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題名 | Ariflo[fef0]--A Brief Report on a New Second-Generation Phosphodiesterase 4 Inhibitor=Ariflo[fef0]:新第二代Phosphodiesterase 4 阻斷劑之簡介 |
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作者 | 葉育雯; 江俊松; 高尚志; Yeh, Yu-wung; Jiang, Jiunn-song; Kao, Shang-jyh; |
期刊 | 胸腔醫學 |
出版日期 | 20001200 |
卷期 | 15:4 2000.12[民89.12] |
頁次 | 頁157-164 |
分類號 | 418.26 |
語文 | eng |
關鍵詞 | 慢性阻塞性肺病; 氣喘; Ariflo[fef0]; Phosphodiesterase; Asthma; Chronic obstructive pulmonary disease; COPD; |
中文摘要 | 治療氣喘以及慢性阻塞性肺病的藥物日新月異,但最常用的仍不外乎乙型交感神經興奮劑、抗乙醯膽鹼、類固醇、以及茶鹼類藥物,phosphodiesterases在人體的生理機能中佔了一極重要之地位,可調節cyclic AMP以及cyclic GMP之作用。如今常用之茶鹼類藥物即為不具特異性之phosphodiesterase阻斷劑,由於不同種類的phosphodiesterase在人體各個器官中分佈不同,理論上可依此選擇性地研發不同效用的藥品。自1970年代起,便有許多研究報告探討具特異性之phosphodiesterase阻斷劑在治療氣喘及慢性阻塞性肺病上潛在性之運用。其中又以phosphodiesterase 4 (PDE4)阻斷劑在肺部疾病的作用最為有效;它可抑制嗜中性白血球(neutrophil)的作用、減低腫瘤壞死因子(TNF-α的合成、抑止肥胖細胞mast cell)顆粒之釋放、以及減低T細胞的增生。但是,目前已研發出的phosphodiesterase阻斷劑由於副作用過大,在臨床上之運用並不廣泛。史克美占藥廠(SmithKline Beecham Pharmaceuticals)即將推出一新的第二代phosphodiesterase 4阻斷劑ArifloTM。第二階段實驗中,ArifloTM可有效地改善運動產生之呼吸困難,增進第一秒最大呼氣量(FEVI),以及減低小支氣管的關閉(small airway closures),比較第一代的phosphodiestrase 4阻斷劑,其副作用遠蚾第一代之phosphodiestease 4阻斷劑為少。此藥之臨床運用功效曾在去年歐洲呼吸年會引起熱烈討論,與會專家感認其將為慢性阻塞性患者增添一治療的新利器,在第三階段實驗結果揭曉之前,為文介紹,以饗讀者。 |
英文摘要 | Even though the search for new medications continues, at the end of the day, we still rely on time-honored drugs such as β-agonist, anti-cholinergics, steroids, and theophylline for the treatment of asthma and chronic obstructive pulmonary diseases. Phosphodiesterases play a very important role in terms of biological functions in the human body. They affect the concentration of cyclic AMP and cyclic GMP. Theophylline, in fact, is a non-specific phosphodiesterase inhibitor. And different isozymes of phosphodiesterases have different distribution properties in various tissues, by targeting different isozymes, one can theoretically develop drugs with different properties acting on different target organs. Since the 1970's there has been intensive research on the potential use of phosphodiesterase inhibitors, and in particular, the phosphodiesterase 4 (PDE4) inhibitors, in treating asthma and chronic obstructive pulmonary diseases. PDE4 inhibitors can inhibit neutrophil functions, decrease TNF α production, impair mast cell degranulation, and decrease T cell proliferation. However, the known PDE inhibitors have not been proved to be clinically useful due to their side effect profiles. SmithKline Beecham Pharmaceuticals is planning to launch a new second-generation PDE4 inhibitor Ariflo. In phase II trials, Ariflo could effectively improve exercise dyspnea scores, increase FEV1, and improve small airway closures. Compared to the first-generation phosphodiesterase 4 inhibitors, Ariflo has markedly improved side effect profiles. |
本系統之摘要資訊系依該期刊論文摘要之資訊為主。