The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 40, Issue 11
Displaying 1-11 of 11 articles from this issue
  • KOHEI HARA
    1987 Volume 40 Issue 11 Pages 1851-1860
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • YOSHIO KABE, HARUAKI OKAMURA
    1987 Volume 40 Issue 11 Pages 1861-1868
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Using 13 patients undergoing operation of the bile duct, cefmenoxime (CMX) transport into the bile and the gallbladder tissue was investigated.
    One gram of CMX was administered through drip infusion over 30 minutes every 12 hours. CMX concentration in bile was measured for samples surgically collected about 103 minutes (75-141 minutes) after the start of CMX administration.
    CMX concentrations in bile samples collected from gallbladder were found to be as high as326.6±432.3μg/ml in patients with neither jaundice nor cystic duct obstruction, indicating sufficient CMX transport. When cystic duct obstructions were present, CMX concentrations were very low, or moderately low if jaundice was also present.
    Changes in CMX concentration were then measured over 6 hours after administration in patients with an external biliary fistula every other day for a period of 7 days, from the first postoperation day. As for horal changes, CMX concentration reached its peak in 2 hours after the start of administration in most cases. Maximum CMX concentrations in patients without jaundice were high, ranging from 313.3 to 1,232.3μg/ml (mean, 641.2μg/ml), and CMX was found at 4.0-76.6μg/ml (mean, 37.4μg/ml), even after 6 hours. As for diurnal changes, CMX was determined to be sufficiently transported into the bile from the first postoperation day. Although CMX concentrations tended to be lower on the fifth postoperation day than on other days, there was no statistical significance in differences in daily concentrations examined.
    CMX concentrations in gallbladder tissues were determined to be 22.7±32.1μg/g, and they decreased over time exponentially.
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  • TAKASHI MOTOHIRO, KEIKO ODA, MASAFUMI ARAMAKI, AKIRA KAWAKAMI, KOICHI ...
    1987 Volume 40 Issue 11 Pages 1869-1880
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Norfloxacin (NFLX) a synthetic oral antibacterial agent of quinolone carboxylic acid, was given to 6 healthy men aged 23 to 29 years and weighing 57 to 88 kg (average 64.7 kg) at a dose of 200 mg (two 100 mg tablets) once after breakfast and its fecal and urinary recoveries were determined for 5 days after the administration. Fecal and urinary recoveries of NFLX or ciprofloxacin (CPFX) were examined under various experimental conditions where the drugs were added to the urine or feces. Effects of the drug on the clinical laboratory test parameters and side effects were also examined. The following results were obtained.
    1. NFLX reached the highest level in the feces in 5 cases in 24 hours and in 1 case in 48 hours; average peak fecal level was 137.1μg/g in 24 hours. Fecal recoveries were 2.32 to 36.90% in 5 days after dosing with an average of 13.83%.
    2. Urinary levels of the drug reached their peaks within 24 hours (average 51.46μg/ml) in all cases and then decreased. Urinary recoveries were 11.15 to 46.44% in 5 days after dosing.Both fecal and urinary levels of the drug varied greatly among the subjects.
    3. The sum of the fecal and the urinary recoveries in each case varied from 13.47 to 76.88% (average 42.24%).
    4. Since the sum of the fecal and the urinary recoveries was very low, the fecal recoveries were determined by additing NFLX to fecal samples at 0, 125,500 and 2,000μg/g and concentrations were assayed. Recoveries were as low as 48.7 to 57.8%. Therefore, the potential influence of the 2 procedures (mixing and homogenation) on the drug recoveries was examined. No difference between 2 procedures existed. When another drug of a similar type, CPFX, was added to the feces, its recovery was also low. Then, the drug residual levels were 89.0, 86.0 and 78.2% immediately after the addition of the drug to GAM broth and after incubation for 6 and for 18 hours at 35°, respectively. Slightly reduced recoveries were obtained with longer time of incubation. Remaining drug levels in feces were determined following the addition of the drug at 50μg/ml in the presence of 1010 cells/ml of Bacteroides fragilis, a common strain of the fecal flora, in 1.0 ml of the GAM broth and recoveries with time were examined against 0-time recovery rate which was defined as 100. Recovery rates were reduced to 85.8 and 74.4% after incubation for 6 hours and for 18 hours at 35°, respectively. It is considered that B. fragilis might affect the NFLX level in the feces through an unknown mechanism. In addition, NFLX recovery levels seem to change slightly dependent on the temperature.
    5. From the 6 cases, 2 cases where the drug recoveries were determined following the addition of the drug were excluded, and feces were collected before the administration of NFLX in the remaining 4 cases, and the drug was added by mixing at concentrations of 200 and 800μg/g. Recoveries of the drug were 50.0 to 56.5% upon the addition of 200μg/g and 52.4 to 61.6% upon the addition of 800μg/g. This low recovery rates might be partly due to the interference with B. fragilis and partly due to temperature-dependency.
    6. Abdominal pain and diarrhea occurred in 1 case following the administration of 200 mg.No abnormal result was noted in any case in clinical laboratory tests.
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  • TADAFUMI NISHIMURA, KAZUO TABUKI, TAKASHI MOTOHIRO, YASUSHI SHIMADA, N ...
    1987 Volume 40 Issue 11 Pages 1881-1890
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The authors administered cefotaxime to 20 children and studied laboratory paramaters concerning peripheral blood: hemoglobin count, blood platelet count, red blood cell count, and hematocrit value, and the coagulation system: protein induced by vitamin K deficiency or by the presence of a vitamin K antagonist II (PIVKA II), hepaplastin test (HPT), prothrombin time (PT) and active partial thromboplastin time (APTT).
    The results obtained are summarized as follows:
    1. Peripheral blood
    No abnormal values were observed.
    2. Coagulation system
    (1) PIVKA II: In all cases, PIVKA II was negative.
    (2) HPT, PT and APTT: In all cases, no significant changes of these values which would suggested the tendency for prolonged bleeding were observed.
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  • KIMIO FUJITA, MINORU KAWAMURA, TAKEO MURAYAMA
    1987 Volume 40 Issue 11 Pages 1891-1894
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fosfomycin (FOM) is an antibiotic which inhibits phospho (enol) pyruvic acid transferase.
    Fifty-five patients with cystitis were treated with the drug for 7 days, at oral doses of 1 g for 3 times a day. Adult females under 70 years of age, visiting the clinic within 2 weeks after the onset, were classified as cases with typical simple cystitis with confirming the bladder irritability, pyuria and bacteriuria. The treatment was effective for 95.0% of these cases. Two cases with atypical cystitis caused by Klebsiella pneumoniae poorly responded to the drug.
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  • KOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUTAKA NAKANE, SHIGEMI ...
    1987 Volume 40 Issue 11 Pages 1895-1905
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Antimicrobial activities of sisomicin (SISO) against clinical isolates obtained in the second half of 1986 were investigated together with other 4 aminoglycosides (AGs)(gentamicin (GM), tobramycin (TOB), dibekacin (DKB), amikacin (AMK)) and 2 cephems (cefotiam, cefotaxime), and were compared to the results reported in the period of late 1970's through early 1980's in Japan.
    1. The incidence of SISO-resistant Staphylococcus aureus in the present study was 18% and is comparable to that of the other studies suggesting that the incidence of SISO resistant strains remains on the stable level. The incidence of SISO-resistant Pseudomonas aeruginosa showed the tendency of slight increase.
    2. SISO-resistant strains of Enterobacter spp., Serratia marcescens and Citrobacter freundii did not show increase from the 1970/1980 levels.
    3. Isolation rates of SISO-resistant indole (+) Proteus varied depending on strains. Isolation rates of SISO-resistant P. vulgaris and Morganella morganii were both as low as 4%, but that of Providencia rettgeri was as high as 60%. Refering to an American study reporting that the Genus Providencia including P. rettgeri showed high incidence of resistance to SISO as well as to GM or TOB, we pointed out that the antimicrobial activity of AGs against Genus Providencia should be evaluated separately from those of other indole (+) Proteus strains.
    4. No SISO-resistant strains of Escherichia coli, Klebsiella pneumoniae or P. mirabilis were found.
    5. SISO had good antimicrobial activity against most of the investigated species and SISO may still be regarded as one of the clinically useful AGs.
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  • SIGNIFICANCE OF 4 CATEGORY SYSTEM INTERPRETATION OF LATAMOXEF DISC SUSCEPTIBILITY TEST
    TETSUO UETE, KIYOMITSU MATSUO
    1987 Volume 40 Issue 11 Pages 1906-1916
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In vitro activities of latamoxef (LMOX) against 249 clinical isolates were determined using the agar dilution method at an inoculum level of 106 CFU/ml. LMOX was highly active against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis (except 2 out of 30 strains) and Proteus vulgaris with MIC values below 3.13μg/ml. It was also active against Enterobacter aerogenes with MIC80 of 1.56μg/ml. LMOX was less active against Serratia marcescens, inhibiting about 43% of strains at a level of 6.25μg/ml. It was also less active against Staphylococcus aureus and Staphylococcus epidermidis, showing MIC80 of 12.5 and 50μg/ml, respectively. LMOX was not active against Enterococcus faecalis and Pseudomonas aeruginosa.
    The reliability of the LMOX disc diffusion susceptibility test for quantitative estimation of antimicrobial activities was also investigated using 8 mm diameter discs (Showa) and 6 mm diameter discs (Difco), both of which contained 30μg/disc of LMOX. These disc susceptibility test results were well correlated with MICs, hence the LMOX disc susceptibility test should be useful for the estimation of proper dose levels of LMOX.
    For the interpretation of LMOX disc test results, if uniform break points of zone diameters were used to test all bacteria, inhibitory zone diameters of Showa discs used on Staphylococcus were relatively large compared to MICs determined, probably due to decarboxylation of LMOX sodium salt in the discs. However, those of Difco discs were not, because Difco discs use LMOX ammonium salt. Both discs also showed relatively large inhibitory zone diameters compared to MICs determined against P. aeruginosa. Using different break points from those used for other bacteria to interpret inhibition zones for Staphylococcus and P. aeruginosa, these disc susceptivility tests should be useful to estimate approximate MICs.
    A 3 category system for the interpretation of disc test results has been used in USA and Europe, but a 4 category system is generally used in Japan. The 3 category system uses break points to classify bacteria into 3 categories of susceptibility according to MIC values as follows: Resistant (R) MIC≥64μg/ml, intermediate (I) MIC 16-32μg/ml, and susceptible (S) MIC≤8μg/ml. The 4 category system uses break points as follows: (+++) MIC≤3μg/ml,(++) MIC≤3-15μg/ml,(+) MIC≥15-60μg/ml,(-) MIC≥60μg/ml.
    Based on pharmacokinetic data on LMOX and the recommended modest dose schedule (2-4 g/day), MIC break points of 3μg/ml and 15μg/ml appear to be more useful than break point of 8μg/ml, for the evaluation of the blood levels of LMOX how many times greater than the MICs.
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  • KAZUO TAKEBE, TOYOICHI TAMURA, KATSUMI ENDO, TATSURO IRIE, KEIICHI SEK ...
    1987 Volume 40 Issue 11 Pages 1917-1922
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    To evaluate the clinical efficacy of carumonam (CRMN, AMA-1080), the drug was used in the treatment of 10 patients including 4 with pneumonia and each with acute tonsillitis, chronic bronchitis, Mycoplasma pneumonia, primary atypical pneumonia (PAP), chronic pyelitis, and acute cystitis. Since β-lactam antibiotics were not active against Mycoplasma pneumonia and PAP, these diseases were excluded from the clinical efficacy evaluation of CRMN. Responses were excellent in 1 patient and good in 7.
    Side effects were not observed. The laboratory test recognized slight elevations of GOT, GPT and eosinophilia in 1 patient and a slight leucopenia in another upon the administration of CRMN.
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  • TETSUO MIURA, IKUO HASHIMOTO, YASUO SAWADA, TAKASHI NAKAMURA, MASAKI N ...
    1987 Volume 40 Issue 11 Pages 1923-1936
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefmetazole (CMZ), with its relatively broad antibacterial spectrum, good stability to /3-lactamases and a high degree of safety, has established a place in the antibacterial therapy.
    In this study the pharmacokinetics of CMZ during and after surgical operations were investigated. CMZ in a dose of 2 g was administered intravenously to 15 cases operated upon for ailments of abdominal organs (10 cases of cholecystolithiasis and 5 cases of early or resectable gastric cancer). The serum samples were taken during and on the 2nd or the 3rd day after operation. Concentrations of CMZ in serum were measured by bioassay with Micrococcus luteus ATCC 9341 and by a high performance liquid chromatography (HPLC) method.
    CMZ concentrations during the operation was at higher level than on the 2nd or the 3rd day after the operation. In cholecystolithiasis, the half-life time (T 1/2) was 2.11 hours during operation and 1.42 hours after the operation. In cases of gastric cancer, T 1/2 was 1.31 hours during operation and 2.21 hours after the operation.
    In cholecystolithiasis, area under the curves (AUCs) were 469.39μg·hr/ml during operation and 294.44μg·/hr/ml after the operation. In cancer cases, AUC's were 339.83μg·hr/ml during and 329.75μg·/hr/ml after operation. Any postoperative infections and adverse reactions were not observed in these cases.
    Therefore, CMZ would be very effective and available for its prophylactic role.
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  • HISASHI AOYAMA, HIROKO SUGIYAMA, TORU ISHII, TATSUKI KAWAUCHI, TAKANOB ...
    1987 Volume 40 Issue 11 Pages 1937-1940
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    After oral administration of 300 mg of ofloxacin (OFLX), the concentration of OFLX in serum peaked at 2 hours and reached 2.88±0.62μg/ml (mean±S.D.). In the fluid of dermal blisters produced by suction, the peak value was 1.74±0.88μg/ml at 4 hours. Pharmacokinetically, Cmax (maximum concentration), Tmax (time of maximum concentration), Ka (absorption rate constant) and AUC0-8hrs.(area under the concentration-time curve) were calculated as 2.65μg/ml, 2.07 hours, 0.79 hr-1 and 14.5μg·hr/ml in serum, and 1.59μg/ml, 4.49 hours, 0.27 hr-1 and 10.1μg·hr/ml, respectively. Therapeutic AUC (area under the curve above minimum effective concentration) were also calculated as 13.3μg·hr/ml (0.14-12.4 hours) in serum, and 11.5μg·hr/ml (0.42-17.3 hours).
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  • KOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUTAKA NAKANE, SHIGEMI ...
    1987 Volume 40 Issue 11 Pages 1941-1945
    Published: 1987
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Methicillin-resistant Staphylococcus aureus (MRSA) were isolated from samples collected from various patients during 1986, and antibacterial activities of 6 aminoglycosides (AGs)(netilmicin (NTL), gentamicin (GM), sisomicin (SISO), dibekacin (DKB), tobramycin (TOB) and amikacin (AMK)) and 4 β-lactam antibiotics (cefazolin (CEZ), cefmetazole (CMZ), cloxacillin (MCIPC) and methicillin (DMPPC)) against these MRSA were evaluated.
    Among these 6 AGs, NTL was the most potent, and its MIC50 and MIC80 were 1.56 and 3.13μg/ml, respectively. Antibacterial activities of GM, SISO, DKB and TOB were weak, and MIC50's of GM and DKB were both 100μg/ml, while those of SISO and TOB were 50 and>100 μg/ml, respectively. Frequency of highly resistant specimens to AMK was rather low and its MIC50 and MIC80 were 12.5 and 25μg/ml, respectively.
    As for antibacterial activities of the above 4 β-lactam antibiotics, the MIC50 and MIC80 of CMZ were 6.25 and 12.5μg/ml, respectively, and therefore, its antibacterial activity to MRSA is relatively good. However, MIC50´s of CEZ, MCIPC and DMPPC were all>100μg/ml, showing poor antibacterial activities.
    Recently, MRSA became a problem in various fields of clinical practice, and a number of literatures reporting refractory infections caused by MRSA have been published 1-5). Since MRSA is featured as multiply resistant bacteria 6), it is known that MRSA is resistant to the majority of existing antibiotics (penicillins, cephems, macrolides, AGs, etc.).
    In 1985, we reported results of our study concerning the antibacterial activities of a number of CEPs and some of AGs against multiply resistant S. aureus including MRSA6). Antibacterial activities mainly of AGs against MRSA freshly isolated from clinical samples have been evaluated in the present study.
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