Details of the Drug

General Information of Drug (ID: DM2HN6Q)

Drug Name
Astemizole
Synonyms
Alermizol; Astemina; Astemisan; Astemisol; Astemison; Astemizol; Astemizolum; Astesen; Emdar; Esmacen; Fustermizol; Hestazol; Hismanal; Histamen; Histaminos; Histazol; Hubermizol; Kelp; Laridal; Metodih; Metodik; Paralergin; Retolen; Rifedot; Rimbol; Romadin; Simprox; Urdrim; Wareezol; Waruzol; AlacanBrand of Astemizole; Alonga Brand of Astemizole; Astemizol Alonga; Astemizol [German]; Astemizol ratiopharm; Astemizole Alacan Brand; Astemizole Alonga Brand; Astemizole Byk Brand; Astemizole Diba Brand; Astemizole Elfar Brand; Astemizole Esteve Brand; Astemizole Fustery Brand; Astemizole ICN Brand; Astemizole Janssen Brand; Astemizole Lesvi Brand; Astemizole McNeil Brand; Astemizole Medinsa Brand; Astemizole Merck Brand; Astemizole Senosiain Brand; Astemizole Septa Brand; Astemizole Smaller Brand; Astemizole Urbion Brand; Astemizole Vita Brand; Astemizole ratiopharm Brand; Byk Brand of Astemizole; Diba Brand of Astemizole; Elfar Brand of Astemizole; Esteve Brand of Astemizole; Fustery Brand of Astemizole; ICN Brand of Astemizole; Janssen Brand of Astemizole; Lesvi Brand of Astemizole; McNeil Brand of Astemizole; Medinsa Brand of Astemizole; Merck Brand of Astemizole; Ratiopharm Brand of Astemizole; Reig Jofre Brand of Astemizole; Senosiain Brand of Astemizole; Septa Brand of Astemizole; Smaller Brand of Astemizole; Urbion Brand of Astemizole; Vita Brand of Astemizole; R 42512; [3H]Astemizole; Alonga, Astemizol; Astemizol [INN-Spanish]; Astemizolum [INN-Latin]; HISMANAL (TN); Hismanal (TN); MJD-30; Nono-Nastizol A; Novo-mastizol A; Ratiopharm, Astemizol; Astemizole [USAN:BAN:INN]; GNF-PF-2461; Astemizole (JAN/USP/INN); Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Withdrawn from market [1]
Therapeutic Class
Antiallergic Agents
Affected Organisms
Humans and other mammals
ATC Code
R06AX11: Astemizole
R06AX: Other antihistamines for systemic use
R06A: ANTIHISTAMINES FOR SYSTEMIC USE
R06: ANTIHISTAMINES FOR SYSTEMIC USE
R: RESPIRATORY SYSTEM
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 458.6
Logarithm of the Partition Coefficient (xlogp) 6
Rotatable Bond Count (rotbonds) 8
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption
The drug is rapidly absorbed from the gastrointestinal tract []
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [2]
Elimination
0.5% of drug is excreted from urine in the unchanged form [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 1 days [3]
Metabolism
The drug is metabolized via the liver []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.36416 micromolar/kg/day [4]
Chemical Identifiers
Formula
C28H31FN4O
IUPAC Name
1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine
Canonical SMILES
COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
InChI
InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
InChIKey
GXDALQBWZGODGZ-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2247
ChEBI ID
CHEBI:2896
CAS Number
68844-77-9
UNII
7HU6337315
DrugBank ID
DB00637
TTD ID
D0Y2HR
VARIDT ID
DR00705
INTEDE ID
DR0147
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

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 [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [7]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [8]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [9]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [9]
Cytochrome P450 2J2 (CYP2J2) DERSX5P CP2J2_HUMAN Substrate [10]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [11]
Cyclic AMP-dependent transcription factor ATF-3 (ATF3) OTC1UOHP ATF3_HUMAN Gene/Protein Processing [12]
Cytochrome P450 2J2 (CYP2J2) OTJBTEH8 CP2J2_HUMAN Biotransformations [13]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Regulation of Drug Effects [14]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Gene/Protein Processing [12]
Metallothionein-1M (MT1M) OTVT8PLU MT1M_HUMAN Gene/Protein Processing [12]
Metallothionein-2 (MT2A) OTHOACHD MT2_HUMAN Gene/Protein Processing [12]
Microtubule-associated protein tau (MAPT) OTMTP2Z7 TAU_HUMAN Protein Interaction/Cellular Processes [15]
Potassium voltage-gated channel subfamily H member 1 (KCNH1) OTZZXWER KCNH1_HUMAN Gene/Protein Processing [16]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [17]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Allergic rhinitis
ICD Disease Classification CA08.0
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 2J2 (CYP2J2) DME CYP2J2 5.13E-02 2.48E-01 6.60E-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 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 Astemizole (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Astemizole and Ivosidenib. Acute myeloid leukaemia [2A60] [18]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Astemizole and Midostaurin. Acute myeloid leukaemia [2A60] [19]
Idarubicin DMM0XGL Moderate Increased risk of prolong QT interval by the combination of Astemizole and Idarubicin. Acute myeloid leukaemia [2A60] [19]
Daunorubicin DMQUSBT Moderate Increased risk of prolong QT interval by the combination of Astemizole and Daunorubicin. Acute myeloid leukaemia [2A60] [19]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Astemizole and Arn-509. Acute myeloid leukaemia [2A60] [20]
Gilteritinib DMTI0ZO Moderate Increased risk of prolong QT interval by the combination of Astemizole and Gilteritinib. Acute myeloid leukaemia [2A60] [21]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Astemizole and Oliceridine. Acute pain [MG31] [22]
Galantamine DMEO794 Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Galantamine. Alzheimer disease [8A20] [19]
Rivastigmine DMG629M Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Rivastigmine. Alzheimer disease [8A20] [19]
Donepezil DMIYG7Z Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Donepezil. Alzheimer disease [8A20] [19]
Metronidazole DMTIVEN Minor Increased risk of prolong QT interval by the combination of Astemizole and Metronidazole. Amoebiasis [1A36] [23]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Ivabradine. Angina pectoris [BA40] [20]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Astemizole and Dronedarone. Angina pectoris [BA40] [19]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Astemizole and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [24]
Cilostazol DMZMSCT Moderate Increased risk of prolong QT interval by the combination of Astemizole and Cilostazol. Arterial occlusive disease [BD40] [19]
Posaconazole DMUL5EW Major Decreased metabolism of Astemizole caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [25]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Levalbuterol. Asthma [CA23] [26]
Terbutaline DMD4381 Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Terbutaline. Asthma [CA23] [27]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Pirbuterol. Asthma [CA23] [26]
Salbutamol DMN9CWF Moderate Increased risk of prolong QT interval by the combination of Astemizole and Salbutamol. Asthma [CA23] [26]
Formoterol DMSOURV Moderate Increased risk of prolong QT interval by the combination of Astemizole and Formoterol. Asthma [CA23] [27]
Zileuton DMVRIC2 Moderate Decreased metabolism of Astemizole caused by Zileuton mediated inhibition of CYP450 enzyme. Asthma [CA23] [28]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [20]
Desipramine DMT2FDC Moderate Increased risk of prolong QT interval by the combination of Astemizole and Desipramine. Attention deficit hyperactivity disorder [6A05] [19]
Ofloxacin DM0VQN3 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Ofloxacin. Bacterial infection [1A00-1C4Z] [29]
Dalfopristin DM4LTKV Major Decreased metabolism of Astemizole caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [30]
Clarithromycin DM4M1SG Major Decreased metabolism of Astemizole caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [25]
Sulfamethoxazole DMB08GE Minor Increased risk of prolong QT interval by the combination of Astemizole and Sulfamethoxazole. Bacterial infection [1A00-1C4Z] [19]
Gemifloxacin DMHT34O Moderate Increased risk of prolong QT interval by the combination of Astemizole and Gemifloxacin. Bacterial infection [1A00-1C4Z] [29]
Norfloxacin DMIZ6W2 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Norfloxacin. Bacterial infection [1A00-1C4Z] [23]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Astemizole and Levofloxacin. Bacterial infection [1A00-1C4Z] [29]
Telithromycin DMZ4P3A Major Decreased metabolism of Astemizole caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [25]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Astemizole and Retigabine. Behcet disease [4A62] [22]
Erdafitinib DMI782S Moderate Increased metabolism of Astemizole caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [31]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Astemizole caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [32]
Loperamide DMOJZQ9 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Loperamide. Bowel habit change [ME05] [33]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Astemizole and Eribulin. Breast cancer [2C60-2C6Y] [19]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Astemizole and Lapatinib. Breast cancer [2C60-2C6Y] [19]
Tucatinib DMBESUA Moderate Decreased metabolism of Astemizole caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [34]
Palbociclib DMD7L94 Moderate Decreased metabolism of Astemizole caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [35]
Tamoxifen DMLB0EZ Moderate Increased risk of prolong QT interval by the combination of Astemizole and Tamoxifen. Breast cancer [2C60-2C6Y] [19]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Astemizole and Bosutinib. Breast cancer [2C60-2C6Y] [20]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Astemizole and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [36]
Olodaterol DM62B78 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Olodaterol. Chronic obstructive pulmonary disease [CA22] [27]
Vilanterol DMF5EK1 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Vilanterol. Chronic obstructive pulmonary disease [CA22] [26]
Salmeterol DMIEU69 Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Salmeterol. Chronic obstructive pulmonary disease [CA22] [27]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Indacaterol. Chronic obstructive pulmonary disease [CA22] [27]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Arformoterol. Chronic obstructive pulmonary disease [CA22] [27]
Fidaxomicin DMFP6MV Minor Decreased clearance of Astemizole due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [23]
Isoproterenol DMK7MEY Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Isoproterenol. Conduction disorder [BC63] [26]
Halothane DM80OZ5 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Halothane. Corneal disease [9A76-9A78] [19]
Propofol DMB4OLE Moderate Increased risk of prolong QT interval by the combination of Astemizole and Propofol. Corneal disease [9A76-9A78] [37]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Sevoflurane. Corneal disease [9A76-9A78] [19]
Clofazimine DMEBOFW Moderate Increased risk of prolong QT interval by the combination of Astemizole and Clofazimine. Crohn disease [DD70] [38]
Mifepristone DMGZQEF Major Decreased metabolism of Astemizole caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [39]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Astemizole and Pasireotide. Cushing syndrome [5A70] [19]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Astemizole and Osilodrostat. Cushing syndrome [5A70] [18]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Astemizole caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [40]
MK-8228 DMOB58Q Moderate Decreased metabolism of Astemizole caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [41]
Aprepitant DM053KT Major Decreased metabolism of Astemizole caused by Aprepitant mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [42]
Sertraline DM0FB1J Major Decreased metabolism of Astemizole caused by Sertraline mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [43]
Trimipramine DM1SC8M Moderate Increased risk of prolong QT interval by the combination of Astemizole and Trimipramine. Depression [6A70-6A7Z] [19]
Nefazodone DM4ZS8M Major Decreased metabolism of Astemizole caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [44]
Paroxetine DM5PVQE Major Decreased metabolism of Astemizole caused by Paroxetine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [43]
Escitalopram DMFK9HG Major Increased risk of prolong QT interval by the combination of Astemizole and Escitalopram. Depression [6A70-6A7Z] [19]
Clomipramine DMINRKW Moderate Increased risk of prolong QT interval by the combination of Astemizole and Clomipramine. Depression [6A70-6A7Z] [19]
Trazodone DMK1GBJ Moderate Increased risk of prolong QT interval by the combination of Astemizole and Trazodone. Depression [6A70-6A7Z] [45]
Doxepin DMPI98T Moderate Increased risk of prolong QT interval by the combination of Astemizole and Doxepin. Depression [6A70-6A7Z] [19]
Maprotiline DMPWB7T Moderate Increased risk of prolong QT interval by the combination of Astemizole and Maprotiline. Depression [6A70-6A7Z] [19]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Astemizole and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [19]
Deutetrabenazine DMUPFLI Moderate Additive CNS depression effects by the combination of Astemizole and Deutetrabenazine. Dystonic disorder [8A02] [46]
Ingrezza DMVPLNC Moderate Additive CNS depression effects by the combination of Astemizole and Ingrezza. Dystonic disorder [8A02] [47]
Cenobamate DM8KLU9 Moderate Increased metabolism of Astemizole caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [48]
Tazemetostat DMWP1BH Moderate Increased metabolism of Astemizole caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [49]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Astemizole and Solifenacin. Functional bladder disorder [GC50] [19]
Itraconazole DMCR1MV Major Decreased metabolism of Astemizole caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [25]
Pentamidine DMHZJCG Moderate Increased risk of prolong QT interval by the combination of Astemizole and Pentamidine. Fungal infection [1F29-1F2F] [19]
Miconazole DMPMYE8 Major Decreased metabolism of Astemizole caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [25]
Ketoconazole DMPZI3Q Major Decreased metabolism of Astemizole caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [25]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Astemizole and Sunitinib. Gastrointestinal stromal tumour [2B5B] [19]
Rifapentine DMCHV4I Moderate Increased metabolism of Astemizole caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [50]
Delavirdine DM3NF5G Major Decreased metabolism of Astemizole caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [30]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Astemizole caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [25]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Astemizole and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [51]
Saquinavir DMG814N Major Decreased metabolism of Astemizole caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [25]
Etravirine DMGV8QU Moderate Increased metabolism of Astemizole caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [52]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Astemizole and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [19]
Amprenavir DMLMXE0 Major Decreased metabolism of Astemizole caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Darunavir DMN3GCH Major Decreased metabolism of Astemizole caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [25]
Atazanavir DMSYRBX Major Decreased metabolism of Astemizole caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [25]
Conivaptan DM1V329 Major Decreased metabolism of Astemizole caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [25]
Polyethylene glycol DM4I1JP Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Polyethylene glycol. Irritable bowel syndrome [DD91] [54]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Astemizole and Crizotinib. Lung cancer [2C25] [55]
Brigatinib DM7W94S Moderate Increased metabolism of Astemizole caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [56]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Astemizole and Ceritinib. Lung cancer [2C25] [19]
PF-06463922 DMKM7EW Moderate Increased metabolism of Astemizole caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [57]
Osimertinib DMRJLAT Moderate Increased metabolism of Astemizole caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [20]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Astemizole and Selpercatinib. Lung cancer [2C25] [58]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Astemizole and Lumefantrine. Malaria [1F40-1F45] [23]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Astemizole and Hydroxychloroquine. Malaria [1F40-1F45] [59]
Primaquine DMWQ16I Moderate Increased risk of prolong QT interval by the combination of Astemizole and Primaquine. Malaria [1F40-1F45] [19]
Idelalisib DM602WT Moderate Decreased metabolism of Astemizole caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [60]
IPI-145 DMWA24P Moderate Decreased metabolism of Astemizole caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [61]
Arsenic trioxide DM61TA4 Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Arsenic trioxide. Mature B-cell lymphoma [2A85] [62]
Arry-162 DM1P6FR Moderate Decreased clearance of Astemizole due to the transporter inhibition by Arry-162. Melanoma [2C30] [23]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Astemizole and Vemurafenib. Melanoma [2C30] [19]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Astemizole and LGX818. Melanoma [2C30] [63]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Astemizole caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [20]
Exjade DMHPRWG Moderate Decreased metabolism of Astemizole caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [64]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Astemizole and Panobinostat. Multiple myeloma [2A83] [65]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Astemizole and Thalidomide. Multiple myeloma [2A83] [23]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Siponimod. Multiple sclerosis [8A40] [23]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Fingolimod. Multiple sclerosis [8A40] [19]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Ozanimod. Multiple sclerosis [8A40] [66]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Astemizole and Romidepsin. Mycosis fungoides [2B01] [22]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Astemizole caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [20]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Astemizole and Nilotinib. Myeloproliferative neoplasm [2A20] [19]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Astemizole and Dasatinib. Myeloproliferative neoplasm [2A20] [67]
Modafinil DMYILBE Minor Increased metabolism of Astemizole caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [68]
Promethazine DM6I5GR Moderate Increased risk of prolong QT interval by the combination of Astemizole and Promethazine. Nausea/vomiting [MD90] [19]
Granisetron DMIUW25 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Granisetron. Nausea/vomiting [MD90] [19]
Dolasetron DMMG26Z Major Increased risk of prolong QT interval by the combination of Astemizole and Dolasetron. Nausea/vomiting [MD90] [19]
Ondansetron DMOTQ1I Moderate Increased risk of prolong QT interval by the combination of Astemizole and Ondansetron. Nausea/vomiting [MD90] [19]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Astemizole and Entrectinib. Non-small cell lung cancer [2C25] [20]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Astemizole and Lofexidine. Opioid use disorder [6C43] [19]
Olaparib DM8QB1D Moderate Decreased metabolism of Astemizole caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [23]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Rucaparib. Ovarian cancer [2C73] [19]
Dextropropoxyphene DM23HCX Moderate Increased risk of prolong QT interval by the combination of Astemizole and Dextropropoxyphene. Pain [MG30-MG3Z] [22]
Buprenorphine DMPRI8G Moderate Increased risk of prolong QT interval by the combination of Astemizole and Buprenorphine. Pain [MG30-MG3Z] [19]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Astemizole and Triclabendazole. Parasitic worm infestation [1F90] [22]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Astemizole and Pimavanserin. Parkinsonism [8A00] [69]
Apomorphine DMX38HQ Moderate Increased risk of prolong QT interval by the combination of Astemizole and Apomorphine. Parkinsonism [8A00] [19]
Abametapir DM2RX0I Moderate Decreased metabolism of Astemizole caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [70]
Famotidine DMRL3AB Moderate Increased risk of prolong QT interval by the combination of Astemizole and Famotidine. Peptic ulcer [DA61] [23]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Astemizole and Macimorelin. Pituitary gland disorder [5A60-5A61] [71]
Lefamulin DME6G97 Major Decreased metabolism of Astemizole caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [72]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Astemizole caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [73]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Astemizole and Degarelix. Prostate cancer [2C82] [20]
ABIRATERONE DM8V75C Moderate Increased risk of prolong QT interval by the combination of Astemizole and ABIRATERONE. Prostate cancer [2C82] [20]
Nilutamide DMFN07X Moderate Increased risk of prolong QT interval by the combination of Astemizole and Nilutamide. Prostate cancer [2C82] [20]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Astemizole and Enzalutamide. Prostate cancer [2C82] [20]
Bicalutamide DMZMSPF Moderate Increased risk of prolong QT interval by the combination of Astemizole and Bicalutamide. Prostate cancer [2C82] [20]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Astemizole and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [74]
Gatifloxacin DMSL679 Major Increased risk of prolong QT interval by the combination of Astemizole and Gatifloxacin. Respiratory infection [CA07-CA4Z] [75]
Quetiapine DM1N62C Moderate Increased risk of prolong QT interval by the combination of Astemizole and Quetiapine. Schizophrenia [6A20] [19]
Mesoridazine DM2ZGAN Major Increased risk of prolong QT interval by the combination of Astemizole and Mesoridazine. Schizophrenia [6A20] [23]
Thioridazine DM35M8J Major Increased risk of prolong QT interval by the combination of Astemizole and Thioridazine. Schizophrenia [6A20] [20]
Aripiprazole DM3NUMH Moderate Increased risk of prolong QT interval by the combination of Astemizole and Aripiprazole. Schizophrenia [6A20] [23]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Astemizole and Iloperidone. Schizophrenia [6A20] [19]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Astemizole and Paliperidone. Schizophrenia [6A20] [19]
Perphenazine DMA4MRX Moderate Increased risk of prolong QT interval by the combination of Astemizole and Perphenazine. Schizophrenia [6A20] [19]
Trifluoperazine DMKBYWI Moderate Increased risk of prolong QT interval by the combination of Astemizole and Trifluoperazine. Schizophrenia [6A20] [19]
Risperidone DMN6DXL Moderate Increased risk of prolong QT interval by the combination of Astemizole and Risperidone. Schizophrenia [6A20] [19]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Astemizole and Amisulpride. Schizophrenia [6A20] [76]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Asenapine. Schizophrenia [6A20] [19]
Pimozide DMW83TP Major Increased risk of prolong QT interval by the combination of Astemizole and Pimozide. Schizophrenia [6A20] [20]
Vardenafil DMTBGW8 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Vardenafil. Sexual dysfunction [HA00-HA01] [19]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Astemizole caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [77]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Astemizole caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [20]
Larotrectinib DM26CQR Moderate Decreased metabolism of Astemizole caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [23]
Armodafinil DMGB035 Minor Increased metabolism of Astemizole caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [68]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Astemizole and LEE011. Solid tumour/cancer [2A00-2F9Z] [19]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Astemizole and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [19]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Astemizole and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [20]
Doxorubicin DMVP5YE Moderate Increased risk of prolong QT interval by the combination of Astemizole and Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [19]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Astemizole and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [19]
Adenosine DMM2NSK Major Increased risk of ventricular arrhythmias by the combination of Astemizole and Adenosine. Supraventricular tachyarrhythmia [BC81] [78]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Astemizole caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [79]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Astemizole due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [80]
Brilinta DMBR01X Moderate Decreased metabolism of Astemizole caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [20]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Lenvatinib. Thyroid cancer [2D10] [19]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Astemizole and Cabozantinib. Thyroid cancer [2D10] [20]
Papaverine DMCA9QP Major Increased risk of prolong QT interval by the combination of Astemizole and Papaverine. Tonus and reflex abnormality [MB47] [81]
Tizanidine DMR2IQ4 Moderate Increased risk of prolong QT interval by the combination of Astemizole and Tizanidine. Tonus and reflex abnormality [MB47] [19]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Astemizole and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [74]
Tacrolimus DMZ7XNQ Moderate Increased risk of prolong QT interval by the combination of Astemizole and Tacrolimus. Transplant rejection [NE84] [19]
Procainamide DMNMXR8 Major Increased risk of prolong QT interval by the combination of Astemizole and Procainamide. Ventricular tachyarrhythmia [BC71] [19]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Astemizole and Propafenone. Ventricular tachyarrhythmia [BC71] [19]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Astemizole and Flecainide. Ventricular tachyarrhythmia [BC71] [19]
Amiodarone DMUTEX3 Major Increased risk of prolong QT interval by the combination of Astemizole and Amiodarone. Ventricular tachyarrhythmia [BC71] [19]
⏷ Show the Full List of 180 DDI Information of This Drug

References

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