A new developed antimicrobial agent, NM441, was evaluated in vitro and in vivo. The results were as follows: 1) Antimicrobial activity: Minimal inhibitory concentrations (MICs) against 503 clinical isolates of 16 different species were determined, and compared with those of the other 4 kinds of drugs, norfloxacin (NFLX), ofloxacin (OFLX), ciprofloxacin (CPFX) and lomefloxacin (LFLX). NM441 showed excellent antimicrobial activities against gram positive and negative bacteria. 2) NM394 concentrations in serum and sputum: A patient with diffuse panbronchiolitis and a patient with bronchiectasis were given 200mg of NM441 orally. Another patient with bronchiectasis was given 300mg of NM441 and 1g of S·M powder. The concentrations in serum were measured at intervals. The peak concentrations in serum were observed immediately after administration orally, and reached 0.9~1.3μg/ml after 2 hours. The peak sputum levels, 0.3~0.5μg/ml, were observed in about 4 hours after administration. These results suggest that NM394 can penetrate rapidly into the sputum. However, S·M powder inhibited absorption of NM441. 3) Clinical efficacy and adverse reaction: Twenty patients with respiratory or urinary tract infection were treated with NM441. An overall efficacy were excellent in 6 cases, good in 10, poor in 2, and not evaluable in 2. Side effect was not observed in any case. As the laboratory abnormal findings, elevation of GOT and GPT in one case was observed. However, since these were mild increase, the safety of NM441 in clinical use was indicated.
|ジャーナル||Japanese Journal of Chemotherapy|
|出版ステータス||Published - 1996|
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