributed from 2.85 to 46.3%. The degrees of changes of the drug concentrations were dependent on individual cases, and did not show the same trend. In addition, changes in the fecal microflora with in 24 hrs after T-3262 administration did not show the same trend.
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PMID:[Clinical trial of T-3262 (Tosufloxacin tosilate) on Salmonella enteritis, and fecal drug concentration and change in the fecal microflora in the acute diarrheal patients. Japan Research Committee of T-3262, Research Group for Acute Infectious Enteritis]. 269 43

The new antibiotic, sulbactam/ampicillin (SBT/ABPC) was administered to 25 children. The results obtained are summarized as follows. 1. In 5 cases of children administered with SBT/ABPC (30 mg/kg) by intravenous drip infusion for 30 minutes, the mean values of T 1/2 (beta) were 0.94 hour (SBT) and 0.86 hour (ABPC) and the mean 6.5 hour urinary excretion rates were 64.2% and 42.9%, respectively. 2. The antibiotic was administered to a total of 25 patients with bronchopneumonia, pneumonia, bronchitis, cervical lymphadenitis, tonsillitis, streptococcal infection, urinary tract infection, felon, periappendicular abscess, sepsis or purulent meningitis. Response to the treatment were excellent in 17 cases, good in 7, fair in 1, and poor in none. The efficacy rate was 96%. From our results, this drug appears to be particularly effective against bronchopneumonia, bronchitis and urinary tract infection. 3. Eruption occurred in 1 of 25 patients and elevation of eosinophil, GOT/GPT, platelet in 3 and descent of WBC in 1 were observed, but these were transient. These results showed that SBT/ABPC is a drug which can be safely used in the pediatric field as well as for adults.
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PMID:[Pharmacokinetic and clinical studies on sulbactam/ampicillin in the pediatric field]. 274 48

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

Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium (IPM/CS) were performed in neonates. The results were as follow: 1. A total of 27 patients consisting of 17 mature and 10 immature infants were treated with IPM/CS. Each dose was 20 mg/20 mg/kg, and it was administered 2 approximately 3 times daily, in a 1-hour intravenous drip infusion for 3 approximately 12 days. The clinical efficacy of IPM/CS in 10 patients with bacterial infections (2 with sepsis, 3 with suspected sepsis, 2 with pneumonia, 2 with urinary tract infection and 1 with acute omphalitis) was evaluated as excellent in all patients, with an efficacy rate of 100%. All 5 causative organisms found in 5 patients (Staphylococcus aureus in 1, Staphylococcus epidermidis in 1, Escherichia coli in 2 and Flavobacterium meningosepticum in 1) were eradicated. Among 27 patients administered IPM/CS, adverse reactions were observed in 2 patients. These were rash and diarrhea. As for abnormal laboratory test values, elevations of GOT and GPT were observed. 2. MICs of IPM against 14 clinical isolates (S. epidermidis 1, S. aureus 6, Streptococcus agalactiae 4, E. coli 1, Enterobacter cloacae 1 and F. meningosepticum 1) from neonatal patients with bacterial infections were examined. IPM showed good antibacterial activity comparable to that of cefotaxime against S. agalactiae; however, the activity against methicillin-resistant S. aureus was poor. 3. Serum levels of IPM and CS were investigated in a total of 22 patients consisting of 15 mature and 7 immature infants after 20 mg/20 mg/kg of IPM/CS was administered. IPM and CS produced peak serum levels at the end of the drip infusion. In mature infants, peak serum levels of IPM and CS were 31.8 micrograms/ml (17.1 approximately 59.0 micrograms/ml) and 59.9 micrograms/ml (35.6 approximately 99.0 micrograms/ml), respectively. In low birth weight infants, these were 25.0 micrograms/ml (16.8 approximately 41.8 micrograms/ml) and 55.2 micrograms/ml (33.8 approximately 82.4 micrograms/ml), respectively. Half-lives of IPM and CS were 1.0 approximately 2.7 hrs. and 0.9 approximately 7.4 hrs. in mature infants, and 1.6 approximately 3.0 hrs. and 1.3 approximately 9.7 hrs. in immature infants, respectively. Generally the longer half-lives were observed in the younger neonates. Serum levels of CS remained higher and half-lives of CS were longer than those of IPM. The pharmacokinetics in neonates were different from those in adults or children.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium in neonates]. 274 57

Therapeutic effects of cefodizime (CDZM, THR-221), a new cephalosporin having a methoxyimino group, were examined in various infectious diseases in children. Clinical efficacy rates were 100% (3/3) in pneumonia, 100% (5/5) in acute bronchitis, 75% (3/4) in upper respiratory infections and 100% (1/1) in each of a croup and a mixed infection with Streptococcus pyogenes and staphylococcal impetigo. Hence, the overall efficacy rate was 92.9% (13/14). Adverse effects were observed in 2 cases, i.e. exanthema provably due to drug allergy in 1 case and a slightly elevated GPT in another. Changes in serum concentrations and urinary excretion of CDZM were examined in a child with no infection. T 1/2 values obtained were 124.5 minutes (bioassay) and 143.4 minutes (high performance liquid chromatography (HPLC]. Eight hour recovery rates in urine were 62.9% (bioassay) and 65.4% (HPLC). CDZM was considered to be a safe and useful drug in treating various infectious diseases in children.
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PMID:[Therapeutic effects of cefodizime in the treatment of various infectious diseases in children]. 279 65

The clinical safety of aztreonam in the treatment of suspected aerobic gram-negative infections was assessed in 346 patients who received single doses and in 2,388 patients who received multiple doses. Of those administered multiple doses, 163 (6.8%) experienced 172 adverse clinical effects. The most common were local reactions at the injection site, rash, diarrhea, and nausea and/or vomiting. Among aztreonam and control groups, three-fold increases in serum aspartate aminotransferase (SGOT) and serum alanine aminotransferase (SGPT) values occurred at comparably low frequencies; the mean values of SGOT and SGPT were slightly higher in patients administered aztreonam than in those given cefamandole. Treatment with aztreonam was discontinued in 51 (2.1%) of 2,388 patients because of adverse clinical effects or abnormal laboratory test values. Suprainfections (infections due to new pathogens occurring at the original site of infection during treatment with the study drug that were treated with another antibiotic) were reported in 2%-6% of aztreonam-treated patients, a frequency similar to that observed in control groups. Aztreonam is well tolerated and has a safety profile similar to that of other beta-lactam antibiotics.
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PMID:Safety profile of aztreonam in clinical trials. 293 85

Aztreonam was used successfully in 17 of 17 patients with orthopedic infections due to gram-negative bacilli (11, osteomyelitis; six, septic arthritis). Duration of treatment ranged from 14 to 55 days, and the period of follow-up was four to 18 months. Causative organisms included Pseudomonas aeruginosa, Serratia marcescens, Enterobacter gergoviae, Citrobacter diversus, Proteus mirabilis, and Enterobacter aerogenes. Aztreonam was well tolerated. The only definite reactions attributable to aztreonam were asymptomatic increases in serum aspartate aminotransferase (SGOT) and serum alanine aminotransferase (SGPT) in four patients; none of these reactions interfered with completion of therapy. Adverse reactions that were possibly attributable to aztreonam included rash (two patients), diarrhea (one patient), and leukopenia (one patient). All of these patients were receiving antibiotics active against gram-positive organisms in mixed infections in addition to aztreonam. Aztreonam is a promising new monobactam without significant toxicity. It has good activity against gram-negative aerobic bacteria, including P. aeruginosa, and is effective in the treatment of serious infections due to gram-negative aerobes.
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PMID:Aztreonam in the treatment of bone and joint infections caused by gram-negative bacilli. 293 86

Ten patients with infections (8 neonates and 2 infants) were treated with 10.2 mg/10.2 mg/kg-37.7 mg/37.7 mg/kg of imipenem/cilastatin sodium (IPM/CS) b.i.d. or t.i.d. by a 1-hour intravenous drip infusion. The plasma concentrations of IPM/CS were determined in 5 of the 10 patients and in the cerebrospinal fluid of 1 patient of the 5. 1. The patients studied included 5 with pneumonia and 1 each with urinary tract infection, omphalitis, suspected meningitis, periproctal abscess and suspected septicemia. Clinical efficacy was evaluated in 9 patients: the patient with suspected meningitis was excluded from the clinical evaluation because the infection was doubtfully due to bacteria. Responses were excellent in 4 and good in 5 patients. No patient with a poor response was observed. All of the 6 etiological isolates obtained from 5 patients (2 strains of Staphylococcus aureus and 1 each of Escherichia coli, Enterococcus faecalis, Streptococcus agalactiae and Bacteroides fragilis) were eradicated. 2. As for side effects, rash was observed in 1 patient and petechiae accompanied by decreases in platelets and reticulocytes and increases in GOT and GPT were observed in another. Other abnormal laboratory test values in addition to the above abnormalities consisted of an increase in GPT in 1 patient and increases in GOT and GPT in another. These side effects and abnormalities in laboratory test values were mild and normalized after discontinuation or completion of IPM/CS administration.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Evaluation of imipenem/cilastatin sodium in neonatal infections]. 321 Mar 3


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