Details of the Drug

General Information of Drug (ID: DM51FY6)

Drug Name
Tacrine
Synonyms
Cognex; Romotal; Tacrina; Tacrinal; Tacrinum; Tenakrin; Tetrahydroaminacrine; Tetrahydroaminoacridine; Tetrahydroaminocrin; Tetrahydroaminocrine; Tha; Tacrine hydrochloride; BBL001044; CS 12602; Cognex (TN); Tacrina [INN-Spanish]; Tacrinal (TN); Tacrine (INN); Tacrine [INN:BAN]; Tacrinum [INN-Latin]; 1,2,3,4-TETRAHYDRO-9-ACRIDINAMINE; 1,2,3,4-TETRAHYDRO-9-ACRIDINAMINE (SEE ALSO 1684-40-8); 1,2,3,4-Tetrahydro-9-acridineamine; 1,2,3,4-Tetrahydro-acridin-9-ylamine; 1,2,3,4-Tetrahydroaminoacridine; 1,2,3,4-tetrahydroacridin-9-amine; 5-Amino-6,7,8,9-tetrahydroacridine (European); 9-AMINOTETRAHYDROACRIDINE; 9-Acridinamine, 1,2,3,4-tetrahydro-(9CI); 9-Amino-1,2,3,4-Tetrahydroacridine Hydrate Hydrochloride Hydrate; 9-amino-1,2,3,4-tetrahydroacridine
Indication
Disease Entry ICD 11 Status REF
Alzheimer disease 8A20 Approved [1]
Therapeutic Class
Parasympathomimetics
Affected Organisms
Humans and other mammals
ATC Code
: Tacrine
N06CB: Psychostimulants in combination with psycholeptics
N06C: PSYCHOLEPTICS AND PSYCHOANALEPTICS IN COMBINATION
N06: PSYCHOANALEPTICS
N: NERVOUS SYSTEM
N06DA01: Tacrine
N06DA: Anticholinesterases
N06D: ANTI-DEMENTIA DRUGS
N06: PSYCHOANALEPTICS
N: NERVOUS SYSTEM
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 198.26
Logarithm of the Partition Coefficient (xlogp) 2.7
Rotatable Bond Count (rotbonds) 0
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [2]
Bioavailability
The bioavailability of drug is 17% []
Clearance
The drug present in the plasma can be removed from the body at the rate of 56 mL/min/kg [3]
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 2 - 4 hours [3]
Metabolism
The drug is metabolized via the hepatic []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 11.5283 micromolar/kg/day [4]
Unbound Fraction
The unbound fraction of drug in plasma is 0.25% [3]
Vd
The volume of distribution (Vd) of drug is 349 +/- 193 L []
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Dementia Not Available APOE OTFOWL2H [5]
Chemical Identifiers
Formula
C13H14N2
IUPAC Name
1,2,3,4-tetrahydroacridin-9-amine
Canonical SMILES
C1CCC2=NC3=CC=CC=C3C(=C2C1)N
InChI
InChI=1S/C13H14N2/c14-13-9-5-1-3-7-11(9)15-12-8-4-2-6-10(12)13/h1,3,5,7H,2,4,6,8H2,(H2,14,15)
InChIKey
YLJREFDVOIBQDA-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
1935
ChEBI ID
CHEBI:45980
CAS Number
321-64-2
UNII
4VX7YNB537
DrugBank ID
DB00382
TTD ID
D0E6YQ
VARIDT ID
DR00183
INTEDE ID
DR1523
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Acetylcholinesterase (AChE) TT1RS9F ACES_HUMAN Inhibitor [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
Glutathione S-transferase alpha-1 (GSTA1) DE4ZHS1 GSTA1_HUMAN Substrate [8]
Cytochrome P450 1A2 (CYP1A2)
Main DME 		DEJGDUW CP1A2_HUMAN Substrate [9]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Acetylcholinesterase (ACHE) OT2H8HG6 ACES_HUMAN Gene/Protein Processing [10]
Apolipoprotein E (APOE) OTFOWL2H APOE_HUMAN Drug Response [5]
Cholinesterase (BCHE) OTOH3WQ9 CHLE_HUMAN Gene/Protein Processing [11]
Cocaine esterase (CES2) OTC647SQ EST2_HUMAN Gene/Protein Processing [12]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Gene/Protein Processing [13]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Drug Response [14]
DNA damage-inducible transcript 3 protein (DDIT3) OTI8YKKE DDIT3_HUMAN Gene/Protein Processing [13]
Liver carboxylesterase 1 (CES1) OT9L0LR8 EST1_HUMAN Gene/Protein Processing [15]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Gene/Protein Processing [16]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_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 Alzheimer disease
ICD Disease Classification 8A20
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Acetylcholinesterase (AChE) DTT ACHE 6.39E-02 -1.07 -1.15
P-glycoprotein 1 (ABCB1) DTP P-GP 6.54E-01 1.95E-01 4.04E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 8.46E-01 -6.63E-03 -4.49E-02
Glutathione S-transferase alpha-1 (GSTA1) DME GSTA1 5.78E-01 3.39E-02 1.54E-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 Tacrine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [18]
Bethanechol DMCLHO0 Moderate Additive cholinergic effects by the combination of Tacrine and Bethanechol. Abnormal micturition [MF50] [19]
Midostaurin DMI6E0R Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Midostaurin. Acute myeloid leukaemia [2A60] [20]
Idarubicin DMM0XGL Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Idarubicin. Acute myeloid leukaemia [2A60] [20]
Daunorubicin DMQUSBT Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Daunorubicin. Acute myeloid leukaemia [2A60] [20]
Gilteritinib DMTI0ZO Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Gilteritinib. Acute myeloid leukaemia [2A60] [20]
Oliceridine DM6MDCF Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Oliceridine. Acute pain [MG31] [18]
Scopolamine DMOM8AL Moderate Antagonize the effect of Tacrine when combined with Scopolamine. Addictive disorder [6C50-6C5Z] [21]
Mepyramine DMB4SFH Moderate Antagonize the effect of Tacrine when combined with Mepyramine. Allergic/hypersensitivity disorder [4A80-4A8Z] [22]
Phenyltoloxamine DMKAEQW Moderate Antagonize the effect of Tacrine when combined with Phenyltoloxamine. Allergic/hypersensitivity disorder [4A80-4A8Z] [22]
Metronidazole DMTIVEN Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Metronidazole. Amoebiasis [1A36] [20]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [23]
Hydroxyzine DMF8Y74 Moderate Antagonize the effect of Tacrine when combined with Hydroxyzine. Anxiety disorder [6B00-6B0Z] [21]
Cilostazol DMZMSCT Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Cilostazol. Arterial occlusive disease [BD40] [20]
Voriconazole DMAOL2S Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Voriconazole. Aspergillosis [1F20] [20]
Posaconazole DMUL5EW Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Posaconazole. Aspergillosis [1F20] [20]
Terbutaline DMD4381 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Terbutaline. Asthma [CA23] [20]
Aminophylline DML2NIB Moderate Increased plasma concentrations of Tacrine and Aminophylline due to competitive inhibition of the same metabolic pathway. Asthma [CA23] [24]
Salbutamol DMN9CWF Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Salbutamol. Asthma [CA23] [18]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Tacrine and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [25]
Desipramine DMT2FDC Moderate Antagonize the effect of Tacrine when combined with Desipramine. Attention deficit hyperactivity disorder [6A05] [21]
Obeticholic acid DM3Q1SM Moderate Decreased metabolism of Tacrine caused by Obeticholic acid mediated inhibition of CYP450 enzyme. Autoimmune liver disease [DB96] [26]
Ciprofloxacin XR DM2NLS9 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Ciprofloxacin XR. Bacterial infection [1A00-1C4Z] [20]
Clarithromycin DM4M1SG Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Clarithromycin. Bacterial infection [1A00-1C4Z] [20]
Gemifloxacin DMHT34O Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Gemifloxacin. Bacterial infection [1A00-1C4Z] [20]
Norfloxacin DMIZ6W2 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Norfloxacin. Bacterial infection [1A00-1C4Z] [18]
Levofloxacin DMS60RB Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Levofloxacin. Bacterial infection [1A00-1C4Z] [20]
Telithromycin DMZ4P3A Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Telithromycin. Bacterial infection [1A00-1C4Z] [18]
Retigabine DMGNYIH Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Retigabine. Behcet disease [4A62] [18]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Tacrine and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [27]
Loperamide DMOJZQ9 Moderate Antagonize the effect of Tacrine when combined with Loperamide. Bowel habit change [ME05] [21]
Eribulin DM1DX4Q Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Eribulin. Breast cancer [2C60-2C6Y] [20]
Tamoxifen DMLB0EZ Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Tamoxifen. Breast cancer [2C60-2C6Y] [20]
Toremifene DMQYUWG Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Toremifene. Breast cancer [2C60-2C6Y] [20]
Bosutinib DMTI8YE Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Bosutinib. Breast cancer [2C60-2C6Y] [20]
PF-04449913 DMSB068 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [20]
Oxaliplatin DMQNWRD Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Oxaliplatin. Colorectal cancer [2B91] [20]
Halothane DM80OZ5 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Halothane. Corneal disease [9A76-9A78] [20]
Propofol DMB4OLE Moderate Increased risk of prolong QT interval by the combination of Tacrine and Propofol. Corneal disease [9A76-9A78] [28]
Sevoflurane DMC9O43 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Sevoflurane. Corneal disease [9A76-9A78] [20]
Clofazimine DMEBOFW Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Clofazimine. Crohn disease [DD70] [18]
Mifepristone DMGZQEF Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Mifepristone. Cushing syndrome [5A70] [20]
Pasireotide DMHM7JS Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Pasireotide. Cushing syndrome [5A70] [20]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Tacrine caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [29]
Sertraline DM0FB1J Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Sertraline. Depression [6A70-6A7Z] [20]
Trimipramine DM1SC8M Moderate Antagonize the effect of Tacrine when combined with Trimipramine. Depression [6A70-6A7Z] [21]
Cyclobenzaprine DM1YBRM Moderate Antagonize the effect of Tacrine when combined with Cyclobenzaprine. Depression [6A70-6A7Z] [21]
Imipramine DM2NUH3 Moderate Antagonize the effect of Tacrine when combined with Imipramine. Depression [6A70-6A7Z] [21]
Fluoxetine DM3PD2C Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Fluoxetine. Depression [6A70-6A7Z] [20]
Nortriptyline DM4KDYJ Moderate Antagonize the effect of Tacrine when combined with Nortriptyline. Depression [6A70-6A7Z] [21]
Escitalopram DMFK9HG Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Escitalopram. Depression [6A70-6A7Z] [20]
OPC-34712 DMHG57U Moderate Antagonize the effect of Tacrine when combined with OPC-34712. Depression [6A70-6A7Z] [21]
Clomipramine DMINRKW Moderate Antagonize the effect of Tacrine when combined with Clomipramine. Depression [6A70-6A7Z] [21]
Trazodone DMK1GBJ Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Trazodone. Depression [6A70-6A7Z] [20]
Amoxapine DMKITQE Moderate Antagonize the effect of Tacrine when combined with Amoxapine. Depression [6A70-6A7Z] [21]
Doxepin DMPI98T Moderate Antagonize the effect of Tacrine when combined with Doxepin. Depression [6A70-6A7Z] [22]
Maprotiline DMPWB7T Moderate Antagonize the effect of Tacrine when combined with Maprotiline. Depression [6A70-6A7Z] [21]
Hyoscyamine DM804UR Moderate Antagonize the effect of Tacrine when combined with Hyoscyamine. Digestive system disease [DE2Z] [21]
Mepenzolate DM8YU2F Moderate Antagonize the effect of Tacrine when combined with Mepenzolate. Digestive system disease [DE2Z] [30]
Oxybutynine DMJPBAX Moderate Antagonize the effect of Tacrine when combined with Oxybutynine. Discovery agent [N.A.] [21]
Tetrabenazine DMYWQ0O Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [20]
Meclizine DMS7T13 Moderate Antagonize the effect of Tacrine when combined with Meclizine. Dizziness and giddiness [MB48] [21]
Deutetrabenazine DMUPFLI Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Deutetrabenazine. Dystonic disorder [8A02] [20]
Ingrezza DMVPLNC Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Ingrezza. Dystonic disorder [8A02] [20]
Carbamazepine DMZOLBI Moderate Antagonize the effect of Tacrine when combined with Carbamazepine. Epilepsy/seizure [8A61-8A6Z] [21]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Cannabidiol. Epileptic encephalopathy [8A62] [25]
Diphenhydramine DMKQTBA Moderate Antagonize the effect of Tacrine when combined with Diphenhydramine. Episodic vestibular syndrome [AB31] [21]
Tropicamide DM1D90W Moderate Antagonize the effect of Tacrine when combined with Tropicamide. Eye anterior segment structural developmental anomaly [LA11] [30]
Solifenacin DMG592Q Moderate Antagonize the effect of Tacrine when combined with Solifenacin. Functional bladder disorder [GC50] [21]
Tolterodine DMSHPW8 Moderate Antagonize the effect of Tacrine when combined with Tolterodine. Functional bladder disorder [GC50] [21]
Darifenacin DMWXLYZ Moderate Antagonize the effect of Tacrine when combined with Darifenacin. Functional bladder disorder [GC50] [21]
Pentamidine DMHZJCG Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Pentamidine. Fungal infection [1F29-1F2F] [20]
Propantheline DM2EN6G Moderate Antagonize the effect of Tacrine when combined with Propantheline. Gastric ulcer [DA60] [21]
Cimetidine DMH61ZB Moderate Antagonize the effect of Tacrine when combined with Cimetidine. Gastro-oesophageal reflux disease [DA22] [21]
Sunitinib DMCBJSR Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Sunitinib. Gastrointestinal stromal tumour [2B5B] [20]
Cyclopentolate DMA8LM5 Moderate Antagonize the effect of Tacrine when combined with Cyclopentolate. General examination [QA00] [30]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Brentuximab vedotin. Hodgkin lymphoma [2B30] [31]
Fostemsavir DM50ILT Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [20]
Efavirenz DMC0GSJ Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Efavirenz. Human immunodeficiency virus disease [1C60-1C62] [32]
Rilpivirine DMJ0QOW Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [20]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Tacrine and Mipomersen. Hyper-lipoproteinaemia [5C80] [33]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Tacrine and Teriflunomide. Hyper-lipoproteinaemia [5C80] [20]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Tacrine and BMS-201038. Hyper-lipoproteinaemia [5C80] [34]
Belladonna DM2RBWK Moderate Antagonize the effect of Tacrine when combined with Belladonna. Infectious gastroenteritis/colitis [1A40] [21]
ITI-007 DMUQ1DO Moderate Antagonize the effect of Tacrine when combined with ITI-007. Insomnia [7A00-7A0Z] [21]
Polyethylene glycol DM4I1JP Moderate Increased risk of lowers seizure threshold by the combination of Tacrine and Polyethylene glycol. Irritable bowel syndrome [DD91] [35]
Alosetron DML2A03 Moderate Decreased metabolism of Tacrine caused by Alosetron mediated inhibition of CYP450 enzyme. Irritable bowel syndrome [DD91] [36]
Clidinium DMUMQZ0 Moderate Antagonize the effect of Tacrine when combined with Clidinium. Irritable bowel syndrome [DD91] [21]
Dicyclomine DMZSDGX Moderate Antagonize the effect of Tacrine when combined with Dicyclomine. Irritable bowel syndrome [DD91] [21]
Methotrexate DM2TEOL Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Methotrexate. Leukaemia [2A60-2B33] [25]
Physostigmine DM2N0TO Moderate Additive cholinergic effects by the combination of Tacrine and Physostigmine. Lips/oral mucosa miscellaneous disorder [DA02] [19]
Ceritinib DMB920Z Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Ceritinib. Lung cancer [2C25] [20]
Osimertinib DMRJLAT Moderate Increased metabolism of Tacrine caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [37]
Capmatinib DMYCXKL Moderate Decreased metabolism of Tacrine caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [38]
Selpercatinib DMZR15V Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Selpercatinib. Lung cancer [2C25] [18]
Lumefantrine DM29GAD Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Lumefantrine. Malaria [1F40-1F45] [18]
Chloroquine DMSI5CB Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Chloroquine. Malaria [1F40-1F45] [20]
Quinine DMSWYF5 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Quinine. Malaria [1F40-1F45] [20]
Primaquine DMWQ16I Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Primaquine. Malaria [1F40-1F45] [20]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [20]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Idelalisib. Mature B-cell leukaemia [2A82] [39]
Arsenic trioxide DM61TA4 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Arsenic trioxide. Mature B-cell lymphoma [2A85] [20]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Clofarabine. Mature B-cell lymphoma [2A85] [40]
Vemurafenib DM62UG5 Moderate Decreased metabolism of Tacrine caused by Vemurafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [41]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Tacrine and LGX818. Melanoma [2C30] [42]
Exjade DMHPRWG Moderate Decreased metabolism of Tacrine caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [43]
Panobinostat DM58WKG Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Panobinostat. Multiple myeloma [2A83] [20]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Thalidomide. Multiple myeloma [2A83] [18]
Siponimod DM2R86O Major Increased risk of bradycardia by the combination of Tacrine and Siponimod. Multiple sclerosis [8A40] [18]
Fingolimod DM5JVAN Moderate Increased risk of atrioventricular block by the combination of Tacrine and Fingolimod. Multiple sclerosis [8A40] [44]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Tacrine and Ozanimod. Multiple sclerosis [8A40] [45]
Neostigmine DM6T2J3 Moderate Additive cholinergic effects by the combination of Tacrine and Neostigmine. Myasthenia gravis [8C6Y] [19]
Pyridostigmine DM8HO1L Moderate Additive cholinergic effects by the combination of Tacrine and Pyridostigmine. Myasthenia gravis [8C6Y] [19]
Ambenonium DMOP0BL Moderate Additive cholinergic effects by the combination of Tacrine and Ambenonium. Myasthenia gravis [8C6Y] [19]
Romidepsin DMT5GNL Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Romidepsin. Mycosis fungoides [2B01] [18]
Nilotinib DM7HXWT Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Nilotinib. Myeloproliferative neoplasm [2A20] [20]
Dasatinib DMJV2EK Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Dasatinib. Myeloproliferative neoplasm [2A20] [20]
Droperidol DM0DXA8 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Droperidol. Nausea/vomiting [MD90] [20]
Dimenhydrinate DM264B3 Moderate Antagonize the effect of Tacrine when combined with Dimenhydrinate. Nausea/vomiting [MD90] [21]
Prochlorperazine DM53SRA Moderate Antagonize the effect of Tacrine when combined with Prochlorperazine. Nausea/vomiting [MD90] [21]
Promethazine DM6I5GR Moderate Antagonize the effect of Tacrine when combined with Promethazine. Nausea/vomiting [MD90] [21]
Granisetron DMIUW25 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Granisetron. Nausea/vomiting [MD90] [20]
Dolasetron DMMG26Z Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Dolasetron. Nausea/vomiting [MD90] [20]
Ondansetron DMOTQ1I Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Ondansetron. Nausea/vomiting [MD90] [20]
Bupropion DM5PCS7 Major Increased risk of lowers seizure threshold by the combination of Tacrine and Bupropion. Nicotine use disorder [6C4A] [46]
Entrectinib DMMPTLH Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Entrectinib. Non-small cell lung cancer [2C25] [18]
Lofexidine DM1WXA6 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Lofexidine. Opioid use disorder [6C43] [20]
Olaparib DM8QB1D Moderate Increased metabolism of Tacrine caused by Olaparib mediated induction of CYP450 enzyme. Ovarian cancer [2C73] [18]
Rucaparib DM9PVX8 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Rucaparib. Ovarian cancer [2C73] [20]
Dextropropoxyphene DM23HCX Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Dextropropoxyphene. Pain [MG30-MG3Z] [18]
Flavoxate DMKV4NL Moderate Antagonize the effect of Tacrine when combined with Flavoxate. Pain [MG30-MG3Z] [21]
Buprenorphine DMPRI8G Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Buprenorphine. Pain [MG30-MG3Z] [20]
Triclabendazole DMPWGBR Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Triclabendazole. Parasitic worm infestation [1F90] [18]
Biperiden DME78OA Moderate Antagonize the effect of Tacrine when combined with Biperiden. Parkinsonism [8A00] [30]
Procyclidine DMHFJDT Moderate Antagonize the effect of Tacrine when combined with Procyclidine. Parkinsonism [8A00] [30]
Pimavanserin DMR7IVC Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Pimavanserin. Parkinsonism [8A00] [20]
Orphenadrine DMW542E Moderate Antagonize the effect of Tacrine when combined with Orphenadrine. Parkinsonism [8A00] [21]
Apomorphine DMX38HQ Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Apomorphine. Parkinsonism [8A00] [20]
Abametapir DM2RX0I Moderate Decreased metabolism of Tacrine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [47]
Lindane DMB8CNL Moderate Increased risk of lowers seizure threshold by the combination of Tacrine and Lindane. Pediculosis [1G00] [48]
Ranitidine DM0GUSX Moderate Antagonize the effect of Tacrine when combined with Ranitidine. Peptic ulcer [DA61] [21]
Methylscopolamine DM5VWOB Moderate Antagonize the effect of Tacrine when combined with Methylscopolamine. Peptic ulcer [DA61] [21]
Famotidine DMRL3AB Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Famotidine. Peptic ulcer [DA61] [20]
Macimorelin DMQYJIR Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Macimorelin. Pituitary gland disorder [5A60-5A61] [20]
Lefamulin DME6G97 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Lefamulin. Pneumonia [CA40] [20]
Degarelix DM3O8QY Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Degarelix. Prostate cancer [2C82] [20]
Fluphenazine DMIT8LX Moderate Antagonize the effect of Tacrine when combined with Fluphenazine. Psychotic disorder [6A20-6A25] [21]
Sorafenib DMS8IFC Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Sorafenib. Renal cell carcinoma [2C90] [20]
Gatifloxacin DMSL679 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Gatifloxacin. Respiratory infection [CA07-CA4Z] [18]
Cyproheptadine DM92AH3 Moderate Antagonize the effect of Tacrine when combined with Cyproheptadine. Rheumatoid arthritis [FA20] [21]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Tacrine and Leflunomide. Rheumatoid arthritis [FA20] [20]
Quetiapine DM1N62C Moderate Antagonize the effect of Tacrine when combined with Quetiapine. Schizophrenia [6A20] [21]
Mesoridazine DM2ZGAN Moderate Antagonize the effect of Tacrine when combined with Mesoridazine. Schizophrenia [6A20] [22]
Thioridazine DM35M8J Moderate Antagonize the effect of Tacrine when combined with Thioridazine. Schizophrenia [6A20] [22]
Aripiprazole DM3NUMH Moderate Antagonize the effect of Tacrine when combined with Aripiprazole. Schizophrenia [6A20] [21]
Iloperidone DM6AUFY Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Iloperidone. Schizophrenia [6A20] [20]
Paliperidone DM7NPJS Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Paliperidone. Schizophrenia [6A20] [20]
Loxapine DM8AI9U Moderate Antagonize the effect of Tacrine when combined with Loxapine. Schizophrenia [6A20] [21]
Perphenazine DMA4MRX Moderate Antagonize the effect of Tacrine when combined with Perphenazine. Schizophrenia [6A20] [21]
Molindone DMAH70G Moderate Antagonize the effect of Tacrine when combined with Molindone. Schizophrenia [6A20] [21]
Chlorpromazine DMBGZI3 Moderate Antagonize the effect of Tacrine when combined with Chlorpromazine. Schizophrenia [6A20] [21]
Thiothixene DMDINC4 Moderate Antagonize the effect of Tacrine when combined with Thiothixene. Schizophrenia [6A20] [21]
Risperidone DMN6DXL Moderate Antagonize the effect of Tacrine when combined with Risperidone. Schizophrenia [6A20] [21]
Asenapine DMSQZE2 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Asenapine. Schizophrenia [6A20] [20]
Pimozide DMW83TP Moderate Antagonize the effect of Tacrine when combined with Pimozide. Schizophrenia [6A20] [21]
Vardenafil DMTBGW8 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Vardenafil. Sexual dysfunction [HA00-HA01] [20]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [25]
Epirubicin DMPDW6T Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Epirubicin. Solid tumour/cancer [2A00-2F9Z] [20]
Vandetanib DMRICNP Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [20]
Triptorelin DMTK4LS Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [20]
Doxorubicin DMVP5YE Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [20]
Pitolisant DM8RFNJ Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Pitolisant. Somnolence [MG42] [20]
Telavancin DM58VQX Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [20]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Tacrine and Naltrexone. Substance abuse [6C40] [49]
Lenvatinib DMB1IU4 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Lenvatinib. Thyroid cancer [2D10] [20]
Cabozantinib DMIYDT4 Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Cabozantinib. Thyroid cancer [2D10] [20]
Tizanidine DMR2IQ4 Major Decreased metabolism of Tacrine caused by Tizanidine mediated inhibition of CYP450 enzyme. Tonus and reflex abnormality [MB47] [50]
Atropine DMEN6X7 Moderate Antagonize the effect of Tacrine when combined with Atropine. Unspecific substance harmful effect [NE6Z] [21]
Triprolidine DM7SWIA Moderate Antagonize the effect of Tacrine when combined with Triprolidine. Vasomotor/allergic rhinitis [CA08] [21]
Carbinoxamine DMCT31R Moderate Antagonize the effect of Tacrine when combined with Carbinoxamine. Vasomotor/allergic rhinitis [CA08] [21]
Brompheniramine DMFOVSD Moderate Antagonize the effect of Tacrine when combined with Brompheniramine. Vasomotor/allergic rhinitis [CA08] [21]
Dexbrompheniramine DMKVWGE Moderate Antagonize the effect of Tacrine when combined with Dexbrompheniramine. Vasomotor/allergic rhinitis [CA08] [21]
Acrivastine DMTIGA0 Moderate Antagonize the effect of Tacrine when combined with Acrivastine. Vasomotor/allergic rhinitis [CA08] [22]
Procainamide DMNMXR8 Moderate Antagonize the effect of Tacrine when combined with Procainamide. Ventricular tachyarrhythmia [BC71] [21]
Propafenone DMPIBJK Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Propafenone. Ventricular tachyarrhythmia [BC71] [20]
Flecainide DMSQDLE Moderate Increased risk of ventricular arrhythmias by the combination of Tacrine and Flecainide. Ventricular tachyarrhythmia [BC71] [20]
⏷ Show the Full List of 186 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: 6687).
2 BDDCS applied to over 900 drugs
3 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4 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
5 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
6 Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002 Jun;(127):6-19.
7 Tacrine sinusoidal uptake and biliary excretion in sandwich-cultured primary rat hepatocytes. J Pharm Pharm Sci. 2014;17(3):427-38.
8 Combined glutathione-S-transferase M1 and T1 genetic polymorphism and tacrine hepatotoxicity. Clin Pharmacol Ther. 2000 Apr;67(4):432-7.
9 Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218.
10 Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changes. Eur J Pharmacol. 1989 Nov 28;173(1):53-64. doi: 10.1016/0014-2999(89)90008-3.
11 Comparative effects of cationic triarylmethane, phenoxazine and phenothiazine dyes on horse serum butyrylcholinesterase. Arch Biochem Biophys. 2008 Oct 15;478(2):201-5.
12 Inhibition of human carboxylesterases hCE1 and hiCE by cholinesterase inhibitors. Chem Biol Interact. 2013 Mar 25;203(1):226-30.
13 High-content imaging-based BAC-GFP toxicity pathway reporters to assess chemical adversity liabilities. Arch Toxicol. 2017 Mar;91(3):1367-1383. doi: 10.1007/s00204-016-1781-0. Epub 2016 Jun 29.
14 Development of a highly sensitive cytotoxicity assay system for CYP3A4-mediated metabolic activation. Drug Metab Dispos. 2011 Aug;39(8):1388-95. doi: 10.1124/dmd.110.037077. Epub 2011 May 3.
15 Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. Chem Biol. 2003 Apr;10(4):341-9. doi: 10.1016/s1074-5521(03)00071-1.
16 Reduction and scavenging of chemically reactive drug metabolites by NAD(P)H:quinone oxidoreductase 1 and NRH:quinone oxidoreductase 2 and variability in hepatic concentrations. Chem Res Toxicol. 2018 Feb 19;31(2):116-126.
17 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
18 Cerner Multum, Inc. "Australian Product Information.".
19 Product Information. Aricept (donepezil). Pfizer US Pharmaceuticals, New York, NY.
20 Canadian Pharmacists Association.
21 Beers MH, Ouslander JG, Rollingher I, Reuben DB, Brooks J, Beck JC "Explicit criteria for determining inappropriate medication use in nursing home residents." Arch Intern Med 151 (1991): 1825-32. [PMID: 1888249]
22 Carnahan RM, Lund BC, Perry PJ, Chrischilles EA "The concurrent use of anticholinergics and cholinesterase inhibitors: rare event or common practice?" J Am Geriatr Soc 52 (2004): 2082-7. [PMID: 15571547]
23 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
24 Product Information. Cognex (tacrine). Parke-Davis, Morris Plains, NJ.
25 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
26 Product Information. Ocaliva (obeticholic acid). Intercept Pharmaceuticals, Inc., New York, NY.
27 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
28 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]
29 Product Information. Isturisa (osilodrostat). Recordati Rare Diseases Inc, Lebanon, NJ.
30 Katz IR, Sands LP, Bilker W, DiFilippo S, Boyce A, D'Angelo K "Identification of medications that cause cognitive impairment in older people: the case of oxybutynin chloride." J Am Geriatr Soc 46 (1998): 8-13. [PMID: 9434659]
31 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
32 Elsharkawy AM, Schwab U, McCarron B, et al. "Efavirenz induced acute liver failure requiring liver transplantation in a slow drug metaboliser." J Clin Virol 58 (2013): 331-3. [PMID: 23763943]
33 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
34 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
35 Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.
36 Product Information. Lotronex (alosetron). Glaxo Wellcome, Research Triangle Park, NC.
37 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
38 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
39 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
40 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
41 Product Information. Zelboraf (vemurafenib). Genentech, South San Francisco, CA.
42 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
43 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
44 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
45 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
46 Product Information. Wellbutrin XL (buPROPion). GlaxoSmithKline, Philadelphia, PA.
47 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
48 Matsuoka LY "Convulsions following application of gamma benzene hexachloride." J Am Acad Dermatol 5 (1981): 98-9. [PMID: 6168673]
49 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
50 Granfors MT, Backman JT, Laitila J, Neuvonen PJ "Tizanidine is mainly metabolized by cytochrome P450 1A2 in vitro." Br J Clin Pharmacol 57 (2004): 349-53. [PMID: 14998432]