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Pharmacokinetic and clinical studies were performed on flomoxef (FMOX, 6315-S), a new oxacephem antibiotic, as follows. 1. Pharmacokinetics Serum concentrations of FMOX were measured in 2 cases given 20 mg/kg bolus injection. In the 2 cases, peak concentrations of the drug were 44.3 and 197 micrograms/ml at 15 minutes, T1/2 (beta) were 0.76 and 0.47 hour and AUC were 44.8 and 169.5 micrograms.hr/ml, respectively. Urinary recovery rates for these cases during 6 hours were 83.1 and 54.9%, respectively. The extremely high peak serum concentration in one case may be attributed to dehydration. 2. Clinical efficacy FMOX was administrated intravenously to 12 patients, 6 with pneumonia, 2 with cellulitis, 1 each with bronchitis, tonsillitis, purulent lymphadenitis and subcutaneous abscess, in doses of 55.0-120.0 mg/kg (average 82.2 mg/kg) t.i.d. for 4-13 days (average 6.2 days). The overall efficacy rate was 100%, with excellent responses in 10 and good in 2. Bacteriological efficacy was excellent; 4 of 5 strains were eradicated and 1 strain was decreased. No clinical side effect was observed. Laboratory abnormality was observed in 1 case with transient eosinophilia. The above results suggested that FMOX would be an useful antibiotic for treating pediatric bacterial infections.

In order to evaluate efficacy and safety, cefamandole, a new cephalosporin, was given intravenously to 12 children with respiratory tract infections (11 cases) and urinary tract infection (1 case), who ranged in age from 2 months to 5 years old. Cefamandole sodium was administered 74 approximately 112 mg/kg/day in three or four equally divided doses by one-shot injection. The overall efficacy rate was 83.3% in 12 cases, i.e., good in 8, fairly good in 2, and poor in 2 cases. No adverse reaction was noted on any of our 12 cases.

Using a new cephamycin antibiotic, cefoxitin, clinical studies were carried out, and the following results were obtained: (1) Cefoxitin was administered to 52 children with 38 respiratory tract infections, 2 urinary tract infections, 1 acute otitis media and others, who ranged in age from 2 months to 11 years old. (2) Cefoxitin was given intravenously at a daily dose of 27.3 mg/kg to 110.5 mg/kg. (3) The overall efficacy rate was 80% in 46 cases, i.e., excellent in 10, good in 27, fair in 7 and poor in 2. (4) Clinical side effects were not seen except exanthema in 1 patient. Elevation of GOT and GPT was seen in 2 patients, elevation of A1-P in 1 and eosinophilia in 2 by laboratory tests. However, these findings were alleviated rapidly following the cessation of therapy.

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.

A clinical trial of ceftizoxime suppositories (CZX-S) was performed to evaluate the therapeutic effectiveness in children with bacterial infection. The subjects were 10 children comprising 4 with pneumonia, 3 with lacunar tonsillitis, 2 with pharyngitis, and 1 with UTI. They were given 1 suppository containing either 125 mg or 250 mg of CZX 2 to 4 times a day. The daily per kg body weight dose ranged from 17.1 to 60.0 mg. The result was "markedly effective" in 3, "effective" in 6, and "failure" was recorded in 1. Bacteriologically, successful eradication of causative organisms was confirmed in all the 4 children who underwent the test. No clinical side effects were observed. The only laboratory test abnormality recorded in a single patient was eosinophilia, which was not definitely ascribable to CZX-S. In conclusion, CZX-S have proved to be a clinically safe and effective antibiotic preparation in infantile infection, even in children whose treatment with conventional antibiotics is associated with difficulties.

In order to evaluate effectiveness of ABPC suppository (KS-R1) in the treatment of bacterial infections of children, the clinical studies were carried out. KS-R1 was given in rectum to 14 patients in doses of 24.2 approximately 65.8 mg/kg (average 38.5 mg/kg) in 3 approximately 4 divided doses for 3 approximately 8 days (average 4.0 days); 6 with acute tonsillitis, 3 with pneumonia, 1 with otitis media, 4 with UTI. The overall efficacy rate was 100%. Bacterial efficacy was good, i.e. 8 of the 8 strains disappeared. Any clinical side effects and laboratory abnormalities were not observed during treatment. The above results suggested that KS-R1 is a useful antibiotics for pediatric bacterial infections.

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.

Clinical studies were performed as follows on aspoxicillin (ASPC), a new semisynthetic penicillin. ASPC was intravenously given to 12 patients in doses of 57.7-129.0 mg/kg on average) t.i.d. or q.i.d. for 4-7 days (5.7 days on average): 9 with pneumonia, 1 with tonsillitis, 1 with purulent lymphadenitis and 1 with urinary tract infection. The overall efficacy rate was 83.3%, i.e. efficacy was excellent in 8 (66.7%), good in 2 (16.7%), fair in 1 (8.3%) and poor in 1 (8.3%). Bacteriological efficacy was excellent, i.e. 6 of the 6 strains disappeared. No clinical side effects were observed during treatment. Laboratory abnormalities were observed in 3 cases, slight elevation of GOT in 1, slight elevations of GOT and GPT in 1 and mild eosinophilia in 1. The above results suggest that ASPC is an useful antibiotic for treating pediatric bacterial infections.

A combination drug of sulbactam/ampicillin (SBT/ABPC) was intravenously administrated to 18 patients with ages 3 months to 10 years 10 months with various acute infections including 14 cases of pneumonia, 1 case each of tonsillitis, subacute bacterial endocarditis, empyema and suspected sepsis. Clinical responses were excellent in 14 cases and good in 4 cases. Bacteriological responses of 8 isolated strains were: 7 strains were eradicated and 1 strain was decreased. No side effect was observed in any case. Eosinophilia was observed in 2 cases, thrombocytosis in 2 cases, elevation of GOT in 1 case and elevations of GOT and GPT in 1 case. From the above results, it seemed that SBT/ABPC was a useful drug for the treatment of bacterial infections in the pediatric field.

In order to evaluate effectiveness of cefroxadine (CXD) in the treatment of bacterial infections of children, the clinical studies were carried out. CXD was orally administered to 30 patients at daily dose of 27.5 approximately 50.0 mg/kg (average 32.3 mg/kg) in 3 approximately 4 divided dose for 3 approximately 10 days (average 4.9 days). The overall efficacy rate in 30 cases was 93.3%, i.e., excellent 22 (73.3%), good in 6 (20.0%), fair in 1 (3.3%) and poor in 1 case (3.3%). Drug eruption and transient eosinophilia were observed in 1 case each out of 30 cases (6.7%), but any other abnormality was not observed throughout this series. Based on the above results, CXD was thus considered to be a useful antibiotic in treatment of pediatric infections.