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 hypotensive

effects 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) ]