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Volume 46, Issue 11
Displaying 1-13 of 13 articles from this issue
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I. RESULTS AGAINST METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUSKOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUMIKO SUZUKI, SHIGEMI ...1993 Volume 46 Issue 11 Pages 939-945
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSWe previously reported a part of the results we obtained regarding antibacteriological synergism between β-lactams and vancomycin (VCM) against methicillin-resistant Staphylococcus aureus (MRSA). This paper reports an additional assessment we made subsequently to the previous report regarding antibacterial effects of different β-lactams and VCM concurrently used against MRSA. Assessed in this study were bacteriological synergistic actions between flomoxef (FMOX) and VCM, latamoxef (LMOX) and VCM, cefpirome (CPR) and VCM and imipenem (IPM) and VCM agaisnt MRSA.
I. Synergistic enhancements of therapeutic activities were observed against MRSA with FMOX+VCM, CPR+VCM and IPM+VCM, but the activity of LMOX+VCM was low.
2. Concentration dependencies of actions of these antibiotic agents against MRSA were strong for β-lactams, but weak for VCM. These observations were opposite of the results for β-lactams and aminoglycosides, or β-lactams and tetracyclines against MRSA we reported previously.
3. It appeared that strong synergistic antibacterial effects were obtained with FMOX or CPR concentrations between 8 and 32μg/ml when used with VCM, and IPM concentrations between 4 and 16μg/ml when used with VCM, hence, in the therapy using these combinations, concentrations and dose intervals of β-lactams employed should be carefully considered.
4. When these antibiotics are used together in in vitro experiments, values of MIC and FIC-index may be different depending upon experimental systems used.View full abstractDownload PDF (766K) -
II. RESULTS AGAINST GRAM-NEGATIVE RODSKOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUMIKO SUZUKI, SHIGEMI ...1993 Volume 46 Issue 11 Pages 946-952
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSEvaluations were made for antibacterial activities of combination uses of flomoxef (FMOX)+vancomycin (VCM) against clinically isolated bacteria of family Enterobacteriaceae, and latamoxef (LMOX)+VCM, cefpirome (CPR)+VCM, and imipenem (IPM)+VCM against also clinically isolated Pseudomonas aeruginosa. The obtained results are summarized as follows.
1. FMOX and VCM appeared to act independently against Enterobacteriaceae without showing synergism or antagonism.
2. Regarding antibacterial effects of LMOX+VCM, or CPR+VCM against P. aeruginosa strains, MIC values under the combined uses were approximately 1 dilution (2 folds) higher than LMOX or CPR used alone, but we did not consider that these results meant the presence of antagonism between the β-lactams and VCM.
3. Experimental results suggested that an antagonistic relationship was present between IPM and VCM against P. aeruginosa. The degree of the antagonism was dependent on VCM concentrations. In other words, when VCM is present at a concentration between 4 and 128μg/ml, MIC values for IPM increased 2 to 4 dilutions (4 to 16 folds), whereas in the presence of 1 to 2μg/ml VCM, MIC values for IPM were close to those of IPM alone. Further, some of this tendency was observed for FMOX against bacteria of family Enterobacteriaceae in the presence of VCM.
4. These results suggest that the dose level of VCM should be considered based on a low range when a combination therapy is considered between β-lactams and VCM in the treatment of infections with MRSA alone or with Gram-negative rods with MRSA.View full abstractDownload PDF (702K) -
TAKESHI TAJIMA, YASUO RONDO, SACHIKO NEGISHI, SHUICHI NISHIMURA, AKIKO ...1993 Volume 46 Issue 11 Pages 953-958
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSPharmacokinetic, bacteriological and clinical studies on S-1108 were performed in children.
The results were as follows:
1. A total of 11 patients were treated with S-1108. Each dose was 3mg/kg, orally administered 3 times daily for 4-14 days. The clinical efficacies of S-1108 in 10 patients with bacterial infections (1 with bacteremia, 4 with pneumonia, 1 with acute maxillary sinusitis, 1 with scarlet fever and 2 with streptococcal pharyngitis) were evaluated as excellent in 8 patients and as good in 2 patients with an efficacy rate of 100%. Only one patient with staphylococcal scalded skin syndrome due to methicillin resistant Staphylococcus aureus (MRSA) who received γ-globulin was not evaluated. Fourteen causative strains of 5 species were found in 10 patients. Three strains of Streptococcus pneumoniae out of 5, 2 of 3 Branhamella catarrhalis strains, none of Staphylococcus aureus and all 3 strains of Streptococcus pyogenes were eradicated.
No adverse reaction was observed in any of the 11 patients.
2. MICs of S-1108 against 5 clinically isolated S. pneumoniae from cases of infections were examined. All of them were relatively highly resistant to penicillins. S-1108 was compared with cefteram pivoxil, cefpodoxime proxetil, cefaclor and cefixime, and it showed better antibacterial activity or than other cephems.
3. Double peaks were obtained in plasma levels of S-1108 orally administered at a dose of 3mg/kg at 30 minutes after meal and were 1.03μg/ml and 0.74μg/ml at 1 and 4 hours after administration, respectively.
Based on the above results and the broad spectrum of antibacterial activity of S-1108, it is considered that S-1108 is a promising antibiotics which is usable as a single agent for a primary therapy of respiratory tract infections in children. In addition, because antibacterial activity of S-1108 against S. aureus is relatively weak, using a relatively high dose of S-1108 in patient with skin soft tissue infection may give favorable result.View full abstractDownload PDF (630K) -
HIDENORI MEGURO, ATSUO MORI, RYOCHI FUJII, ITARU TERASHIMA1993 Volume 46 Issue 11 Pages 959-966
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSA new oral cephem antibiotic, S-1108, was evaluated for its clinical efficacy and safety in children. S-1108 was effective in 95% of the 59 examined cases of respiratory, middle ear, skin and urinary tract infections. S-1108 was highly effective in infections of Streptococcus pyogenes, Haemophilus influenzae and Escherichia coli, but was less effective in penicillin-resistant Streptococcus pneumoniae and Staphylococcus aureus infections.
The serum half-life was 1.26±0.36 hours upon after meal administration of 4mg/kg. No severe adverse reaction was encountered.
From these data, S-1108 appears to be safe and effective in children with susceptible bacterial infections.View full abstractDownload PDF (702K) -
HIRONOBU AKITA, TAKAO YOKOTA, KEISUKE SUNAKAWA, SATOSHI IWATA, YOSHITA ...1993 Volume 46 Issue 11 Pages 967-977
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSLaboratory and Clinical Studies on S-1108, a new oral cephem antibiotic, were carried out to evaluate its usefulness at a dose between 2 and 4mg/kg a day for 7 to 14 days in the pediatric field.
1) Pharmacokinetic studies 5-1108 at a dose of 2mg/kg was administered to evaluate the pharmacokinetic parameters in I subject. Cmax, T1/2 and AUC were 0.69 hour, 1.42 hours and 2.15μg·hr/ml, respectively.
2) Antimicrobial activities MICs against various clinically isolated oraganisms (Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Branhamella catarrhalis, Escherichia colt and Haemophilus influenzae) were determined. The MIC values of S-1006 were similler to those of cefteram, the MICs against S. pyogenes, and H. influenzae were 0.025 and 0.10μg/ml, respectively.
3) Clinical studies S-1108 was administered to patients with various pediatrics infections in 34 cases (upper respiratory tract infections: 12 cases, lower respiratory tract infections: 5 cases, urinary tract infections: 9 cases, skin and soft tissue infection: 6 cases, otitis media: 2 cases). Clinical efficacy rate was evaluated according to “Standard of clinical evaluation in pediatrics field”. The responses were all good or excellent.
4) Side reactions
There were no serious adverse reactions in any cases. The above results suggest that S-1108 is potent effective and safe agent in the pediatric field at a dose between 2-4mg/kg (t. i. d.) a day.View full abstractDownload PDF (903K) -
KENJI NIINOU, HAJIME SATO1993 Volume 46 Issue 11 Pages 978-990
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSPharmacokinetic and clinical studies on S-1108, a new oral cephem antibiotic, were performed in pediatric infections and the following results were obtained.
1. Pharmacokinetics studies Pharmacokinetics of S-1108 was studied in 4 children (3y 7m-11y 1m) using doses of 2mg/kg (n=2) and 4mg/kg (n=2). The average peak plasma level was 0.88mg/ml at 2 hours after administration of 2mg/kg and 2.00μg/ml at 3 hours after administration of 4mg/kg, and plasma half-lives were 1.45 and 0.96 hours, respectively. Average cumulative urinary recovery rates at 0-6 hours were 30.0 and 34.8%, respectively.
2. Clinical studies
S-1108 was administered to 32 patients with various infectious diseases (6 with acute tonsillitis, 2 each with pertussis and acute bronchitis, 3 with pneumonia, 4 with scarlet fever, 5 with impetigo contagiosa, 6 with acute urinary infection and 1 each with subcutaneous abscess, impetigo, vulvitis and urethritis) at daily doses between 6-12mg/kg/day, t. i. d., for 5-12 days. Clinical responses were excellent in 17 patients, good in 13, and poor in 2, and the efficacy rate was 93.8%. Bacteria were indentified and 33 strains of 12 species were found. The eradication rate was 93.9%. No side effects were observed in 43 patients. Abnormal laboratory test values were observed in 2 patients, 1 with elevation of eosino. and the other with elevations of GOT and GPT.
The results suggest that S-1108 may be a very useful and safe drug for the treatment of pediatric infections.View full abstractDownload PDF (1240K) -
YOSHIKIYO TOYONAGA, TOSHIHIDE ISHIHARA, TOHRU TEZUKA, TOMOAKI SANO, HI ...1993 Volume 46 Issue 11 Pages 991-1002
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSParmacokinetic and clinical studies on S-1108, a new oral cephem antibiotic, were performed in the field pediatrics. The following results were obtained.
1) Antibacterial activities
Antibacterial activities of S-1006, the active form of S-1108, were studied against clinically isolated strains of (Staphylococcus aureus (n=5), Streptococcus pneumoniae (n=6), Streptococcus pyogenes (n=3), Haemophilus influenzae (n=8), Branhamella catarrhalis (n=5) and Haemophilus parainfluenzae (n=2). MIC values ranged ≤0.025-1.56 for GPC and 50.025-0.78μg/ml for GNR.
2) Absorption and excretion Blood concentrations and urinary excretion rates of S-1108 were measured upon administration of S-1108 after meal at dose of 3mg/kg (n=4), 4mg/kg (n=1) and 6mg/kg (n=1). The peak blood concentrations of S-1006 at a dose of 3mg/kg (n=4), ranged from 0.57 to 1.82/μg/ml at 1, 2 and 4 hours after dosing. Mean pharmacokinetic parameters T1/2 and AUC were 1.29±0.69 hours and 4.47±2.25μg·hr/ml, respectively. At a dose of 4mg/kg and 6mg/kg, peak concentrations were 1.79 and 1.27μg/ml at 2 and 3 hours after treatment, T1/2 and AUC were 1.34 and 1.11 hours, and 8.19 and 5.65μg·hr/ml, respectively.
Urinary recovery rates ranged from 13.0 to 37.2% for the first 8 hours after administration.
3) Clinical studies
Clinical efficacies were examined in 32 cases of various pediatric infections including 5 cases of acute pneumonia, 11 cases of bronchitis, 2 cases of scarlet fever, 8 cases of tonsillitis, 1 case of pharyngitis, 2 cases of otitis media and 3 cases of UTI. Clinical efficacy rate was 96.9% (31/32) and bacteriological eradication rate was 87.1% (27/31).
There were no side effects and abnormal laboratory test values except 1 case (Eosino. 2→10%) in the 32 cases.View full abstractDownload PDF (1247K) -
HARUHI NAKAMURA, NAOICHI IWAI, MITSUNOBU MIYAZU, YUMI WATANABE1993 Volume 46 Issue 11 Pages 1003-1016
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSWe performed laboratory and clinical evaluation of S-1108 granules, a new oral cephalosporin antibiotic, in the pediatric field.
1. Pharmacokinetics of S-1108 was examined with 6 patients, at a dose of 4mg/kg that was orally ingested 30 minutes after meal.
Mean plasma concentrations at 30 minutes, 1, 2, 4, 6 and 8 hours after dose were 0.35, 0.63, 0.86, 0.75, 0.37 and 0.09μg/ml, respectively, with a half life of 1.14 hours. The urinary recoverry rate in the first 8 hours was 25.5%.
2. The clinical efficacy of S-1108 was evaluated in 31 patients with various infectious diseases. S-1108 was administered at doses ranging 2 to 4.2mg/kg/dosage, 3 times a day for 1/3 to 10 days. Clinical effects were excellent in 19, good in 12, with an efficacy rate of 100%. Bacteriologically, all causative organisms except two of Staphylococcus aureus and Haemophilus influenzae were eradicated, with an eradication rate of 80%.
As an adverse reaction, mild diarrhea was noted in 2 patients. Slight elevations of GOT and/ or GPT were noted in 2 patients. Only 1 child had difficulty ingesting the antibiotic preparation.
From the above results, we have concluded that S-1108 is a highly effective and safe for patients with various infectious diseases in the pediatric fields.View full abstractDownload PDF (1400K) -
KUNIYOSHI KUNO, AKIMASA OGAWA, FUMIO HAYAKAWA, KAZUE ITO, MASARU KONDO ...1993 Volume 46 Issue 11 Pages 1017-1024
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSClinical studies on S-1108, a new oral cephem antibiotic, were carried out in the field of pediatrics. The following results were obtained.
1. The peak plasma level of S-1006 when administered after meal at a dose of 4mg/kg was 2.47μg/ml at an hour, and the serum half-life was 0.81 hour. The 4 hours urinary excretion rate of S-1006 was 35.7%.
2. 5-1108 was administered to 15 children with various infections (3 patients with pneumonia, 3 with acute bronchitis, 4 with scarlet fever, 2 with acute tonsillitis, 1 with phlegmon and 2 with urinary tract infections). The overall clinical efficacy rate was 100%.
3. Side effects or abnormal laboratory test values were not observed except for diarrhea in 1 and eosinophilia in 1.View full abstractDownload PDF (675K) -
KENJI KITAMURA, TOSHIAKI IHARA, HITOSHI KAMIYA, EIICHI AZUMA, MASAHIRO ...1993 Volume 46 Issue 11 Pages 1025-1029
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSWe administered S-1108 to 16 children with ages ranging from 7 month to 15 years at doses between 1.8 and 6.0mg/kg×3/day for 3 to 13 days. We evaluated the efficacy and safety of S-1108 in 11 children with respiratory tract infections, 3 urinary tract infections, and 2 skin infections. The efficacy rate of S-1108 was 100% and bacteriological eradication rate was 83.3%. No adverse effects were observed. These results suggested that S-1108 could be used safely in children.View full abstractDownload PDF (538K) -
MASARU KUBOTA, HARUKI MIKAWA, TOHRU MOMOI, SUSUMU HOSOI, HIDEKAZU NAKA ...1993 Volume 46 Issue 11 Pages 1030-1034
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTo evaluate the efficacy, the safety and the usefulness of a novel and esterified cephem antibiotic for oral use, S-1108, in pediatric infections, a clinical trial was performed. The study subjects were 15 patients including 9 with acute pharyngitis, 1 with acute tonsillitis, 2 with acute bronchitis, 1 with chronic pyelonephritis, 1 with acute abscess of the skin and 1 with impetigo contagiosa.
S-1108 was administered orally at a dose of 3.7mg/kg to 12.5mg/kg t. i. d. for 4 to 9 days.
Clinical effects were excellent in 7 cases, good in 6, fair in 1 and poor in 1. The Overall efficacy rate was 86.7%. Bacteriologically, causative organisms were all eradicated in evaluable 4 cases.
As to side effects, diarrhea was observed in 2 cases. No abnormal laboratory test values were obtained.View full abstractDownload PDF (541K) -
TADAFUMI NISHIMURA, KUMIKO SUGITA, SHIGEYUKI AOKI, MICHIO TAKAGI1993 Volume 46 Issue 11 Pages 1035-1039
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSNine pediatric patients with bacterial infections (5 cases of tonsillitis, 3 cases of impetigo and 1 case of UTI) were treated with S-1108, and the efficacy and the safety were evaluated.
The clinical responses to 5-1108 treatment were excellent in 7 cases and good in 2. The efficacy rate was 100%. Bacteriologically, the causative organisms (Streptococcus pyogenes, Staphylococcus aureus, Haemophilus parainfluenzae and Escherichia coil) were eradicated. No clinical side effects were observed.
Elevation of CK in 2 cases and eosinophilia in 1 case were noted.View full abstractDownload PDF (499K) -
1993 Volume 46 Issue 11 Pages 1040-1044
Published: November 25, 1993
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSDownload PDF (542K)
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