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Clinical effects of SY5555 dry syrup, a new oral penem antibiotic, were analysed in 20 children with various bacterial infections. Ages of the patients varied from 8 months to 14 years. Doses of SY5555 were varied from 12.8 mg/kg/day to 30.5 mg/kg/day, and it was administered in 3 divided dosages. Clinical efficacy rates were as follows; 6/7 in acute bronchitis, 5/5 in pharyngotonsillitis, 3/3 in acute otitis media and 2/2 in cystitis and 3/3 in impetigo contagiosa. The overall rate was 95.0% (19/20). Bacteriologically, eradications were obtained with 1/2 strains of Streptococcus pyogenes, 3/3 of Staphylococcus aureus, 1/1 of Haemophilus influenzae, and each of Staphylococcus epidermidis, Haemophilus parainfluenzae, coagulase-negative staphylococci and Serratia marcescens. Diarrhea was observed in 1 patient. And elevated eosinophiles or GPT was observed in one patient each. In vivo pharmacokinetics of SY5555 was examined in 2 cases. Peak plasma levels were observed at 1 hour after dosage in one patient and at 2 hours in another upon oral administration of 8.3 mg/kg of SY5555, and peak levels were 2.44 and 1.38 micrograms/ml respectively. Half-lives of SY5555 were 1.39 and 0.59 hr. Concentrations of SY5555 in urine after administration were 70.2 (2-4 hrs.) to 91.0 (0-5 hrs.) micrograms/ml, respectively. SY5555 dry syrup is considered as an useful and safe antibiotic in treating the infectious diseases in children.

Three children with severe candidal infections were treated with fluconazole (FLCZ). An excellent effect or a partial effect was obtained in each case. Case 1 was a boy with candida esophagitis. He had been treated for relapsed ALL and became febrile with severe swallowing pain. FLCZ was administered intravenously and he became afebrile after 10 days of the therapy. Case 2 was a boy with candida pneumonitis. He had been treated for relapsed ALL and became febrile with diffuse infiltration in chest X-ray. FLCZ was administered intravenously and he became afebrile transiently, though fever and abnormal X-ray shadows reappeared soon and died of pneumonia and leukemic infiltrations. Case 3 was a girl with candida pneumonitis. She had been treated for relapsed neuroblastoma and became febrile and dyspneic. She was treated with intravenous FLCZ with no effects and died of pneumonia. All three patients showed positive results in 2 of 3 markers for candida infection, including, Cand-Tec, D-arabinitol and fungal index. FLCZ was well tolerated and no adverse effects or abnormal laboratory test results were observed. FLCZ was considered as an effective and safe antifungal agent in the treatment for fungal infections in children.

Therapeutic effects of cefprozil (CFPZ, BMY-28100), a new cephalosporin, were examined in various infectious diseases in children. Clinical efficacy rates were 50% (2/4) in acute bronchitis, 80% (4/5) in pharyngitis, 0% in laryngitis, 100% (7/7) in tonsillitis, 100% (8/8) in impetigo contagiosa, furuncle and posthitis. Hence, the overall efficacy rate was 84% (21/25). Adverse effects were observed in 1 case with slightly elevated serum GOT and GPT. Changes in serum concentrations and urinary excretion of CFPZ were examined in 4 and 2 children without infection, respectively. T 1/2 values obtained were between 1 hour to 2 hours (bioassay). Six hour recovery rates in urine were 51.8% and 77.8% (bioassay). CFPZ was considered to be a safe and useful drug in treating various infectious diseases in children.

The clinical efficacy and the pharmacokinetics of cefpirome (CPR, HR 810), a new semisynthetic cephalosporin derivative, were investigated in children with various infectious diseases. CPR showed high blood peak levels, relatively long half-life and high levels in urine. Excellent clinical efficacy was obtained in 2/3 cases with pneumonia, 3/4 cases with upper respiratory infection, 2/2 cases with cutaneous and soft tissue infection and 1/1 case with urinary tract infection. The overall efficacy rate was 80%. No clinical adverse effects were observed while slightly elevated GPT and GOT, decreased platelet were detected in 4 cases without clinical problems. CPR should be an useful and safe drug in treating infectious diseases in children.

The therapeutic effects of cefminox (CMNX, MT-141), a new synthetic cephalosporin antibiotic, were examined in the treatment of various pediatric infections. Patients treated were infants and children ranging from 12 days after birth to 12 years old suffering from bronchopneumonia in 10 cases, urinary tract infection in 6 cases, pharyngitis in 2 cases, cervical lymphadenitis in 2 cases, suppurative meningitis, cervical abscess, mastoiditis, peritonitis, bronchitis in 1 case each, total of 25 cases. As regards method of administration, CMNX from a vial was dissolved in physiological saline or distilled water for injection, and the solution was administered by 3 to 5 minutes one shot intravenous injection (15 cases), or CMNX was diluted with large volume parenteral product and administered by 30 to 60 minutes drip infusion (10 cases). The dosage of the drug was 21.3 to 165.5 mg/kg/day. The administration was continued for 3 to 13 days except 1 case. As regards clinical efficacy, good or excellent results were obtained in all cases except 3 cases, 1 case was urinary tract infection with cerebral palsy and vesicoureteral reflux, and 1 case was bronchopneumonia with Down syndrome and endocardial cushion defect, the other was suppurative meningitis. Total effective rate was 88%. No clinical side effects nor abnormal laboratory findings obviously attributable to CMNX were observed.

The therapeutic effect of ceftizoxime suppositories (CZX-S) was studied in 8 physically handicapped patients, comprising 6 with pharyngitis, 1 with pneumonia, and 1 with urinary tract infection. The clinical effect was "excellent" in 7 and "good" in 1. Neither adverse reactions nor abnormal laboratory test findings attributable to CZX-S were detected. CZX-S proved to be useful in physically handicapped children, especially in those not suited to treatment with oral or intravenous preparations.

T-1982 (cefbuperazone) was given at a daily dose of 42-80 mg/kg to 7 children with bacterial infections; 3 with bacterial intestinitis, 1 with bronchitis, 1 with tonsillitis and 2 with urinary tract infections. Clinical effectiveness was obtained in 6 cases, and the rate was 85.7%. Bacteriological responses were "disappeared" in 4 cases, "decreased" in 1 case and "unknown" in 2 cases. No noticeable side effects were observed except elevation of eosinophil in 1 case.

In order to ascertain the therapeutic effects of cefoxitin (CFX), a new semisynthetic cephamycin antibiotic, it was administered to pediatric patients with several infections. There were 8 patients with acute respiratory disease (ARD), 3 with urinary tract infection (UTI), 2 with appendicitis complicated with peritonitis, 2 with scarlet fever, one each of left coxitis, infected medial cervical cyst, febrile illness after a V-P shunt operation, purulent parotitis and intractable diarrhea with fever, namely, a total of 20 patients aged from one month to 11 years 6 months. A CFX vial which contained 1 g of CFX was used in two ways, i.e., one shot intravenous injection and drip infusion. The dosage of the drug varied from 57 to 121 mg/kg/day and the administration was continued from 2 to 20 days. Clinical effects were evaluated as follows: when cardinal symptoms disappeared within 3 days it was considered to be 'excellent'; within 5 days 'good'; and no change of clinical symptoms within 5 days 'poor'. The bacteriological effect was expressed as 'eliminated', 'unchanged' and 'undetermined'. Clinical efficacy evaluated as 'excellent' occurred in 11 cases, 'good' in 8 cases and 'poor' in 1 case, the efficacy rate being 95.0%. When classified by the disease, the efficacy rate was as follows: 'good' to 'excellent' in 7 out of the 8 cases of ARD, 'excellent' in all of the 3 cases of UTI, 'good' and 'excellent' in the 2 cases of scarlet fever and in the 2 cases of peritonitis, 'excellent' in each case of left coxitis, purulent parotitis and intractable diarrhea with fever, 'good' in each case of infected medial cervical cyst and febrile illness with a V-P shunt operation. From the bacteriological point of view, 'eliminated' occurred in 5 cases, 'reduced' in 1 case and 'undetermined' in the 2 cases of ARD, 'eliminated' in all of the 3 cases of UTI, 'eliminated' in 1 case and 'undetermined' in the 1 case of peritonitis, 'undetermined' in the 2 cases of scarlet fever, 'eliminated' in each case of infected medial cervical cyst and purulent parotitis and 'undetermined' in the other cases. Antimicrobial efficacy measured by MIC was compared with CEZ and CET, and the results were as follows: CFX was inferior to the two cephalosporins for S. aureus, it was between CEZ and CET for H. influenzae and H. parainfluenzae, and CFX was superior to CEZ and CET for E. coli. All of the 3 antibiotics had poor antimicrobial efficacy for P. aeruginosa and S. faecalis. There were neither clinical side effects nor abnormal laboratory findings which were obviously attributable to CFX during and after administration of the drug.

Clinical application to ascertain the effects of aspoxicillin (ASPC), a new semisynthetic penicillin antibiotic, upon several infectious diseases of children was performed in 7 cases with pneumonia, 5 cases with acute bronchitis, each case with tonsillitis, enterocolitis, urinary tract infection and suspected sepsis. ASPC was injected by drip infusion and the dosage was 63-117 mg/kg/day in 3 and 4 times a day. Clinical efficacy obtained as "excellent" was in 7 cases, "good" in 8 cases "poor" in 1 case, and efficacy rate was 93.8%. From the bacteriological point of view, eliminated in each of H. influenzae, H. parainfluenzae, group A beta-Streptococcus and unchanged in a case of E. coli. There were transient thrombocytopenia in 2 cases and eosinophilia in 3 cases.

Clinical and bacteriological effects of ampicillin suppository (KS-R1) were determined in 9 cases with urinary tract infection and 13 cases with upper respiratory tract infection in children. Clinical effects were excellent in 1 case, good in 18 cases, fair in 2 cases and poor in 1 case. Bacteriological effects were eradication in 6 cases, decrease in 1 case, persistance in 3 cases and replacement in 1 case among 11 cases which were measured the pathogens before and after treatment. As to the side effects, one patient showed watery diarrhea, and another one showed the elevation of GOT. KS-R1 is considered to be a useful drug for the treatment of infection in children both clinically and bacteriologically.

We have evaluated sultamicillin (SBTPC) fine granules for pharmacokinetics and therapeutic effectiveness in children. The results are summarized as follows. 1. Pharmacokinetic parameters after the oral administration of single dose of 5.0 mg per kg body weight in 1 child were as follows: The peak serum concentrations of ampicillin (ABPC) and sulbactam (SBT) were 1.92 micrograms/ml at 1 hour and 1.85 micrograms/ml at 1 hour, respectively. The half-lives in serum and urinary excretion rate for ABPC and SBT were similar. 2. A clinical study was performed on 15 children with infections, including 4 with tonsillitis, 5 with pharyngitis, 2 each with bronchitis, cystitis, and urinary tract infections. Doses ranging from 6.7 to 18.2 mg/kg body weight were given tid. or qid. Lengths of treatment ranged from 5 to 10 days. The therapeutic responses were considered "excellent" in 6 and "good" in 9, with an effectiveness rate of 100%. 3. As to side effects of the drug, diarrhea was observed in 1 patient. It was concluded that SBTPC was a promising drug for the treatment of bacterial infections in children.

The therapeutic effects of cefmenoxime (CMX), a new synthetic cephalosporin antibiotic, were examined in the treatment of various pediatric infections. Patients treated were infants and children ranging from one-month-old to 13-year-old suffering from pharyngitis in 2 cases, bronchopneumonia in 3 cases, cervical lymphadenitis in 2 cases, urinary tract infections in 7 cases, tympanitis in 2 cases, suppurative meningitis, sepsis, subcutaneous apostem, acute enteritis, chest wall apostem, phlegmon, staphylococcal scalded skin syndrome in 1 case each, a total of 23 cases. As regards method of administration, CMX from a vial was dissolved in physiological saline or distilled water for injection, and the solution was administered by 3 to 5 minutes one short intravenous injection (14 cases), or CMX was diluted with large volume parenteral product and administered by 30 to 60 minutes drip infusion (9 cases). The dosage of the drug was 30 to 200 mg/kg/day; 103 mg/kg/day and under in 21 cases, 150 mg/kg/day and 200 mg/kg/day in 1 case each. The administration was continued for 3 to 27 days. As regards clinical efficacy, "good" or "excellent" results were obtained in all the cases except 2 cases, one was alpha-Streptococcus acute tympanitis supervening neuroblastoma, and the other was Pseudomonas urinary tract infection. The efficacy rate was 91.3% with excellent in 11 cases, good in 10 cases. As regards bacteriological effects, of 13 strains of Gram-positive bacteria, 10 strains were eliminated and 3 strains were not changed, while of 10 strains of Gram-negative bacteria, 8 strains were eliminated and 2 strains were reduced; thus CMX showed better results against Gram-negative bacteria rather than against Gram-positive ones. The antimicrobial activity of CMX against Gram-positive bacteria was inferior to those of CTM and CEZ, but CMX showed the highest antimicrobial activity against Gram-negative bacteria. No clinical side effects nor abnormal laboratory findings obviously attributable to CMX were observed.

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.