Clinical and basic studies on NM441 in ophthalmology
We clinically evaluated NM441, a new pyridone carboxylic acid derivative, in anterior eye infections and studied the penetration of the drug into aqueous humor of cataractal patients at 1-4.7h after oral administration. In this trial, clinical cases were: hordeolum in 1, dacryocystitis in 1, and ker...
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| Published in | Japanese Journal of Chemotherapy Vol. 44; no. Supplement1; pp. 551 - 553 |
|---|---|
| Main Authors | , , , , |
| Format | Journal Article |
| Language | Japanese |
| Published |
Japanese Society of Chemotherapy
1996
公益社団法人 日本化学療法学会 |
| Subjects | |
| Online Access | Get full text |
| ISSN | 1340-7007 1884-5886 |
| DOI | 10.11250/chemotherapy1995.44.Supplement1_551 |
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| Abstract | We clinically evaluated NM441, a new pyridone carboxylic acid derivative, in anterior eye infections and studied the penetration of the drug into aqueous humor of cataractal patients at 1-4.7h after oral administration. In this trial, clinical cases were: hordeolum in 1, dacryocystitis in 1, and keratitis in 6 patients, whose ages ranged from 59 to 80 years (mean 69 years). NM441 was given at a dose of 200mg twice daily, and the duration of treatment was 3-8 days (mean 6 days). Clinical effect was excellent in 5, good in 3 cases, and no cases were assessed as poor. No adverse effect was observed. After a single oral dose of 200mg of NM441, the aqueous level of NM394 was 0.007-0.099μg/ml, and the aqueous/serum ratio was 1.8-12.4%. From the above results, we consider NM441 to be a useful antimicrobial agent for anterior eye infections. |
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| AbstractList | We clinically evaluated NM441, a new pyridone carboxylic acid derivative, in anterior eye infections and studied the penetration of the drug into aqueous humor of cataractal patients at 1-4.7h after oral administration.In this trial, clinical cases were: hordeolum in 1, dacryocystitis in 1, and keratitis in 6 patients, whose ages ranged from 59 to 80 years (mean 69 years). NM441 was given at a dose of 200mg twice daily, and the duration of treatment was 3-8 days (mean 6 days). Clinical effect was excellent in 5, good in 3 cases, and no cases were assessed as poor. No adverse effect was observed. After a single oral dose of 200mg of NM441, the aqueous level of NM394 was 0.007-0.099μg/ml, and the aqueous/serum ratio was 1.8-12.4%.From the above results, we consider NM441 to be a useful antimicrobial agent for anterior eye infections.
新しいピリドンカルボン酸系合成抗菌剤であるNM441の前眼部感染症に対する臨床効果を検討した。また, NM441内服1～4.7時間後の白内障手術時に採取した房水中の薬剤濃度も測定した。臨床例の対象は, 麦粒腫1例, 涙嚢炎1例, 角膜炎6例で, 年齢は59～80歳 (平均69歳) であった。投与量は1日に200mg×2回で, 投与日数は3～8日 (平均6日) であった。全症例8例中, 「著効」5例, 「有効」3例であり「無効」例はみられなかった。副作用は全く認められなかった。房水中のNM394濃度は0.007～0.099μg/ml, 房水血清比は1.8～12.4%であった。以上の結果より, 本剤は前眼部感染症に対して有用な薬剤であると考えられた。 We clinically evaluated NM441, a new pyridone carboxylic acid derivative, in anterior eye infections and studied the penetration of the drug into aqueous humor of cataractal patients at 1-4.7h after oral administration. In this trial, clinical cases were: hordeolum in 1, dacryocystitis in 1, and keratitis in 6 patients, whose ages ranged from 59 to 80 years (mean 69 years). NM441 was given at a dose of 200mg twice daily, and the duration of treatment was 3-8 days (mean 6 days). Clinical effect was excellent in 5, good in 3 cases, and no cases were assessed as poor. No adverse effect was observed. After a single oral dose of 200mg of NM441, the aqueous level of NM394 was 0.007-0.099μg/ml, and the aqueous/serum ratio was 1.8-12.4%. From the above results, we consider NM441 to be a useful antimicrobial agent for anterior eye infections. |
| Author | Otani, Etsuko Yasuda, Fuyuko Hara, Jiro Kawamura, Toshihiko Kawaguchi, Satoshi |
| Author_FL | 大谷 悦子 安田 冬子 川口 敏 川村 俊彦 原 二郎 |
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| References | 1) Barza M: Principles of tissue penetration of antibiotics. J Antimicrob Chemother 8: 7-28, 1981 14) Hara J, Ozawa T, Otani E, Kawamura T: Basic and clinical studies on Fleroxacin in anterior eye infections. 17th Internal Congress of Chemotherapy, Berlin, June 23-28, 1991 4) El Baba F Z, Trousdale M D, Gauderman W J, Wagner D G, Liggett P E: Intravitreal penetration of oral ciprofloxacin in humans. Ophthalmology 99: 483-486, 1992 7) 新家 真: 抗生物質の前房内移行性-その定量的解析法について-. 日眼86: 1766-1771, 1982 13) 宮尾益也, 田沢博, 本山まり子, 鈴木明子, 大石正夫: 最近の抗菌剤の前房水内移行に関する検討-全身投与-: 318-323, 1993 9) 原二郎, 張野正誉, 岡本茂樹: 前眼部感染症に対するT-3762の臨床効果. Chemotherapy 36: 1444-1447, 1988 3) 大石正夫: 臓器内濃度および分泌物内濃度の測定とその意義. 化学療法の領域3: 847-850, 1987 8) 松本文夫, 柴孝也: キノロン薬の薬動力学. キノロン薬 (上田泰, 他編), p107-120, ライフサイエンス社, 東京, 1991 2) Wise R: Protein binding of β-lactams: the effects on activity and pharmacology particularly tissue penetration II. J Antimicrob Chemother 12: 105-118, 1983 15) 井上愼三, 松村香代子, 西原勝, 三崎昌史: ヒトにおけるロメフロキサシン内服後の特異な房水内動態-とくにメラニンの関与について-. あたらしい眼科10: 87-90, 1993 17) Bron A M, Pchinot A P, Garcher C P, Guyonnet G A, Kazmierczak A M, Schott D A, Lecoeur H: The ocular penetration of oral sparfloxacin in humans. Am J Ophthalmol 117: 322-327, 1994 6) Lesk M R, Ammann H, Marcil G, Vinet B, Lamer L, Sebag M: The penetration of oral ciprofloxacin into the aqueous humor, vitreous, and subretinal fluid of humans. Am J Ophthalmol 115: 623-628, 1993 20) Donnenfeld E D, Schrier A, Perry H D, Aulicino T, Gombert M E, Snyder R: Penetration of topically applied ciprofloxacin, norfloxacin, and ofloxacin into the aqueous humor. Ophthalmology 101: 902-905, 1994 18) Salvanet A, Fisch A, Lafaix C, Montay G, Dubayle P, Forestier F, Haroche G: Pefloxacin concentrations in human aqueous humour and lens. J Antimicrob Chemother 18: 199-201, 1986 16) 三井幸彦: フルオロキノロン剤の問題点. あたらしい眼科9: 215-223, 1992 11) 原二郎, 小沢孝好, 荒木かおる, 満田久年: Sparfloxacinの前眼部細菌感染症に対する臨床効果と房水中濃度. Chemotherapy 39: 697-700, 1991 12) 大石正夫, 他 (4施設および関連施設): 眼科領域におけるFleroxacin (FLRX) の基礎的検討ならびに臨床的評価. あたらしい眼科8: 1627-1645, 1991 10) 大石正夫, 他 (9施設および関連施設): 眼科領域における新合成抗菌剤NY-198 (Lomefloxacin) の基礎的検討ならびに臨床的評価. あたらしい眼科6: 1041-1065, 1989 5) 大石正夫, 宮尾益也, 阿部達也, 本山まり子: 抗菌剤の薬動力学的パラメーターと眼感染症に対する臨床効果-経口セフェム剤について-. 眼臨87: 1711-1714, 1993 19) von Gunten S, Lew D, Paccolat F, Vaudaux P, Brazitikos P D, Leuenberger P M: Aqueous humor penetration of ofloxacin given by various routes. Am J Ophthalmol 117: 87-89, 1994 |
| References_xml | – reference: 3) 大石正夫: 臓器内濃度および分泌物内濃度の測定とその意義. 化学療法の領域3: 847-850, 1987 – reference: 4) El Baba F Z, Trousdale M D, Gauderman W J, Wagner D G, Liggett P E: Intravitreal penetration of oral ciprofloxacin in humans. Ophthalmology 99: 483-486, 1992 – reference: 6) Lesk M R, Ammann H, Marcil G, Vinet B, Lamer L, Sebag M: The penetration of oral ciprofloxacin into the aqueous humor, vitreous, and subretinal fluid of humans. Am J Ophthalmol 115: 623-628, 1993 – reference: 8) 松本文夫, 柴孝也: キノロン薬の薬動力学. キノロン薬 (上田泰, 他編), p107-120, ライフサイエンス社, 東京, 1991 – reference: 13) 宮尾益也, 田沢博, 本山まり子, 鈴木明子, 大石正夫: 最近の抗菌剤の前房水内移行に関する検討-全身投与-: 318-323, 1993 – reference: 14) Hara J, Ozawa T, Otani E, Kawamura T: Basic and clinical studies on Fleroxacin in anterior eye infections. 17th Internal Congress of Chemotherapy, Berlin, June 23-28, 1991 – reference: 19) von Gunten S, Lew D, Paccolat F, Vaudaux P, Brazitikos P D, Leuenberger P M: Aqueous humor penetration of ofloxacin given by various routes. Am J Ophthalmol 117: 87-89, 1994 – reference: 5) 大石正夫, 宮尾益也, 阿部達也, 本山まり子: 抗菌剤の薬動力学的パラメーターと眼感染症に対する臨床効果-経口セフェム剤について-. 眼臨87: 1711-1714, 1993 – reference: 10) 大石正夫, 他 (9施設および関連施設): 眼科領域における新合成抗菌剤NY-198 (Lomefloxacin) の基礎的検討ならびに臨床的評価. あたらしい眼科6: 1041-1065, 1989 – reference: 7) 新家 真: 抗生物質の前房内移行性-その定量的解析法について-. 日眼86: 1766-1771, 1982 – reference: 1) Barza M: Principles of tissue penetration of antibiotics. J Antimicrob Chemother 8: 7-28, 1981 – reference: 17) Bron A M, Pchinot A P, Garcher C P, Guyonnet G A, Kazmierczak A M, Schott D A, Lecoeur H: The ocular penetration of oral sparfloxacin in humans. Am J Ophthalmol 117: 322-327, 1994 – reference: 20) Donnenfeld E D, Schrier A, Perry H D, Aulicino T, Gombert M E, Snyder R: Penetration of topically applied ciprofloxacin, norfloxacin, and ofloxacin into the aqueous humor. Ophthalmology 101: 902-905, 1994 – reference: 9) 原二郎, 張野正誉, 岡本茂樹: 前眼部感染症に対するT-3762の臨床効果. Chemotherapy 36: 1444-1447, 1988 – reference: 11) 原二郎, 小沢孝好, 荒木かおる, 満田久年: Sparfloxacinの前眼部細菌感染症に対する臨床効果と房水中濃度. Chemotherapy 39: 697-700, 1991 – reference: 12) 大石正夫, 他 (4施設および関連施設): 眼科領域におけるFleroxacin (FLRX) の基礎的検討ならびに臨床的評価. あたらしい眼科8: 1627-1645, 1991 – reference: 16) 三井幸彦: フルオロキノロン剤の問題点. あたらしい眼科9: 215-223, 1992 – reference: 15) 井上愼三, 松村香代子, 西原勝, 三崎昌史: ヒトにおけるロメフロキサシン内服後の特異な房水内動態-とくにメラニンの関与について-. あたらしい眼科10: 87-90, 1993 – reference: 2) Wise R: Protein binding of β-lactams: the effects on activity and pharmacology particularly tissue penetration II. J Antimicrob Chemother 12: 105-118, 1983 – reference: 18) Salvanet A, Fisch A, Lafaix C, Montay G, Dubayle P, Forestier F, Haroche G: Pefloxacin concentrations in human aqueous humour and lens. J Antimicrob Chemother 18: 199-201, 1986 |
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| SubjectTerms | NM394 NM441 ニューキノロン系合成抗菌剤 房水中濃度 |
| Title | Clinical and basic studies on NM441 in ophthalmology |
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