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Clinical evaluation of ceftizoxime suppository (CZX-S), a new antibiotic rectal suppository, was performed in 5 cases with bacterial infections in pediatric field (2 with acute bronchitis, 1 with acute tonsillitis, UTI and pertussis, respectively) and the following results were obtained; Blood levels of CZX at 10-20 minutes after administration of CZX-S at a dose of 10.0-26.3 mg/kg in 5 cases were 3.26-23.3 micrograms/ml and the urinary excretion rates within 6 hours were 15.2, 60.1, 60.2% in 3 of 5 cases measured respectively. Clinical effects were excellent in 3 and good in 2 cases. Slight elevation of GOT and GPT was observed in 1 case. No other side effects were observed. The patients' tolerability against rectal suppository was good. From the above results, we concluded that CZX-S is useful for treating the pediatric patients with various infections.
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PMID:[The clinical evaluation of ceftizoxime suppositories in the pediatric field]. 386 83

A fundamental and clinical study of ceftizoxime (CZX) suppositories was performed in pre-school and school-age children. The average time courses of CZX serum and urinary concentrations after administration of CZX suppository 250 mg (i.e. per kg body weight doses of 8.3-10.9 mg) to 4 school-age children were as follows. Serum concentrations: 6.1 micrograms/ml at 15 minutes, 6.3 micrograms/ml at 30 minutes, 3.8 micrograms/ml at 1 hour, 1.7 microgram/ml at 2 hours, 0.5 microgram/ml at 4 hours and 0.2 microgram/ml at 6 hours with a biological half-life of 1.43 hours. Urinary concentrations: 885 micrograms/ml for 0-2 hours, 209 micrograms/ml for 2-4 hours and 112 micrograms/ml for 4-6 hours with an average 6-hour urinary recovery rate of 25.6%. The clinical and biological effectiveness and adverse reactions were studied in 11 infants and school-age children afflicted with various infections (acute purulent tonsillitis, 1; acute bronchitis, 3; acute pneumonia, 4; and UTI, 3). The clinical responsiveness was "excellent" in 8, "good" in 2, and "failure" was recorded in 1, with an overall efficacy of 90.9% inclusive of "excellent" and "good". The microbiological effectiveness of CZX suppositories on presumed pathogenic organisms comprising 4 strains of H. influenzae, 1 strain of H. parainfluenzae, and 3 strains of E. coli was satisfactory, as evidenced by the substantially high eradication rate of 87.5%. The only organism that survived CZX suppository treatment was 1 strain of H. influenzae which however was greatly decreased. The only side effect was diarrhea in 1 patient, which however did not necessitate withdrawal of the drug. The only laboratory test abnormality was GOT and GPT elevation in 1 patient which was normalized within 8 days. In conclusion, CZX suppositories were found to be efficacious and safe for treatment of bacterial infections in children.
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PMID:[Clinical studies of ceftizoxime suppositories in respiratory tract infections and urinary tract infections in children]. 386 84

Laboratory and clinical studies were performed as follows on cefminox (CMNX, MT-141), a new cephamycin antibiotic. Pharmacokinetics Serum concentrations of CMNX were measured in 4 patients given CMNX for prophylactic purpose during cardiac catheterization. In 2 patients given 20 mg/kg of CMNX by intravenous bolus injection, the average of peak serum concentration was 178.9 micrograms/ml at 15 minutes. The mean urinary recoveries in these 2 cases was 66.9% within 6 hours after injection. In 2 patients given 20 mg/kg of this drug by 1 hour drip infusion, the peak serum concentration was obtained at the time drip was completed, and the average value was 68.3 micrograms/ml. Clinical efficacy CMNX was administrated intravenously to 13 patients in dose of 52.9 approximately 96.0 mg/kg t.i.d. or q.i.d. for 4 approximately 7 days; 3 with tonsillitis, 6 with bronchitis, 1 with bronchopneumonia, 1 with UTI, 1 with lymphadenitis and 1 with enterocolitis. The overall efficacy rate was 92.3%, i.e., efficacy was excellent in 12, and poor in 1. Bacteriological efficacy was excellent, i.e., 3 of 3 strains disappeared. Side effects were observed in 3 cases, i.e., 1 case of eruption, 1 case of diarrhea and 1 case of transient eosinophilia. The above results suggest that CMNX is a useful antibiotic for treating pediatric bacterial infections.
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PMID:[Laboratory and clinical studies on cefminox in the pediatric field]. 389 7

Aspoxicillin (ASPC), a new semisynthesized penicillin, was administered to 20 children; by one shot intravenous injection in the doses of 10, 20 and 40 mg/kg to each of 3 children, and by intravenous drip infusion in the doses of 20 and 40 mg/kg over a period of 1 hour to 8 and 3 children, respectively, and the serum levels, urinary levels and recovery rates were determined. ASPC was administered to 1 patient with tuberculous pleurisy in the dose of 20 mg/kg by one shot intravenous injection, then the thoracic fluid level and serum level were determined. In addition, ASPC was administered to 3 children with tonsillitis, 3 with bronchitis, 40 with pneumonia, one each for pleuropneumonia, pleurisy, lung abscess, scarlet fever, staphylococcal scalded skin syndrome and purulent lymphadenitis and 2 with UTI (total 54 children), in the mean dose of 81.4 mg/kg/day t.i.d. (12 children) or q.i.d. (42 children) by one shot intravenous injection for 6 days on the average, and clinical effectiveness and bacteriological response were evaluated in these cases, and adverse reactions and abnormal laboratory findings were examined in the 60 cases which included 6 drop-out cases. After the administration of ASPC to 9 children; 10, 20 and 40 mg/kg to each of 3 children, by one shot intravenous injection, the mean serum levels reached to the peak of 58.4, 147.0 and 221.0 mcg/ml, respectively, in 5 minutes. The mean half-lives were 1.03, 1.01 and 1.23 hours, and the mean areas under the curve (AUCs) were 44.9, 94.1 and 192.9 mcg X hr/ml, respectively. A dose response was seen among the 3 dosage levels. After the administration of ASPC to 11 children; 20 and 40 mg/kg to 8 and 3 children, respectively, by intravenous drip infusion over a period of 1 hour, the mean serum levels reached to the peak of 58.2 and 114.0 mcg/ml, respectively, on completion of the administration. The mean half-lives were 1.22 and 1.09 hours, and the mean AUCs were 109.4 and 181.7 mcg X hr/ml, respectively. A dose response was observed between the 2 dosage levels. In the above mentioned each 3 cases receiving one shot intravenous injection in the dose of 10, 20 and 40 mg/kg, the mean urinary levels of ASPC reached to the peak of 1,000.0, 2,300.0 and 4,350.0 mcg/ml, respectively, at 0 approximately 2 hours after the administration, and the urinary recovery rates during the first 6 hours were 66.1, 66.5 and 56.9%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Fundamental and clinical studies of aspoxicillin in the pediatric field]. 406 28

Aztreonam (AZT) was evaluated for its safety, clinical efficacy and pharmacokinetics in children. AZT was effective in all the 16 children with Gram-negative bacterial infections. The diagnoses included acute bronchitis and pneumonia (11), UTI (2), UTI with bacteremia (1), purulent meningitis (1) and acute mucositis (1). The etiologic agents were H. influenzae (10), B. catarrhalis (1), N. meningitidis group C (1), E. coli (3) and P. aeruginosa (2). The serum half-life was approximately 1.2 hours after intravenous bolus injection. Penetration into the inflamed cerebrospinal fluid was good not only in acute purulent meningitis but also in viral meningitis. From the present study, AZT is a safe and effective antibiotic when used in children with Gram-negative bacterial infections.
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PMID:[Clinical and pharmacokinetic evaluations of aztreonam in children]. 409 55

Sulbactam/cefoperazone (SBT/CPZ) was evaluated in the treatment of pediatric patients to have the following results: Peak serum concentrations which occurred just after the drip infusion of 20 mg/kg SBT/CPZ were 36.4 micrograms/ml and 8.6 micrograms/ml for CPZ and SBT, respectively. The half-life of CPZ was 1.91 hours, and that of SBT, 0.97 hour. Following the 40 mg/kg drip infusion, the peak serum concentration of CPZ was 79.1 micrograms/ml, and that of SBT, 27.0 micrograms/ml. The half-lives were 1.99 hours for CPZ, and 1.07 hours for SBT, respectively. In 6 hours after drip infusion of 20 mg/kg and 40 mg/kg 21.7, 37.0% of CPZ and 41.6, 85.6% of SBT were excreted in urine. Daily doses of about 50-90 mg/kg SBT/CPZ were administered by intravenous or drip infusion to 26 pediatric patients with acute infections such as lacunar tonsillitis, bronchitis, bronchopneumonia, suppurative diseases caused by Staphylococcus (staphylococcal scalded skin syndrome), purulent parotitis, cervical lymphadenitis, phlegmon and acute UTI related with ABPC/CPZ resistant beta lactamase producing E. coli. SBT/CPZ demonstrated the bacteriological effect on all the causative organisms. The clinical efficacy was also confirmed with the efficacy rate of 88.5%. No side effects were observed in all the cases though transient eosinophilia developed in 2 patients.
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PMID:[Fundamental and clinical studies of sulbactam/cefoperazone in the field of pediatrics]. 609 10

Laboratory and clinical studies were performed as follows on ceftizoxime (CZX), a new cephalosporin antibiotic. 1. Susceptibility of clinically isolated bacteria to CZX and cefotiam (CTM) or sulbenicillin (SBPC). Antibacterial activities of CZX and CTM were compared against S. aureus, E. coli, K. pneumoniae, E. cloacae, H. influenzae and E. aerogenes; CZX was compared with SBPC against Ps. aeruginosa. CZX and CTM were nearly equal in activity against S. aureus, but CZX was found to be more active than CTM by 1--10 tubes against E. coli, K. pneumoniae, E. cloacae, H. influenzae and E. aerogenes. Against Ps. aeruginosa, CZX and SBPC were nearly equal in activity. 2. Serum concentration and urinary recovery. Serum concentrations of CZX were measured in 6 patients given CZX for prophylactic purpose during cardiac catheterization. In 2 patients given 20 mg/kg of CZX intravenously, the average serum concentration was 38.9 micrograms/ml at 30 minutes after intravenous bolus injection. In 3 patients given 10 mg/kg of CZX by intravenous drip infusion, the peak average serum concentration was 28.1 micrograms/ml at the end of infusion. Urinary recovery in 2 patients tested was 81.1% and 92.5% until 6--7 hours after intravenous bolus injection. 3. Clinical efficacy. CZX was given intravenously to 24 patients in doses of 30--111 mg/kg (57.1 mg/kg on an average) t.i.d. or q.i.d. for 3--16 days (5.5 days on an average): 1 with lacunar tonsillitis, 4 with acute bronchitis, 12 with pneumonia, 2 with enterocolitis, 2 with soft tissue infection, 2 with lymphadenitis and 1 with UTI. The overall efficacy rate was 95.8%, i.e., efficacy was excellent in 10 (41.7%), good in 13 (54.2%), and poor in 1 (4.2%). Bacteriological efficacy was excellent, i.e. 21 of the 23 strains disappeared. One patient had mild and transient diarrhea, but no other laboratory abnormalities were observed during treatment. The above results suggest that CZX is 1 of the most useful antibiotics for treating pediatric infections, especially due to Gram negative bacteria.
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PMID:[Laboratory and clinical studies of ceftizoxime in pediatrics (author's transl)]. 627 7

Laboratory and clinical studies were performed on cefmenoxime (CMX), a new cephalosporin antibiotic, and the following results were obtained. 1. Susceptibility of clinically isolated bacteria to CMX and cefotiam (CTM) or cefazolin (CEZ) Antimicrobial activity of CMX was compared with that of CTM and CEZ against S. aureus, S. epidermidis, S. pneumoniae, H. influenzae and E. coli. CEZ and CTM were more active than CMX against S. aureus, S. epidermidis and S. pneumoniae. But CMX was found to be more active by 1-10 tubes than CEZ and CTM against H. influenzae and E. coli. 2. Clinical efficacy. CMX was intravenously administered to 19 patients; 3 with lacunar tonsillitis, 2 with acute bronchitis, 8 with bronchopneumonia, 3 with UTI, 1 with septicemia, 1 with acute panperitonitis, 1 with S.S.S.S. at daily doses of 30-115 mg/kg (64.6 mg/kg on an average) t.i.d. or q.i.d. for 3-17 days (6.1 days on an average). The overall efficacy rate was 94.7%, i.e., efficacy was excellent in 10 cases (52.6%), good in 8 cases (42.1%), and poor in 1 case (5.3%). Bacteriological efficacy was good, i.e. 16 of the 19 strains disappeared. Transient eosinophilia was observed in 1 patient, but no other laboratory abnormality was observed during treatment. The above results suggest that CMX is 1 of the useful antibiotics in treatment of pediatric infections, especially due to Gram negative bacteria.
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PMID:[Laboratory and clinical studies of cefmenoxime in the pediatric field]. 630 38

The authors have carried out the laboratory and clinical studies of cefadroxil (CDX). The results were as follows; The sensitivity was measured by plate dilution method on 27 strains of S. aureus and E. coli, 26 strains of K. pneumoniae isolated from patients. The distribution of sensitivity of S. aureus was 3.13-12.5 microgram/ml and the peak of distribution was 3.13 microgram/ml and 6.25 microgram/ml, of E. coli was 6.25 microgram/ml by 10(8) cells/ml. And the distribution of sensitivity of K. pneumoniae was 6.25-25 microgram/ml and its peak was 6.25 microgram/ml by 10(8) cells/ml. CDX were given orally at dose of 10 mg/kg to 3 children. The serum levels of CDX were 10.5 +/- 1.78 microgram/ml, 15.8 +/- 3.25 microgram/ml, 12.0 +/- 0.41 microgram/ml and 3.9 +/- 0.9 microgram/ml at 0.5, 1, 2, 4 hours after administration respectively, and was 2.3 +/- 0.48 microgram/ml at 6 hours. The urinary excretion rate was 55.6% up to 8 hours after administration. CDX were administered to 39 cases of pediatric infectious disease (26 cases with tonsillitis, 5 cases with enterocolitis, 3 cases with UTI, 2 cases with impetigo, each one case with bronchitis, cervical lymphadenitis and epididymitis). And CDX were given 25.0-65.2 mg/kg daily. Clinical results obtained were above good in all cases. No side effects were observed in any cases, except for one case, with diarrhea, 6 cases with the elevation of serum transaminase and 1 case with eosinophilia.
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PMID:[Laboratory and clinical studies of cefadroxil (author's transl)]. 701 97

We investigated pharmacokinetics and clinical effectiveness of a newly developed cephem antibiotic cefozopran (SCE-2787, CZOP) against various pediatric infections in 18 institutions and their affiliates. We obtained the following results. 1. Serum concentration and urinary excretion rates Pharmacokinetics of CZOP in children was examined after intravenous injection and 30-minute drip infusion of 10, 20 and 40 mg/kg of CZOP. Peak serum concentrations of CZOP in 30 minutes after intravenous injection were 21.7, 51.5 and 77.8 micrograms/ml, respectively, showing a clear dose response. Half-lives were 1.99, 1.85 and 1.67 hours, respectively. In the first 6 hours after administration, urinary excretion rates of CZOP were 87.3, 67.4 and 84.1%, respectively. In the cases of 10, 20 and 40 mg/kg administration of CZOP 30-minute drip infusion, peak serum concentration of CZOP in 30 minutes, when the infusion was completed, were 38.1, 72.8 and 95.6 micrograms/ml, respectively. Again, there was a clear dose response. Half-lives were 1.67, 1.69 and 1.43 hours, respectively. In the first 6 hours after administration, urinary excretion rates of CZOP were 53.9, 59.7 and 77.3%, respectively. Cerebrospinal fluid concentrations of CZOP administered by intravenous injection of 50 mg/kg to patients with purulent meningitis were 1.6 to 43.4 micrograms/ml in 1 to 1.5 hours after administration. 2. Clinical study Clinical efficacy was evaluated in 337 cases. The largest number of cases, 138 cases, were found in 2 to < 6-year olds. The majority of the patients were under age 9, and 70 cases were of less than 1-year old infants. 183 cases were males and 154 cases were females. In terms of illness, a majority, or 185 cases, suffered from pneumonia, followed by 39 cases of UTI and 23 infections of the skin and soft tissue. There were 7 cases of purulent meningitis. In 218 cases, CZOP was administered at a daily dose of 60- < 80 mg/kg. The drug was administered for 6-10 days, the most frequent duration, in 188 cases. In the cases where causative organisms were identified (group A), the efficacy rates ("excellent" and "good") obtained were 100% (5/5) against purulent meningitis, 100% (2/2) against sepsis, 98.3% (119/121) against pneumonia, 100% (13/13) against acute bronchitis, 100% (11/11) against upper respiratory tract infection, 96.3% (26/27) against UTI. Overall, "excellent" and "good" responses were observed in 97.5% (197/202) of cases with known causative organisms.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Pharmacokinetic and clinical studies with cefozopran in the pediatric field. Pediatric Study Group of Cefozopran]. 811 68


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