The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 45, Issue 12
Displaying 1-12 of 12 articles from this issue
  • KOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUMIKO SUZUKI, KANAE SU ...
    1992 Volume 45 Issue 12 Pages 1609-1621
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We obtained bacterial strains which were clinically isolated and identified from outpatients with various infections in medical institutions throughout Japan. Possible antibacterial activities ofrokitamycin (RKM) were examined against these isolates.
    Minimum inhibitory concentrations (MICs) were determined through a comparative study with reference drugs. The results of the study are summarized as follows.
    1. Resistance patterns of 400 isolates which were highly resistant to macrolides (MLs) with MIC values 100μg/ml were classified into 55 patterns. Staphylococcus spp. showed cross resistance to 14-membered ring MLs with 100% cross resistance observed between erythromycin (EM) and clarithromycin (CAM), and 85.2% between EM and oleandomycin (OL). Fewer isolates showed strong resistance to 16-membered ring MLs than to 14-membered ring MLs. Cross resistances observed among the Staphylococcus isolates were 100% between acetylmidecamycin (MDM-AC) and kitasamycin (leucomycin (LM)), 93.9% between MDM-AC and josamycin (JM), and 53.3% between MDM-AC and RKM. Streptococcus spp. and Peptococcus spp. showed very similar resistance patterns to both 14-and 16-membered ring MLs, but resistance patterns to RKM were quite different.
    Most of anaerobic streptococci and Bacteroides fragilis group had similar resistance patterns to 14-and 16-membered ring MLs, but in some cases a pattern similar to that of Staphylococcus spp. was observed.
    2. When ML-resistant bacteria isolated during 1975 to 1980 were compared to those isolated in 1986 and 1989, it was observed that resistance of Staphylococcus aureus remained almost unchanged, that of Streptococcus pyogenes was lower in the later years than during 1975 to 1980, but that of Streptococcus pneumoniae increased.
    3. Most of ML-resistances of the resistant isolates were inducible, but extents of induction varied depending on drugs tested. Strong inductions were observed when 14-membered ring MLs were used, but inductions were minimal with 16-membered ring MLs. RKM appeared to induce resistance to the least extent. From these results, it appears that the RKM is quite useful clinically even in the 1990s.
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  • YASUHIRO MOCHIZUKI, SHUICHI KANAZASHI, DAISUKE HATA, HIDEO OHKUBO, SET ...
    1992 Volume 45 Issue 12 Pages 1622-1634
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ, BMY-28100), a new oral cephalosporin, was evaluated for its efficacy and safety in 42 children with bacterial infections (Table 1), and the following results were obtained.
    1. CFPZ was administered in 3 or 4 divided doses at daily dosages ranging from 15.3 to 60.0mg/kg to 42 patients (19 cases of acute tonsillitis and/or laryngitis, pharyngitis, 13 cases of pneumonia, 2 cases each of suppurative cervical lymphadenitis and UTI, and 1 case each of scarlet fever, acute otitis media, suppurative parotitis, impetigo contagiosa, furuncle and acute enteritis) and the following clinical results were obtained: excellent; 24 cases, good; 14 cases, fair; 4 cases. The overall efficacy rate was 90.5% (Table 3).
    2. MICs of CFPZ against 50 strains of isolated organisms are shown in Table 4. In 19 cases out of 28 cases examined, causative organisms were successfully eradicated and strain of Staphylococcus aureus was decreased in 1 case.
    3. Diarrhea was observed in 2 cases (cases 8, 11). In case 8, the symptom disappeared spontaneously. Case 11 improved immediately after the administration of the drug was stopped. Among 39 children who went through laboratory tests, eosinophilia which seemed to be related to the administration of this drug was observed in 2 cases (cases 29, 38). Slight elevations of S-GOT and S-GPT were found in 1 case (case 22)(Table 7).
    4. These data suggest that CFPZ is a safe and useful new antibiotic in the treatment of children with susceptible bacterial infections.
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  • MAN WOO, HIROHIKO HIGASHINO, URARA KOHDERA, MAKIKO NAKAMURA, HIROHIDE ...
    1992 Volume 45 Issue 12 Pages 1635-1641
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ, BMY-28100), a new oral cephalosporin, was evaluated for its antibacterial activity and clinical efficacy. Thirty-four patients were treated with 7.7-36.2mg/kg per day of CFPZ divided into 3 times. A total of 33 patients including 3 with acute pneumonia, 2 with acute bronchitis, 17 with acute upper respiratory tract infections, 4 with urinary tract infections, 1 with suppurative lymphadenitis and 6 with other soft tissue infections were evaluated for clinical efficacy except for 1 patient whose general conditions were too serious to continue to be treated with orally medication.
    Clinical effects were excellent in 8 patients and good in 23 but 2 cases were excluded because they were suspected for viral infections, hence the overall efficacy rate was 100%.
    Bacteriological responses were confirmed on 6 (66.7%) strains which were eradicated by the treatment out of 9 strains identified. CFPZ showed stronger antibacterial activities than those ofcefaclor.
    Side effects or abnormal laboratory test results were observed in 2 patients; nausea and pallor of face in 1 patient and an increase of eosinophile in 1. The above findings suggest that CFPZ is a safe and useful antibiotics for the treatment of bacterial infections in pediatric patients.
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  • TSUNEKAZU HARUTA, TSUTOMU TSUTSUI, SHIGEKAZU KUROKI, KAN-ETSU OKURA, Y ...
    1992 Volume 45 Issue 12 Pages 1642-1649
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil granule preparation was administered orally to 16 patients (ages ranging 8 months to 9 years and 6 months) with pediatric bacterial infections at daily dose levels between 29.4 and 35.7mg/kg divided into 3 or 4 doses. The following results were obtained.
    1. Sixteen patients including 5 with pharyngitis, 3 with tonsillitis, 3 with lacunar tonsillitis, 2 with pneumonia, 2 with contagious impetigo and 1 with scarlet fever were treated. Clinical effects were excellent in 9 cases and moderate in 7, with an overall efficacy rate of 100%.
    2. Organisms suspected as pathogens included 17 strains (10 strains of Haemophilus influenzae, 2 of Haemophilus parainfluenzae, 3 of Streptococcus pyogenes and 2 of Staphylococcus aureus). Bacteriologically, eradication of pathogens were observed for 11 strains, but no changes were obtained for 5 (all Haemophilus), and unknown results were obtained for 1, thus the eradication rate was 68.8%.
    3. No side effects were observed. Abnormal laboratory test results included 2 cases of increase in platelets, and 2 of increase in eosinophils, but those were not significant.
    4. No refusal of the drug occurred due to its taste or odor.
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  • TAKANORI SEKIGUCHI, YOSHIROU SHIINO, KAZUYOSHI MURAKAWA, MIDORI NISHIM ...
    1992 Volume 45 Issue 12 Pages 1650-1657
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ, BMY-28100) fine granules were given orally to 21 children with acute bacterial infections including 15 cases of acute tonsillitis and 3 each of acute bronchitis and urinary tract infections. Good to excellent clinical responses were obtained in 19 of the 21 patients and bacterial eradications were obtained for all 11 strains found in these cases. Loose stool and eosinophilia were observed in 1 case each.
    From the above clinical results, it appears that CFPZ is a useful antibiotic for the treatment of pediatric patients with various bacterial infections.
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  • SEIKYO FURUKAWA, TAKASHIGE OKADA
    1992 Volume 45 Issue 12 Pages 1658-1662
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ, BMY-28100) granules were administered to 20 children with bacterial infections: acute tonsillitis 8, acute bronchitis 10, purulent lymphadenitis 1, urinary tract infection 1.
    Daily doses ranged 29-50mg/kg. The drug was given orally, 3 times a day and the durations of administration were 5 to 9 days.
    Clinical efficacies were excellent in 16 cases and good in 4 cases, hence the overall efficacy rate was 100%.
    No side effects were observed in any of these cases. As for abnormal laboratory test values, thrombocytosis was observed in 1 case.
    From the above results, we consider CFPZ granules to be a useful drug for the treatment of pediatric patients with various bacterial infections.
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  • MICHINORI ITO, EIJI TAKEDA, YASUHIRO KURODA
    1992 Volume 45 Issue 12 Pages 1663-1666
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ, BMY-28100), a new non-ester cephem, was administered to 15 pediatric patients with infectious diseases. The patients included 6 boys and 9 girls from 10 months to 11 years old and they were given oral doses of 18.5-41.7mg/kg/day for 3 to 8 days.
    Clinical efficacies were excellent in 3 cases and good in 12 cases, hence the total efficacy rate was 100%.
    Eosinophilia occured in 1 case as side effect of the drug, but no other side effects were not found during or after the treatment.
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  • YUKIKAZU KAINOU, SHUHEI MATSUMOTO, KAICHI KIDA, HIROSHI MATSUDA
    1992 Volume 45 Issue 12 Pages 1667-1675
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    1. Serum levels of cefprozil (CFPZ, BMY-28100) after single oral administration of 7.5mg/kg were 2.9-5.5μg/ml at 1 hour and trace at 6 hours.
    2. Urinary excretion rates of CFPZ were 45.7-102.3% within 6 hours (HPLC).
    3. CFPZ was administrated at doses ranging 19-47.3mg/kg/day to 17 cases of pediatric infections including 16 cases with respiratory infections and 1 case with external otitis.
    Good clinical and bacteriological responses were obtained in all cases.
    4. As side effect, diarrhea was observed in 1 case.
    As abnormal laboratory test results, eosinophillia was observed in 5 cases.
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  • HIROSHI WAKIGUCHI, NAOFUMI OHISHI, SHINJI KIDO, TOMOMI TAKECHI, KOJI T ...
    1992 Volume 45 Issue 12 Pages 1676-1683
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    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.
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  • TAKASHI MOTOHIRO, MASAFUMI ARAMAKI, KEIKO ODA, AKIRA KAWAKAMI, TATSUHI ...
    1992 Volume 45 Issue 12 Pages 1684-1699
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ), a newly developed cephalosporin in fine granular form, was administered to pediatric patients with skin and soft tissue infections. MICs were determined for 6 drugs including CFPZ, cephalexin (CEX), cefaclor (CCL), ampicillin (ABPC), methicillin (DMPPC), cloxacillin (MCIPC) against 53 clinical isolates of Staphylococcus aureus from these patients. An inoculum size of 106 CFU/ml was used in the MIC-determinations.
    CFPZ was given to 73 patients with ages ranging from 6 months to 10 years and 8 months and 71 cases were evaluable for clinical effects as follows; impetigo (65), Staphylococcal scalded skin syndrome (1), furuncle (1), subcutaneous abscess (3), and periproctal abscess (1).
    To study clinical efficacy, bacteriological effects and safety of this drug, a mean dose of 8.4mg/kg with 3-4 daily dosages (57 cases of t. i. d. and 14 cases of q. i. d.) was administered for an average of 6 days. The results obtained are summarized as follows.
    1. With regard to the 53 isolates of S. aureus, MICs of CFPZ against 52 strains (98.1%) ranged from 0.78 to 3.13μg/ml. 45 strains (84.9%) were inhibited at 0.78μg/ml. MIC90 of CFPZ was 1.56μg/ml, but MIC against 1 strain of Methicillin-resistant S. aureus (MRSA) was 100μg/ml.
    The MIC90 of CEX and CCL were 6.25μg/ml and MIC of CEX and CCL against 1 MRSA strain were 200 and 100μg/ml, respectively. The MIC90 of ABPC, DMPPC and MCIPC were 6.25, 3.13 and 0.39μg/ml, respectively. CFPZ showed the second highest activity after MCIPC against S. aureus.
    2. CFPZ showed very good clinical responses and clinical effects in 71 patients all of whom judged by doctors in charge as having “good” or better responses.
    3. For impetigo patients, the evaluable cases by score 3, 5 and 7 days after administration of the drug were 52, 39 and 20 patients, respectively. The efficacy rates on these days were 90.4, 100 and 100%, respectively.
    The efficacy rate at a daily dose of 30.1-45.0mg/kg on day 3 was 17.2% higher than that at 22.5-30.0mg/kg, and the “excellent” response rate of 30.1-45.0mg/kg group was 45.3% greater. Because of these results, it is expected that good clinical effects can be obtained at a daily dose of 22.5-30.0mg/kg of CFPZ, but better responses can be expected at 30.1-45.0mg/kg in 3-4 divided doses given for 5 days.
    4. Bacteriological effects of CFPZ were determined against 60 strains of S. aureus. All bacteria were eradicated and there were no differences among different daily dosages.
    5. No patients were reported to show adverse reactions on difficulty in taking CFPZ. Though the number of patients treated in this study was small, no cases with abnormal laboratory test results were observed.
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  • TAKASHI MOTOHIRO, MASAFUMI ARAMAKI, KEIKO ODA, AKIRA KAWAKAMI, TATUSHI ...
    1992 Volume 45 Issue 12 Pages 1700-1735
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ), a newly developed oral cephalosporin in a fine granular form for pediatric use, was administered to children with bacterial infections. MICs were determined for 6 drugs including CFPZ, cephalexin (CEX), cefaclor (CCL), ampicillin (ABPC), methicillin (DMPPC) and cloxacillin (MCIPC) against the following 84 strains isolated from cases to which CFPZ was administered; 55 strains of Gram-possitive cocci (GPC) including 2 strains of Staphylococcus aureus, 49 strains of Streptococcus pyogenes, 4 strains of Streptococcus pneumoniae, and 29 strains of Gram-negative bacilli (GNB) including 10 strains of Haemophilus influenzae, 18 strains of Escherichia coli, and 1 strain of Proteus mirabilis. MIC determination of these strains was done with an inoculum size of 106 CFU/ml.
    In pharmacokinetic studies, serum concentrations, urinary concentrations and urinary recovery rates were investigated using bioassay and high-performance liquid chromatography (HPLC). CFPZ was orally administered 30 minutes before meals to 9 children with ages ranging from 7 years and 1 month to 12 years and 3 months. Three groups of 3 children were tested with doses of 4.0, 7.5 and 15.0 mg/kg, respectively.
    In addition to the above, clinical and bacteriological studies were performed in a total of 160 cases consisting of children with ages ranging 5 months to 12 years and 5 months. A mean dose of 8.6 mg/kg in 3-4 divided doses (130 cases of t. i. d. and 30 cases of q. i. d.) was administered for an average of 7 days. The 160 cases included 34 cases of pharyngitis, 5 cases of tonsillitis, 8 cases of acute bronchitis, 8 cases of pneumonia, 52 cases of scarlet fever, 4 cases of acute purulent otitis media, 47 cases of urinary tract infection, 1 case of purulent lymphadenitis and 1 case of posthitis. Adverse reactions and abnormal clinical laboratory test results were also examined in 166 cases, including 6 cases excluded from the evaluation of clinical efficacy. The results obtained are summarized as follows:
    1. With regard to GPC, MICs of CFPZ against 2 strains of S. aureus were 0.78 or 1.56μg/ml and CFPZ showed the second highest activity to MCIPC. MICs of CFPZ against 49 strains of S. pyogenes were all less than 0.025μg/ml. These MIC values were the same as those of ABPC and superior to those of the other 4 drugs. MICs against 4 strains of S. pneumoniae ranged from 0.20 to 1.56μg/ml, these values were the same as or similar to those of DMPPC and MCIPC and superior to those of CEX and CCL, but inferior to those of ABPC.
    Regarding GNB, all MICs against 10 strains of H. influenzae were 1.56 or 3.13μg/ml and the MIC90 of CFPZ was 3.13μg/ml. It was similar to those of CCL and DMPPC, lower than those of CEX and MCIPC and higher than that of ABPC. MICs against 18 strains of E. coli ranged from 0.78 to 50μg/ml and the MIC90 was 12.5μg/ml. These MIC values were similar to those of CEX and CCL and superior to those of ABPC, DMPPC and MCIPC. MIC against 1 strain of P. mirabilis was 1.56μg/ml, and was similar to the MICs of CCL and ABPC and superior to the MICs of CEX, DMPPC and MCIPC.
    2. CFPZ was administered to 9 cases at 4.0, 7.5 and 15.0mg/kg, respectively, for 3 cases each and serum concentration was determined by bioassay. Average peak concentrations for each dose group were 3.18, 3.88 and 8.43μg/ml, respectively. Thus a dose response was observed between the 4.0 or 7.5 mg/kg and 15.0mg/kg dose groups.
    Average half-lives for the 3 groups were very similar, 1.0, 1.2 and 1.1 hours, respectively. Mean AUCs were 7.8, 9.9 and 25.2μg·hr/ml, respectively and a dose response was observed between the 4.0 or 7.5mg/kg and 15.0mg/kg dose groups. The mean pharmacokinetic parameters determined by the HPLC method showed similar results to those of bioassay.
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  • KIYOAKI NAGANO, HIDENORI MAEDA, TADAMICHI YANAGI, YOSHIROU TSUJI, HAJI ...
    1992 Volume 45 Issue 12 Pages 1736-1744
    Published: December 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefprozil (CFPZ, BMY-28100) is a new oral cephem antibiotic without an ester linkage. Pharmacokinetic and clinical studies using CFPZ 10% fine granules were performed in pediatric patients.
    1. Pharmacokinetic investigation
    Peak serum concentrations of CFPZ after dose of 7.5mg/kg and 10mg/kg were, respectively, 3.65±0.24μg/ml and 6.38±3.23μg/ml at 1-2 hours. The average half-life with 7.5mg/kg administration was 0.90±0.16 hours and that with 10mg/kg was 1.29±0.50 hours. The urinary excretion of CFPZ was about 45% (35.3-50.0%) in 6 hours.
    2. Clinical investigation
    Enrolled in the study were 22 patients including 4 with pharyngitis, 3 with tonsillitis, 3 with bronchitis, 5 with pneumonia, 4 with urinary tract infection, and 1 each with pertussis, purulent lymphadenitis and otitis media. Responses were excellent in 14 patients, good in 5 patients and fair in 1 patient. In the assesment of the bacteriological efficacy, 8 out of 17 strains of organism identified previous to the treatment were eradicated, 5 strains were found replaced by other bacteria and 4 strains persisted, hence the eradication rate was 76.5%
    3. No adverse reactions attributable to the drug were observed. From the above results, it has been concluded that CFPZ is a highly effective and safe agent for moderate respiratory and urinary tract infections in children.
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