Detail

Vardenafil

Description

Name: Vardenafil
Type: small molecule
Groups: approved
Indication: Used for the treatment of erectile dysfunction
Accession Number: DB00862 ( APRD00699)
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.
Structure:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Levitratablet, film coated20 mg/1oral15-05-2008US
Levitratablet, film coated10 mg/1oral15-05-2008US
Levitratablet5 mgoral17-03-2004Canada
Levitratablet10 mgoral17-03-2004Canada
Levitratablet20 mgoral17-03-2004Canada
Levitratablet, film coated20 mg/1oral27-01-2004US
Levitratablet, film coated10 mg/1oral05-03-2004US
Levitratablet, film coated20 mg/1oral28-10-2011US
Levitratablet, film coated5 mg/1oral15-05-2008US
Levitratablet, film coated20 mg/1oral22-04-2011US
Levitratablet, film coated10 mg/1oral15-05-2008US
Levitratablet, film coated10 mg/1oral22-04-2011US
Levitratablet, film coated5 mg/1oral22-04-2011US
Levitratablet, film coated20 mg/1oral22-04-2011US
Staxyntablet (orally disintegrating)10 mgoral25-08-2011Canada
Staxyntablet, orally disintegrating10 mg/1oral08-03-2012US

Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
StaxynVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
LevitraVardenafil
StaxynVardenafil

Categories
  • Vasodilator Agents
  • Phosphodiesterase 5 Inhibitors
  • Anti-Impotence Agents

Pharmacology

Indication: Used for the treatment of erectile dysfunction
Pharmacodynamics: Not Available
Mechanism of action: 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.
Absorption: Vardenafil is rapidly absorbed with absolute bioavailability of approximately 15%.
Volume of distribution:
  • 208 L

Protein binding: 95%
Metabolism: Not Available
Route of elimination: 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).
Half life: 4-5 hours
Clearance: Not Available
Toxicity: Symptoms of overdose include vision changes and back and muscle pain.
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Bayer healthcare pharmaceuticals inc

Packagers:
Dosage forms
FormRouteStrength
Tabletoral10 mg
Tabletoral20 mg
Tabletoral5 mg
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral5 mg/1
Tablet (orally disintegrating)oral10 mg
Tablet, orally disintegratingoral10 mg/1

Prices
Unit descriptionCostUnit
Levitra 2.5 mg tablet$18.66tablet
Levitra 10 mg tablet$19.04tablet
Levitra 20 mg tablet$19.04tablet
Levitra 5 mg tablet$19.04tablet

Patents
CountryPatent NumberApprovedExpires (estimated)
2309332Canada2002-12-032018-10-31
6362178United States1998-10-312018-10-31

Interactions

Drug Interactions
DrugInteraction
AcebutololVardenafil may increase the antihypertensive activities of Acebutolol.
AlfuzosinVardenafil may increase the hypotensive activities of Alfuzosin.
AliskirenVardenafil may increase the antihypertensive activities of Aliskiren.
AlprostadilThe risk or severity of adverse effects can be increased when Vardenafil is combined with Alprostadil.
AmilorideVardenafil may increase the antihypertensive activities of Amiloride.
AmlodipineVardenafil may increase the antihypertensive activities of Amlodipine.
Amyl NitriteVardenafil may increase the vasodilatory activities of Amyl Nitrite.
AprepitantThe serum concentration of Vardenafil can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Vardenafil can be increased when it is combined with Atazanavir.
AtenololVardenafil may increase the antihypertensive activities of Atenolol.
AvanafilThe risk or severity of adverse effects can be increased when Vardenafil is combined with Avanafil.
Azilsartan medoxomilVardenafil may increase the antihypertensive activities of Azilsartan medoxomil.
BenazeprilVardenafil may increase the antihypertensive activities of Benazepril.
BendroflumethiazideVardenafil may increase the antihypertensive activities of Bendroflumethiazide.
BetaxololVardenafil may increase the antihypertensive activities of Betaxolol.
BisoprololVardenafil may increase the antihypertensive activities of Bisoprolol.
BoceprevirThe serum concentration of Vardenafil can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Vardenafil can be decreased when it is combined with Bosentan.
BumetanideVardenafil may increase the antihypertensive activities of Bumetanide.
CandesartanVardenafil may increase the antihypertensive activities of Candesartan.
CaptoprilVardenafil may increase the antihypertensive activities of Captopril.
CarvedilolVardenafil may increase the antihypertensive activities of Carvedilol.
CeritinibThe serum concentration of Vardenafil can be increased when it is combined with Ceritinib.
ChlorothiazideVardenafil may increase the antihypertensive activities of Chlorothiazide.
ChlorthalidoneVardenafil may increase the antihypertensive activities of Chlorthalidone.
CilazaprilVardenafil may increase the antihypertensive activities of Cilazapril.
CitalopramVardenafil may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Vardenafil can be increased when it is combined with Clarithromycin.
ClevidipineVardenafil may increase the antihypertensive activities of Clevidipine.
ClonidineVardenafil may increase the antihypertensive activities of Clonidine.
CobicistatThe serum concentration of Vardenafil can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Vardenafil can be increased when it is combined with Conivaptan.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Vardenafil.
DarunavirThe serum concentration of Vardenafil can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Vardenafil can be increased when it is combined with Dasatinib.
DiltiazemVardenafil may increase the antihypertensive activities of Diltiazem.
DofetilideVardenafil may increase the QTc-prolonging activities of Dofetilide.
DoxazosinVardenafil may increase the hypotensive activities of Doxazosin.
EnalaprilVardenafil may increase the antihypertensive activities of Enalapril.
EnalaprilatVardenafil may increase the antihypertensive activities of Enalaprilat.
EplerenoneVardenafil may increase the antihypertensive activities of Eplerenone.
EprosartanVardenafil may increase the antihypertensive activities of Eprosartan.
Erythrityl TetranitrateVardenafil may increase the vasodilatory activities of Erythrityl Tetranitrate.
ErythromycinThe serum concentration of Vardenafil can be increased when it is combined with Erythromycin.
EsmololVardenafil may increase the antihypertensive activities of Esmolol.
Ethacrynic acidVardenafil may increase the antihypertensive activities of Ethacrynic acid.
EthanolEthanol may increase the hypotensive activities of Vardenafil.
EtravirineThe serum concentration of Vardenafil can be decreased when it is combined with Etravirine.
FelodipineVardenafil may increase the antihypertensive activities of Felodipine.
FluconazoleThe metabolism of Vardenafil can be decreased when combined with Fluconazole.
FosaprepitantThe serum concentration of Vardenafil can be increased when it is combined with Fosaprepitant.
FosinoprilVardenafil may increase the antihypertensive activities of Fosinopril.
FurosemideVardenafil may increase the antihypertensive activities of Furosemide.
Fusidic AcidThe serum concentration of Vardenafil can be increased when it is combined with Fusidic Acid.
GoserelinVardenafil may increase the QTc-prolonging activities of Goserelin.
GuanfacineVardenafil may increase the antihypertensive activities of Guanfacine.
HydralazineVardenafil may increase the antihypertensive activities of Hydralazine.
HydrochlorothiazideVardenafil may increase the antihypertensive activities of Hydrochlorothiazide.
IdelalisibThe serum concentration of Vardenafil can be increased when it is combined with Idelalisib.
IndapamideVardenafil may increase the antihypertensive activities of Indapamide.
IndinavirThe serum concentration of Vardenafil can be increased when it is combined with Indinavir.
IrbesartanVardenafil may increase the antihypertensive activities of Irbesartan.
IsosorbideVardenafil may increase the vasodilatory activities of Isosorbide.
Isosorbide DinitrateVardenafil may increase the vasodilatory activities of Isosorbide Dinitrate.
Isosorbide MononitrateVardenafil may increase the vasodilatory activities of Isosorbide Mononitrate.
IsradipineVardenafil may increase the antihypertensive activities of Isradipine.
ItraconazoleThe serum concentration of Vardenafil can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Vardenafil can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Vardenafil can be increased when it is combined with Ketoconazole.
LabetalolVardenafil may increase the antihypertensive activities of Labetalol.
LeuprolideVardenafil may increase the QTc-prolonging activities of Leuprolide.
LisinoprilVardenafil may increase the antihypertensive activities of Lisinopril.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Vardenafil.
LosartanVardenafil may increase the antihypertensive activities of Losartan.
LuliconazoleThe serum concentration of Vardenafil can be increased when it is combined with Luliconazole.
MannitolVardenafil may increase the antihypertensive activities of Mannitol.
MecamylamineVardenafil may increase the antihypertensive activities of Mecamylamine.
MethyclothiazideVardenafil may increase the antihypertensive activities of Methyclothiazide.
MethyldopaVardenafil may increase the antihypertensive activities of Methyldopa.
MetolazoneVardenafil may increase the antihypertensive activities of Metolazone.
MetoprololVardenafil may increase the antihypertensive activities of Metoprolol.
MifepristoneThe serum concentration of Vardenafil can be increased when it is combined with Mifepristone.
MinoxidilVardenafil may increase the antihypertensive activities of Minoxidil.
MoexiprilVardenafil may increase the antihypertensive activities of Moexipril.
MolsidomineMolsidomine may increase the hypotensive activities of Vardenafil.
MoxonidineVardenafil may increase the antihypertensive activities of Moxonidine.
NadololVardenafil may increase the antihypertensive activities of Nadolol.
NebivololVardenafil may increase the antihypertensive activities of Nebivolol.
NefazodoneThe serum concentration of Vardenafil can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Vardenafil can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Vardenafil can be increased when it is combined with Netupitant.
NicardipineVardenafil may increase the antihypertensive activities of Nicardipine.
NifedipineVardenafil may increase the antihypertensive activities of Nifedipine.
NimodipineVardenafil may increase the antihypertensive activities of Nimodipine.
NisoldipineVardenafil may increase the antihypertensive activities of Nisoldipine.
NitroglycerinVardenafil may increase the vasodilatory activities of Nitroglycerin.
NitroprussideVardenafil may increase the antihypertensive activities of Nitroprusside.
OlmesartanVardenafil may increase the antihypertensive activities of Olmesartan.
PalbociclibThe serum concentration of Vardenafil can be increased when it is combined with Palbociclib.
PenbutololVardenafil may increase the antihypertensive activities of Penbutolol.
PerindoprilVardenafil may increase the antihypertensive activities of Perindopril.
PhenoxybenzamineVardenafil may increase the hypotensive activities of Phenoxybenzamine.
PhentolamineVardenafil may increase the hypotensive activities of Phentolamine.
PindololVardenafil may increase the antihypertensive activities of Pindolol.
PosaconazoleThe serum concentration of Vardenafil can be increased when it is combined with Posaconazole.
PrazosinVardenafil may increase the hypotensive activities of Prazosin.
PropranololVardenafil may increase the antihypertensive activities of Propranolol.
QuinaprilVardenafil may increase the antihypertensive activities of Quinapril.
RamiprilVardenafil may increase the antihypertensive activities of Ramipril.
ReserpineVardenafil may increase the antihypertensive activities of Reserpine.
RiociguatVardenafil may increase the hypotensive activities of Riociguat.
RitonavirThe serum concentration of Vardenafil can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Vardenafil can be increased when it is combined with Saquinavir.
SildenafilThe risk or severity of adverse effects can be increased when Vardenafil is combined with Sildenafil.
SilodosinVardenafil may increase the hypotensive activities of Silodosin.
SimeprevirThe serum concentration of Vardenafil can be increased when it is combined with Simeprevir.
SotalolVardenafil may increase the antihypertensive activities of Sotalol.
SpironolactoneVardenafil may increase the antihypertensive activities of Spironolactone.
StiripentolThe serum concentration of Vardenafil can be increased when it is combined with Stiripentol.
TadalafilThe risk or severity of adverse effects can be increased when Vardenafil is combined with Tadalafil.
TamsulosinVardenafil may increase the hypotensive activities of Tamsulosin.
TelaprevirThe serum concentration of Vardenafil can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Vardenafil can be increased when it is combined with Telithromycin.
TelmisartanVardenafil may increase the antihypertensive activities of Telmisartan.
TerazosinVardenafil may increase the hypotensive activities of Terazosin.
TetrahydrobiopterinTetrahydrobiopterin may increase the hypotensive activities of Vardenafil.
TimololVardenafil may increase the antihypertensive activities of Timolol.
TorasemideVardenafil may increase the antihypertensive activities of Torasemide.
TrandolaprilVardenafil may increase the antihypertensive activities of Trandolapril.
TriamtereneVardenafil may increase the antihypertensive activities of Triamterene.
ValsartanVardenafil may increase the antihypertensive activities of Valsartan.
VerapamilVardenafil may increase the antihypertensive activities of Verapamil.
VoriconazoleThe serum concentration of Vardenafil can be increased when it is combined with Voriconazole.

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • 1,2,4-triazines
  • Alkyl aryl ethers
  • Azacyclic compounds
  • Heteroaromatic compounds
  • Hydrocarbon derivatives
  • N-alkylpiperazines
  • N-substituted imidazoles
  • Phenol ethers
  • Sulfonamides
  • Sulfonyls
  • Trialkylamines

substituent:
  • 1,2,4-triazine
  • 1,4-diazinane
  • Alkyl aryl ether
  • Amine
  • Aromatic heteropolycyclic compound
  • Azacycle
  • Azole
  • Benzenesulfonamide
  • Ether
  • Heteroaromatic compound
  • Hydrocarbon derivative
  • Imidazole
  • N-alkylpiperazine
  • N-substituted imidazole
  • Organoheterocyclic compound
  • Organonitrogen compound
  • Organooxygen compound
  • Organosulfur compound
  • Phenol ether
  • Piperazine
  • Sulfonamide
  • Sulfonic acid derivative
  • Sulfonyl
  • Tertiary aliphatic amine
  • Tertiary amine
  • Triazine

References

Synthesis Reference: 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.
General Reference: Not Available
External Links:
ResourceLink
RxListhttp://www.rxlist.com/cgi/generic3/levitra.htm
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/lev1688.shtml
Drugs.comhttp://www.drugs.com/cdi/vardenafil.html

ATC Codes:
  • Array

AHFS Codes:
  • 24:12.12

MSDS: Download
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