| 词条 | Vardenafil |
| 释义 |
| verifiedrevid = 458460083 | IUPAC_name = 4-[2-Ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4.3.0]nona-3,7,9-trien-2-one | image = Vardenafil structure.svg | width = 250 | tradename = Levitra, Staxyn, Vivanza | Drugs.com = {{drugs.com|monograph|vardenafil-hydrochloride}} | MedlinePlus = a603035 | pregnancy_AU = B3 | pregnancy_US = B | licence_EU = yes | legal_AU = S4 | legal_UK = POM | legal_US = Rx | legal_status = Rx-only | routes_of_administration = Oral | bioavailability = 15% | protein_bound = 95% | metabolism = Hepatic (CYP3A4) | elimination_half-life = 4–5 hours | excretion = Biliary | IUPHAR_ligand = 7320 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 224785-90-4 | ATC_prefix = G04 | ATC_suffix = BE09 | ATC_supplemental = | PubChem = 110634 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00862 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 99300 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = UCE6F4125H | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1520 | KEGG = D08668 | C=23 | H=32 | N=6 | O=4 | S=1 | molecular_weight = 488.604 g/mol | smiles = O=C2\=C(/Nn1c(nc(c12)C)CCC)c3cc(ccc3OCC)S(=O)(=O)N4CCN(CC)CC4 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C23H32N6O4S/c1-5-8-20-24-16(4)21-23(30)25-22(26-29(20)21)18-15-17(9-10-19(18)33-7-3)34(31,32)28-13-11-27(6-2)12-14-28/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,30) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = SECKRCOLJRRGGV-UHFFFAOYSA-N }} Vardenafil (INN) is a PDE5 inhibitor used for treating erectile dysfunction that is sold under the trade names Levitra (Bayer AG, GSK, and SP), Staxyn in India, and Vivanza in Italy. HistoryVardenafil was co-marketed by Bayer Pharmaceuticals, GlaxoSmithKline, and Schering-Plough under the trade name Levitra. As of 2005, the co-promotion rights of GSK on Levitra have been returned to Bayer in many markets outside the U.S. In Italy, Bayer sells vardenafil as Levitra and GSK sells it as Vivanza. Thus, because of European Union trade rules, parallel imports might result in Vivanza sold next to Levitra in the EU. An orally disintegrating form, marketed as Staxyn and Levitra Soft, has been gaining approvals in countries such as the United States[1] and Canada.[2] Clinical use{{main|PDE5 inhibitor}}Vardenafil's indications and contraindications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). The difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ring methyl group to an ethyl group. Tadalafil is structurally different from both sildenafil and vardenafil. Vardenafil's relatively short effective time is comparable to but somewhat longer than sildenafil's. Beyond its indications for erectile dysfunction, vardenafil may be effective in the treatment of premature ejaculation, where it may significantly increase the time from penetration to ejaculation.[3] Adverse drug reactionsThe common, adverse drug reactions (side effects) are the same as with other PDE5 inhibitors. The frequent vardenafil-specific side-effect is nausea; the infrequent side effects are abdominal pain, back pain, photosensitivity, abnormal vision, eye pain, facial edema, hypotension, palpitation, tachycardia, arthralgia, myalgia, rash, itch, and priapism. One possibly serious, but rare, side effect with vardenafil is heart attack. Also, in rare cases, vardenafil use may cause priapism, a very painful emergency condition that can cause impotence if left untreated.[4] On 18 October 2007, the U.S. Food and Drug Administration (FDA) announced that a warning about possible deafness (sudden hearing loss) would be added to the drug labels of vardenafil, and other PDE5 inhibitors.[5] Drug interactionsVardenafil, 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).[6][7][8] 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).[9][10] Dose formsIt 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[11] (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.[12] Tainted supplementsThe USFDA has found vardenafil and other synthetic PDE5 inhibitors in numerous products marketed as "herbal" supplements or "all natural" products for male enhancement.[13][14] Notes1. ^{{cite web | title=New erectile dysfunction treatment STAXYN™ approved in the U.S. - Pharmaceutical Processing | website=pharmpro.com | date=2010-06-21 | url=https://www.pharmpro.com/News/Feeds/2010/06/pharmaceutical-companies-bayer-new-erectile-dysfunction-treatment-staxyn-approve | archive-url=https://web.archive.org/web/20120406122727/https://www.pharmpro.com/News/Feeds/2010/06/pharmaceutical-companies-bayer-new-erectile-dysfunction-treatment-staxyn-approve | archive-date=2012-04-06 | dead-url=yes}} 2. ^{{cite web|url=http://www.newswire.ca/en/story/832217/staxyn-new-innovation-in-erectile-dysfunction-helps-younger-men-rise-to-the-occasion|title=STAXYN® - New Innovation in Erectile Dysfunction Helps Younger Men Rise to the Occasion|publisher=}} 3. ^{{cite journal|title=Effects of vardenafil administration on intravaginal ejaculatory latency time in men with lifelong premature ejaculation|author=A Aversa|display-authors=etal|volume=21|issue=4|doi=10.1038/ijir.2009.21|pmid=19474796|journal=International Journal of Impotence Research|pages=221–227|date=July 2009}} 4. ^{{cite web|url=http://www.medscape.com/viewarticle/549253_6|title=Counseling Patients About Sexual Issues: Drug-Induced Priapism|author= 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.|accessdate=2010-12-06|publisher=Medscape}} 5. ^{{cite web | url=http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2007/ucm109012.htm| title= FDA Announces Revisions to Labels for Cialis, Levitra and Viagra| date= 2007-10-18| publisher= Food and Drug Administration | accessdate=2009-08-06 }} 6. ^{{Cite journal|last=Kloner|first=Robert A.|date=2005-12-26|title=Pharmacology and drug interaction effects of the phosphodiesterase 5 inhibitors: focus on alpha-blocker interactions|journal=The American Journal of Cardiology|volume=96|issue=12B|pages=42M–46M|doi=10.1016/j.amjcard.2005.07.011|issn=0002-9149|pmid=16387566}} 7. ^{{Cite journal|last=Carson|first=Culley C.|date=February 2006|title=PDE5 inhibitors: are there differences?|journal=The Canadian Journal of Urology|volume=13 Suppl 1|pages=34–39|issn=1195-9479|pmid=16526979}} 8. ^{{Cite web|url=https://www.erectiledysfunction.com/levitra/|title=Levitra for Treatment of Erectile Dysfunction|website=www.erectiledysfunction.com|language=en-US|access-date=2017-10-27}} 9. ^{{Cite journal|last=Lepor|first=Herbert|last2=Lepor|first2=Norman E|last3=Hill|first3=Lawrence A|last4=Trohman|first4=Richard G|date=2008|title=The QT Interval and Selection of Alpha-Blockers for Benign Prostatic Hyperplasia|journal=Reviews in Urology|volume=10|issue=2|pages=85–91|issn=1523-6161|pmc=2483321|pmid=18660858}} 10. ^{{Cite book|url=https://books.google.com/?id=PaiBU04wrrgC&pg=PA1079&lpg=PA1079&dq=vardenafil++QT+interval++amiodarone#v=onepage&q=vardenafil%20%20QT%20interval%20%20amiodarone&f=false|title=2011 Nurse's Drug Handbook|last=Learning|first=Jones & Bartlett|date=2010-06-29|publisher=Jones & Bartlett Publishers|isbn=9781449653729|language=en}} 11. ^{{cite web|url=https://www.drugs.com/dosage/levitra.html| title=Levitra Dosage| publisher=Drugs.com| accessdate=2018-02-23}} 12. ^{{cite web|url=http://www.medicinenet.com/vardenafil/article.htm| title= Vardenafil| publisher=Medicine Net| accessdate= 2014-02-18}} 13. ^{{cite web | url = https://www.accessdata.fda.gov/scripts/sda/sdNavigation.cfm?sd=tainted_supplements_cder&displayAll=false&page=1 | title = Tainted Products Marketed as Dietary Supplements | publisher = United States Food and Drug Administration}} 14. ^{{cite journal | doi = 10.1001/jamanetworkopen.2018.3337| pmid = 30646238| pmc = 6324457| title = Unapproved Pharmaceutical Ingredients Included in Dietary Supplements Associated with US Food and Drug Administration Warnings| journal = JAMA Network Open| volume = 1| issue = 6| pages = e183337| year = 2018| last1 = Tucker| first1 = Jenna| last2 = Fischer| first2 = Tessa| last3 = Upjohn| first3 = Laurence| last4 = Mazzera| first4 = David| last5 = Kumar| first5 = Madhur}} External links
6 : Erectile dysfunction drugs|Lactams|PDE5 inhibitors|Phenol ethers|Piperazines|Sulfonamides |
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