Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0149514 (bronchitis)
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Clinical efficacy and safety of cefprozil (CFPZ, BMY-28100), a newly developed oral cephalosporin, were studied in our pediatric department. Clinical effectiveness, bacteriological effectiveness and side effects were studied in 116 pediatric patients with ages ranging 4 months to 11 years. CFPZ was given 4.6-14.1 mg/kg daily in 3 times for 3-10 days. Clinical efficacies were evaluated in 112 patients, and the therapeutic effectiveness were excellent in 1 and good in 6 for 7 patients with acute pharyngitis, excellent in 24 and good in 26 for acute purulent tonsillitis, excellent in 3, good in 8 and fair in 1 for acute bronchitis, excellent in 21, good in 7, fair in 1 and poor in 1 for acute pneumonia, excellent in 1 acute purulent parotitis, excellent in 2 and good in 7 for acute UTI, good in 1 impetigo, fair in 1 periproctal abscess and good in 1 acute enteritis. The effectiveness rate was 96.4%. Bacteriologically, 4 strains of Staphylococcus aureus (beta-lactamase producing strains), 1 strain of Staphylococcus epidermidis (beta-lactamase producing strain), 2 strains of Streptococcus pneumoniae, 2 strains of Streptococcus agalactiae, 4 strains of beta-Streptococcus, 1 strain of Klebsiella pneumoniae (beta-lactamase producing strain) and 1 strain of Salmonella C2 were all disappeared, and of 22 strains of Streptococcus pyogenes, 20 strains were disappeared, 1 was decreased and 1 was unknown, of 5 strains of Escherichia coli (3 beta-lactamase producing strains), 4 were disappeared and 1 was decreased, of 29 strains of Haemophilus influenzae (14 beta-lactamase producing strains), 14 were disappeared, 11 were decreased, 3 persisted and 1 was unknown and of 2 strains of Haemophilus parainfluenzae (1 beta-lactamase producing strain), 1 was disappeared and 1 persisted. The bacteriological eradication rates for Gram-positive bacteria and Gram-negative bacteria were 97.1% and 56.8%, respectively, and the drug was especially effective against Gram-positive bacteria. No side effects nor refusal of ingestion were observed. As abnormalities in laboratory test results, 3 cases of elevation of eosinophil counts and 1 of elevation of platelet counts were observed. In conclusion, CFPZ was considered to be a safe and highly effective antibiotic in pediatric infections.
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PMID:[Clinical study on cefprozil in pediatrics]. 149 36

Cefpirome (HR 810, CPR), a new cephem antibiotic, was investigated for its experimental and clinical studies in pediatrics. The results obtained are summarized as follows. 1. Plasma and urinary levels of CPR were determined in 2 children (age 5 and 7 years) after the one shot intravenous injection of the drug at 20 mg/kg. Average plasma levels of the drug were 44.7 micrograms/ml, 28.5 micrograms/ml, 10.5 micrograms/ml, 4.6 micrograms/ml and 1.5 micrograms/ml at 1/2 hour, 1 hour, 2 hours, 4 hours and 6 hours, respectively, and the average half life was 1.57 hours. Average urinary levels of the drug were 1,785 micrograms/ml, 545 micrograms/ml and 198 micrograms/ml at 0-2 hours, 2-4 hours, 4-6 hours, respectively and the average urinary elimination rate was 52.0%. The results were nearly equivalent to those in adults except for urinary elimination rate which tended to be slightly lower than that in adults. 2. Cerebrospinal fluid levels in 3 cases of purulent meningitis treated with CPR were investigated. Cerebrospinal fluid levels in a case of Neisseria meningitidis were 11.5-23.1 micrograms/ml at 1 hour and 0.94 microgram/ml at 5 hours after intravenous injection of 44.4 mg/kg, 4 times a day. Cerebrospinal fluid levels in a case of Streptococcus pneumoniae were 1.01-4.23 micrograms/ml at 1 hour after intravenous injection of 49.0 mg/kg, 6 times a day, and in the other case with Streptococcus pneumoniae, the levels were 16.8-37.1 micrograms/ml at 1 hour, 11.3 and 3.60 micrograms/ml at 3 and 4 hours after intravenous injection 52.2 mg/kg, 6 times a day. These results are not inferior to those with cefotaxime or ceftriaxone. These levels appear to be higher than MIC90 values against Escherichia coli, Streptococcus agalactiae, S. pneumoniae or Haemophilus influenzae which are the major pathogens of these diseases. 3. CPR was given to 62 patients and clinical efficacy, bacteriological response and adverse reactions were evaluated. Evaluated cases for clinical efficacy included 3 cases of purulent meningitis, 1 case of acute purulent otitis media, 2 cases of acute purulent tonsillitis, 1 case of acute bronchitis, 49 cases of acute pneumoniae, 1 case of scarlet fever, 1 case of acute osteomyelitis, 1 case of acute enterocolitis, and 2 cases of acute UTI, totalling 61 cases. Clinical efficacies were excellent in 38 cases, good in 22 cases and fair in 1 case with an efficacy rete of 98.4% (excellent + good).(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Laboratory and clinical studies on cefpirome in pediatrics]. 188 1

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

Cefixime, the first oral third generation cephalosporin, was administered to 2,832 patients in the USA, UK, FRG and France. 478/1063 patients were treated for urinary tract infections (upper or lower UTI) with 200 mg cefixime bid; clinical cure was obtained in 92 and 96 per cent of upper and lower UTI respectively, and bacteriological cure in 97.5 and 89 per cent of the cases; among 142 patients with a 1 month follow-up, no relapse or reinfection was observed in 78 per cent of cases. Of 521 patients treated for lower respiratory tract infection, 355 received 200 mg cefixime bid and 166 received a single daily dose of 400 mg. Clinical cure was obtained in 88 per cent and 93 per cent patients with pneumonia or bronchitis respectively, with bacteriological cure in 93.2 and 93.8 per cent. Among ENT infections, the most interesting study was in the treatment of sinusitis and otitis. Good clinical results were shown in nearly 95 per cent of cases, with bacteriological cure in more than 90 per cent. The safety studies demonstrated a global 6.6 per cent incidence of undesirable effect. These manifestations were mild and reversible, consisting of abdominal discomfort and minor diarrhea in most cases. The overall effectiveness of cefixime appears to be similar to that of established compounds as far as susceptible pathogens are concerned. However, in clinical trials, cefixime seemed to be effective on isolated bacteria unresponsive to conventional antibiotics.
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PMID:[Efficacy and tolerability of cefixime in international and French studies]. 253 May 48

We have carried out laboratory and clinical studies on cefpodoxime proxetil (CS-807, CPDX-PR). The results are summarized as follows. CPDX-PR was given via oral administration to each 2 children at a single dose of 3 mg/kg and to each of 3 children in a 100 mg tablet. After the oral administration, mean peak serum levels of CPDX obtained for the 2 dose levels were 1.86 +/- 0.35 micrograms/ml and 2.16 +/- 0.63 micrograms/ml at 2 hours, respectively, and mean half-lives were 1.31 +/- 0.02 hours and 1.47 +/- 0.18 hours, respectively. The mean urinary excretion rate of CPDX was 32.8 +/- 1.0% in the first 12 hours after the oral administration of 3 mg/kg. When a dose of 100 mg tablet was given to each of the 3 children, urinary excretion rates in the first 12 hours were 43.5%, 48.6% and 24.8%, respectively. Treatment with CPDX-PR was done in 38 cases of pediatric bacterial infections; 19 cases of tonsillitis, 3 cases of pharyngitis, 1 case of bronchitis, 3 cases of pneumonia, 3 cases of scarlet fever, 2 cases of impetigo, 4 cases of UTI and 1 case each of phlegmone, subcutaneous abscess and balanitis. Results obtained were excellent in 23 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 cefpodoxime proxetil in pediatric field]. 281 Jul 32

We have carried out laboratory and clinical studies on cefteram pivoxil (CFTM-PI, T-2588). The results are summarized as follows. CFTM-PI was given through oral administration to 2 children each at dose levels of 1.5 mg/kg, 3 mg/kg and 6 mg/kg. After administration, mean peak serum levels of CFTM obtained for the 3 dose levels were 0.66 +/- 0.01 microgram/ml, 1.26 +/- 1.05 micrograms/ml and 2.28 +/- 0.95 micrograms/ml at 2 hours, respectively, and mean half-lives were 1.07 +/- 0.52 hours, 1.32 +/- 0.76 hours and 2.53 +/- 1.70 hours, respectively. Mean urinary excretion rates of CFTM were 19.0 +/- 4.0%, 9.4 +/- 1.5% and 19.9 +/- 4.0% in the first 8 hours after administration of 1.5 mg/kg, 3 mg/kg, 6 mg/kg, respectively. Treatment with CFTM-PI was made in 36 cases of pediatric bacterial infections including 20 cases of tonsillitis, 3 cases of bronchitis, 6 cases of scarlet fever, 3 cases of UTI and 1 case each of bronchopneumonia, abscess, staphylococcal scalded skin syndrome and vaginitis. Results obtained were excellent in 22 cases, good in 14 cases. No significant side effect due to the drug was observed in any cases.
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PMID:[Laboratory and clinical studies of cefteram pivoxil in pediatric field]. 281 Jul 60

Pharmacokinetic and clinical studies of imipenem/cilastatin sodium (MK-0787/MK-0791), a newly developed combined antibiotic in a 1:1 ratio, were performed in the field of pediatrics. The MK-0787/MK-0791 was administered to 15 children. Ten and 20 mg/kg doses of MK-0787 were administered by a intravenous drip infusion for 30 minutes to 3 children each. In the remaining 9 cases, MK-0787 doses of 10, 20 and 30 mg/kg were administered to 3 children each by a 1 hour intravenous drip infusion. Levels of MK-0787 and MK-0791 in plasma, urine and urinary recovery rate of the drugs were also determined. In addition, MK-0787/MK-0791 was administered to a total of 29 children; 2 children with bronchitis, 16 with pneumonia, 4 with UTI, 2 with purulent lymphadenitis and 1 child each with tonsillitis, septicemia suspected disease, peritonitis, staphylococcal scalded skin syndrome and osteomyelitis/bacteremia. The average single dose was 15.3 mg/kg of MK-0787 and administrations were performed by 20-60 minutes intravenous drip infusion 3-4 times daily for an average period of 6 days. The clinical and bacteriological effects of this drug were evaluated in these cases and adverse reactions and unusual laboratory findings were also studied in a total of 33 cases including 4 other drop-out cases. Results of these studies were summarized as follows. In 6 children, 3 each who were given doses of 10 or 20 mg/kg, the mean peak plasma concentrations of the drugs were found at the end of the 30 minutes-infusion with values of 35.20 and 74.90 micrograms/ml for MK-0787 and 44.85 and 93.32 micrograms/ml for MK-0791 after the dose of 10 and 20 mg/kg, respectively. The peak plasma levels of MK-0791 were approximately 1.3 times higher than those of MK-0787 and higher peak levels were observed in the groups with larger doses of either drugs. In the 10 mg/kg group, the mean half-lives of MK-0787 and MK-0791 were 0.97 and 0.71 hour, respectively and those values were 0.89 and 0.63 hour, respectively in the 20 mg/kg group. In both group, MK-0787 tended to have longer half-lives than MK-0791. In 9 children, 3 each who were administered doses of 10, 20 and 30 mg/kg by a 1 hour intravenous drip infusion had the highest plasma levels for both MK-0787 and MK-0791 at the end of the infusion.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Pharmacokinetic and clinical studies of imipenem/cilastatin sodium in the pediatric field]. 346 84

Fundamental and clinical studies on cefuzonam (L-105, CZON), a newly semisynthesized cephem antibiotic, were carried out in the field of pediatrics and the following results were obtained. Antibacterial activities of CZON against clinically isolated strains of Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, S. pyogenes, Escherichia coli, Klebsiella pneumoniae, Haemophilus parainfluenzae and H. influenzae were compared with those of cefmenoxime (CMX), latamoxef (LMOX), cefoperazone (CPZ), cefmetazole (CMZ), cefotiam (CTM) and cefazolin (CEZ). CZON was nearly as active as CEZ against S. aureus and S. epidermidis and superior to other antibiotics against other Gram-positive cocci. Against Gram-negative rods, CZON was as active as CMX and superior to other 5 antibiotics compared. Serum concentrations and urinary excretion rates after intravenous bolus injection of CZON at doses of 10 mg/kg, 20 mg/kg and 40 mg/kg for 5 minutes in 1, 5 and 4 cases, respectively, were determined. Mean serum concentrations of CZON at these dose levels were 11.0, 43.8 and 111.5 micrograms/ml at 15 minutes, 2.4, 10.3 and 30.3 micrograms/ml at 1 hour and 0.17, 0.72 and 1.28 micrograms/ml at 4 hours, with serum half-lives of 1.79, 0.88 and 1.19 hours, respectively. Mean cumulative urinary excretion rates within 6 hours after administration were 47.9, 56.3 and 40.3%, respectively. Thirty-four pediatric patients with various bacterial infections (tonsillitis 2, acute bronchitis 1, pneumonia 14, pyothorax 1, sepsis 1, suppurative lymphadenitis 1, UTI 13 and enteritis 1) were treated with CZON at a daily dose of 40-94 mg/kg t.i.d. or q.i.d.. The overall clinical efficacy rate was 94.1%. No adverse reactions were observed except 2 cases with mild diarrhea. Abnormal laboratory findings were also mild; slight elevation of GOT and GPT in 2, eosinophilia in 1 and thrombocytosis in 1. These results clearly indicate the usefulness of CZON in the treatment of bacterial infections in children.
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PMID:[Fundamental and clinical studies on cefuzonam in the field of pediatrics]. 359 89

Fundamental and clinical studies were carried out on cefixime (CFIX) 5% granules, and the results are summarized below. Antimicrobial activity Antimicrobial activities of CFIX, cefaclor, cefroxadine, cephalexin and amoxicillin (AMPC) were studied against clinical isolates. CFIX showed greater activities than all the other antibiotics against E. coli, K. pneumoniae, H. influenzae, P. mirabilis, E. cloacae and S. marcescens, but it was slightly less active than AMPC against S. pyogenes. Absorption and excretion Serum concentrations and urinary excretions of CFIX were determined following single or repeated oral administration. In 8 patients given single dose of CFIX 1.5 or 3.0 mg/kg, mean serum concentrations were 1.27 and 1.09 micrograms/ml at 2 hours, 1.27 and 1.35 micrograms/ml at 4 hours, 0.85 and 1.10 micrograms/ml at 6 hours, 0.17 and 0.24 micrograms/ml 12 hours after administration, respectively. Mean serum half-lives were 2.54 hours for the dose of 1.5 mg/kg and 2.60 hours for 3.0 mg/kg. Urinary recovery rates in the 12-hours urine varied 6.7 to 33.6%, with an average of 13.5%. In 3 patients given a repeated dose of CFIX 3.0 or 5.6 mg/kg b.i.d., the serum concentrations were 0.23-1.01 micrograms/ml at 0 hour, 1.91-2.80 micrograms/ml at 2-4 hours and 1.13-2.07 micrograms/ml at 6-8 hours after administration. Clinical study The CFIX was given orally by mainly b.i.d. at a daily dose of 4.4-11.6 mg/kg for 4-15 days to a total of 33 patients consisting of 3 patients with pneumonia, 3 with bronchitis, 9 with tonsillitis, 15 with UTI, one each with scarlet fever, lymphadenitis and colitis. Clinical responses were excellent in 24 patients, good in 8 and fair in 1, with an effectiveness rate of 97.0%. All of the 21 bacterial isolates examined were eradicated after CFIX treatments including 3 beta-lactamase producing strains. No side effects of abnormal laboratory findings were observed in these patients.
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PMID:[Fundamental and clinical studies on cefixime (5% granules) in the pediatric field]. 376 37

We have evaluated cefixime (CFIX) fine granules for pharmacokinetics and therapeutic effectiveness in children with infections. The results were summarized as follows. Pharmacokinetic parameters after the oral administration of single doses of 1.5 mg and 6.0 mg per kg body weight in a cross-over design in 1 child were as follows: The peak serum CFIX concentrations were 0.65 microgram/ml at 2 to 3 hours and 3.33 micrograms/ml at 4 hours for the low and the high doses, respectively; the respective biological half-lives were 2.4 hours and 2.5 hours, and urinary recovery was 10.3% at 8 hours and 5.2% at 12 hours, respectively. A clinical study was performed on 19 children with infections, including 7 with bronchitis; 3 each with tonsillitis, UTI, and cervical lymphadenitis; and 1 each with pharyngitis, retroauricular lymphadenitis, and enteritis. Doses ranging from 1.8 to 7.8 mg/kg body weight were given b.i.d. or t.i.d. The period of treatment ranged from 3 to 13 days. The therapeutic response was considered "excellent" in 15 and "good" in 4, with an effectiveness rate of 100%. No side effects were observed. The only abnormal laboratory findings was a slight elevation of GOT and GTP recorded in 1 child. It was concluded that CFIX was a promising drug for the treatment of bacterial infections in children.
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PMID:[Fundamental and clinical studies on cefixime in pediatrics]. 376 44


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