[in Japanese]

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Cefdinir (CFDN, FK482) was evaluated in children with infections. CFDN was glven at a daily dose of 6.4-19.8mg/kg in 2 or 3 divided portions. CFDN was effective in 94% of32 cases with respiratory tract, middle ear, urinary tract or skin structure infections. Side effects were loose stool and diarrhea (12.5%). In a phamacokinetic study, 6. 0mg/kg of CFDN was given to each of the subjects before meal. C_max was 0.81±0.38μg/ml, T1/2 was 2.31±0.77 hours. Antibacterial activity against Staphylococcus aureus was the most excellent of oral cephem antibiotics tested.
The data suggest that CFDN 10% granular preparation is safe and effective when used in children with infections caused by susceptible bacteria.

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Ten% cefdinir (CFDN, FK482) granular preparation, a new oral cephalosporin preparation intended for children, was given to children with various infections. The results obtained are summarized as follows.
1. Ten% CFDN granules were administered to a total of 21 children with upper or lower respiratory tract infections, urinary tract infections or infectious impetigo at daily doses of 6.4-18mg/kg divided into 3 portions.
Clinical efficacies were “excellent” in 13 patients, “good” in 7 patients and “unknown” in 1 patient (viral infection), hence an efficacy of 100% was obtained.
2. Bacteria identified in various disease cases included 19 strains of 7 species, and the eradication rate was 100%.
3. No side effects were noted in any of the children. Laboratory test results showed an abnormality in 1 case with eosinophilia.
These results suggest that 10% CFDN granules as well as 5% CFDN granules may be a very useful and safe drug for the treatment of pediatric infections.

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Clinical evaluationso f cefdinir (CFDN) 10% granule were carriedo ut. The obtained results are summarized as fbllows.
1. Clinical responses to CFDN of 23 patients with pediatric infections were excellent in 11 and good in 8. The overall efficacy rate was 82.6%.
2. Bacteriologically, the eradication rate for 23 strains of bacteria identified to be pathogens was evaluated and was 82.6%.
3. Side effects observed were diarrhea in 2 of 25 patients. The incidence was 8.0%. Abnormal laboratory test results observed included 2 cases with elevation of GOT and 1 case with elevation of GPT.
These results suggest that CFDN 10% granule, as well as 5% granule, may be a very useful and safe drug for the treatment of pediatric infections.

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Cefdinir (CFDN) was administered to pediatric patients with acute infectious diseases. A summary of the results obtained is as follows.
1. Pharmacokinetic parameters were determined in a girl. In comparison to reported data in adults, T_maxshorter, C_max was slightly lower, and the plasma half life of CFDN was somewhat longer.
2. Clinical efficacy was studied in 11 children with acute tonsillitis (6 patients), scarlet fever (1 patient), acute pharyngitis (1 patient), acute pneumonia (1 patient), acute otitis media (1 patient) and acute cervical lymphadenitis (1 patient). Responses to the treatment were excellent in 7 (63.6%) and good in 2 (18.2%).
3. No adverse reactions were noted in this study.

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Five percent fine granule preparation of cefdinir (CFDN, FK482) was administered to 30 patients with acute febrile respiratory tract infections (RTI) at 4.9-21.1mg/kg/day divided into 3 portions. And 10% fine granule preparation of CFDN was also administered to 11 patients with acute febrile RTI and 1 patient with urinary tract infection at 10.0-20.0mg/kg/day divided into 3 portions.
Good clinical effects observed in 21 of 24 patients (87.5%) with actue pharyngitis, 12 of 13 patients (92.3%) with acute tonsillitis, 2 of 4 patients (50.0%) with pneumonia and a patient with urinary tract infection.
From these patients, 34 causative organisms were isolated. Ten (83.3%) of 12 strains of Staphylococcus aureus, all 6 strains of Streptococcus pyogenes and 1 strain of Streptococcus pneumoniae, 6 (46.2%) of 13 strains of Haemophillus influenzae and 1 strain of Escherichia coli were eradicated from these patients.
Among the patients with pneumonia, CFDN 20mg/kg/day dose group showed better clinical responses and better bacteriological effects against H. influenzae among the patients given CFDN 20 mg/kg/day dose group than those given CFDN 5 mg/kg/day dose group.
Side effects were noted in 2 cases, one case had soft stools and the other had diarrheas.

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Clinical evaluational in pediatrics on cefdinir (CFDN, FK482)(5% fine granules), a new oral cephem, was performed.
1.CFDN was administered to 112 pediatric patients with ages between l month to l3 years with various infections. Dose levels used were 3.0-8.9 mg/kg (mean 5.1mg/kg) t.i.d. for 3-14 days (mean 6.7 days). The studied patients included 2 patients with scarlet fever, 6 with acute pharyngitis, 6 with acute rhinopharyngitis, 52 with acute purulent tonsillitis, 8 with acute bronchitis, 24 with acute pneumonia, 7 with acute urinary tract infections, 1 with acute vaginitis, and 6 with impetigo. Total doses ranged from 0.6 to 4.05 g. One hundred eleven of the 112 patients were evaluated fbr clinical efncacy and all the patients were evaluated for safety.
2.Clinical effects were excellent in 51 cases, good in 57, and fair in 3 with an extremely high emcacy rate of 97.3%. Efncacy rates were 100% in scarlet fever, acute pharyngitis, acute purulent tonsillitis, acute bronchitis, acute vaginitis and impetigo, and 83.3%, 95.7%, 85.7% in acute rhinopharyngitis, acute pneumonia, and acute urinary tract infections, respectively. Good clinical effects were observed regardless of diseases.
3. Causative organisms were identified in 79 cases, of which 71 were fbund to be monobacterial infections and 8 were found to be multi-bacterial infections. In mono-bacterial infections, clinical emcacies were 100% fbr those caused by Staphylococcus aureus/Streptococcus pyogenes/ Streptococcus pneumoniae/β-Streptococcus except those in A and B groups with an overall efncacy of 100% against Gram-positive cocci (GPC) and they were 89.5%, 100%, 100% for those caused by Haemophilus influenzae, Hoemophilus parainfluenzae, and Escherichia coli, respectively, with an overall emcacy of 90.3% in Gram-negative rods (GNR). In multi-bacterial infections also, a clinical emcacy of 100% was obtained.
4. Bacteriological effects were studied for 89 strains in the 79 cases. The eradication rate for a few strains of S.pneumoniae was low, 25%, but it was 100% for S.aureus, with the same results for S.Pyogenes, and β-Streptococcus. The eradication rate on GPC was high 94.1%.
Among GNR, 66.7% of E.coli, 50.0% of H. influenzae, and 71.4% of H. parainfluenzae was eradicated. The overall eradication rate for GNR was 55.3%, lower than that for GPC. Microbial substitutions were observed in 13 cases, with Haemophilus sp. replacing other bacteria.
5. Diarrhea and soft stools were noted in 4 and 2 patients, respectively. The severity of these side effects, however, was slight and it was possible to continue the CFDN treatment. Feces with brick red color were uniquely observed in 1 diarrheal patient. In laboratory test results, eosinophilia was noted only in l patient. There were no other abnormal results in laboratory tests. None of the patients refused or complained of difficulty in intaking the drug via oral route, and the compliance of CFDN was equal to other oral cephem preparations for pediatrics.
In conclusion, CFDN 5% fine granule preparation was considered to be effective and safe in the treatment of pediatric infections.

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Pharmacokinetic, bacteriological, and clinical studiesoncefdinir (CFDN, FK482)(10% fine granules), a new oral cephem, were performed in pediatrics.
1.Bioequivalencies of plasma concentrations and urinary excretions of CFDN 5% and10% fine granules were investigated on 3 pediatric patients with ages between 5 to 13 years administered with a drug in fasting state at a dose level of 3mg/kg using a cross over method.Average plasma concentrations in a group of patients administered with 5% fine granules peaked at 3 hours after administration with a level of 1.05±0.29μg/ml (mean±S.E) and decreased to 0.12±0.05μg/mlat 8 hours with a half-life of 1.48±0.09 hours.In the group administered with 10%fine granules, average plasma concentrations peaked at 2 hours after administration with a level of 1.32±0.12μg/ml, and decreased to 0.20±0.11μg/ml at 8 hours with a half-life of 1.68±0.28 hours. The first 8-hour urinary recovery rates of CFDN in the 5% and 10% fine granules groups averaged 19.64± 5.69% and 23.37±2.36%, respectively.
Both average and individual plasma concentrations and urinary recovery rates in the patients of the 10% fine granules group were somewhat higher than those of the 5% fine granules group, but no significant differences were observed between the 2 groups including areas under concentrations.
2. CFDN 10% fine granule preparation was administered to 33 pediatric patients with ages between 1 to 13 years with various infections, and its clinical effects, bacteriological effects and safety were assessed.
In 31 of the 33 patients (2 patients were excluded since they were with non-bactedal infections) clinical effects were excellent in all of 9 patients with scarlet fever (3), acute pharyngitis (3) or impetigo (3), excellent in 12 and good in 3 of 15 patients with acute purulent tonsillitis, and excellent in 4 and good in 3 of 7 patients with acute pneumonia. The overall efficacy rate was 100%.
Bactedological effects against causative organisms were evaluated. All the identified Staphylococcus aureus (4 strains) and Streptococcus agalactiae (1) were eradicated. Of 10 strains of Strettococcus pyogenes, 9 strains were eradicated and the other one was reduced. Of 7 strains of Haemophilus influenzae 4 were eradicated, 1 persisted and the fate of the remaining 2 were unknown. The overall eradication ratewas 90.0%. Microbial substitutions were observed in 5 patients. The new, replacing bacteria were all Haemothilus spp. Diarrhea was noted in 4 patients, but no other side effects nor abnormal laboratory tests results were observed.
One patient complained of difnculty in intaking the oral drug. No other compliance problems were noted with this drug.
In conclusion, CFDN 10% fine granule preparation was considered to be effective and safe in the treatment of pediatric infections, the outcome was similar to that with 5% fine granules.

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Clinical studies on 10% fine granules of cefdinir (CFDN), a new cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows.
1. Half-lives of CFDN in plasma in 3 children when administered on an empty stomach were 1.77 hours (3mg/kg per os) and1.47hours (6mg/kg per os), respectively. Eight hour urinary excretion rates of CFDN were 21.5% (3 mg/kg per os) and 16.4% (6 mg/kg per os), respectively.
2. CFDN was administered to 11 children with various bacterial infections: 1 patient with scarlet fever, 1 with pharyngotonsillitis, 3 with acute bronchitis, 3 with pneumonia and 3 with urinary tract infections. The overall clincal efficacy rate was 90.9%.
3. Loose stool was noted in 1 patient. No abnormal laboratory test values were encountered.

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We have carried out laboratory and clinical studies on cefdinir (CFDN) 5% and 10% fine granule preparations. The results are summarized as follows.
CFDN 5% fine granule preparation was given via oral route to each of 2 children in the fasting state at a single dose of 3 mg/kg. After administration, the mean peak plasma level of CFDN was 0.76μg/ml at 4 hours and the mean half-life was 1.77 hours. The mean urinary excretion rate of CFDN was 31.5% in the first 12 hours after oral administration. CFDN 10% fine granule preparation and CFDN 100 mg capsule were given via oral route 3 chidren and to another child in the fasting state at single doses of 3 mg/kg and 2.63 mg/kg, respectively. After administration of 10% granules the mean peak plasma level of CFDN was 0.73μg/ml at 2 hours and the mean half-life was 1.62 hours. The peak serum level obtained after administration of CFDN 100mg capsule was 0.91μg/ml at 2 hours and the half-life was 1.08 hours. The mean urinary excretion rate obtained with CFDN 10% fine granules was 26.2% in the first 8 hours after oral administration and the urinary excretion rate obtained with CFDN 100 mg capsule was 19.7% in the first 12 hours after oral administration.
Treatment with CFDN 5% fine granules was made for a total of 48 cases of pediatric bacterial infections including 21 cases of tonsillitis, 12 cases of scarlet fever, 3 cases of pharyngitis, 5 cases of impetigo, 1 case of subcutaneous abscess, 1 case of furuncle, 5 cases of UTI. Results obtained were excellent in 30 cases, good in 18 cases. Treatment with CFDN 10% fine granules was made for a total of 16 cases of pediatric bacterial infections including 6 cases of tonsillitis, 3 cases of pneumonia, 4 cases of scarlet fever, 2 cases of impetigo, 1 case of UTI. Results obtained were excellent in 8 cases, good in 7 cases, poor in 1 case.
No significant side effects due to the drugs were observed except 2 cases (1 case with 5% preparation and another with 10%) with eosinophilia, 3 cases (all with 5%) with diarrhea and 1 case each of elevated GOT & GPT (with 5%) and elevated GOT, GPT & Al-P (with 10%).

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The Pharmacokinetics and clinical effectiveness of cefdinir (CFDN, FK 482) were examined in pediatric patients. The results are summarized as follows.
1. Plasma concentrations and urinary excretions of CFDN after administration of 5%fine granules were investigated on 4 children at a dose level of 6 mg/kg. Average plasma concentrations peaked at 4 hours after administration at 0.99μg/ml with a half-life of 2.12 hours. The first 24-hour urinary recovery rates of CFDN in 3 children averaged 22.0%.
2. CFDN was given to 24 children (11 with pharyngitis, 3 with tonsillitis, 8 with scarlet fever, 1 with urinary tract infection and 1 with enteritis due to Salmonella); 15 were treated with 5% fine granules and 9 with 10% fine granules at daily doses of about 10 mg/kg in 2 to 3 divided portions. Clinical effects were excellent in 16, good in 7 and not evaluable in 1, with an overall efficacy rate of 100%.
3. Identified causative organisms were 12 strains of Streptococcus pyogenes, 4 of Haemophilus influenzae, 5 of Haemophilus parainfluenzae, 1 of Escherichia coli, and 1 of Salmonella. Bacteriological effects were rated as “eradicated” for 19 strains, “unchanged” for 4 with an eradication rate of 82.6%.
4. No side effects were observed. As for abnormal laboratory test results, a transient decrease of white blood cells was observed in 1 patient.
5. The CFDN fine granule preparations were preferably accepted by the children.
6. The fine granular preparations of CFDN, a new oral antibiotic, were useful for the treatment of bacterial infections in pediatrics.

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We studied pharmacokinetics and clinical effects of 5% and 10% fiine granules of cefdinir (FK 482, CFDN), a new oral cephalosporin, in the pediatric field and the following results were obtained.
1.Phamacokinetics (blood concentration and urinary excretion)
Pharmacokinetics of CFDN in 163 children was investigated. Cmax and T 1/2 were 0.92±0.45μg/ml and l.95±1.06hours, respectively, in the fasting state, and were 0.63±0.29μg/ml and 2.26±0.65hours, respectively, in the non-fasting state, at a dose level of 3mg (potency)/kg.
At a dose level of 6mg (potency)/kg, Cmax and T 1/2were 1.29±0.49μg/ml and 2.11±1.85 hours, respectively, in the fasting state and were 1.28±0.48μg/ml and 2.01±0.84 hours, respectively, in the non-fasting state.Data of Cmax and AUC showed that blood concentration of the drug depended on dose levels.
Urinary recovery rates in the first 8 hours were 20.5±8.8% in the fasting state and 14.8±5.9% in the non-fasting at a dose level of 3 mg (potency)/kg and 16.5±6.7% and 17.8±2.4%, respectively, at 6mg (potency)/kg.
2.Clinical effects
Clinical effects of CFDN on various infbctions were studied in 612 children who were treated with 5% fine granules of CFDN (5% granule group) and in 208 With 10% fine granules of CFDN (10% granule group).
CFDN granules were administered mainly atdaily doses of 9.0-18.0mg (potency)/kg in 3 divided portions.
Clinical efficacy rates in 428 children of the 5% granule group and in 159 of the 10% granule group from whom causative bacteria were isolated, were 94.9% and 96.2%, respectively.
The clinical efficacy rates for patients who were responsive to previous antibiotic therapy were 91.2% in the 5% granule group and 100% in the 10% granule group.
Bacteriological eradication rate was 82.1 % for 491 strains in the 5% granule group, and was 84.0% for 175 strains in the 10% granule group.
The incidences of side effects were 3.9% (24/608) in the 5% fine granule group and 5.8% (12/206) in the 10% granule group. All of the side effects were slight gastrointestinal disorders, and no serious side effects were found. As for clinical laboratory test results, slight elevations of eosinophile, platelet or transaminase were observed.
Based on the above results, it is considered that the appropriate dose levels of CFDN for pediatric infections ranged from 9.0 to 18.0 mg (potency)/kg a day, divided into 3 portions.

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