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virility drug (trade name Levitra) used to treat erectile dysfunction in men (同)Levitra

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/17 21:17:43」(JST)

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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.

History

Vardenafil 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

Vardenafil's indications and contra-indications 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 reactions

The 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 interactions

Vardenafil, as with all PDE5 inhibitors, should not be used by men taking nitrate medications, because combining them with vardenafil might provoke potentially life-threatening hypotension (low blood pressure).

Further, Vardenafil causing lengthening of the QT interval. Therefore it should not be taken by men taking other medications that affect the QT interval (such as amiodarone).

Dose forms

Levitra 20mg Oral Tablet

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^[6] (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.^[7]

Notes

^ http://www.pharmpro.com/News/Feeds/2010/06/pharmaceutical-companies-bayer-new-erectile-dysfunction-treatment-staxyn-approve/
^ http://www.newswire.ca/en/story/832217/staxyn-new-innovation-in-erectile-dysfunction-helps-younger-men-rise-to-the-occasion
^ A Aversa et al. "Effects of vardenafil administration on intravaginal ejaculatory latency time in men with lifelong premature ejaculation". Retrieved 2010-12-14.
^ 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. Retrieved 2010-12-06.
^ "FDA Announces Revisions to Labels for Cialis, Levitra and Viagra". Food and Drug Administration. 2007-10-18. Retrieved 2009-08-06.
^ "How Do I Take Levitra". HealthExpress. Retrieved 2014-02-18.
^ "Vardenafil". Medicine Net. Retrieved 2014-02-18.

External links

Official Levitra website
PubChem Information

UpToDate Contents

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1. 男性性機能不全の治療 treatment of male sexual dysfunction
2. 心血管疾患患者における性的活動 sexual activity in patients with cardiovascular disease
3. 成人における肺高血圧症の治療 treatment of pulmonary hypertension in adults
4. 初期治療に抵抗性を示したレイノー現象の治療 treatment of the raynaud phenomenon resistant to initial therapy
5. 糖尿病における勃起不全 erectile dysfunction in diabetes mellitus

English Journal

Persistent phototransformation products of vardenafil (Levitra®) and sildenafil (Viagra®).

Herbert LP1, Becker-Krail DB1, Cory WC2.
Chemosphere.Chemosphere.2015 Sep;134:557-62. doi: 10.1016/j.chemosphere.2014.12.011. Epub 2015 Jan 10.
As pharmaceutically active compounds (PhACs) are increasingly detected in the aquatic environment, the importance of investigating their transformation products-products of naturally occurring hydrolysis, biodegradation, and solar-mediated photochemical reactions - for persistence and ecotoxicity re
PMID 25585868

"One-shot" analysis of PDE-5 inhibitors and analogues in counterfeit herbal natural products using an LC-DAD-QTOF system.

Bortolini C1, Pivato A, Bogialli S, Pastore P.
Analytical and bioanalytical chemistry.Anal Bioanal Chem.2015 Aug;407(20):6207-16. doi: 10.1007/s00216-015-8801-4. Epub 2015 Jun 14.
A highly selective and robust method for simultaneous screening and confirmation of target and non-target phosphodiesterase type 5 (PDE-5) inhibitor analogues within a single chromatographic run in counterfeit herbal products was developed. The protocol, based on an easy and rapid extraction with a
PMID 26072210

Object memory enhancement by combining sub-efficacious doses of specific phosphodiesterase inhibitors.

Bollen E1, Akkerman S1, Puzzo D2, Gulisano W2, Palmeri A2, D'Hooge R3, Balschun D3, Steinbusch HW1, Blokland A4, Prickaerts J5.
Neuropharmacology.Neuropharmacology.2015 Aug;95:361-6. doi: 10.1016/j.neuropharm.2015.04.008. Epub 2015 Apr 17.
The second messengers cGMP and cAMP have a vital role in synaptic plasticity and memory processes. As such, phosphodiesterases inhibitors (PDE-Is), which prevent the breakdown of these cyclic nucleotides, represent a potential treatment strategy in memory decline. Recently it has been demonstrated t
PMID 25896769

Japanese Journal

PDE4 and PDE5 regulate cyclic nucleotide contents and relaxing effects on carbachol-induced contraction in the bovine abomasum

Journal of Veterinary Medical Science 77(1), 15-19, 2015
NAID 130004781006

PDE4 and PDE5 regulate cyclic nucleotide contents and relaxing effects on carbachol-induced contraction in the bovine abomasum

Journal of Veterinary Medical Science, 2014
NAID 130004699209

国立医薬品食品衛生研究所における痩身や強壮を標榜する健康食品中の医薬品成分の分析と同定

YAKUGAKU ZASSHI 134(2), 197-202, 2014
NAID 130003391159

Related Pictures

★リンクテーブル★

リンク元	「シルデナフィル」「バルデナフィル」「LEVITRA」
拡張検索	「vardenafil hydrochloride hydrate」「vardenafil dihydrochloride」

「シルデナフィル」

Vardenafil
Systematic (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
Clinical data
Trade names	Levitra, Staxyn, Vivanza
AHFS/Drugs.com	monograph
MedlinePlus	a603035
Pregnancy; category	B3 (Au), B (U.S.);
Legal status	AU: Prescription Only (S4); UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	15%
Protein binding	95%
Metabolism	Hepatic (CYP3A4)
Half-life	4–5 hours
Excretion	Biliary
Identifiers
CAS Registry Number	224785-90-4
ATC code	G04BE09
PubChem	CID: 110634
IUPHAR ligand	7320
DrugBank	DB00862
ChemSpider	99300
UNII	UCE6F4125H
ChEMBL	CHEMBL1520
Chemical data
Formula	C23H32N6O4S
Molecular mass	488.604 g/mol
	SMILES O=C2\N=C(/Nn1c(nc(c12)C)CCC)c3cc(ccc3OCC)S(=O)(=O)N4CCN(CC)CC4;
	InChI InChI=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) ; Key:SECKRCOLJRRGGV-UHFFFAOYSA-N ;
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