CLINICAL STUDIES OF T-3262 IN RESPIRATORY INFECTION

• Published in: CHEMOTHERAPY Vol. 36; no. Supplement9-Clinical; pp. 413 - 417
• Main Authors: KAWAI TAKESHI, ONAKA AKIO, TOYODA TAKEO
• Format: Journal Article
• Language: English
• Published: Japanese Society of Chemotherapy 1988; 公益社団法人 日本化学療法学会
• Subjects: T-3262; 呼吸器感染症; 喀痰内濃度
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.36.supplement9-clinical_413

We clinically evaluated T-3262, a pyridone-carboxylic acid derivative, in respiratory infection.The subjects were 12 cases: bronchopneumonia 4, diffuse panbronchiolitis 3, acute bronchitis 2 and 1 each of acute exacerbation of chronic bronchitis, bacterial pyothorax and pharyngitis. Causative organisms were 3 strains of Pseudomonas aeruginosa, 2 of Haemophilus influenzae, one each of Streptococcus pneumoniae, Streptococcus aureus, Klebsiella sp., Haemophilus parainfluenzae, Acinetobacter and Enterobacter cloacae. Two cases were superinfected and three were found with normal flora. The daily dose was 450-900 mg, and the duration of the trial was 7-42 days (mean, 20.6 days). The total dose was 3.15-21.0g and the mean was 11.7g.The bacteriological results were eradication in 5 cases, colonization in 1, and persistent infection in 2 of diffuse panbronchiolitis due to P. aeruginosa.Clinical efficacy was excellent in 2 cases (16.7%), good in 5 (41.7%), fair in 2 (16.7%) and poor in 3 (25.0%).Vomiting and upper abdominal pain was observed in one case each.For evaluation of drug transfer to sputum, 300 mg of T-3262 was administered to 2 cases of diffuse panbronchiolitis. Maximum sputum concentration was observed at 3 or 6 h at a concentration of 0.25 or 0.16μg/ml, which was 30% or 42% of that in serum. Our data showed that transfer of T-3262 into sputum was relatively good. ピリドンカルボン酸系抗菌剤T-3262を, 呼吸器感染症に投与し, 臨床評価を試みた。対象疾患は, 肺炎2例, 気管支肺炎2例, びまん性汎細気管支炎3例, 急性気管支炎2例, 慢性気管支炎の急性増悪1例, 細菌性膿胸1例, 咽頭炎1例の合計12例である。起炎菌は, Pseudomonas aerugtnosa 3株, Haemophilus influenzae 2株, Streptococcus pneumoniae, Streptococcus pyogenes, Klebsiella sp., Haemophilus parainfuenzae, Acinetobacter, Enterobacter cloacae各1株で, 複数菌感染症2例, 正常細菌叢3例であった。投与量は1日450～900mgで, 投与日数7～42日間で平均20.6日間, 総投与量は3.15～21.0g, 平均11.7gで, 細菌学的治療効果は, 治療による除菌3例, 菌交代1例, 菌不変2例 (いずれもびまん性汎細気管支炎のP. aeruginosa), 不明3例であった。臨床効果を判定すると, 著効2例 (16.7%), 有効5例 (41.7%), やや有効2例 (16.7%), 無効3例 (25.0%) であった。副作用は, 上腹部痛と嘔吐が1例ずつみられた。びまん性汎細気管支炎の2例にT-3262を300mg投与し喀痰への移行を検討したが, 最大喀痰中濃度は3および6時間後に0.25および0.16μg/mlであった。それぞれのピーク時の値で血清中濃度に対する比をみると30および42%であり, 喀痰への移行の良い薬であることがわかった。