1. Cefmetazole (CMZ) exerted excellent antibacterial effect in vitro for E. coli, Klebsiella spp. and Staphylococcus spp. bacteria isolated from clinical specimens in high yield (more than 40%). The effect was better than that of the conventionally used cephalosporin antibiotic agents.
CMZ was also effective for anaerobic bacteria, such as Bacteroides spp., and the antibacterial spectra were broader than those of CEZ and CET.
2. Clinical effects of CMZ were examined for the postoperative traumatic infections and postoperative peritonitis in the field of surgery, and it was found that the effect of CMZ was seen in more than 80% in the both A and B groups; that is, CMZ was administered to the A group as the first choice, and CMZ was administered to the subjects to which CEZ and CET and other penicillin antibiotics were administered in vain (B group).
3. No side effects and influence on the laboratory test values were observed, and it may be said that CMZ is a safe antibiotic agent in the field of surgery.

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We carried out experimental and clinical studies on tobramycin (TOB), zand the following results obtained.
1. Antibacterial activity
Minimum inhibitory concentration (MIC) of TOB against clinically isolated 20 strains of P. aeruginosa, E. coli, K. pneumoniae, P. mirabilis, S. marcescens and S. faecalis was determined. Except of S. marcescens, the great part of those strains were under than 25 μg/ml.
2. Clinical effect
TOB was treated 11 patients with chronic complicated urinary tract infection in the dose of 40-60 mg twice a day for 5 days by intravenous drip infusion. Clinical effect was excellent in 2 patients, good in 4 and poor in 5, efficacy rate was 55%.
In bacteriological effects, eradication rate of causative 12 strains was 67%.
Side effect was not observed for all cases.

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Tobramycin (TOB) was administrated by intravenousdrip infusion for 1 hour, to 15 patients with intractable chronic respiratory tract infections due to P. aeruginosa, and the following results were obtained.
1. Criteria of clinical effects
We have made new criteria for the evaluation of the therapeutic effects on respiratory tract infections (Tables 1, 2). Clinical items were divided into 4 grades and radiographic ones into 6 to 11 grades. Each item was separately scored as followed; excellent was scored as 1 point when 3 or more grade upward-shifts were seen after the treatment, good as 2 points in case of 2 grade upward-shifts, fair as 3 points in case of 1 grade upward-shift, unchanged as 4 points in case of no shift, impairment as 5 points in case of downward-shift. The integrated evaluation of the items was made according to the average points for the evaluated items; overall excellent was 1.9 or less, overall good 2.0 to 2.9, overall fair 3.0 to 3.5 and overall poor as 3.6 or more.
2. Clinical effects
Overall clinical effects were evaluated as good in 7 cases, fair in 4 and poor in 4 out of 15 patients, and rate of good score was 46.7%. According to the dosage groups, rate of good score was 50% in the dose of 60mg three times a day, 0% in the dose of 90mg twice a day and 62.5% in the dose of 120mg twice a day.
Eradication rate of P. aeruginosa was 33.3%.
Neither adverse side effects nor abnormal laboratory findings were observed.

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Clinical studies and serum levels on tobramycin (TOB) using intravenous drip infusion were carried out and the following results were obtained.
1. Clinical results
Nineteen patients with various infections including 11 respiratory tract infections, 7 urinary tract infections and a wound infection were treated with TOB 20-60mg b. i. d. and t. i. d. by intravenous drip infusion for 1 hour during 4 to 16 days.Clinical effects were excellent in 10 cases, good in 4 cases, fair in 2 cases and failure in 3 cases. It was 73.7% of the efficacy rate of the drug.
Side effects were observed in 2 cases of oliguria and increase in BUN, S-creatinine and S-potassium.
2. Serum levels of TOB
Serum levels of TOB administrated 30 or 60mg intravenous drip infusion for 1 hour were measured in first and final administration of 8 patients.The peak serum levels were 3.1-5.0μg/ml at the end of infusion in first 60mg administration of the drug,.and 3.8-5.3μg/ml in final 60mg administration of the drug.

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[in Japanese]

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In order to evaluate the efficacy and safety ofpivmecillinam (melysin tablet, PMPC), PMPC was administered to 78 chronic UTI cases in the field of obstetrics and gynecology (posthysterectomy infection, chronic cystitis, chronic pyelonephritis and etc.). In principle, daily 400mg of PMPC was administered for 2 weeks.
(1) Overall clinical efficacy judged by doctor was evaluated in 78 cases and the result was; excellent in 17, good in 37, fair in 10, poor in 13 and unknown in 1 case with the effectiveness rate ofm 69.2%.
(2) Overall clinical efficacy judged by criteria for clinical evaluation in complicated UTI recommended by UTI study member was evaluated in 54 cases and the result was; excellent in 15, good in 20 and poor in 19 cases with the overall efficacy rate of 64.8%, the result of which was similar to that of doctor's judgement.
(3) Efficacy on pyuria was evaluated in 72 cases and it was cleared in 27, decreased in 25, unchanged in 20 and unknown in 6 cases. Efficacy on bacteriuria was evaluated in 72 cases and it was eliminated in 44, decreased in 9, replaced in 8, unchanged in 8 and unknown in 9 cases.
(4) Side effect, considered by doctors to be caused by PMPC administration, was noticed in 3 out of 78 cases (3.8%), all of which was mild gastrointestinal disturbance and the administration of PMPC, was continued. Abnormal change of laboratory finding considered by doctors to be caused by PMPC administration was noticed in 1 out of 78 cases, which was slight elevation of GOT and GPT values.
It is therefore considered that PMPC appear to be useful drug for the maintenance therapy of chronic UTI in the field of obstetrics and gynecology.

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[in Japanese]

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[in Japanese]

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Laboratory studies of CFX were performed on susceptibility of 123 strains isolated from 72 patients with septicemia by disc sensitibity method in comparison with CER and ABPC. Antibacterial activity of CFX was superior against Escherichia coli, Klebsiella, Serratia marcescens and Proteus than that of CER and ABPC, especially against Serratia marcescens and Bacteroides which were mostly resistant to CER and ABPC.
CFX was administrated to 8 patients with septicemia. Clinical effects were obtained, excellent and good in5patients and poor in3, and effective rate was 63%. No side effects were observed.
The above results indicate that CFX is mainly useful in the treatment of infections caused by Gram-negative bacilli, especially resistant to penicillins, cephalosporins, and Bacteroides.

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This clinical trial was designed to evaluate the efficacy, safety and patient tolerance of cefoxitin in 23 patients who were admitted to the hospital from March 1980 to November 1980.The daily dose of cefoxitin for 21 adult patients (ages ranged from 26 to 74 years old) were 6g for the treatment of infections, and 2 to 6g for the prevention of infections by either direct or intermittent intravenous infusions.Two children were given 100mg/kg of cefoxitin either by direct or intermittent intravenous infusions 2 to 3 times a day in divided doses.
Summary of findings:
I.Treatment of intracranial infections
1.A 60-year-old man with a brain abscess was admitted to the hospital after the unsuccessful treatment with a cephalothin for 9 days. After, the initiation of therapy with cefoxitin, given 6g a day for 3 days, the abscess was surgically removed. On the second day of treatment with cefoxitin following the operation, his highest temperature was 37.0°C and was normal on the third day of treatment.He was discharged after 12 days after the surgical procedure.
2.A 56-year-old woman with cerebrospinal rhinorrhea and meningitis after the transsphenoidal removal of pituitary microadenoma responded satisfactorily to therapy with cefoxitin, given 6g a day for 14 days after the unsuccessful treatment with a cephalothin.
II. The prevention of infections following surgical operation of the central nervous system
1. Seventeen patients undergoing surgical procedures were treated with cefoxitin for the prevention of postoperative infections.None of the 17 patients developed postoperative infections.
2. A 53-year-old man undergoing repair of cerebrospinal rhinorrhea in the possibly contaminated area was successfully treated with cefoxitin, given intravenous 2g every 8 hours for 10 days without meningitis having developed.
III.The treatment and prevention of complications
1. A 74-year-old comatose male with a brain stem concussion, who was expectorating insufficiently and had difficulty swallowing and developed into pneumonia as a complication. He was succe sfully treated with cefoxitin, given intravenous 6g a day for2weeks.
2. A 26-year-old male with a brain stem concussion complicated by pneumonia and a urinary tract infection was successfully treated with the same dose regimen of cefoxitin as the previous patient.
3. The prevention of complications
A 58-year-old male with pontine glioma undergoing a tracheotomy was administered cefoxitin for the prevention of pulmonary complication.He died of pontine glioma after the three-month treatment.
IV.Side effects
Results of skin sensitivity tests given prior to the administration of cefoxitin were negative in all of the23patients.Neither anaphylaxis nor other allergic reactions or thrombophlebitis occurred with the intravenous administration of cefoxitin. No abnormalities in blood, hepatic function or renal function were observed.Anorexia occurred in 1 patient who was given cefoxitin, 6g a day.

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[in Japanese]

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Both bacteriological and clinical studies of the effectiveness of cefoxitin (CFX) in the treatment of infections associated with abdominal surgery have been carried out at Tokyo Metropolitan Toshima Hospital from September1979through August1980.The results of these studies are summarized in the following:
1.The clinical isolates from the29surgical patients were studied and anaerobes were found in 16patients (55% of the patients).B. fragilis was found in11of the 16 patients (69%) from whom anaerobes were isolated.In all of these patients, aerobes were also isolated-most frequently E.coli or K. pneumoniae.
2.The in vitro antibacterial activity of cefoxitin (CFX) against 83 clinical isolates was compared to that of cephalothin (CET), cefazolin (CEZ) and carbenicillin (CBPC).The activity of CFX against Gram-positive bacteria was generally slightly inferior to that of the other 3 antibiotics.Among the Gram-negative aerobic organisms, CEZ was the most active against E. coli and CFX and CEZ against K. pneumoniae.However, CFX, with MIC's of 0.78-12.5μg/ml, showed the greatest activity against B.fragilis, followed by CBPC, CEZ and CET, in order of decreasing activity.
3.CFX was administered in a 1-hour drip infusion to3patients following abdominal surgery, and concentrations of CFX in the serum and the exudate were measured.Peak serum concentrations were obtained at the end of the infusion, with a mean peak level of 97.93μg/ml. Peak concentrations in the exudate were observed 30 to 60minutes later and varied from 21.10 to 56.25μg/ml.
4. Of the 20 patients administered of CFX, complete clinical and bacteriological data of anaerobic infections were available in8patients.The clinical evaluation was ‘good’ in 7 patients and ‘fair’ in 1.The bacteriological evaluation was ‘eradicated’ in 5 patients and ‘decreased’ in 3. As for side effects, elevations of S-GOT and S-GPT were observed in4of the 20 patients received CFX, but these abnormalities might also be attributable to other factors such as underlying disease, surgical intervention etc.No other side effects were found in these patients.

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Miloxacin, a novel chemotherapeutic agent, has been reported to have very potent antibacterial activity to E.coli, Klebsiella, Proteus and other Gram-negative rods and be excreted into bile at high levels.Therefore, the effectiveness of miloxacin against biliary tract infections and its excretion into bile in patients were investigated. The results were as follows:
i) Comparative studies on the excretion of miloxacin, nalidixic acid (NA) and cephalexin (CEX) into bile of patients operated in gallbladder were performed by a crossover method. The maximum concentration of miloxacin after oral administration of 500 mg ranged from 18.2 to 24.0μg/ml and were much higher than those of NA (5.3μg/ml) and CEX (3.4μg/ml). The mean recovery of miloxacin within 6 hours was 0.256%and much greater than those of NA (0.075%) and CEX (0.027%).
ii) Into bile, intact miloxacin and itsm etabolites (the glucuronides of miloxacin and M-2) were excreted but M-1 was scarcely excreted. Regression analysis of the concentrations by the bioassay compared with those of intact miloxacin by the HPLC method gave a good correlation with r=0.96.
iii) The clinical effectiveness against the biliary tract infections was investigated in 29 cases. Miloxacin showed the excellent effect in 8 cases and the good effect in 17 cases, giving an effective ratio of 86.2%.Especially, all of the cases dosed with miloxacin over 34 mg/kg in a day showed excellent or good results.
iv) The rates of clinical effectiveness were 85. 7, 80.0% and 71.4% in E. coil, Klebsiella and Proteus infections, respectively. The antibacterial activity of miloxacin against 27 strains isolated in this test was more potent than those of NA and CEX.
v) During the clinical tests, none of any side effect with miloxacin was observed in both of subjective and objective symptoms.
These results show that miloxacin is expected to be fully applicable on the therapy of biliary tract infections.

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