Sildenafil
1.化學名:Sildenafil citrate
2.商品名:Sildenafil citrate [Viagra威而鋼,威而剛,偉哥-Pfizer]
1998.3.27 FDA核准
3.化學結構: 5-[2-Ethoxy-5-(4-methylpiperazin-1-ylsulfonyl) phenyl]-1-methyl-3-
propyl-6,7-dihydro-1H-Pyrazolo [4,3-d] pyrimidin-7-one

4.分類:
•藥理分類: Phosphodiesterase (cGMP subtype 5) inhibitor磷酸二酯媒抑制劑
•治療分類: Male erectile dysfunction男性勃起不能
•懷孕危險分類: B
•授乳:不建議使用
•小兒使用:不適
5.作用機轉:
(1)cGMP為使陰莖海綿體平滑肌鬆弛之化學介質
(2)cGMP很快被Phosphodiesterase(磷酸二酯媒媒)所破壞,在陰莖組織內之
Phosphodiesterase以5次型居多
(3)Sildenafil為具有選擇性(cGMP-subtype 5)之Phosphodiesterase inhibitor

1.臨床療效:
(1)以問卷調查方式顯示Sildenarfil之療效在七成左右
例數:532例男性
劑量:Sildenafil 25,50,100mg期間:12星期
評估:International Index of Erectile Function,15-item questionaire結論: •劑量增加,效果增強100mg 100%勃起增強•行房能力
用藥組 69%安慰組22%用藥組: 每月成功行房5.9次;安慰劑組1.5次
[Goldstein I:Oral sildenafil in the treatment of erectile dysfunction.NEJM 1998;338:1397-1404]
(2)口服30分鐘以後配合視覺刺激(Visual sexual stimulation)可維持2小時左右
2.適用症與劑量:
(1)Male erectile dysfunction,Impotence男性勃起不能--
是否適用於女性尚在評估中(2)劑量:行房前1小時口服Sildenafil 25mg,50mg,100mg St
3.代謝:與血中蛋白質緊密結合,無法經由血液透析排除,甚少由尿液中排出
4.副作用:6-18%
[Goldstein I,1998](1)Headache頭痛
(2)Flushing潮紅 (3)Dyspepsia消化不良(4)Nasal congestion鼻充血
(5)Urinary tract infection泌尿道感染(6)Abnormal vision視覺障礙,藍色色彩
(7)Diarrhea腹瀉(8)Dizziness頭暈
(9)Rash皮疹10.禁忌:
與Nitrated(硝化物)合用,會導致強烈降壓作用
(Potentiate the hypotensiveeffects of nitrates)
11.參考資料:
(1)陳國群
最新內分泌學 (Current Endocrinology) (近日內出版) 8-3章 Impotence性無能(2)Goldstein I:Oral sildenafil in the treatment of erectile dysfunction. NEJM:1998;338:1397-1404.
(3)Editorial,Utiger DR:A Pill for impotence. NEJM 1998;338:1458-1459.
(4)Feldman HA,Goldstein I:Impotence and is medical and psychosocial correlates:
Results of the Massachusetts male aging study. J Urol 1994;151:54-61.
(5)Boolell M:Sildenafil,a novel effective oral therapy for male erectile dysfwnction.
B J Urol 1996;78:257-261.
(6)Boolell M:Sildenafil:an orally active type 5 cyclic GMP,specific phosphodiesterase inhibitor
for the treatment of penile erectile dysfunction.
International Journal of Impotence Research 1996;8:47-52.
(7)林儒廷:Viagra果真「威而鋼」
中國時報 87.6.8 (?)(8)道不遠:我是威而鋼的接受試驗者
中國時報 87.6.8(9)Viagra仿單
12.感謝:
感謝台灣輝瑞藥廠
劉文淑小姐 學術支援[87.12.11 (五) ]