User:Hiko.C/伐地那非
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臨床資料 | |
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商品名 | Levitra, Staxyn |
AHFS/Drugs.com | Monograph |
MedlinePlus | a603035 |
懷孕分級 | |
给药途径 | 口服 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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藥物動力學數據 | |
生物利用度 | 15% |
血漿蛋白結合率 | 95% |
药物代谢 | 肝臟(CYP3A4) |
生物半衰期 | 4至5小時 |
排泄途徑 | 膽管 |
识别信息 | |
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CAS号 | 224785-90-4 ![]() |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
ChEMBL | |
化学信息 | |
化学式 | C23H32N6O4S |
摩尔质量 | 488.604 g/mol |
3D模型(JSmol) | |
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![](http://images.weserv.nl/?url=//upload.wikimedia.org/wikipedia/commons/thumb/2/2e/000805lg_Levitra.jpg/220px-000805lg_Levitra.jpg)
伐地那非(Vardenafil)是一种第五型磷酸二酯酶抑制剂。用於治療男性陰莖勃起功能障礙。該藥能夠協助男性在性行為時能達到及維持勃起,另外也可用於治療早發性射精[1]。。其品牌名稱為「Levitra」,中國大陸譯名為「艾力达」,香港譯名為「立威大」,台灣則譯為「樂威壯」(德國拜耳)。伐地那非在上市後起初由拜耳、格蘭素史克以及先靈葆雅三家藥廠共同行銷。[2]2005年時拜耳從格蘭素史克藥廠手中將美國之外地區的行銷權購回。[3]目前市面上有拜耳藥廠的Levitra[4]、格蘭素史克使用的Vivanza[5]、以及劑型為口溶崩散劑的Staxyn與Levitra Soft等等[6][7]。
適應症與機轉
伐地那非的適應症及禁忌症與其他第五型磷酸二酯酶抑制劑相同[4],作用則與西地那非相似[4]。伐地那非與西地那非的主要差異在其結構,兩種分子之間有一個氮原子的位置不同,另外西地那非在其哌嗪環有甲基修飾[8],而伐地那非則是有乙基修飾[9]。伐地那非的作用時間相當短,但比起西地那非略長[10]。
不良反應
伐地那非的常見不良反應與其他第五型磷酸二酯酶抑制劑相同,常見的有頭痛、臉紅、以及噁心,此外還有腹痛、背痛、光敏感、視覺異常等等[11]。
心肌梗死是伐地那非少見但嚴重的潛在不良反應[12]。在某些情況下也可能造成陰莖異常勃起而需要緊急處理,如果不即時處理有可能會造成勃起功能障礙[12]。2007年時美國食品藥物管理局警告伐地那非等第五型磷酸二酯酶抑制劑可能引發急性聽覺障礙[13]。
藥物交互作用
Vardenafil, as with all PDE5 inhibitors, should not be used by people taking nitrate medications, because combining them with vardenafil might provoke potentially life-threatening hypotension (low blood pressure).[14][15][16]
Further, vardenafil causes lengthening of the QT interval. Therefore, it should not be taken by people taking other medications that affect the QT interval (such as amiodarone).[17][18]
Dose forms
![](http://images.weserv.nl/?url=//upload.wikimedia.org/wikipedia/commons/thumb/2/2e/000805lg_Levitra.jpg/220px-000805lg_Levitra.jpg)
It is available in 2.5 mg, 5 mg, 10 mg, and 20 mg doses in round orange tablets. The normal starting dose is 10 mg[4] (roughly equivalent to 50 mg of sildenafil). Vardenafil should be taken 1 to 2 hours prior to sexual activity, with a maximum dose frequency of once per day. In some territories, such as the UK, only certain doses may be available.
Vardenafil is also available under the name Staxyn as a tablet which dissolves on the tongue rather than being swallowed in the form of a pill.[19]
Tainted supplements
The USFDA has found vardenafil and other synthetic PDE5 inhibitors in numerous products marketed as "herbal" supplements or "all natural" products for male enhancement.[20][21]
外部連結
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- ^ A Aversa; et al. Effects of vardenafil administration on intravaginal ejaculatory latency time in men with lifelong premature ejaculation. International Journal of Impotence Research. July 2009, 21 (4): 221–227 [2010-12-14]. PMID 19474796. doi:10.1038/ijir.2009.21.
- ^ Bayer AG and GlaxoSmithKline, Worldwide co-promotion agreement for vardenafil to treat erectile dysfunction 已忽略未知参数
|pubdate=
(帮助) - ^ GSK's Levitra Co-Promotion Rights Transferred Back to Bayer in Most Major Markets Outside the U.S.. 2005-1-11 [2019-01-05]. (原始内容存档于2019-01-05) (英语).
- ^ 4.0 4.1 4.2 4.3 Levitra. Drugs.com. [2018-02-23]. (原始内容存档于2019-01-02).
- ^ Vivanza. Drugs.com. [2019-01-05]. (原始内容存档于2019-01-05) (英语).
- ^ New erectile dysfunction treatment STAXYN™ approved in the U.S. - Pharmaceutical Processing. pharmpro.com. 2010-06-21. (原始内容存档于2012-04-06).
- ^ STAXYN® - New Innovation in Erectile Dysfunction Helps Younger Men Rise to the Occasion.
- ^ Sildenafil. www.chemspider.com. 已忽略文本“ C22H30N6O4S ” (帮助)
- ^ Tadalafil. www.chemspider.com. [2019-01-05].
- ^ 歐洲藥物管理局. SCIENTIFIC DISCUSSION: Cialis (PDF).
- ^ Common Side Effects of Levitra (Vardenafil HCl) Drug Center. (原始内容存档于2017-07-16) (英语).
- ^ 12.0 12.1 Schools of Pharmacy (Glen L. Stimmel, Pharm.D., and Mary A. Gutierrez, Pharm.D.) and Medicine (Glen L. Stimmel, Pharm.D.), University of Southern California, Los Angeles, California. Counseling Patients About Sexual Issues: Drug-Induced Priapism. Medscape. [2010-12-06].
- ^ FDA Announces Revisions to Labels for Cialis, Levitra and Viagra. Food and Drug Administration. 2007-10-18 [2009-08-06].
- ^ Kloner, Robert A. Pharmacology and drug interaction effects of the phosphodiesterase 5 inhibitors: focus on alpha-blocker interactions. The American Journal of Cardiology. 2005-12-26, 96 (12B): 42M–46M. ISSN 0002-9149. PMID 16387566. doi:10.1016/j.amjcard.2005.07.011.
- ^ Carson, Culley C. PDE5 inhibitors: are there differences?. The Canadian Journal of Urology. February 2006,. 13 Suppl 1: 34–39. ISSN 1195-9479. PMID 16526979.
- ^ Levitra for Treatment of Erectile Dysfunction. www.erectiledysfunction.com. [2017-10-27] (美国英语).
- ^ Lepor, Herbert; Lepor, Norman E; Hill, Lawrence A; Trohman, Richard G. The QT Interval and Selection of Alpha-Blockers for Benign Prostatic Hyperplasia. Reviews in Urology. 2008, 10 (2): 85–91. ISSN 1523-6161. PMC 2483321
. PMID 18660858.
- ^ Learning, Jones & Bartlett. 2011 Nurse's Drug Handbook. Jones & Bartlett Publishers. 2010-06-29. ISBN 9781449653729 (英语).
- ^ Vardenafil. Medicine Net. [2014-02-18].
- ^ Tainted Products Marketed as Dietary Supplements. United States Food and Drug Administration.
- ^ Tucker, Jenna; Fischer, Tessa; Upjohn, Laurence; Mazzera, David; Kumar, Madhur. Unapproved Pharmaceutical Ingredients Included in Dietary Supplements Associated with US Food and Drug Administration Warnings. JAMA Network Open. 2018, 1 (6): e183337. doi:10.1001/jamanetworkopen.2018.3337.