2108 CHEMOTHERAPY SEPT Table 1 Antimicrobial spectrum Fig. 1

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2108 CHEMOTHERAPY SEPT. 1977 Table 1 Antimicrobial spectrum Fig. 1

VOL. 25 NO. 7 CHEM 014 HERAPY 2109 Table 2 Susceptibility distribution of Staphylococcus aureus to aminoglycosides (54 strains) Table 3 Susceptibility distribution of E. coli to aminoglycosides (54 strains)

2110 CHEMOTHERAPY SEPT. 1977 Table 4 Susceptibility distribution of Proteus sp. to aminoglycosides (27 strains) Table 5 Susceptibility distribution of Klebsiella to aminoglycosides (27 strains) Table 6 Susceptibility distribution of Pseudomonas aeruginosa to aminoglycosides (54 strains)

VOL. 25 NO. 7 CH5MOTHERAPY 2111 Table 7 Serum levels of KW-1062 (40 mg i. m.) Fig. 2 Cross resistance (Pseudomonas aeruginosa 54 strains) Fig. 4 Standard curve of KW-1062 Fig. 3 Cross resistance (Pseudomonas aeruginosa 54 strains) Fig. 5 Serum level of KW-1062 (40 mg i. m. ) Test org.: B. subtilis. ATCC 6633 Medium : HIA, 5ml single laver Method : paper disc method Standard curve : using Moni -trol I serum

CHEMOTHERAPY SEPT. 1977 Table 8 Urinary excretions of KW-1062 (40 mg i. m.) Table 9 Tissue concentrations of KW-1062 Fig. 6 Urinary excretion of KW-1062 (40mg i.m.) Fig. 7 Tissue concentration of KW-1062 (20 mg/kg i. m. )

VOL. 25 NO. 7 CHEMOTHERAPY 2113 Fig. 8 Bioautogram of KW-1062 Solvent : CHCl3: MeOH: NH4OH : H2O= 1 : 4 : 2 : 1 Adsorbent : Spotfilm (Tokyo Kasei) Test org. : B. subtilis ATCC 6633

2114 CHEMOTHERAPY SEPT. 1977 Fig. 9 T. N. 59 yrs male, Haemopyothorax (rupture of herniated colon through traumatic fissure of diaphragma) Fig. 10 K. T. 47 yrs male, Local peritonitis after gastrectomy (B- II) (perforative duodenal ulcer) Fig. 11 T. M. 51 yrs male, Post-op. intra-abdominal abscess (gallstone with cholecystitis)

VOL. 25 NO. 7 CHEMOTHERAPY 2115 5) ISHIYAMA, S. ; I. NAKAYAMA, H. IWAMOTO, S. IWAI, I. MURATA & M. OHASHI : Clinical use of tobramycin in patients with surgical infection due to gram-negative bacilli. J. Infect. Diseases 134 (Suppl. ) : 178 `481 August, 1976 STUDIES ON KW-1062 IN SURGERY-ANTIBACTERIAL ACTIVITIES, ABSORPTION, EXCRETION, METABOLISM AND CLINICAL APPLICATION TAKASHI SAKABE, ISSEI NAKAYAMA, HIDEO IWAMOTO, SHIGETOMI IWAI, MUTSUMI TAKATORI, TAKAMICHI KAWABE, MITSURU OHASHI, IKUO MURATA, HIROAKI SUGIYAMA and YUKO MIZUASHI Third Department of Surgery, Nihon University, School of Medicine SHUNJI ISHIYAMA Research Institute of Sciences, Nihon University 1. KW-1062, a new aminoglycoside antibiotic, was studied on antibacterial activities, absorption, excretion, metabolism and clinical application. 2. KW-1062 has a broad antibacterial spectrum against gram-positive and gram-negative bacteria, which is similar to that of gentamicin (GM). 3. The susceptibility of KW-1062 against clinically isolated strains from surgical focuses was determined, and the following results were obtained. Antibacterial activity of KW-1062 against Staph. aureus was similar to that of GM and tobramycin (TUB), and regarding the activity against E. coli, KW-1062 was similar to dibekacin and a little less than GM. The activity of KW-1062 against Proteus sp. was similar to that of GM, and against Klebsiella, it was almost equal to that of TUB and less than that of GM. Against Pseudomonas aeruginosa, KW-1062 was as active as GM. 4. Three: healthy adults were administered 40 mg of KW-1062 intramuscularly, and 30 minutes after dosing the serum level reached the peak, 2. 47 Đg/ml. Urinary recovery of KW-1062 during 6 hours in these cases was 75. 8% on an average.

2116 CHEMOTHERAPY SEPT. 1977 5. Tissue level of KW-1062 in rats was highest in the kidney and serum, but it was not detectable in the liver. 6. Bioautogram of the urine collected from healthy adults having intramuscular administration of 40 mg of KW-1062 showed no metabolites with antibacterial activity except KW-1062 itself. 7. Clinical response to KW-1062 in surgical infectious diseases was good in 4 cases, fair in 1 case and poor in 2 cases. A dose of KW-1062 was 40-80 mg/time. It appeared effective when intramuscular injection at this dose was given three times/day. 8. As a side effect, the elevation of GOT and GPT was observed in 1 case, but it was unknown if the elevation was due to KW-1062, because of combination with another antibiotic agent. Side effect which may have been caused by KW-1062 was not observed, including of this case.

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