The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 47, Issue 1
Displaying 1-10 of 10 articles from this issue
  • MASASHI NIIDA, TAKASHI YOSHIDA, AKIRA KOHMOTO, MASATOSHI OGAWA, HAJIME ...
    1994 Volume 47 Issue 1 Pages 1-10
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We studied the combined effect of fosfomycin (FOM) with sulbactam/cefoperazone (SBT/CPZ) on clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA, 246 strains) and Pseudomonas aeruginosa (190 strains) in vitro.
    In ratio of mixed serum concentration of antibiotics at three hours after intravenous administration, the combination of FOM with SBT/CPZ and alone of arbekacin showed over 90% in cumulative percentage of MIC against MRSA and P. aeruginosa. The effect of the combination of FOM and SBT/CPZ was observed in MRSA strains of >16μg/ml of SBT/CPZ MIC and >256μg/ml FOM MIC.
    As well as in P. aeruginosa strains, the effect of the combination of FOM and SBT/CPZ was observed in strains of >16μg/ml of SBT/CPZ MIC and <256μg/ml FOM MIC, but it was not remarkable in strains of >256μg/ml FOM MIC. These results suggests that the combination treatment of FOM and SBT/CPZ may be effective for mixed infection of MRSA and P. aeruginosa.
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  • β-Lactamase Study Group in Chubu-area
    YASUHISA ITO, MINORU KANEMATSU, JIRO YURA, KAZUE UENO, KUNITOMO WATANA ...
    1994 Volume 47 Issue 1 Pages 11-21
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Antimicrobial susceptibilities and β-lactamase production of clinical isolates from 1986 to 1991 except 1988 were determined.
    β-Lactamase was detected frequently in Escherichia coli (84.7%), Klebsiella pneumoniae (65.4%), Staphylococcus aureus (62.3%), and not frequently in Haemophilus influenzae (22.4%).
    Methicillin-resistant S. aureus was also resistant to many antimicrobials except to arbekacin and minocycline, and imipenem showed markedly high activity against methicillin-sensitive S. aureus.
    Susceptibilities of E. coli and K. pneumoniae to cefuzonam, imipenem and ofloxacin were quite high and that of H. influenzae to ofloxacin and cefuzonam was also very high.
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  • YOSHIKAZU ISHII, AKIRA OHNO, KEIZO YAMAGUCHI
    1994 Volume 47 Issue 1 Pages 22-28
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In vitro activities of broad-spectrum quinolones (sparfloxacin (SPFX), ciprofloxacin (CPFX), lomefloxacin (LFLX), fleroxacin (FLRX), and levofloxacin (LVFX) were examined against clinical bacterial isolates: Klebsiella pneumoniae, Haemophilus influenzae, Moraxella subgenus Branhamella catarrhalis, Methicillin-sensitive Staphylococcus aureus (MSSA), Methicillin-resistant Staphylococcus aureus (MRSA), Enterococcus faecalis, Enterococcus faecium, and Streptococcus pneumoniae). Antibacterial activities of SPFX, CPFX, and LVFX against Gram-negative bacteria such as K. pneumoniae, M.(B) catarrhalis and H. influenzae were better than those of FLRX and LFLX. SPFX showed the highest activity against all Gram-positive bacteria tested in this study. However, strains showed high MIC (≥16μg/ml) to SPFX were found among MRSA, E. faecalis, and E. faecium, whose isolation frequencies were 28.6%, 10.0%, and 6.7%, respectively. The results of this study suggest that resistant strains of Gram-positive bacteria against new quinolone might increase among clinical isolates.
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  • IZUMI HAYASHI, MASANORI SAKURAI, MASAO ICHIKI, IMAO SEKINE, KOUNOSUKE ...
    1994 Volume 47 Issue 1 Pages 29-39
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pseudomonas aeruginosa has been a major bacterial partner when MRSA (Methicillin-resistant Staphylococcus aureus) is isolated clinically. Hence, we studied the in vitro combined effect of fosfomycin (FOM) plus sulbactam/cefoperazone (SBT/CPZ) against mixed infections of MRSA and P. aeruginosa.
    The combined effect of FOM plus SBT/CPZ was observed through an FIC index using the checkerboard method, log reduction of colony counts on the time killing curve, and morphological cahnges observed using sacanning electron micrography. Under serum concentration at 3 hours after administration in consider of pharmacokinetics, the combination effect was also evaluated.
    Furthermore, we evaluated a time-lag combination therapy in which FOM is administerd 60 minutes before SBT/CPZ administration for mixed infections.
    Synergistic effects of FOM plus SBT/CPZ were clearly observed against mixed infections of MRSA and P. aeruginosa. Log reduction of colony counts on the time killing curve seemed to be an appropriate indicator in the evaluation of synergistic effects.
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  • TOSHIO ITOYAMA, YUKIYO AOKI, TAMIO HIRATANI, KATSUHISA UCHIDA, HIDEYO ...
    1994 Volume 47 Issue 1 Pages 40-49
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Effects of various factors on in vitro antifungal activities of omoconazole nitrate (OMZ) were investigated with bifonazole (BFZ) as the reference drug using an agar dilution method and a broth dilution method. Composition of the culture medium significantly altered the activity as determined by minimum inhibitory concentration (MIC) of OMZ; OMZ exhibited a greater anti-Candida activity (smaller MIC values) on casitone agar (CA) than on Sabouraud dextrose agar (SDA). Anti-Candida activity of OMZ was the highest in pH 5 medium, but it was lowered by an increase of inoculum size, a prolongation of the incubation period and the addition of calf serum to the medium. Anti-Trichophyton activity of OMZ was not influenced with these factors except for the addition of calf serum. The activity of OMZ was fungicidal against Candida at pH 5.0 and against Trichophyton at pH 5.0 and 6.6. The geometric mean MIC of OMZ was lower than that of BFZ against C. albicans freshly-isolated on acid CA.
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  • KATSUHISA UCHIDA, HIDEYO YAMAGUCHI
    1994 Volume 47 Issue 1 Pages 50-56
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Prophylactic effect was studies of a novel oral antifungal agent terbinafine (TBF) on the development of local infection in guinea pigs after inoculation of Trichophyton mentagrophytes. TBF was administered orally in a single dose of 6.25 or 12.5mg/kg, 8, 24, 48 or 72 hrs before the inoculation, and the drug effect was assessed on the basis of local symptoms and culture study. The result of experiments demonstrated that oral TBF more or less prevented the development of the dermatophytic infection, depending on the dosage and the timing of administration, the complete prevention was achieved in the animals that were administered with 12.5mg/kg of TBF 24 hrs prior to the inoculation of T. mentagrophytes. This suggests a good transferability and intracutaneous retaining of orally administered TBF.
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  • RYOCHI FUJII, KOUZOU FUJITA, YOHKO SAKATA, TOSHIAKI ABE, TAKESHI TAJIM ...
    1994 Volume 47 Issue 1 Pages 57-83
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • HIROMI TAKEUCHI, HISAAKI IKOMA, TAKEO SUZUKI, MIKIO NAKAJIMA, YUUJI KO ...
    1994 Volume 47 Issue 1 Pages 84-92
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In this study, we evaluated the clinical efficacy of cefpodoxime proxetil (CPDX-PR) in otorhinolaryngological infections.
    The subjects were 205 patients (85 men and 120 women) with various otorhinolaryngological infections, aged from 16 to 81 years (mean 49.2 years): 113 patients had acute infections, 25 patients had chronic infections and 67 patients had acute exacerbation of chronic infections.
    1. Clinical evaluation
    The overall efficacy rate was 75.6%. When classified by disease, the efficacy rate was 84.9%, 60.0%, 65.6% in acute infections, chronic infections and acute exacerbation of chronic infections, respectively.
    2. Bacteriological evaluation
    Frequencies of isolation of different organisms were studied: 49 strains of Staphylococcus aureus, 27 strains of Staphylococcus sp. and 15 strains of Streptococcus sp. were found in the decreasing order of frequencies.
    Antibacterial activities against S. aureus, Staphylococcus sp. and several other organisms were compared among CPDX-PR, ampicillin, cefaclor, cefteram and norfloxacin: CPDX-PR showed the highest activity.
    3. Side effect
    Mild urticaria was observed in only 1 patient. Abnormal laboratory test results were mild elevation of GOT and GPT in 3 of 43 patients.
    Based on the above results, we consider that CPDX-PR is useful for treatment of otorhinolaryngological infections.
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  • HIDEMITSU NAKAGAWA, MASANOBU YAMADA, KOJI TOKIYOSHI, YOJI MIYAWAKI, TA ...
    1994 Volume 47 Issue 1 Pages 93-101
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Concentrations of potassium clavulanate (CVA) and ticarcillin sodium (TIPC) in the plasma and cerebrospinal fluid (CSF) of patients after neurosurgical intervention were determined at various times after a 1-hour drip infusion (3.2-g dose). Patients whose blood-brain barriers were supposed to be maintained in almost a normal condition were selected. CSF was obtained through a catheter placed in the anterior horn of the lateral ventricle in all the patients. Maximum plasma levels (μg/ml) of 57.6 to 384.0 with an average of 169.7 (TIPC) and 0.41 to 26.2 with an average of 6.1 (CVA) were achieved at the termination of infusion. The maximum CSF levels (μg/ml) were 0.61 to 18.8 (TIPC) and 0.1 to 6.81 (CVA) with mean values of 4.5 and 1.2, respectively. Plasma half lives (T1/2)(minute) were 24 to 93 (TIPC) and 32 to 227 with mean values of 58 and 127, respectively. The mean values of the CSF half lives (minute) were 237 (TIPC) and 113 (CVA). The ratios (%) of CSF levels to plasma levels in maximum concentration (Cmax), AUC (area under concentraiton curve) and half life (T1/2) were calculated.Cmax ratios were 0.2 to 29.2 (TIPC) and 1.4 to 69.8 (CVA) with mean values of 4.4 and 22.8, respectively. AUC ratios were 0.3 to 23.5 (TIPC) and 1.1 to 70.2 (CVA) with mean values of 4.3 and 22.4, respectively. T1/2 ratios were 1.3 to 18 (TIPC) and 1.1 to 4.3 (CVA) with mean values of 5.5 and 2.3, respectively. These values indicate that CVA/TIPC may be classfied into a group of antibiotics with good penetration into the CSF.
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  • RYOCHI FUJII, TOSHIAKI ABE, TSUYOSHI TAJIMA, ITARU TERASHIMA, HIDENORI ...
    1994 Volume 47 Issue 1 Pages 102-123
    Published: January 25, 1994
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We investigated pharmacokinetics and clinical effectiveness of a newly developed cephem antibiotic cefozopran (SCE-2787, CZOP) against various pediatric infections in 18 institutions and their affiliates. We obtained the following results.
    1. Serum concentration and urinary excretion rates
    Pharmacokinetics of CZOP in children was examined after intravenous injection and 30-minute drip infusion of 10, 20 and 40mg/kg of CZOP. Peak serum concentrations of CZOP in 30 minutes after intravenous injection were 21.7, 51.5 and 77.8μg/ml, respectively, showing a clear dose response. Half-lives were 1.99, 1.85 and 1.67 hours, respectively. In the first 6 hours after administration, urinary excretion rates of CZOP were 87.3, 67.4 and 84.1%, respectively.
    In the cases of 10, 20 and 40mg/kg administration of CZOP 30-minute drip infusion, peak serum concentration of CZOP in 30 minutes, when the infusion was completed, were 38.1, 72.8 and 95.6μg/ml, respectively. Again, there was a clear dose response. Half-lives were 1.67, 1.69 and 1.43 hours, respectively. In the first 6 hours after administration, urinary excretion rates of CZOP were 53.9, 59.7 and 77.3%, respectively.
    Cerebrospinal fluid concentrations of CZOP administered by intravenous injection of 50mg/kg to patients with purulent meningitis were 1.6 to 43.4μg/ml in 1 to 1.5 hours after administration.
    2. Clinical study
    Clinical efficacy was evaluated in 337 cases. The largest number of cases, 138 cases, were found in 2 to <6-year olds. The majority of the patients were under age 9, and 70 cases were of less than 1-year old infants. 183 cases were males and 154 cases were females. In terms of illness, a majority, or 185 cases, suffered from pneumonia, followed by 39 cases of UTI and 23 infections of the skin and soft tissue. There were 7 cases of purulent meningitis. In 218 cases, CZOP was administered at a daily dose of 60-<80mg/kg. The drug was administered for 6-10 days, the most frequent duration, in 188 cases.
    In the cases where causative organisms were identified (group A), the efficacy rates (“excellent” and “good”) obtained were 100%(5/5) against purulent meningitis, 100%(2/2) against sepsis, 98.3%(119/121) against pneumonia, 100%(13/13) against acute bronchitis, 100%(11/11) against upper respiratory tract infection, 96.3%(26/27) against UTI. Overall,“excellent” and “good” responses were observed in 97.5%(197/202) of cases with known causative organisms.
    In the cases in whom causative organisms were not identified (group B), the efficacy rates were 98.4%(63/64) against pneumonia, 100%(9/9) against acute bronchitis, 50%(3/6) against upper respiratory tract infection, 100%(12/12) against UTI, 92.9%(13/14) against purulent lymphadenitis, 100%(17/17) against skin and soft tissue infection, 100%(2/2) against purulent meningitis and 50%(1/2) against suspected sepsis. The overall efficacy rate was 95.6%(129/135) for all the cases where causative organisms were not identified.
    Especially, the efficacy rates for “excellent” were very high, and they were 74.3%(150/202) for group A, 55.6%(75/135) for group B.
    The efficacy rate was 97.0%(258/266) for the group given a daily dose of 40-80mg/kg (t. i. d.).
    Bacteriologically, 77 Gram-positive strains (96.3%) out of 80 strains as well as 155 Gramnegative strains (94.5%) out of 164 strains were eradicated. Thus out of the 244 strains of known causative bacteria, 232 strains (95.2%) were eradicated. In 93 cases where more than 3 days of previous treatment resulted in “poor” efficacy, CZOP showed “excellent” or “good” responses in 90 cases (96.8%). Bacteriologically, 24 Gram-positive strains (96.0%) were eradicated out of the 25 strains on which previous treatment was not effective. Moreover, out of the 57 Gram-negative strains, 53 strains (93.0%) were eradicated.
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