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題名 | 碳酸酐酶抑制劑6-Hydroxyethoxy-2-benzothiazole Sulfonamide靜脈注射後之兔眼藥物動力學=The Ocular Pharmacokinetics of a Topical Carbonic Anhydrase |
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作者 | 呂大文; 高繼文; 江樵熹; 張澶榮; 林秋燕; | 書刊名 | 中華民國眼科醫學會雜誌 |
卷期 | 38:1 1999.03[民88.03] |
頁次 | 頁33-40 |
分類號 | 418.2323 |
關鍵詞 | 碳酸酐酶抑制劑; 藥物動力學; 青光眼; Carbonic anhydrase inhibitor; Glaucoma; 6-Hydroxyethoxy-2-benzothiazole Sulfonamide; 6-HS; Ocular pharmacokinetics; |
語文 | 中文(Chinese) |
中文摘要 | 磺腰類碳酸酐�t抑制劑臨床上常用來治療高血壓與青光眼。但因此類藥物於系統 性使用時,常伴隨令患者難以忍受之副作用,諸如: 倦怠感、尿路結石、體重減輕、白血球 減少與再生不良性貧血等,因此用於治療青光眼時,常作為第二線用藥,或用於急性青光眼 之治療。另外碳酸酐�t抑制劑之降眼壓藥理機轉雖已大部份明瞭,但因文獻上有關碳酸酐�t 抑制劑藥物之眼部藥物動力學報導較為缺乏, 故在本研究申我們以 6-Hydroxyethoxy-2-benzothiazole Sulfonamide(6-HS) 作為碳酸酐�t抑制劑之模式藥物, 研究其於兔子靜脈注射後在眼部組織之藥物動力學變化, 結果發現 6-HS 於 Alpha -chymotrypsin 導致之青光眼兔眼之房水液與虹膜 -- 睫狀體複合體之分佈與排除速率皆與 正常兔眼顯著不同,在正常兔眼之房水液中 6 -HS 之排除半衰期為 231 分鐘而在青光眼兔 眼則為 130.8 分鐘 (P<0.01),在正常眼之虹膜 -- 睫狀體複合體中 6-HS 之末相排除半衰 期為 198 分鐘而在青光眼兔眼為 63 分鐘 (P<0.01)。 |
英文摘要 | Carbonic anhydrase inhibitors (CAIs) are very effective in treating glaucoma, but their clinical usefulness was limited to as second line antiglaucoma medications or acute glaucoma due to a variety of systemic side effects included fatigue, urolithiasis, body weight loss, and aplastic anemia. In addition, although the mechanisms for CAIs to decrease intraocular pressure (IOP) were mostly understood, yet there were very few reports on the ocular pharmacokinetics of CAIs. In this study, we used 6-hydroxythoxy-2-benzothiazole sulfonamide (6-HS) as a model drug to evaluate its pharmacokinetics in the rabbit ocular tissue after intravenous injection. We found that the elimination rate constants in the aqueous humor and iris-ciliary body complex between alpha-chymotrypsin induced glaucoma eyes and normal eyes were significantly different. In the aqueous humor, the elimination half life for 6-HS in normal rabbit eyes and glaucoma eyes were 231 minutes and 130.8 minutes respectively (P<0.01). In the iris-ciliary body complex, the elimination half life for 6-HS in normal rabbit eyes and glaucoma eyes were 198 minutes and 63 minutes respectively (P< 0.01). |
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