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KAZUO KUROKAWA, NOBUO FUJIMURA, TAKEHIKO YOKOTA
1974 Volume 27 Issue 4 Pages
429-433
Published: August 25, 1974
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KANJI SEIGA, MASAO MINAGAWA, NORIO FURUTA, KUNIHIKO YAMAJI, YOKO SUGIY ...
1974 Volume 27 Issue 4 Pages
434-437
Published: August 25, 1974
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SUSUMU NAKAZAWA, HAJIME SATO, OSAMU WATANABE, NAOMICHI FUJII, SHU OKA, ...
1974 Volume 27 Issue 4 Pages
438-445
Published: August 25, 1974
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MICHIAKI KAWANO, KIYOHIRO IRIMAJIRI, JUJI HIGUCHI, TOMOKOU CHIYAMA, EI ...
1974 Volume 27 Issue 4 Pages
446-450
Published: August 25, 1974
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Amikacin (BB-K8) was administered intramuscularly to the patients having respiratory infections with the dose of 200 or 400mg daily and clinical effect was observed. Clinical as well as bacteriological effects were noted in 9 of 14 patients without hepatic and renal side effects. Antimicrobial therapy with BB-K8 was considered to be more effective in the patients of minor respiratory infections than the complicated ones. It may be necessary for the daily doses of 400mg to obtain good clinical effects.
Antimicrobial activity of BB-K8
in vitro was tested on 66 strains of gram negative bacilli which were isolated from the clinical specimens. All of
Klebsiella sp.,
Cloaca, Citrobacter and 67% strains of
Pseudomonas aeruginosa were inhibited at the concentration of less than 12.5mcg/ml.
From the clinical and bacteriological aspects, the antibiotic may be indicated to treat the infections of gram-negative bacilli.
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HIROSHI HATANO, HISAYA TOKUDA, CHUICHIRO KAYABA
1974 Volume 27 Issue 4 Pages
451-455
Published: August 25, 1974
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YASUHIRO MINE, SHIGEO NONOYAMA, MINORU NISHIDA, SACHIKO GOTO, SHOGO KU ...
1974 Volume 27 Issue 4 Pages
456-462
Published: August 25, 1974
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Bicyclomycin was studied for its antigenicity and cross-reactivity with benzylpenicillin. This antibiotic was bound covalently to protein under weakly alkaline conditions. Bicyclomycin or protein conjugates produced antibodies specific to this antibiotic when injected into rabbits, guinea pigs or monkeys as shown by passive hemagglutination, hemagglutination inhibition tests, quantitative precipitin inhibition, and passive cutaneous anaphylaxis. However, no hemagglutinating antibodies were produced in rabbits after continued administration of bicyclomycin by the oral route. There was no cross-reactivity between bicyclomycin and benzylpenicillin by passive hemagglutination or inhibition tests, quantitative precipitin inhibition, and passive cutaneous anaphylaxis reaction.
Bicyclomycin is a new antibiotic active against gram-negative bacilli. The chemical structure, antimicrobial activity and other properties of this antibiotic have been described1. 2.3.4). The present paper deals with its antigenic activity, production of circulating antibodies in experimental animals, and study of elicitation its cross-reactivity with benzylpenicillin.
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IN VITRO ANTIBACTERIAL ACTIVITY OF TUM-N ON TUBERCLE BACILLI ISOLATED FROM PATIENTS
TATSUNORI SHIMIZU
1974 Volume 27 Issue 4 Pages
463-470
Published: August 25, 1974
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Tuberactinomycin-N (TUM-N) is an antibiotic isolated from the culture filtrate of
Streptomyces griseoverticillotus var.
tuberactius N 6-130 by ANDO
et al. of Toyo Jozo Co., Ltd. A report has been published1) to demonstrate its remarkable antibiotic activity against tubercle bacilli and to prove the therapeutic effect equivalent to that of viomycin (VM) in experimental tuberculosis of mice and guinea pigs2). Its ototoxicity was reported to be lower than that of VM, capreomycin (CPM) and kanamycin (KM) in its study on guinea pigs3). Its clinical effect was studied in the cases resistant to the conventional anti-tuberculous drugs and found that TUM-N is effective and has little side effect4, 5).
The author presents in this paper the test results obtained from his observation of the
in vitro antibacterial activity of TUM-N and other conventional antituberculous drugs against 100 strains of tubercle bacilli isolated from the patients who had never been submitted to TUM-N treatment.
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YOH-ICHI ONODA, YUKINORI TSUNEMATSU, KISEKO KAMEI
1974 Volume 27 Issue 4 Pages
471-474
Published: August 25, 1974
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Bacteriological and clinical studies of a new aminoglycosidic antibiotic, lividomycin (LVDM), were performed on gonococci. The results are summarized as follows:
1) Twenty-six strains of clinically isolated gonococci in 1973 showed the MICs of 4-32 μg/ml,
its peak being 16 and 32 μg/ml. 2) LVDM was intramuscularly administered once a day for 1-6 days to the patients with acute gonorrhoea. Clinical effect was judged by the resolution of symptoms and disappearance of gonococci which was observed under microscope and by cultivation. Ten cases and nine cases were treated with 1 g and 2 g of LVDM once a day, respectively. The results obtained were excellent is 3 cases and in 6 cases, good in 1 case and no case, and ineffective in 6 cases and in 3 cases, respectively. The effect of LVDM for 3 consecutive days with daily dose of 2 g seemed to be the best to cure gonorrhea.
3) No side effect was observed.
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YUTAKA KANAZAWA, TOSHIO KURAMATA
1974 Volume 27 Issue 4 Pages
475-480
Published: August 25, 1974
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Transmission of multiple drug-resistance (tetracycline: TC, chloramphenicol: CP, streptomycin: SM, sulfisoxazole: SA or TC, SM, SA) through conjugation from
Escherichia coil to some strains of
Yersinia enterocolitica and
vice versa were confirmed. The findings demonstrate that
Y. enterocoliticais capable of serving as a host to carry the R-factor of enterobacterial origin.
In primary transmission, the transfer of R-factor was notably low in frequency and patterns of resistance displayed by the recipient were almost analogous to those shown by the donors with a few exceptions of segregation of TC-resistance.
Retransmission was more frequent than in the case of primary transmission and the recipient exhibited the patterns of resistance almost similar to the one of the donor.
In serial subcultures of drug-resistant exconjugants of
Y. enterocolitica in drug-free media, no segregation of multiple drug-resistance was noticed after the 10th transfer. After storage at -20° C for 10 months, segregation of TC-resistance alone and of simultaneous multiple resistance were observed in some strains. No experimental evidence was obtained for the involvement of R-factor in the drug-resistance of
Y. enterocolitica to ampicillin or cephaloridine.
So far, attempts have not been successful to demonstrate the transmission of drug-resistance through conjugation in any of three
Y. enterocolitica strains resistant to SM, to SM and SA or to SM, SA and TC, respectively, that were isolated from intestinal contents of slaughtered swines.
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COMPARISON WITH SODIUM AMPICILLIN IN BLOOD LEVEL AND TISSUE DISTRIBUTION IN RABBITS
KEIZO MATSUMOTO, YOSHIO UZUKA, IWAO UMEZAWA, KANKI KOMIYAMA, TOYOHIKO ...
1974 Volume 27 Issue 4 Pages
481-484
Published: August 25, 1974
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Ampicillin trihydrate aqueous suspension (AB-PC Sol), a new ampicillin formulation for intramuscular injection, was studied on its blood level and tissue distribution comparatively with sodium ampicillin solution (AB-PC Na) by using rabbits.
Blood level was tested by cross-over method using three rabbits at 20 mg/kg single dose by intramuscular injection, and tissue distribution after 100 mg/kg administration of each drugs was studied separately.
From the result of both experiments, AB-PC Sol was proved to have significantly longer duration of effective antibiotic level in blood and tissues than AB-PC Na, though higher peak levels of the activity were observed by AB-PC Na.
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PROTECTIVE EFFECTS AGAINST EXPERIMENTAL INFECTIONS IN MICE AND RATS
SHIGEYUKI YOKOIYAMA, MINORU TORIYA, TAKUJI ANDO, KEIZO MATSUMOTO
1974 Volume 27 Issue 4 Pages
485-489
Published: August 25, 1974
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Ampicillin trihydrate aqueous suspension (AB-PC Sol), a new ampicillin formulation for intramuscular injection, was studied on its protective effects against experimental infections with
Streptococcus hemolyticus S 23,
Proteus morganii strain 0237,
Staphylococcus aureus 226 and
S. aureus strain 0040 in rats and mice.
Against the infection with S. hemolyticus S 23 in rats, AB-PC Sol proved to be more effective than sodium ampicillin (AB-PC Na). Higher protective effects of AB-PC Sol in comparison with AB-PC Na were observed also against infections with AB-PC resistant strains,
P. morganii strain 0237,
S. aureus 226 and
S. aureus strain 0040 in mice.
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AKIRA ITO, FUMIO KODAMA, AKIO DAMISHIRO, SHIGEKI ODAGIRI, KOKICHI FUKU ...
1974 Volume 27 Issue 4 Pages
490-493
Published: August 25, 1974
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KANJI SEIGA, KUNIHIKO YAMAJI, YOKO SUGIYAMA
1974 Volume 27 Issue 4 Pages
494-496
Published: August 25, 1974
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KENJI TANADA, KEN HIROSE, TATEO HORI, TSUTOMU SAKURAGI, HIROSHI KANETA ...
1974 Volume 27 Issue 4 Pages
497-510
Published: August 25, 1974
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AKIO ICHINOSAWA, TADAO OCHI
1974 Volume 27 Issue 4 Pages
511-516
Published: August 25, 1974
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KOJI NADAUCHI, KAORU SHIMADA
1974 Volume 27 Issue 4 Pages
517-521
Published: August 25, 1974
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TOYOKO OGURI, NOZOMU KOZAKAI
1974 Volume 27 Issue 4 Pages
522-525
Published: August 25, 1974
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TATSUNORI SHIMIZU
1974 Volume 27 Issue 4 Pages
526-531
Published: August 25, 1974
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Amoxycillin, a new broad-spectrum semi-synthetic penicillin developed by the Beecham Research Laboratories is quite similar in antibacterial spectrum to ampicillin1, 2, 3). The chemical structure of amoxycillin is shown in Fig. 1. Laboratory and clinical studies have reported that amoxycillin is well absorbed orally and that the serum levels of amoxycillin are higher than those of ampicillin4, 5.6).
In this experiment the author performed the laboratory evaluation of amoxycillin and reports here the results.
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PROLONGED ORAL ADMINISTRATION IN DOGS
AKIO TACHIBANA, MASAYUKI KOMIYA, TAKURO SADO, KUNIICHIRO YANO
1974 Volume 27 Issue 4 Pages
532-538
Published: August 25, 1974
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In order to study cumulation of josamycin propionate (JM-P) after prolonged oral administration, doses of 200 mg/kg per day (5 times that of human daily dose) were given to dogs for successive 21 days, and plasma and tissue levels, rates of urinary excretion and metabolites recovered from urine were examined once a week during an experimental period of 21 days.
1. Plasma levels were measured at 3, 8 and 24 hours after the medication on the 1st, 7th, 14th and 21st days of the experiment. No marked difference was observed among plasma level curves of these examination days, indicating no influence on plasma levels exerted by prolonged administration.
2. Tissue levels along with the plasma level of animals sacrificed were measured at 3 hours after the medication on the next day of each of the above examination days. Levels in lungs, liver, kidneys and plasma showed no change during the experiment. Levels in spleen rose in the later half of the experimental period, that is, on the 15th and 22nd days, but they only reached a plateau not higher than the levels in lungs and liver.
3. Rates of excretion into 24-hour urine showed no change caused by prolonged medication, and metabolic patterns of urine metabolites were similar during the course of the experiment.
Thus three-week oral administration of 200 mg/kg per day of josamycin propionate in dogs revealed no change in plasma levels, tissue levels, rates of urinary excretion and metabolic patterns of urine metabolites, except for higher spleen levels on the 15th and 22nd days which were, however, not higher than those of lungs and liver. It was concluded that josamycin propionate showed no significant cumulation after prolonged oral administration.
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TOKUICHI TAKAGI, YOSHIHISA NOZAKI, SHIRO TACHIKAWA, SHINJI USUDA
1974 Volume 27 Issue 4 Pages
539-548
Published: August 25, 1974
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Pharmacological effects of josamycin propionate (JM-P), a new macrolide antibiotic derivative, were additionally investigated and the following results were obtained.
1. When JM-P was administered orally at doses up to 1,000 mg/kg, no measurable effects were observed in rotarod performance test, traction method, fighting behavior, tremorine test in mice and conditioned avoidance response of rats. Both monosynaptic and polysynaptic reflexes were slightly increased with JM-P 10 mg/kg given intravenously in cats. On injecting intracerebrally, JM-P gave rise to abnormal gait, clonus and jumping in mice and 50% convulsion dose was 11.0 mg/kg.
2. No influence was detected on constriction of isolated guinea-pig tracheal muscle produced by acetylcholine, while an inhibition was observed on that of isolated guinea-pig was deferens caused by adrenaline at 1×10
-4g/ml of JM-P. A slight inhibition was seen on contractions of isolated guinea-pig ileum elicited by ACh or barium chloride at a high concentration (1×10
-3g/ml) of JM-P. JM-P at 1×10
-4 g/ml or higher doses caused dose dependent decrease in spontaneous movement of isolated non-gravid rat uterus. No effects were seen on digestive propulsion of mice after oral administration of JM-P at a dose of 1,000 mg/kg.
3. Dose-dependent decrease in heart rate and blood pressure with increased blood flow of carotid and femoral artery were observed at doses of not less than 10 mg/kg of JM-P given intravenously in anesthetized dogs. The hypotensive effect induced by JM-P given intravenously was not inhibited by the pretreatment with atropine or diphenhydramine in anesthetized cats. JM-P at a dose of 100 mg/kg given intravenously gave rise to respiratory inhibition, decreased heart rate and blood pressure, and drop of wave height in P, Q and ST, and prolongation of P-Q, P-R, P-P intervals in anesthetized dogs. These changes disappeared after 90 minutes. On isolated guineapig atria, a depression of amplitude of contraction and a decrease of heart rate were observed at 1×10
-4g/ml or higher doses of JM-P, and no influence was seen on cardiac promotion induced by noradrenaline with 1×10
-4g/ml of JM-P.
4. No effects were observed on hemolytic resistance and coagulation of whole blood in rabbits at 300 mg/kg of JM-P given orally.
5. On urine volume and pH, and urinary excretion of sodium or pottasium, no influence was seen in rats with 1,000 mg/kg of JM-P given orally.
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MINORU YAMAGISHI, KUNIHIKO KOJIMA
1974 Volume 27 Issue 4 Pages
549-555
Published: August 25, 1974
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A new antibiotic, 3', 4'-dideoxykanamycin B (DKB) was administered to 28 cases ranging from newborns to school children, combining with ampicillin, chephaloridine, and methicillin. In 15 cases, the administeration of DKB was effective to prevent infections. In 8 of 13 remaining cases DKB was effective. No side effects were noticed in all the cases.
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TOSHIYUKI MATSUMURA, TAKUJI ANDO, TETSU SAITO
1974 Volume 27 Issue 4 Pages
556-565
Published: August 25, 1974
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