The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 32, Issue 2
Displaying 1-17 of 17 articles from this issue
  • I. TERATOGENICITY TEST
    TAKEMI KOEDA, MASAHIDE MORIGUCHI
    1979 Volume 32 Issue 2 Pages 155-163
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The teratogenicity study of fosfomycin-Na(FOM-Na)was undertaken in Wistar rats and New Zealand white rabbits.
    Rats were treated intraperitoneally at dose levels of 125,250,750 and 1,500mg/kg/day from day 7 to day 17 of gestation, and rabbits were treated intravenously at dose levels of 80,100,200,400 and 800mg/kg/day from day 6 to day 18 of gestation.
    In the case of rats, two-thirds of pregnant mothers in each group was sacrificed on day 20 of gestation and then their fetuses were examined for external, visceral and skeletal observation. The remaining mothers were allowed to deliver naturally, and then their offsprings were examined for postnatal development.
    In the case of rabbits, all pregnant mothers were sacrificed on day 29 of gestation and their fetuses were examined.
    Body weight of rat mothers during gestation were decreased and 4 mothers were dead until day 20 of gestation in the maximum dose. In this dose, foetal toxicity was recognized too.
    However, external, visceral and skeletal anomalies related with FOM-Na treatment were not observed in all groups. No effect on development of offsprings was observed.
    No effect of treatment of FOM-Na to rabbits was found except foetal body weight was slightly decreased in the maximum dose.
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  • II. FERTILITY TEST
    TAKEMI KOEDA, MASAHIDE MORIGUCHI
    1979 Volume 32 Issue 2 Pages 164-170
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The fertility study of fosfomycin-Na (FOM-Na) was undertaken in Wistar rats.
    FOM-Na was administered intraperitoneally at dose levels of 125,250,750 and 1,500 mg/kg/day. The male rats were continuously treated with FOM-Na from 63 days before mating and the females were treated from 14 days before mating. The males and females were treated through the mating period and then the pregnant rats were treated until 7 days of gestation.
    All pregnant rats were sacrificed on day 20 of gestation and then their fetuses were examined for external, visceral and skeletal observation.
    Mean body weight of males decreased and 6 males and 3 females died in the maximum dose. However, no significant differences were found between treated groups and the control with regard to fertility rate and pregnant rate.
    External, visceral and skeletal anomalies related with FOM-Na treatment were not observed.
    In this experiment, no effects of FOM-Na for reproductive performance in rats were observed.
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  • III. PERI-AND POST-NATAL EXAMINATION
    TAKEMI KOEDA, MASAHIDE MORIGUCHI
    1979 Volume 32 Issue 2 Pages 171-179
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The peri-and post-natal study of fosfomycin-Na (FOM-Na) was undertaken in Wistar rats.
    FOM-Na was administered intraperitoneally at dose levels of 250,750 and 1,500 mg/kg/day from day 14 of gestation to day 21 after delivery.
    It could be conculuded that delivery rate in the 750 and 1,500 mg/kg groups decreased, but no influence of FOM-Na was found on postnatal development of offspring (F1) and neonate (F2) without maximum dose.
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  • TAKEMI KOEDA, UICHI SHIBATA, HIROYASU ASAOKA, YOSHIO YAMAKI, MASANORI ...
    1979 Volume 32 Issue 2 Pages 180-190
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The pharmacological effects of fosfomycin sodium, a new antibiotic agent, were studied on central nervous system, neuromuscular junction, isolated smooth muscles, blood coagulation, red blood cell resistance, body temperature, permeability of skin vessels and Igg and Ige antibody formation in laboratory animals.
    Fosfomycin sodium inhibited activities on the isolated smooth muscles, elevated body temperature, and increased permeability of skin vessels.
    Any of these actions, however, was noticeable only when it was administered in higher doses. Except for these above effects, fosfomycin sodium did not show any actions.
    Consequently, it can be concluded that fosfomycin sodium has no specific pharmacological actions.
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  • KAORU SHIMADA, TAKASHI INAMATSU, KYOKO SATO
    1979 Volume 32 Issue 2 Pages 191-194
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The antimicrobial activity of 24 Bacteroides fragilis, 13 Bacteroides thetaiotaomicron and 5 Bacteroides vulgatus, all of which were recent clinical isolates, was determined by the agar dilution technique. These three species had similar susceptibility patterns, but the B. thetaiotaomicron strains were generally less susceptible than the B. fragilis strains. Clindamycin was very active against 81% of the Bacteroides strains at 3.1 mcg/ml of less while 21% of the Bacteroides strains had MICs of 100 mcg/ml or above. Metronidazole was active against all Bacteroides strains at 1.6 mcg/ml or less.
    The patients with decubitus ulcers and B. fragilis septicemia, who responded satisfactorily to the combination of metronidazole and tobramycin, were presented.
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  • TAKASHI MOTOHIRO, YASUTAKA SAKATA, TOORU NISHIYAMA, KOJI ISHIMOTO, KAO ...
    1979 Volume 32 Issue 2 Pages 195-204
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A clinical trial of the newly developed CS-1170 was carried out at our department.
    1. Intravenous administration of 15 mg/kg either by one-shot injection (2 cases) or by drip infusion (2 cases) and 50 mg/kg by one-shot injection (1 case) resulted in the following findings:
    a. Serum concentration of the drug was as favorable as the conventional cephalosporins.
    b. In the single case of purulent meningitis, the drug was detected in the cerebrospinal fluid. However, further study will be required to substantiate this finding.
    c. The high urinary concentration observed up to 6 hours after administration suggests the clinical usefulness of the drug against urinary tract infections.
    d. Urinary recovery rates in 2 patients were lower as compared with the cephalosporins, but this may be partly due to the small quantities of the urine excreted in these patients.
    2. The daily intravenous administration of average 133 mg/kg of CS-1170, either by injection or by drip infusion (divided into 4 doses a day), to 21 patients with various infections resulted in the clinical efficacy rate of 79%; bacteriologically, CS-1170 produced excellent results in the six cases from which bacteria was isolated, yielding a favorable overall response rate of 81%.
    3. Side effects: One patient complained of vascular pain, 2 patients developed rash and another developed glycosuria, while elevation of LDH was seen in another patient. However, GOT, GPT, Al-P, BUN and creatinine in the patients were not altered by the administration of CS-1170.
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  • NAOICHI IWAI, AKIRA SASAKI, JUNKO FUTAMURA, MITSUNOBU MIYATSU, TAMIKO ...
    1979 Volume 32 Issue 2 Pages 205-220
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • TADAFUMI NISHIMURA, YASUSHI KOTANI, TOSHIO TAKASHIMA, KENJI HIROMATSU
    1979 Volume 32 Issue 2 Pages 221-226
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The authors have carried out the pharmacokinetics and clinical studies of CS-1170. The results were as follows; CS-1170 was given by drip infusion for 1 hour dose of 20 mg per kg body weight to 3 children. The maximum blood level was reached at one hour after drip infusion. This blood levels were 38μg/ml, 68μg/ml and 86μg/ml, respectively,(mean 64μg/ml), and level at 2 hours, 11.5μg/ml, 9.4μg/ml, 16μg/ml respectively,(mean 12.3μg/ml), the blood level at 6 hours was not determined.
    The urinary excretion rates were 94.8-96.8% up to 6 hours after drip infusion dose of 20mg perkg body weight.
    CS-1170 was effective in 7 of 8 cases with pediatric bacterial infections. An ineffective case was a pneumonia due to Serratia marcescens. No side effect was observed except for 2 cases with diarrhea and one case with elevation of GOT and GPT.
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  • SUSUMU NAKAZAWA, HAJIME SATO, KENJI NIINO, SHINICHI NAKAZAWA, YUICHI H ...
    1979 Volume 32 Issue 2 Pages 227-237
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental studies and clinical evaluation of CS-1170 were carried out in the field of pediatrics, and the following results were obtained:
    1) A high serum concentration of the drug was observed by 30 minutes after the commencement of intravenous drip infusion of 20 and 30 mg/kg, with the peak appearing at the end of the infusion. Serum level of 10.0μg/ml or more was observed even 2 hours after the completion of the drip infusion.
    2) The peak of serum concentration appeared at 30 minutes after intravenous injection of 20 mg/kg, and the blood level 4 hours after the injection was 4.3μg/ml or more.
    3) Excretion of the drug into the urine by 6 hours after intravenous drip infusion or one-shot injection was 60% or more on the average, with the major portion of the drug in the active state excreted by 4 hours after the administration.
    4) Twenty-five children with acute infections (5 types of diseases) were treated with CS-1170 mainly by intravenous drip infusion, and the following clinical results were obtained: The overall clinical effective rate of 96.0% was obtained with the daily dosage of CS-1170 ranging mostly from 50 to 80 mg/kg in the total 25 cases including 7 cases of acute bronchitis (100%), 13 cases of bronchopneumonia (92.3%), 3 cases of acute urinary tract infections (100%), a case each of staphylococal exanthema and lymphadenitis in the neck (100%).
    5) Thorough analyses of the liver and kidney functions and the hematological features at the time of, and about 10 days after the administration of CS-1170 in each case so far revealed no abnormality. The drug did not affect the site of injection or the whole body.
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  • KAZUAKI NAGAMATSU, ISAMU HAMADA
    1979 Volume 32 Issue 2 Pages 238-240
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    CS-1170 was administered to 9 cases of the pediatric field. The clinical effect was good in 6 cases, fair in 2, and poor in one. The doses ranged from 80 mg/kg to 100 mg/kg, and an intravenous injection of 300 mg/kg was given in only one case.
    In the poor case, continuous instillation of 100 mg/kg was given. In the 2 fair cases, the patients with septicemia received 80 mg/kg and 300 mg/kg, respectively. There was no improvement in clinical findings, but the bacteria alone disappeared.
    As side effects, vasalgia due to intravenous injection was observed in 2 cases, but it disappeared by the intravenous injection of 500 mg dissolved in 10 ml. No case showed eruption, diarrhea, or acidophilia. GOT or GPT increased in no case either.
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  • MIKIO MINAMITANI, KEI HACHIMORI, NORIKO TOMORI
    1979 Volume 32 Issue 2 Pages 241-246
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Clinical efficacy of CS-1170 in 13 children with acute infections was evaluated. The daily dosage was 20-40mg/kg in 4 cases, 50-70 mg/kg in 8 cases and 100 mg/kg in 1 case, with the period of administration ranging from 2 to 4 days in 9 cases and from 6 to 10 days in 4 cases. The drug was given intravenously, either by drip infusion or by injection. The result was excellent in 3 cases, good in 6 cases, fair in 1 case and poor in 1 case, with 2 cases excluded from the evaluation of efficacy: thus, the rate of response was 82%.
    In 5 cases of acute respiratory tract infections, the results were excellent in 2 cases, good in 1 case and poor in 1 case, while 1 case of mycoplasma pneumonia was excluded from this determination.
    In 5 cases of acute enteritis, excellent result was obtained in 1 case, good results in 3 cases and fair in 1 case. The drug had shown good results in a case of varicella plus impetigo, and in another case of Ritirsa's disease (dermatitis exfoliative neonatorum), but a case (fever of central origin) was excluded from this evaluation. All cases showed negative result in the cutaneous reaction test, however, a patient developed nettle rash 8 days after commencement of the drug administration.
    No abnormality was found in the hematopoietic, liver and kidney functions of the patients.
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  • MINORU SAWAI, RYOCHI FUJII
    1979 Volume 32 Issue 2 Pages 247-252
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    CS-1170 was used for treatment of 26 children who were diagnosed as bacterial infections, and a response rate of 88% was obtained as the drug was effective in 15 of 17 determinable caws.
    In our evaluation, daily dosage of 75-270 mg/kg (100-200 mg/kg in the majority of the cases) was divided into 4 doses, and administered intravenously by one-shot injection over a 10-minute period.
    The period of drug administration ranged from 1.5 to 25.5 days, but in most cases it was 3 to 6 days.
    Elevation of GOT and GPT as a side effect of the drug was seen in one case (3.8%), which was reverted to normal level upon cessation of the drug administration.
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  • ETSUHIDE YAMAMOTO, HAJIME SUNAKAWA, GEN-IKU KOHAMA
    1979 Volume 32 Issue 2 Pages 253-258
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • YASUSHI OHASHI, MASAKI ABE, KEN SAITO, HIDEMORI MIZUTANI, SUSUMU ONISH ...
    1979 Volume 32 Issue 2 Pages 259-264
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • TSUYOSHI MIURA, KENJI KATAYAMA, TATSUO WADA
    1979 Volume 32 Issue 2 Pages 265-277
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • TOSHIHITO SEKI, SHINJI SHIMADA, KUNIAKI OHARA
    1979 Volume 32 Issue 2 Pages 278-281
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • KOICHI NAKANISHI, TAKANORI MIKI, KUNIHIKO ADACHI, OSAMU TERANOBU, KEIK ...
    1979 Volume 32 Issue 2 Pages 282-290
    Published: February 25, 1979
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Eight cases of malignant tumors of the head and neck were treated with NK 631 on a dosage schedule of 10 mg at a time 3 times weekly, by intravenous one-shot injection or intravenous drip infusion, to observe its therapeutic effects and adverse reactions. The treatment was assessed markedly effective in 3, moderately effective in 1 and ineffective in 4 of them. The treatment was also assessed moderately or markedly effective in 3 and ineffective in 2 out of squamous cell carcinoma cases. Hematologic findings, serum electrolytes and enzymologic findings were normal, but the pulmonary function examinations revealed a tendency for PaO2to decrease slightly. In 1 case where frequent cough was observed, the cough was mitigated on withdrawal of the treatment. The adverse reactions that evolved included fever, alopecia, eruptions, nausea and vomiting, and pigmentation of the nail. To summarize these findings, the authors were impressed with NK 631 that the agent would exert an excellent antitumor effect, compared with bleomycin, and that its effect would evolve at the early stage of its treatment. Fixed drug eruption was observed as an adverse reaction of this drug in 1 case; however, the adverse reactions of this bleomycin analog appear similar to those of its parent compound, bleomycin.
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