著者

三輪 芳弘 山路 昭 中浜 肇 折田 義正 福原 吉典 鎌田 武信 石橋 道男 市川 靖二 高原 史郎 園田 孝夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.108, no.11, pp.1087-1092, 1988-11-25 (Released:2008-05-30)

参考文献数

15

被引用文献数

1 1

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A method of high performance liquid chromatography for the determination of unchanged furosemide and its metabolites in the plasma and urine of human subjects is reported. A reversed phase Hibar Lichrosorb RP-8 column was applied to the present method. Furosemide from samples was extracted with diethylether. Beta-glucronidate of furosemide was determined after the addition of beta-glucronidase. 4-Chloro-5-sulfamoyl-anthranilic acid (CSA) was determined by the supernatant obtained from ten minutes centrifugation of the urine with ethanol. In the plasma and urine concentrations of unchanged furosemide of healthy volunteers, there were recognized differences among individuals. In patients with chronic renal failure, urine concentration of beta-glucronidate of furosemide increased in response to impairment of creatinine clearance. CSA could be detected only in the urine of patients receiving renal transplantation under a large dose administration of furosemide (above 200mg/d during rejection). And CSA does not seem to be an artifact product by the procedures of extraction. No interference could be observed by the drugs co-administered with furosemide. The present method can be utilized for a routine drug monitoring system of furosemide. Mechanism of formation of metabolites of furosemide should be further studied.

著者

中野 悦次 吉岡 俊昭 松田 稔 園田 孝夫 矢野 久雄 伊原 義博 黒田 秀也 岸本 知己 櫻井 勗 内田 欽也 児島 康行 中村 隆幸 清原 久和 佐川 史郎 関井 謙一郎 古武 敏彦 宇佐美 道之 三木 恒治 黒田 昌男 細木 茂 前田 修 友岡 義夫 吉村 一宏 水谷 修太郎 岩尾 典夫 三好 進 井上 彦八郎 本城 充 藤岡 秀樹 本多 正人 高羽 津 岡 聖次 松宮 清美 原 恒男 三宅 修 坂口 洋 竹山 政美 板谷 宏彬 宇都宮 正登 伊東 博 新 武三 永野 俊介 市川 靖二 野島 道生 長船 匡男 客野 宮治 山口 誓司 多田 安温

出版者

泌尿器科紀要刊行会

雑誌

泌尿器科紀要 (ISSN:00181994)

巻号頁・発行日

vol.36, no.5, pp.635-642, 1990-05

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膀胱乳剤にフェルビナクのエチルエステルを封入させたLM-001静注剤を尿路結石による疼痛と膀胱・前立腺手術後の膀胱切迫感に対する有効性ならびに安全性について検討した.1)尿路結石による疼痛に対しては53例中49例に効果がみられた.有効例49例中41例までが本剤投与15分以内に効果が発現した.また26例において効果が24時間以上持続した.2)膀胱・前立腺手術後の膀胱切迫感に対しても29例中25例に効果がみられた.有効例25例中16例までが15分以内に効果発現した.また13例において効果が24時間以上持続した.3)副作用として血管痛,熱感,視力軽度低下,血圧の一時低下がみられたが,いずれもきわめて軽度で何ら処置することもなく短期間に消失した.また,3例に白血球増多,1例にA1-pの上昇がみられたが,その程度は軽度であり,すぐに正常化した.4)LM-001は尿路結石による疼痛の緩和と膀胱・前立腺手術後の膀胱切迫感に対し,速効性で高い有効率を示し,かつ作用時間が長いこと,また副作用がきわめて少ないことから優れた薬剤と評価し得たClinical effect of LM-001, a prostaglandin synthetic inhibitor developed from a drug delivery system, was evaluated in 54 patients with pain from urinary tract stones (stone pain) and 32 with vesical urgency after an operation on bladder or prostate. LM-001, felbinac ethyl incorporated in lipid microsphere, wes intravenously administered at the onset of stone pain or vesical urgency. Of 54 with stones and 32 with urgency, 53 and 29 were eligible for response, respectively. The symptoms improved or disappeared in some cases just after the administration and in the majority of patients within 15 minutes, in 49 of 53 patients with stone pain. Further, the effectiveness lasted over 24 hours in 26 of the 49 responding to this agent. On one hand, improvement or disappearance of vesical urgency was recognized in 25 of 29 patients, and the effectiveness was observed shortly after injection in 16 and lasted over 24 hours in 13 cases. Toxicities of this drug were investigated in 54 patients with stone pain and 32 with urinary urgency. Side effects consisted of pain at the injection site in 4, a slight fall of blood pressure in 1, slight visual disturbance in 1, body heat sensation in 1, leukocytosis in 3 and elevation of alkaline phosphatase in 1. These symptoms were transient and disappeared without use of any agent. LM-001 is concluded to be a useful drug for controlling stone pain and vesical urgency since an immediate effect, long durability and high response rates were obtained without severe side