Gene/Protein Disease Symptom Drug Enzyme Compound
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Aspoxicillin (ASPC), a new penicillin for injection, was evaluated for its efficacy and safety in 29 children with bacterial infection (Table 1), and the following results were obtained. MICs of ASPC to 26 strains of isolated organisms are shown in Table 2. MICs to 4 out of 13 strains of H. influenzae were higher than 6.25 micrograms/ml. MICs to 5 strains of S. pneumoniae were lower than 0.78 microgram/ml and 1 out of 3 strains of S. aureus and 1 strain of E. coli showed higher MICs than 100 micrograms/ml. ASPC was administered in 3 or 4 divided doses at a daily dosage ranging from 21 to 98 mg/kg by 30 minutes drip infusion or intravenous injection to 29 patients (16 cases of pneumonia, 8 cases of tonsillitis, 3 cases of bronchitis, 1 case of urinary tract infection, 1 case of impetigo) and the following clinical results were obtained: excellent; 11 cases, good; 11 cases, fair; 3 cases, poor; 1 case. The overall efficacy rate was 85% (Table 3, 4). No clinical side-effects were observed in any of the patients. Leukopenia was noted in 1 case. Slight elevation of GOT and GPT was noted in 2 cases, and minimal elevation of GOT was observed in other 2 cases (Table 5). These data suggest that ASPC is an useful new antibiotic in the treatment of children with susceptible bacterial infection and may be used as the first choice antibiotic for the treatment of respiratory tract infection in children.
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PMID:[Clinical evaluation of aspoxicillin in children]. 385 58

Aspoxicillin (TA-058, ASPC) was given intravenously to 20 children with the following acute bacterial infections; 11 cases of bronchopneumonia, 5 cases of urinary tract infection, 2 cases of acute bronchitis, 1 case of staphylococcal scalded skin syndrome and 1 case of subcutaneous abscess. Clinical effectiveness was obtained in 14 cases out of 20 cases (70%) and bacteriological eradication in 8 cases out of 10 cases (80%). With ASPC the following side effects developed; transient diarrhea in 1 case, eruption in 1 case and slight elevation of GOT in 1 case. From the above clinical results, it is apparent that ASPC is an useful antibiotic for treating pediatric patients with various kinds of bacterial infections.
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PMID:[Clinical experience with aspoxicillin in the pediatric field]. 385 63

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