The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 26, Issue 3
Displaying 1-14 of 14 articles from this issue
  • WITH SPECIAL REFERENCE TO SUCH DERIVATIVES OF CEPHALOSPORINC AS CEFAZOLIN, C EPHALORIDINE AND CEPHALOTHIN
    MORIYOSHI FUKADA
    1973 Volume 26 Issue 3 Pages 197-214
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Chemotherapy during the perinatal period is still a very important matter, and the chemotherapeutic agents selected for use during this period should have the following properties: prompt efficacy, broad spectrum, bactericidal action, administration by injection and few side effects.
    Several antibiotics which satisfy such requirements are synthesized, however there are few reports of studies made concerning their application to the pregnant women during the perinatal period.
    In this paper the results of studies on the use of cephalosporin C derivatives as cephaloridine (CER), cephalothin (CET) and cefazolin (CEZ) during the perinatal period are reported.
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  • TOYOKO OGURI, MASAJI SHIDARA, NOZOMU KOSAKAI
    1973 Volume 26 Issue 3 Pages 215-220
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We identified serological groups of haemolytic streptococci and serological types of group A streptococci isolated from clinical materials, and examined the chemotherapeutic susceptibility of haemolytic streptococci.
    From pharyngeal swabs and sputa the group A and B streptococci were isolated dominantly, but the strains from urines were almost identified as group B. Among group A streptococci type 12 was dominant.
    All strains tested were very sensitive to benzyl penicillin and cephaloridine, and they were inhibited by 0.20 mcg/ml of these two drugs. Among groups A, B, C, and G, the group B streptococci were less sensitive to benzyl penicillin and cephaloridine than other groups.
    About 47% of strains tested were resistant to tetracycline and about 6% were resistant to chloramphenicol. Two strains of the group A streptococci were resistant to macrolides.
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  • I ACUTE TOXICITY IN MICE AND RATS
    TAKEMI KOEDA, MASUZO ODAKI, TAKASHI HISAMATSU, HITOSHI SASAKI, MASAYUK ...
    1973 Volume 26 Issue 3 Pages 221-227
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    3', 4'-Dideoxykanamycin B (DKB) is a new aminoglycoside antibiotic derived from kanamycin B by UMEZAWA, et al. This agent has a remarkable effectivenesst o kanamycin-resistantb acteria and Pseudomonas aeruginosa.
    Studies on acute toxicity of DKB were carried out by intravenous, intramuscular, intraperitoneal, subcutaneous and oral administration to ICR strain mice and Wistar strain rats.
    The LD50 values for male and female mice were 72.3 and 62.6 mg/kg (as base activity) i. v.; 604.7 and 430.9 mg/kg i. p.; 430.9 and 396.2 mg/kg i. m., and 528.2 and 521.3 mg/kg s.c., respectively. For mice administered with DKB orally, LD50 was over 6,950 mg/kg in both sexes. Those for male and female rats were 177.2 and 140.4 mg/kg i. v.; 799.3 and 1014.7 mg/kg i. p.; 559.5 and 576.9 mg/kg i. m., and 1,668.0 and 1,376.1 mg/kg s. c., respectively. Oral LD50 for rats was over 6,950 mg/kg, and there was no sex difference of the toxicity as well as in mice.
    Slight degenerations were histopathologically observed in the kidney but not in the other organs of animals in each experimental group. These results were favourable in comparison with those of gentamicin used as a control agent.
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  • TAKEMI KOEDA, MASUZO ODAKI, TAKASHI HISAMATSU, HITOSHI SASAKI, MASAYUK ...
    1973 Volume 26 Issue 3 Pages 228-246
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The subacute toxicity of 3', 4'-dideoxykanamycin B (DKB) was investigated with Wistar rats and rabbits to which DKB was administered intramuscularly for 35 days.
    At the dose less than 200 mg/kg, no rat died, but 8 male and 4 female rats died at the dose of 400 mg/kg. Irrespective of dose, no death was found in the DKB-treated rabbits.
    Daily administration of more than 100 mg/kg DKB in rats and more than 40 mg/kg in rabbits resulted in slight changes in values of blood chemistry studies and urine analysis.
    By the administration of higher dosage of DKB for 35 days, histochemical changes in kidney and liver such as atrophy and vacuolation of tubular epithelial cells, cyst formation in the cortex, hydronephrosis, KUPFFER'S cel l mobilizationa nd round cell infiltration into GLISSON'S capsules were observed.
    No other significant effect of DKB was observed in the other organs of the animals.
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  • TAKEMI KOEDA, MASUZO ODAKI, TAKASHI HISAMATSU, HITOSHI SASAKI, MASAYUK ...
    1973 Volume 26 Issue 3 Pages 247-261
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The chronic toxicity of 3', 4'-dideoxykanamycin B (DKB) was investigated with Wistar rats and female Beagle dogs. DKB was administered intramuscularly to male rats at 4 different doses from 25 to 200mg/kg and to female rats at 6 different doses from 5 to 150mg/kg for 182 days. Beagle dogs were administered intramuscularly with DKB at 5 different doses from 5 to 50mg/kg for 91 days.
    All ten 200mg/kg-dosed male rats, one 100mg/kg-dosed male rat, six 150mg/kg-dosed female rats, one 25mg/kg-dosed dog and two 50mg/kg-dosed dogs were dead during the course of the experiment.
    The daily dose of DKB at higher dosage levels caused an elevation in blood urea nitrogen and a reduction in number of erythrocytes. Histopathologically, the lesions such as atrophy and vacuolation of renal tubular epithelial cells, infiltration of round cells into the renal interstitium, degeneration of hepatic cells and anemia were observed in both animals administered with DKB at higher dosage levels.
    No other toxic effect was observed in the organs of the DKB treated animals.
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  • Pharmacokinetic Analysis in Man
    TOKUJI ICHIKAWA, IWAO NAKANO, ISAO HIROKAWA, KIYOKI OKADA, MASAHIRO AB ...
    1973 Volume 26 Issue 3 Pages 262-266
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetic analysis of DKB (3', 4'-dideoxykanamycin B) was performed on serum concentrations following intramuscular administration in seven adult patients.
    The disposition of DKB administered intramuscularly was adequately described by a two compartment open model, which is generally represented with the department of administered site and the department of blood and tissue.
    The biologic half life of DKB was 1.8-4 hours in patients with normal renal function, but in other side it was more than 10 hours in a patient with failured renal function. The two pharmacokinetic parameters of DKB, the biologic half life and the volume of distribution, found in repeated administration to the same patient, were in the little range of deviation for each individual patient, except one patient who had failured renal function.
    On the other hand, the rate constants for transportation from the administered site to the blood and tissue, were in the wide range of deviation for each patient.
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  • YUTAKA KOBAYASHI, KYOJI AKAISHI, TOSHIKAZU NISHIO, YOHNOSUKE KOBAYASHI ...
    1973 Volume 26 Issue 3 Pages 267-276
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Josamycin propionate (ca. 50mg/kg per day for 7 days) was given orally to 25 childrensuffering from lacunar tonsillitis (19 cases), scarlet fever (2 cases) and cervicalis lymphadenitis (4 cases), and the following results were obtained.
    1) Out of 19 cases of lacunar tonsillitis, theresult was excellent in eight, good in five, and poor in six, the efficacy rate being 68.4%. Among two cases of scarlet fever, the one showed excellent response, but remaining one case did not respond. Two cases each of four cervicalis lymphadenitis gave good and poor responses respectively. The efficacy rate was to 64.0% in total.
    2) Mild gastrointestinal disturbances were observed in four of 25 cases, but in none of them, withdrawal of medication was necessary. No side effects were detected in urine and blood findings, S-GOT, S-GPT, alkalline phosphatase and BUN values examined in all the patients before and after the medication.(In four cases of infants, the urine examination was not performed.)
    3) Some discussionw as made on the situation of macrolidea ntibioticsi n the treatment of pediatric respiratory infections, and it was concluded that josamycin propionate is a useful antibiotic in pediatric field.
    4) Individual fluctuation in the absorption of oral josamycin propionate was suggested from ex cellent responses observed ineffective cases which were not to be expected from its overallefficacy rate. Thus, in poorly responding cases, increase of dosage will be recommended regardless of the usual dosage of 50mg/kg per day.
    5) The taste and flavour of this preparation were considered acceptable to children.
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  • NOBUHIKO KOMATSU, NOBORU NAGUMO, SACHIE OKUBO, KENICHI KOIKE
    1973 Volume 26 Issue 3 Pages 277-283
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The intraperitoneal administration of schizophyllan proved to increase the nonspecinc protective activity of mouse against experimental bacterial infections.
    1) The degree of the protective effect of schizophyllan differed considerably according to species of bacteria used for challenge. The results are as follows:
    Marked effect: Staphylococcus aureus, Escherichia coli and Klebsklla pneumoniae.
    Moderate effect: Pseudomonas aeruginosa and Proteus vulgaris.
    Slight effect: Diplococcus pneumoniae and Salmonella enteritidis.
    2) The time course for changes of viable bacterial number in mouse organs showed that the multiplication of the infected bacteria was more remarkably inhibited and the organisms were more rapidly eliminated in schizophyllan-treated mice than in controls.
    3) The increase of both carbon clearance rate and phagocytic index could be recognized after the administration of schizophyllan into normal mice.
    4) The stimulation of humoral antibody formation could not be seen after immunizing the schizophyllan-treated mice with heat-killed bacteria.
    Pretreatment of mouse with schizophyllan is considered to be effective nonspecifically on various kind of acute bacterial infections by stimulating the reticulo-endothelial system of the host.
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  • KANJI SEIGA, MASAO MINAKAWA, KUNIHIKO YAMAJI, YOKO SUGIYAMA
    1973 Volume 26 Issue 3 Pages 284-289
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • JYOICHI KUMAZAWA, SEIICHI NAKAMUTA, SHUNRO MOMOSE
    1973 Volume 26 Issue 3 Pages 290-293
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Twenty patients with urinary-tract infections were treated with HI-63 (ampicillin for aqueous suspension) by intramuscular route. Good results were obtained in 11 cases (55%). No appreciable side effects were noted except for 4 cases with some pain at the site of injection.
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  • FUMIHIKO UBA, KYOSHU GO, YURUKO OKAMOTO, HIROSHI OKUBO
    1973 Volume 26 Issue 3 Pages 294-296
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • JYOJI ISHIGAMI, YASUMASA TAKAHASHI
    1973 Volume 26 Issue 3 Pages 297-300
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • MASAMICHI OTSUKA, KAYOKO TETSUTANI
    1973 Volume 26 Issue 3 Pages 301-305
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
  • HAMAO UMEZAWA
    1973 Volume 26 Issue 3 Pages 306-310
    Published: June 25, 1973
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Both 3', 4'-dideoxykanamycin B (DKB) and kanamycin B (KMB) inhibited to a similar extent the poly-U directed incorporation of 14C-phenylalanine into protein. In contrast, miscoding activity, i. e. stimulation of poly-U directed incorporation of a false amino acid (such as 14C-isoleucine) into protein, of DKB was much less than that of KMB. Both antibiotics possibly compete for common binding sites on the 30 S ribosomal subunit since the total miscoding activity, if they were allowed to act in combination, did not appear to be a simple sum of each but varied depending on the relative ratio of each concentration. Although DKB primarily inhibited protein synthesis in E. coli like KMB, its inhibition of nucleic acid synthesis was more obvious than that of KMB. DKB was a bacteriocidal antibiotic like KMB.
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