FDA批準他達拉非用于治療良性前列腺增生作者：admin信息來源：www點擊數： 196更新時間：2011-10-272011年10月6日，美國食品藥品管理局（FDA）批準他達拉非(tadalafi，商品名Cialis)用于治療良性前列腺增生(benign prostatic hyperplasia ，BPH)，該疾病表現為前列腺增大。他達拉非于2003年被批準用于治療ED，在我國也已獲準進口，商品名：西力士。BPH的常見癥狀包括排尿困難、尿無力、尿急、包括夜間在內的尿頻。在兩項臨床試驗中，根據國際前列腺癥狀分級標準(the International Prostate Symptom Score ，IPSS)評估BPH癥狀，與安慰劑組患者相比，每天服用一次5mg他達拉非的患者BPH癥狀上有顯著統計學差異。上述試驗基于IPSS總分減少的研究結果。在第三項試驗中，同時患有ED和BPH的患者每天服用一次5mg他達拉非，與安慰劑組患者相比，患者的ED和BPH癥狀均有改善。測定ED的改善程度采用國際勃起功能指數（the International Index of Erectile Function）的評級標準。服用硝酸鹽類的患者應禁用他達拉非，例如硝酸甘油，因為聯合用藥可導致血壓降低的危險性。也不推薦他達拉非與受體阻斷劑聯合用藥，因為在聯合用藥治療BPH方面也沒有足夠的研究，且也存在血壓降低的風險。FDA批準的其他8種用于治療BPH的藥物：保列治（非那雄胺）、適尿通（度他雄胺）、Jalyn（度他雄胺附加坦索羅辛）和受體阻斷劑類：高特靈（特拉唑嗪）、可多華（多沙唑嗪）、坦洛新（坦索羅辛）、Uroxatral（阿夫唑嗪）、Rapaflo（西羅多辛）。Cialis相當于偉 哥， 一種治療性 功能障礙的藥物。 臨床證明，藥效可長達36小時，30分鐘起效。由于cialis的藥效可延續性，不需要擔心幾小時內失效。你和你的伴侶可以好好放松并且享受。cialis的好處：藥效長達36小時快速見效很管用使你準備好不必就餐而食百萬人使用可以在網上買窗體頂端【藥物名稱】Tadalafil, GF-196960, IC-351, Cialis化學結構式(Chemical Structure):參考文獻No.27672標題:Tetracyclic derivs., process of preparation and use作者:Daugan, A.C.-M. (Icos Corp.)來源:EP 0740668; JP 1997508113; US 5859006; US 6025494; US 6127542; WO 9519978合成路線圖解說明: Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.參考文獻No.32434標題:Use of cGMP-phosphodiesterase inhibitors to treat impotence作者:Daugan, A.C.-M. (Icos Corp.)來源:JP 1999509221; US 6140329; WO 9703675合成路線圖解說明: Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.參考文獻No.46213標題:Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use作者:Gellibert, F.; Daugan, A.C.-M. (Icos Corp.)來源:US 6143746合成路線圖解說明: Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.參考文獻No.606182標題:IC-351作者:Mart韓, L.; Sorbera, L.A.; Leeson, P.A.; Casta馿r, J.來源:Drugs Fut 2001,26(1),15合成路線圖解說明: Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole derivative (III). The acylation of (III) with chloroacetyl chloride (IV) and NaHCO3 in chloroform yields the chloroacetyl derivative (V), which is finally cyclized with methylamine in methanol.參考文獻No.757016標題:The discovery of tadalafil: A novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-Hexahydropyrazino1,2:1,6pyrido3,4-bindole-1,4-dione analogues作者:Daugan, A.; Grondin, P.; Ruault, C.; Le Monnier de Gouville, A.C.; Coste, H.; Linget, J.M.; Kirilovsky, J.; Hyafil, F.; Labaudiniere, R.來源:J Med Chem 2003,46(21),4533合成路線圖解說明: Cyclization of D-tryptophan methyl ester (I) with piperonal (II) by means of TFA in dichloromethane gives, after separation of the undesired trans-isomer by flash chromatography, the (1R,3R-cis)-pyrido-indole d