[in Japanese]

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Bacteria clinically isolated from patients of otitis media and otitis externa were collected from various medical facilities across Japan during years 1988, 1990 and 1992, and minimum inhibitory concentrations (MICs) of cefmenoxime and of reference drugs were determined against these strains. A comparative analyses of the obtained results revealed some trends described below.
1. Methicillin-resistant Staphylococcus aureus (MRSA), multiple drug resistant Coagulasenegative staphylococci (CNS) and multiple drug resistant Proteus spp. showed a year to year trend toward a steady increasing. Relative frequencies of occurrence of MRSA in these years, however, remained comparable to that of early 1980's.
2. A year to year trend toward increasing was also found for resistant or insensitive Streptococcus pneumoniae to penicillins and cephems.
3. Multiple drug-resistant Pseudomonas aeruginosa strains were also detected but they showed no trend toward increasing.

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In order evaluate antimicrobial activities of cefodizime (CDZM), minimum inhibitory concentrations (MIC's) of CDZM and other control drugs were determined against various clinical isolates, that were sent to our center from nation-wide medical institutions or were isolated and identified in our laboratory from various specimens of infected patients.
The followings are a sumary of the results:
1. Bacterial species with no or few strains resistant to cephems including CDZM included Streptococcus pyogenes, Haemophilus influenzae, Citrobacter diversus, most of Klebsiella pneumoniae and Proteus mirabilis. Some strains of Klebsiella oxytoca were resistant to cephems increases in β-lactams resistant Streptococcus pneumoniae and cephem resistant Escherichia coli seemed likely. Among Citrobacter freundii, Enterobacter spp., Serratia marcescens, Proteus vulgaris, Morganellamorganii and Providencia spp. belonging to a category of so-called “mildly toxic bacteria”, high portions of the strains examined were resistant to cephems including CDZM and these strains were also resistant to new quinolones, thus they showed multiple drug resistance.
2. MIC₉₀'s of CDZM against Streptococcus spp., H. influenzae, Moraxella subgenus Branhamella catarrhalis, E. coli, Klebsiella spp. and P. mirabilis, frequently found in daily treatment of infections, were less than ≤0.025 to 1.56 μg/ml. This indicates that CDZM would be expected to have enough antibiotic activity in infections caused by above mentioned bacteria. However, cautions are needed in the treatment of infections by β-lactam resistant S. pneumoniae, cephem resistant E. coli and cephem resistant K. oxytoca with CDZM.
3. Among the above mentioned “mildly toxic bacteria”, many multiple drug resistant strains exist. Therefore, we evaluated an usefulness of concomitant use of CDZM with aminoglycosides in the treatment of infections by these bacteria, using other reports which indicates the usefulness in vitro and in vivo.
4. Antibacterial activities of CDZM we observed in this study seem to indicate that CDZM concentrations in infected areas are maintained at above MIC levels for relatively long periods of time.

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The in vitro activity of cefpirome (CPR) was compared with that of cefazolin (CEZ), cefotiam (CTM), flomoxef (FMOX), cefotaxime (CTX), ceftazidime (CAZ) and imipenem/cilastatin (IPM/CS) against 384 clinical isolates, for tested by the broth microdilution method. The activity of CPR against Staphylococcus aureus (MIC₅₀, 1 μg/ml) and Enterococcus faecalis (MIC₅₀), 8 μg/ml) was better than CTX and CAZ, but slightly less than IPM/CS. CPR and other antibacterial agents were not effect against methicillin resistant S. aureus and Enterococcus faecium. The activity of CPR against Enterobacteriaceae was as good as that of CTX, CAZ, and IPM/CS, and more effective than CEZ, CTM and FMOX. The MIC₅₀ of CPR for Acinetobacter calcoaceticus (2 μg/ml) and the MIC₅₀ of CPR for Pseudomonas aeruginosa (8 μg/ml) were as good as that of CAZ. Conclusionly, CPR was a new broad spectrum cephalosporin as compared with used cephalosporins.

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Minimum inhibitory concentrations (MICs) were determined for polymyxin B (PL-B), gentamicin, ofloxacin and norfloxacin against clinically isolated microbial strains collected since November 1992, and the following conculusions were obtained:
1. Judging from the MIC distribution of PL-B against the studied strains including multi-drug resistant organisms of major strains of family Enterobacteriaceae, such as Escherichia coli, Klebsiella pneumoniae, Enterobacter spp., and Pseudomonas aeruginosa, it appeared that no PL-B resistant strains were detected among those Gram-negative organisms within the antimicrobial spectrum of PL-B.
2. MICs of PL-B against most strains including methicillin resistant Staphylococcus aureus and coagulase-negative staphylococci were distributed between 100 and 800 μg/ml. These results supported reports of other investigators that the eradication of Staphylococcus spp. including MRSA (methicillinresistant S. aureus) was possible by the use of PL-B at 1 mg/ml.
3. MIC distribution of PL-B against organisms of the Bacteroides fragilis group was almost the same as the results described above.

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The therapeutic efficacies of 1% neticonazole (SS717) cream and solution on experimental cutaneous Candida albicans infection produced in prednisolone-treated guinea pigs were compared with those of 1% bifonazole (BFZ). Active preparations or blank vehicles were applied once daily for 3 consecutive days starting 5 days postinfection. Therapeutic effects were assessed on the basis of viable counts recovered from the infected loci 9 days postinfection. In animals treated with SS 717 or BFZ cream, a significant mycological improvement was observed when compared to untreated controls. A significant therapeutic efficacy of a SS717 cream compared to cream vehicle was also noted, while there was no significant difference in the recovery of Candida between the untreated control group and the cream vehicle-treated groups. The mycological result of the SS717 solution treated group was significantly superior to those of the untreated control group, the solution vehicle-treated group and the BFZ solution-treated group. The treatment with a solution vehicle or a BFZ solution appeared to lower, though not to a significant level, viable counts at the infected loci.
These results led us to the conclusion that both SS717 cream and solution preparations exhibited significantly superior activity to that of BFZ in experimental cutaneous candidasis of guinea pigs.

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Efficacy of fluconazole (FLCZ), an anti-fungal agent of triazole derivatives, was evaluated in patients with systemic mycoses and suspected mycoses associated with hematologic malignancies including leukemia, myelodysplastic syndrome and malignant lymphoma. Plasma β-D-glucan levels, the differences between the levels determined toxicolor test and in endospecy test, were also investigated.
Fourteen patients with systemic mycoses and 31 patients with suspected mycotic infections were treated with intravenous administration of FLCZ at a daily dose of 400 mg. Exellent to good responses were observed in 4 of the 14 patients (28.6%) with definitive diagnosis of mycosis, and in 18 of the 31 patients (58.1%) with suspected fungal infections, with an overall efficacy rate of 48.9% (22/45).
Levels of plasma β-D-glucan correlated well with efficacies of FLCZ in 19 of 30 patients. In several cases, however, plasma β-D-glucan levels were low during the entire course of treatment. Even in 10 cases of definite mycosis, 4 cases showed low levels of plasma β-D-glucan (below 15 μg/ml by repeated determinations).
The results indicate that FLCZ is an effective agent for the treatment of severe systemic fungal infections in patients with hematologic disorders. Deep seated mycosis cannot be ruled out even when its plasma levels of β-D-glucan are low.

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We evaluated the efficacy and safety of combination therapy with sulbactam/cefoperazone (SBT/CPZ) and amikacin sulfate (AMK) in severe infections associated with hematological disorders.
The clinical efficacy rate in 82 evaluable patients was 70.7%. The efficacy rate in sepsis from which causative organisms were isolated was high, 75% (3/4). No siginificant difference was found between those cases for which no previous antibiotic therapies were made and those for which antibiotic therapies were done and changed to the combination during the course of the therapies.
No side effects nor substantial abnormal laboratory test results attributable to the test drugs were observed.
From these observations, we have concluded that the combination therapy with SBT/CPZ plus AMK is a very useful empiric therapy for severe infections associated with hematological disorders.

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Clinical effects of sulbactam/cefoperazone (SBT/CPZ) was studied on variety of bacterial infections in the fields of internal medicine focused mainly on respiratory infections. The total 135 infections were consisted of 103 respiratory infections, 15 urinary tract infections, 4 sepsis, 7 biliary tract infetions, and 6 other infections, of which 86 patients had underlying diseases. The daily doses of SBT/CPZ were 2 to 6 g divided into 2 to 3 times i. v. or d. i. v., and the duration of administration was from 3 to 35 days.
The clinical effects were judged by the attending doctors based on the changes in fever, cough, rales, chest rentogenograms, white blood cell counts, CRP values, ESR, etc. The total efficacy rate was 76.9%, and 69.0% of the isolated organism was eradicated by SBT/CPZ.
The side effect was noted in 1 case, and the abnormal laboratory findings were noted in 1 case, however it was difficult to determine whether they were due to SBT/CPZ.
These results suggest that the clinical usefulness of SBT/CPZ for the infections in the fields of internal medicine.

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Carnitine metabolism was studied in 16 pediatric patients with various infections under the treatment with cefditoren pivoxil (CDTR-PI) in granular form. Pivalic acid released from pivaloyloxymethyl ester of the drug was metabolized to pivaloylcarnitine. As results, an increase in urinary carnitine excretion (predominantly as pivaloylcarnitine) and, a decrease in free carnitine concentration and a high acyl/free carnitine ratio in serum (plasma) were observed during the treatment. When the dosing was terminated, pivaloylcarnitine in plasma and then in urine disappeared, and the concentration of free carnitine, acyl/free carnitine ratio returned to the normal range. No carnitinerelated side effects were observed throughout the study.

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