To a total of 31 patients (18 in-and 13 out-patients) having respiratory infections, we administered ofloxacin (OFLX) orally at a daily dose of 300 to 600mg and examined its clinical effect. The clinical effect in the 31 cases was as good as 83.9%. Among these cases, 6 cases showed Pseudomonas aeruginosa, thereby indicating the effective rate of OFLX at 50%.
In the present examination, we experienced cases in which OFLX-resistant P. aeruginosaappeared in the cases of long-term administration of OFLX. Therefore, our clinic carried out the sensitivity test of P. aeruginosa against OFLX, gentamicin (GM) and imipenem (IPM) in 1987, using clinically-segregated strains of P. aeruginosa obtained by sputum tests.
The sensitive strains, which were 100% sensitive to OFLX, GM, IPM respectively in 1985, showed, in segregated strains in 1987, sensitivity of OFLX 57.1%, GM 85.7% and IPM 100%, thus indicating the high resistance-acquiring frequency of P. aeruginosa against OFLX.

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Infectious episodes in 90 patients with hematological disorders were treated with sulbactam/cefoperazone (SBT/CPZ), a new combination drug of a potent S-lactamase inhibitor, sodium sulbactam, and a third generation cephalosporin, sodium cefoperazone. Clinical responses to the SBT/CPZ regimen were excellent in 23 cases, good in 30 cases, fair in 11 cases, and poor in 26 cases. The overall efficacy rate (percentage of cases showing excellent or good responses) was 58.9%. Efficacy rates classified according to different infections were: 80% in documented sepsis, 57.6% in suspected sepsis, 61.1% in pneumonia and 50% in other infections. One episode of side effect was encountered with redness and itching of skin. Hepatic disorders were observed in 3 cases. These adverse reactions, however, were not serious. These results indicate that SBT/CPZ has a high therapeutic efficacy to severe infections in patients with hematological disorders.

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Forty one patients with infections associated with leukemia and related disorders were treated with cefpiramide (CPM). In 26 patients among them, we were able to evaluate the effectiveness of CPM against infections. Fifteen patients were not evaluated, because 6 patients were subjected to additional therapy such as γ-globurin and other antibiotics, 5 were prophylactically treated, 2 had fever episode which were retrospectively reviewed to be originated from tumor mass, 1 received too short a duration of administration of CPM (2 days) to evaluate its effectiveness, and 1 with whom no precise data were recorded. Excellent responses were observed in 10 patients (38.5%) and good responses in 6 (23.1%) among these 26, with a total efficacy rate of 61.5%. Whereas, we found only one patient who showed an unfavorable side effect out of 31 patients including the 26 and 5 other patients who were prophylactically treated. The side effect observed was a mild bleeding tendency occurred in 77 years old female at 11 days after CPM was administrated. The bleeding tendency was easily diminished with the cessation of CPM treatment and a parenteral use of vitamin K. These results suggest that CPM is an effective and safe antibiotic for the treatment of infections in patients with leukemia and related disorders.

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Twenty-six children were treated with cefteram pivoxil (CFTM-PI) and the clinical efficacy and side effects were evaluated. Ages of the patients ranged from 8 months to 9 years. Doses of CFTM-PI ranged 17.5-20.1mg/kg/day for 4 to 19 days. The twenty-six patients including 10 patients with tonsillitis, 1 pharyngitis, 3 otitis media, 2 scarlet fever, 1 bronchopneumonia, 1 lymphadenitis, 6 urinary tract infections, 1 vaginitis and 1 staphylococcal scalded skin syndrome were evaluated for clinicall efficacy. Results were excellent in 11, good in 13, and fair in 2 patients. Out of the 26 patients, one case showed elevated GOT and GPT, and another case showed elevated GOT.
The pharmacokinetic study of CFTM-PI was performed in 9 fasting patients whose ages ranged from 2 to 11 years. Serum peak concentrations of CFTM were 0.92 to 1.05μg/ml (mean 0.99μg/ml) at 1 to 2 hours after a dose of 1.5mg/kg each to 3 patients, 1.12 to 1.38μg/ml (mean 1.25μg/ml) after a dose of 3mg/kg each to 3 patients and 0.66 to 2.1μg/ml (mean 1.17μg/ml) after a dose of 6mg/kg each to 3 patients. The portions of the drug excreted into urine within 8 hours were 8.9% and 14.7% in 2 patients, each given a dose of 1.5 mg/kg, from 13.0 to 23.1% (mean 18.4%) in 3 patients, each given a dose of 3mg/kg, and 6.3% and 8.7% in 2 patients, each given a dose of 6mg/kg.

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Cefteram pivoxil (CFTM-PI), in fine granules, was studied in pediatric infections and the results obtained are summarized below. It is concluded that CFTM-PI fine granule is an effective drug for the treatment of pediatric infections.
1. The pharmacokinetics of CFTM-PI fine granules was studied in 7 patients (5 males, 2 females) whose ages ranged from 9 to 15 years.
(1) In 2 patients, administered with the drug at a dose of 3mg/kg in the fasting state, serum peak concentrations of CFTM at 2 hours after administration were 0.66 and 0.53μg/ml, and T1/2 were 1.40 and 1.32 hours, respectively. Urinary recovery rates in the first 8 hours were relatively low at 5.8 and 10.8%, respectively.
(2) In 1 patient, the drug administered at a dose of 6mg/kg in the fasting state, serum peak concentration of CFTM at 2 hours after administration was 3.0μg/ml, T1/2 was 2.16 hours, and urinary recovery rate in the first 8 hours was 13.8%.
In another 2 patients, CFTM-PI administered at a dose of 6mg/kg after meal, serum peak concentrations of CFTM at 4 hours after administration were 5.8 and 2.5μg/ml, T1/2 of the latter was 1.93 hours, and urinary recovery rates in the first 8 hours were 27.0 and 14.4%, respectively.
(3) In yet another 2 patients, CFTM-PI tablets was administered at a dose level of 150mg after meal. Serum peak concentrations of CFTM were 1.7 and 1.6μg/ml at 2 hours and 4 hours after administration, respectively, T 1/2 of the former was 1.38 hours, and urinary recovery rates were 24.1 and 15.5%, respectively.
2. Clinical results
CFTM-PI as fine granules was administered to 18 patients, and the following results were obtained.
(1) 12 cases (6 males, 6 females) with their ages ranged from 3 months to 12 years were administered with the drug at a dose of 10mg/kg/day, divided into 3 equal portions. Clinical efficacies were fair in 1 case with bronchopneumonia, good in 3 cases with bronchitis and in 4 cases with tonsillitis/pharyngitis, excellent in 1 and good in another with scarlet fever, and good in 1 and poor in another with urinary tract infection (UTI)
(2) Six cases (4 males, 2 females) with their ages were 6 and 7 years were administered with CFTM-PI at a dose of 20mg/kg/day divided into 3 equal portions. Clinicalefficacies were good in 1 case with bronchopneumonia, 2 cases with bronchitis and 3 cases with tonsillitis/pharyngitis.
(3) Bacteriological responses were: eradication in 4 of 4 strains of Haemophilus influenzae, eradication in 3 and unknown in 1 of 4 strains of Streptococcus pyogenes, eradication of 1 strain of Escherichia coli and no change of 1 strain ofKlebsiella pneumoniae identified in a case of UTI.
3. No refusal of the drug due to its taste occurred and no adverse reaction was observed.

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Cefteram pivoxil (CFTM-PI), a newly developed oral cephem antibiotic was administered to treat 16 children with various infections. The results were summarized as follows.
1. The clinical responses were “excellent” in 7, “good” in 5, “fair” in 3 and “poor” in 1, with 75.0% efficacy rate.
2. No side effects and no abnormal laboratory findings were observed.

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Pharmacokinetic and clinical studies of cefteram pivoxil (CFTM-PI, T-2588) fine granules in children were performed and the following results were obtained.
1. Peak serum concentrations in 4 children given orally a dose of 3mg/kg and 2 children given orally a dose of 6mg/kg after meal were reached in 3 to 4 hours and the concentration curves were dependent on dosage levels. The urinary recovery rates up to 8 hours were 29.7% in children given a dose of 3mg/kg and 29.7% in children given a dose of 6mg/kg.
2. Clinical efficacies were evaluated in 38 patients with bacterial infections. Twenty seven patients were given each doses of 3mg/kg in 3 times a day and other 11 patients each doses of 6mg/kg in 3 times. Clinical effects of CFTM-PI were excellent in 18, good in 19, fair in 1 case, hence the overall clinical efficacy rate was 97.4%.
3. Bacteriologically, 24 strains of causative organisms were isolated. The overall bacteriological eradication rate was 81.8%. Antimicrobial activities were excellent especially against Streptococcus pyogenes, Streptococcus pneumoniae, and Haemophilus influenzae.
4. As for the side effects, slight loose stools were observed in 2 cases, and in laboratory tests, elevations of GOT and GPT were observed in 1 case and an elevation of eosinophile was observed in 1 case. But no one needed any treatment.
5. CFTM-PI is a useful and safe oral antibiotic for the treatment of bacterial infections in pediatrics.

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The influence of cefteram pivoxil (CFTM-PI), a new oral cephalosporin, on the intestinal bacterial flora was studied in tetra-contaminated mice and in pediatric patients.
CFTM-PI in fine granular form was administered at a dose of 10mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of organisms: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. No remarkable change was observed in the fecal viable cell count except that slight decrease in E. coli count was observed on days 2 to 5 after starting administration.
The subjects in pediatric study were 5 children, 3 boys and 2 girls at ages from 6 months to 10 years 4 months, with infections. Their body weights ranged from 3.5 to 28.0kg.
CFTM-PI in fine granular form was administered at each dose of 3.0 to 3.8mg/kg, 3 times daily for 5 to 11 days. During the administration of CFTM-PI, there were some variations in the change of the fecal bacterial flora noticed between subjects. Although Enterobacteriaceae tended to decrease and Enterococci tended to increase, other main aerobes and anaerobes were almost unchanged in most cases. There was no case in which glucose non-fermenting Gram-negative rods and fungi became predominant. In a 10 years 4 months old boy, the fecal concen-tration of CFTM, the active form of CFTM-PI, was 72.20μg/g and a remarkable decrease of total anaerobe count was observed.
In feces, CFTM-PI and CFTM were detected in 4 and 2 cases respectively, and their concen-trations were 1.50-89.65μg/g and 2.25-72.20μg/g, respectively. β-Lactamase activities in feces were positive in all cases.
From the above, CFTM-PI is considered to be a drug with relatively less influence on the intestinal bacterial flora. But as high concentrations of drugs were detected in feces under some circumstances, we need to pay attention to fecal drug concentrations.

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Clinical evaluations of cefteram pivoxil (CFTM-PI, T-2588) were carried out. The obtained results are summarized as follows.
1. Clinical responses to CFTM-PI of 39 patients with pediatric infections were excellent in 16, good in 21, fair in 1 and poor in 1. The overall efficacy rate was 94.9%.
2. Bacteriologically, eradication rates for 39 isolates presumed to be pathogens were evaluated. The eradication rates obtained were 94.1% in 17 strains of Gram-positive cocci, 90.9% in 22 strains of Gram-negative rods.
3. Side effects observed were diarrhea in 2 patients, diarrhea and abdominal pain in 1, erythema and edema in 1. The incidence was 8.7%. An abnormal value found in clinical laboratory tests was eosinophilia in 1 patient.
The results suggested that CFTM-PI might be a very useful and safe drug for the treatment of pediatric infections.

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A new oral cephem antibiotic, cefteram pivoxil (CFTM-PI, T-2588), was studied for clinical efficacy in the field of pediatrics.
CFTM-PI was given orally to 23 patients with the following acute bacterial infections: 6 cases of acute tonsillitis, 8 of acute bronchitis, 2 of scarlet fever, 4 of bronchopneumonia, 1 of acute otitis media with sinusitis and 2 of urinary tract infections.
Clinical results were “excellent” in 8, “good” in 14, “poor” in 1: the efficacy rate was 95.7%. As an adverse reaction, diarrhea was observed in 1 patient.
From the above clinical results, it appears that CFTM-PI is a useful antibiotic for the treatment of pediatric patients with various bacterial infections.

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Bacteriological, pharmacokinetic and clinical studies were done on the effect of cefteram pivoxil (CFTM-PI, T-2588)(10% granules), a new oral cephalosporin, in the field of pediatrics. The results are summerlized below.
1. Antibacterial activities
Antibacterial activities of CFTM against Staphylococcus aureus and Streptococcus pyogenes were studied comparatively with activities of cefaclor (CCL), cephalexin (CEX) and ampicillin (ABPC). MICs of CFTM against S. aureus were distributed in a range between 0.78 and 12.5 μg/ml, with a peak value of 3.13 μg/ml, which were similar to MIC ranges of CEX and CCL. MICs of CFTM against all strains of S. pyogenes were ≤0.025 μg/ml, which were similar to MIC of ABPC. CFTM was approximately 2 to 3 folds more effective than CCL or CEX.
2. Absorption and excretion
Serum concentrations and urinary excretions of CFTM were determined in doses of 3mg/kg (non-fasting) and 6mg/kg (non-fasting and fasting). In non-fasting subjects, peak concentrations of CFTM in serum were dose-dependent and were 1.15-2.3 μg/ml and 1.8-3.6 μg/ml at 2-3 hours, 0.125-0.78 μg/ml and 0.245-0.97 μg/ml at 6 hours, respectively, for the 2 dose levels. Serum half-lives were 1.03-2.65 hours for the dose of 3mg/kg and 1.07-4.83 hours for 6mg/kg. In fasting subjects, the mean peak serum concentrations were 1.73 μg/ml at 2 hours and 1.13 μg/ml at 6 hours for the dose of 6 mg/kg.
Urinary recovery rates in the first 6 hours varied 5.3-19.2%.
3. Clinical study
Clinical efficacies were examined in a total of 41 cases including 9 cases of bacterial pneumonia, 10 cases of bronchitis, 11 cases of tonsillitis, 7 cases of urinary tract infections, 3 cases of scarlet fever and 1 case of otitis media. Clinical efficacies were excellent in 30 cases, good in 10 cases, poor in 1 case, hence the efficacy rate was 97.6%. All of the 28 bacteria identified in these cases were eradicated after CFTM-PI treatments. No noticeable abnormalities were found as side effects. An elevation of eosinophile, an increase of platelet count and elevations of GOT and GPT were observed in 3 patients.

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Cefteram pivoxil (CFTM-PI, T-2588), a new oral cephalosporin antibiotic, was evaluated for its safety and efficacy in children. Fifty-three patients with bacterial infections were treated with 8.3 to 21.8 mg/kg/day of CFTM-PI. The drug was very effective (efficacy rate 98.1%) in pharyngitis, otitis media, tracheobronchitis, pneumonia and skin infections. The antibacterial potency was very good against Haemophilus influenzae, Streptococcus pyogenes and Streptococcus pneumoniae, and was comparable with cephalexin against Staphylococcus aureus. No severe adverse reaction was encountered with the CFTM-PI therapy. The data suggest that CFTM-PI is a safe and effective antibiotic when used in children with susceptible bacterial infections.

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The usefulness of a new cephem antibiotic, cefteram pivoxil (CFTM-PI, T-2588), was evaluated in the field of pediatrics.
1. Thirty-one patients were enrolled in the study. They included 20 boys and 11 girls with ages 8 month to 8 years 7 month.
2. The patients were treated with CFTM-PI at a dose levels ranging 3.0-4.2mg/kg in 3 divided portions. The administration was done orally for a duration between 3 and 13 days, with a total dose between 27.3 and 130.0 mg/kg.
3. The patients were diagnostically classified into the following categories: 11 with acute pharyngitis, 1 with acute nasopharyngitis, 6 with acute tonsillitis, 9 with acute bronchitis, 2 with scarlet fever, 1 with purulent parotitis and 1 with purulent cervical lymphadenitis.
4. Clinical responses to the treatment were excellent in 14, good in 13, fair in 1 and poor in 3 patients with an overall efficacy rate of 87.1%.
5. Bacteriological responses were as follows: of 29 bacterial strains presumed to be pathogens, 23 were eradicated, 2 unchanged and 4 unknown, with an eradication rate of 92.0%.
6. Neither adverse reactions nor abnormal changes in laboratory test values were observed with the medication in any patients during and after the end of the treatment. None of the patients refused the medication.
CFTM-PI was found very effective and safe in treating pediatric infections: it is a useful drug in the field of pediatrics.

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Cefteram pivoxil (CFTM-PI) was administered to 37 patients with acute febrile upper or lower respiratory infections and 3 patients with urinary tract infections at 10mg/kg/day divided into 3 portions.
Good clinical effects were observed in all the cases.
As for the bacteriological effect, the evaluable 24 strains (60.0%) were eradicated among 43 strains identified in 37 cases with the treatment with CFTM-PI. Only 2 strains were eradicated among 9 strains of Staphylococcus aureus. Among 3 patients with urinary tract infections with Escherichia coli, 2 strains were eradicated from urine after the administration of CFTM-PI.
Four cases showed mild diarrhea among 40 cases. It was not clear whether the diarrhea was due to the administration of CFTM-PI.

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Cefteram pivoxil (CFTM-PI, T-2588) was administered to pediatric patients with acute infectious diseases, and a summary of the results obtained are as follows.
1. Pharmacokinetic parameters determined in 1 patient appears to be comparable to those of adults.
2. Clinical efficacy was studied on 16 children with acute urinary tract infections, acute upper respiratory infections, acute sinusitis, acute otitis media and acute cervical lymphadenitis. Responses to the treatment were excellent in 7 (43.8%) and good in 9 (56.3%).
3. No adverse reactions were noted in this study.

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Laboratory and clinical studies on cefteram pivoxil (cefteram) a new cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows:
1. Serum concentrations, urinary concentrations and urinary recovery rates of cefteram (CFTM) were determined upon oral administration after meal of cefteram pivoxil (CFTM-PI) at doses of 3mg/kg granules in 2 cases and 6mg/kg granules in 2. Peak serum levels of CFTM were obtained at 3 hours in 2 cases and 4 hours in 2 cases after administration of the drug with a range of 0.74-2.2μg/ml with half-lives of 0.77-3.62 hours. Urinary recovery rates in 8 hours after administration ranged from 9.6-23.0%.
2. MICs of CFTM against 22 clinical isolates (Streptococcus pyogenes 4 strains, Streptococcus pneumoniae 4, Staphylococcus aureus 2, Branhamella catarrhalis 1, Haemophilus influenzae 8, Haemophilus parainfluenzae 1, and Escherichia coli 2) were compared with those of cefaclor (CCL), cephalexin (CEX), and ampicillin (ABPC). The antibacterial activity of CFTM was superior to those of CCL and CEX, and was superior against Gram-negative rods and equal against Gram-positive cocci to those of ABPC.
3. Twenty-six pediatric patients with acute infectious diseases (scarlet fever 3 cases, tonsillitis 7, epiglottitis 1, bronchitis 5, pneumonia 5, urinary tract infection 3, cervical lymphadenitis 2) were treated with CFTM-PI at daily doses of 9.3-15.3mg/kg t. i. d. as a rule. The efficacy rates were 100% clinically and 70% bacteriologically.
4. Side effects or abnormal laboratory test values were not observed except for an increased platelet count in 1 case.

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