Miloxacin (MLX), a new synthetic antibacterial agent, was compared to nalidixic acid (NA) for e treatment of chronic complicated urinary tract infections in a double-blind trial.
The daily dose of MLX was one half of NA, and the patients were treated with either 1.5 g of LX or 3.0g of NA for 5 days.
Of 176 patients studied, 79 were excluded and 7 were dropped out from the analysis of evaluation. 1 other patients completed the study; 47 received MLX and 43 NA. The results obtained were as follows:
1) The effective ratio of chronic complicated urinary tract infections in the MLX group was 36.2% d 34.9% in the NA group. There was no significant difference in the clinical efficacy of both drugs.
2) The responses on pyuria were effective in 36.2% of the the MLX group and in 48.8% of the NA oup. The difference was not statistically significant.
3) The effects of both drugs on bacteriuria were similar and there was no significant difference tween them.
4) The bacteriological responses on the clinical isolates showed no statistical difference in the ratio eradication of both drugs: the eradication of 46.2% in the MLX group and 61.1% in the NA group.
5) Clinical usefulness of both drugs was evaluated on each patient by each attending doctor, and 6% of the patients was evaluated as useful in the MLX group and 55.8% in the NA group. There as no significant difference in the usefulness of both drugs.
6) Clinical symptoms as side effects were observed in 5 patients of those receiving MLX (5.6%) d 9 receiving NA (10.5%).
No major abnormalities of laboratory data due to the drug therapy were observed except for incase of BUN values occurring in each one patient and increase of BUN and serum creatinine values each one patient of both groups.
The incidence of side effects showed no significant difference between the two groups.
7) These results suggest that MLX seems to be a useful substitutive drug to NA in the treatment chronic complcated urinary tract infections.

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Cefapirin, a new injectable semisynthetic cephalosporin, was administered by continuous infusion to 137 patients with genitourinary tract infections to evaluate therapeutic efficacy, antimicrobial activity and pharmacokinetic characteristic of the drug. The results obtained were as follows:
1) The clinical results of 12 patients with acute simple pyelonephritis were excellent in 8 cases (66.7%) and good in 4 cases (33.3%).
2) The clinical results of 72 patients with complicated urinary tract infections were excellent in 11 cases (15.3%), good in 16 cases (22.2%) and poor in 45 cases (62.5%).
3) The clinical results of 48 patients with infections of the male genital organ were excellent in 21 cases (43.8%), good in 19 cases (39.6%) and poor in 8 cases (16.7%).
4) Ten patients exhibited side effects: two with skin rash, one with stridor, one with nausea and vomiting, one with nausea and itching, and 5 with elavated serum transaminases.
5) Cefapirin was effective against E. coli, Streptococcus faecalis and Klebsiella while generally ineffective against Pseudomonas and Serratia.
6) The serum concentrations were higher in patients with impaired renal function.
7) Sixty-seven per cent of the administered dose was excreted in the urine during the first 6 hours of infusion in patients with normal renal function while the urinary excretion rate declined in patients with impaired renal function as a degree of impairment advanced.

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Laboratory and experimental studies on tobramycin were performed, and the following results were obtained:
1) Antibacterial activity
The sensitivity of 70 strains of Pseudomonas aeruginosa isolated from burn wounds to tobramycin was measured, and compared with that to gentamicin and dideoxykanamycin B.
Generally, in MIC values, the antibacterial activity of tobramycin was superior to that of gentamicin and dideoxykanamycin B.
2) Tissue concentration
After a single intramuscular injection of 5 mg tobramycin/kg to rabbits, the concentration of tobramycin in the serum and in the skin were determined.
The peak of concentration in the serum was obtained after 30 minutes (average 186.6μg/ml). On the other hand, the peak of concentration in the skin was obtained after 60 minutes (average 28.0μg/ml). The tobramycin level in the skin was about 20% of that in the serum.

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A strain of Neisseria gonorrhoeae producing beta-lactamase was initially isolated in Japan in October 1977. The patient was a male tourist coming back from South-East Asia through Bangkok where he presumably was infected. Although the latent period was relatively long (7 days) and the symptoms were slight, no other findings which could be distinguished from ordinary gonorrhoeae were observed. Since the patient was allergic to penicillin, the therapy was scheduled as follows which resulted in complete healing of the disease: On the 1 st day 2g followed by 1 g a day of KM on each 3rd and 5th day were injected intramuscularly. At the same time 250 mg of sigmamycin were jointly administered daily every 6 hours for 4 days from the first day of treatment.
The strain 52-45 isolated was in complete agreement in morphology, staining- and biochemical properties with the standard strain of N.gonorrhoeae. Since the beta-lactamase activity was demonstrated by either of the three tests, i. e., rapid iodometric, rapid acidometric, as well as chromogenic cephalosporin test, the strain was identified as PPNG.
The beta-lactamase activity of the strain was strongly affected by inoculum size (inocum-size effect) with PCG, ABPC, and CER, but the effect was not so pronounced with MCIPC, CET, and CEX, to which, however, its activity proved weak. The enzyme was, therefore, presumed to be TEM type (Richmond Type III), and suspected of its plasmid origin. Among other drugs, it was susceptible against TC, CM, KM, and SPEC, excepting only SM to which it was resistant.
The introduction of PPNG from outside Japan was for the first time confirmed with this case, from which the initial isolation of PPNG in Japan was made as far as the domestic report was concerned, though CDC Weekly Report has listed one figure from Japan without touching its contents.

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Acute pyelonephritis was induced by retrograde bacterial infection in female rats treated with a renal toxic agent, 2-bromoethylamine hydrobromide (BEA). The necrotic lesion was developed exclusively in renal papilla when the dehydrated rats were treated intraperitoneally (ip) with 100 to 150 mg/kg of BEA, but the cortex area of the kidneys was histopathologically normal. Three days after the treatment, the rats were infused retrogradely 1.0 ml of suspension (10⁶ bacteria/ml) of Escherichia coli, Proteus mirabilis or Pseudomonas aeruginosa via the urethra. Maximum growth of the microorganisms was observed in kidneys and bladder urine 3 to 5 days after the infection, but the bacteria were not detected in sera, spleens and lebers of same rats. The observation that the focus formation localized in the renal pelvis was confirmed histopathologically. No renal infection occurred in intact rats without BEA treatment. This model is useful for the study of renal infection and for the therapeutic evaluation of antimicrobial agents, because it is technically simple and rerpoducible in establishment of pyelonephritis.

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Cefmetazole (CS-1170) for parenteral use, a new antibiotic of cephalosporin series with marked resistance to β-lactamase, was used in 33 patients hospitalized due to acute or subacute infection of the abdominal organs; 17 patients with appendicitis, 12 with cholecystitis with cholelithiasis and others.
Cefmetazole in a dose of 1 g was given intravenously during the operation. Tissue specimens were taken from various sites of the removed organs. Tissue specimens and bile or plasma samples were subsequently taken at intervals. Cefmetazole concentration was determined according to the bioassay method with ATCC 9341 strain of Micrococcus luteus.
Cefmetazole concentration in purulent ascites and A-bile increased gradually for 1 hour, followed by a slow decline. Cefmetazole was detected in the white B-bile, obtained through the gallbladder wail at 30-40 minutes after intravenous administration.
Cefmetazole concentration in infectious gallbladder wall and inflammatory soft tissues reached the peak at 10-15 minutes after the intravenous administration, followed by a slow decline. Cefmetazole concentration in the infected gallbladder wall and appendix was directly proportional to the degree of the pathological changes of inflammation. Cefmetazole was distributed quickly in the seriously infected organ or tissue, and stayed for a relatively long time.

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A new antibiotic, piperacillin (PIPC) was applied to experimental and clinical studies. Using 10 dogs, concentrations of serum and oral tissues were investigated. The results were obtained as follows: mandibular bone marrow showed a drug level of 51. 25±24.74 μg/g after 15 minutes, 23.16 ± 10.42μg/g after 60 minutes (PIPC 100 mg/kg i. v.).
According to these experimental results, PIPC was applied clinically to 7 cases of mandibular osteomyelitis, and concentrations of the serum and the mandibular bone marrow were investigated. Results in clinical cases revealed that the drug levels in mandibular bone marrow were 11-16μg/g after 15 minutes, and 2-6μg/g after 60 minutes (PIPC 50mg/kg i. v.).

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