General Information of Drug (ID: DMTBGW8)

Drug Name
Vardenafil
Synonyms
VDN; Levitra (TN); VARDENAFIL, LEVITRA; Vardenafil (INN); 1-((3-(3,4-Dihydro-5-methyl-4-oxo-7-propylimidazo(5,1-f)-as-triazin-2-yl)-4-ethoxyphenyl)sulfonyl)-4-ethylpiperazine; 2-(2-Ethoxy-5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl)-5-methyl-7-propyl-3H-imidazo(5,1-f)(1,2,4)triazin-4-one; 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one; 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE; 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4-ol
Indication
Disease Entry ICD 11 Status REF
Erectile dysfunction HA01.1 Approved [1], [2]
Therapeutic Class
Antiimpotence Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 488.6
Topological Polar Surface Area (xlogp) 2.5
Rotatable Bond Count (rotbonds) 8
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Bioavailability
The bioavailability of drug is 15% [4]
Clearance
The clearance of drug is 56 L/h [5]
Elimination
4% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 4 - 5 hours [6]
Metabolism
The drug is metabolized via the hepatic enzyme CYP3A4 [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.5847 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.05% [6]
Vd
The volume of distribution (Vd) of drug is 208 L [5]
Water Solubility
The ability of drug to dissolve in water is measured as 0.11 mg/mL [3]
Chemical Identifiers
Formula
C23H32N6O4S
IUPAC Name
2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one
Canonical SMILES
CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C
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)
InChIKey
SECKRCOLJRRGGV-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
135400189
ChEBI ID
CHEBI:46295
CAS Number
224785-90-4
DrugBank ID
DB00862
TTD ID
D0C9SY
VARIDT ID
DR00169
INTEDE ID
DR1673
ACDINA ID
D00721

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Phosphodiesterase 5A (PDE5A) TTJ0IQB PDE5A_HUMAN Binder [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [9]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [10]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Erectile dysfunction
ICD Disease Classification HA01.1
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Phosphodiesterase 5A (PDE5A) DTT PDE5A 1.60E-01 -0.25 -0.99
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.78E-02 4.07E-01 1.09E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 3.90E-02 -3.45E-01 -1.49E+00
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Vardenafil (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Vardenafil and Ivosidenib. Acute myeloid leukaemia [2A60] [39]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Midostaurin. Acute myeloid leukaemia [2A60] [40]
Idarubicin DMM0XGL Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Idarubicin. Acute myeloid leukaemia [2A60] [40]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Arn-509. Acute myeloid leukaemia [2A60] [41]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Gilteritinib. Acute myeloid leukaemia [2A60] [42]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Oliceridine. Acute pain [MG31] [40]
Rivastigmine DMG629M Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Rivastigmine. Alzheimer disease [8A20] [40]
Metronidazole DMTIVEN Moderate Decreased metabolism of Vardenafil caused by Metronidazole mediated inhibition of CYP450 enzyme. Amoebiasis [1A36] [43]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Vardenafil and Ivabradine. Angina pectoris [BA40] [41]
Bepridil DM0RKS4 Major Increased risk of prolong QT interval by the combination of Vardenafil and Bepridil. Angina pectoris [BA40] [43]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Vardenafil and Dronedarone. Angina pectoris [BA40] [40]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Vardenafil and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [44]
Cilostazol DMZMSCT Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Cilostazol. Arterial occlusive disease [BD40] [40]
Posaconazole DMUL5EW Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Posaconazole. Aspergillosis [1F20] [40]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Levalbuterol. Asthma [CA23] [45]
Terbutaline DMD4381 Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Terbutaline. Asthma [CA23] [46]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Pirbuterol. Asthma [CA23] [46]
Salbutamol DMN9CWF Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Salbutamol. Asthma [CA23] [45]
Formoterol DMSOURV Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Formoterol. Asthma [CA23] [46]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [41]
Desipramine DMT2FDC Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Desipramine. Attention deficit hyperactivity disorder [6A05] [40]
Ofloxacin DM0VQN3 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Ofloxacin. Bacterial infection [1A00-1C4Z] [47]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Vardenafil caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [48]
Clarithromycin DM4M1SG Major Decreased metabolism of Vardenafil caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [49]
Sulfamethoxazole DMB08GE Moderate Decreased metabolism of Vardenafil caused by Sulfamethoxazole mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [43]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Vardenafil and Sparfloxacin. Bacterial infection [1A00-1C4Z] [47]
Gemifloxacin DMHT34O Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Gemifloxacin. Bacterial infection [1A00-1C4Z] [47]
Norfloxacin DMIZ6W2 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Norfloxacin. Bacterial infection [1A00-1C4Z] [47]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Levofloxacin. Bacterial infection [1A00-1C4Z] [47]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Vardenafil caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [43]
Lomefloxacin DMVRH9C Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Lomefloxacin. Bacterial infection [1A00-1C4Z] [40]
Telithromycin DMZ4P3A Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Telithromycin. Bacterial infection [1A00-1C4Z] [40]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Retigabine. Behcet disease [4A62] [40]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Eribulin. Breast cancer [2C60-2C6Y] [40]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Lapatinib. Breast cancer [2C60-2C6Y] [40]
Tucatinib DMBESUA Moderate Decreased metabolism of Vardenafil caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [43]
Palbociclib DMD7L94 Moderate Decreased metabolism of Vardenafil caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [43]
Alpelisib DMEXMYK Moderate Increased metabolism of Vardenafil caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [50]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Bosutinib. Breast cancer [2C60-2C6Y] [41]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [51]
Olodaterol DM62B78 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Olodaterol. Chronic obstructive pulmonary disease [CA22] [46]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Vilanterol. Chronic obstructive pulmonary disease [CA22] [45]
Salmeterol DMIEU69 Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Salmeterol. Chronic obstructive pulmonary disease [CA22] [46]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Indacaterol. Chronic obstructive pulmonary disease [CA22] [46]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Arformoterol. Chronic obstructive pulmonary disease [CA22] [46]
Isoproterenol DMK7MEY Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Isoproterenol. Conduction disorder [BC63] [45]
Halothane DM80OZ5 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Halothane. Corneal disease [9A76-9A78] [40]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Sevoflurane. Corneal disease [9A76-9A78] [40]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Probucol. Coronary atherosclerosis [BA80] [40]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Vardenafil and Pasireotide. Cushing syndrome [5A70] [40]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Osilodrostat. Cushing syndrome [5A70] [41]
Lumacaftor DMCLWDJ Moderate Increased metabolism of Vardenafil caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [52]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Vardenafil caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [43]
Ethanol DMDRQZU Moderate Additive hypotensive effects by the combination of Vardenafil and Ethanol. Cystitis [GC00] [41]
MK-8228 DMOB58Q Moderate Decreased metabolism of Vardenafil caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [43]
Sertraline DM0FB1J Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Sertraline. Depression [6A70-6A7Z] [40]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Vardenafil caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [43]
Selegiline DM6034S Moderate Additive hypotensive effects by the combination of Vardenafil and Selegiline. Depression [6A70-6A7Z] [53]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Vardenafil and Isocarboxazid. Depression [6A70-6A7Z] [53]
Escitalopram DMFK9HG Major Increased risk of prolong QT interval by the combination of Vardenafil and Escitalopram. Depression [6A70-6A7Z] [40]
Clomipramine DMINRKW Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Clomipramine. Depression [6A70-6A7Z] [40]
Doxepin DMPI98T Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Doxepin. Depression [6A70-6A7Z] [40]
Maprotiline DMPWB7T Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Maprotiline. Depression [6A70-6A7Z] [40]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [40]
Deutetrabenazine DMUPFLI Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Deutetrabenazine. Dystonic disorder [8A02] [54]
Ingrezza DMVPLNC Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Ingrezza. Dystonic disorder [8A02] [55]
Stiripentol DMMSDOY Moderate Decreased metabolism of Vardenafil caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [43]
Rufinamide DMWE60C Moderate Increased metabolism of Vardenafil caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [41]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Solifenacin. Functional bladder disorder [GC50] [40]
Itraconazole DMCR1MV Major Decreased metabolism of Vardenafil caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [49]
Miconazole DMPMYE8 Moderate Decreased metabolism of Vardenafil caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [43]
Ketoconazole DMPZI3Q Major Decreased metabolism of Vardenafil caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [49]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Sunitinib. Gastrointestinal stromal tumour [2B5B] [40]
Sulfinpyrazone DMEV954 Moderate Decreased metabolism of Vardenafil caused by Sulfinpyrazone mediated inhibition of CYP450 enzyme. Gout [FA25] [43]
Boceprevir DMBSHMF Major Decreased metabolism of Vardenafil caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [43]
Simeprevir DMLUA9D Moderate Decreased metabolism of Vardenafil caused by Simeprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [56]
Telaprevir DMMRV29 Major Decreased metabolism of Vardenafil caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [57]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Vardenafil caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [43]
Rifapentine DMCHV4I Moderate Increased metabolism of Vardenafil caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [58]
Procarbazine DMIK367 Moderate Additive hypotensive effects by the combination of Vardenafil and Procarbazine. Hodgkin lymphoma [2B30] [53]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Vardenafil caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [43]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [59]
Cobicistat DM6L4H2 Major Decreased metabolism of Vardenafil caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [41]
Saquinavir DMG814N Major Decreased metabolism of Vardenafil caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [60]
Etravirine DMGV8QU Moderate Increased metabolism of Vardenafil caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [61]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [40]
Darunavir DMN3GCH Moderate Decreased metabolism of Vardenafil caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [43]
Atazanavir DMSYRBX Moderate Decreased metabolism of Vardenafil caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [49]
Gemfibrozil DMD8Q3J Moderate Decreased metabolism of Vardenafil caused by Gemfibrozil mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [43]
Fenofibrate DMFKXDY Moderate Decreased metabolism of Vardenafil caused by Fenofibrate mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [43]
BMS-201038 DMQTAGO Moderate Decreased metabolism of Vardenafil caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [43]
Conivaptan DM1V329 Moderate Decreased metabolism of Vardenafil caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [62]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Vardenafil caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [43]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Polyethylene glycol. Irritable bowel syndrome [DD91] [41]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Phenolphthalein. Irritable bowel syndrome [DD91] [40]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Vardenafil and Crizotinib. Lung cancer [2C25] [63]
Brigatinib DM7W94S Moderate Increased metabolism of Vardenafil caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [64]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Vardenafil and Ceritinib. Lung cancer [2C25] [40]
PF-06463922 DMKM7EW Moderate Increased metabolism of Vardenafil caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [65]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Vardenafil and Osimertinib. Lung cancer [2C25] [66]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Vardenafil and Selpercatinib. Lung cancer [2C25] [41]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Vardenafil and Lumefantrine. Malaria [1F40-1F45] [49]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Vardenafil and Halofantrine. Malaria [1F40-1F45] [67]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Vardenafil and Hydroxychloroquine. Malaria [1F40-1F45] [68]
Primaquine DMWQ16I Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Primaquine. Malaria [1F40-1F45] [40]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [41]
Idelalisib DM602WT Moderate Decreased metabolism of Vardenafil caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [43]
IPI-145 DMWA24P Moderate Decreased metabolism of Vardenafil caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [43]
Arsenic trioxide DM61TA4 Major Increased risk of ventricular arrhythmias by the combination of Vardenafil and Arsenic trioxide. Mature B-cell lymphoma [2A85] [69]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Vardenafil and Vemurafenib. Melanoma [2C30] [40]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and LGX818. Melanoma [2C30] [70]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Vardenafil caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [41]
Danazol DML8KTN Moderate Decreased metabolism of Vardenafil caused by Danazol mediated inhibition of CYP450 enzyme. Menstrual cycle bleeding disorder [GA20] [43]
Exjade DMHPRWG Moderate Decreased metabolism of Vardenafil caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [71]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Vardenafil and Panobinostat. Multiple myeloma [2A83] [72]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Vardenafil and Thalidomide. Multiple myeloma [2A83] [49]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Vardenafil and Siponimod. Multiple sclerosis [8A40] [49]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Vardenafil and Fingolimod. Multiple sclerosis [8A40] [40]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Vardenafil and Ozanimod. Multiple sclerosis [8A40] [73]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Romidepsin. Mycosis fungoides [2B01] [40]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Vardenafil caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [43]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Dasatinib. Myeloproliferative neoplasm [2A20] [74]
Promethazine DM6I5GR Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Promethazine. Nausea/vomiting [MD90] [40]
Granisetron DMIUW25 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Granisetron. Nausea/vomiting [MD90] [40]
Ondansetron DMOTQ1I Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Ondansetron. Nausea/vomiting [MD90] [40]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Entrectinib. Non-small cell lung cancer [2C25] [49]
Levomethadyl Acetate DM06HG5 Major Increased risk of prolong QT interval by the combination of Vardenafil and Levomethadyl Acetate. Opioid use disorder [6C43] [41]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Vardenafil and Lofexidine. Opioid use disorder [6C43] [40]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Rucaparib. Ovarian cancer [2C73] [40]
Buprenorphine DMPRI8G Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Buprenorphine. Pain [MG30-MG3Z] [40]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Triclabendazole. Parasitic worm infestation [1F90] [40]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Vardenafil and Safinamide. Parkinsonism [8A00] [53]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Vardenafil and Rasagiline. Parkinsonism [8A00] [53]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Pimavanserin. Parkinsonism [8A00] [75]
Abametapir DM2RX0I Moderate Decreased metabolism of Vardenafil caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [76]
Famotidine DMRL3AB Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Famotidine. Peptic ulcer [DA61] [49]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Vardenafil and Macimorelin. Pituitary gland disorder [5A60-5A61] [77]
Lefamulin DME6G97 Major Decreased metabolism of Vardenafil caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [78]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Vardenafil caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [43]
Ritodrine DM4V6RL Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Ritodrine. Preterm labour/delivery [JB00] [46]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Degarelix. Prostate cancer [2C82] [41]
ABIRATERONE DM8V75C Moderate Increased risk of prolong QT interval by the combination of Vardenafil and ABIRATERONE. Prostate cancer [2C82] [41]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Enzalutamide. Prostate cancer [2C82] [41]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Relugolix. Prostate cancer [2C82] [41]
Bicalutamide DMZMSPF Moderate Decreased metabolism of Vardenafil caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [43]
Levomepromazine DMIKFEL Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Levomepromazine. Psychotic disorder [6A20-6A25] [40]
Gatifloxacin DMSL679 Major Increased risk of prolong QT interval by the combination of Vardenafil and Gatifloxacin. Respiratory infection [CA07-CA4Z] [79]
Leflunomide DMR8ONJ Moderate Decreased metabolism of Vardenafil caused by Leflunomide mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [43]
Quetiapine DM1N62C Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Quetiapine. Schizophrenia [6A20] [40]
Mesoridazine DM2ZGAN Major Increased risk of prolong QT interval by the combination of Vardenafil and Mesoridazine. Schizophrenia [6A20] [40]
Aripiprazole DM3NUMH Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Aripiprazole. Schizophrenia [6A20] [49]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Vardenafil and Iloperidone. Schizophrenia [6A20] [40]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Paliperidone. Schizophrenia [6A20] [40]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Vardenafil and Amisulpride. Schizophrenia [6A20] [80]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Asenapine. Schizophrenia [6A20] [40]
Pimozide DMW83TP Major Increased risk of prolong QT interval by the combination of Vardenafil and Pimozide. Schizophrenia [6A20] [41]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Vardenafil caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [43]
Larotrectinib DM26CQR Moderate Decreased metabolism of Vardenafil caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [43]
Armodafinil DMGB035 Minor Increased metabolism of Vardenafil caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [81]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Vardenafil and LEE011. Solid tumour/cancer [2A00-2F9Z] [40]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Vardenafil and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [40]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [41]
Doxorubicin DMVP5YE Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [40]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Pitolisant. Somnolence [MG42] [41]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [40]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Vardenafil caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [82]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Lenvatinib. Thyroid cancer [2D10] [40]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Vardenafil and Cabozantinib. Thyroid cancer [2D10] [41]
Tacrolimus DMZ7XNQ Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Tacrolimus. Transplant rejection [NE84] [40]
Trimeprazine DMEMV9D Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [83]
Procainamide DMNMXR8 Major Increased risk of prolong QT interval by the combination of Vardenafil and Procainamide. Ventricular tachyarrhythmia [BC71] [43]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Propafenone. Ventricular tachyarrhythmia [BC71] [40]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Vardenafil and Flecainide. Ventricular tachyarrhythmia [BC71] [40]
Amiodarone DMUTEX3 Major Increased risk of prolong QT interval by the combination of Vardenafil and Amiodarone. Ventricular tachyarrhythmia [BC71] [43]
⏷ Show the Full List of 174 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Aspartame E00402 134601 Flavoring agent
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Crospovidone E00626 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Hexahydric alcohol E00083 5780 Diluent; Flavoring agent; Humectant; Plasticizing agent
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
⏷ Show the Full List of 9 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Vardenafil 10 mg tablet 10 mg Disintegrating Oral Tablet Oral
Vardenafil 10 mg tablet 10 mg Oral Tablet Oral
Vardenafil 2.5 mg tablet 2.5 mg Oral Tablet Oral
Vardenafil 20 mg tablet 20 mg Oral Tablet Oral
Vardenafil 5 mg tablet 5 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7320).
2 Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66.
3 BDDCS applied to over 900 drugs
4 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
5 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
6 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
7 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8 The effect of vardenafil, a potent and highly selective phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, on the cardiovascular response to exercise in patients with coronary artery disease. J Am Coll Cardiol. 2002 Dec 4;40(11):2006-12.
9 Erectile dysfunction drugs changed the protein expressions and activities of drug-metabolising enzymes in the liver of male rats. Oxid Med Cell Longev. 2016;2016:4970906.
10 The contributions of cytochromes P450 3A4 and 3A5 to the metabolism of the phosphodiesterase type 5 inhibitors sildenafil, udenafil, and vardenafil. Drug Metab Dispos. 2008 Jun;36(6):986-90.
11 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
12 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
13 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
14 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
15 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
16 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
17 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
18 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
19 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
20 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
21 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
22 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
23 Drug Interactions Flockhart Table
24 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
25 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
26 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
27 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
28 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
29 Pulmonary arterial hypertension: the most devastating vascular complication of systemic sclerosis. Rheumatology (Oxford). 2009 Jun;48 Suppl 3:iii25-31.
30 Increased expression of the nitric oxide synthase gene and protein in corpus cavernosum by repeated dosing of udenafil in a rat model of chemical d... Asian J Androl. 2009 Jul;11(4):435-42.
31 Anti-platelet therapy: phosphodiesterase inhibitors.Br J Clin Pharmacol.2011 Oct;72(4):634-46.
32 Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8.
33 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
34 cGMP-hydrolytic activity and its inhibition by sildenafil in normal and failing human and mouse myocardium. J Pharmacol Exp Ther. 2009 Sep;330(3):884-91.
35 Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008 Sep;71(9):1513-7.
36 Exisulind induction of apoptosis involves guanosine 3',5'-cyclic monophosphate phosphodiesterase inhibition, protein kinase G activation, and attenuated beta-catenin. Cancer Res. 2000 Jul 1;60(13):3338-42.
37 Highlights of the society for medicinesresearch symposium held december 10th 2009 at the national heart and lung institute, London, UK. Drugs of the Future 2010, 35(4): 349-358.
38 Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6033-6.
39 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
40 Canadian Pharmacists Association.
41 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
42 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
43 Product Information. Levitra (vardenafil). Bayer, West Haven, CT.
44 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
45 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
46 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
47 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
48 Gunston GD, Mehta U "Potentially serious drug interactions with grapefruit juice." S Afr Med J 90 (2000): 41. [PMID: 10721388]
49 Cerner Multum, Inc. "Australian Product Information.".
50 Product Information. Piqray (alpelisib). Novartis Pharmaceuticals, East Hanover, NJ.
51 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
52 Cerner Multum, Inc. "Canadian Product Information.".
53 Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
54 Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
55 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
56 Product Information. Olysio (simeprevir). Janssen Pharmaceuticals, Titusville, NJ.
57 Product Information. Incivek (telaprevir). Vertex Pharmaceuticals, Cambridge, MA.
58 Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO.
59 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
60 Bertics PJ, Wiepz GJ "New Developments with Vancomycin-Resistant Enterococci: E. faecium-Friend or Foe?" J Infect Dis (2009):. [PMID: 19604048]
61 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
62 Hall MCS, Ahmad S "Interaction between sildenafil and HIV-1 combination therapy." Lancet 353 (1999): 2071-2. [PMID: 10376645]
63 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
64 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
65 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
66 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
67 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
68 Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
69 Ohnishi K, Yoshida H, Shigeno K, et al. "Prolongation of the QT interval and ventricular tachycardia in patients treated with arsenic trioxide for acute promyelocytic leukemia." Ann Intern Med 133 (2000): 881-5. [PMID: 11103058]
70 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
71 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
72 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
73 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
74 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
75 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
76 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
77 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
78 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
79 Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]
80 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
81 Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
82 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
83 Iannini PB "Cardiotoxicity of macrolides, ketolides and fluoroquinolones that prolong the QTc interval." Expert Opin Drug Saf 1 (2002): 121-8. [PMID: 12904146]