Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q29983 (MIC)
21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Norfloxacin (NFLX, AM-715), a new quinolone antibiotic agent, was evaluated clinically and bacteriologically for its efficacy and safety in pediatrics by a study group organized with pediatricians from all over the country. A summary of the results of the evaluation is as follows. 1. Incidence of NFLX-resistant strains (MIC over 12.5 micrograms/ml) isolated from children with various infections was 1.6% (8/512). One resistant strain was observed among 45 isolates of Staphylococcus aureus, and none among 30 isolates of Pseudomonas aeruginosa. 2. After single oral administration of 1.5-2.9, 3.0-4.8 and 5.1-6.1 mg/kg NFLX in tablet form at fasting, mean peak values of serum concentration of 0.37, 0.56, 0.92 micrograms/ml, T1/2 of 2.5, 2.6, 2.6 hours and urinary recovery rates in 8 hours at 25.3, 25.3, 27.1% were observed, respectively. 3. Clinical effects were studied chiefly in intestinal and urinary tract infections. Among 317 patients from whom pathogens had been isolated, responses to the treatment were excellent in 187, good in 79, fair in 9, poor in 7, and unknown in 35 cases. The overall efficacy rate was 94.3% (266/282) and the efficacy rate for excellent responses was 70.3% (187/266). Among all the 406 patients treated, including those with undetermined pathogens, responses were excellent in 233, good in 106, fair in 11, poor in 11, and unknown in 45 cases. The overall efficacy rate was 93.9% (339/361). 4. Clinical effects of NFLX classified by diseases with identified pathogens were 81.8% (9/11) for acute pneumonia, 80.8% (21/26) for other respiratory infections, 95.8% (23/24) for bacillary dysentery, 98.6% (70/71) for Campylobacter enteritis, 100% (24/24) for Salmonella enteritis, 100% (6/6) for other acute enteritis and 98.1% (104/106) for urinary tract infections. Including other infections as high as 94.3% (266/282) of efficacy rate was obtained in total. There was no significant difference in NFLX efficacies between unidentified and identified pathogens. Thus, the total clinical efficacy rate was 93.9% (339/361). 5. The total eradication rate of 325 pathogens evaluable was 84.3%, with identical eradication rates for Gram-positive cocci (GPC) (43/51) and for Gram-negative rods (GNR) (231/274). 6. The optimal daily dose of NFLX seemed to be in a range between 6.0 and 12.0 mg/kg, and the optimal duration of treatment to be 7 days for children over 5 years old. 7. The clinical efficacy in treating P. aeruginosa infections in 12 patients was 100% (11/11) and the eradication rate was 83.3% (10/12).(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Evaluation of norfloxacin in the pediatric field. Pediatric Study Group for Norfloxacin]. 219 14

We have evaluated norfloxacin (NFLX), a fluoroquinolone agent, in tablet form for its efficacy and safety in the field of pediatrics. 1. Mean serum concentrations of NFLX following oral administration to 3 children at dose levels of 3.2 mg/kg, 3.7 mg/kg and 5.4 mg/kg were, respectively, 0.7 microgram/ml, 0.18 microgram/ml and 0.64 microgram/ml at 2-4 hours. Mean serum half-lives (T1/2) of NFLX were 2.5-2.9 hours and mean urinary recovery rates in the first 6 hours after administrations were 7.1-30.7%, depending on dose levels. 2. Antibacterial activities of NFLX against clinically isolated 30 organisms from children were determined. MIC of NFLX against Staphylococcus aureus was similar to that of ABPC, 0.39-25 micrograms/ml. MIC of NFLX against Escherichia coli was approximately less than or equal to 0.10 microgram/ml. This MIC value was lower than other antibiotics. MIC of NFLX against Vibrio parahaemolyticus was less than or equal to 0.10 microgram/ml. 3. NFLX was administered to 30 patients (7 patients with Salmonella enteritis, 7 patients with Campylobacter enteritis, 5 patients with other enteritis, 1 patient with bacillary dysentery, 8 patients with urinary tract infection, 2 patients with skin soft tissue infection). The clinical responses of these 30 patients were as follows; excellent: 24 patients, good: 4 patients. The efficacy rate was 93.3%. 4. The bacteriological efficacy rate of NFLX against clinically isolated 29 organisms from children was 75.9%, including 3 cases in which other antimicrobial agents had been ineffective. Especially against Salmonella spp. was superior to other agents tested. 5. Neither clinical adverse reaction nor abnormal laboratory data was found in any of these 33 patients.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Pharmacokinetic, bacteriological and clinical studies in the pediatric field on norfloxacin]. 239 51

The fundamental and clinical studies of aztreonam (AZT) were performed. The results were as follows: The MICs of AZT for E. coli and Salmonella sp. which were recently isolated in the pediatric field were less than 0.78 micrograms/ml. AZT also was effective against ABPC/PIPC-resistant bacteria. The MIC of AZT for V. parahaemolyticus was less than 1.56 micrograms/ml. The peak serum levels of AZT which were occurred just after the 1 hour drip infusion of 10-30 mg/kg were 60.5-136.8 micrograms/ml, and at 6 hours after infusion the serum levels were 1.3-6.1 micrograms/ml; therefore, the dose response was proved. The mean half-lives (T 1/2) were between 1.21 and 1.36 hours. The excretion rates in urine up to 6 hours after intravenous drip infusion were between 32.7 and 77.5%. The ratio of the cerebrospinal fluid concentration to serum in the child with purulent meningitis was 3.5% at 1 hour after the intravenous injection at the dose of 69 mg/kg, and the ratios of the subdural fluid levels to serum were 31.3-37.5%. The levels of AZT into the feces by the multiple dosage were 0-840 micrograms/g. Twenty-five pediatric patients with acute infections had been treated by intravenous injection or drip infusion at the doses of 49-120 mg/kg/day (almost 50-100 mg/kg/day) for 4 to 13 days. The efficacy rate of excellent + good was 84% and that of excellent + good + fair was 96%. The efficacy rate of excellent + good was 100% in all cases with upper/lower respiratory tract infection, bronchopneumonia, and acute urinary tract infection caused by Gram-negative rods. The clinical efficacy was observed in all cases with acute bacterial enteritis. Although AZT was clinically effective against Salmonella enteritis, bacteriological efficacy on the causative organisms was not observed in some cases. Although AZT was bacteriologically effective in 1 patient with typhoid, it did not alleviated fever. AZT showed activity to 9 strains isolated from the culture of throat swab, urine and feces. No side effects were clinically observed in all cases, while slight elevations of laboratory findings were observed in 4 cases.
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PMID:[Fundamental and clinical studies of aztreonam in the field of pediatric]. 409 57

Fundamental and clinical evaluation on ceftriaxone (CTRX, Ro 13-9904) was performed in the pediatric field and the following results were obtained. The MIC of CTRX against the recently isolated 10 strains of B. pertussis was less than or equal to 0.05 microgram/ml at inoculum size of 10(6) CFU/ml. The blood level of CTRX after intravenous drip infusion with 10 to 20 mg/kg for 30 minutes to 1 hour reached a peak ranging from 45.3 to 137 micrograms/ml at the end of infusion. The effective blood level was maintained up to 12 hours to be 3.52 to 26.7 micrograms/ml at that time. The half-life time was over 6 hours in most cases, but the multiple intravenous dosage did not cause any elevation of the blood level. The urine excretion rate till 12 to 24 hours after intravenous drip infusion ranged from 58.2 to 84.2%. The excretion of CTRX into the cerebrospinal fluid was favorable in the acute period when administered by intravenous drip infusion in the child with S. pneumoniae purulent meningitis, which was considered to be satisfactory for treatment against the bacteria susceptible to CTRX. The active CTRX was transferred into the feces by the multiple dosage. CTRX was administered by intravenous drip infusion in 26 cases with acute pediatric infections. The clinical efficacy was observed in all the cases with upper/lower respiratory tract infections including bronchopneumonia and pertussis, and the cases with acute urinary tract infections caused by ABPC-resistant E. coli, administered by intravenous drip infusion twice daily with about 40-50 mg/kg/day. The bactericidal efficacy was seen against all bacteria except Salmonella. CTRX by intravenous drip infusion was effective against S. pneumoniae purulent meningitis; the clinical symptom was rapidly improved while the culture of causative strains from the cerebrospinal fluid turned negative. Although CTRX was clinically effective against Salmonella enteritis and typhoid, bacteriological and symptomatological relapses were observed in some cases. An increase in dose of CTRX is considered to be needed for these diseases. No adverse reaction was found clinically but soft stool in 1 case while eosinophilia and thrombocytosis were observed each in 1 out of 30 cases in laboratory test. The efficacy was good or higher in all the 26 cases (100%) administered by intravenous drip infusion. The above-mentioned results indicate that CTRX is useful in the pediatric field.
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PMID:[Evaluation on ceftriaxone in the pediatric field]. 609 3

Clinical evaluation of cefmetazole were made in the treatment of bacterial infections in the newborn infants and the following results were obtained. 1) Five infants, 7 approximately 58 days of age, received a single intravenous one-shot injection of 22.2 approximately 24.5 mg/kg dose of cefmetazole, and blood concentrations were determined. The average level was 62.6 micrograms/ml (30 minutes), 46.3 micrograms/ml (1 hour), 26.8 micrograms/ml (2 hours), 8.7 micrograms/ml (4 hours) and 2.4 micrograms/ml (6 hours), and T 1/2 was 87.7 minutes. Almost similar values were obtained when the drug was given by a 30-minute drip infusion and sufficiently exceeded the MIC to the bacteria to which cefmetazole was indicated. 2) In two patients, who had been operated for choledochal cyst and received an intravenous drip infusion of the drug, the persistence of the blood concentration was remarkably long, T 1/2 being 192 and 222 minutes, respectively. This problem still remains to be elucidated. 3) The following 22 patients were treated with an intravenous one-shot or drip infusion of cefmetazole, i.e., 45.6 to 107.1 mg/kg divided in 2 approximately 3 doses; 14 patients aged 1 to 21 days, 2 aged 1 to less than 2 months, 3 aged 2 to less than 3 months and 3 aged older than 3 months. However, in purulent meningitis, larger dose was given intravenously 6 times daily. Diseases included sepsis (4 cases), purulent meningitis (3), peritonitis (1) SSS syndrome (3), subcutaneous abscess (2), urinary tract infection (8) and Salmonella enteritis (1), and their causative organisms were E. coli (13 strains), K. pneumoniae (1), S. typhimurium (1), S. aureus (6) and group B Streptococcus (1). Overall efficacy rate in 22 cases was 90.9%. i.e., excellent in 11, good in 9 and failure in 2. Two cases of failure were a patient with peritonitis and visceral eventration due to umbilical hernia and a patient with a chromosomal aberration and urinary tract infection caused by E. coli. Reasons for such a treatment failure appeared to reside in host factors. 4) Adverse reactions included each one case of skin rash and diaper rash, 3 cases of eosinophilia and 5 cases of elevation of transaminase levels, all of which were mild and transient. 5) Based on the above results, cefmetazole is considered to be a potent new antibiotic which should be indicated as the first choice drug in the treatment of neonatal bacterial infections. The recommended dosage is as follows: 50 mg/kg given intravenously 6 times daily for bacterial meningitis and 20 approximately 25 mg/kg intravenously or by a drip infusion 2 to 3 times daily for other infections.
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PMID:[Cefmetazole in the treatment of bacterial infections in the newborn (author's transl)]. 694 Oct 35