The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 35, Issue 6
Displaying 1-29 of 29 articles from this issue
  • KEIMEI MASHIMO
    1982 Volume 35 Issue 6 Pages 1365-1373
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The antibacterial spectrum of cefroxadine was as wide as that of CEX, and its antibacterial effect was as strong as that of CEX or even 2-fold stronger against E.coli and Klebsiella.Cefroxadine was also proved to have stronger bactericidal or bacteriolytic effect than CEX and have better affinity with penicillin binding proteins.In clinical trials, an efficacy rate of82.7% was achived in a total of2,009cases of various infections analyzed.Cefroxadine displayed particularly good clinical and bacteriological effects for the infections of skin, soft tissues, respiratory tract and urinary tract.The rate of bacteria eradication in a total of1,410cases was 81.6%, showing good results against the bacteria such as S.aureus (83.9%, 167/199), E.coli (89.0%, 528/593), Klebsiella (78.0%, 78/100) and P.mirabilis (80.0%, 36/45).As for side effects, their incidence was a low of only2.3%, the main ones being eruption and gastrointestinal symptoms just as recognized in conventional cephalosporins, and none of them was serious.Abnormal laboratory test values were only increases in eosinophil, SGOT, S-GPT and Al-P values, and their incidence was low.
    From these findings, we may say that the drug is an effective, safe, and useful antibiotic among all other orally administered cephalosporins.
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  • MASAO SUWAKI, MASAMI IKEDA, NAOHIRO KASHIWA, NOZOMI NOHARA, TAKASHI NA ...
    1982 Volume 35 Issue 6 Pages 1374-1378
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    1. Fortimicin (KW-1070) was found to be similar to amikacin in vitro activity against S. aureus of 27strains and S. epidermidis of 17strains isolated in dermatological field.
    2. Serum and skin levels of the drug were determined in rats.Mean serum levels (n=4) were 4.91mcg/ml at1/4hour, 3.40mcg/ml at1/2hour, 2.40mcg/ml at1hour and0.51mcg/ml at2hours. The corresponding skin levels were2.15mcg/g, 2.27mcg/g, 0.83mcg/g and0.19mcg/g.
    3. Seven cases with dermatological infections were treated with fortimicin.No side effects were observed both in subjective symptoms and in laboratory findings.
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  • TETSUO TAGUCHI, MASAHIDE FUJITA, KAZUYOSHI TOMITA, SEIICHI MATSUNAGA, ...
    1982 Volume 35 Issue 6 Pages 1379-1386
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Fortimicin (KW-1070), a new aminoglycoside antibiotic was administered to17patients suffering from surgical infections (peritonitis4cases, periproctal abscess5cases, subphrenic abscess3cases, suture abscess2cases, dead space infection2cases, perineal abscess1case). The results obtained are as follows.
    1) Clinical effect of fortimicin was excellent in5, good in10and poor in2out of17cases.The effective rate was88.2% (15/17).
    2) No significant side effect was observed.
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  • SHIZUAKI HOSOMA, ROKURO SEIKO, TOSHIO ITO
    1982 Volume 35 Issue 6 Pages 1387-1390
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A new aminoglycoside antibiotic, fortimicin, was administered intramuscularly to3patients (panperitonitis). Clinical response was excellent in2cases and good in1case.The effective rate was 100%.In these patients, fortimicin was given in a dose of600mg, 2or3times daily for6to7days. No adverse effect was observed.Therefore fortimicin was suggested to be a useful drug for the treatment of panperitonitis.
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  • SHOZO KAWAMURA
    1982 Volume 35 Issue 6 Pages 1391-1394
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A dose of 200 mg or 300 mg of fortimicin was administered intramuscularly once a day for 4-6 days in 12 cases of otorhinolaryngological infections.
    Clinical response obtained in these cases was excellent in 8 cases (66.7%), good in 3 cases (25.0%). The effective rate was 91.7%.
    No side effect was observed in these 12 cases.
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  • NAOKI MATSUYA, MINORU MURATA, SAO TAKAKU
    1982 Volume 35 Issue 6 Pages 1395-1398
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Bacteriological and clinical studies of fortimicin in the field of ophthalmology were performed and the results obtained were as follows.
    1. The concentration of fortimicin in serum, primary aqueous humor and secondary aqueous humor after intramuscular injection of 30 mg/kg to rabbit reached the peak value of 23.36μg/ml after 1/2 hour, 6.07μg/ml after 1 hour and 60.6μg/ml after 1 hour, respectively.
    2. The concentration of fortimicin in primary aqueous humor after subconjunctival injection of 10mg (0.5 ml) in the rabbit eye reached the peak value of 8.06μg/ml after 1/2 hour.
    3. The concentration of fortimicin in plasma and primary aqueous humor after intramuscular injection of 200mg in patients of cataract before operation reached the value of 8.85μg/ml and 0.74μg/ml after 1 hour.
    4.Fortimicin was administered to 5 cases of internal hordeolum and 2 cases of corneal ulcer.
    Clinical effects were excellent in 3 cases, good in 2 cases and fair in 2 cases.
    Side effect was observed diarrhea, but the causal relationship with fortimicin was unknown.
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  • FUMIO KOMODA, YOSHIYUKI IHARA, SHIGEKI YOKOYAMA, TADAO GOTO
    1982 Volume 35 Issue 6 Pages 1399-1401
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A new aminoglycoside antibiotic, fortimicin, was administered intramuscularly at a dose of 200 mg, and the tissue distribution of the drug was investigated with time-course in the uterine fundus, uterine cervix, oviduct, endometrium and ovary.
    Patients who required total hysterectomy or uterine appendices resection due to uterine myoma,etc. were studied.
    The uterus levels of fortimicin were about 2 mcg/g at 2 hours after intramuscular administration in the uterine fundus and uterine cervix and reduced to trace after 8-9 hours.
    The genital organs levels of fortimicin were ranged from 0.71 to 4.6 mcg/g at 1-3 hours after intramuscular administration and then reduced to the levels of 0.79 mcg/g in the oviduct, of 0.25 mcg/g in the endometrium and of 0.45mcg/g in the ovary after 5 hours.
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  • 1982 Volume 35 Issue 6 Pages 1402-1404
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • TOSHIMITSU UCHIYAMA, MADELEINE LEMEIGNAN, PAUL LECHAT
    1982 Volume 35 Issue 6 Pages 1405-1410
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    It is known that aminoglycoside antibiotics can produce theneuromuscular blockade which is mainly based on their antireleasing action of acetylcholine (Ach) at neuromuscular junctions1, 2). The neuromuscular blocking actions of kanamycin sulfate (KM) were firstly reported in vivo by TIMMERMAN et al.3) and its presynaptic blocking action was suggested by SINGHet al.4). Furthermore, pre-and post-junctional blocking actions of KM were clearly showed in vitro, and it was confirmed that KM can act preferentially at the presynaptic site and that the antireleasing action of KM can be completely antagonized by 3, 4-diaminopyridine in vitro2)3, 4-Diaminopyridine can reverse the neuromuscular depression by amikacin5), polymyxin B, lincomycin and clindamycin6) in vitro and 4-aminopyridine (4-AP) can reverselincomycin-pancuronium-induced neuromuscular blockade in man7). KM has not only the neuromuscular blocking action but also the cardiovascular depressive action8)as have the other aminoglycoside antibiotics9, 10, 11, 12, 13).
    The aim of this study was to examine whether, as in vitro experiments of neuromuscular system, 4-AP could antagonize the neuromuscular and cardiovascular depressive actions of KM in anesthetized rats.
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  • I.MICROBIOLOGICAL ASSAY METHOD, AND ABSORPTION DISTRIBUTION AND EXCRETION IN RATS
    AKIO TACHIBANA, CHIEKO IKEDA, KUNIICHIRO YANO
    1982 Volume 35 Issue 6 Pages 1411-1426
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The 15-lactam and aminoglycoside groups of antibiotics are often used in combination.This paper reports a bioassay method for each of cefotetan and sisomicin concentration in body fluids, and pharmacokinetics of both drugs following intravenous administration of cefotetan and intramuscular administration of sisomicin alone and in combination to rats.
    As to cefotetan determination, a previously reported bioassay method was modified by increasing the NaC1 concentration in the sensitivity test agar from 0 to 6%, using Bacillus subtilis ATCC 6633 as the test organism. To assay for sisomicin in the presence of cefotetan, Pseudomonas aeruginosa ATCC 8689, resistant to the j3-lactam antibiotic, was used.
    Cefotetan (20 mg/kg intravenous) and sisomicin (10 mg/kg intramuscular) were administered concomitantly to rats.The mean plasma concentrations of cefotetan and sisomicin were 16.3 μg/ml and 16.1fÈg/ml, at 30 minutes after administration respectively. The concentrations were declined to 2.20fÈg/ml for cefotetan and 2.53fÈg/mi for sisomicin at 90 minutes after dosing administration.The calculated plasma half-lives (T 1/2/3) were 21.3 minutes for cefotetan and 22.2 minutes for sisomicin.The plasma and tissue concentrations of cefotetan administered in combination with sisomicin were nearly the same as those of cefotetan alone. Urinary excretion of cefotetan and sisomicin in the concomitant administration was carried out in rats. Recoveries in urine were 45.9% of the dose for cefotetan and 85.6% of the dose for sisomicin for a period of 24 hours. When each drug was administered alone to rats, cefotetan and sisomicin were recovered 49.8% and 81.6%, respectively, of the dose in the 24-hour urine.
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  • II. ABSORPTION AND EXCRETION IN DOGS
    CHIEKO IKEDA, AKIO TACHIBANA, KUNIICHIRO YANO
    1982 Volume 35 Issue 6 Pages 1427-1436
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Beagle dogs.The mean plasma concentrations of cefotetan administered in combination with sisomicin at the above dosages were 98.0μg/ml at 5 minutes, 45.7μg/ml at 30 minutes and 3.46μg/ml at 4 hours. These plasma concentrations of cefotetan were similar to those of cefotetan administered alone to the corresponding dogs.The calculated plasma half-lives (T1/21β) of cefotetan were 53.9 minutes in combination with sisomicin and 57.4 minutes alone.The excretion of cefotetan in dog urine were 52.4% and 50.2% of the dose after administration in combination with sisomicin and alone, respectively, during 24 hours.The results indicate that there were no significant differences in the pharmacokinetics of cefotetan alone or in combination with sisomicin in dogs.
    The maximum concentrations of sisomicin in dogs administered in combination with cefotetan were 20.2μg/ml at 30 minutes after dosing. The concentrations of 11.7μg/ml at 2 hours and 3.13μg/ml at 4 hours of administration were maintained in plasma.The calculated plasma half-lives of sisomicin were 68.8 minutes in combination with cefotetan and 86.4 minutes alone.The urinary recoveries of sisomicin were 79.3% and 76.1% in combination with cefotetan and alone, respectively, during 24 hours.There were no significant differences in the pharmacokinetics of sisomicin alone and in combination with cefotetan in dogs.
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  • KOJI OKAMOTO, YUKIHIKO TOKUNAGA, MAMORU FUKUYAMA, YUKIKATSU OKADA, SAT ...
    1982 Volume 35 Issue 6 Pages 1437-1440
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Seven patients who were performed thoracotomy for the disease of the chest, were administered cefotiam dihydrochloride 2.0 g for about an hour by intravenous drip infusion during their operation. Antibiotic levels of serum and intrathoracic tissues (a piece of lung parenchyma, parietal pleura, pulmonary hilar lymph node, chest wall muscle, pulmonary cyst and nerve) were determined, and an evaluation of bactericidal effect was discussed.
    In this study, we found that antibiotic level of poor blood suppled lung, so called the destroyed lung was remarkably high.This means that a high concentration of cefotiam dihydrochloride to intrathoracic tissue is effective against postoperative infection.
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  • TETSUO UETE, YUKIE TSUZAKI, SETSUKO FURUKAWA, KIYOMITSU MATSUO
    1982 Volume 35 Issue 6 Pages 1441-1461
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Reliability of cefotiam disc diffusion susceptibility test was investigated for determining whether the disc results correlate with minimal inhibitory concentration (MIC) or not.The results of Showa disc and Oxoid disc were well correlated.The inhibitory zone size of Showa disc and MIC were also well correlated, indicating reliability of the cefotiam disc test. The disc result, was observed over 84% of clinically isolated S.aureus, S.epidermidis, S.pneumoniae, S.pyogenes, E.coli, K.pneumoniae, P. mirabilis and H.influenzae.Their mean MICs were less than about 1.5 μg/ml.Such a result should be useful for the determination of drug dose in various clinical conditions in order to obtain the proper drug levels in blood and tissues.
    The results of antibiotic disc diffusion susceptibility test with various bacteria isolated from clinical materials were compared.
    Cefotiam revealed a potent antimicrobial activity against Gram-positive cocci, showing a similar potency to that of cephalothin and cefazolin.However, it showed a stronger activity againt Gramnegative bacilli than that of cephalothin, cefazolin, cephalexin and cefoxitin, revealing less resistant strains. Cephalosporins developed recently such as cefotaxime, cefoperazone, ceftizoxime, latamoxef etc. show very potent antimicrobial activity against Gram-nagative bacilli, but their activity against S. aureus and S. epidermidis is weaker than that of cefotiam, cephalothin, cefazolin etc. Therefore, cefotiam can be considered as one of the drugs of first choice for surgical perioperative prophylaxis and blind therapy.
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  • TAKASHYI OSHIDA, TADAHIRWO ATANABE, TOMOKSOH OMURA, SAWAKOS OMEYA, RYO ...
    1982 Volume 35 Issue 6 Pages 1462-1474
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Midecamycin acetate is a diacetyl derivative of midecamycin1, 2), a macrolide antibiotic with a 16-membered ring, prepared by introducing acyl groups to 9 and 3position of its parent compound, as shown in Fig.1. 3) Its metabolic pathway and chemical structures of its metabolites have already been elucidated from a study on its metabolism4, 5)(Fig.1).
    In the present study midecamycin acetate and its metabolites were evaluated bacteriologically both in vitro and in vivo with following results.
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  • YOSHIKIYO TOYONAGA, YOSHIIE KUROSU, MORIMASA SUGITA, MAKOTO HORI
    1982 Volume 35 Issue 6 Pages 1475-1492
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Laboratory and clinical studies were carried out on 9, 3-diacetylmidecamycin(MOM), and the following results were obtained.
    (1) In vitro tests
    The antibacterial activity of MOM was determined against S. aureus and S.pyogenes each 54 strains, and comparison was made with the activities of EM, MDM and CEX.To MOM when the undiluted culture broth was used, the sensitivity peak of S.aureus, was found to occur in the range of0.39-0.78μg/ml, while the peak occurred at0.39μg/ml when the 100-fold dilution of the culture broth was employed. EM and MDM showed low MIC values in a small number of the S.aureus and their sensitivity distribution patterns were similar to that seen with MOM. With MOM, 11strains showed MICs of50μg/ml or more, while there were20such strains for MDM and25for EM.
    Comparison with CEX, on the other hand, showed that, when using the undiluted culture broths of the test strains as the inocula, the activity of MOM was superior by3tubes. When the100-fold dilutions of the broths were employed, however, the reverse was true: The results with CEX were superior by about 1 tube.
    The plot of the results of MOM in vitro activity against S. pyogenes revealed a wide distribution of MICs from0.05 to ≥100μg/ml when the undiluted culture broths were employed as the inocula. The curve showed2peaks of sensitivity: at0.1μg/ml and25μg/ml.When the100-fold dilutions of the culture broths were used, the MIC distribution was from0.05 to12.5μg/ml, with a sensitivity peak occurring at0.1μg/ml.In comparison with the other3test antibiotics, these results with MOM were slightly inferior.
    (2) Absorption and distribution studies
    Eight subjects, ranging in age from5to14years, were used in this study. At2hours after eating, these subjects were orally administered MOM in a dose of20mg/kg (3 subjects), 15mg/kg (2 subjects) or10mg/kg (3 subjects). The concentration of MOM in the serum was then monitored. In the20mg/kg administration group, the MOM serum concentration was 0.55μg/ml at 1 hour, 1.3μg/ml at2hours, 1.11μg/ml at3hours, 0.68μg/ml at4hours and not detectable at6hours. Similarly, in the15mg/kg administration group, the MOM serum concentration was0.60μg/ml at1hour, 0.59μg/ml at2hours and0.44μg/ml at4hours. In the10mg/kg dosage group, MOM serum concentrations was0.54, 0.48 g/ml and0.32μg/ml at1, 2and4hours. There were somemoderate differences between there3MOM administration groups in terms of the time of the peak serum concentration and the slope of the concentration decrease, but they did show a dose response.
    The urinary recovery rate during the6-hour period following the dosing was found to range from 1.24to4.24%in the20mg/kg MOM dosage group. The corresponding value was between 0.96 and 1.89%in the15mg/kg dosage group and0.73to1.87%in the10mg/kg dosage group.
    In another study, 6subjects were used;they ranged in age from4to16years. MOM was administered to these subjects in the early morning when they were in a fasting state. The dosage levels were20mg/kg and10mg/kg, and the transfer of the drug to the serum was measured. In the20mg/ kg dosage group, the MOM serum concentrations were found to be1.75μg/ml at1hour, 2.60μg/ml at 2hours, 1.61μg/ml at4hours and0.73μg/ml at6hours. The10mg/kg dosage group was found to show concentrations of1.95μg/mi at1hour, 0.73μg/ml at2hours, 0.47μg/ml at4hours and0.40μg/ml at6hours. In the previous study, when the subjects were administered MOM after a meal, MOM could not be detected in the serum at6hours after the dosing, but in these fasting subjects even the 6-hour serum concentration was higher than the4-hour concentration in the non-fasted subjects. The urinary recovery rate was determined for the 3 subjects who were administered MOM at20mg/kg in this study;their individual 6-hour values were1.97, 4.37% and 4.79%, which are in fact rather low.
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  • Clinical research group for cefmetazole YASUO ASADA
    YASUO ASADA, SETSUKO NISHIJIMA, MOTOAKI OZAKI, SHIGETARO SOTOMATSU, SA ...
    1982 Volume 35 Issue 6 Pages 1493-1510
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The therapeutic efficacy and safety of cefmetazole, a cephamycin-derived antibiotic in an injectable form were evaluated in patients with pyogenic infection in the dermatological field. Especially, it was found to be extremely effective for the skin diseases due to staphylococci or streptococci. The results obtained were the following; marked improvement in 18 cases and moderate improvement in34cases out of 61 cases, attaining efficacy of 86.7%. Side effects were noted as the rise of GOT and GPT in 3cases, which were normalized by ceasing its further administration. The MIC of cefmetazole against Staphylococcus aureus isolated out of foci was0.39-6.25μg/ml, while those of CEZ, CXM and ABPC used as the controls exceeded50μg/ml in some cases. It is considered thus, that cefmetazole, issuperior to these other antibiotics also in terms of MIC.
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  • YUTAKA FUJIMAKI, SHOZO KAWAMURA, RINYA SUGITA, HIROYUKI OHSAWA, KOICHI ...
    1982 Volume 35 Issue 6 Pages 1511-1522
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We had reported the fundamental study on the utility of a new cephem antibiotic, cefmetazole (CMZ).On the basis of the results we administered CMZ to patients to investigate its clinical utility in this study.
    1.CMZ was administered to 53patients including 4 infants.They consisted of 30cases of acute tonsillitis, 10 of peritonsillar abscess, 10 of laryngitis or pharyngitis, and 3 of sinusitis.
    2. One or 2 g CMZ was administered to an adult patient except for 1 case and0.5g to an infant patient once or twice daily for at least 3days. The method of administration was one shot intravenous injection, intravenous drip infusion or intramuscular injection.
    3.The strict criteria for evaluating the efficacy of a drug were made and used for judging the efficacy of CMZ.
    4.CMZ was clinically effective in 100% of patients with acute tonsillitis, 100% of those with peritonsillar abscess, 90% of those with laryngitis or pharyngitis, and 67% of those with sinusitis.
    5.Bacteriologically, a single sort of bacerium was isolated in most cases of acute tonsillitis, laryngitis and pharyngitis and in the half of cases of peritonsillar abscess. Two and more sorts of bacteria were isolated in the other cases. The main bacteria isolated were β-Streptococcus, S. pneumoniae and H. influenzae. Anaerobic bacteria, mostly Peptococcus spp. and Peptostreptococcus spp., were detected in peritonsillar abscess.
    6.The clinical results agreed with the clinicobacteriological results. All the bacteria detected before treatment of CMZ disappeared. CMZ also acted effectively in cases in which H.influenzae was suspected to be a causative organism.
    7.The present results of CMZ treatment were similar to those of cefazolin (CEZ) treatment published so far.
    8. Thus, CMZ was confirmed fundamentally and clinically to be a very useful drug for infection of the upper respiratory tract.
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  • SHUNKICHI BABA, HIROTAKA ITO, HARUJI KINOSHITA, KANETAKA MURAI, KENJI ...
    1982 Volume 35 Issue 6 Pages 1523-1552
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefmetazole (CMZ) was compared to cefazolin (CEZ) for efficacy and safety in the treatment of suppurative otitis media (including acute otitis media and chronic otitis media in acute aggravating stage) under well controlled clinical trials.The therapeutic effects were analysed statistically in172 patients (82 administered CMZ, 90administered CEZ).The adverse reactions were also analyzed statistically in199patients (CMZ99, CEZ100) in whom the judgement was possible.
    1.The efficacy rate of CMZ (72.3% for good to excellent response) was assessed by physicians in charge to be similar to that of CEZ (59.3%). This was the same being assessed by the committee, too (CMZ64.6%, CEZ56.7%)
    2.When patients were classified into 2groups (acute otitis media, chronic otitis media in acute aggravating stage) with respect to diagnosis, statistically significant difference in clinical efficacy assessed by physiciants in charge was observed in the cases with chronic otitis media (CMZ, CEZ). In addition, the improvements of flares on the drum membrane and the mucous membrane of eardrum were significantly better in the CMZ group than in the CEZ group.
    3.Bacteriologically, 16cases (19.8%) of S. aureus were resistant to CEZ, while only 1 case (1.2%) to CMZ.CMZ was judged to be effective in 5of the 6cases in which CEZ-resistant strains were detected.
    4.Side effects were found in 2cases (2.0%) treated with CMZ: one complained of retching and abdominal pain and the other developed skin eruption. On the other hand, only1case (1.0%) developed skin eruption in the CEZ group.
    These results suggest that CMZ is a new antibiotic agent which is highly valuable in the treatment of suppurative otitis media.
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  • HAJIME KAWASAKI, YUMI YAMADA, TOMOKO TAKEI, MASATOYO AKIYOSHI
    1982 Volume 35 Issue 6 Pages 1553-1561
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The ototoxicity of netilmicin (NTL) in pregnant guinea pigs (Hartley strain) and the newborn was examined and compared to that of gentamicin (GM).
    NTL was administered intramuscularly at dose of90mg/kg to pregnant guinea pigs from day0today35of pregnancy (the early period of pregnancy) or from day42of pregnancy to1day prior to delively (the late period of pregnancy). GM at dose of45mg/kg or physiological saline were administered intramuscularly to pregnant guinea pigs during the late period of pregnancy. Four of5dams given NTL during the early period of pregnancy, 4of7dams given NTL during the late period of pregnancy, and2of4dams given GM during the late period of pregnancy died.
    No pinna reflex loss in frequency range from2to20KHz were detected in mother guinea pigs treated with NTL either during the early period of pregnancy or during the late period of pregnancy.
    GM caused a loss of pinna reflex at20KHz in mother guinea pigs treated during the late period of pregnancy. Histopathologically, no damages were detected in the cochlea of mother guinea pigs treated with NTL during the early or late period of pregnancy, whereas slight scattered loss of hair cells was seen in the vestibulum.However, GM at dose of45mg/kg, caused an incomplete scattered loss of outer hair cells in the spiral organ, moderate atrophy of the spiral ganglion cells and a partial loss of hair cells in the vestibular organs in mother guinea pigs treated during the late period of pregnancy. In newborn guinea pig from the pregnant one treated with NTL during the early period of pregnancy, there was no loss of pinna reflex. The same results were obtained in newborn guinea pigs from the pregnant ones treated with either NTL or GM during the late period of pregnancy.No histopathological damages were detected.
    The present study suggests that NTL has a minimal effect on the auditory and vestibular organs in pregnant guinea pigs and the newborn and is considered to be1of the aminoglycosides with low ototoxic potential.
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  • SACHIKO MASUDA, KOICHI DEGUCHI
    1982 Volume 35 Issue 6 Pages 1562-1566
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Clinical effects of spectinomycin (TrobicinR, 2 g, i.m., once a day) and ampicillin (1g/day, p.o., in4divided doses, for2days) given in combination on acute gonorrhea in female patients were studied, and sensitivity of isolated gonococci to each of these antibiotics was determined.
    1.Clinical effects were evaluated by cultures of gonococci from discharge collected at72hours after spectinomycin administration and12hours after the last dose of ampicillin and both subjectiveand objective clinical findings.Among20cases of gonorrhea treated, 12cases (60.0%) proved excellent in therapeutic results, 6cases (30.0%) good, 1case fair and1 case produced no response.The success rate comprising excellent and good was90.0%. The only side effect reported was pain of injection site in1case on3days after initiation of treatment, but no induration was noted.
    2.MICs of spectinomycin and ampicillin for gonococci collected from the20cases were determined. Spectinomycin showed MICs of6.25-12.5μg/ml against 108CFU/ml and3.13-12.5μg/ml against 106 CFU/ml.These values were below the blood concentration obtained at6hours after intramuscular administration of2g of spectinomycin.Ampicillin had MICs of0.1-25μg/ml against108CFU/ml and 0.1-3.13μg/ml against106CFU/ml.Five strains, MICs of which were6.25-25μg/ml against 108 CUF/ ml, wereβ-lactamase-producing.
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  • KEIZO SUZUKI
    1982 Volume 35 Issue 6 Pages 1567-1578
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    1.Clinical pharmacology: The pharmacological studies on gentamicin (GM) were carried out in some clinical patients.The peak serum level following intramuscular injection (i.m.) of GM60mg was4.69μg/ml after1hour.When same dose of the drug was given by drip infusion (d.i.) over1.5and 2 hours, the peak serum concentrations were 5.17μg/ml and5.08μg/ml, respectively.No marked differences in the results of pharmacokinetic studies between i.m and d.i.were observed.
    2.Clinical results: GM was administered in a dose of60mg once or twice a day by d.i.against 18cases with chronic complicated UTIs.The duration of treatment varied but usually5days.An overall excellent or moderate effect was seen in78%with the criteria proposed by the UTI committee.
    3.Clinical chemistry and laboratory findings: The clinical abnormal values from laboratory tests of renal, hepatic functions and peripheral hematology in patients treated with GM were observed in1 case which was a slight increase of BUN (12.5-22.2mg/di) and a slight elevation of GOT (30.8-48.6u).The abnormal values, however, returned to normal within 10 days after the discontinuance of the drug.
    4.Clinical tolerance: No adverse reactions were encountered in all treated cases.
    5.Summary: Based on the clinical pharmacology and clinical studies, drip infusion administration of GM can be given safely and effectively in treatment of chronic complicated UTI.
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  • CLINICAL EVALUATION FOR A LARGE DOSE OF AMIKACIN INJECTED INTRAVENOUSLY
    YOSHIAKI MORIYAMA, MASARU URUSHIYAMA, MASAYUKI OHNISHI, SATORU KOYAMA, ...
    1982 Volume 35 Issue 6 Pages 1579-1584
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In this study, we treated severe infections (21cases) accompanied with induction chemotherapy in20patients with acute leukemia by the combination of a large dose (600-1,200mg/day) of amikacin with other antibiotics.Infections during induction chemotherapy of acute leukemia consisted of sepsis (8cases), pneumonia (7) and others (6), and most of causative organisms were Gram-negative bacteria, such as Ps.aeruginosa (7strains), Flavobacterium (5), Serratia (3), Ps. cepacia (2), E.coli (2) and others.
    The combination chemotherapy of a large dose of amikacin with other antibiotics was found to be effective (71.4%) for such infections.Side effects were negligible except for drug eruptions.Therefore, a large dose of amikacin should be given for the treatment of severe infections accompanied with induction chemotherapy of acute leukemia.
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  • Study group of cefmenoxime in the field of obstetric and genecological infections
    ZENJIRO TAKASE, KATSUMI NODA, MOTOKI HAYASAKI, SHINICHI IWASA, RYUTARO ...
    1982 Volume 35 Issue 6 Pages 1585-1609
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The study group was organized to evaluate the usefulness of cefmenoxime (CMX) injection, anew synthetic cephalosporin, for the treatment of infections in the field of obstetrics and gynecology. Fundamental and clinical studies were made by the society and the following results were obtained.
    1. The peak distribution of CMX's MIC for E. coli, Klebsiella sp., Enterobacter sp., Bacteroides sp. and Peptococcus sp.isolated from obstetrical and gynecological infections with relatively high frequencies are 0.1, ≤0.05, 0.2, 3.13, 1.56μg/ml, respectively, with an inoculation of108cells/ml.
    2.When1g of CMX is administered by intravenous drip infusion for1hour, the maximum concentrations in various tissues of female genital organs were as follows: 14.2 and 13.2μg/g in ovary and oviduct, respectively, at1.20 hours after the start of administration, and 16.9 and 26.3μg/g in corpus uteri and cervix uteri, respectively, after 1 hour. As for the transfer to the exudate in the pelvic dead cavity, the peak concentration was 15.6μg/ml after 2.13 hours.
    3.In the clinical studies, CMX was given to 258 cases with female genital organ infections and others. As for the clinical effects, with exclusion of 3 cases in which other antibiotics are concomitantly used, responses were excellent in 76 cases, good in 162 cases and poor in 17 cases, among 255 cases in total.The efficacy rate was93.3%.
    The efficacy rates by diseases were 97.1% (68/70) for intrauterine infections, 88.8% (79/89) for intrapelvic infections, 98.4% (62/63) for adnexitis, and 100% (23/23) for infections of external genital organs.As for the clinical effects on causative bacteria, the efficacy rates were 100% (19/19) for single infections due to Gram-positive bacteria, 94.8% (55/58) for single infections due to Gram-negative bacteria, and 88.2% (15/17) for single infections due to anaerobic bacteria.And its efficacy rates were 89.6% (69/77) for mixe infection cases.
    Side effects were observed in2cases (0.8%);1case with eruption, and 1 case with diarrhea and and vomiting. As for abnormal laboratory findings, lower white blood cell count was observed in2 cases and elevation of the values regarding hepatic functions in9cases. All cases were returned to the normal after the completion of the administration.
    Cefmenoxime 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 cefmenoxime will be a useful addition to the antibiotics for the therapy of these infections.
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  • HIROYOSHI SAWADA, HIROTO ISHIKURA, YOHICHIROH IZUMI, TADAO USUI, HIROS ...
    1982 Volume 35 Issue 6 Pages 1610-1614
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefoxitin (CFX) was administered to 12 patients for evaluation of clinical effects of CFX against secondary infections complicated with hematopoietic malignancies, and the following results were obtained.
    1. The clinical effects were excellent in 1 and good in 8 out of 11 cases with efficacy rate of 81.8%. Out of 12 cases treated with CFX, 1 case was excluded from clinical evaluation because of prophylactic use.It is noted that all cases with pyelitis showed good response to CFX.
    2. The serum levels of CFX were determined in 1 patient with renal failure. After intravenous drip infusion of 2 g in 200 ml of glucose solution, the serum concentrations were 67.2μg/ml and 7.53μg/ml at 14 hours and 24 hours (after hemodialysis), respectively.
    3. No side effects attributed to CFX were observed.
    These results indicate that CFX is an effective and safe antibiotic for the treatment of severe infections accompanying hematopoietic malignancies.
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  • YOSHIKI TAKAHASHI, KAISUKE SUZUKI
    1982 Volume 35 Issue 6 Pages 1615-1622
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefoxitin (CFX) was administered to total 25 patients who were admitted to the surgical ward of the hospital.
    The results of these studies are as follows.
    1) Disc susceptibility tests of the 20 strains (many Gram-negative bacilli and 2 strains of anaerobic Bacteroides) isolated from the patients to antibiotic were performed and 17 strains were good susceptibility to CFX.
    2) In9 patients of postoperative infections, 8 patients (including 2 patients with infections due to mixed E. coli and Bacteroides) were good with the clinical efficacy rate of 88.9%.
    3) In 16 patients used for prevention of postoperative infections, 15 patients were good with the clinical efficacy rate of 93.8%.
    4) No side effects were noted due to CFX.
    The results of these studies demonstrated that CFX is safe and effective in treatment of infections and for prevention of postoperative infections in the field of gastrosurgery.
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  • INFECTIONS IN FIELD OF OBSTETRICS AND GYNECOLOGY
    MAKOTO MURAKAMI, NOBUKO KUSUDA, MAKOTO YOSHIDA, TADAYUKI ISHIMARU, TOO ...
    1982 Volume 35 Issue 6 Pages 1623-1628
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefoxitin (CFX) was administered to 14 patients with various infections and to 46 patients for the purpose of prophylaxis of postoperative infections, at daily dose of3-6 g for duration of 3-13 days.
    Out of 60 patients treated with CFX, 51 patients showed excellent or good response to CFX and effective rate was 85%. No serious side effects was observed.
    It is recognized that CFX is an excellent drug for, the treatment and prophylaxis of obstetrical gynecological infections, because of high effectiveness andsafety.
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  • JOJI NAKAMURA, KOJI YAMADA, KATSUICHI SHUTO, HIROHUTO MARUMO
    1982 Volume 35 Issue 6 Pages 1629-1648
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    General pharmacological effects of KW-1414, a new orally-active antifungal agent, were studied, and the following results were obtained.
    1. KW-1414400mg/kg, p.o.caused significant depression on spontaneous activity, prolongation of pentobarbital sodium induced hypnosis, hypothermia and augmentation of reserpine-induced hypothermia in mice.In addition, KW-1414400mg/kg, p.o.showed slight muscle relaxant and anticonvulsive activities in mice.Ptosis and slight passivity were also observed at this dose.But KW-1414100mg/kg, p.o.caused only augmentation of reserpine-induced hypothermia, and any of the above effect was not found at the dose of25mg/kg, p.o.KW-141410mg/kg, i.v.had no effect on body temperature in rats and mice, on spontaneous EEG in rabbits and on spinal reflex in cats.
    2. KW-14143mg/kg, i.v.lowered femoral blood pressure, increased femoral blood flow transiently and decreased heart rate in dogs.In isolated atria of guinea pigs, KW-1414 10-4M decreased atrial rate and atrial contractile force significantly.But KW-1414had no effect on respiratory rate, ECG and blood pressure reflex induced by bilateral carotid artery occulusion and asphyxia in dogs at the dose of10mg/kg, i.v.KW-1414100mg/kg, p.o.also had no effect on heart rate in conscious rabbits. And KW-1414 10-4m did not influenced hemolysis and hemopexis in rabbit blood.
    3. KW-1414caused dose-dependently contraction of nictitating membrane induced by adrenaline hydrochloride injection, but had no effect on that induced by electric stimulation in cats.And KW-1414 10mg/kg, i.v.had no effect on pressure-response induced by noradrenaline or acetylcholine chloride injection.
    4. KW-1414at high doses had non-specific depression on contraction of isolated smoo th muscles induced by various agonists and on spontaneous movement of isolated smooth muscles. And KW-1414 10-4m caused relaxation of isolated tracheal smooth muscle of guinea pigs.But KW-1414had no effect on intestinal propulsion in mice.
    5. KW-1414 10-4M augmented the contraction of isolated phrenic nerve-diaphragm preparation induced by electric stimulation in rats.But KW-141410mg/kg, i.v.scarcely influenced the contraction of tibialis anterior muscle-sciatic nerve preparation induced by electric stimulation in rabbits.
    6. KW-1414decreased urinary volume and electrolyte excretion in rats dose-dependently, while it had no local anesthetic activity in guinea pigs.And KW-1414had no effect on gastric secretion, on spontaneous bile excretion in rats and on dermal tissue permeability in rabbits.
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  • 1982 Volume 35 Issue 6 Pages 1649-1651
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Download PDF (444K)
  • 1982 Volume 35 Issue 6 Pages 1652-1657
    Published: June 25, 1982
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Download PDF (314K)
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