CHEMOTHERAPY
Online ISSN : 1884-5894
Print ISSN : 0009-3165
ISSN-L : 0009-3165
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Volume 37, Issue 9
Displaying 1-10 of 10 articles from this issue
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  • DISTRIBUTION OF T-3262 (TOSUFLOXACIN TOSILATE) IN PROSTATIC TISSUE
    SHIGERU IKEDA, KIYOSHI NISHIMURA, AKIRA ISHIBASHI
    1989 Volume 37 Issue 9 Pages 1149-1153
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1149
    JOURNAL FREE ACCESS
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    We investigated the distribution and metabolism of T-3262 (tosufloxacin tosilate) in the rat prostate, coagulating ducts and seminal vesicles by microautoradiography.
    After administration of 14C-T-3262, the ventral prostate, coagulating ducts and seminal vesicles were removed, frozen immediately in hexan and dry ice, and sectioned in cryostat in 4 μm sections. The sections were then placed on to slides which were precoated with emulsion, in a dark room. After 3 weeks' exposure, development and fixation was done in the usual manner. The samples were stained with hematoxyline and eosine.
    The results of the present study indicate that 14C-T-3262 was distributed in the connective, interstitial and follicular tissues.
    From this study, T-3262 seems to be an effective agent against bacterial prostatitis.
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  • A NEW DNA GYRASE INHIBITOR INDUCES CONVULSIONS
    A CASE REPORT AND ANIMAL EXPERIMENTS
    GOU TAKEO, NORITOSHI SHIBUYA, MASAKATSU MOTOMURA, HAJIME KANAZAWA, HAR ...
    1989 Volume 37 Issue 9 Pages 1154-1159
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1154
    JOURNAL FREE ACCESS
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    A 64-year-old woman taking a 5-day course of 300mg/day of enoxacin (ENX) and fenbufen (FBF) for acute cystitis had a generalized convulsion and loss of consciousness. There was no past history suggestive of epileptic seizure. During the first 2 hours after admission, she had three episodes of concurrent generalized tonic seizure and irritability. Four hours after admission, she regained consciousness, at which time the neurological findings were normal except for hyperreflexia. No abnormality was found in brain CT scan, EEG and ECG. Laboratory findings revealed mild leucocytosis and an abnormal increase in CK. The CK level rose to 17, 712 IU/L on the 4th hospital day and normalized on the 13th hospital day. The CK isozyme showed 100% MM fraction. Needle EMG and muscle biopsy showed no abnormalities.
    We carried out an animal experiment to examine convulsion in relation to new quinolone antimicrobial agents and FBF. We found that convulsions were induced in mice not only by ENX but also by ciprofloxacin when administered together with FBF.
    On the other hand, ofloxacin together with FBF did not induce convulsions. Anti-convulsive agents such as valproic acid, GABOB, PG-E2, phenobarbiturate and diazepam failed to prevent these convulsions.
    We suggest that ENX may cause convulsions by affecting the GABA receptor·Cl- ionophore complex.
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  • BACTERIOLOGICAL EVALUATION OF OPC-7251, A NEW PYRIDONE CARBOXYLIC ACID ANTIMICROBIAL AGENT
    1. IN VITRO ANTIBACTERIAL ACTIVITY
    SHIGEKATSU KAWABATA, KINUE OHGURO, FUMIE MUKAI, KAZUNORI OHMORI, HISAS ...
    1989 Volume 37 Issue 9 Pages 1160-1178
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1160
    JOURNAL FREE ACCESS
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    The antibacterial activity of OPC-7251 was compared with that of tetracycline (TC), erythromycin (EM), clindamycin (CLDM), gentamicin (GM), norfloxacin (NFLX), ofloxacin (OFLX) and enoxacin (ENX). The results were as follows:
    (1) OPC-7251 had a potent and broad spectrum of antibacterial activity against aerobic Grampositive, aerobic Gram-negative and anaerobic bacteria.
    (2) OPC-7251 had potent antibacterial activity against clinically isolated strains of Propionibacterium acnes and Staphylococcus epidermidis, which are known as exogenous factors inacne vulgaris.
    OPC-7251 also had potent antibacterial activity against clinically isolated strains of Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa.
    (3) The antibacterial activity of OPC-7251 was augmented in an acidic medium and was little influenced by the inoculum size.
    (4) The mode of antibacterial action of OPC-7251 was bactericidal.
    (5) The incidence of bacterial strains which developed spontaneous resistance to OPC-7251 was low. OPC-7251 did not cause cross-resistance to NFLX, OFLX and ENX.
    We therefore anticipate that OPC-7251 will show clinical efficacy in acne vulgaris and other skin infections.
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  • BACTERIOLOGICAL EVALUATION OF OPC-7251, A NEW PYRIDONE CARBOXYLIC ACID ANTIMICROBIAL AGENT
    2. THERAPEUTIC EFFECT OF OPC-7251 CREAM ON EXPERIMENTAL INFECTION MODEL IN MICE
    SHIGEKATSU KAWABATA, HIROSHI MASADA, HIROKAZU WAKEBE, KAZUNORI OHMORI, ...
    1989 Volume 37 Issue 9 Pages 1179-1183
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1179
    JOURNAL FREE ACCESS
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    We evaluated the antibacterial activity of OPC-7251, a new synthetic antibacterial agent for topical use, using an experimental mouse model of infection subcutaneously induced with Propionibacterium acnes, Staphylococcus epidermidis and Staphylococcus aureus, and an experimental Pseudomonas aeruginosa burn wound infection model in mice.
    (1) 0.25%, 0.5% and 1% OPC-7251 cream showed potent and concentration-dependent antimicrobial activity in the experimental P.acnes subcutaneous infection in mice. In particular, the 1% cream was more active than 1% EM ointment used as a reference.
    2) 0.25%, 0.5% and 1% OPC-7251 cream showed more potent antimicrobial activity than 1% EM ointment in the experimental S.epidermidis subcutaneous infection in mice.
    (3) 0.5% and 1% OPC-7251 cream showed more potent antimicrobial activity than 2% FA ointment and 1% EM ointment in the experimental S.aureus subcutaneous infection in mice.
    (4) 0.25%, 0.5% and 1% OPC-7251 cream showed potent antimicrobial activity in the experimental P.aeruginosa burn wound infection in mice. In contrast, 0.1% GM ointment and 1% silver sulfadiazine cream did not show any definite antimicrobial activity.
    We therefore anticipate thet OPC-7251 cream will show efficacy in treating acne vulgaris and other skin infections.
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  • ANTIBACTERIAL SUBSTANCES IN AMNIOTIC FLUID
    TETSURO CHIMURA, NOBUYUKI MORISAKI
    1989 Volume 37 Issue 9 Pages 1184-1188
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1184
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    Antibacterial and related substances in amniotic fluid were determined using amniotic fluid samples obtained from 19 infection-free pregnant women between weeks 26 and 42 of pregnancy.
    1) The following substances increased as pregnancy progressed:
    Lysozyme [y=x/(92.68-0.305 x), γ=0.907]
    Transferrin [y=x/(57.87-0.170 x), γ=0.893]
    IgG [y=2.08×10-9x0.45769, γ=0.921]
    C3 [y=x/(328.65-0.771 x), γ=0.719]
    2) The following substances were not correlated with the progression of pregnancy: elastase, C4, C5, Fe, Zn and α1-antitrypsin. Elastase, Zn and α1-antitrypsin showed concentrations of 62.22±11.5, 18.0±6.13 and <45μg/dl, respectively, at the end of pregnancy. The concentration of nine amino acids in amniotic fluid was lower than in blood obtained from normal subjects.
    Thus, some antibacterial substances were found to increase in the amniotic fluid with the progression of pregnancy. These substances appear to be closely related with fetal development and metabolism and play major roles in the prevention of infections.
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  • ANTIBACTERIAL ACTIVITY OF AMNIOTIC FLUID AND ITS EFFECTS ON ANTIBACTERIAL ACTIVITY OF CEFUZONAM AND LYSOZYME
    TETSURO CHIMURA, NOBUYUKI MORISAKI, CHOICHIRO TAKAHASHI
    1989 Volume 37 Issue 9 Pages 1189-1194
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1189
    JOURNAL FREE ACCESS
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    The antibacterial activity and/or synergistic effects of amniotic fluid alone, amniotic fluid+cefuzonam (CZON) and amniotic fluid+CZON+lysozyme on clinical isolates of the following three organisms were evaluated: Staphylococcus aureus, Escherichia coli and Streptococcus agalactiae. The amniotic fluid was obtained from 20 pregnant women with no infection between weeks 26 and 42 of pregnancy.
    1) Only 2 of the 20 amniotic fluid samples (10%) showed antibacterial activity against the three organisms when used alone.
    2) CZON and amniotic fluid showed no synergistic effect on E.coli, while bacteriostatic activity was noted against S.aureus for 4 and 8 hours, respectively, when the drug was used in combination with heat-treated and untreated amniotic fluid.
    3) The MIC of CZON remained unchanged upon addition of untreated amniotic fluid with respect to E.coli, while it decreased (by one dilution) with respect to S.agalactiae (2/20 samples or 10%) and S.aureus (7/20 samples or 35%). The MIC of CZON increased (by one dilution) withrespect to E.coli upon addition of heat-treated amniotic fluid (2/20 samples or 10%).
    4) The MIC decreased with respect to the three organisms in some amniotic samples when lysozyme was added to mixtures of CZON and untreated amniotic fluid. However, lysozyme had no effect on heat-treated amniotic fluid.
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  • EFFECT OF ANTIBIOTIC ADMINISTRATION ON CHEMILUMINESCENCE AND ADHERENCE OF HUMAN NEUTROPHILS
    YOKO FUKASE, YOSHIHIRO ABE, TSUNEO TAKAHASHI, MAKOTO ISHIKAWA
    1989 Volume 37 Issue 9 Pages 1195-1199
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1195
    JOURNAL FREE ACCESS
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    We evaluated the effect of cefpimizole sodium (CPIZ) on neutrophil functions, such as adherence activity and luminol-dependent chemiluminescence, in 5 cancer patients given CPIZ to prevent infection after angiography.
    1) Before administration of CPIZ, adherence activity and chemiluminescence of neutrophils were suppressed in all the cancer patients compared with healthy controls.
    2) After administration of CPIZ for 3 or 4 days, the chemiluminescence of neutrophils in 2 patients increased remarkably to the level of healthy controls and that in 3 patients wasenhanced slightly.
    3) Adherence activity of neutrophils also increased moderately in 3 patients after administration of CPIZ.
    These results suggest that CPIZ has the effect of augmenting neutrophil functions.
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  • PHARMACOKINETICS OF BILIARY EXCRETION TYPE ANTIBIOTIC (CEFOPERAZONE) IN ELDERLY PATIENTS
    TAKASHI INAMATSU, MAKIKO FUKAYAMA, AKIHIKO KATOU, MASANORI NISHINAGA
    1989 Volume 37 Issue 9 Pages 1200-1204
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1200
    JOURNAL FREE ACCESS
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    Pharmacokinetics of cefoperazone (CPZ) in 7 elderly patients (mean age, 76. 4 years) without renal or hepatic disorders were compared with those in 6 younger healthy volunteers. The half-life of the beta-phase was 3.1 h in the elderly group after intravenous injection of 1g of CPZ, 1.6 times longer than in the younger group. The AUC in the elderly group was larger than in the younger. The volume of distribution (Vd), total clearance, renal clearance and non-renal clearance were smaller than those of the younger group.
    The 15 min retention rate of indocyanine green (ICGR15') was examined in 27 elderly persons without apparent renal or hepatic disorders. Evaluation of ICGR classified by age revealed that ICGR15' was 12.1% in the elderly group above 80 years old and was slightly larger than in the other group. These results suggest that a slight disorder of the drug excretion mechanism existed in the elderly group.
    Generally, the prolongation of the half-life of biliary excretion type antibiotics is less pronounced than that of urinary excretion type antibiotics in elderly patients. However, when compared with younger patients with renal disturbance, drug elimination in the elderly patients was impaired by both routes of biliary and urinary excretion.
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  • [title in Japanese]
    1989 Volume 37 Issue 9 Pages 1205-1218
    Published: September 25, 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.1205
    JOURNAL FREE ACCESS
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  • Errata
    1989 Volume 37 Issue 9 Pages 1227
    Published: 1989
    Released on J-STAGE: August 04, 2011
    DOIhttps://doi.org/10.11250/chemotherapy1953.37.9_1227
    JOURNAL FREE ACCESS
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