Fig. 1 Chemical structure of KW-1070
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1 Fig. 1 Chemical structure of KW-1070
2 Fig. 2 Sensitivity distribution of clinical isolates Fig. 4 Sensitivity distribution of clinical isolates Fig. 3 Sensitivity distribution of clinical isolates Fig. 5 Sensitivity distribution of clinical isolates
3 Fig.6 Sensitivity distribution of clinical isolates Fig. 8 Sensitivity distribution of clinical isolates Fig.7 Sensitivity distribution of clinical isolates Fig.9 Sensitivity distribution of clinical isolates
4 Table 1 Serum concentration of KW-1070 in healthy volunteer 400 mg, one shot i.m. Table 3 Serum concentration of KW-1070 in IND_ injection Table 2 Urinary concentration and recovery of KW-1070 in healthy volunteer 400 mg, one shot i.m. Fig. 10 Serum concentration of KW-1070 Healthy volunteer, n=4, 400mg one shot i. m.
5 Fig. 11 Urinary concentration and recovery of KW-1070 Healthy volunteer, n=4, 400 mg one shot i. m.
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10 Table5 Overall clinical efficacy of KW-1070 in complicated U. T. I. (5 days treatment) Overall effectiveness rate 31/47 (66.0%) Table6 Overall clinical efficacy of KW-1070 classified by type of infection
11 Table 7 Bacteriological response to KW-1070 Table 8 Bacteriological response to KW-1070 Relationship between response and sensitivity of clinical isolates Table 9 Clinical efficacy on complicated U.T.I. classified by type of infection and daily dosis
12 Table 10 Clinical efficacy on acute uncomplicated pyelonephritis
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15 Table 12 Clinical abnormal values in treated cases
16 1) OHASHI, Y.; H. KAWABE, K. SATO, N. NAKAMU- RA, S. KURASHIGE & S. MITSUHASHI : In vitro and in vivo antibacterial activity of KW-1070, a new aminoglycoside antibiotic. Antimicr. Agents & Chemoth. 17 : 138 `.143, ) SAITO, A.; Y. UEDA & M. AKIYOSHI : Experimental studies on the ototoxicity and nephrotoxicity of fortimicin A. Current chemotherapy and infectious disease. Proceedings of the 11 th ICC and the 19 th ICAAC. 401-%, 403, American Society for Microbiology. Washington, D. C., ) GIROLAMI, R. L. & J. M. STAMM. Fortimicins A and B, new aminoglycoside antibiotics. IV. In vitro study of fortimicin A compared with other aminoglycosides. J. Antibiotics 30 : 564 `570, 1977 LABORATORY AND CLINICAL STUDIES OF KW-1070 IN THE TREATMENT OF CHRONIC COMPLICATED URINARY TRACT INFECTIONS KEIZO SUZUKI Department of Urology, Hiratsuka Municipal Hospital ICHIRO NAGAKUBO, HISAO MITSUI and TADASHI OGAWA Department of Urology, Tachikawa Kyosai Hospital YORIO NAIDE, NORIHIKO OKISHIO and NOBUYOSHI NAGASE Department of Urology, Clinical Laboratory of Bacteriology, School of Medicine, Fujita Gakuen University KW-1070, a new derivative of aminoglycosides was evaluated in laboratory and clinical studies. In in vitro studies, KW-1070 had two- to eight-fold stronger activity against the strains of S. marcescens, indole-positive Proteus sp. than gentamicin (GM). Against P. aeruginosa, there was no significant difference of the activity between the two drugs. However, the drug showed less potent against the isolates of E. coli, Citrobacter, Klebsiella and Enterobacter by two- to eight-fold than GM did. The concentrations of serum and urinary recovery rate after 400mg i. m. administration of KW in 4 healthy adult volunteers were assayed. The mean peak serum level was 22.2ƒÊg/ml at 0.5 hour after dosing. Six hours later, the serum level decreased to 2.9ƒÊg/ml. The urinary recovery rate was 77.0% within 6 hours. When 200mg dose of KW-1070 was administered by i. v. drip in 1 hour, the serum concentrations achieved 13.0pg/m1 on an average of 6 specimens at the end of infusion. In clinical use, 50 patients (47 chronic urinary tract infections and 3 acute pyelonephritis) were treated. KW-1070 was administered at a daily dose of 400mg or 800mg per day i. m. or i. v. d.. Overall effectiveness rate was 66.0% (31/47) in the treatment of chronic urinary tract infections with an evaluation of UTI comittee's criteria. Three cases of pyelonephritis were totally cured bacteriologically in 5 days treatments. No major side effects were noted. Only in 3 patients pain at injection sites occurred. In clinical values, a slight elevation of BUN in one case and that of GOT in another one case were observed, although they returned normal within weeks after the discontinuance of the drug. It was concluded that KW-1070 is a safe, well tolerated aminoglycoside in the treatment of stubborn urinary tract infections especially caused by S. marcescens, Proteus sp. and P. aeruginosa.
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