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Namespace Prefixes

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Statements

Subject Item
n2:DB00862
rdf:type
n3:Drug
n3:description
Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.
n3:dosage
n19:271B50C4-363D-11E5-9242-09173F13E4C5 n19:271B50BF-363D-11E5-9242-09173F13E4C5 n19:271B50C0-363D-11E5-9242-09173F13E4C5 n19:271B50C1-363D-11E5-9242-09173F13E4C5 n19:271B50C2-363D-11E5-9242-09173F13E4C5 n19:271B50BB-363D-11E5-9242-09173F13E4C5 n19:271B50BC-363D-11E5-9242-09173F13E4C5 n19:271B50BD-363D-11E5-9242-09173F13E4C5 n19:271B50BE-363D-11E5-9242-09173F13E4C5 n19:271B50C3-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3:halfLife
4-5 hours
n3:indication
Used for the treatment of erectile dysfunction
n3:manufacturer
n9:271B50B6-363D-11E5-9242-09173F13E4C5
owl:sameAs
n16:DB00862 n23:DB00862
dcterms:title
Vardenafil
adms:identifier
n5:99300 n7:DB00862 n8:Vardenafil n10:14776 n11:PA10229 n12:110634 n13:0085-1923-01 n18:D09989 n20:46506777
n3:mechanismOfAction
Vardenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by vardenafil enhances erectile function by increasing the amount of cGMP.
n3:packager
n9:271B50B4-363D-11E5-9242-09173F13E4C5 n9:271B50B5-363D-11E5-9242-09173F13E4C5 n9:271B50AD-363D-11E5-9242-09173F13E4C5 n9:271B50AE-363D-11E5-9242-09173F13E4C5 n9:271B50AB-363D-11E5-9242-09173F13E4C5 n9:271B50AC-363D-11E5-9242-09173F13E4C5 n9:271B50B3-363D-11E5-9242-09173F13E4C5 n9:271B50B1-363D-11E5-9242-09173F13E4C5 n9:271B50B2-363D-11E5-9242-09173F13E4C5 n9:271B50AF-363D-11E5-9242-09173F13E4C5 n9:271B50B0-363D-11E5-9242-09173F13E4C5
n3:patent
n26:6362178 n26:2309332
n3:routeOfElimination
After oral administration, vardenafil is excreted as metabolites predominantly in the feces (approximately 91-95% of administered oral dose) and to a lesser extent in the urine (approximately 2-6% of administered oral dose).
n3:synonym
Vardénafil 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-F][1,2,4]triazin-4(1H)-one Levitra Vardenafil Vardenafilum
n3:toxicity
Symptoms of overdose include vision changes and back and muscle pain.
n3:volumeOfDistribution
* 208 L
n21:hasAHFSCode
n31:24-12-12
n3:proteinBinding
95%
n3:salt
n3:synthesisReference
Yogesh S. Deshpande, Sandra Brueck, Julia Schulze Nahrup, Birgit Schnitter, Ganesh Gat, Javed Hussain, "PROCESS FOR THE PREPARATION OF A MEDICAMENT COMPRISING VARDENAFIL HYDROCHLORIDE TRIHYDRATE." U.S. Patent US20100159003, issued June 24, 2010.
n24:hasConcept
n25:M0387383
foaf:page
n28:vardenafil.html n29:lev1688.shtml n30:levitra.htm
n3:IUPAC-Name
n6:271B50C9-363D-11E5-9242-09173F13E4C5
n3:InChI
n6:271B50CF-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n6:271B50CE-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n6:271B50CB-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n6:271B50CC-363D-11E5-9242-09173F13E4C5
n3:SMILES
n6:271B50CD-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n6:271B50C7-363D-11E5-9242-09173F13E4C5 n6:271B50DF-363D-11E5-9242-09173F13E4C5
n3:logP
n6:271B50C5-363D-11E5-9242-09173F13E4C5 n6:271B50C8-363D-11E5-9242-09173F13E4C5 n6:271B50E1-363D-11E5-9242-09173F13E4C5
n3:logS
n6:271B50C6-363D-11E5-9242-09173F13E4C5
n21:hasATCCode
n22:G04BE09
n3:H-Bond-Acceptor-Count
n6:271B50D5-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n6:271B50D6-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n6:271B50D0-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n6:271B50D1-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n6:271B50D3-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n6:271B50D2-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n6:271B50D4-363D-11E5-9242-09173F13E4C5
n3:absorption
Vardenafil is rapidly absorbed with absolute bioavailability of approximately 15%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
224785-90-4
n3:category
n3:clearance
* 56 L/h
n3:containedIn
n17:271B50B9-363D-11E5-9242-09173F13E4C5 n17:271B50BA-363D-11E5-9242-09173F13E4C5 n17:271B50B7-363D-11E5-9242-09173F13E4C5 n17:271B50B8-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n6:271B50DB-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n6:271B50DD-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n6:271B50DE-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n6:271B50E0-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n6:271B50DA-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n6:271B50D9-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n6:271B50DC-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n6:271B50CA-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n6:271B50D7-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n6:271B50D8-363D-11E5-9242-09173F13E4C5