The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 45, Issue 4
Displaying 1-12 of 12 articles from this issue
  • KOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUTAKA NAKANE, YUMIKO S ...
    1992 Volume 45 Issue 4 Pages 359-363
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Against strains of Branhamella catarrhalis which were separated from various RTIs (respiratory tract infections) in 1991 antimicrobial activities (MICs) of cefetamet (CFMT) were determined, and the following conclusions were obtained.
    1. The MIC80 of CFMT against B. catarrhalis was 0.39μg/ml, which was higher than that of cefixime (CFIX) by one dilution or twofold, but was lower than that of cefpodoxime (CPDX) by two dilutions or fourfold and that of cefotiam (CTM) by three dilutions or eightfold.
    2. The fact that all of the 50 strains tested were β-lactamase producers appeared to indicate that CFMT was stable against BRO-1 and BRO-2 β-lactamases produced by B. catarrhalis.
    3. Blood concentrations of the test drug, CFMT, and control drugs upon normal single doses were calculated using pharmacokinetic parameters. Lengths of time periods during which drug concentrations stayed above their MICs against B. catarrhalis obtained in this study were determined for CFMT, CFIX, CPDX and CTM. They were, respectively, 12 hours, 12 hours, 6 hours and 2 hours, thus CFMT appeared to remain above MIC for sufficiently long time for the treatment of RTIs which are affected by B. catarrhalis directly or indirectly.
    Download PDF (536K)
  • NAO-AKI WATANABE, NAOKI ASAKAWA, TOSHIO TOYOSAWA, RYOICHI HIRUMA, KATS ...
    1992 Volume 45 Issue 4 Pages 364-370
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Administration of latamoxef and cefoperazone, reported to act like disulfiram in humans, caused a depression of mitochondrial low Km aldehyde dehydrogenase (low Km ALDH) activity in rats. In addition, a marked increase of blood acetaldehyde concentration was observed when rats were given alcohol orally at 18 hours after administration of these cephalosporins. However, mitochondrial low Km ALDH activity and blood acetaldehyde level were not altered by repeated administration of 300mg and 1,000mg of cefclidin (CFCL, E1040) or E1077 per kg. From these results, it was concluded that neither CFCLn or E1077 affected the alcohol metabolizing-system.
    Download PDF (854K)
  • KUNIYOSHI KUNO, AKIMASA OGAWA, FUMIO HAYAKAWA, HIDETOSHI TAKEUCHI, KAZ ...
    1992 Volume 45 Issue 4 Pages 371-380
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Laboratory and clinical studies on panipenem/betamipron (PAPM/BP), a new carbapenem antibiotic, were carried out in the field of pediatrics and the following results were obtained.
    1. The antibacterial activities of panipenam (PAPM) against clinically isolated organisms in our department were high overall.
    2. After 30 minutes intravenous infusion of PAPM/BP at a dose of 10mg/10mg/kg in 1 and of 20mg/20mg/kg in 2 children, peak plasma levels of PAPM ranged from 33.21 to 75.66μg/ml at the end of the infusion. The half-lives were 0.81 to 0.93 hours. The cumulative urinary recovery rates in the first 6 hours after the start of drip infusion ranged from 10.7 to 40.4%.
    3. PAPM/BP was administered to 16 pediatric patients with various infections. The clinical and bacteriological efficacy rates were both 100%.
    4. No side effects were observed. Abnormal laboratory test results were also mild; slight elevation of GOT, GOT/GPT and eosinophylia in 1 each and thrombocytosis in 2.
    Download PDF (835K)
  • NAOICHI IWAI, HARUHI NAKAMURA, MITSUNOBU MIYAZU, YUMI WATANABE, YOICHI ...
    1992 Volume 45 Issue 4 Pages 381-397
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetic and clinical studies in pediatrics were performed on panipenem/betamipron (PAPM/BP), a combined drug of a carbapenem antibiotic (panipenem) and organic ion inhibitor (betamipron) at a weight ratio of 1: 1.
    1. Plasma levels and urinary excretion were studied when PAPM/BP, at 10mg/10mg/kg (4 cases) or 20mg/20mg/kg (5 cases), was administered using intravenous drip infusion in 30 minutes to 9 children (4-14 years old).
    The plasma PAPM level at the end of drip infusion was 30.75±4.98μg/ml in the cases administered with 10mg/10mg/kg and 68.72±5.73μg/ml in the cases administered with 20mg/20mg/kg. Drug concentrations then gradually decreased with half-lives of 1.08±0.09 hours and 0.98±0.02 hour, and reached 0.39±0.14μg/ml and 0.62±0.06μg/ml, respectively, after 5.5 hours.
    Plasma BP levels at the end of drip infusion was 18.93±3.75μg/ml in the cases administered 10mg/10mg/kg and 37.09±2.68μg/ml in the cases administered 20mg/20mg/kg, and half-lives were 0.55±0.07 hour and 0.61±0.03 hour, respectively; the plasma BP level could not be determined in any cases after 5.5 hours.
    Mean urinary recovery rates of PAPM in the first 6 hours after the start of intravenous drip infusion were 33.0±6.1% in the cases administered 10mg/10mg/kg and 21.8±2.3% in the cases administered 20mg/20mg/kg and those of BP were 77.0±2.4% and 76.6±7.3%, respectively.
    2. When PAPM/BP, was administrated at 31.3mg/31.3mg/kg thought by intravenous drip infusion in 30 minutes to 1 case of purulent meningitis, PAPM levels were 0.76μg/ml at the end of drip infusion but varied between 0.80 to 1.97μg/ml 30 minutes after the end of drip infusion during 8 days of treatment.
    3. PAPM/BP was administered to 43 cases, 47 diseases of bacterial infections in the domain of pediatrics to study its clinical efficacy, bacteriological efficacy and adverse reactions. Single doses were 5.2mg/5.2mg to 31.3mg/31.3mg/kg; frequencies of administration were 3 to 4 times a day, and durations of administration were 3 1/3 to 11 days; and total dosages ranged between 1.125g/1.125g and 11.0g/11.0g.
    Responses were rated as “excellent” in acute purulent tonsillitis 6 cases, acute suppurative cholangitis 1 case, acute enteritis 3 cases and purulent meningitis 1 case, as “good” in cellulitis 1 case and acute urinary tract infection 1 case, as “excellent” in 1 and “good” in 3 out of 4 cases of acute purulent otitis media and as “excellent” in 22 and “good” in 7 out of 30 cases of acute pneumonia. In all the evaluable cases, the resluts were rated as “good” or “excellent”.
    As for the bacteriological effects on Staphylococcus aureus 1 strain, Streptococcus pyogenes 1 strain, Streptococcus pneumoniae 10 strains, Haemophilus influenzae 12 strains and Escherichia coli 1 strain which were detected as the pathogenic bacteria in these cases, the results were rated as “disappeared” in all the cases except 1 strain of H. influenzae which was rated as “decreased”.
    No adverse reactions were observed. As abnormal changes in laboratory data, elevation of GOT was observed in 1 case and increases in platelet counts in 3 cases.
    Download PDF (1722K)
  • MASARU IDO, MASAHIRO ITOH, MINORU SAKURAI, TOSHIAKI IHARA, HITOSHI KAM ...
    1992 Volume 45 Issue 4 Pages 398-407
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (PAPM/BP), a mixture of a newly synthesized carbapenem antibiotic panipenem (PAPM) and N-benzoyl-β-alanine, betamipron (BP), was evaluated for pharmacokinetics, in vivo and in vitro antimicrobial effect, and clinical efficacy in pediatric patients.
    Intravenous drip infusion of either 10mg/10mg/kg or 20mg/20mg/kg of PAPM/BP for 30 minutes resulted in maximum plasma concentrations of 36.6μg/ml and 92.5μg/ml, half lives (T 1/2β) of 1.17 hours and 0.88 hours, and urinary excretion until 6 hours of 29% and 17.7%, respectively.
    Antibacterial activities of PAPM against Gram-positive cocci and Gram-negative rods isolated from pediatric patients were equal to or slightly stronger than those of imipenem, ceftazidime, cefoperazone, and piperacillin. Clinical effects of PAPM/BP evaluated in 17 patients were as follows; excellent in 8 cases, good in 8 cases, and fair in 1 case. The overall efficacy rate was 94.1%.
    Elevations of GOT and/or GPT were observed in 2 patients and transient eosinophilia was observed in 1 patient.
    Download PDF (859K)
  • TADAFUMI NISHIMURA, KAZUO TABUKI, SHIGEYUKI AOKI, MICHIO TAKAGI
    1992 Volume 45 Issue 4 Pages 408-415
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We have carried out clinical studies on panipenem/betamipron (PAPM/BP, CS-976). The results are summarized as follows.
    Treatment with PAPM/BP was made in 21 cases of pediatric bacterial infections including 2 cases of tonsillitis, 15 cases of pneumonia and 1 case each of bronchitis, scarlet fever, urinary tract infection and otitis media.
    Results obtained were excellent in 15 cases, good in 6 cases.
    No significant side effects due to the drug were observed in any cases.
    Download PDF (894K)
  • INCLUDING CASES OF PENICILLIN-RESISTANT STREPTOCOCCUS PNEUMONIAE MENINGITIS
    TSUNEKAZU HARUTA, KAN-ETSU OHKURA, SHIGEKAZU KUROKI, HIROYUKI NIKAMI, ...
    1992 Volume 45 Issue 4 Pages 416-423
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The efficacy and the safety of panipenem/betamipron (PAPM/BP), a new carbapenem antibiotic against infections in pediatrics were studied. The obtain results are summarized as follows.
    1. The transfer of PAPM/BP to cerebrospinal fluid (CSF) was studied in 2 cases of purulent meningitis. The PAPM/BP levels in CSF in a dose 26.1mg/kg peaked at 3.21μg/ml on sampling 30 minutes after administration, followed by decreasing gradually with the improvement in clinical symptoms and came to 0.86μg/ml on the 12th day (30 minutes after administration).
    2. PAPM/BP at dose levels of 50mg/kg to 69mg/kg a day (daily doses of 104mg/kg, 175mg/kg 4 times a day for 2 cases of purulent meningitis) was administered by intravenous drip infusion 3 times daily for 4 to 15 days to 2 cases of purulent meningitis (including 1 case of penicillin-resistant Streptococcus penumoniae meningitis), 3 cases of pneumonia, 2 cases of phlegmon, 2 cases of periproctal abscess and 2 cases of urinary tract infections for a total of 11 cases. As results, all the cases showed good responses including 5 excellent and 6 good responses. Bacteriological efficacies in all of the 9 eligible cases were assessed as “eradicated”.
    3. As for the safety, an increase in the platelet count and slight evaluation of GOT and GPT were seen in 1 case as abnormal changes in the laboratory findings, although no side-effect was observed.
    4. The results above show that PAPM/BP is useful for the treatment of general infections in pediatrics and that a daily dose of about 60mg/kg given in 3 divided doses in effective enough. This preparation may be useful for purulent meningitis as well, but further studies are needed as to the dosage.
    Download PDF (894K)
  • SEIKYO FURUKAWA, TAKASHIGE OKADA
    1992 Volume 45 Issue 4 Pages 424-429
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Studies were carried out on the clinical efficacy of panipenem/betamipron (PAPM/BP) against bacterial infections. The results are summarized as follows:
    1. PAPM/BP were administered to total 21 patients (7 cases of pneumonia, 1 case of bronchitis, 3 cases of cellulitis, 2 cases of purulent lymphadenitis, 2 cases of otitis media, 1 case of purulent parotitis, 1 case of sinusitis, 1 case of mastoiditis, 2 cases of urinary tract infection and 1 case of purulent meningitis) by drip intravenous injection.
    2. Clinical responses of PAPM/BP were excellent in 12 cases, good in 7, poor in 1 and unknown in 1 case. The overall efficacy rate was 95.0%.
    3. Concentration of PAPM in cerebrospinal fluid after 1 hour drip intravenous administration in 1 case of purulent meningitis were 6.84μg/ml at the acute stage and 3.28μg/ml at the recovering stage.
    4. Neither side effects nor abnormal laboratory findings were observed except 1 case of increase of thrombocytosis out of 19 cases.
    5. From the results, PAPM/BP was determined to be an efficacious and safe drug for the therapy of pediatric infection.
    Download PDF (616K)
  • TAKANORI SEKIGUCHI, TAKASHI OKAMOTO, KATSUAKI OHARA, HIROKO KOUZAN, AT ...
    1992 Volume 45 Issue 4 Pages 430-436
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (PAPM/BP) was given by 30 minutes drip infusion to 15 children with acute bacterial infections including 11 with acute pneumonia, 2 each with staphylococcal scalded skin syndrome and urinary tract infections.
    Good to excellent clinical responses were obtained in all of the 15 patients and bacterial eradications were obtained for all 12 strains identified in these cases.
    Urticaria considered to be drug related was observed in 1 patient. Slight elevations of GOT and GPT and eosinophilia were observed in 1 case each. From the above clinical results, it appears that PAPM/BP is a useful antibiotic for treatment of pediatric patients with various bacterial infections.
    Download PDF (682K)
  • HIDEO MORITA, FUMIHIKO HAMADA, MIKIYA FUJIEDA, TAKUTOSHI HOSOKAWA, AKI ...
    1992 Volume 45 Issue 4 Pages 437-442
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We conducted clinical studies on panipenem/betamipron (PAPM/BP), a newly developed parenteral carbapenem antibiotic, for its clinical application in the field of pediatrics.
    1. A clinical study was performed on 13 children with infections, including 6 with acute bronchopneumonia, 1 each with acute pharyngitis, acute bronchitis, sepsis, staphylococcal scalded skin syndrome, urinary tract infection, subcutaneous abscess and furuncle.
    PAPM/BP was administered by intravenous drip infusion. Doses varied from 12 to 27mg/kg body weight were given t. i. d. or q. i. d. Lengths of treatment ranged from 4 to 25 days.
    Clinical efficacies were excellent in 3 and good in 9 cases, with an efficacy rate of 92%.
    2. No adverse reactions were observed. In laboratory tests, elevations of GOT, GPT and urobilinogen were observed in 3 cases. It was concluded that PAPM/BP was a promising drug for the treatment of bacterial infections in children.
    Download PDF (562K)
  • YOSHIKI FUJISAWA, HISAMICHI TAUCHI, KAICHI KIDA, HIROSHI MATSUDA
    1992 Volume 45 Issue 4 Pages 443-451
    Published: April 25, 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Panipenem/betamipron (PAPM/BP) is a mixture of panipenem (PAPM), carbapenem antibiotic, and betamipron (BP), N-benzoyl-β-alanine. The adverse reaction to PAPM of the kidney is reduced by the addition of BP to PAPM which inhibits the anion transport in the kidney tubules.
    We studied the pharmacokinetics and the clinical efficacies of PAPM/BP in children and we evaluated the antibacterial activities of PAPM by determining MIC values of PAPM in vitro against organisms isolated in our children's hospital from January to December, 1990.
    1. Pharmacokinetics 10mg/kg of PAPM/BP (10mg PAPM/10mg BP) was administered intravenously by drip infusion to 7 children. The mean blood concentration of PAPM was 14.8μg/ml at the peak, and the mean half life was 0.9 hours in blood. PAPM was not detected in blood 3 hours after the time when the peak values were attained.
    2. Clinical studies 10mg/kg of PAPM/BP was administered intravenously 3 times a day to 18 cases including 15 of respiratory infections, 2 of otitis media and 1 of sepsis. The clinical efficacies of PAPM/BP were excellent or good in 17 out of thd 18 cases. All causative organisms isolated in 5 cases, Methicillin-sensitive Staphylococcus aureus (MSSA)(1 case), Streptococcus pneumoniae (1), Haemophilus influenzae (2) and Branhamella catarrhalis (1) were eradicated in a few days upon the administrations of PAPM/BP.
    No adverse reactions due to PAPM/BP were observed, but a slight elevation of platelet counts in blood was observed in I case, which was normalized soon after the end of the treatment.
    3. Antibacterial activities in vitro The 198 organisms were isolated in this experiment, including Methicillin-resistant
    S. aureus (MRSA)(21 strains), MSSA (22), Staphylococcus epidermidis (16), S. pneumoniae (4), Enterococcus faecalis (16), and other Gram-positive organisms (29), and Escherichia coli (14), H. influenzae (7), Klebsiella pneumoniae (8), Pseudomonas aeruginosa (11), B. catarrhalis (7), and other Gram-negative organisms (43). The MIC50 values of PAPM against the Gram-positive isolates except MRSA were 0.025 to 1.56μg/ml, and those of PAPM against the Gram-negative isolates except P. aeruginosa were 0.025 to 0.78μg/ml. These results indicate that PAPM/BP may be useful to various bacterial infections caused by Gram-positive or Gram-negative organisms in children.
    Download PDF (876K)
  • 1992 Volume 45 Issue 4 Pages 452-
    Published: 1992
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
feedback
Top