CHEMOTHERAPY
Online ISSN : 1884-5894
Print ISSN : 0009-3165
ISSN-L : 0009-3165
Volume 38, Issue 5
Displaying 1-9 of 9 articles from this issue
  • KAZUO IWATA, TAKAKO YAMASHITA, HIROKO UEHARA, YOSHINORI NOZAWA
    1990 Volume 38 Issue 5 Pages 435-443
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    The in vitro resistance of Trichophyton mentagrophytes to piritetrate (M-732), a new thiocarbamate antidermatophytic compound, was studied in comparison with a reference thiocarbamate, tolnaftate. It was found that this fungus was not readily able to develop resistance to either of these compounds. After a long period of serial subculturing of six strains in Sabouraud dextrose broths and on Sabouraud dextrose agar slants containing increasing concentrations of compound, only one strain of each eventually became highly resistant to tolnaftate in either media. None of the strains acquired resistance to piritetrate. The two tolnaftate-resistant strains thus obtained manifested morphological, biochemical and pathological changes and showed partial cross-resistance to piritetrate.
    Download PDF (4565K)
  • KAZUHIRO TATEDA, KEIZO YAMAGUCHI, YOSHIKAZU ISHII, KAZUNORI SHIMOGUCHI ...
    1990 Volume 38 Issue 5 Pages 444-449
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    Vibrio cholerae non-01 are organisms that are biochemically indistinguishable from V.cholerae but do not agglutinate in vibrio group 1 antiserum. Some of these strains have been known to produce a cholera-like toxin and cause dehydrating gastroenteritis in humans. Some reports state that more than 20% of V.cholerae isolated from blood are non-01 especially in patients with liver disease. We investigated drug susceptibility and resistance mechanisms to beta-lactam antibiotics in clinical (10 strains) and environmental isolates (80 strains) of V.cholerae non-01. Of the antibiotics tested, ceftizoxime and ofloxacin were extremely active against V.cholerae non-01: both antibiotics inhibited growth of all strains with 0.025 mg/l. None of the 10 strains of the clinical isolates was resistant to other antibiotics tested. On the other hand, 30 strains of the 80 environmental isolates (37.5%) were resistant to ampicillin (ABPC). All these strains showed MICs of ≥12.5 mg/l and all produced beta-lactamase. In a substrate profile study of this enzyme, it was clarified that the beta-lactamase produced by V.cholerae non-01 was basically penicillinase. There is a possibility thit thus resistance to ABPC in environmental isolates of V.cholerae will spread to clinical isolates. We therefore need to be on our guard against the emergence of resistant strains in clinical V.cholerae non-01 infection.
    Download PDF (973K)
  • SEN SUZUKI, SEIICHI NAKANO, MAKOTO YANAGAWA, JUICHI KAWAMURA, ITSUO YA ...
    1990 Volume 38 Issue 5 Pages 450-452
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    Aztreonam (AZT), a new kind of antibiotic which is fairly stable against β-lactamase, was tried on patients with benign prostatic hyperplasia (BPH) and its blood and bladder wall tissue levels were determined. The subjects were 11 patients with BPH who all underwent retropubic prostatectomy. As soon as the operation was started, 100 ml of saline solution in which 2 g of AZT had been dissolved was administered by intravenous drip infusion for 10 min. Sixty minutes after the infusion about 1 g of tissue was harvested across all layers of bladder wall, and 2 ml of blood was drawn at the same time. The mean tissue level was 65.4±13.6μg/ml, and the mean tissue level was 38.8±25.3μg/g, consistent with the reported transport of existing cephem antibiotics to the blood and bladder wall.
    Download PDF (366K)
  • INFLUENCE OF MEAL AND SOLVENTS ON SERUM CONCENTRATION AND EFFICACY
    SHUICHI MIYAZAKI, YOSHIHISA ISHIDA, MITSUHIRO KATSUTA, YASUKO KANEKO, ...
    1990 Volume 38 Issue 5 Pages 453-460
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    We studied the influence of meal and solvents on the therapeutic efficacy of quinolones and oral cephems. The serum concentration and ED50 of oral antimicrobial agents suspended in water or milk were determined in fasted or non-fasted mice.
    When cefixime, ofloxacin or enoxacin was orally administered to fasted mice, the serum concentration of each drug was higher than when water was used as a solvent. In contrast, when cefpodoxime proxetil or ciprofloxacin was administered to non-fasted mice, the serum concentration was higher in fasted mice. When cefaclor was suspended in water, the serum concentration in non-fasted mice was higher than that in fasted mice, but in fasted mice it was higher than in non-fasted when milk was used as a solvent. These results affected the drugs' efficacy in mice systemically infected with Klebsiella pneumoniae, in whom Cmax correlated best with ED50. However, the ED50 of cephems suspended in milk was lower than that in cephems suspended in water.
    Download PDF (935K)
  • KAZUYA KAWAHARA
    1990 Volume 38 Issue 5 Pages 461-476
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    To clarify the relationship between CNS toxicity and penetration of fluoroquinolones into human cerebrospinal fluid (CSF), five agents, namely, norfloxacin (NFLX), enoxacin (ENX), ofloxacin (OFLX), ciprofloxacin (CPFX) and fleroxacin (AM-833) were given preoperatively to 193 patients with urological diseases. CSF and blood samples were collected during spinal anesthesia at surgery.
    1) Firstly, a single dose of 200 mg of drug was given to patients 3 h before lumbar anesthesia. The mean CSF concentration (mean±SE) of AM-833 (0.412±0.082μg/ml) was the highest, followed by OFLX, ENX, CPFX, and NFLX. There were statistically significant differences among AM-833, OFLX>ENX**>CPFX, NFLX**p<0.01, DUNCAN'S multiple comparison procedures) The CSF/serum concentration ratio showed essentially the same tendency.
    2) NFLX, ENX or OFLX was given in consecutive doses of 600 mg /day, t. i. d. for 3 days, or CPFX at 600 mg/day, t.i.d. for 5 days, or AM-833 at 200 mg /day once a day for 3 days. CSF samples were collected 3 h after the last dose. In the consecutive dose group, CSF concentrations and CSF/serum ratios were as follows: ENX**(0.661±0.085μg/ml, 0.289±0.028), OFLX**(0.935 ± 0.156μg/ml, 0.315±0.032), CPFX**(0.128±0.014μg/ml, 0.125±0.011) and AM-833*(0.898±0.136μg/ml, 0.304±0.122)*p<0.05, **p<0.01, STUDENT'S t-test). Thus, higher CSF levels and CSF/serum ratios were demonstrated in the consecutive dose group.
    3) In the single-dose group of 300 mg of AM-833, the CSF concentration was 0.599± 0.134 μg/ml and the CSF/serum ratio 0.198±0.228. In the consecutive dose group, these values were 1.292±0.154μg/ml and 0.323±0.217. These data suggest dose-dependency for fluoroquinolones.
    4) A pharmacokinetic analysis was performed in 28 patients given OFLX and in 25 given AM-833. Plasma and CSF concentration-time profiles of these agents were fitted to a one-compartment open model. The half-life in plasma was 3.9 h for OFLX and 9.0 h for AM-833. CSF levels peaked at 6 h for OFLX and 7 h for AM-833, and subsequently decreased gradually.
    These findings suggest that fluoroquinolones penetrated into CSF in patients who had never suffered from cerebrospinal disease.
    Download PDF (2348K)
  • HIDEYASU MATSUYAMA, NORIO YAMAMOTO, SATORU YOSHIHIRO, JISABURO SAKATOK ...
    1990 Volume 38 Issue 5 Pages 477-483
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    Ten patients with advanced bladder cancer (T 2-T 4) were treated by intra-arterial infusion, and the following pharmacokinetic parameters related to CDDP were studied:
    #1) the pharmacokinetic behavior of intravenous (i. v.) and intra-arterial (i. a.) CDDP administration.
    #2) the relationship between pharmacokinetic parameters (free Pt AUC) and clinical efficacy.
    #3) the relationship between intratumoral concentration of platinum (Pt) and clinical efficacy.
    Fifty to 120 mg/body of CDDP, 30 mg/body of ADM, and 20μg/body of angiotensin II were infused through both internal iliac arteries within 15 min and this protocol was repeated 1 to 3 times simultaneously with 30 Gy irradiation.
    There was good correlation between the free Pt AUC and i.a. administered CDDP dose/creatinine clearance (r=0.728), and an even higher correlation for i. v. administration (r=0.918).The relationship between free Pt AUC and clinical efficacy was not significant. However, intratumoral Pt concentrations in clinically effective cases were higher than in ineffective cases, the critical Pt concentration being 2μg/g (wet tissue).
    Intra-arterial CDDP infusion therapy has not only a regional, but also a systemic chemotherapeutic effect. It is noteworthly that the free Pt AUC was not significantly different for i. a. and i. v. administration.
    Download PDF (872K)
  • HARUO KUROKI, AKIRA NAKAMURA
    1990 Volume 38 Issue 5 Pages 484-488
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    A six year-old girl with complicated cyanotic heart disease and asplenia was affected by a brain abscess of the right temporal lobe. She was successfully treated with surgical aspiration followed by drainage and intravenous administration of imipenem/cilastatin sodium for five weeks.
    The offending pathogen isolated from the abscess was microaerophilic Streptococcus, for which the MIC of imipenem was 0.01μg/ml.
    We think it worthwhile to give imipenem/cilastatin sodium in the treatment of the central nervous system infections, including brain abscesses.
    Download PDF (4294K)
  • YOSHINOBU OHSAKI, SHINOBU OSANAI, YUJI AKIBA, SAKAE ISHIDA, HIROYUKI M ...
    1990 Volume 38 Issue 5 Pages 489-498
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    We used cefixime (CFIX) in the treatment of 65 patients with respiratory infections: 50 with acute respiratory infection, including 27 with bronchitis and 23 with pneumonia. The other 15 patients were considered to have chronic respiratory infections, including chronic bronchitis, bronchiectasis 4, bronchiolitis 1, and 6 cases of other lung diseases with secondary infection. CFIX in 100 mg capsules was administered orally. As a rule, the daily dose was 200 mg.
    The efficacy rate was 80.0% in the 50 patients with acute infections, and 60.0% in the 15 patients with chronic infections. CFIX showed satisfactory antibiotic activity in mild to moderate acute respiratory infections, for which 200 mg /day was an effective dose. On the other hand, the efficacy rate for the 200 mg /day dose was lower in chronic respiratory infections. Some additional therapy and/or 400 mg/day of CFIX should be given to patients with complicated respiratory infections. Side effects were observed in 6.1% of these patients, but none were serious. We consider CFIX to be a useful antibiotic in the treatment of respiratory infections.
    Download PDF (1294K)
  • 1990 Volume 38 Issue 5 Pages 499-526
    Published: May 25, 1990
    Released on J-STAGE: August 04, 2011
    JOURNAL FREE ACCESS
    Download PDF (5417K)
feedback
Top