The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 37, Issue 12
Displaying 1-27 of 27 articles from this issue
  • RYOCHI FUJII
    1984 Volume 37 Issue 12 Pages 2261-2270
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Nineteen eighty-three (1983) demographic data in Japan show that the infant mortality rate was 6.2per 1, 000 births, reaching the lowest level in the world. On the other hand, the mean life at birth wasexpected to be 74.20 years in males and 79.78 years in females, reaching the highest level in the world. A rapid improvement was made as compared with 1947 data, i.e., the infant mortality rate as high as 76.7per 1, 000 births and the mean life expected at birth as short as 50.06 years in males and 53.96 years infemales1).
    Many factors have contributed to this improvement. One of them is the increase of GNP and resultantimprovement of living environments and public hygiene. A more important thing is the commercialavailability of antibiotics and resultant sharp decrease of mortality from infections.
    Many antibiotics have been developed in Japan. In addition, many other antibiotics developed inother countries have been comparatively freely imported to Japan. A wide variety of antibiotics havethus been clinically used. Japan differs greatly in this respect from other countries developing antibiotics.
    Penicillin studies in Japan were started in 1944. However, penicillins remained within experimentaluse. Only a small quantity of penicillins released by the Allied Occupation Forces was clinically usedafter the termination of World War II. However, penicillins did not become commercially available inJapan until 1946 in which penicillin production was started on the foundation established by R & Defforts made during the war and by kind cooperation of the U.S. forces.
    The reason why the history of antibiotic production and consumption in Japan has differed fromthat in other countries was clarified by the author at the 5th International Congress of Chemotherapy in19672).
    This paper is intended to briefly explain changes in the consumption of major antibiotics in Japanduring the age of antibiotics, and at the same time, to report these things in English because little is knownabout them to oversea countries. With this in mind, you are kindly asked to allow me to frequentlyquote my previous reports.
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  • KOZO FUJITA, HIROSHI SAKATA, KOICHI MURONO, HAJIME YOSHIOKA, SHIZUO MA ...
    1984 Volume 37 Issue 12 Pages 2271-2282
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Twenty-eight pediatric patients were treated with ceftriaxone (Ro 13-9904, CTRX) in the doses ranging from 8.75 to 25mg/kg every 12 hours for 3.5 to 11.5 days, and the clinical efficacy and side effects were evaluated. Among the 21 children with bacterial infections including pneumonia, acute bronchitis, otitis media, tonsillitis and urinary tract infections, the results were excellent in 9, good in 11, and fair in 1 patient. Out of the 28 patients, 2 patients had diarrhea, 3 patients had slightly elevated serum concentrations of transaminases, and 2 patients showed eosinophilia.
    The serum concentrations of CTRX in 5 children ranged from 50.0 to 93.8μg/ml (mean 75.0μg/ml) at 15minutes and from 10.2 to 15.6μg/ml (mean 13.4μg/ml) at 6 hours after 10mg/kg intravenous bolus injection of CTRX. The serum half-lives were from 2.61 to 8.30 hours (mean 6.16 hours), and urinary recovery rates were from 43.3 to 58.0% (mean 48.5%) during 0-6 hours and from 52.0 to 66.1% (mean 59.4%) during 0-12 hours. After 20mg/kg intravenous bolus injection of CTRX in 4 children, the serum concentrations of CTRX were from 118.8 to 162.5μg/ml (mean 139.1μg/ml) at 15 minutes and from 18.0 to 21.1μg/ml (mean 19.2μg/ml) at 6 hours. The serum half-lives were 4.07 to 6.34 hours (mean 5.13 hours), and urinary recovery rates were 38.6 to 51.1% (mean 45.4%) during 0-6 hours and from 54.8 to 64.0% (mean 59.0%) during 0-42 hours. Patients with impairment of renal function were excluded from this pharmacokinetic study.
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  • MIKIO MINAMITANI, KEI HACHIMORI, KAZUYOSHI KANEDA
    1984 Volume 37 Issue 12 Pages 2283-2297
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (Ro 13-9904, CTRX), developed by F. Hoffmann-La Roche Ltd. in Switzerland, was used for the pediatric infections and the following results were obtained.
    1. The mean blood level of CTRX in 2 children after a 60-minute intravenous drip infusion with 20mg/kg was 58.6μg/ml at 30 minutes, 75.0μg/ml at 1 hour, 39.85μg/ml at 2 hours, 27.74μg/ml at 4 hours, 20.71μg/ml at 6 hours, 11.72μg/ml at 12 hours and 3.91μg/ml at 24 hours while the half-life time was 5.9 hours in one child and 7.6 hours in the other.
    2. CTRX was used in 22 children with acute infections consisting of 3 with acute pharyngeal tonsillitis, 4 with acute bronchitis, 8 with bronchopneumonia, 6 with infections of skin soft tissue and 1 with salmonellosis. The results were excellent in 5 cases and good in 17, indicating an efficacy rate of 100%.
    Out of 10 cases where the causative strains were detected, 4 cases were followed about the activities of the respective bacteria, i. e., H. influenzae, Streptococcus group A, S. aureus and Salmonella group B, all of which were eradicated after the end of administration. The daily dose of CTRX ranged from 30 to 50mg/kg and generally a larger dose was used for serious infections. CTRX was administered twice daily in 20 out of 22 cases, by an intravenous injection in 4 and an intravenous drip infusion in 18, for 2 to 4 days in 16 and 5 to 8 1/2 days in 6.
    3. No clinical adverse reactions were observed while the laboratory test found a slight elevation of GOT in one and that of GOT and GPT in another.
    From the above results, CTRX was judged to be a highly useful drug for treatment of pediatric infections.
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  • TAKASHI SATOH, KAZUHIDE MURE, TETSUYA SHIMIZU
    1984 Volume 37 Issue 12 Pages 2298-2303
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (CTRX), a new cephalosporin antibiotic, was evaluated in the field of obstetrics and gynecology and the following results were obtained.
    The concentration of CTRX after an intravenous injection with 1g was determined in the uterine artery, cubital vein and in the intrapelvic genital tissues such as the oviduct, ovary, endometrium, myometrium, cervix uteri and portio vaginalis. The peak level was 160μg/ml at 26 minutes after injection both in the uterine arterial serum and cubital venous serum, 48 and 38μg/g at 1 hour and 18 minutes in the tissues of oviduct and ovary, respectively, 54 and 50μg/g at 48 minutes in the myometrium and cervix uteri, respectively, while 46μg/g at 39 minutes in the portio vaginalis. The mean level 18 to 24 hours after administration was 19μg/ml in the uterine arterial serum and cubital venous serum and 6.3μg/g in the intrapelvic genital tissues.
    A case of intrapelvic infection clinically showed an excellent response without any side effects by intravenous drip infusion with 2g divided as twice a day for 7 days.
    The above results show that CTRX is useful in the field of obstetrics. and gynecology
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  • NANKUN CHO, HIROKO WATANABE, KIYOSHI YOSHIDA, SHUICHI MORIYAMA, HITOSH ...
    1984 Volume 37 Issue 12 Pages 2304-2319
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (Ro 13-9904, CTRX), a new cephem antibiotic, was studied in the field of obstetrics and gynecology, and the following results were obtained.
    1. The absorption and tissue penetration of CTRX into intrapelvic genital organs were good. The peak serum level in the uterine artery after a single intravenous injection and that after an intravenous drip infusion for 30-60 minutes, both with 1g, were 162.5μg/ml and 84.4-93.8μg/ml, respectively. High concentrations were obtained also in genital organ tissues; the maximum concentration was 93.8μg/g by intravenous injection and 56.3-59.4μg/g by intravenous drip infusion. Changes in the tissue concentration were similar to those in the serum, the level over MICH against main pathogenic organisms being maintained for a long time.
    2. The penetration of CTRX into intrapelvic dead space exudate was good. The level reached a peak of 18.8μg/ml 2 hours after an intravenous injection with 1g and 13.3μg/ml after 12 hours, while the level over MIC80 against main pathogenic organisms was maintained for a long time.
    3. CTRX was effective in 15 out of 16 cases (93.8%) with gynecoobstetric infections such as intrauterine, intrapelvic, adnexal infections, and postoperative wound infections, administered with 1 g twice a day. No side effects were observed.
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  • YUKIO MATSUI, MASAKAZU NODA, TATSUYA KOHARA
    1984 Volume 37 Issue 12 Pages 2320-2327
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (Ro 13-9904, CTRX) was studied about the tissue transfer in the gynecoobstetric field and the following results were obtained.
    1. The transfer of CTRX into the uterine tissues and adnexa was favorable following an intravenous injection with 1g. The mean serum level 1 hour after administration was 123.3μg/ml while the tissue level ranged from 26 to 48μg/g.
    2. The level in the pelvic dead space exudate reached a peak 3 to 6 hours after administration and got higher than the serum level at 5 to 6 hours.
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  • KEIICHI SAKAKURA, SHIGERU HAYASHI
    1984 Volume 37 Issue 12 Pages 2328-2337
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental and clinical studies on ceftriaxone (CTRX, Ro 13-9904) were performed in the field of obstetrics and gynecology and the following results were obtained.
    1. The serum concentration was maintained at a high level to remain 22μg/ml about 24 hours after intravenous injection with 1g CTRX.
    2. The level in each tissue except myometrium reached a peak of 50μg/g or higher at 54 minutes after intravenous injection with 1g CTRX.
    3. The peak level in the dead space exudate, obtained 4 to 6 hours after intravenous injection was 77μg/ml with 1g, and 125μg/ml and 115μg/ml with 2g.
    4. The clinical efficacy was observed in all the cases (excellent in 1 and good in 3) consisting of 1 with BARTHOLIN'S abscess, 2 with adnexitis and 1 with pelvioperitonitis.
    5. Neither adverse reaction nor posttreatment laboratory test abnormality was observed in any case.
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  • MASAKI KUWABARA, KAZUNARI MATSUI
    1984 Volume 37 Issue 12 Pages 2338-2342
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone(Ro 13-9904, CTRX), a newly developed third-generation cephem antibiotic, reportedly has an antibacterial spectrum of wide-range and shows a much greater activity than cefazolin especially against Gram-negative bacteria and satisfactory effectiveness against anaerobes. In the gyneco-obstetric infections, the relation between the level in the intrapelvic organs and MIC is an important subject in many respects. The levels in the blood and each tissue determined in 54 cases, as presented in Fig. 2, show that a high concentration can be maintained for a long time. In particular the half-life time in the uterine artery and cubital vein was 8.2 hours and 7.8 hours, respectively, which was longer than that of any other existing antibiotics. This fact suggests that CTRX exhibits sufficient efficacy when administered intravenously even in a small dosage of 1g in the present study. The clinical efficacy was good or above in all the 7 cases treated. There was neither clinical adverse reaction nor laboratory test abnormality found during and after the administration in any of the 54 cases in the fundamental study and 7 cases in the clinical study. It is suggested from the above-mentioned results that CTRX is an unprecedentedly useful antibiotic with an antibacterial spectrum of wide-range.
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  • KUNIHIKO ITOH, HIDEAKI KONDOH, MOTOKI HAYASAKI, KATSUMI NODA
    1984 Volume 37 Issue 12 Pages 2343-2348
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Excretion of ceftriaxone (Ro 13-9904, CTRX) into female genital organs was studied by determining its concentration in the dead space exudate of the patients who received radical hysterectomy due to uterocervical cancer. Data analysis was performed by the three-compartment model. The serum peak level of CTRX in the cubital vein was 177.74μg/ml 1 hour after the initiation of intravenous drip infusion for 1 hour with 1g.
    The concentration of CTRX in the exudate of pelvic dead space reached a peak of 62.75μg/ml 4.61 hours after the start of administration and still showed a very high level of 25μg/ml at 24 hours. The AUC of the excretion into the exudate of pelvic dead space was 1,432.43μg·hr/ml.
    These results indicate that CTRX is a clinically useful drug, being excreted into the exudate of pelvic dead space favorably.
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  • KEIU NINOMIYA, TOSHIKO YOSHIMOTO, YUKIO HASEGAWA
    1984 Volume 37 Issue 12 Pages 2349-2354
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In vitro activity of ceftriaxone (CTRX) was examined by agar plates dilution method against 398 strains isolated from the infections in the field of obstetrics and gynecology.
    MIC90 of CTRX against Staphylococcus (107 strains), E. coli (54 strains), K. pneumoniae (27 strains), Peptococcus and Peptostreptococcus (106 strains) and Bacteroides (104 strains) was more than 100μg/ml, less than 0.20μg/ml, less than 0.20μg/ml, 6.25μg/ml and 50μg/ml, respectively.
    The concentrations of CTRX 16.9 hours after 1 hour intravenous drip infusion with 1g were 46.2μg/ml in the uterine artery, 48.0μg/ml in the cubital vein, 11.0μg/g in the endometrium, myometrium and cervix uteri, and 14.0μg/g in the portio vaginalis. These concentrations of CTRX in the serum and uterine tissues were higher than the level required to inhibit 90% of the strains of E. coli, K. pneumoniae, and Peptococcus and Peptostreptococcus, isolated from the infections in the field of obstetrics and gynecology.
    Clinical efficacy of CTRX was evaluated in 7 cases consisting of 2 with puerperal fever and one each with puerperal intrauterine infection, intrauterine infection, pyometra, adnexitis and BARTHOLIN'S abscess.
    Clinical and bacteriological efficacies were seen in 6 and 4 cases, respectively.
    Neither noteworthy adverse reactions nor laboratory abnormalities were observed throughout this study.
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  • TAKAO YAMAMOTO, JINSUKE YASUDA, MASAAKI KANAO, HIROJI OKADA
    1984 Volume 37 Issue 12 Pages 2355-2363
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental and clinical studies on ceftriaxone (CTRX, Ro 13-9904), a new cephalosporin antibiotic, were carried out with the following results.
    1. Concentration of CTRX was examined in serum, internal genital organs and retroperitoneal fluid after single intravenous administration of 1.0g dose.
    The venous serum level of CTRX was 156μg/ml at 5 minutes after the administration.
    The favorable transfer of CTRX to internal genital organs and retroperitoneal fluid was demonstrated.
    2. In clinical trial, CTRX was given to 10 cases with obstetrical and gynecological infections such as endometritis, adnexitis, pelvic peritonitis and parametritis.
    The efficacy was evaluated as excellent in 1 case, good in 8 cases and poor in 1 case.
    No side effects were observed in any of the cases treated with CTRX.
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  • TAKAHISA HORII, MASANORI IKEDA, YOSHIHIDE OKUMURA, KENSAKU TESHIMA, KI ...
    1984 Volume 37 Issue 12 Pages 2364-2370
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental and clinical studies on ceftriaxone (Ro 13-9904, CTRX), a new cephem antibiotic, were carried out with the following results.
    1. Following each 1.0g of drip infusion, transfer of CTRX to female genital organs was found to be excellent. Transfer of CTRX to exudate of the pelvic dead space was also excellent. And high concentration of CTRX was kept for long time after administration.
    2. CTRX was given to 7 cases. It was effective for 5 cases and ineffective for 2 cases.
    3. The above results demonstrated that CTRX is a safe and effective drug.
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  • YOSHIMASA TSUJI, KIMIHIKO ITOH, IKUKO MORIYAMA, MOTOHIKO ICHIJO
    1984 Volume 37 Issue 12 Pages 2371-2376
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    It is reported that ceftriaxone (Ro 13-9904, CTRX) has a half-life time of 7 to 8 hours. In the present study, the serum level 18 hours after intravenous injection with 1g CTRX was as high as 9.3μg/ml while obviously a higher tissue concentration was maintained compared with other drugs. These facts suggest that CTRX is effective against infections and that the dosage and frequency of administration could be reduced. The global evaluation revealed that CTRX was clinically effective in all the 4 cases with infections. As the adverse reaction, light leukopenia was observed only in 1 case out of the present 4 cases and 20 others administered with CTRX.
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  • FUMIO DOKO
    1984 Volume 37 Issue 12 Pages 2377-2383
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (Ro 13-9904, CTRX), a new cephalosporin antibiotic, was basically and clinically studied in the field of obstetrics and gynecology. The following results were obtained.
    1. The pelvic dead space exudate and serum levels of CTRX were measured in patients with radical hysterectomy with pelvic lymphadenectomy for uterine cervical cancer after the intravenous injection of 1g. Immediately after the injection, the serum level increased to 146μg/ml on average and thereafter declined rapidly. The pelvic dead space exudate level attained the peak of 88μg/ml after 4 hours and thereafter declined gradually but was 74μg/ml even at 8 hours after the injection.
    2. A total of 13 cases comprising 2 with intrauterine infection, 5 with pelveoperitonitis, 4 with adnexitis and 2 with external genital organ infection were intravenously treated with CTRX at a dose of 1g twice daily for 3-7 days. The clinical results were good in 12 cases and unknown in 1 case. Eruption was noted in 1 case.
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  • KOJI HIRABAYASHI, ETSUKO OKADA
    1984 Volume 37 Issue 12 Pages 2384-2390
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftriaxone (Ro 13-9904, CTRX), a newly developed cephalosporin antibiotic, was fundamentally evaluated through determination of the levels in the female genital organ tissues and in the pelvic dead space exudate. CTRX was also studied on its clinical efficacy in 13 cases with gynecoobstetric infections. The transmission of CTRX into the female genital organ tissues was favorable: the peak level in each tissue was as high as 38 to 63μg/g 18 to 37 minutes after administration. The level in each tissue even after about 18 hours remained around 10μg/g, suggesting its better transmission into the tissues than other drugs. The transmission into the pelvic dead space exudate was also good: the level reached a peak of 100 to 120μg/ml 1 to 3 hours after administration and still ranged from 74 to 76μg/ml even after about 12 hours.
    The clinical efficacy was excellent in 5, good in 5 and poor in 3 out of 13 cases with gynecoobstetric infections and the efficacy rate was 76.9%. Neither adverse reaction nor laboratory test abnormality was observed in any case.
    The above-mentioned results suggest that CTRX is a useful antibiotic for gynecoobstetric infections.
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  • MOTOHIRO BONGO, REMO SHIMIZU, KATSUYOSHI SAKAE, SHOJI HAYASHI, MITSUO ...
    1984 Volume 37 Issue 12 Pages 2391-2396
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    One gram of ceftriaxone (Ro 13-9904, CTRX), a new cephalosporin antibiotic, was given intravenously to a total of 25 patients prior to abdominal total hysterectomy for uterine myoma with or without small benign ovarian tumor. Bilateral uterine arteries were clamped at 0.5, 1, 2, 6, 12 and 24 hours after administration, and serum samples and uterine tissues were taken for the measurement of CTRX concentration by bioassay method. A little difference was found in the serum concentration between cubital venous and uterine arterial serum, the half-lives being 8.0 and 7.9 hours, respectively. The initial concentrations were estimated to be 153μg/mi and 160μg/ml, respectively. The tissue peak concentrations were obtained at 30 minutes in the myometrium, portio vaginalis, oviduct and ovary, and at 1 hour in the endometrium and cervix uteri. These were 41, 51, 51, 39, 42 and 47μg/g, respectively. The tissue concentrations after peak decreased in the same manner as the serum concentrations. Judging from its favorable transfer into the uterine tissues, CTRX was evaluated to be clinically useful in the treatment of obstetrical and gynecological infections.
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  • YUKIKO HARAMAKI, IKUO NAKAYAMA, NAOHIRO MATSUO, KATSUHIKO UCHIDA, KOHI ...
    1984 Volume 37 Issue 12 Pages 2397-2405
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX), a new cephalosporin antibiotic, was performed in the field of obstetrics and gynecology and the following results were obtained.
    1. The concentration of CTRX after intravenous injection was determined in the arterial and venous blood, and in the internal genital organs and a favorable tissue transfer was observed.
    2. The clinical efficacy rate was not very high (40%); good in 2 out of 5 cases with gynecoobstetric infections, but it is notable that efficacy was recognized in the case which B. fragilis was detected.
    3. Neither adverse reaction nor laboratory test abnormality was seen to be attributable to CTRX in any case.
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  • KENJI KUBOTA
    1984 Volume 37 Issue 12 Pages 2406-2415
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The study was done to evaluate the usefulness of ceftriaxone (Ro 13-9904, CTRX) injection for the treatment of infections in the field of obstetrics and gynecology.
    Fundamental and clinical studies were made and following results were obtained. When 1g of CTRX is administered by intravenous single shot, the concentrations in various tissues of female genital organs were as follows: 40 μg/g in oviduct, 30 μg/g in ovary, 23 μg/g and 32 μg/g in corpus uteri and cervix uteri, respectively, at 2 hours 20 minutes after single shot. As for the transfer to the exudate in the pelvic dead space, the peak concentrations were 66-69 μg/ml after 4-5 hours. In the clinical studies, CTRX was given to 20 cases with female genital organ infections and others. As for the clinical effects, responses were excellent in 2 cases, good in 18 cases among 20 cases in total. The efficacy rate was 100%. As for the clinical effects on causative bacteria, the efficacy rates were 100% for single infections due to Gram-positive bacteria (6/6), due to Gram-negative bacteria (1/1), for mixed infection (3/3). Side effect was observed in 1 case with diarrhea. CTRX showed a satisfactory clinical efficacy and a potent bacteriological effect in treatment of the infections in the field of obstetrics and gynecology, and it has been concluded that CTRX will be a useful addition to the antibiotics for the therapy of these infections.
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  • OSAMU FUKUDA, SHINICHI MIYAMURA, SATORU INOUE, MASAO MAEYAMA
    1984 Volume 37 Issue 12 Pages 2416-2419
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fundamental study on tissue distribution of ceftriaxone (Ro 13-9904, CTRX), a new cephalosporin parenteral antibiotic, was studied and the following results were obtained.
    CTRX had been administered by intravenous drip infusion with 1g to 9 cases who received simple total hysterectomy. The level of CTRX in the cubital venous serum and uterine arterial serum was determined as well as the tissue concentration in the oviduct, ovary, endometrium, myometrium, cervix uteri and portio vaginalis. The level in the oviduct and portio vaginalis was generally high, although it was observed only in a few cases. The variation of the level in the myometrium was large. CTRX is expected to be clinically useful considering the fact that its half-life time is 8.5 hours, which is longer than that of existing cephalosporin antibiotics.
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  • ISAO MIYAKAWA, KEIICHI TANIYAMA, KIMIHIRO NAGAI, HIROSHI YASUDA, NORIM ...
    1984 Volume 37 Issue 12 Pages 2420-2426
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The concentrations of ceftriaxone (Ro 13-9904, CTRX) in peripheral venous serum, uterine arterial serum and intrapelvic genital organs were determined by bioassay, using the cylinder-plate diffusion method, in 26 women with simple total hysterectomy.
    With an intravenous injection of CTRX 1 g, the maximum levels of peripheral venous serum and uterine arterial serum were 116.23 μg/ml and 112.76 μg/ml, respectively.
    Also, the biological half-life (T 1/2) was 6.85 hours in peripheral venous serum and 7.31 hours in uterine arterial serum. The concentrations of CTRX in peripheral venous and uterine arterial serum were more than 7.8 μg/ml at 24 hours after injection and maintained at a higher level than the minimal inhibitory concentration necessary for most E. coli strains for at least 24 hours.
    The concentrations of CTRX in intrapelvic genital organs were kept higher than the minimal inhibitory concentration against E. coli at 24 hours after injection, and the ratios of the concentrations inuterine tube and endometrium to that of in peripheral venous serum were 0.474±0.080 and 0.272±0.087, respectively.
    Since CTRX is characterized by more potent antibacterial activity than some other antibiotics and the long-acting efficacy, intravenous administration of CTRX at 1g or 2g per day may be an adequate dose for infections of the female urogenital tract.
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  • Pediatric Study Group of Sulbactam/Cefoperazone
    RYOCHI FUJII, HIDENORI MEGURO, OSAMU ARIMASU, JIN MASHIKO, TAKESHI TAJ ...
    1984 Volume 37 Issue 12 Pages 2427-2456
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Bacteriological and clinical effect of a newly developed SBT/CPZ in the treatment for pediatric patients was assessed by a study group consisting of 15 institutions. The results were as follows.
    1. Antibacterial effect
    Susceptibility studies were performed with 93 clinical isolates. The MIC of SBT/CPZ was one-tube inferior or almost similar to that of CPZ in susceptible organisms. In CPZ-resistant organisms at the inoculum of 108 cells/ml, however, SBT/CPZ was much superior to CPZ on the basis of the MIC.
    When the MIC of SBT/CPZ was compared to that of CPZ in 27 strains which have high β-lactamase-producing activity, it was found that many of CPZ-resistant organisms were susceptible to SBT/CPZ.
    2. Serum concentration and urinary excretion
    The serum concentrations of SBT and CPZ were 33.2 μg/ml and 79.2 μg/mI, respectively at 15 minutes after 20 mg/kg SBT/CPZ was administered by intravenous bolus injection, and those of SBT and CPZ, 51.0 μg/ml and 108.3 μg/ml, respectively following 40 mg/kg SBT/CPZ therapy. The serum concentrations of CPZ were 2.1-2.4 times as high as those of SBT. The concentrations were dose-related. The half-lives of SBT and CPZ following 20 mg/kg SBT/CPZ administration were 0.94 hour and 1.50 hours, respectively, and those following 40 mg/kg SBT/CPZ were 0.95 hour and 1.53 hours, respectively. There was no significant difference between 20 mg/kg and 40 mg/kg administrations. When compared between SBT and CPZ, CPZ had slightly longer half-lives.
    At the termination of 1 hour drip infusion of 20 mg/kg SBT/CPZ, the serum concentrations of SBT and CPZ were 16.7 μg/ml and 40.1 μg/ml, respectively. In the case of 40 mg/kg, the levels of SBT and CPZ were 38.6 μg/ml and 94.9 μg/ml, respectively. The concentrations were found to be dose-related as were following intravenous bolus injections. The SBT half-lives obtained after 20 mg/kg and 40 mg/kg SBT/CPZ administrations were 1.39 hours and 0.89 hour, respectively; those of CPZ, 2.00 hours and 1.44 hours, respectively.
    The highest urinary concentration occurred 0-2 hours after intravenous bolus injections of 20 mg/kg or 40 mg/kg SBT/CPZ. Urinary excretion of SBT over 6 hours was 60.0% and 67.7%, and that of CPZ, 21.2% and 25.0%, indicating higher urinary excretion for SBT.
    When 20 mg/kg SBT/CPZ or 40 mg/kg was administered over 1 hour by drip infusion, urinary excretion became the highest at 1-3 hours after administration. Urinary excretion of SBT over 7 hours following 20 mg/kg and 40 mg/kg SBT/CPZ was 68.8% and 80.3%, respectively, and that of CPZ, 24.4% and 27.3%. The results were similar to those observed following intravenous bolus injections.
    3. Clinical results
    Out of a total of 286, 264 patients were assessed on clinical efficacy. Twenty-two patients were dropouts or excluded.
    The clinical efficacy was excellent or good in 148 out of 156 patients in whom causative organisms were isolated, with the efficacy rate of 94.9%. The efficacy rate in 108 patients in whom causative organisms were not detected was 91.7% which was not significantly different from that in the former group. The total efficacy rate was 93.6%; excellent or good in 247 out of 264 patients.
    In bacteriological studies, 166 out of 174 causative strains were eradicated with the eradication rate of 95.4%. Out of 27 β-lactamase producing strains, 25 were eradicated. The eradication rate was 92.6%.
    The clinical efficacy was excellent or good in 40 patients out of 44 who had not responded to other antibiotics. The efficacy rate was 90.9%.
    4. Side effects and laboratory tests
    Out of a total of 286 patients, 279 were examined on side effects and laboratory-test abnormality. Seven patients were excluded from the assessment because they had failed to follow the predetermined administration schedule. The side effects observed were fever, rash, soft stool and diarrhea.
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  • YOSHIKIYO TOYONAGA, YOSHIIE KUROSU, HIRONORI NAKAMURA, MORIMASA SUGITA ...
    1984 Volume 37 Issue 12 Pages 2457-2477
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Sulbactam (SBT) in a novel β-lactamase inhibitor from Pfizer and combined with cefoperazone (CPZ) ina 1:1 ratio (SBT/CPZ). Fundamental and clinical studies on SBT/CPZ were executed. The antibacterial activity of SBT/CPZ was compared with those of SBT, CPZ and CEZ against clinical isolates of S. aureus and E. coil which were not susceptible to CEZ. SBT alone did not show any activity against S. aureus, MICs against all strains were over than 100 μg/ml on the inoculations of undiluted and 100-fold diluted specimen. CPZ showed MICs over than 100 μg/ml against approximately 70% of the isolates on the undiluted inoculation, and on the 100-fold diluted inoculation, the MIC50 and MIC70 were 12.5 μg/ml and 100 μg/ml, respectively. SBT/CPZ showed better activity than CPZ by 2-8 folds against the strains highly resistant to CPZ; the MIC50 on the undiluted inoculation was 50 μg/ml. Against E. colt, the characteristic of SBT/CPZ was shown more clearly. The MICs of CPZ were over than 100 μg/ml against approximately 70% of the isolates on the undiluted inoculation, but SBT/CPZ showed MIC50 at 25 μg/ml. On the 100-fold diluted inoculation, SBT/CPZ was 4-8-fold superior than CPZ against strains on which MICs of CPZ were over than 12.5 μg/ml.
    Serum levels were determined by a bolus intravenous injection and by intravenous drip infusion of 10, 20, 40 mg/kg of SBT/CPZ. When administered by a bolus injection, the peak level was seen at 30 minutes in most patients: 8.7, 14.7 or 27.0 μg/ml of SBT and 30.1, 42.5 or 76.4 μg/ml of CPZ were detected with the 3 different doses. These levels were dose-dependent, and decreased slowly to 0.3, 0.3 or 0.3 μg/ml of SBT and 2.9, 2.8 or 3.3 μg/ml of CPZ at 6 hours after administration. Half-lives were 1.39, 1.20 or 0.98 hour for SBT and 1.77, 1.59 or 1.42 hours for CPZ.
    The same 3 doses were given by intravenous drip infusion. The peak levels obtained at the end of infusion (1 hour after initiation of infusion) were 15.3, 14.4 or 43.2 μg/mI for SBT and 33.4, 38.2 or 104.2 μg/ml for CPZ, respectively. The levels were somewhat low in 20 mg/kg group. After the end of infusion, these levels decreased fairly rapidly, and after 6 hours almost the same levels of 0.4, 0.5 or 0.3 μg/ml for SBT and 1.4, 3.9 or 3.3 μg/ml for CPZ were detected. Half-lives were 1.46, 1.05 or 0.89 hours for SBT and 1.48, 1.56 or 1.28 hours for CPZ. Thus the half-lives for SBT were diversified, but for CPZ they were not prominent.
    Urinary recovery rates after a bolus injection were 55.2-102.1% of SBT and 11.9-44.8% of CPZ. By intravenous drip infusion (1 hour) 24.8-94.8% of SBT and 6.1-33.9% of CPZ were recovered in the urine during 6 hours.
    SBT/CPZ was given to 19 patients with bronchopneumonia (10 cases), urinary tract infections (6 cases), otitis media (1), phlegmonous cellulitis (1) or purulent lymphadenitis (1), and produced excellent or good efficacy in all patients. They were with moderate degree of infections and the dose was 30-60 mg/kg/day in most cases.
    Side effects were not observed in any cases. As for laboratory abnormalities, elevations of GOT and GPT in 1 case, GOT elevation in 2 cases and OPT elevation in 1 case were detected, but their degrees were mild enough to continue the administration of SBT/CPZ.
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  • ISAO OBATA, FUKUSHO RYU, NOBUYUKI IMAGAWA, KAZUHIKO OCHIAI, KIYOHIKO K ...
    1984 Volume 37 Issue 12 Pages 2478-2494
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Efficacy and safety of sulbactam/cefoperazone (SBT/CPZ) was studied on gynecological infections. The results obtained are as follows:
    1. In the treatment of 31 cases of gynecological infections, the clinical efficacy of SBT/CPZ was assessed as excellent in 9 cases and effective in 22 cases.
    2. As for the bacteriological effects of SBT/CPZ, clinically isolated organisms were completely (100%) eradicated.
    3. In comparison with MICs of CPZ, SBT/CPZ was found to show a combined effect on Gram-negative and Gram-positive organisms in the order mentioned, but this effect was not observed against anaerobes. The combined effect of SBT/CPZ on β-lactamase producing bacteria was also investigated in the same manner. As a result, SBT/CPZ was found to exert a combined effect on β-lactamase strains of S. aureus, S. epidermidis, E. coil, B. catarrhalis and B. fragilis.
    4. The laboratory tests performed before and after administration of SBT/CPZ revealed rise in GOT and GPT values in 1 case, GPT values in 2 cases and eosinophil in 1 case. However, these rises were all mild and required no particular measures.
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  • SUZUAKI SHIMIZU, MASAMI HIRANO, SHIGERU SHIRAKAWA, NOBUYUKI MINAMI, RY ...
    1984 Volume 37 Issue 12 Pages 2495-2505
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Ceftizoxime (CZX) was given by intravenous injection in daily doses of 2-8g to 103 patients with severe infections complicating hematopoietic disorders. The clinical effect was evaluated in 95 of the 103 patients. The causative organisms were identified in 22 patients but were unknown in the remaining 73. Infected sites were the respiratory tract, urinary tract, soft tissue, and blood. The overall effectiveness rate (inclusive of marked and moderate) was 61.1% (58/95). The effectiveness rate was 63.6% (14/22) in patients in whom the causative organisms were identified and 60.3% (44/73) in patients in whom the causative organisms could not be identified and 60.0% (18/30) in 30 patients with less than 100 neutrophils per mm3 before treatment. No side effects were noted except drug fever in 1 patient. Abnormal hepatic function was seen in 6 patients but was not attributed to the drug in any case. The results indicate that CZX is a safe and useful antibiotic for the treatment of severe infectious complications in hematopoietic disorders.
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  • TATSUMI UCHIDA, SHIN MATSUDA, HIDEO KIMURA, TADASHI SATOH, TOSHIYUKI I ...
    1984 Volume 37 Issue 12 Pages 2506-2518
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Clinical evaluation of cefmenoxime (CMX, Bestcall®) was examined in the infection associated with hematological disorders, respiratory tract and other disorders. Clinical effectiveness for severe infection of hematological disorders was 47.4% in good and 84.2% in fair response, however, in the respiratory tract infections, 89.7% in good responce was obtained. Opportunistic infection due to Gram-negative bacilli are often experienced in patients with hematological disorders. It was discussed that CMX would be a good therapeutic agent against infectious diseases associated with hematological disorders because it's antibacterial spectrum would be parallel to pathogens of such disorders.
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  • KANJI SEIGA, YOKO SUGIYAMA
    1984 Volume 37 Issue 12 Pages 2519-2530
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefbuperazone (CBPZ), a new cephamycin antibiotic, was studied for the distribution in the genital organs and the excretion to the pelvic dead space exudate by bioassay, and the following results were obtained.
    1. CBPZ was rapidly distributed into the various tissues by intravenous drip infusion of 0.5g and 1.0g for 1 hour. Those levels depended on serum levels and the ratios (tissue level/serum level) were about 15-25%.
    2. Obvious dose response between 0.5g and 1.0g of CBPZ was recognized for serum levels as well as tissue levels.
    3. Serum and tissue levels were respectively analyzed by two-and three-compartment open model. Consequently, the obtained simulation curve approximated to the observed results.
    4. The simulation curve and pharmacokinetic parameters by one-compartment open model were ap-propriate for CBPZ levels in the pelvic dead space exudate.
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  • 1984 Volume 37 Issue 12 Pages 2531-2534
    Published: December 25, 1984
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Download PDF (484K)
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