The influence of MUELLER-HINTON (MH) broth (from BBL Microbiology Systems, and Difco Laboratories) of minimum inhibitory concentrations (MIC) of cefuzonam (CZON), flomoxef (FMOX), imipenem (IPM), and minocycline (MINO) for 100 strains of Staphylococcus aureus was investigated. Antibacterial activity of MINO was stronger than any other antibiotics.MICs of CZON for 16 strains (14 of 50 methicillin-resistant S. aureus (MRSA), 2 of 50 methicillinsensitive S. aureus) were >4-fold greater when tested in BBL MH broth than when tested in Difco MH broth, thus, different media altered categories of some strains (8 of 50 MRSA) from susceptible to resistant. MICs of FMOX in the BBL MH broth for 12 of 50 MRSA strains rose gt;4-fold compared to the Difco MH broth. On the other hand, MICs of IPM and MINO were affected very little by the different brand of MH broth used.

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Clinical evaluation of ceftibuten (CETB, 7432-S) was performed in 20 patients with acute bronchitis.
They were consisted of 10 males and 10 females aged from 20 to 80 years old.
CETB was given orally in daily dose of 300mg (18 cases) or 600mg (2 cases) in three divided portions.
The duration of administration was 3 to 14 days. Especially they were given for 7 days in 16 cases.
A total of 11 strains comprising 4 strains of Staphylococcus aureus, 2 strains of β-Streptococcus and 1 strain each of Streptococcus pneumoniae, Branhamella catarrhalis, Klebsiella oxytoca, Serratia marcescens, Acinetobacter lwofii were identified from sputa before administration. All of the above bacteria were eradicated but, in 1 case, a strain of Streptococcus pyogenes appered after the treatment (eradication ratio =100%).
The clinical efficacy rate was 100%: Responses were excellent in 3 cases and good in 17 cases
There was no side effect and no abnormal changes in laboratory test results.
From the avobe results, it is concluded that CETB is effective, safe and useful new oral cephem on acute bronchitis.

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We evaluated the therapeutic efficacy of ceftibuten (CETB, 7432-S), a new cephem antibiotic for oral use, in chronic respiratory tract infections. A daily dose of 400 mg (b.i.d.: 15 cases) or 600 mg (t.i.d.: 5 cases) of CETB was given orally for 3-14 days (mean: 10.6 days) to 20 patients: 9 with infected bronchiectasis, 3 with infection supervened on pulmonary emphysema, 3 with acute pneumonia (supervened on bronchiectasis in 2 of 3 cases), 2 with infected bronchial asthma, 1 each with infection supervened on old pulmonary tuberculosis, chronic bronchitis and pulmonary fibrosis. The clinical effects were excellent in 3, good in 11, fair in 3 and poor in 3. Eighteen strains were identified as causative organisms. Eight of 15 strains for which bacteriological responses were evaluable were eradicated by the use of CETB. Eosinophilia in 2 patients and an elevation of S-GPT value was observed in 1 patient. These adverse reactions disappeared after the completion of the therapy. From the abov results, we conclude that CETB is one of the most useful antibiotics for oral use as a first choice in chronic respiratory tract infections.

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Twenty-four patients with complicated urinary tract infections (UTI) were received ceftibuten (CETB) 400 mg b.i.d. orally for 5 days, and the following results were obtained. One of the recipients was excluded for negative bacteriuria before treatment.
According to the criteria for evaluation of clinical efficacy of antimicrobial agents on UTI, 23 patients were assessed: 9 of them were judged to show excellent responses, 6 to have moderate responses and 8 poor responses. The overall efficacy was 65%. Four patients with indwelling catheter failed to show positive clinical response, but 15 out of 19 patients without indwelling catheter responded positively.
As to bacteriological responses, organisms included Gram-positive cocci were eradicated in 28, replaced in 9 and persisted in 6 strains. Of 24 Gram-negative rods except 1 strain ofPseudomonas sp., 23 (96%) were eradicated.
Safety evaluation was made in all 24 patients received CETB. No adverse reactions were observed in any cases. As to laboratory test results, slight, transient elevations of GOT, GPT and Al-P of serum were noted in 1 patient. Their values, however, returned to normal levels in 4 weeks.

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Oral new quinolone, norfloxacin (NFLX, AM-715), was evaluated for its safety, efficacy and pharmacokinetics in children.
1. NFLX was effective in 88.0% of 25 cases infected with Haemophilus influenzae, Pseudomonas aeruginosa, Escherichia coli, Campylobacter jejuni, Staphylococcus aureus including methicillin-resistant strains, and other bacteria.
2. After single oral administration of 50 mg and 100 mg NFLX tablet at fasting, mean peak values of serum concentration were 0.35, 0.48-Eg/ml and T 1/2 values were 2.2, 2.7 hours, respectively.
3. No adverse reactions suggestive for arthropathy were encountered with NFLX therapy with daily doses of 4.6-35.7 mg/kg (maximum 600 mg Per day) and duration of 3 to 19 days.
From these preliminary data, NFLX seems to have a place in the treatment of pediatric infectious diseases.

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We have evaluated norfloxacin (NFLX), a fluoroquinolone agent, in tablet form for its efficacy and safety in the field of pediatrics.
1. Mean serum concentrations of NFLX following oral administration to 3 children at dose levels of 3.2 mg/kg, 3.7 mg/kg and 5.4 mg/kg were, respectively, 0.7 μg/ml, 0.18 μg/ml and 0.64 μg/ml at 2-4 hours.
Mean serum half-lives (T 1/2) of NFLX were 2.5-2.9 hours and mean urinary recovery rates in the first 6 hours after administrations were 7.1-30.7%, depending on dose levels.
2. Antibacterial activities of NFLX against clinically isolated 30 organisms from children were determined.
MIC of NFLX against Staphylococcus aureus was similar to that of ABPC, 0.39-25 μg/ml.
MIC of NFLX against Escherichia coli was approximately <0.10 μg/ml. This MIC value was lower than other antibiotics.
MIC of NFLX against Vibrio parahaemolyticus was <0.10 μg/ml.
3. NFLX was administered to 30 patients (7 patients with Salmonella enteritis, 7 patients with Campylobacter enteritis, 5 patients with other enteritis, 1 patient with bacillary dysentery, 8 patients with urinary tract infection, 2 patients with skin soft tissue infection).
The clinical responses of these 30 patients were as follows; excellet: 24 patients, good: 4 patients. The efficacy rate was 93.3%.
4. The bacteriological efficacy rate of NFLX against clinically isolated 29 organisms from children was 75.9%, including 3 cases in which other antimicrobial agents had been ineffective.
Especially against Salmonella spp. was superior to other agents tested.
5. Neither clinical adverse reaction nor abnormal laboratory data was found in any of these 33 patients.
NFLX was considered to be a useful and safe antimicrobial agent in pediatric patients with an excellent bactericidal capacity.

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In bacteriological, pharmacokinetic and clinical studies on norfloxacin (NFLX, AM-715), the following results were obtained:
1. Antibacterial activity of NFLX, nalidixic acid (NA), amoxicillin (AMPC), cefaclor (CCL), erythromycin (EM) and fosfomycin (FOM) against clinically isolated bacteria was examined, and it was found that MIC₈₀ of NFLX against Staphylococcus aureus was 3.13 μg/ml, thus NFLX exhibited stronger antimicrobial activity than NA, AMPC, CCL, EM and FOM. NFLX also showed good activities to those strains of S. aureus which were resistance to NA, AMPC, CCL, EM and FOM.
2. MIC₈₀ of NFLX against Escherichia coli was 0.05 μg/ml or lower, thus NFLX showed better activity than NA, AMPC, CCL, EM and FOM.
3. In single oral administration at fasting of NFLX at dose levels of 1.5-2.4 and 2.5-3.4 mg/kg in tablet form mean peak values of serum concentration were 0.32 μg/ml reached in 1 hour and 0.38 μg/ml in 2 hours, T1/2's obtained were 1.7-4.0 and 2.2-2.9 hours and AUC's were 1.54±0.52 and 2.02±0.93 μg·hr/ml, respectively. Urinary recovery rates of 11.6-46.9%, 13.8-35.4% in 6-8 hours were demonstrated with the 2 ranges of dose levels, respectivery.
4. NFLX was administrated to 34 patients consisting of 8 cases of acute pneumonia, 3 cases of acute tonsillitis, 3 cases of bacterial colitis, 19 cases of urinary tract infections and 1 case of purulent parotitis.
The clinical efficacy rate was 97.1% including 34 cases with excellent results in 28, good in 5 and fair in 1.
5. The bacterial eradication rate was 96.8% (30/31) with one exception of a Campylobacter jejuni strain.
6. NFLX was given to patients according to a dosing regimen with 4.5-21.4 mg/kg/day dose levels for 3 doses daily except 1 case of UTI where 2 daily doses were given daily.
7. No adverse reactions were observed.
Abnormal laboratory test value was obtained in 1 case where eosinophilia was found.
The above results have suggested that NFLX is a useful and safe antimicrobial agent against bacterial infections in children.

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Norfloxacin (NFLX, AM-715) is a new quinolone antibacterial agent. In the present study, we carried out laboratory and clinical investigations on NFLX in the field of pediatrics. The obtained results are summarized as follows.
1. NFLX was very active against Escherichia coli, Salmonella sp., Klebsiella sp., Enterobactersp. and Pseudomonas aeruginosa among Gram-negative rods.
Antibacterial activities of NFLX against Gram-positive cocci were lower than those against Gram-negative rods but superior to activities of usual quinolone agents.
MIC values of NFLX against Campylobacter jejuni were distributed in a range of <0.05-0.78μg/ml.
2. A peak serum level of 0.49 μg/ml was observed in 2 subjects and its urinary recoveries were 13.7%, 21.5%, respectively.
3. Clinical efficacies to NFLX were excellent in 25 patients and good in 9 patients with a efficacy rate of 92%.
In a bacteriological examination, causative organisms were eradicated with an eradication rate of 87%.
4. No side effects were observed except eosinophillia in 1 patient.
These findings indicate that NFLX will be useful and safe drug against bacterial infections in pediatrics.

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Pediatric infections were treated with norfloxacin (NFLX), a pyridonecarboxylic acid antibiotic developed by Kyorin Co., Ltd., to investigate its clinical efficacy.
1. Thirteen patients were treated with NFLX. These patients included of 5 with Campylobacter enteritis, 4 with Salmonella enteritis, 3 with dysentery and 1 with acute enteritis.
2. Of 14 pathogens identified, complete eradications were observed with 13 strains and partial eradication was seen in 1 case. Thus, overall eradication rate was 92.9%.
3. These were no symptoms nor abnormal laboratory findings which indicated an occurence of side effect due to the NFLX treatment.

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Bacteriological and clinical studies on norfloxacin (NFLX) were carried out in the field of pediatrics, and the results obtained are summarized as follows:
1. The MICs of NFLX against clinically isolated organisms were determined to compare with MICs of nalidixic acid, amoxicillin, cefaclor, erythromycin and fosfomycin. NFLX had low MICs against both Gram-positive and Gram-negative bacteria and, particularly, showed higher antimicrobial activity to Escherichia coli, Salmonella sp., Klebsiella pneumoniae, Pseudomonas aeruginosa, Haemophilus influenzae and Campylobacter jejuni than any other drugs tested.
2. Seventeen pediatric patients (11 cases of enteritis, 4 cases of urinary tract infections, 1 case of tonsillitis and 1 case of pyoderma) were treated orally with NFLX in daily doses ranging from 3.1 to 16.7 mg/kg t.i.d. for 6-14 days. Rates of clinical effectiveness and bacterial elimination were 94.1% and 58.8%, respectively.
3. None of the treated children showed clinical symptoms indicating the occurrence of side effects nor abnormal laboratory findings except 1 patient with eosinophilia.
These results indicate the usefulness of NFLX in the treatment of bacterial infections in the pediatric field.

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We administered norfloxacin (NFLX) to 16 children aged 3 to 14 year-old at the dose of 5.2 to 17.2 mg/kg/day. We evaluated the efficacy and safety of NFLX in 6 children with respiratory tract infections, 8 urinary tract infections, and 2 gastrointestinal tract infections. Efficacy rate of NFLX was 93.8% and eradicated rate was 92.9%. Any adverse effects were not observed. These results suggested that NFLX could be used safely to the children

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We have carried out laboratory and clinical studies on norfloxacin (NFLX, AM-715).
The results are summarized as follows.
NFLX was given through oral administration to one child each at dose levels of 1.7 mg/kg, 2.4 mg/kg and 3.2 mg/kg. After administration, peak serum levels of NFLX obtained for the 3 dose levels were 0.16 μg/ml at 1 hour, 0.69 μg/ml at 2 hours, 0.81 μg/ml at 1 hour, respectively, and half-lives were 2.5 hours, 1.8 hours and 2.7 hours, respectively.
NFLX was given through oral administration to 2 children at a dose level of 4.4 mg/kg and to another child at a dose level of 4.8 mg/kg. After administration, mean peak serum levels of NFLX obtained were 1.17 ±0.48 μg/ml and half-lives were 3.0 ±0.5 hours.
Urinary excretion rates of NFLX were 14.5% and 28.4% in the first 8 hours after administration of 1.7 mg/kg and 3.2 mg/kg, respectively, and 29.1% in the first 6 hours after administration of 2.4 mg/kg.
Mean urinary excretion rates of NFLX were 38.5 ±13.0% in the first 8 hours after administration of 4.4 mg/kg and 4.8 mg/kg.
Treatment with NFLX was made in 33 cases of pediatric bacterial infections including 5 cases of tonsillitis, 14 cases of enteritis, 10 cases of UTI and 1 case each of bronchitis, balanoposthitis, impetigo and pustulosis. Results obtained were excellent in 14 cases, good in 15cases.
No significant side effect due to the drug was observed in any cases.

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We studied clinical effects of norfloxacin (NFLX, AM-715) tablets. The results we found are summerized as follows:
1. Ten patients with 5 diseases were medicated with 7.0-14.8 mg/kg of the drug 3 times daily for 6-8 days.
They consisted of one-each with tonsilitis, pharyngitis, bronchitis, 4 with Campylobacter enteritis, 3 with other enteritis. Clinical responses to the treatment were excellent in 8, good in 1 and fair in 1, with an efficacy rate of 90%. Bacteriologically, of 9 isolates for which changes in populations were followed, 6 were eradicated and 3 remained unchanged, with an eradication rate of 66.7%.
2. No.adverse reactions nor abnormal laboratory test values attributable to the drug were observed.
3. These results suggest that this new quinolone drug may be useful, against bacterial infections in children 6 years and older.

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We have investigated bioavailability, clinical efficacy, side effect and antimicrobial activity of norfloxacin (NFLX) to evaluate the efficacy and safety in the pediatric field.
Results are summarized as follows
1. After oral administration of 100 mg, T_max was 2 hours and T 1/2 were 4.2 and 2.6 hours in 2 cases.
2. In 10 cases of urinary tract infection (UTI) and 4 cases of intestinal tract infection (ITI), clinical efficacy rate was 100% (14/14).
3. In UTI, causative bacteria were all eradicated. In ITI, 1 case with Campylobacter jejuni remained unchanged. Overall eradication rate was 92.9% (13/14).
4. Antimicrobial activities to clinically isolated organisms such as Gram-negative rods or Staphylococcus aureus, MIC of NFLX was cleary surperior to those of cefaclor, amoxicillin, nalidixic acid, fosfomycin and erythromycin.
5. Side effect of dipsia was observed in 1 case and eosinophillia was found in 1 case.But these reactions were mild and we wewe able to continue the administration of the drug.
The above results suggest that NFLX is a useful and safe drug for the therapy of UTI and ITI in the pediatric field.

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We have evaluated norfloxacin (NFLX) tablets for therapeutic effectiveness and safety in children. The results are summarized as follows.
1. A clinical study was performed on 14 children with infections, including 12 with urinary tract infections and 2 with acute bronchitis. Doses ranging from 1.7 to 5.4 mg/kg body weight were given b. i. d. or t. i. d. Lengths of treatment ranged from 3 to 15 days. The therapeutic responses were considered “excellent” in 8 and “good” in 5, with an efficacy rate of 93%.
2. Side effects were observed in 2 cases, one with light-headed feeling and one with vomiting. In clinical laboratory tests, eosinophilia was found in 2 cases and GOT was slightly elevated in 1 case. It has been concluded that NFLX is a usable drug for the treatment of bacterial infections in children.

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Norfloxacim (NFLX, AM-715), a new synthetic antibacterial agent, was administered to 18 child patients with infectious diseases. The patients included 5 boys and 13 girls from 3 to 14 years of ages. They were given orally dosage ranging 5.2-17.9 mg/kg/day for 4 to 14 days.
Clinical efficacies were excellent in 1 case, good in 16 cases, unknown in 1 case, hence the total efficacy rate was determined to be 100%.
There were no cases which showed side effects of the drug and no abnormal laboratory test values were observed during the treatment.

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We have evaluated the effectiveness and safety of norfloxacin (NFLX) in 18 children with infectious diseases.
Doses ranging from 5.6 to 18.8 mg/kg/day for t. i. d. or q. i. d. were used.
The causative bacteria were Campylobacter jejuni in 3 cases, Salmonella typhimurium in 1, Staphylococcus aureus in 2, Haemophilus infiuenzae in 1 and unknown in 11 cases.
Except 1 strain of S. aureus, all the bacteria mentioned above were eradicated.
Clinical effects were excellent in 8, good in 8, poor in 2, and the total efficacy rate was88.9%.
No side effects nor abnormal laboratory test results were observed.
These results have shown that the NFLX is a usefull drug for infectious diseases in the pediatric field.

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Norfloxacin (NFLX) tablets with a potency of 50 mg/tablet or 100 mg/tablet were administered at doses of 1 to 4 tablets (1.5 to 6.1 mg/kg) orally 30 minutes before meals to 12 children with ages ranging from 8 years 9 months to 12 years 5 months, and serum/urinary NFLX levels and urinary recovery rates were determined. The drug sensitivity tests for NFLX and 10 other drugs were conducted against 128 strains of Shigella sonnei (106 CFU/ml) which had been isolated from pediatric patients with bacillary dysentery. In order to evaluate clinical and bacteriological effects of NFLX and its safety in the pediatric field, NFLX 50 mg tablets were administered t. i. d.(mean 8.3 mg/kg) for 5 days to 42 pediatric patients with bacillary dysentery. Similarly, this drug was administered in b.i.d. or t.i.d.(mean 6.7 mg/kg) for 4 days to 4 pediatric patients with urinary tract infections.
The following results were obtained:
1. According to the dosage, the subjects were devided into 3 groups with dose levels 1.5-2.8 mg/kg, 3.1-4.7 mg/kg and 5.2-6.1 mg/kg. These groups had 5, 2 and 5 subjects, respectively.Mean serum drug concentrations for the 3 dosage groups were at peak levels of 0.27, 0.64 and 1.51 μg/ml at 4, 2 and 1 hour (s) after administration, respectively. Pharmacokinetic parameters for these dosage groups were as follows: T_max values were 3.0, 3.0 and 1.2 hours; C_max values were 0.32, 0.78 and 1.56 μg/ml; serum half-lives were 2.2, 2, 4 and 2.3 hours; and AUCs were 1.65, 3.98 and 6.06 μg·hr/ml, respectively. Thus, dose-dependent responses were observed among the 3 dosage groups.
2. Mean peak urinary drug concentrations for the 3 dosage groups were 45.8,109.2 and 215.1 μg/ml, respectively, and the peaks appeared 2-4 hours after administration. Mean recovery rates up to 8 hours after administration were 18.3%, 24.5% and 28.7%, respectively for the 3 dosages.
3. In a drug sensitivity test against 128 strains of S. sonnei, the most frequent MIC value of NFLX was 0.78 μg/ml against 65 strains, followed by 0.39 μg/ml for 56 strains. Together, these strains accounted for 94.5% of the strains tested. No registant strain to this drug was observed and the antibacterial activity of this drug was second only to colistin, similar to that of ofloxacin, better than those of enoxacin and seven other drugs.
4. Clinical efficacy rate of NFLX against bacillary dysentery was 95.2% in 21 cases in which the evaluation was possible. Clinical effect for urinary tract infections was evaluable in 3 cases and the drug was effective in all those cases (1 case droped out).
5. The bacteriological effect was evaluated in 42 patients with bacillary dysentery. Eradication was achieved in 40 cases and persistence of pathogenes was observed in 2 cases. Thus, the eradication rate was 95.2%. The pathogens reappeared, however in 7 (17.5%) of 40 cases that had once become negative. In 3 cases of urinary tract infections in which the evaluation was possible, pathogens (Escherichia coli) were eradicated.
6. In all 46 cases, no side effect nor abnormal clinical laboratory test values were observed.

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