The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Volume 41, Issue 10
Displaying 1-16 of 16 articles from this issue
  • I. FERTILITY STUDY
    J. M. TESH, P. A. MCANULTY, C. R. WILLOUGHBY, C. HIGGINS, S. A. TESH, ...
    1988 Volume 41 Issue 10 Pages 1341-1351
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Lomefloxacin (NY-198), a new antibacterial agent, was administered daily by gavage to groups of 22 male and 22 female rats at dosages of 30, 100 or 300mg/kg/day. Males were dosed for 71 days before pairing and then until termination, and females were dosed for 15 days before pairing, throughout mating and until Day 7 of gestation. Females were killed on Day 20 of gestation for examination of their uterine contents. Males were killed after approximately 14 weeks treatment and their reproductive organs were weighed and retained.
    At 300mg/kg/day the majority of animals showed increased salivation, water intake was slightly increased throughout the treatment period in males and before pairing in females whereas food intake showed a slight, transient reduction during the first few days of treatment in both sexes. Body weight gain of males was marginally depressed during the first week of treatment, but no other signs of reaction to treatment were observed.
    At 30 and 100mg/kg/day some animals exhibited increased salivation after being dosed.
    At all dosages, NY-198 was without adverse effects upon mating performance and fertility, or upon survival, growth and development in utero.
    On the basis of the above results it is considered that the no effect level with respect to reproduction and breeding performance of treated F0 animals and the in utero development of the foetuses was 300mg/kg/day.
    A dosage of 100mg/kg/day was considered to be the no effect level for somatic changes in the F0 animals, and even at the highest dosage of 300mg/kg/day only slight effects were recorded on the F0 animals.
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  • II. TERATOLOGY STUDY
    J. M. TESH, P. A. MCANULTY, C. R. WILLOUGHBY, S. A. TESH, O. K. WILBY
    1988 Volume 41 Issue 10 Pages 1352-1369
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Lomefloxacin (NY-198), a new antibacterial agent, was administered daily by gavage to groups of 32 pregnant female rats of the CD strain at dosages of 30, 100 or 300mg/kg/day from Day 7 to Day 17 of gestation. Twenty-one females in each group were killed on Day 20 of gestation for examination of their uterine contents. Eleven females in each group were allowed to deliver their litters and the offspring were examined for growth and functional development.
    At the highest dosage (300mg/kg/day), there was a small reduction in maternal weight gain and a transient reduction in food intake during the treatment period. Foetal and placental weights were markedly reduced. However, survival. growth and development of F1 offspring were unaffected and, with the possible exception of a slight reduction in F2 foetal weight, their reproductive performance was unimpaired.
    At the intermediate level (100mg/kg/day), maternal body weight gain and food intake during the treatment period were slightly reduced but, with this exception, the performance of F0 females and of the F1 generation was essentially similar to that of the vehicle controls.
    At the lowest dosage (30mg/kg/day), no adverse effects were recorded on either the F0 females or the F1 generation.
    On the basis of the above results 30mg/kg/day was considered to be the no effect level for the F0 females treated during gestation while 100mg/kg/day administered during gestation to F0 females had no effect upon performance of the F1 generation.
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  • III. PERINATAL AND POSTNATAL STUDY
    J. M. TESH, P. A. MCANULTY, C. R. WILLOUGHBY, C. HIGGINS, S. A. TESH, ...
    1988 Volume 41 Issue 10 Pages 1370-1384
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Lomefloxacin (NY-198), a new antibacterial agent, was administered daily by gavage to groups of 22 pregnant female rats of the CD strain at dosages of 30, 100 or 300mg/kg/day from Day 17 of gestation to Day 21 of lactation. Females were allowed to deliver their litters and the offspring were examined for growth and functional development.
    There was a slight maternal response at the highest dosage (300mg/kg/day), including increased salivation after dosing, reduced food intake in the treated period of gestation and increased water intake during the lactation period. Gestation length was slightly increased, although remaining within the laboratory background control range; in consequence, body weight of F1 offspring at Day 1 post partum was slightly increased.
    At 100mg/kg/day, a few females showed increased salivation after dosing and there was a slight increase in gestation length. Birth weight of F1 offspring was slightly increased at 30 and 100mg/kg/day but all values were within laboratory background control ranges.
    The survival, functional responses and fertility of F1 offspring were essentially unaffected by NY-198.
    On the basis of the above results, 30mg/kg/day was considered to be the no-effect level for the F0 females treated during late gestation and lactation whilst 300mg/kg/day administered to the F0 females had no adverse effect upon their offspring.
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  • HISASHI FUNADA, TOSHIHIKO MACHI, TAMOTSU MATSUDA
    1988 Volume 41 Issue 10 Pages 1385-1389
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In an attempt to define a clinical index for the timing of blood cultures in febrile patients with acute leukemia, subjective symptoms at onset of bacteremia were investigated in a total of 109 consecutive episodes. General malaise, chills, and nausea and vomiting were most frequently observed (66%, 59%, and 50%, respectively). The gastrointestinal (GI) symptoms including nausea and vomiting, abdominal discomfort and fullness, abdominal pain, and diarrhea were encountered in 72% of all the episodes, forming the second largest group next to those closely associated with high fever. These GI symptoms were usually mild and of brief durations, and their occurrence had no relation to sites of infections or etiology of bacteremia. In some cases, nausea and vomiting were aggravated by intensive antileukemic chemotherapy or massive GI bleeding. It was thus suggested that GI symptoms, particularly nausea and vomiting, concomitant with a remarkable, sometimes abrupt rise in temperature during granulocytopenia may serve as a useful index for the timing for blood collection for culture to improve the probability of detection of bacteremia.
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  • KATSU SAIONJI
    1988 Volume 41 Issue 10 Pages 1390-1406
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Influence of human albumin on bactericidal or antibacterial activities of 11 β-lactams were examined. The 11 β-lactams included second generation cephems (cefsulodin, cefotiam and cefmetazole), third generation cephems (ceftazidime, latamoxef, cefmenoxime, cefoperazone, cefotetan and cefpiramide) and monobactams (carumonam and aztreonam).
    The micro-broth-dilution method was used to determine antibacterial activities. Bactericidal activities were determined using the time-kill method. Used in the broth-dilution method were 2 media, MUELLER-HINTON broth (MHB) and the same medium supplemented with 5g human albumin/dl (MHB-A). The first experiment was to compare minimum inhibitory concentrations (MICs) determined in MHB were compared with those in MHB-A of 6 antibiotics against Staphylococcus aureus FDA 209P JC-1, of 7 antibiotics against Escherichia coli ATCC 25922 and of 5 antibiotics against Pseudomonas aeruginosa NCTC 10490. MICs using MHB-A were higher than MIC using MHB for 2 of the 6 antibiotics against S. aureus, and for all the 7 antibiotics against E. coli, and for 3 of the 5 antibiotics against P. aeruginosa.
    The second experiment was done to compare MICs of 5 antibiotics determined in MHB-A with those determined in MHB against 10 clinical isolates of S. aureus, of 6 antibiotics against 10 clinical isolates of Klebsiella pneumoniae and of 6 antibiotics against 10 clinical isolates of P. aeruginosa. The results obtained in the second experiment were varied for different antibiotics and different strains of organisms, and same antibiotics produced different results for different strains. MICs determined in MHB-A were lower than those in MHB for antibiotics with relatively low protein binding rates against 22 of 170 isolates tested (12.9%), whereas the former was higher than the latter against 103 out of 170 isolates tested (60.6%). MICs of antibiotics with relatively high protein binding rates showed an opposite trend.
    In the third experiment, time-kill curves were determined in the 2 media for 5 antibiotics against S. aureus FDA 209P JC-1, for 6 drugs against E. coli ATCC 25922 and for 5 drugs against P. aeruginosa NCTC 10490. The concentrations of these antibiotics used were 1/2×MIC, 1×MIC and 2×MIC. MICs determined in the first experiment were used here. Time-kill curves determined in MHB-A didn't reflect MICs determined in MHB. Using MHB-A, antibiotics with lower MICs determined in MHB-A showed bactericidal activities in lower concentrations.
    Human albumin influenced antibacterial or bactericidal activities of β-lactams. The influence was significant for antibiotics with relatively high protein binding rates, but not so for those with relatively low protein binding rates. Hence we must take this into account in choosing antibiotics for treatment at hand.
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  • EVALUATION OF DISC SUSCEPTIBILITY TEST AND ITS INTERPRETATION SYSTEM
    TETSUO UETE, KIYOMITSU MATSUO
    1988 Volume 41 Issue 10 Pages 1407-1417
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In vitro activities of cefuzonam (CZON) against 273 clinical isolates were studied through the evaluation of MIC's and the results of disc susceptibility test. The MIC's were determined using the agar dilution method at an inoculum level of 106 CFU/ml. The MIC80's of CZON against Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris, Haemophilus influenzae and Citrobacter spp. were less than 0.20μg/ml. The MIC80's against Serratia marcescens and Enterobacter aerogenes were both 6.25μg/ml, and that against Pseudomonas aeruginosa was 100μg/ml. The MIC80's against Staphylococcus aureus and Staphylococcus epidermidis were 25 and 6.25μg/ml, respectively. Approximately 70% of strains of S. aureus were inhibited at concentrations less than 1.56μg/ml.
    For the interpretation of the CZON Showa 30μg disc susceptibility test, a 4 category system was used. In the 4 category system for Showa disc containing CZON, the following classification inhibitory zone diameters has been proposed:(_??_) MIC≤3μg/ml,(_??_) MIC>3-15μg/ml,(+) MIC>15-60μg/ml,(-) MIC<60μg/ml.
    Reliability of the CZON disc tests in estimating approximate MIC values was studied using Showa 30μg discs and discs prepared in this laboratory containing 1-10μg CZON. A good negative correlation was observed between inhibitory zone diameters and MIC's, showing the reliability of the disc method. The results of the test using Showa 30μg disc against various clinical isolates were accurately classified into the 4 groups except those against P. aeruginosa. Some strains of P. aeruginosa showed false positive results, exhibiting relatively larger inhibitory zone diameters compared with MIC's against these organisms. As CZON is not effective against P. aeruginosa a much better overall correlation between MIC's and the disc test would result when P. aeruginosa was excluded. With Showa 30μg discs of various cephalosporins, subclassification of strains with MIC less than 3μg/ml cannot be achieved. In this study, however, it was demonstrated that differentiation of strains with MIC's less than 0.5-1.56μg/ml was possible when discs containing 1-10μg of CZON were used.
    According to recent concepts on pharmacokinetics for antibiotics including penetration of drugs into tissues and inflammatory fluids, serum protein binding of drugs appears to be one of the important determinants of drug distribution in the body. Only free, unbound drug molecules can readily pass through capillary pores into tissue fluids except in hepato-biliary system. In addition, serum protein-bound drugs show decreased antimicrobial activities compared to unbound, free molecules. Therefore, levels of free, unbound and serum-bound antibiotics in plasma must be considered with respect to clinical efficacy.
    Based on antimicrobial activities and pharmacokinetic data obtained through the recommended modest dosage schedule (2-4g/day) for CZON, the application of MIC break points of 0.5 and 1.56μg/ml in addition of 3 and 15μg/ml appear to have clinical significance in evaluating antimicrobial activities of unbound, free CZON as well as serum bound drug. Thus the use of low dose discs (1-10μg) in addition to 30μg discs are proposed.
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  • EVALUATION OF DISC SUSCEPTIBILITY TEST AND ITS INTERPRETATION SYSTEM
    KIYOMITSU MATSUO, TETSUO UETE
    1988 Volume 41 Issue 10 Pages 1418-1429
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    To interpret of the cefoperazone (CPZ) disc susceptibility test, a 4 category system is used in Japan, but a 3 category system is used in the U. S. A. and Europe. In the 4 category interpretation system of Showa CPZ disc the following classification is used:(_??_) MIC≤3μg/ml,(_??_) MIC>3-15μg/ml,(+) MIC>15-60μg/ml,(-) MIC>60μg/ml. In the 3 category system the classification used is as follows: susceptible MIC≤16μg/ml, moderately susceptible MIC>16-32μg/ml, resistant MIC>32μg/ml, or susceptible MIC ≤32μg/ml, moderately susceptible MIC>32-64μg/ml, resistant MIC>64μg/ml, depending on dose levels, 1 or 2 g.
    Reliability of the CPZ disc susceptibility test in estimating approximate MICs by classifying the test results into 4 categories was studied using discs containing 1, 2, 5, 10, 30 and 75μg. The MICs were determined using the agar dilution method at an inoculum level of 106 CFU/ml. A good negative correlation was observed between inhibitory zone diameters and MICs, showing reliability of the test using these discs. The results obtained with discs containing 30 or 75μg of CPZ were well categorized into the 4 groups mentioned above. Some strains of Pseudomonas aeruginosa and Enterococcus faecalis, however, showed false positive results. When different break points of inhibitory zone diameters than those used for other bacteria were used for P. aeruginosa, and E. faecalis was excluded from the test, an excellent correlations were obtained.
    With 30 or 75μg discs, it was unable to subclassify strains against which MICs of CPZ were below 3μg/ml. However, with discs containing 1 to 10μg, it was possible to separate the strains against which MICs were less than 0.5μg/ml. The fact that most frequent values of MICs of CPZ against Escherichia colt, Klebsiella pneumoniae, Proteus spp., Haemophilus influenzae, Streptococcus pyogenes etc. were less than 0.5μg/ml supports the usefulness of low dose discs.
    According to recently ongoing concepts on the pharmacokinetics of antibiotics and their penetration into tissues and inflammatory fluids, serum protein binding appear to be one of the important determinants of drug distribution in the body. Only free, unbound drug molecules can readily pass through capillary pores into tissue fluids except into hepatic biliary system. Furthermore, the binding to serum proteins of antibiotics decreases their antimicrobial activity. Therefore, plasma levels of free, unbound CPZ as well as total amounts must be evaluated with respect to the antimicrobial activity.
    Based on the antimicrobial activity and pharmacokinetic data obtained with recommended modest dose schedule (2-6g/day) of CPZ, MIC break points of 3 and 15μg/ml utilized in the 4 category system are more useful than those of 16 and 32μg/ml used in the 3 category system for evaluating the antimicrobial activity of free, unbound CPZ levels in blood. Use of low dose (1-10μg) discs in addition to 30 or 75μg discs enable us to more precisely evaluate plasma levels of CPZ with respect to its clinical efficacy.
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  • KANJI SEIGA, TAKASHI SYOJI, KEN-ICHI TSUCHIYAMA, YOKO SUGIYAMA
    1988 Volume 41 Issue 10 Pages 1430-1444
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We previously reported a study on the antimicrobial action of a chemically synthesized drug, ofloxacin (OFLX) and on its transfer in. This paper describes the results of our clinical study on OFLX.
    1. Only small fractions of intra-blood OFLX were transported into female organs such as uterus, ovary and fallopian tube. Our study with the normal delivery method shows that umbilical cord blood concentrations of OFLX is a third to a sixth of maternal blood concentrations and is achieved through trans-placental transfer. Its transfer into amniotic fluid, however, is very low.
    2. Forty-one cases, including cases of female intrapelvic inflammation, urinary tract infection, puerperal mastitis, etc., were administered with OFLX at levels of 200-400mg/day for 3-40 days. OFLX were found to be effective in 35 cases.
    3. We observed 113 cases to which OFLX was administered, and found only 4 cases of gastrointestinal disturbance and 1 case of suspicion of drug eruption as side effects. Laboratory tests showed no abnormalities due to OFLX in blood, serum biochemical or urine value in the cases examined (26 to 51 cases depending on test).
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  • YOSHIAKI KUMAMOTO, SHIGERU SAKAI, TAKAOKI HIROSE, TAKUJI TSUNEKAWA, TO ...
    1988 Volume 41 Issue 10 Pages 1445-1479
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Efficacy and safety of ofloxacin (OFLX), a new quinolone antibacterial agent, were investigated in cases of sexually transmitted male urethritis and cervicitis. Chlamydial infections occupied a large part of the patients enrolled. This study was conducted in 29 institutions.
    A total of 1, 126 patients with gonococcal, chlamydial or non-gonococcal non-chlamydial infections were enrolled in the study. The general dosing regimen of oral OFLX was 100mg t. i. d. or 200mg t. i. d. for 14 consecutive days.
    Along with the clinical efficacy evaluated by doctors in charge, therapeutic and clinical efficacies were determined according to standardized evaluation criteria. The evaluation of therapeutic efficacy was based on bacterial eradication. On the other hand, clinical efficacy was determined upon the improvement in causative bacteria, WBC counts in smear (or initial urine) specimens and urethra/cervical discharges. Clinical efficacy was determined on 7 and 14 days after starting the medication, except for gonococcal infections for which the efficacy was determined on Day 3 and Day 7. The results obtained are summarized as follows.
    1. Efficacy evaluation by standardized criteria
    Therapeutic efficacy rates in gonococcal infections were 97.9% (93/95) on Day 3 and 100% (119/119) on Day 7. In chlamydial infections, the rates were 77.7% (363/467) on Day 7 and 93.6% (392/419) on Day 14. Chlamydial urethritis rated 94.8% (239/252) and cervicitis 91.6% (153/167) on Day 14.
    Clinical efficacy rates in gonococcal infections were 63.2% (60/95) on Day 3 and 95.8% (114/119) on Day 7. In chlamydial infections, they were 70.0% (327/467) on Day 7 and 89.7% (376/419) on Day 14. Chlamydial urethritis rated 88.5% (223/252) and cervicitis 91.6% (153/167) on Day 14. Clinical efficacy rates in non-gonococcal non-chlamydial infections were 93.3% (97/104) for male urethritis and 65.9% (27/41) for cervicitis on Day 14.
    2. Clinical efficacy determined by doctors in charge
    A total of 1,028 cases, 752 urethritis and 276 cervicitis cases, was evaluated by doctors in charge. Clinical efficacy rates were 90.3% for urethritis and 92.4% for cervicitis.
    3. Safety
    Safety evaluations was conducted in 1,087 patients. Side effects were observed in 23 patients among them (2.12%). None of them were deemed serious.
    General laboratory examinations were conducted for 169 patients. Abnormal findings were seen in 11 patients (6.51%) or 13 cases, all of which were minor.
    The results of this multi-center clinical trial demonstrated that OFLX is effective and well tolerated in the treatment of sexually transmitted disease (STD), both gonococcal and chlamydial infections.
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  • RANDOMIZED STUDY ON PREVENTIVE EFFICACY OF CEFMETAZOLE VERSUS CEPHALOTHIN FOR POSTOPERATIVE INFECTION OF GASTRIC AND COLORECTAL CANCER
    KANEO KIKUCHI, HIROYUKI SHIMIZU
    1988 Volume 41 Issue 10 Pages 1480-1492
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Effectiveness of prophylactic administration of cefmetazole (CMZ)(A) for postoperative infection was compared with that of cephalothin (B) using patients undergoing resection of gastric cancers or colorectal cancers as subjects in cooperation with 19 major hospitals in the Tohoku districts. Using the envelope method, each hospital allocated, at random, patients with each organ removed into groups A and B. Either drug was administrated at 4g/day (in 2 divided doses) for 7 days. Registered patients with gastric cancers amounted to 114 in group A and 113 in group B; those with colorectal cancers were 63 each in groups A and B. As to background factors, advanced cancers were found more in group A with gastric cancers, and operations took more time on the average in this group; however, there were no significant differences in other factors between the 2 groups with gastric cancers and in the all factors between A and B groups with colorectal cancers. Rates of ineffective prophylaxis judged by physicians in charge were 3.9% and 21.0%, respectively, in groups A and B with gastric cancers, and 5.0% and 20.7%, respectively, in groups A and B with colorectal cancers. Rates of ineffective prophylaxis determined by committees were 16.7% and 31.0% among the former, and 8.3% and 29.3% among the latter, respectively. Ineffectiveness rates in group A with gastric cancers or colorectal cancers were significantly lower in all the evaluations, and CMZ was, therefore, comfirmed to have stronger efficacy.
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  • TAKASHI MOTOHIRO, MASAFUMI ARAMAKI, KEIKO ODA, AKIRA KAWAKAMI, KOICHI ...
    1988 Volume 41 Issue 10 Pages 1493-1502
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A dry syrup preparation for infants and children of a newly developed 16-membered macrolide antibiotic, rokitamycin, was administered to 5 neonates and low birth weight infants of 6 to 25 days after births at a dose level of 10mg/kg on an empty stomach then plasma drug levels were determined. The dry syrup preparation was also given to a total of 19 Chlamydia trachomatis infection cases of 7 days to 8 months old neonates, low birth weight infants and infants including 12 cases of pneumonia, 2 cases of conjunctivitis and 5 non-symptomatic carriers at an average daily dose level of 48.1mg/kg in 2 to 4 doses for an average of 19 days and its clinical effects, bacteriological effectiveness, side effects and effects on laboratory test values were examined. The obtained results are summarized as follows.
    1. Because the test subjects were neonates and premature infants, obtainable amounts of blood samples were limited, thus it was not possible to determine time courses of plasma drug levels to reach their peaks. Peak plasma levels, however, were speculated to be similar to those in children. Plasma half-lives of the drug were also not determinable, but they seemed to be somewhat longer than those in children.
    2. Clinical efficacies were determinable in the 2 cases of conjunctivitis and 10 of the 12 cases of pneumonia, with excellent or good results in both cases of the former and with excellent or good results in 9 of the 10 determinable cases of the latter. Thus, the overall efficacy rate was high, 91.7%.
    3. Bacteriological efficacies were determinable in 18 cases including non-symptomatic carriers. C. trachomatis was eradicated in 16 of the cases with an overall efficacy rate of 88.9%.
    4. Diarrhea was observed in 2 cases, which were suspected as side effects of the drug.
    5. No abnormalities were observed in the laboratory test results. Judging from the above results, this drug appears to be useful for the treatment of C. trachomatis infections of neonates, low birth weight infants and infants.
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  • TAKASHI MOTOHIRO, MASAFUMI ARAMAKI, KEIKO ODA, AKIRA KAWAKAMI, KOICHI ...
    1988 Volume 41 Issue 10 Pages 1503-1516
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Rokitamycin (RKM) dry syrup, a newly developed macrolide antibiotic, was administered to children with ages between 6 months and 15 years and 10 months suffering from skin and soft tissue infections including 41 cases of impetigo, one case of staphylococcal scalded skin syndrome (SSSS) and 2 cases of subcutaneous abscess totalling 44 oases. The average daily dose level used was 31.3mg/kg divided into 3 or 4 doses, for an average of 6 days of treatment. MICs of 4 different macrolide antibiotics including RKM, erythromycin (EM), josamycin (JM) and midecamycin acetate (MDM acetate) were determined against 32 bacterial strains isolated from these cases including 30 strains of Staphylococcus aureus and 2 strains of Streptococcus pyogenes. The inoculum level used was 106 cells/ml. Among these strains of bacteria, 20 strains of S. aureus and 1 strain of S. pyogenes were also used, at the same inoculum size, for the determination of MICs of 4 β-lactam antibiotics including 3 different penicillins such as ampiciIlin (ABPC), methicillin (DMPPC) and cloxacillin (MCIPC) and cefaclor (CCL), a cephem antibiotic. RKM was then evaluated through the above treatment for its clinical efficacy, bacteriological effects, side effects and effects on laboratory test values. Obtained results are summarized as follows.
    1. Activities of drugs tested were compared to each other. MIC90 of RKM against S. aureus averaged 0.39μg/ml, and against no strains of S. aureus showed MIC values of higher than 25μg/ml, thus, the antibacterial activity of RKM against S. aureus was the highest among the 8 drugs tested. The activity of MCIPC was next highest followed by that of DMPPC. MIC determination was done on only 2 strains, or, for some drugs, only one strain, of S. pyogenes, and RKM showed activities somewhat lower than ABPC and EM, and similar to JM and CCL within the limited testing.
    2. Clinical efficacies of RKM determined by doctors in charge were 97.6% in the 41 cases of impetigo, with good or excellent efficacies were observed, 100% in the single case of SSSS and the 2 cases of subcutaneous abscess. Thus an overall efficacy on the 44 cases was rated very high, at 97.7%.
    3. Clinical efficacy rating according to accumulated scores was determinable in 37 cases including all the 3 diseases on the third day of treatment with an efficacy rate of 89.2%. Ratings were determinable on the fifth and the seventh days of treatment in 24 and 21 cases, respectively, with all the cases judged good or excellent. From these results, it seemed that 5 days or longer treatment with a daily dose level of 20 to 40mg/kg divided into 3 or 4 doses would be required to obtain an overall efficacy rate above 90%.
    4. For the determination of bacteriological effectiveness, effects of drugs on 2 species of bacteria were evaluated individually with 1 case of mixed infection. Twenty four out of 36 cases of S. aureus infections were evaluable with a bacterial eradication rate of 79.2%. Both of the 2 cases of S. pyogenes infection were evaluable with bacterial eradication observed in both cases, thus, the overall eradication rate was 80.8%. If those cases from which S. aureus had been isolated but samples for bacteriological examination became unavailable because symtoms of infection had disappeared early were included in the efficacy rating as cases of the causative organisms being eradicated, eradication would be considered to have occurred in 33 cases out of 38, thus the eradication rate would be 86.8%, which would be quite high.
    5. No side effect was observed in any of the cases. No refusal of the drug occurred, either. In a few cases examined before and after the treatment with RKM for a comparison of laboratory test values, no abnormal changes were observed.
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  • JIRO YURA, NAGAO SHINAGAWA, AKIRA MIZUNO, SUSUMU WATANABE, MASAHIDE AN ...
    1988 Volume 41 Issue 10 Pages 1517-1537
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    In order to objectively evaluate the effectiveness, safety and usefulness of the new oral cephem cefpodoxime proxetil (CS-807, CPDX-PR) for the treatment of skin and soft tissue infections, a double-blind comparative study was undertaken using cefaclor (CCL) as the control drug. CPDX-PR and CCL were administered for 7 days at daily doses of 400mg (divided into 2 portions) and 750mg (divided into 3 portions), respectively.
    A total of 243 patients (118 in the CPDX-PR group and 125 in the CCL group) was treated in this study. The effectiveness, safety and usefulness were evaluated in 222 (106 in the CPDX-PR group and 116 in the CCL group), 234 (113 in the CPDX-PR group and 121 in the CCL group) and in 223 patients (107 in the CPDX-PR group and 116 in the CCL group), respectively. There were no differences in patients' backgrounds between the 2 groups, except for the presence on the absence of surgical treatments.
    The results we obtained are summarized below:
    1. In the evaluation of clinical efficacy by the subcommittee, excellent, good, fair and poor efficacy were observed in 36, 43, 17 and 10 patients in the CPDX-PR group, respectively; the efficacy rate was, therefore, calculated to be 74.5%. As for the CCL group, respective results were observed in 50, 39, 17 and 10 patients, indicating an efficacy rate of 76.7%. There was no significant difference between the 2 groups. Improvement rates judged by physicians in charge were 80.2% in the CPDX-PR group and 88.8% in the CCL group. Moreover, no significant difference in diseases or severity were found between the 2 groups.
    2. As for the bacteriological efficacy, the 2 groups showed high elimination rates, as 90.1% and 91.6% of the disease causing bacteria were eliminated in the CPDX-PR group and in the CCL group, respectively. Elimination rates in single infections with Staphylococcus aureus were determined to be 85.7% in the CPDX-PR group and 85.0% in the CCL group.
    3. Although 6 patients in the CPDX-PR group and 2 patients in the CCL group developed side effects, which were mainly gastrointestinal symptoms, there was no significant difference in the incidence of side effects between the 2 groups. Abnormal laboratory values were found in 5 patients in the CPDX-PR group and 1 patient in the CCL group.
    4. There was no significant difference in the usefulness between the 2 groups.
    Based on these results, it was judged that CPDX-PR is useful for the treatment of skin and soft tissue infections, as CCL.
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  • SHIGEKI ODAGIRI, KEIICHIROU MATSUNAGA, KANEO SUZUKI, KOU MUROHASHI, HI ...
    1988 Volume 41 Issue 10 Pages 1538-1544
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Twelve patients with respiratory tract infections were treated with cefpodoxime proxetil (CS-807, CPDX-PR), a new cephem antibiotic. It was given orally at a dose of 200mg 2 times a day for 4-15 days. Its clinical effects were evaluated as excellent in 1 case, good in 9 cases and poor in 2 cases. The efficacy rate was 83.3%. Its bacteriological effects were evaluated as eradication in 5 strains and decrement in 1 strain. The eradication rate was 83.3%. No adverse reactions and disorder of laboratory findings due to CPDX-PR were observed.
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  • TETSURO CHIMURA, MASAKI NAKAHARA
    1988 Volume 41 Issue 10 Pages 1545-1549
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The antibacterial activity of human cervical mucus in non pregnant or pregnant women were investigated employing the standard blood agar plates. Antibacterial activity of lysozyme and combined effect of lysozyme with cefmetazole (CMZ) were also investigated.
    The results obtained are summarized as follows:
    1. Cervical mucus had an antibacterial activity against Bacillus subtilis, but had no antibacterial activity to any other organisms tested. When cervical mucus was heated at 100°C for 5 minutes, its antibacterial activity was lost.
    2. Antibacterial activity of cervical mucus combined with CMZ were obtained againstStreptococcus pyogenes only, and no effect was observed against other organisms.
    3. Lysozyme had an antibacterial activity against Escherichia coli, B. subtilis, Staphylococcus aureus, Bacteroides fragilis, but when combined with CMZ no antibacterial activity was observed.
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  • NAOKI KATO, HARU KATO, KYOKO OTSUBO, AKIHISA TAKEDA, YASUHISA ITO, MIN ...
    1988 Volume 41 Issue 10 Pages 1550-1556
    Published: October 25, 1988
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The in vitro activity of minocycline (MINO) against Chlamydia trachomatis and its efficacy in the treatment of C. trachomatis-associated nongonococcal urethritis were investigated. Six isolates of C. trachomatis were inhibited at 0.06μg/ml of MINO and 5 isolates at 0.03μg/ml. All cases received oral MINO twice daily for 7 or more days in doses of 100mg. In 5 of 31 cases, 2g of spectinomycin was intramuscularly administrated together with MINO only once. C. trachomatis was eliminated in all cases tested. Excellent results were obtained in 26 cases (84%); urethral discharge and polymorphonuclear cells (PMN) disappeared or decreased to normal levels (3 cells/hpf or less) in these cases. Ureaplasma urealyticum was isolated from 8 cases, 7 of which became free of ureaplasmal infection. MINO seemed to be less effective on the decrease of PMN in the urethral smear in cases infected coincidentally with C. trachomatis and U. urealy-ticum than in cases infected with C. trachomatis alone. No subjective side effects were observed in any of the 31 cases studied. In conclusion, MINO was a useful antimicrobial agent for the treatment of C. trachomatis- and U. urealyticum-associated nongonococcal urethritis.
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