General Information of Drug (ID: DM4KLPT)

Drug Name
Terfenadine
Synonyms
Aldaban; Allerplus; Cyater; Hisfedin; Rapidal; Seldane; Teldane; Teldanex; Terdin; Terfedura; Terfemundin; Terfen; Terfenadina; Terfenadinum; Terfenidine; Terfex; Ternadin; Triludan; Aliud Brand of Terfenadine; Balkis Saft Spezial; Bial Brand of Terfenadine; Cantabria Brand of Terfenadine; Ct Arzneimittel Brand of Terfenadine; Dolorgiet Brand of Terfenadine; Heumann Brand of Terfenadine; Hoechst Brand of Terfenadine; Merck dura Brand of Terfenadine; Mundipharma Brand of Terfenadine; Ratiopharm Brand of Terfenadine; Sigma Tau Brand of Terfenadine; Stadapharm Brand of Terfenadine; Terfenadin AL; Terfenadin Heumann; Terfenadin Stada; Terfenadin von ct; Wolff Brand of Terfenadine; MDL 9918; RMI 9918; RMI9918; T 9652; Ct-Arzneimittel Brand of Terfenadine; MDL-9918; RMI-9918; Seldane (TN); Sigma-Tau Brand of Terfenadine; Teldane (TN); Terfenadin-ratiopharm; Terfenadina [INN-Spanish]; Terfenadinum [INN-Latin]; Triludan (TN); Terfenadine (JAN/USAN/INN); Terfenadine [USAN:BAN:INN:JAN]; Alpha-(4-[1,1-Dimethylethyl]phenyl)-4-[hydroxydiphenylmethyl]-1-piperidinebutanol; Alpha-(p-tert-Butylphenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Alpha-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperdinebutanol; Alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Alpha-(4-(1,1-dimethylethyl)phenyl)-4-(hydroxydiphenyl-methyl)-1-piperidine butanol; 1-(4-tert-Butylphenyl)-4-(4-(alpha-hydroxybenzhydryl)piperidino)-butan-1-ol; 1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butan-1-ol; 1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol; 1-(p-tert-Butylphenyl)-4-(4'-(alpha-hydroxydiphenylmethyl)-1'-piperidyl)butanol; 1-[4-(1,1-dimethylethyl)phenyl]-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}butan-1-ol
Indication
Disease Entry ICD 11 Status REF
Allergy 4A80-4A85 Withdrawn from market [1], [2]
Therapeutic Class
Antihistamines
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 471.7
Topological Polar Surface Area (xlogp) 6.6
Rotatable Bond Count (rotbonds) 9
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
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 3.5 hours [4]
Metabolism
The drug is metabolized via the hepatic [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 4.24008 micromolar/kg/day [6]
Water Solubility
The ability of drug to dissolve in water is measured as 0.006 mg/mL [3]
Chemical Identifiers
Formula
C32H41NO2
IUPAC Name
1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol
Canonical SMILES
CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O
InChI
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
InChIKey
GUGOEEXESWIERI-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
5405
ChEBI ID
CHEBI:9453
CAS Number
50679-08-8
DrugBank ID
DB00342
TTD ID
D08SOF
VARIDT ID
DR00755
INTEDE ID
DR1558

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [7], [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [10]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [11]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [12]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [13]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [13]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Allergy
ICD Disease Classification 4A80-4A85
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.74E-01 0.13 0.43
P-glycoprotein 1 (ABCB1) DTP P-GP 6.54E-01 1.95E-01 4.04E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.57E-01 9.43E-03 1.29E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.70E-01 2.98E-02 1.22E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.35E-01 2.78E-02 2.09E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.76E-01 1.26E-01 8.27E-01
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 Terfenadine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Terfenadine and Ivosidenib. Acute myeloid leukaemia [2A60] [65]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Midostaurin. Acute myeloid leukaemia [2A60] [66]
Daunorubicin DMQUSBT Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Daunorubicin. Acute myeloid leukaemia [2A60] [66]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Arn-509. Acute myeloid leukaemia [2A60] [67]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Oliceridine. Acute pain [MG31] [68]
Galantamine DMEO794 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Galantamine. Alzheimer disease [8A20] [66]
Rivastigmine DMG629M Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Rivastigmine. Alzheimer disease [8A20] [66]
Donepezil DMIYG7Z Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Donepezil. Alzheimer disease [8A20] [66]
Metronidazole DMTIVEN Minor Increased risk of prolong QT interval by the combination of Terfenadine and Metronidazole. Amoebiasis [1A36] [69]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Terfenadine and Ivabradine. Angina pectoris [BA40] [67]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Terfenadine and Dronedarone. Angina pectoris [BA40] [66]
Hydroxyzine DMF8Y74 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Hydroxyzine. Anxiety disorder [6B00-6B0Z] [66]
Cilostazol DMZMSCT Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Cilostazol. Arterial occlusive disease [BD40] [66]
Voriconazole DMAOL2S Major Decreased metabolism of Terfenadine caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [70]
Posaconazole DMUL5EW Major Decreased metabolism of Terfenadine caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [70]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Levalbuterol. Asthma [CA23] [71]
Terbutaline DMD4381 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Terbutaline. Asthma [CA23] [72]
Pirbuterol DMI5678 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Pirbuterol. Asthma [CA23] [71]
Salbutamol DMN9CWF Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Salbutamol. Asthma [CA23] [71]
Formoterol DMSOURV Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Formoterol. Asthma [CA23] [72]
Zileuton DMVRIC2 Major Decreased renal excretion of Terfenadine caused by Zileuton. Asthma [CA23] [73]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [67]
Desipramine DMT2FDC Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Desipramine. Attention deficit hyperactivity disorder [6A05] [66]
Ofloxacin DM0VQN3 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Ofloxacin. Bacterial infection [1A00-1C4Z] [74]
Ciprofloxacin XR DM2NLS9 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Ciprofloxacin XR. Bacterial infection [1A00-1C4Z] [66]
Dalfopristin DM4LTKV Major Decreased metabolism of Terfenadine caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [75]
Clarithromycin DM4M1SG Major Decreased metabolism of Terfenadine caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [70]
Sulfamethoxazole DMB08GE Minor Increased risk of prolong QT interval by the combination of Terfenadine and Sulfamethoxazole. Bacterial infection [1A00-1C4Z] [66]
Gemifloxacin DMHT34O Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Gemifloxacin. Bacterial infection [1A00-1C4Z] [74]
Norfloxacin DMIZ6W2 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Norfloxacin. Bacterial infection [1A00-1C4Z] [69]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Levofloxacin. Bacterial infection [1A00-1C4Z] [74]
Telithromycin DMZ4P3A Major Decreased metabolism of Terfenadine caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [70]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Retigabine. Behcet disease [4A62] [68]
Erdafitinib DMI782S Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [76]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Terfenadine caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [77]
Loperamide DMOJZQ9 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Loperamide. Bowel habit change [ME05] [78]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Eribulin. Breast cancer [2C60-2C6Y] [66]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Lapatinib. Breast cancer [2C60-2C6Y] [66]
Tucatinib DMBESUA Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Tucatinib. Breast cancer [2C60-2C6Y] [79]
Palbociclib DMD7L94 Moderate Decreased metabolism of Terfenadine caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [80]
Tamoxifen DMLB0EZ Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Tamoxifen. Breast cancer [2C60-2C6Y] [66]
Toremifene DMQYUWG Major Increased risk of prolong QT interval by the combination of Terfenadine and Toremifene. Breast cancer [2C60-2C6Y] [66]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Bosutinib. Breast cancer [2C60-2C6Y] [67]
Sotalol DML60TN Major Increased risk of prolong QT interval by the combination of Terfenadine and Sotalol. Cardiac arrhythmia [BC9Z] [81]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Olodaterol. Chronic obstructive pulmonary disease [CA22] [72]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Vilanterol. Chronic obstructive pulmonary disease [CA22] [71]
Salmeterol DMIEU69 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Salmeterol. Chronic obstructive pulmonary disease [CA22] [72]
Indacaterol DMQJHR7 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Indacaterol. Chronic obstructive pulmonary disease [CA22] [72]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Arformoterol. Chronic obstructive pulmonary disease [CA22] [72]
Oxaliplatin DMQNWRD Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Oxaliplatin. Colorectal cancer [2B91] [66]
Isoproterenol DMK7MEY Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Isoproterenol. Conduction disorder [BC63] [71]
Halothane DM80OZ5 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Halothane. Corneal disease [9A76-9A78] [66]
Propofol DMB4OLE Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Propofol. Corneal disease [9A76-9A78] [82]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Sevoflurane. Corneal disease [9A76-9A78] [66]
Clofazimine DMEBOFW Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Clofazimine. Crohn disease [DD70] [83]
Mifepristone DMGZQEF Major Decreased metabolism of Terfenadine caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [84]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Terfenadine and Pasireotide. Cushing syndrome [5A70] [66]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Osilodrostat. Cushing syndrome [5A70] [65]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Terfenadine caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [85]
MK-8228 DMOB58Q Moderate Decreased metabolism of Terfenadine caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [86]
Aprepitant DM053KT Major Decreased metabolism of Terfenadine caused by Aprepitant mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [87]
Sertraline DM0FB1J Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Sertraline. Depression [6A70-6A7Z] [66]
Trimipramine DM1SC8M Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Trimipramine. Depression [6A70-6A7Z] [66]
Imipramine DM2NUH3 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Imipramine. Depression [6A70-6A7Z] [66]
Fluoxetine DM3PD2C Major Decreased metabolism of Terfenadine caused by Fluoxetine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [88]
Nefazodone DM4ZS8M Major Decreased metabolism of Terfenadine caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [89]
Escitalopram DMFK9HG Major Increased risk of prolong QT interval by the combination of Terfenadine and Escitalopram. Depression [6A70-6A7Z] [66]
Clomipramine DMINRKW Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Clomipramine. Depression [6A70-6A7Z] [66]
Trazodone DMK1GBJ Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Trazodone. Depression [6A70-6A7Z] [90]
Amoxapine DMKITQE Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Amoxapine. Depression [6A70-6A7Z] [66]
Mirtazapine DML53ZJ Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Mirtazapine. Depression [6A70-6A7Z] [91]
Protriptyline DMNHTZI Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Protriptyline. Depression [6A70-6A7Z] [66]
Doxepin DMPI98T Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Doxepin. Depression [6A70-6A7Z] [66]
Maprotiline DMPWB7T Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Maprotiline. Depression [6A70-6A7Z] [66]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [66]
Deutetrabenazine DMUPFLI Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Deutetrabenazine. Dystonic disorder [8A02] [92]
Ingrezza DMVPLNC Moderate Additive CNS depression effects by the combination of Terfenadine and Ingrezza. Dystonic disorder [8A02] [93]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Terfenadine caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [94]
Cenobamate DMGOVHA Moderate Increased metabolism of Terfenadine caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [95]
Stiripentol DMMSDOY Moderate Decreased metabolism of Terfenadine caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [96]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Solifenacin. Functional bladder disorder [GC50] [66]
Itraconazole DMCR1MV Major Decreased metabolism of Terfenadine caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [70]
Pentamidine DMHZJCG Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Pentamidine. Fungal infection [1F29-1F2F] [66]
Terbinafine DMI6HUW Minor Decreased metabolism of Terfenadine caused by Terbinafine mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [97]
Miconazole DMPMYE8 Major Decreased metabolism of Terfenadine caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [70]
Cimetidine DMH61ZB Major Decreased metabolism of Terfenadine caused by Cimetidine mediated inhibition of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [98]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Sunitinib. Gastrointestinal stromal tumour [2B5B] [66]
GS-5885 DMSL3DX Moderate Decreased clearance of Terfenadine due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [99]
Rifapentine DMCHV4I Moderate Increased metabolism of Terfenadine caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [100]
Delavirdine DM3NF5G Major Decreased metabolism of Terfenadine caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [75]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Terfenadine caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [70]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [101]
Efavirenz DMC0GSJ Major Decreased metabolism of Terfenadine caused by Efavirenz mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [102]
Saquinavir DMG814N Major Decreased metabolism of Terfenadine caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [70]
Etravirine DMGV8QU Moderate Increased metabolism of Terfenadine caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [103]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [66]
Amprenavir DMLMXE0 Major Decreased metabolism of Terfenadine caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [104]
Darunavir DMN3GCH Major Decreased metabolism of Terfenadine caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [70]
Atazanavir DMSYRBX Major Decreased metabolism of Terfenadine caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [70]
Ritonavir DMU764S Major Decreased metabolism of Terfenadine caused by Ritonavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [70]
BMS-201038 DMQTAGO Moderate Decreased clearance of Terfenadine due to the transporter inhibition by BMS-201038. Hyper-lipoproteinaemia [5C80] [105]
Diltiazem DMAI7ZV Moderate Decreased metabolism of Terfenadine caused by Diltiazem mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [106]
Conivaptan DM1V329 Major Decreased metabolism of Terfenadine caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [70]
Tolvaptan DMIWFRL Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [69]
Polyethylene glycol DM4I1JP Major Increased risk of ventricular arrhythmias by the combination of Terfenadine and Polyethylene glycol. Irritable bowel syndrome [DD91] [107]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Terfenadine and Crizotinib. Lung cancer [2C25] [108]
Brigatinib DM7W94S Moderate Increased metabolism of Terfenadine caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [109]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Terfenadine and Ceritinib. Lung cancer [2C25] [66]
PF-06463922 DMKM7EW Moderate Increased metabolism of Terfenadine caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [110]
Osimertinib DMRJLAT Moderate Decreased metabolism of Terfenadine caused by Osimertinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [67]
Capmatinib DMYCXKL Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [111]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Terfenadine and Selpercatinib. Lung cancer [2C25] [112]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Terfenadine and Lumefantrine. Malaria [1F40-1F45] [69]
Chloroquine DMSI5CB Major Increased risk of prolong QT interval by the combination of Terfenadine and Chloroquine. Malaria [1F40-1F45] [113]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Terfenadine and Hydroxychloroquine. Malaria [1F40-1F45] [113]
Quinine DMSWYF5 Major Decreased metabolism of Terfenadine caused by Quinine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [114]
Primaquine DMWQ16I Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Primaquine. Malaria [1F40-1F45] [66]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [67]
Idelalisib DM602WT Moderate Decreased metabolism of Terfenadine caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [115]
IPI-145 DMWA24P Moderate Decreased metabolism of Terfenadine caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [116]
Arsenic trioxide DM61TA4 Major Increased risk of prolong QT interval by the combination of Terfenadine and Arsenic trioxide. Mature B-cell lymphoma [2A85] [117]
Ibrutinib DMHZCPO Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Ibrutinib. Mature B-cell lymphoma [2A85] [67]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Terfenadine and Vemurafenib. Melanoma [2C30] [66]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and LGX818. Melanoma [2C30] [118]
Lasmiditan DMXLVDT Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Lasmiditan. Migraine [8A80] [119]
Exjade DMHPRWG Moderate Decreased metabolism of Terfenadine caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [120]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Terfenadine and Panobinostat. Multiple myeloma [2A83] [121]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Terfenadine and Thalidomide. Multiple myeloma [2A83] [69]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Terfenadine and Siponimod. Multiple sclerosis [8A40] [69]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Terfenadine and Ozanimod. Multiple sclerosis [8A40] [122]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Romidepsin. Mycosis fungoides [2B01] [68]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Terfenadine caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [67]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Terfenadine and Nilotinib. Myeloproliferative neoplasm [2A20] [66]
Imatinib DM7RJXL Moderate Decreased metabolism of Terfenadine caused by Imatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [123]
Modafinil DMYILBE Moderate Increased metabolism of Terfenadine caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [69]
Droperidol DM0DXA8 Major Increased risk of prolong QT interval by the combination of Terfenadine and Droperidol. Nausea/vomiting [MD90] [66]
Prochlorperazine DM53SRA Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Prochlorperazine. Nausea/vomiting [MD90] [66]
Promethazine DM6I5GR Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Promethazine. Nausea/vomiting [MD90] [66]
Granisetron DMIUW25 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Granisetron. Nausea/vomiting [MD90] [66]
Dolasetron DMMG26Z Major Increased risk of prolong QT interval by the combination of Terfenadine and Dolasetron. Nausea/vomiting [MD90] [66]
Ondansetron DMOTQ1I Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Ondansetron. Nausea/vomiting [MD90] [66]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Entrectinib. Non-small cell lung cancer [2C25] [67]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Terfenadine and Lofexidine. Opioid use disorder [6C43] [66]
Olaparib DM8QB1D Moderate Decreased metabolism of Terfenadine caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [69]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Rucaparib. Ovarian cancer [2C73] [66]
Dextropropoxyphene DM23HCX Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Dextropropoxyphene. Pain [MG30-MG3Z] [68]
Buprenorphine DMPRI8G Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Buprenorphine. Pain [MG30-MG3Z] [66]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Triclabendazole. Parasitic worm infestation [1F90] [68]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Pimavanserin. Parkinsonism [8A00] [124]
Abametapir DM2RX0I Moderate Decreased metabolism of Terfenadine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [125]
Famotidine DMRL3AB Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Famotidine. Peptic ulcer [DA61] [69]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Terfenadine and Macimorelin. Pituitary gland disorder [5A60-5A61] [126]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Terfenadine and Lefamulin. Pneumonia [CA40] [127]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Terfenadine caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [128]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Degarelix. Prostate cancer [2C82] [67]
ABIRATERONE DM8V75C Moderate Increased risk of prolong QT interval by the combination of Terfenadine and ABIRATERONE. Prostate cancer [2C82] [67]
Nilutamide DMFN07X Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Nilutamide. Prostate cancer [2C82] [67]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Enzalutamide. Prostate cancer [2C82] [67]
Flutamide DMK0O7U Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Flutamide. Prostate cancer [2C82] [67]
Bicalutamide DMZMSPF Major Decreased metabolism of Terfenadine caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [129]
Alfuzosin DMZVMKF Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Alfuzosin. Prostate hyperplasia [GA90] [66]
Fluphenazine DMIT8LX Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Fluphenazine. Psychotic disorder [6A20-6A25] [66]
Bosentan DMIOGBU Moderate Increased metabolism of Terfenadine caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [130]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Terfenadine and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [131]
Sorafenib DMS8IFC Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Sorafenib. Renal cell carcinoma [2C90] [66]
Gatifloxacin DMSL679 Major Increased risk of prolong QT interval by the combination of Terfenadine and Gatifloxacin. Respiratory infection [CA07-CA4Z] [132]
Quetiapine DM1N62C Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Quetiapine. Schizophrenia [6A20] [66]
Mesoridazine DM2ZGAN Major Increased risk of prolong QT interval by the combination of Terfenadine and Mesoridazine. Schizophrenia [6A20] [69]
Thioridazine DM35M8J Major Increased risk of prolong QT interval by the combination of Terfenadine and Thioridazine. Schizophrenia [6A20] [67]
Aripiprazole DM3NUMH Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Aripiprazole. Schizophrenia [6A20] [69]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Paliperidone. Schizophrenia [6A20] [66]
Haloperidol DM96SE0 Major Increased risk of prolong QT interval by the combination of Terfenadine and Haloperidol. Schizophrenia [6A20] [66]
Perphenazine DMA4MRX Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Perphenazine. Schizophrenia [6A20] [66]
Chlorpromazine DMBGZI3 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Chlorpromazine. Schizophrenia [6A20] [66]
Clozapine DMFC71L Major Increased risk of prolong QT interval by the combination of Terfenadine and Clozapine. Schizophrenia [6A20] [66]
Trifluoperazine DMKBYWI Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Trifluoperazine. Schizophrenia [6A20] [66]
Risperidone DMN6DXL Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Risperidone. Schizophrenia [6A20] [66]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Terfenadine and Amisulpride. Schizophrenia [6A20] [133]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Asenapine. Schizophrenia [6A20] [66]
Vardenafil DMTBGW8 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Vardenafil. Sexual dysfunction [HA00-HA01] [66]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Terfenadine caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [67]
Larotrectinib DM26CQR Moderate Decreased metabolism of Terfenadine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [69]
Armodafinil DMGB035 Moderate Increased metabolism of Terfenadine caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [69]
LEE011 DMMX75K Major Decreased metabolism of Terfenadine caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [66]
Epirubicin DMPDW6T Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Epirubicin. Solid tumour/cancer [2A00-2F9Z] [66]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Terfenadine and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [66]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [67]
Doxorubicin DMVP5YE Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [66]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Pitolisant. Somnolence [MG42] [66]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [66]
Adenosine DMM2NSK Major Increased risk of ventricular arrhythmias by the combination of Terfenadine and Adenosine. Supraventricular tachyarrhythmia [BC81] [134]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Terfenadine caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [135]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Terfenadine due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [136]
Brilinta DMBR01X Moderate Decreased metabolism of Terfenadine caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [67]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Lenvatinib. Thyroid cancer [2D10] [66]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Terfenadine and Cabozantinib. Thyroid cancer [2D10] [67]
Papaverine DMCA9QP Major Increased risk of prolong QT interval by the combination of Terfenadine and Papaverine. Tonus and reflex abnormality [MB47] [137]
Tizanidine DMR2IQ4 Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Tizanidine. Tonus and reflex abnormality [MB47] [66]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Terfenadine and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [131]
Tacrolimus DMZ7XNQ Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Tacrolimus. Transplant rejection [NE84] [66]
Procainamide DMNMXR8 Major Increased risk of prolong QT interval by the combination of Terfenadine and Procainamide. Ventricular tachyarrhythmia [BC71] [66]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Propafenone. Ventricular tachyarrhythmia [BC71] [66]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Terfenadine and Flecainide. Ventricular tachyarrhythmia [BC71] [66]
Amiodarone DMUTEX3 Major Increased risk of prolong QT interval by the combination of Terfenadine and Amiodarone. Ventricular tachyarrhythmia [BC71] [66]
⏷ Show the Full List of 204 DDI Information 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: 2608).
2 Comparative tolerability of second generation antihistamines. Drug Saf. 1999 May;20(5):385-401.
3 BDDCS applied to over 900 drugs
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 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.
6 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
7 Small mouse cholangiocytes proliferate in response to H1 histamine receptor stimulation by activation of the IP3/CaMK I/CREB pathway. Am J Physiol Cell Physiol. 2008 Aug;295(2):C499-513.
8 Second-generation antihistamines: a comparative review. Drugs. 1999 Jan;57(1):31-47.
9 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.
10 Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs. Clin Pharmacokinet. 2005;44(3):279-304.
11 Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92.
12 Effects of serum albumin and liver cytosol on CYP2C9- and CYP3A4-mediated drug metabolism. Drug Metab Pharmacokinet. 2002;17(6):522-31.
13 Drug Interactions Flockhart Table
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 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.
23 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
24 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.
25 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
26 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.
27 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
28 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
29 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
30 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
31 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.
32 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.
33 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.
34 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.
35 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
36 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
37 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
38 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
39 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
40 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
41 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
42 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
43 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.
44 Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
45 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.
46 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
47 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
48 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.
49 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
50 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
51 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
52 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
53 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
54 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
55 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
56 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.
57 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
58 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
59 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
60 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
61 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
62 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
63 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
64 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
65 Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
66 Canadian Pharmacists Association.
67 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
68 Iannini PB "Cardiotoxicity of macrolides, ketolides and fluoroquinolones that prolong the QTc interval." Expert Opin Drug Saf 1 (2002): 121-8. [PMID: 12904146]
69 Cerner Multum, Inc. "Australian Product Information.".
70 Ament PW, Paterson A "Drug interactions with the nonsedating antihistamines." Am Fam Physician 56 (1997): 223. [PMID: 9225677]
71 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
72 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
73 Awni WM, Cavanaugh JH, Leese P, Kasier J, Cao GL, Locke CS, Dube LM "The pharmacokinetic and pharmacodynamic interaction between zileuton and terfenadine." Eur J Clin Pharmacol 52 (1997): 49-54. [PMID: 9143867]
74 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
75 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]
76 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
77 Product Information. Sonata (zaleplon) Wyeth-Ayerst Laboratories, Philadelphia, PA.
78 Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747]
79 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
80 Product Information. Ibrance (palbociclib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
81 Feroze H, Suri R, Silverman DI "Torsades de pointes from terfenadine and sotalol given in combination." Pacing Clin Electrophysiol 19 (1996): 1519-21. [PMID: 8904547]
82 Hanci V, Aydin M, Yurtlu BS, et.al "Anesthesia induction with sevoflurane and propofol: evaluation of P-wave dispersion, QT and corrected QT intervals." Kaohsiung J Med Sci 26 (2010): 470-7. [PMID: 20837343]
83 Product Information. Lamprene (clofazimine). Novartis Pharmaceuticals, East Hanover, NJ.
84 He K, Woolf TF, Hollenberg PF "Mechanism-based inactivation of cytochrome P-450-3A4 by mifepristone (RU486)." J Pharmacol Exp Ther 288 (1999): 791-7. [PMID: 9918590]
85 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
86 Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
87 Product Information. Emend (aprepitant). Merck & Company Inc, West Point, PA.
88 Marchiando RJ, Cook MD "Probable terfenadine-fluoxetine-associated cardiac toxicity." Ann Pharmacother 29 (1995): 937-8. [PMID: 8547749]
89 Product Information. Serzone (nefazodone). Bristol-Myers Squibb, Princeton, NJ.
90 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]
91 Product Information. Remeron (mirtazapine). Organon, West Orange, NJ.
92 Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
93 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
94 Product Information. Trileptal (oxcarbazepine) Novartis Pharmaceuticals, East Hanover, NJ.
95 Product Information. Xcopri (cenobamate). SK Life Science, Inc., Paramus, NJ.
96 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
97 Long CC, Hill SA, Thomas RC, Johnston A, Smith SG, Kendall F, Finlay AY "Effect of terbinafine on the pharmacokinetics of cyclosporin in humans." J Invest Dermatol 102 (1994): 740-3. [PMID: 8176256]
98 Hey JA, Delprado M, Egan RW, Kreutner W "Terfenadine, astemizole, and ebastine produce QTc interval prolongation in an experimental model predictive of adverse clinical ECG effects." Ann Allergy Asthma Immunol 76 (1996): 476. [PMID: 8630724]
99 Product Information. Harvoni (ledipasvir-sofosbuvir). Gilead Sciences, Foster City, CA.
100 Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO.
101 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
102 Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE.
103 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
104 Gonzalez MA, Estes KS "Pharmacokinetic overview of oral second-generation H-1 antihistamines." Int J Clin Pharmacol Ther 36 (1998): 292-300. [PMID: 9629995]
105 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
106 Abernethy DR, Egan JM, Dickinson TH, Carrum G "Substrate-selective inhibition by verapamil and diltiazem: differential disposition of antipyrine and theophylline in humans." J Pharmacol Exp Ther 244 (1988): 994-9. [PMID: 3252045]
107 Hill AG, Parry BR "Hypokalaemia following bowel cleansing with sodium phosphate." N Z Med J 109 (1996): 347. [PMID: 8862361]
108 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
109 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
110 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
111 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
112 Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN.
113 Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
114 Martin ES, Rogalski K, Black JN "Quinine may trigger torsades de pointes during astemizole therapy." Pacing Clin Electrophysiol 20 (1997): 2024-5. [PMID: 9272545]
115 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
116 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
117 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]
118 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
119 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
120 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
121 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
122 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
123 Product Information. Gleevec (imatinib mesylate). Novartis Pharmaceuticals, East Hanover, NJ.
124 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
125 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
126 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
127 Product Information. Fareston (toremifene). Schering Laboratories, Kenilworth, NJ.
128 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
129 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
130 Product Information. Tracleer (bosentan). Acetelion Pharmaceuticals US, Inc, South San Francisco, CA.
131 Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
132 Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]
133 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
134 Celiker A, Tokel K, Cil E, Ozkutlu S, Ozme S "Adenosine induced torsades de pointes in a child with congenital long QT syndrome." Pacing Clin Electrophysiol 17 (1994): 1814-7. [PMID: 7838793]
135 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
136 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
137 Goto M, Sato M, Kitzazawa H, et.al "Papaverine-induced QT interval prolongation and ventricular fibrillation in a patient with a history of drug-induced QT prolongation." Intern Med 53 (2014): 1629-31. [PMID: 25088875]