Details of the Drug

General Information of Drug (ID: DMUTEX3)

Drug Name
Amiodarone
Synonyms
Amidorone; Aminodarone; Amiobeta; Amiodarex; Amiodarona; Amiodarons; Amiodaronum; Amiohexal; Amjodaronum; Ancar; Aratac;Arycor; Braxan; Corbionax; Cordarex; Cordarone; Kordaron; Labaz; Ortacrone; Pacerone; Rytmarone; Sedacoron; Sedacorone; Tachydaron; ASTA Medica Brand of Amiodarone Hydrochloride; Alphapharm Brand of Amiodarone Hydrochloride; Amiodarone Base; Armstrong Brand of Amiodarone Hydrochloride; Berenguer Infale Brand of Amiodarone Hydrochloride; Betapharm Brand of Amiodarone Hydrochloride; Cordarone Intravenous; G Gam Brand of Amiodarone Hydrochloride; Hexal Brand of Amiodarone Hydrochloride; Leurquin Brand of Amiodarone Hydrochloride; Pharma Investi Brand of Amiodarone Hydrochloride; Sanofi Winthrop Brand of Amiodarone Hydrochloride; Wyeth Brand of Amiodarone Hydrochloride; Ethylaminoethoxy)benzoyl]benzofuran; L 3428; L3428; SKF 33134A; Amio-Aqueous IV; Amiodarona [INN-Spanish]; Amiodaronum [INN-Latin]; Aratac (TN); Arycor (TN); Atlansil (TN); Cordarone (TN); L-3428; Pacerone (TN); Pms-Amiodarone; SKF 33134-A; Amiodarone (USAN/INN); Amiodarone [USAN:BAN:INN]; Ketone, 2-butyl-3-benzofuranyl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl; Ketone, 2-butyl-3-benzofuranyl 4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl (7CI,8CI); (2-Butyl-3-benzofuranyl)(4-(2-(diethylamino)ethoxy)-3,5-diidophenyl)methanone; (2-butyl-1-benzofuran-3-yl)(4-{[2-(diethylamino)ethyl]oxy}-3,5-diiodophenyl)methanone; (2-butyl-1-benzofuran-3-yl)-[4-(2-diethylaminoethyloxy)-3,5-diiodophenyl]methanone; (2-butyl-1-benzofuran-3-yl){4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl}methanone; (2-butylbenzofuran-3-yl)-[4-(2-diethylaminoethoxy)-3,5-diiodo-phenyl]-methanone; (2-{4-[(2-butyl-1-benzofuran-3-yl)carbonyl]-2,6-diiodophenoxy}ethyl)diethylamine; 2-Butyl-3-(3,5-diiodo-4-(2-diethylaminoethoxy)benzoyl)benzofuran; 2-Butyl-3-(3,5-diiodo-4-(beta-diethylaminoethoxy)benzoyl)benzofuran; 2-Butyl-3-(4'-beta-N-diethylaminoethoxy-3',5'-diiodobenzoyl)benzofuran; 2-Butyl-3-[3,5-diiodo-4-(2-di; 2-Butyl-3-benzofuranyl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl ketone; 2-Butyl-3-benzofuranyl p-((2-diethylamino)ethoxy)-m,m-diiodophenyl ketone; 2-Butyl-3-benzofuranyl p-[(2-diethylamino)ethoxy]-m,m-diiodophenyl ketone; 2-n-Butyl-3',5'-diiodo-4'-N-diethylaminoethoxy-3-benzoylbenzofuran
Indication
Disease Entry ICD 11 Status REF
Tachyarrhythmias BC71 Approved [1], [2]
Therapeutic Class
Antiarrhythmic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 3 Molecular Weight (mw) 645.3
Topological Polar Surface Area (xlogp) 7.6
Rotatable Bond Count (rotbonds) 11
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Clearance
The drug present in the plasma can be removed from the body at the rate of 1.9 mL/min/kg [4]
Elimination
0% 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 820 hours [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 41.37459 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.0002% [4]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 60 L/kg [4]
Water Solubility
The ability of drug to dissolve in water is measured as 0.7 mg/mL [3]
Chemical Identifiers
Formula
C25H29I2NO3
IUPAC Name
(2-butyl-1-benzofuran-3-yl)-[4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl]methanone
Canonical SMILES
CCCCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I
InChI
InChI=1S/C25H29I2NO3/c1-4-7-11-22-23(18-10-8-9-12-21(18)31-22)24(29)17-15-19(26)25(20(27)16-17)30-14-13-28(5-2)6-3/h8-10,12,15-16H,4-7,11,13-14H2,1-3H3
InChIKey
IYIKLHRQXLHMJQ-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2157
ChEBI ID
CHEBI:2663
CAS Number
1951-25-3
DrugBank ID
DB01118
TTD ID
D0L5WM
VARIDT ID
DR00642
INTEDE ID
DR0093
ACDINA ID
D00031

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Potassium channel unspecific (KC) TT1VOHK NOUNIPROTAC Modulator [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [8]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [9]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [10]
Cytochrome P450 1A1 (CYP1A1) DE6OQ3W CP1A1_HUMAN Substrate [11]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [11]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [12]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [13]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Amiodarone
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Propafenone DMPIBJK Major Increased risk of prolong QT interval by the combination of Amiodarone and Propafenone. Ventricular tachyarrhythmia [BC71] [78]
Flecainide DMSQDLE Major Decreased metabolism of Amiodarone caused by Flecainide mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [79]
Coadministration of a Drug Treating the Disease Different from Amiodarone (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Amiodarone and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [80]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Amiodarone and Ivosidenib. Acute myeloid leukaemia [2A60] [81]
Midostaurin DMI6E0R Major Increased risk of prolong QT interval by the combination of Amiodarone and Midostaurin. Acute myeloid leukaemia [2A60] [81]
Idarubicin DMM0XGL Major Increased risk of prolong QT interval by the combination of Amiodarone and Idarubicin. Acute myeloid leukaemia [2A60] [81]
Arn-509 DMT81LZ Major Increased risk of prolong QT interval by the combination of Amiodarone and Arn-509. Acute myeloid leukaemia [2A60] [81]
Gilteritinib DMWQ4MZ Major Increased risk of prolong QT interval by the combination of Amiodarone and Gilteritinib. Acute myeloid leukaemia [2A60] [81]
Oliceridine DM6MDCF Major Increased risk of prolong QT interval by the combination of Amiodarone and Oliceridine. Acute pain [MG31] [81]
Emapalumab DMZG5WL Moderate Altered metabolism of Amiodarone due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [82]
Siltuximab DMGEATB Moderate Altered metabolism of Amiodarone due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [82]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Ivabradine. Angina pectoris [BA40] [82]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Amiodarone and Dronedarone. Angina pectoris [BA40] [81]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Amiodarone and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [81]
Cilostazol DMZMSCT Moderate Decreased metabolism of Amiodarone caused by Cilostazol mediated inhibition of CYP450 enzyme. Arterial occlusive disease [BD40] [81]
Posaconazole DMUL5EW Major Decreased metabolism of Amiodarone caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [83]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Amiodarone and Levalbuterol. Asthma [CA23] [84]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Amiodarone and Pirbuterol. Asthma [CA23] [85]
Budesonide DMJIBAW Moderate Decreased metabolism of Amiodarone caused by Budesonide mediated inhibition of CYP450 enzyme. Asthma [CA23] [86]
Aminophylline DML2NIB Moderate Decreased metabolism of Amiodarone caused by Aminophylline mediated inhibition of CYP450 enzyme. Asthma [CA23] [87]
Roflumilast DMPGHY8 Moderate Decreased metabolism of Amiodarone caused by Roflumilast mediated inhibition of CYP450 enzyme. Asthma [CA23] [82]
Lisdexamfetamine DM6W8V5 Major Increased risk of prolong QT interval by the combination of Amiodarone and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [81]
Desipramine DMT2FDC Major Increased risk of prolong QT interval by the combination of Amiodarone and Desipramine. Attention deficit hyperactivity disorder [6A05] [81]
Ofloxacin DM0VQN3 Major Increased risk of prolong QT interval by the combination of Amiodarone and Ofloxacin. Bacterial infection [1A00-1C4Z] [88]
Dalfopristin DM4LTKV Major Decreased metabolism of Amiodarone caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [89]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Amiodarone and Sparfloxacin. Bacterial infection [1A00-1C4Z] [88]
Gemifloxacin DMHT34O Major Increased risk of prolong QT interval by the combination of Amiodarone and Gemifloxacin. Bacterial infection [1A00-1C4Z] [88]
Levofloxacin DMS60RB Major Increased risk of prolong QT interval by the combination of Amiodarone and Levofloxacin. Bacterial infection [1A00-1C4Z] [88]
Troleandomycin DMUZNIG Major Increased risk of prolong QT interval by the combination of Amiodarone and Troleandomycin. Bacterial infection [1A00-1C4Z] [90]
Retigabine DMGNYIH Major Increased risk of prolong QT interval by the combination of Amiodarone and Retigabine. Behcet disease [4A62] [81]
Cariprazine DMJYDVK Moderate Decreased metabolism of Amiodarone caused by Cariprazine mediated inhibition of CYP450 enzyme. Bipolar disorder [6A60] [82]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Amiodarone and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [91]
Eribulin DM1DX4Q Major Increased risk of prolong QT interval by the combination of Amiodarone and Eribulin. Breast cancer [2C60-2C6Y] [81]
Talazoparib DM1KS78 Major Decreased clearance of Amiodarone due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [82]
Lapatinib DM3BH1Y Major Increased risk of prolong QT interval by the combination of Amiodarone and Lapatinib. Breast cancer [2C60-2C6Y] [81]
Tucatinib DMBESUA Moderate Decreased metabolism of Amiodarone caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [92]
Cabazitaxel DMPAZHC Moderate Decreased metabolism of Amiodarone caused by Cabazitaxel mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [93]
Bosutinib DMTI8YE Major Increased risk of prolong QT interval by the combination of Amiodarone and Bosutinib. Breast cancer [2C60-2C6Y] [81]
Macitentan DMP79A1 Moderate Decreased metabolism of Amiodarone caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [94]
Iodipamide DMXIQYS Moderate Increased risk of ventricular arrhythmias by the combination of Amiodarone and Iodipamide. Cholelithiasis [DC11] [95]
Corticotropin DMP9TWZ Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Corticotropin. Chronic kidney disease [GB61] [96]
PF-04449913 DMSB068 Major Increased risk of prolong QT interval by the combination of Amiodarone and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [81]
Olodaterol DM62B78 Moderate Increased risk of prolong QT interval by the combination of Amiodarone and Olodaterol. Chronic obstructive pulmonary disease [CA22] [85]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Amiodarone and Vilanterol. Chronic obstructive pulmonary disease [CA22] [84]
Indacaterol DMQJHR7 Moderate Increased risk of ventricular arrhythmias by the combination of Amiodarone and Indacaterol. Chronic obstructive pulmonary disease [CA22] [85]
Arformoterol DMYM974 Moderate Increased risk of prolong QT interval by the combination of Amiodarone and Arformoterol. Chronic obstructive pulmonary disease [CA22] [85]
Anisindione DM2C48U Major Decreased metabolism of Amiodarone caused by Anisindione mediated inhibition of CYP450 enzyme. Coagulation defect [3B10] [97]
Panitumumab DMQPD1F Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Panitumumab. Colorectal cancer [2B91] [96]
Intedanib DMSTA36 Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Intedanib. Colorectal cancer [2B91] [98]
Ulipristal DMBNI20 Minor Decreased metabolism of Amiodarone caused by Ulipristal mediated inhibition of CYP450 enzyme. Contraceptive management [QA21] [82]
Halothane DM80OZ5 Major Increased risk of prolong QT interval by the combination of Amiodarone and Halothane. Corneal disease [9A76-9A78] [81]
Sevoflurane DMC9O43 Major Increased risk of prolong QT interval by the combination of Amiodarone and Sevoflurane. Corneal disease [9A76-9A78] [81]
Probucol DMVZQ2M Major Increased risk of prolong QT interval by the combination of Amiodarone and Probucol. Coronary atherosclerosis [BA80] [81]
Oxtriphylline DMLHSE3 Moderate Decreased metabolism of Amiodarone caused by Oxtriphylline mediated inhibition of CYP450 enzyme. Cough [MD12] [87]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Amiodarone and Pasireotide. Cushing syndrome [5A70] [81]
Osilodrostat DMIJC9X Major Increased risk of prolong QT interval by the combination of Amiodarone and Osilodrostat. Cushing syndrome [5A70] [81]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Amiodarone caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [99]
Rivaroxaban DMQMBZ1 Moderate Decreased metabolism of Amiodarone caused by Rivaroxaban mediated inhibition of CYP450 enzyme. Deep vein thrombosis [BD71] [100]
Vilazodone DM4LECQ Moderate Decreased metabolism of Amiodarone caused by Vilazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [101]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Amiodarone caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [102]
Escitalopram DMFK9HG Major Increased risk of prolong QT interval by the combination of Amiodarone and Escitalopram. Depression [6A70-6A7Z] [81]
Clomipramine DMINRKW Major Increased risk of prolong QT interval by the combination of Amiodarone and Clomipramine. Depression [6A70-6A7Z] [81]
Doxepin DMPI98T Major Increased risk of prolong QT interval by the combination of Amiodarone and Doxepin. Depression [6A70-6A7Z] [81]
Ospemifene DMC4GEI Moderate Decreased metabolism of Amiodarone caused by Ospemifene mediated inhibition of CYP450 enzyme. Dyspareunia [GA12] [103]
Deutetrabenazine DMUPFLI Major Increased risk of prolong QT interval by the combination of Amiodarone and Deutetrabenazine. Dystonic disorder [8A02] [81]
Ingrezza DMVPLNC Major Increased risk of prolong QT interval by the combination of Amiodarone and Ingrezza. Dystonic disorder [8A02] [81]
Cenobamate DMGOVHA Moderate Increased metabolism of Amiodarone caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [104]
Stiripentol DMMSDOY Moderate Decreased metabolism of Amiodarone caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [82]
Brivaracetam DMSEPK8 Minor Decreased metabolism of Amiodarone caused by Brivaracetam mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [82]
Rufinamide DMWE60C Moderate Increased metabolism of Amiodarone caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [82]
Phenobarbital DMXZOCG Major Increased metabolism of Amiodarone caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [105]
Eslicarbazepine DMZREFQ Major Increased metabolism of Amiodarone caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [105]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Amiodarone and Cannabidiol. Epileptic encephalopathy [8A62] [82]
Nadolol DMW6GVL Moderate Increased risk of atrioventricular block by the combination of Amiodarone and Nadolol. Essential hypertension [BA00] [106]
Tazemetostat DMWP1BH Moderate Increased metabolism of Amiodarone caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [107]
Solifenacin DMG592Q Major Increased risk of prolong QT interval by the combination of Amiodarone and Solifenacin. Functional bladder disorder [GC50] [81]
Mirabegron DMS1GYT Minor Decreased metabolism of Amiodarone caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [108]
Itraconazole DMCR1MV Major Decreased metabolism of Amiodarone caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [83]
Ripretinib DM958QB Moderate Decreased metabolism of Amiodarone caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [80]
Sunitinib DMCBJSR Major Increased risk of prolong QT interval by the combination of Amiodarone and Sunitinib. Gastrointestinal stromal tumour [2B5B] [81]
Avapritinib DMK2GZX Moderate Decreased metabolism of Amiodarone caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [82]
Dichlorphenamide DMH7IDQ Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Dichlorphenamide. Glaucoma [9C61] [96]
Metipranolol DMJMVKI Moderate Increased risk of atrioventricular block by the combination of Amiodarone and Metipranolol. Glaucoma [9C61] [106]
Levobunolol DMTNFCQ Moderate Increased risk of bradycardia by the combination of Amiodarone and Levobunolol. Glaucoma [9C61] [106]
Carvedilol DMHTEAO Moderate Increased risk of bradycardia by the combination of Amiodarone and Carvedilol. Heart failure [BD10-BD1Z] [106]
Digitoxin DMWVIGP Major Increased plasma concentration of Amiodarone and Digitoxin due to competitive binding of plasma proteins. Heart failure [BD10-BD1Z] [109]
Boceprevir DMBSHMF Major Decreased metabolism of Amiodarone caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [110]
Simeprevir DMLUA9D Moderate Decreased metabolism of Amiodarone caused by Simeprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [111]
Telaprevir DMMRV29 Major Decreased metabolism of Amiodarone caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [82]
Rifapentine DMCHV4I Major Increased metabolism of Amiodarone caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [105]
Brentuximab vedotin DMWLC57 Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Brentuximab vedotin. Hodgkin lymphoma [2B30] [112]
MK-1439 DM215WE Minor Decreased metabolism of Amiodarone caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [113]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Amiodarone caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [81]
Fostemsavir DM50ILT Major Increased risk of prolong QT interval by the combination of Amiodarone and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [81]
Cobicistat DM6L4H2 Major Decreased metabolism of Amiodarone caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [114]
Dolutegravir DMCZGRE Minor Decreased metabolism of Amiodarone caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [115]
Etravirine DMGV8QU Moderate Increased metabolism of Amiodarone caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [116]
Rilpivirine DMJ0QOW Major Increased risk of prolong QT interval by the combination of Amiodarone and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [81]
Darunavir DMN3GCH Moderate Decreased metabolism of Amiodarone caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [117]
Maraviroc DMTL94F Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Maraviroc. Human immunodeficiency virus disease [1C60-1C62] [118]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Amiodarone and Mipomersen. Hyper-lipoproteinaemia [5C80] [119]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Amiodarone and Teriflunomide. Hyper-lipoproteinaemia [5C80] [81]
BMS-201038 DMQTAGO Major Decreased metabolism of Amiodarone caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [120]
Acebutolol DM0TI4U Moderate Increased risk of bradycardia by the combination of Amiodarone and Acebutolol. Hypertension [BA00-BA04] [106]
Aliskiren DM1BV7W Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [81]
Penbutolol DM4ES8F Moderate Increased risk of atrioventricular block by the combination of Amiodarone and Penbutolol. Hypertension [BA00-BA04] [106]
Nebivolol DM7F1PA Moderate Increased risk of bradycardia by the combination of Amiodarone and Nebivolol. Hypertension [BA00-BA04] [106]
Tolvaptan DMIWFRL Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [121]
Pirfenidone DM6VZFQ Major Decreased metabolism of Amiodarone caused by Pirfenidone mediated inhibition of CYP450 enzyme. Idiopathic interstitial pneumonitis [CB03] [80]
Retapamulin DM9JXB7 Minor Decreased metabolism of Amiodarone caused by Retapamulin mediated inhibition of CYP450 enzyme. Impetigo [1B72] [122]
Lesinurad DMUR64T Moderate Decreased metabolism of Amiodarone caused by Lesinurad mediated inhibition of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [123]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Amiodarone caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [80]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Amiodarone caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [124]
ITI-007 DMUQ1DO Moderate Decreased metabolism of Amiodarone caused by ITI-007 mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [125]
Quazepam DMY4D87 Minor Additive CNS depression effects by the combination of Amiodarone and Quazepam. Insomnia [7A00-7A0Z] [126]
Estazolam DMZGXUM Minor Additive CNS depression effects by the combination of Amiodarone and Estazolam. Insomnia [7A00-7A0Z] [126]
Polyethylene glycol DM4I1JP Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Polyethylene glycol. Irritable bowel syndrome [DD91] [127]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Amiodarone and Phenolphthalein. Irritable bowel syndrome [DD91] [81]
Remimazolam DMLVSYX Minor Additive CNS depression effects by the combination of Amiodarone and Remimazolam. Labour/delivery anaesthesia complication [JB0C] [126]
Naloxegol DML0B41 Minor Decreased clearance of Amiodarone due to the transporter inhibition by Naloxegol. Large intestine motility disorder [DB32] [128]
Pemigatinib DM819JF Moderate Decreased metabolism of Amiodarone caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [82]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Amiodarone and Crizotinib. Lung cancer [2C25] [81]
Brigatinib DM7W94S Moderate Increased metabolism of Amiodarone caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [129]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Amiodarone and Ceritinib. Lung cancer [2C25] [81]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Amiodarone caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [130]
PF-06463922 DMKM7EW Moderate Decreased metabolism of Amiodarone caused by PF-06463922 mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [131]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Amiodarone and Osimertinib. Lung cancer [2C25] [81]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Amiodarone caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [132]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Amiodarone and Selpercatinib. Lung cancer [2C25] [81]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Amiodarone and Halofantrine. Malaria [1F40-1F45] [133]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Amiodarone and Hydroxychloroquine. Malaria [1F40-1F45] [81]
Inotuzumab ozogamicin DMAC130 Major Increased risk of prolong QT interval by the combination of Amiodarone and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [81]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Amiodarone and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [134]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Amiodarone and Idelalisib. Mature B-cell leukaemia [2A82] [135]
IPI-145 DMWA24P Moderate Decreased metabolism of Amiodarone caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [136]
Arsenic trioxide DM61TA4 Major Increased risk of prolong QT interval by the combination of Amiodarone and Arsenic trioxide. Mature B-cell lymphoma [2A85] [137]
Acalabrutinib DM7GCVW Moderate Decreased metabolism of Amiodarone caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [138]
Ibrutinib DMHZCPO Moderate Decreased metabolism of Amiodarone caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [139]
Ponatinib DMYGJQO Moderate Decreased metabolism of Amiodarone caused by Ponatinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [140]
Arry-162 DM1P6FR Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Arry-162. Melanoma [2C30] [80]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Amiodarone and Vemurafenib. Melanoma [2C30] [81]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Amiodarone caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [82]
Exjade DMHPRWG Moderate Decreased metabolism of Amiodarone caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [141]
Flibanserin DM70DTN Moderate Decreased metabolism of Amiodarone caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [142]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Amiodarone and Panobinostat. Multiple myeloma [2A83] [81]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Siponimod. Multiple sclerosis [8A40] [80]
Ozanimod DMT6AM2 Major Increased risk of prolong QT interval by the combination of Amiodarone and Ozanimod. Multiple sclerosis [8A40] [81]
Romidepsin DMT5GNL Major Increased risk of prolong QT interval by the combination of Amiodarone and Romidepsin. Mycosis fungoides [2B01] [81]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Amiodarone caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [82]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Amiodarone and Nilotinib. Myeloproliferative neoplasm [2A20] [81]
Ruxolitinib DM7Q98D Minor Decreased metabolism of Amiodarone caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [82]
Dasatinib DMJV2EK Major Increased risk of prolong QT interval by the combination of Amiodarone and Dasatinib. Myeloproliferative neoplasm [2A20] [81]
Entrectinib DMMPTLH Major Increased risk of prolong QT interval by the combination of Amiodarone and Entrectinib. Non-small cell lung cancer [2C25] [81]
Polythiazide DMCH80F Major Increased risk of ventricular arrhythmias by the combination of Amiodarone and Polythiazide. Oedema [MG29] [96]
Levomethadyl Acetate DM06HG5 Major Increased risk of prolong QT interval by the combination of Amiodarone and Levomethadyl Acetate. Opioid use disorder [6C43] [82]
Lofexidine DM1WXA6 Major Increased risk of prolong QT interval by the combination of Amiodarone and Lofexidine. Opioid use disorder [6C43] [81]
S-297995 DM26IH8 Moderate Decreased metabolism of Amiodarone caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [82]
Olaparib DM8QB1D Moderate Decreased metabolism of Amiodarone caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [143]
Rucaparib DM9PVX8 Major Increased risk of prolong QT interval by the combination of Amiodarone and Rucaparib. Ovarian cancer [2C73] [81]
MK-4827 DMLYGH4 Moderate Decreased clearance of Amiodarone due to the transporter inhibition by MK-4827. Ovarian cancer [2C73] [144]
Triclabendazole DMPWGBR Major Increased risk of prolong QT interval by the combination of Amiodarone and Triclabendazole. Parasitic worm infestation [1F90] [81]
Rasagiline DM3WKQ4 Major Decreased metabolism of Amiodarone caused by Rasagiline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [80]
Pimavanserin DMR7IVC Major Increased risk of prolong QT interval by the combination of Amiodarone and Pimavanserin. Parkinsonism [8A00] [81]
Abametapir DM2RX0I Moderate Decreased metabolism of Amiodarone caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [145]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Amiodarone and Macimorelin. Pituitary gland disorder [5A60-5A61] [146]
Lefamulin DME6G97 Major Decreased metabolism of Amiodarone caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [147]
Ergonovine DM0VEC1 Moderate Decreased metabolism of Amiodarone caused by Ergonovine mediated inhibition of CYP450 enzyme. Postpartum haemorrhage [JA43] [148]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Amiodarone caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [149]
Degarelix DM3O8QY Major Increased risk of prolong QT interval by the combination of Amiodarone and Degarelix. Prostate cancer [2C82] [81]
ABIRATERONE DM8V75C Major Increased risk of prolong QT interval by the combination of Amiodarone and ABIRATERONE. Prostate cancer [2C82] [81]
Enzalutamide DMGL19D Major Increased risk of prolong QT interval by the combination of Amiodarone and Enzalutamide. Prostate cancer [2C82] [81]
Darolutamide DMV7YFT Minor Decreased metabolism of Amiodarone caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [150]
Bicalutamide DMZMSPF Major Increased risk of prolong QT interval by the combination of Amiodarone and Bicalutamide. Prostate cancer [2C82] [81]
Silodosin DMJSBT6 Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Silodosin. Prostate hyperplasia [GA90] [151]
Dutasteride DMQ4TJK Moderate Decreased metabolism of Amiodarone caused by Dutasteride mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [152]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Amiodarone due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [82]
Ixekizumab DMXW92T Moderate Altered metabolism of Amiodarone due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [82]
Levomepromazine DMIKFEL Major Increased risk of prolong QT interval by the combination of Amiodarone and Levomepromazine. Psychotic disorder [6A20-6A25] [81]
Riociguat DMXBLMP Moderate Decreased metabolism of Amiodarone caused by Riociguat mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [80]
Everolimus DM8X2EH Moderate Decreased metabolism of Amiodarone caused by Everolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [153]
Axitinib DMGVH6N Moderate Decreased metabolism of Amiodarone caused by Axitinib mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [82]
Temsirolimus DMS104F Moderate Decreased metabolism of Amiodarone caused by Temsirolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [154]
Tocilizumab DM7J6OR Moderate Altered metabolism of Amiodarone due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [82]
Canakinumab DM8HLO5 Moderate Altered metabolism of Amiodarone due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [82]
Tofacitinib DMBS370 Moderate Decreased metabolism of Amiodarone caused by Tofacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [80]
Rilonacept DMGLUQS Moderate Altered metabolism of Amiodarone due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [82]
Golimumab DMHZV7X Moderate Altered metabolism of Amiodarone due to Golimumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [82]
Dexamethasone DMMWZET Major Increased metabolism of Amiodarone caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [105]
Sarilumab DMOGNXY Moderate Altered metabolism of Amiodarone due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [82]
Quetiapine DM1N62C Major Increased risk of prolong QT interval by the combination of Amiodarone and Quetiapine. Schizophrenia [6A20] [81]
Aripiprazole DM3NUMH Moderate Decreased metabolism of Amiodarone caused by Aripiprazole mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [80]
Paliperidone DM7NPJS Major Increased risk of prolong QT interval by the combination of Amiodarone and Paliperidone. Schizophrenia [6A20] [81]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Amiodarone and Amisulpride. Schizophrenia [6A20] [81]
Asenapine DMSQZE2 Major Increased risk of prolong QT interval by the combination of Amiodarone and Asenapine. Schizophrenia [6A20] [81]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Amiodarone caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [155]
LDE225 DMM9F25 Moderate Decreased metabolism of Amiodarone caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [156]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Amiodarone caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [82]
Larotrectinib DM26CQR Moderate Decreased metabolism of Amiodarone caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [80]
Docetaxel DMDI269 Major Decreased clearance of Amiodarone due to the transporter inhibition by Docetaxel. Solid tumour/cancer [2A00-2F9Z] [157]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Amiodarone and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [82]
Armodafinil DMGB035 Minor Decreased metabolism of Amiodarone caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [80]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Amiodarone and LEE011. Solid tumour/cancer [2A00-2F9Z] [81]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Amiodarone and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [158]
Triptorelin DMTK4LS Major Increased risk of prolong QT interval by the combination of Amiodarone and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [81]
Taxol DMUOT9V Moderate Decreased metabolism of Amiodarone caused by Taxol mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [159]
Pitolisant DM8RFNJ Major Increased risk of prolong QT interval by the combination of Amiodarone and Pitolisant. Somnolence [MG42] [81]
Telavancin DM58VQX Major Increased risk of prolong QT interval by the combination of Amiodarone and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [81]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Amiodarone due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [160]
Apixaban DM89JLN Moderate Decreased metabolism of Amiodarone caused by Apixaban mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [82]
Brilinta DMBR01X Moderate Decreased metabolism of Amiodarone caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [82]
Lenvatinib DMB1IU4 Major Increased risk of prolong QT interval by the combination of Amiodarone and Lenvatinib. Thyroid cancer [2D10] [81]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Amiodarone and Cabozantinib. Thyroid cancer [2D10] [81]
Saxagliptin DMGXENV Moderate Decreased metabolism of Amiodarone caused by Saxagliptin mediated inhibition of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [82]
Trimeprazine DMEMV9D Major Increased risk of prolong QT interval by the combination of Amiodarone and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [81]
⏷ Show the Full List of 212 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
Allura red AC dye E00338 33258 Colorant
Quinoline yellow WS E00309 24671 Colorant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 12 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Amiodarone 200 mg tablet 200 mg Oral Tablet Oral
Amiodarone 100 mg tablet 100 mg Oral Tablet Oral
Amiodarone 300 mg tablet 300 mg Oral Tablet Oral
Amiodarone 400 mg tablet 400 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: 2566).
2 New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
3 BDDCS applied to over 900 drugs
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 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
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
7 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
8 The metabolism of amiodarone by various CYP isoenzymes of human and rat, and the inhibitory influence of ketoconazole. J Pharm Pharm Sci. 2008;11(1):147-59.
9 Potentially significant drug interactions of class III antiarrhythmic drugs. Drug Saf. 2003;26(6):421-38.
10 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.
11 A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor. Drug Metab Dispos. 2000 Nov;28(11):1303-10.
12 Role of desethylamiodarone in the anticoagulant effect of concurrent amiodarone and warfarin therapy. J Cardiovasc Pharmacol Ther. 2001 Oct;6(4):363-7.
13 Functional characterization of five novel CYP2C8 variants, G171S, R186X, R186G, K247R, and K383N, found in a Japanese population. Drug Metab Dispos. 2005 May;33(5):630-6.
14 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.
15 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
16 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.
17 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
18 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.
19 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.
20 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
21 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.
22 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
23 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
24 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
25 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
26 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
27 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
28 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
29 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
30 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
31 Allelic variants of human cytochrome P450 1A1 (CYP1A1): effect of T461N and I462V substitutions on steroid hydroxylase specificity. Pharmacogenetics. 2000 Aug;10(6):519-30.
32 Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4'-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metab Dispos. 2002 Aug;30(8):869-74.
33 Cytochrome P450 isoforms catalyze formation of catechol estrogen quinones that react with DNA. Metabolism. 2007 Jul;56(7):887-94.
34 Preferred orientations in the binding of 4'-hydroxyacetanilide (acetaminophen) to cytochrome P450 1A1 and 2B1 isoforms as determined by 13C- and 15N-NMR relaxation studies. J Med Chem. 1994 Mar 18;37(6):860-7.
35 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
36 A common CYP1B1 polymorphism is associated with 2-OHE1/16-OHE1 urinary estrone ratio. Clin Chem Lab Med. 2005;43(7):702-6.
37 Cytochromes P450 in crustacea. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol. 1998 Nov;121(1-3):157-72.
38 Disruption of endogenous regulator homeostasis underlies the mechanism of rat CYP1A1 mRNA induction by metyrapone. Biochem J. 1998 Apr 1;331 ( Pt 1):273-81.
39 Pharmacogenomics in drug-metabolizing enzymes catalyzing anticancer drugs for personalized cancer chemotherapy. Curr Drug Metab. 2007 Aug;8(6):554-62.
40 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
41 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
42 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
43 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
44 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
45 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
46 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
47 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
48 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
49 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
50 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
51 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
52 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
53 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
54 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
55 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
56 Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
57 Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
58 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
59 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
60 New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126.
61 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
62 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
63 High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8.
64 Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91.
65 CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6.
66 Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21.
67 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
68 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
69 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
70 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
71 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
72 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
73 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
74 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
75 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
76 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
77 Azimilide. Drugs. 2000 Feb;59(2):271-7; discussion 278-9.
78 Buss J, Neuss H, Bilgin Y, Schlepper M "Malignant ventricular tachyarrhythmias in association with propafenone treatment." Eur Heart J 6 (1985): 424-8. [PMID: 4043097]
79 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
80 Cerner Multum, Inc. "Australian Product Information.".
81 Canadian Pharmacists Association.
82 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
83 Fabre G, Julian B, Saint-Aubert B, Joyeux H, Berger Y "Evidence for CYP3A-mediated N-deethylation of amiodarone in human liver microsomal fractions." Drug Metab Dispos 21 (1993): 978-85. [PMID: 7905403]
84 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
85 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
86 Bolland MJ, Bagg W, Thomas MG, Lucas JA, Ticehurst R, Black PN "Cushing's syndrome due to interaction between inhaled corticosteroids and itraconazole." Ann Pharmacother 38 (2004): 46-9. [PMID: 14742792]
87 Soto J, Sacristan JA, Arellano F, Hazas J "Possible theophylline-amiodarone interaction." DICP 24 (1990): 1115. [PMID: 2275239]
88 Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]
89 Bailey DG, Dresser GR, Kreeft JH, Munoz C, Freeman DJ, Bend JR "Grapefruit-felodipine interaction: Effect of unprocessed fruit and probable active ingredients." Clin Pharmacol Ther 68 (2000): 468-77. [PMID: 11103749]
90 Nattel S, Ranger S, Talajic M, et al "Erythromycin-induced long QT syndrome: concordance with quinidine and underlying cellular electrophysiologic mechanism." Am J Med 89 (1990): 235-8. [PMID: 2382671]
91 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
92 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
93 Product Information. Jevtana (cabazitaxel). sanofi-aventis , Bridgewater, NJ.
94 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
95 Goernig M, Kirmeier T, Krack A, Hartog CS, Figulla HR, Leder U "Iohexol contrast medium induces QT prolongation in amiodarone patients." Br J Clin Pharmacol 58 (2004): 96-98. [PMID: 15206999]
96 Antonelli D, Atar S, Freedberg NA, Rosenfeld T "Torsade de pointes in patients on chronic amiodarone treatment: contributing factors and drug interactions." Isr Med Assoc J 7 (2005): 163-5. [PMID: 15792261]
97 Caraco Y, Chajek-Shaul T "The incidence and clinical significance of amiodarone and acenocoumarol interaction." Thromb Haemost 62 (1989): 906-8. [PMID: 2595664]
98 Product Information. Ofev (nintedanib). Boehringer Ingelheim, Ridgefield, CT.
99 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
100 Product Information. Xarelto (rivaroxaban). Bayer Inc, Toronto, IA.
101 Product Information. Viibryd (vilazodone). Trovis Pharmaceuticals LLC, New Haven, CT.
102 Product Information. Serzone (nefazodone). Bristol-Myers Squibb, Princeton, NJ.
103 Product Information. Osphena (ospemifene). Shionogi USA Inc, Florham Park, NJ.
104 Product Information. Xcopri (cenobamate). SK Life Science, Inc., Paramus, NJ.
105 Product Information. Cordarone (amiodarone). Wyeth-Ayerst Laboratories, Philadelphia, PA.
106 Leor J, Levartowsky D, Sharon C, Farfel Z "Amiodarone and beta-adrenergic blockers: an interaction with metoprolol but not with atenolol." Am Heart J 16 (1988): 206-7. [PMID: 3394625]
107 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
108 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
109 Bajaj BP, Baig MW, Perrins EJ "Amiodarone-induced torsades de pointes: the possible facilitatory role of digoxin." Int J Cardiol 33 (1991): 335-7. [PMID: 1743800]
110 Product Information. Victrelis (boceprevir). Schering-Plough Corporation, Kenilworth, NJ.
111 Product Information. Olysio (simeprevir). Janssen Pharmaceuticals, Titusville, NJ.
112 Product Information. VFEND (voriconazole). Pfizer U.S. Pharmaceuticals, New York, NY.
113 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
114 Product Information. Stribild (cobicistat/elvitegravir/emtricitabine/tenofov). Gilead Sciences, Foster City, CA.
115 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
116 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
117 Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ.
118 Product Information. Selzentry (maraviroc). Pfizer U.S. Pharmaceuticals Group, New York, NY.
119 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
120 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
121 Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
122 Product Information. Altabax (retapamulin topical). GlaxoSmithKline, Research Triangle Park, NC.
123 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
124 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
125 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
126 Kerin NZ, Aragon E, Faitel K, Frumin H, Rubenfire M "Long-term efficacy and toxicity of high- and low-dose amiodarone regimens." J Clin Pharmacol 29 (1989): 418-23. [PMID: 2661600]
127 Hill AG, Parry BR "Hypokalaemia following bowel cleansing with sodium phosphate." N Z Med J 109 (1996): 347. [PMID: 8862361]
128 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
129 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
130 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
131 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
132 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
133 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]
134 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
135 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
136 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
137 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]
138 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
139 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
140 Product Information. Iclusig (ponatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
141 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
142 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
143 Product Information. Lynparza (olaparib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
144 Product Information. Zejula (niraparib). Tesaro Inc., Waltham, MA.
145 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
146 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
147 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
148 Francis H, Tyndall A, Webb J "Severe vascular spasm due to erythromycin-ergotamine interaction." Clin Rheumatol 3 (1984): 243-6. [PMID: 6236021]
149 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
150 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
151 Product Information. Rapaflo (silodosin). Watson Pharmaceuticals, Corona, CA.
152 Product Information. Duagen (dutasteride). GlaxoSmithKline Healthcare, Pittsburgh, PA.
153 Product Information. Afinitor (everolimus). Novartis Pharmaceuticals, East Hanover, NJ.
154 Product Information. Torisel (temsirolimus). Wyeth-Ayerst Laboratories, Philadelphia, PA.
155 Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.
156 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
157 Aronson JK, Grahame-Smith DG "Clinical pharmacology: adverse drug interactions." Br Med J 282 (1981): 288-91. [PMID: 6779990]
158 Product Information. Vandetanib (vandetanib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
159 Bergmann TK, Filppula AM, Launiainen T, Nielsen F, Backman J, Brosen K "Neurotoxicity and low paclitaxel clearance associated with concomitant clopidogrel therapy in a 60 year old Caucasian woman with ovarian carcinoma." Br J Clin Pharmacol (2015):. [PMID: 26446447]
160 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".