用户:Hiko.C/伐地那非
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临床资料 | |
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商品名 | Levitra, Staxyn |
AHFS/Drugs.com | Monograph |
MedlinePlus | a603035 |
怀孕分级 | |
给药途径 | 口服 |
ATC码 | |
法律规范状态 | |
法律规范 |
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药物动力学数据 | |
生物利用度 | 15% |
血浆蛋白结合率 | 95% |
药物代谢 | 肝脏(CYP3A4) |
生物半衰期 | 4至5小时 |
排泄途径 | 胆管 |
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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伐地那非(Vardenafil)是一种第五型磷酸二酯酶抑制剂。用于治疗男性阴茎勃起功能障碍。该药能够协助男性在性行为时能达到及维持勃起,另外也可用于治疗早发性射精[1]。。其品牌名称为“Levitra”,中国大陆译名为“艾力达”,香港译名为“立威大”,台湾则译为“乐威壮”(德国拜耳)。伐地那非在上市后起初由拜耳、格兰素史克以及先灵葆雅三家药厂共同行销。[2]2005年时拜耳从格兰素史克药厂手中将美国之外地区的行销权购回。[3]目前市面上有拜耳药厂的Levitra[4]、格兰素史克使用的Vivanza[5]、以及剂型为口溶崩散剂的Staxyn与Levitra Soft等等[6][7]。
适应症与机转
伐地那非的适应症及禁忌症与其他第五型磷酸二酯酶抑制剂相同[4],作用则与西地那非相似[4]。伐地那非与西地那非的主要差异在其结构,两种分子之间有一个氮原子的位置不同,另外西地那非在其哌嗪环有甲基修饰[8],而伐地那非则是有乙基修饰[9]。伐地那非的作用时间相当短,但比起西地那非略长[10]。
不良反应
伐地那非的常见不良反应与其他第五型磷酸二酯酶抑制剂相同,常见的有头痛、脸红、以及恶心,此外还有腹痛、背痛、光敏感、视觉异常等等[11]。
心肌梗死是伐地那非少见但严重的潜在不良反应[12]。在某些情况下也可能造成阴茎异常勃起而需要紧急处理,如果不即时处理有可能会造成勃起功能障碍[12]。2007年时美国食品药物管理局警告伐地那非等第五型磷酸二酯酶抑制剂可能引发急性听觉障碍[13]。
药物交互作用
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
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]
外部链接
- ^ 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].
- ^ 欧洲药物管理局. 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.