Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0149514 (bronchitis)
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We have carried out laboratory and clinical studies on norfloxacin (NFLX, AM-715). The results are summarized as follows. NFLX was given through oral administration to one child each at dose levels of 1.7 mg/kg, 2.4 mg/kg and 3.2 mg/kg. After administration, peak serum levels of NFLX obtained for the 3 dose levels were 0.16 micrograms/ml at 1 hour, 0.69 micrograms/ml at 2 hours, 0.81 micrograms/ml at 1 hour, respectively, and half-lives were 2.5 hours, 1.8 hours and 2.7 hours, respectively. NFLX was given through oral administration to 2 children at a dose level of 4.4 mg/kg and to another child at a dose level of 4.8 mg/kg. After administration, mean peak serum levels of NFLX obtained were 1.17 +/- 0.48 micrograms/ml and half-lives were 3.0 +/- 0.5 hours. Urinary excretion rates of NFLX were 14.5% and 28.4% in the first 8 hours after administration of 1.7 mg/kg and 3.2 mg/kg, respectively, and 29.1% in the first 6 hours after administration of 2.4 mg/kg. Mean urinary excretion rates of NFLX were 38.5 +/- 13.0% in the first 8 hours after administration of 4.4 mg/kg and 4.8 mg/kg. Treatment with NFLX was made in 33 cases of pediatric bacterial infections including 5 cases of tonsillitis, 14 cases of enteritis, 10 cases of UTI and 1 case each of bronchitis, balanoposthitis, impetigo and pustulosis. Results obtained were excellent in 14 cases, good in 15 cases. No significant side effect due to the drug was observed in any cases.
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PMID:[Laboratory and clinical studies of norfloxacin in pediatric field]. 239 57

Clarithromycin (TE-031, A-56268) is a new 14-membered ring macrolide antibiotic developed by Taisho Pharmaceutical Co., Ltd. TE-031 has a methoxy group at position 6 in its structure. In the present study, we carried out laboratory and clinical investigations on TE-031 in the field of pediatrics. The obtained results are summarized as follows. The antibacterial activity of TE-031 was investigated against 16 clinically isolated strains of Streptococcus pyogenes, Staphylococcus aureus, Haemophilus influenzae, Bordetella pertussis and Campylobacter jejuni. TE-031 showed antibacterial activity comparable to erythromycin. The pattern of changes in TE-031 concentrations in the blood after administration was investigated. In subjects administered the granular preparation of TE-031, Cmax values were 0.64 micrograms/ml in 1 subject given a 5 mg/kg dosage, and 5.94 and 9.02 micrograms/ml in 2 subjects administered with 10 mg/kg. The tablet form of TE-031 was administered to 3 subjects at 5 mg/kg, and Cmax values were 2.09-3.92 micrograms/ml, while T 1/2 values were in a range of 2.9-3.8 hours. When drug concentrations in the urine were investigated, it was found that 6-hour recovery rates were 9.9% (dose: 5 mg/kg) and 53.4% (dose: 10 mg/kg) in the subjects administered the granular form, whereas recovery rates averaged 36.8% in the tablet-administered subjects. In the clinical trial, TE-031 was administered in 2-3 doses/day for 2-18 days. In cases given the granular form, dosages were 12-38 mg/kg/day, while tablets were administered at 12-29 mg/kg/day. The overall clinical efficacy rate was 92.8%, i.e., the drug was effective in 64 of 69 patients. TE-031 was ineffective in 1 case of otitis media, but efficacious in 10 of 10 (100%) cases of upper respiratory infection, 15 of 18 (83.3%) cases of bronchitis and pneumonia, 5 of 6 (83.3%) cases of pertussis, 13 of 13 (100%) cases of mycoplasmal pneumonia, 4 of 4 (100%) cases of Chlamydia psittaci pneumonia, 16 of 16 (100%) cases of gastroenteritis (including 15 cases of Campylobacter gastroenteritis), and 1 (100%) case of impetigo. In bacteriological studies conducted on the patients, the overall elimination rate was 93.1%, i.e., bacterial elimination was obtained in 27 of 29 cases. TE-031 showed especially good bacteriological efficacy (100%) against C. jejuni and B. pertussis, which were eliminated from all of 15 and 2 cases examined, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Laboratory and clinical studies on clarithromycin in pediatrics]. 252 42

Clarithromycin (TE-031, A-56268) was orally administered to 20 children with the following acute bacterial infections; 1 case of acute pharyngitis, 3 cases of acute tonsillitis, 11 cases of acute bronchitis, 1 case of exacerbation of chronic bronchitis, 1 case of acute bronchopneumonia, 2 cases of Mycoplasma pneumonia and 1 case of impetigo. Clinical effectiveness was obtained in 15 out of the 20 cases (75.0%). No clinical side effects and laboratory abnormalities were observed. The above results suggest that TE-031 is a useful antibiotics for treating pediatric patients with various bacterial infections.
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PMID:[Clinical experience with clarithromycin in the pediatric field]. 252 51

A newly developed macrolide clarithromycin (TE-031, A-56268), with antibacterial spectrum and antibacterial activity nearly equal to those of erythromycin (EM), shows beneficial characteristics such as a higher blood level, higher recovery rate in urine, and better penetration into each tissue than conventional macrolides (MLs). TE-031 has been studied in adults against various infections and proved to be useful. The present paper describes the results of a study in children to examine the usefulness of TE-031 granules and tablets with a potency of 50 mg. TE-031 granules were administered to 132 children with ages from 6 months to 13 years and 10 months. Excluded from the evaluation were 12 cases in which clinical effects were deemed unevaluable. The evaluable subjects consisted of 1 case with pharyngitis, 3 with tonsillitis, 9 with acute bronchitis, 19 with pneumonia, 19 with mycoplasmal pneumonia, 2 with scarlet fever, 20 with Campylobacter enteritis, 11 with impetigo, 2 with subcutaneous abscess, 18 with primary atypical pneumonia and 16 with acute enteritis of unidentified pathogens; a total of 120 subjects. An average daily dose of TE-031 was 25.9 mg/kg, divided into 3 doses except 1 case with 2 daily doses and lengths of the treatment averaged 7 days. TE-031 tablets each containing 50 mg potency, were administered to 49 subjects with ages from 3 year and a month to 14 years consisting of 8 cases with pharyngitis, 1 with tonsillitis, 1 with acute bronchitis, 4 with pneumonia, 14 with mycoplasmal pneumonia, 4 with scarlet fever, 5 with Campylobacter enteritis, 7 with impetigo, 1 with atypical pneumonia, 1 with Salmonella gastroenteritis and 3 with acute enteritis caused by unidentified pathogens, at an average daily dose of 13.5 mg/kg dived into 2-4 doses (2 doses/day for 12 cases, 3 doses for 32, 4 doses for 5) for 7 days on the average. In addition to examine the clinical and bacteriological effects of the 2 dosage forms of TE-031, minimum inhibitory concentrations (MICs) were determined for 9 antibiotics consisting of 5 MLs including TE-031, EM, josamycin (JM), midecamycin acetate (MDM acetate), and rokitamycin (RKM), 3 penicillins including ampicillin (ABPC), methicillin, cloxacillin and 1 cephem antibiotic, cefaclor (CCL), against 29 strains consisting of 12 strains of Staphylococcus aureus, 7 of Streptococcus pyogenes, 2 of Streptococcus pneumonia 2 of Haemophilus influenzae and 6 of Campylobacter jejuni, out of 71 strains of pathogens or possible pathogens that had been isolated from the cases given TE-031.
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PMID:[Clinical study on clarithromycin granule and tablet in the field of pediatrics]. 252 56

Pharmacokinetic and clinical studies on cefmenoxime (CMX) in neonates and infants were conducted. 1. CMX 20 mg/kg was administered by intravenous bolus injection to 6 neonates (with ages 2 to 20 days) and 5 infants (with ages 36 to 107 days) and its serum concentration and urinary excretion rates were determined. In the neonates, serum concentrations of CMX after intravenous administration reached peak levels of 48.2 to 90.7 micrograms/ml (mean 70.4 +/- 14.3 micrograms/ml) in 1/4 hour, then declined with half-lives of 1.27 to 5.19 hours (mean 2.28 +/- 1.56 hours), and were 3.6 to 16.9 micrograms/ml (mean 8.3 +/- 6.0 micrograms/ml) at 6 hours. In the infants, serum concentrations at 1/4 hour were 67.5 to 111.0 micrograms/ml (mean 95.5 +/- 18.0 micrograms/ml); half-lives were 0.64 to 0.94 hour (mean 0.81 +/- 0.13 hour); and the serum concentrations at 6 hours were 0.2 to 1.1 micrograms/ml (mean 0.7 +/- 0.4 micrograms/ml). Mean peak serum concentrations in the neonates tended to be lower than those in the infants, but higher than those in children. Regarding the age differences of serum concentrations due to age in the neonates, their peak levels tended to be lower in younger ones. Half-lives were shorter in older subjects and, in early infancy, approached values observed in children. Urinary recovery rates in the first 6 hours after intravenous administration ranged from 43.6 to 87.5% (mean 61.6 +/- 14.6%) in the neonates and from 52.1 to 90.8% (mean 78.0 +/- 15.1%) in the infants. Thus, recovery rates were high even in younger subjects and tended to be higher in older subjects. 2. CMX was administered to 27 neonates and 4 infants to investigate its clinical effect, bacteriological effect and side effects. Clinical efficacy ratings of the drug in 19 neonate cases that could be evaluated (1 with purulent meningitis, 2 with suspected septicemia, 1 with acute bronchitis, 12 with acute pneumonia, 1 with impetigo, 1 with periumbilical abscess and 1 with acute pyelonephritis) were "excellent" in 14 cases, "good" in 4, and "poor" in 1. The efficacy rate covering "excellent" and "good" was 94.7%. In 4 infants (2 with acute pneumonia, 1 with periumbilical abscess and 1 with acute pyelonephritis), "excellent" was obtained in 2 cases and "good" in 2 cases. Thus, all the cases showed "good" or higher ratings. Bacteriologically, 1 strain of Staphylococcus aureus and 3 strains of Escherichia coli in neonates were eradicated while, in infants, 1 strain of S. aureus persisted but 1 of E. coli was eradicated.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Pharmacokinetic and clinical studies on cefmenoxime in neonates and infants]. 261 19

During 8 months from October 1986 to May 1987, the clinical efficacy of sulbactam/ampicillin (SBT/ABPC) was evaluated in 63 pediatric inpatients with various infections. Clinical efficacies were evaluable in 58 patients among them (consisting of 2 patients with sepsis, 3 with tonsillitis, 12 with bronchitis, 6 with bronchopneumonia, 24 with pneumonia, 1 with phlegmon, 2 with lymphadenitis, 1 with impetigo and 7 with urinary tract infection) and were excellent in 40 patients and good in 17 with an overall efficacy rate of 98.3%. Bacteriological efficacies were assessed in 25 patients and 27 strains of organisms (consisting of 3 strains of Staphylococcus aureus, 2 Streptococcus pneumoniae, 1 Streptococcus pyogenes, 2 beta-Streptococcus, 1 Gram-positive cocci, 5 Escherichia coli, 1 Enterobacter aerogenes, 7 Haemophilus influenzae, 2 Haemophilus parainfluenzae, 1 Branhamella catarrhalis, 1 Proteus mirabilis and 1 Salmonella subgenus I). Bacteriological eradication rates were 88.9% for Gram-positive organisms, 66.7% for Gram-negative organisms and 74.1% overall. No superinfection was observed in any of patients treated. Side effects and clinical laboratory parameter abnormalities observed consisted of diarrhea in 7 (11.1%) of the 63 patients, eosinophilia in 2 (3.3%) of 61 tested, thrombocytosis in 3 (5.5%) of 55, elevation of direct bilirubin in 1 (3.3%) of 30, elevation of total bilirubin in 1 (3.1%) of 32, elevation of GOT in 4 (6.8%) of 59 and elevation of GPT in 1 (1.7%) of 59 patients tested. As an effect on the hemostatic mechanism of this drug, PIVKA II was detected in 1 patient (4.2%) of 24 tested, but findings of other coagulation tests were normal and none of patients showed bleeding tendency or inhibition of platelet aggregation. From the above results, it appears that SBT/ABPC is an efficacious and safe drug in the treatment of bacterial infections of pediatric patients.
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PMID:[Clinical studies on sulbactam/ampicillin in the field of pediatrics]. 266 49

We have carried out laboratory and clinical studies on sulbactam/ampicillin (SBT/ABPC). The results are summarized as follows. SBT/ABPC was given by 30-minute drip infusion to 1 child at a single dose of 15 mg/kg and to 2 children at a single dose of 30 mg/kg. After the 30-minute drip infusion, peak serum levels of ABPC(SBT) obtained for the 2 dose levels were 18.0 micrograms/ml (12.4 micrograms/ml) for the former dose level and 81.0 micrograms/ml (53.7 micrograms/ml) and 300 micrograms/ml (200 micrograms/ml) for the latter at the end of injection, and half-lives were 0.84 hour (0.82 hour) for the former and 0.96 hour (1.44 hours) and 0.93 hour (1.19 hours) for the latter. In another trial, SBT/ABPC was given to 1 child at a single dose of 60 mg/kg. After the 30-minute drip infusion, peak serum level of ABPC (SBT) was 82.3 micrograms/ml (45.9 micrograms/ml), and half-life was 1.20 hours (1.36 hours). The urinary excretion rates of ABPC (SBT) were 51.3% (49.5%), 55.8 +/- 10.4% (65.3 +/- 9.1%), 74.0% (76.1%) up to 6 hours after the 30-minute drip infusion of 15 mg/kg, 30 mg/kg and 60 mg/kg, respectively. Treatment with SBT/ABPC was made in 21 cases of pediatric bacterial infections: 8 cases of tonsillitis, 4 cases of bronchitis, 3 cases of pneumonia and 1 case each of pharyngitis, peritonsillar abscess, lymphadenitis, impetigo, abscess and urinary tract infection. Results obtained were excellent in 14 cases, good in 7 cases. No significant side effect due to the drug was observed in any cases except 1 case of fever and rash.
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PMID:[Laboratory and clinical studies of sulbactam/ampicillin in pediatric field]. 274 49

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

Cefpodoxime proxetil (CPDX-PR, CS-807) was given orally to 18 children with acute bacterial infections including 10 with acute tonsillitis, 3 with acute bronchitis, 1 with pneumonia, 3 with staphylococcal scalded skin syndrome and 1 with infectious impetigo. Daily dosages per kg bodyweight ranging from 7.5 to 18 mg were given in 2 or 3 divided doses per day for 5 to 15 days. Clinical responses were excellent in 3 (16.7%), good in 11 (61.1%), fair in 4 (22.2%) and poor in 0 (0%), with an overall efficacy rate of 77.8%. Good bacteriological responses were obtained in 6 out of the 7 cases from which pathogens were identified. No side effect was observed. The above results suggest that CPDX-PR is a useful new oral cephalosporin derivative for the treatment of bacterial infections in children.
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PMID:[Clinical studies on cefpodoxime proxetil in the pediatric fields]. 281 Jul 23

Cefpodoxime proxetil (CS-807, CPDX-PR), a new cephalosporin antibiotic, was investigated for its usefulness in pediatrics. 1. The total number of patients treated were 21 with their ages ranging from 3 months to 9 years and 1 month, consisting of 5 male and 16 female infants. 2. Single dosages of the drug ranged between 4.4 mg and 5.8 mg/kg with oral administration for 3 times daily in fasting. A total aggregated dosage was between 46.4 mg/kg and 200.0 mg/kg. The length of administration was 3 to 12 days. 3. The breakdown of symptoms were 9 cases of acute pharyngitis, 5 cases of acute tonsillitis, 3 cases of acute bronchitis, and 1 case each of impetigo + purulent rhinitis, cervical lymphadenitis, scarlet fever, and urinary tract infection. 4. The clinical efficacy rate was 100% with 18 excellent responses and 3 good responses. 5. The bacteriological efficacy rate was 90.9% in eradication rate, based on results on 17 strains of suspected causative microorganism among which 10 strains were eradicated, 1 strain was decreased, and 6 strains were unknown. 6. There was no side effect during the treatment and after the discontinuation, while, in clinical laboratory tests, GOT and GPT were elevated in 1 case which was judged as abnormal. No patient refused the drug. CPDX-PR was considered to be very useful drug because of its excellent efficacy and safety in pediatrics in treating infectious diseases.
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PMID:[Study of efficacy, safety and dosage on cefpodoxime proxetil in pediatric infections]. 281 Jul 26


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