The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 47, Issue 7
Displaying 1-14 of 14 articles from this issue
  • [in Japanese], [in Japanese]
    1994 Volume 47 Issue 7 Pages 845-852
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • [in Japanese], [in Japanese]
    1994 Volume 47 Issue 7 Pages 853-860
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • [in Japanese], [in Japanese]
    1994 Volume 47 Issue 7 Pages 861-868
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • TSUNEKAZU HARUTA, SHIGEKAZU KUROKI, KAN-ETSU OKURA, HIROYUKI NIKAMI, T ...
    1994 Volume 47 Issue 7 Pages 869-872
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The transferability of biapenem (L-627) to cerebrospinal fluid (CSF) was studied employing rabbits with experimental meningitis caused by Staphylococcus aureus.
    The mean plasma concentration was 192±12.8μg/ml at 15 minutes after inravenous administration of the drug at a dose level of 100mg/kg. The mean concentration in CSF was maximum at 45 minutes after administration at 11.4±2.19μg/ml.
    Pharmacokinetic parameters calculated from these values were as follows, Cmax (CSF/plasma): 5.96%; AUC (CSF/plasma): 8.15% between 15 and 60 minutes, 12.1% between 15 and 120 minutes and 15.0% between 15 and 180 minutes; T 1/2 for L-627 in CSF: 152 minutes; T 1/2 (CSF/plasma): 3.34.
    In comparison with those of other β-lactam antibiotics that were obtained in the same way, the transferability of L-627 was intermediate, and in considration of the antimicrobial potency against the main pathogens of meningitis, it appears worthwhile of running clinical trials for this drug.
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  • KOZO FUJITA, MICHITO YOSHIKAWA, KOICHI MURONO, SHIZUO MARUYAMA, HIROSH ...
    1994 Volume 47 Issue 7 Pages 873-877
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Twenty-four children were treated with biapenem (L-627) and the clinical efficacy and side effects were evaluated. The ages of the patients ranged from two months to 11.5 years and their body weights from 5.9 to 43.5kg. Doses given were 5.5-12.4mg/kg every 8 hours for 2.67 to 11.33 days. Those patients who responded well to L-627 treatment included11children with pneumonia, 1 with scarlet fever, 1 with cervical lymphadenitis, 2 with cellulitis, 6 with urinary tract infection. Among 21 children, the results were excellent in 13 and good in 8. The drug was well tolerated, although slightly elevated serum concentrations of transaminases occurred in 2 patients among the 24 patients.
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  • NAOKI FUKUSHIMA, AKASHI ISHIKAWA, AIKO TAKASU, YOSHINORI WAGATSUMA
    1994 Volume 47 Issue 7 Pages 878-881
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Biapenem (L-627) was evaluated for its efficacy and safety. The following results were obtained.
    L-627 was given to 9 patients with infections: 3 with pneumonia, 1 with acute bronchopneumonia, 1 with acute bronchitis, 1 with bacteremia, 1 with tonsillitis, 2 with exceptional case. Therapeutic responses were excellent in 3, good in 4, with an efficacy rate of 100%.
    Adverse reactions were noted. No abnormalities were shown in laboratory data.
    It has been concluded that L-627 is a useful drug for the treatment of bacterial infections in children.
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  • AKIRA WATANABE, KENJI SATOH
    1994 Volume 47 Issue 7 Pages 882-888
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Biapenem (L-627) was given intravenously to 17 children with acute bacterial infections including 3 with purulent tonsillitis, 1 with bronchitis, 4 with pneumonia, 2 with sepsis, 3 with pyelonephritis, 2 with SSSS.(2 cases are omitted from evaluation because of Mycoplasma pneumonia and infectious mononucleosis)
    Daily dosages per kg bodyweight ranging from 18.3 to 60mg were given in 3 divided doses per day for 4 to 6 days.
    Clinical responses were excellent in 12 (80%), good in 2 (13.3%), fair in 1 (6.7%) and poor in 0 (0%), with an overall efficacy rate of 93.3%.
    Good bacteriological responses were obtained in all of the 9 cases from which pathogens Were identified.
    A side effect is observed in only 1 case with mild diarrhea.
    The above results suggest that L-627 is a useful new carbapenem derivative for the treatment of bacterial infections in children.
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  • YOSHIKI KAKIZAKI, MASARU YOKOYAMA, NORITAKE TSUSHIMA
    1994 Volume 47 Issue 7 Pages 889-895
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cinical and pharmacokinetic studies were performed on a new carbapenem antibiotic, biapenem (L-627), in children with acute infectious diseases and the results were as follows:
    1) Clinical efficacies were evaluated on the intravenous-administration at daily doses of 17-37.5mg/kg for 4-7 consecutive days in 12 children; 8 children with pneumonia, 2 with cervical lymphadenitis, 1 with pyelonephritis and 1 with suspected sepsis. The clinical efficacies were excellent in 6 patients, good in 5 and poor in 1, yielding an efficacy rate of 91.7%. No side effects or abnormalities of the clinical laboratory tests were observed in 16 children including 12 children evaluated for the efficacy.
    2) L-627 was administered at a dose of 6mg/kg or 12mg/kg, using 30 minutes drip infusion, to 5 children. Maximum concentrations of L-627 in plasma were observed at the end of administration and the values varied from 21.0 to 38.4μg/ml (mean: 31.7±9.3, n=3) at 6mg/kg and 39.0 and 58.8μg/ml (mean: 48.9, n=2) at 12mg/kg. The half-lives in plasma (β phase) were from 0.73 to 1.41 hours (0.98±0.38, n=3) and 0.88 and 0.90 hours (0.89, n=2), and the urinary recovery rates in the first 6 hours were between 61.5 and 69.9% (65.5±4.2, n=3) and 64.7 and 81.1% (72.9, n=2) at 6mg/kg and 12mg/kg, respectively.
    The results indicate that L-627 is effective and safe in children with acute infectious diseases and suggest the usefulness of L-627 in the pediatric field.
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  • TAKESHI TAJIMA, RYOU NIIMI, MASAAKI KOBAYASHI, SACHIKO NEGISHI, YASUO ...
    1994 Volume 47 Issue 7 Pages 896-902
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The results are summarized as follows:
    1. A total of 10 patients were treated with biapenem (L-627). We received informed concent from all of their parents. Each dose was 6mg/kg, and it was administered 3 times daily (40mg/kg, 4 times daily in meningitis), in a 30-minute intravenous drip infusion for 5-17 days. The clinical efficacies of L-627 in 10 patients with bacterial infections (1 with purulent meningitis, 1 with sepsis, 5 with pneumonia, 2 with urinary tract infection and 1 with purulent tonsillitis) were evaluated as excellent in 8 patients, as good in 2 patients with an efficacy rate of 100%. Seven causative organisms found in 5 patients (Streptococcus pneumoniae in 2, Moraxella (Branhamella) catarrhalis in 2, Haemophilus influenzae in 2 and Pseudomonas aeruginosa in 1) were eradicated.
    No adverse reaction was observed in any of the 10 patients.
    2. Pharmacokinetic studies
    Peak plasma concentrations of L-627 were 12.5-13.7μg/ml at the dose of 6mg/kg administered by 30-minute drip infusion.
    Plasma half-lives of L-627 in the β-phase avaraged 0.72 hour (0.63-0.80 hour).
    CSF concentration/plasma concentration ratios of L-627 were 1.12/8.16μg/ml (Day 2, 1.17 hours after at dose of 20mg/kg), 0.88/3.44μg/ml (Day 3, 4.0 hours after at dose of 30mg/kg) and 0.68/5.12μg/ml (Day 13, 3.0 hours after at dose of 40mg/kg) administered by 30-minute drip infusion in the child with purulent meningitis (case 1).
    Based on the above results and the extremely broad spectrum of antibacterial activity of L-627, it is considered that L-627 is a promising antibiotic usable as a single agent for the primary therapy of severe infections in children and immunocompromised host.
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  • HIDENORI MEGURO, RYOCHI FUJII, ITARU TERASHIMA, NOBUYASU ISHIKAWA, HAR ...
    1994 Volume 47 Issue 7 Pages 903-913
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Biapenem (L-627) was evaluated for its safety and efficacy in 27 children with various bacterial infections. L-627 was effective in cases with osteomyelitis due to Staphylococcus aureus, pneumonia and purulent meningitis due to penicillin-resistant Streptococcus pneumoniae, and urinary tract infections due to Enterococcus faecalis, Escherichia coli, or Pseudomonas aeruginosa. However, L-627 failed to produce good responses in 2 of 7 cases of Haemophilus influenzae infections.
    Pharmacokinetic parameters of 30-minutes infusion of 12mg/kg were as follows: Cmax 29-46μg/ml, T1/2 0.68-0.94 hr. Adverse reactions were minimal.
    These data suggest that L-627 is safe in children, and is valuable especially for treatment of infections in immunocompromised hosts and infections due to multiplly resistant bacteria.
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  • KENICHI MIKUNI, TOSHIAKI KOBAYASHI, TSUYOSHI MATSUYAMA, NOBUO WATANABE
    1994 Volume 47 Issue 7 Pages 914-920
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We studied the clinical efficacy of biapenem (L-627), a new parenteral carbapenem β-lactam antibiotic in the pediatric field. L-627 was administered intravenously to 11 patients with ages ranging 2 months to 10 years and 5 months with acute infectious diseases. Doses ranged 28.1 to 72.6mg/kg/day. The diagnosed diseases included 7 respiratory tract infections, 1 purulent meningitis, 1 sepsis, 1 cervical lymphadenitis and 1 urinary tract infection. Two of these cases one with Mycoplasma infection and the other which had been administered with other antimicrobial agents were not evaluated. The clinical efficacy rate was 77.8% (7/9) and the bacteriological eradication rate was 66.7% (4/6).
    Laboratory examinations revealed that there was one case with elevated liver enzyme levels with showing elevation of GOT, GPT and LDH. No other side effects attributable to this drug were observed.
    Thus, it appears that L-627 is a useful antibiotic in treating moderate to severe acute bacterial infections in children.
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  • YUTAKA KUSUMOTO, HIRONOBU AKITA, YOSHITAKE SATO, SATOSHI IWATA, YOSHIN ...
    1994 Volume 47 Issue 7 Pages 921-931
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Bacteriological and clinical studies in the pediatric field have been performed on biapenem (L-627), a newly-developed carbapenem antibiotic, and the following results were obtained.
    1. In the pharmacokinetic study, the plasma concentration of L-627 showed dose-dependant change: Cmax was 14.6μg/ml and AUC was 15.4μg·hr/ml with the administration of 6mg/kg, while Cmax was 49.2μg/ml and AUC was 60.1μg·hr/ml with the administration of 12mg/kg. After the administration of 6mg/kg, the urinary concentration reached maximum within 2 hours and the cumulative urinary excretion rate in the first 6 hours was 49.4%.
    2. Antibacterial activities of L-627 against 27 strains of clinical isolates were determined. MICs of L-627 against such Gram-positive cocci as Staphylococcus aureus, Streptococcus pneumoniae and Streptococcus pyogenes were sufficiently low, and those against such Gram-negative rods as Haemophilus influenzae, Escherichia coli and Bordetella pertussis were satisfactory and as low as those of imipenem or ceftazidime.
    3. Clinical efficacies of L-627 were evaluated in 36 cases of bacterial infections. The overall efficacy rate was 100%, and excellent responses in 26 cases and good in 10 cases were obtained. As for bacteriological efficacies, all strains except 1 of B. pertussis were eradicated and a high eradication rate of 96.6% was obtained.
    4. No side effects were observed in 37 evaluated cases. As abnormal laboratory test results, eosinophilia was noted in 2 cases (5.4%), but they returned to normal values rapidly after the drug was discontinued.
    From these results, it has been concluded that L-627 is a safe and effective drug to be used in treatment of pediatric infectious diseases.
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  • KUNIYOSHI KUNO, AKIMASA OGAWA, FUMIO HAYAKAWA, MASARU KONDO, AKIHISA O ...
    1994 Volume 47 Issue 7 Pages 932-939
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Laboratory and clinical studies on biapenem (L-627), a new carbapenem antibiotic, were carried out in the field of pediatrics.
    1. Antibacterial activities of L-627 against clinically isolated organisms in our department were generally high.
    2. After 30 minutes intravenous infusion of L-627 at a dose of 10mg/kg in 3 and of 12mg/kg in 2 children, peak plasma levels of L-627 ranged from 25.6 to 44.6μg/ml at the end of the infusion. The half-lives were from 0.68 to 0.94 hours. The cumulative urinary recovery rates in the first 6 hours after the start of drip infusion ranged from 11.4 to 47.5%.
    3. 14 patients with various bacterial infections were treated with L-627. The clinical efficacy rate was also 92.9% and the bacteriological efficacy rate was also 92.9%.
    4. No side effects were observed. A few abnormal laboratory test results were obtained, but they were mild with slight elevation of GOT/GPT and plateletes in 1 each.
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  • TADAFUMI NISHIMURA, KUMIKO SUGITA, SHIGEYUKI AOKI, MICHIO TAKAGI
    1994 Volume 47 Issue 7 Pages 940-949
    Published: July 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We have carried out bacteriological and clinical studies on L-627. The results are summarized as follows.
    Treatment with L-627 was made in 14 cases of pediatric bacterial infections including 5 cases of pneumonia and 2 cases each of tonsillitis, urinary tract infection and one case each of colitis, and phlegmon. Results obtained were excellent in 11 cases, good in 2 cases and poor in one case.
    The bacteriological effect of L-627 was excellent, all causative organisms (Staphylococcus aureus one strain, Streptococcus pyogenes 2 strains, Streptococcus pneumoniae 3 strains, Escherichia coli 3 strains, Haemophilus influenzae one strain, Haemophilus parainfluenzae one strain) were eradicated.
    No significant side effects due to the drug were observed in any cases, except 2 cases each of elevated eosinophil counts and elevated platelet counts.
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