Details of the Drug

General Information of Drug (ID: DMA4MRX)

Drug Name
Perphenazine
Synonyms
Chlorperphenazine; Chlorpiprazine; Decentan; Emesinal; Etaperazin; Etaperazine; Ethaperazine; Fentazin;PZC; Perfenazina; Perfenazine; Perphenan; Perphenazin; Perphenazinum; Thilatazin; Tranquisan; Trifaron; Trilafon; Trilifan; Triphenot; Perfenazina [Italian]; Perphenazine [Trilafon]; Perphenazine maleate; P 6402; Sch 3940; Apo-Perphenazine; F-mon; Perfenazina [INN-Spanish]; Perphenazinum [INN-Latin]; SCH-3940; Siquil (TN); Triavil (TN); Perphenazine [INN:BAN:JAN]; Perphenazine (JP15/USP/INN); Gamma-[4-(beta-Hydroxyethyl)piperazin-1-yl]propyl-2-chlorophenothiazine; Gamma-(4-(beta-Hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine; 1',1-(2-Idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina; 1',1-(2-Idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina [Italian]; 1-(2-Hydroxyethyl)-4-(3-(2-chloro-10-phenothiazinyl)propyl)piperazine; 1-(2-Hydroxyethyl)-4-[3-(2-chloro-10-phenothiazinyl)propyl]piperazine; 1-Piperazineethanol, 4-[3-(2-chlorophenothiazin-10-yl)propyl]-, trihydrochloride; 2-(4-[3-(2-Chloro-10H-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol; 2-Chloro-10-(3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl)phenothiazine; 2-Chloro-10-(3-(4-(2-hydroxyethyl)piperazin-1-yl)propyl)phenothiazine; 2-Chloro-10-3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl phenothiazine; 2-Chloro-10-3-[1-(2-hydroxyethyl)-4-piperazinyl]propyl phenothiazine; 2-Chloro-10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazine; 2-[4-[3-(2-Chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol;2-{4-[3-(2-Chloro-phenothiazin-10-yl)-propyl]-piperazin-1-yl}-ethanol; 2-{4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl}ethanol; 4-(3-(2-Chlorophenothiazin-10-yl)propyl)-1-piperazineethanol; 4-[3-(2-Chloro-10H-phenothiazin-10-yl)propyl]-1-piperazineethanol; 4-[3-(2-Chlorophenothiazin-10-yl)propyl]-1-piperazineethanol
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Approved [1], [2]
Therapeutic Class
Antipsychotic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 404
Topological Polar Surface Area (xlogp) 4.2
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Bioavailability
The bioavailability of drug is 40% [3]
Clearance
The drug present in the plasma can be removed from the body at the rate of 27 mL/min/kg [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 8 - 12 hours [4]
Metabolism
The drug is metabolized via the hepatic [3]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.99015 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.07% [4]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 18 L/kg [4]
Chemical Identifiers
Formula
C21H26ClN3OS
IUPAC Name
2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
Canonical SMILES
C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO
InChI
InChI=1S/C21H26ClN3OS/c22-17-6-7-21-19(16-17)25(18-4-1-2-5-20(18)27-21)9-3-8-23-10-12-24(13-11-23)14-15-26/h1-2,4-7,16,26H,3,8-15H2
InChIKey
RGCVKNLCSQQDEP-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
4748
ChEBI ID
CHEBI:8028
CAS Number
58-39-9
DrugBank ID
DB00850
TTD ID
D02HED
VARIDT ID
DR00759
INTEDE ID
DR1264
ACDINA ID
D00521

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Antagonist [6], [7]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [8]
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 [10]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [10]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [12]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [10]
Cytochrome P450 2C18 (CYP2C18) DEZMWRE CP2CI_HUMAN Substrate [10]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Schizophrenia
ICD Disease Classification 6A20
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Dopamine D2 receptor (D2R) DTT DRD2 2.50E-02 -0.08 -0.49
P-glycoprotein 1 (ABCB1) DTP P-GP 9.39E-02 1.07E-01 2.80E-01
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 8.54E-01 1.24E-02 7.20E-02
Cytochrome P450 2C18 (CYP2C18) DME CYP2C18 5.67E-02 2.96E-03 1.50E-02
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.82E-04 -1.35E-01 -5.84E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.36E-01 1.62E-02 1.08E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 2.40E-01 -3.31E-02 -1.97E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 7.30E-01 -1.91E-02 -1.41E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 1.90E-01 -9.81E-03 -5.96E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-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 Same Disease as Perphenazine
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Mesoridazine DM2ZGAN Major Increased risk of prolong QT interval by the combination of Perphenazine and Mesoridazine. Schizophrenia [6A20] [91]
Aripiprazole DM3NUMH Moderate Additive anticholinergic effects by the combination of Perphenazine and Aripiprazole. Schizophrenia [6A20] [92]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Perphenazine and Iloperidone. Schizophrenia [6A20] [91]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Paliperidone. Schizophrenia [6A20] [91]
Molindone DMAH70G Moderate Additive anticholinergic effects by the combination of Perphenazine and Molindone. Schizophrenia [6A20] [92]
Thiothixene DMDINC4 Moderate Additive anticholinergic effects by the combination of Perphenazine and Thiothixene. Schizophrenia [6A20] [92]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Perphenazine and Amisulpride. Schizophrenia [6A20] [93]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Asenapine. Schizophrenia [6A20] [91]
Pimozide DMW83TP Major Increased risk of prolong QT interval by the combination of Perphenazine and Pimozide. Schizophrenia [6A20] [94]
⏷ Show the Full List of 9 DDI Information of This Drug
Coadministration of a Drug Treating the Disease Different from Perphenazine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Perphenazine and Ivosidenib. Acute myeloid leukaemia [2A60] [95]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Midostaurin. Acute myeloid leukaemia [2A60] [91]
Idarubicin DMM0XGL Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Idarubicin. Acute myeloid leukaemia [2A60] [91]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Arn-509. Acute myeloid leukaemia [2A60] [94]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Perphenazine and Oliceridine. Acute pain [MG31] [96]
Phenyltoloxamine DMKAEQW Moderate Additive anticholinergic effects by the combination of Perphenazine and Phenyltoloxamine. Allergic/hypersensitivity disorder [4A80-4A8Z] [97]
Memantine DMD9WSC Moderate Additive anticholinergic effects by the combination of Perphenazine and Memantine. Alzheimer disease [8A20] [92]
Rivastigmine DMG629M Moderate Antagonize the effect of Perphenazine when combined with Rivastigmine. Alzheimer disease [8A20] [98]
Metronidazole DMTIVEN Minor Increased risk of prolong QT interval by the combination of Perphenazine and Metronidazole. Amoebiasis [1A36] [99]
Isosorbide dinitrate DMBI4JG Moderate Additive hypotensive effects by the combination of Perphenazine and Isosorbide dinitrate. Anal fissure/fistula [DB50] [100]
Trimethaphan DMHF4IQ Moderate Additive hypotensive effects by the combination of Perphenazine and Trimethaphan. Aneurysm/dissection [BD50] [101]
Bepridil DM0RKS4 Major Increased risk of prolong QT interval by the combination of Perphenazine and Bepridil. Angina pectoris [BA40] [91]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Perphenazine and Dronedarone. Angina pectoris [BA40] [91]
Amyl nitrite DMJKO05 Moderate Additive hypotensive effects by the combination of Perphenazine and Amyl nitrite. Angina pectoris [BA40] [100]
Nifedipine DMSVOZT Moderate Additive hypotensive effects by the combination of Perphenazine and Nifedipine. Angina pectoris [BA40] [100]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Perphenazine and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [102]
Cilostazol DMZMSCT Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Cilostazol. Arterial occlusive disease [BD40] [91]
Posaconazole DMUL5EW Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Posaconazole. Aspergillosis [1F20] [91]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Levalbuterol. Asthma [CA23] [103]
Terbutaline DMD4381 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Terbutaline. Asthma [CA23] [104]
Pirbuterol DMI5678 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Pirbuterol. Asthma [CA23] [104]
Salbutamol DMN9CWF Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Salbutamol. Asthma [CA23] [103]
Formoterol DMSOURV Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Formoterol. Asthma [CA23] [104]
Lisdexamfetamine DM6W8V5 Moderate Antagonize the effect of Perphenazine when combined with Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [105]
Clarithromycin DM4M1SG Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Clarithromycin. Bacterial infection [1A00-1C4Z] [91]
Sulfamethoxazole DMB08GE Minor Increased risk of prolong QT interval by the combination of Perphenazine and Sulfamethoxazole. Bacterial infection [1A00-1C4Z] [91]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Perphenazine and Sparfloxacin. Bacterial infection [1A00-1C4Z] [106]
Gemifloxacin DMHT34O Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Gemifloxacin. Bacterial infection [1A00-1C4Z] [106]
Norfloxacin DMIZ6W2 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Norfloxacin. Bacterial infection [1A00-1C4Z] [106]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Levofloxacin. Bacterial infection [1A00-1C4Z] [106]
Lomefloxacin DMVRH9C Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Lomefloxacin. Bacterial infection [1A00-1C4Z] [91]
Telithromycin DMZ4P3A Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Telithromycin. Bacterial infection [1A00-1C4Z] [91]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Retigabine. Behcet disease [4A62] [91]
Cariprazine DMJYDVK Moderate Additive anticholinergic effects by the combination of Perphenazine and Cariprazine. Bipolar disorder [6A60] [92]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Eribulin. Breast cancer [2C60-2C6Y] [91]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Lapatinib. Breast cancer [2C60-2C6Y] [91]
Acetylcholine DMDF79Z Moderate Antagonize the effect of Perphenazine when combined with Acetylcholine. Cataract [9B10] [107]
Umeclidinium DM4E8O9 Moderate Additive anticholinergic effects by the combination of Perphenazine and Umeclidinium. Chronic obstructive pulmonary disease [CA22] [108]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Olodaterol. Chronic obstructive pulmonary disease [CA22] [104]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Vilanterol. Chronic obstructive pulmonary disease [CA22] [103]
Tiotropium DMFDC0Q Moderate Additive anticholinergic effects by the combination of Perphenazine and Tiotropium. Chronic obstructive pulmonary disease [CA22] [108]
Salmeterol DMIEU69 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Salmeterol. Chronic obstructive pulmonary disease [CA22] [104]
Revefenacin DMMP5SI Moderate Additive anticholinergic effects by the combination of Perphenazine and Revefenacin. Chronic obstructive pulmonary disease [CA22] [108]
Indacaterol DMQJHR7 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Indacaterol. Chronic obstructive pulmonary disease [CA22] [104]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Arformoterol. Chronic obstructive pulmonary disease [CA22] [104]
Dihydrocodeine DMB0FWL Major Additive CNS depression effects by the combination of Perphenazine and Dihydrocodeine. Chronic pain [MG30] [109]
Isoproterenol DMK7MEY Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Isoproterenol. Conduction disorder [BC63] [103]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Sevoflurane. Corneal disease [9A76-9A78] [91]
Remifentanil DMZTXCH Major Additive CNS depression effects by the combination of Perphenazine and Remifentanil. Corneal disease [9A76-9A78] [96]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Probucol. Coronary atherosclerosis [BA80] [91]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Perphenazine and Pasireotide. Cushing syndrome [5A70] [91]
Cyclandelate DMO0R76 Moderate Additive hypotensive effects by the combination of Perphenazine and Cyclandelate. Dementia [6D80-6D8Z] [100]
Selegiline DM6034S Moderate Additive hypotensive effects by the combination of Perphenazine and Selegiline. Depression [6A70-6A7Z] [110]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Perphenazine and Isocarboxazid. Depression [6A70-6A7Z] [110]
Escitalopram DMFK9HG Major Increased risk of prolong QT interval by the combination of Perphenazine and Escitalopram. Depression [6A70-6A7Z] [91]
OPC-34712 DMHG57U Moderate Additive anticholinergic effects by the combination of Perphenazine and OPC-34712. Depression [6A70-6A7Z] [92]
Clomipramine DMINRKW Moderate Increased plasma concentrations of Perphenazine and Clomipramine due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [111]
Doxepin DMPI98T Moderate Increased plasma concentrations of Perphenazine and Doxepin due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [112]
Maprotiline DMPWB7T Moderate Additive anticholinergic effects by the combination of Perphenazine and Maprotiline. Depression [6A70-6A7Z] [92]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Perphenazine and Esketamine. Depression [6A70-6A7Z] [99]
Mepenzolate DM8YU2F Moderate Additive anticholinergic effects by the combination of Perphenazine and Mepenzolate. Digestive system disease [DE2Z] [92]
Oxybutynine DMJPBAX Moderate Additive anticholinergic effects by the combination of Perphenazine and Oxybutynine. Discovery agent [N.A.] [92]
Tetrabenazine DMYWQ0O Major Additive antidopaminergic effects by the combination of Perphenazine and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [113]
Deutetrabenazine DMUPFLI Major Increased risk of prolong QT interval by the combination of Perphenazine and Deutetrabenazine. Dystonic disorder [8A02] [114]
Zonisamide DM0DTF7 Major Increased risk of hyperpyrexia by the combination of Perphenazine and Zonisamide. Epilepsy/seizure [8A61-8A6Z] [115]
Diphenhydramine DMKQTBA Moderate Antagonize the effect of Perphenazine when combined with Diphenhydramine. Episodic vestibular syndrome [AB31] [116]
Ethacrynic acid DM60QMR Moderate Additive hypotensive effects by the combination of Perphenazine and Ethacrynic acid. Essential hypertension [BA00] [101]
Phenoxybenzamine DM8KSQH Moderate Additive hypotensive effects by the combination of Perphenazine and Phenoxybenzamine. Essential hypertension [BA00] [100]
Nadolol DMW6GVL Moderate Additive hypotensive effects by the combination of Perphenazine and Nadolol. Essential hypertension [BA00] [100]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Solifenacin. Functional bladder disorder [GC50] [91]
Mirabegron DMS1GYT Moderate Decreased metabolism of Perphenazine caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [117]
Tolterodine DMSHPW8 Moderate Additive anticholinergic effects by the combination of Perphenazine and Tolterodine. Functional bladder disorder [GC50] [92]
Terbinafine DMI6HUW Moderate Decreased metabolism of Perphenazine caused by Terbinafine mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [118]
Ketoconazole DMPZI3Q Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Ketoconazole. Fungal infection [1F29-1F2F] [91]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Sunitinib. Gastrointestinal stromal tumour [2B5B] [91]
Pilocarpine DMV9ADG Moderate Antagonize the effect of Perphenazine when combined with Pilocarpine. Glaucoma [9C61] [107]
Carvedilol DMHTEAO Moderate Additive hypotensive effects by the combination of Perphenazine and Carvedilol. Heart failure [BD10-BD1Z] [100]
Chlorothiazide DMLHESP Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Chlorothiazide. Heart failure [BD10-BD1Z] [99]
Bumetanide DMRV7H0 Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Bumetanide. Heart failure [BD10-BD1Z] [99]
Procarbazine DMIK367 Moderate Additive CNS depression effects by the combination of Perphenazine and Procarbazine. Hodgkin lymphoma [2B30] [110]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Perphenazine caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [119]
Saquinavir DMG814N Major Increased risk of prolong QT interval by the combination of Perphenazine and Saquinavir. Human immunodeficiency virus disease [1C60-1C62] [120]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [91]
Isosorbide mononitrate DMYLMU0 Moderate Additive hypotensive effects by the combination of Perphenazine and Isosorbide mononitrate. Hydrocephalus [8D64] [100]
Cinacalcet DMCX0K3 Moderate Decreased metabolism of Perphenazine caused by Cinacalcet mediated inhibition of CYP450 enzyme. Hyper-parathyroidism [5A51] [99]
Eprosartan DM07K2I Moderate Additive hypotensive effects by the combination of Perphenazine and Eprosartan. Hypertension [BA00-BA04] [100]
Acebutolol DM0TI4U Moderate Additive hypotensive effects by the combination of Perphenazine and Acebutolol. Hypertension [BA00-BA04] [100]
Captopril DM458UM Moderate Additive hypotensive effects by the combination of Perphenazine and Captopril. Hypertension [BA00-BA04] [100]
Penbutolol DM4ES8F Moderate Additive hypotensive effects by the combination of Perphenazine and Penbutolol. Hypertension [BA00-BA04] [100]
Methyldopa DM5I621 Moderate Additive hypotensive effects by the combination of Perphenazine and Methyldopa. Hypertension [BA00-BA04] [100]
Nebivolol DM7F1PA Moderate Additive hypotensive effects by the combination of Perphenazine and Nebivolol. Hypertension [BA00-BA04] [100]
Levamlodipine DM92S6N Moderate Additive hypotensive effects by the combination of Perphenazine and Levamlodipine. Hypertension [BA00-BA04] [100]
TAK-491 DMCF6SX Moderate Additive hypotensive effects by the combination of Perphenazine and TAK-491. Hypertension [BA00-BA04] [100]
Trichlormethiazide DMHAQCO Moderate Additive hypotensive effects by the combination of Perphenazine and Trichlormethiazide. Hypertension [BA00-BA04] [100]
Diazoxide DML1538 Moderate Additive hypotensive effects by the combination of Perphenazine and Diazoxide. Hypertension [BA00-BA04] [100]
Felodipine DMOSW35 Moderate Additive hypotensive effects by the combination of Perphenazine and Felodipine. Hypertension [BA00-BA04] [100]
Quinapril DMR8H31 Moderate Additive hypotensive effects by the combination of Perphenazine and Quinapril. Hypertension [BA00-BA04] [100]
Deserpidine DMRH7CV Moderate Additive hypotensive effects by the combination of Perphenazine and Deserpidine. Hypertension [BA00-BA04] [100]
Telmisartan DMS3GX2 Moderate Additive hypotensive effects by the combination of Perphenazine and Telmisartan. Hypertension [BA00-BA04] [100]
Irbesartan DMTP1DC Moderate Additive hypotensive effects by the combination of Perphenazine and Irbesartan. Hypertension [BA00-BA04] [100]
Clevidipine butyrate DMW4M97 Moderate Additive hypotensive effects by the combination of Perphenazine and Clevidipine butyrate. Hypertension [BA00-BA04] [100]
Belladonna DM2RBWK Moderate Additive anticholinergic effects by the combination of Perphenazine and Belladonna. Infectious gastroenteritis/colitis [1A40] [92]
Amantadine DMS3YE9 Moderate Additive anticholinergic effects by the combination of Perphenazine and Amantadine. Influenza [1E30-1E32] [121]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Perphenazine caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [122]
ITI-007 DMUQ1DO Moderate Additive anticholinergic effects by the combination of Perphenazine and ITI-007. Insomnia [7A00-7A0Z] [92]
Polyethylene glycol DM4I1JP Moderate Increased risk of lowers seizure threshold by the combination of Perphenazine and Polyethylene glycol. Irritable bowel syndrome [DD91] [91]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Phenolphthalein. Irritable bowel syndrome [DD91] [91]
Physostigmine DM2N0TO Moderate Antagonize the effect of Perphenazine when combined with Physostigmine. Lips/oral mucosa miscellaneous disorder [DA02] [98]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Perphenazine caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [94]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Perphenazine and Crizotinib. Lung cancer [2C25] [123]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Perphenazine and Ceritinib. Lung cancer [2C25] [91]
Dacomitinib DMOH8VY Moderate Decreased metabolism of Perphenazine caused by Dacomitinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [124]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Perphenazine and Osimertinib. Lung cancer [2C25] [125]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Perphenazine and Lumefantrine. Malaria [1F40-1F45] [99]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Perphenazine and Halofantrine. Malaria [1F40-1F45] [126]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Perphenazine and Hydroxychloroquine. Malaria [1F40-1F45] [127]
Primaquine DMWQ16I Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Primaquine. Malaria [1F40-1F45] [91]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [94]
Arsenic trioxide DM61TA4 Major Increased risk of prolong QT interval by the combination of Perphenazine and Arsenic trioxide. Mature B-cell lymphoma [2A85] [128]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Perphenazine and Vemurafenib. Melanoma [2C30] [91]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and LGX818. Melanoma [2C30] [129]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Perphenazine and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [130]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Perphenazine and Lasmiditan. Migraine [8A80] [131]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Perphenazine and Flibanserin. Mood disorder [6A60-6E23] [132]
Thalidomide DM70BU5 Moderate Additive CNS depression effects by the combination of Perphenazine and Thalidomide. Multiple myeloma [2A83] [133]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Perphenazine and Siponimod. Multiple sclerosis [8A40] [99]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Perphenazine and Fingolimod. Multiple sclerosis [8A40] [91]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Perphenazine and Ozanimod. Multiple sclerosis [8A40] [134]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Romidepsin. Mycosis fungoides [2B01] [91]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Perphenazine caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [94]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Perphenazine and Nilotinib. Myeloproliferative neoplasm [2A20] [91]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Dasatinib. Myeloproliferative neoplasm [2A20] [135]
Dextroamphetamine DMMIHVP Moderate Antagonize the effect of Perphenazine when combined with Dextroamphetamine. Narcolepsy [7A20] [105]
Phenindamine DMDTC7R Moderate Additive anticholinergic effects by the combination of Perphenazine and Phenindamine. Nasopharyngitis [CA00] [92]
Dimenhydrinate DM264B3 Moderate Additive anticholinergic effects by the combination of Perphenazine and Dimenhydrinate. Nausea/vomiting [MD90] [92]
Promethazine DM6I5GR Moderate Additive anticholinergic effects by the combination of Perphenazine and Promethazine. Nausea/vomiting [MD90] [92]
Rolapitant DM8XP26 Moderate Decreased metabolism of Perphenazine caused by Rolapitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [136]
Cyclizine DM9G7BS Moderate Additive anticholinergic effects by the combination of Perphenazine and Cyclizine. Nausea/vomiting [MD90] [92]
Metoclopramide DMFA5MY Major Additive antidopaminergic effects by the combination of Perphenazine and Metoclopramide. Nausea/vomiting [MD90] [137]
Granisetron DMIUW25 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Granisetron. Nausea/vomiting [MD90] [91]
Ondansetron DMOTQ1I Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Ondansetron. Nausea/vomiting [MD90] [91]
Bupropion DM5PCS7 Major Increased risk of lowers seizure threshold by the combination of Perphenazine and Bupropion. Nicotine use disorder [6C4A] [91]
Phendimetrazine DM6TS1N Moderate Antagonize the effect of Perphenazine when combined with Phendimetrazine. Obesity [5B80-5B81] [105]
Amfepramone DM9YSNQ Moderate Antagonize the effect of Perphenazine when combined with Amfepramone. Obesity [5B80-5B81] [105]
Lorcaserin DMG6OYJ Moderate Increased risk of hyperprolactinemic effects by the combination of Perphenazine and Lorcaserin. Obesity [5B80-5B81] [138]
Benzphetamine DMIJATC Moderate Antagonize the effect of Perphenazine when combined with Benzphetamine. Obesity [5B80-5B81] [105]
Polythiazide DMCH80F Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Polythiazide. Oedema [MG29] [99]
Levomethadyl Acetate DM06HG5 Major Increased risk of prolong QT interval by the combination of Perphenazine and Levomethadyl Acetate. Opioid use disorder [6C43] [94]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Perphenazine and Lofexidine. Opioid use disorder [6C43] [91]
Apraclonidine DMO4PVE Moderate Additive CNS depression effects by the combination of Perphenazine and Apraclonidine. Optic nerve disorder [9C40] [139]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Rucaparib. Ovarian cancer [2C73] [91]
Oxymorphone DM65AGJ Major Additive CNS depression effects by the combination of Perphenazine and Oxymorphone. Pain [MG30-MG3Z] [96]
Levorphanol DMGS80V Major Additive CNS depression effects by the combination of Perphenazine and Levorphanol. Pain [MG30-MG3Z] [96]
Dezocine DMJDB0Y Major Additive CNS depression effects by the combination of Perphenazine and Dezocine. Pain [MG30-MG3Z] [96]
Buprenorphine DMPRI8G Major Additive CNS depression effects by the combination of Perphenazine and Buprenorphine. Pain [MG30-MG3Z] [140]
Hydrocodone DMQ2JO5 Major Additive CNS depression effects by the combination of Perphenazine and Hydrocodone. Pain [MG30-MG3Z] [96]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Triclabendazole. Parasitic worm infestation [1F90] [91]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Perphenazine and Safinamide. Parkinsonism [8A00] [110]
Pergolide DM14MAE Moderate Antagonize the effect of Perphenazine when combined with Pergolide. Parkinsonism [8A00] [141]
Opicapone DM1BKA6 Moderate Antagonize the effect of Perphenazine when combined with Opicapone. Parkinsonism [8A00] [141]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Perphenazine and Rasagiline. Parkinsonism [8A00] [110]
Levodopa DMN3E57 Moderate Antagonize the effect of Perphenazine when combined with Levodopa. Parkinsonism [8A00] [141]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Pimavanserin. Parkinsonism [8A00] [142]
Bromocriptine DMVE3TK Moderate Antagonize the effect of Perphenazine when combined with Bromocriptine. Parkinsonism [8A00] [141]
Methylscopolamine DM5VWOB Moderate Additive anticholinergic effects by the combination of Perphenazine and Methylscopolamine. Peptic ulcer [DA61] [92]
Famotidine DMRL3AB Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Famotidine. Peptic ulcer [DA61] [99]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Perphenazine and Macimorelin. Pituitary gland disorder [5A60-5A61] [143]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Perphenazine and Lefamulin. Pneumonia [CA40] [144]
Ritodrine DM4V6RL Moderate Increased risk of ventricular arrhythmias by the combination of Perphenazine and Ritodrine. Preterm labour/delivery [JB00] [104]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Degarelix. Prostate cancer [2C82] [94]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Enzalutamide. Prostate cancer [2C82] [94]
Bicalutamide DMZMSPF Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Bicalutamide. Prostate cancer [2C82] [94]
Terazosin DM3JCVS Moderate Additive hypotensive effects by the combination of Perphenazine and Terazosin. Prostate hyperplasia [GA90] [100]
Silodosin DMJSBT6 Moderate Additive hypotensive effects by the combination of Perphenazine and Silodosin. Prostate hyperplasia [GA90] [100]
Levomepromazine DMIKFEL Moderate Additive anticholinergic effects by the combination of Perphenazine and Levomepromazine. Psychotic disorder [6A20-6A25] [92]
Gatifloxacin DMSL679 Major Increased risk of prolong QT interval by the combination of Perphenazine and Gatifloxacin. Respiratory infection [CA07-CA4Z] [145]
Neupro DMHEAB1 Moderate Additive hypotensive effects by the combination of Perphenazine and Neupro. Restless legs syndrome [7A80] [141]
Vardenafil DMTBGW8 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Vardenafil. Sexual dysfunction [HA00-HA01] [91]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Perphenazine and LEE011. Solid tumour/cancer [2A00-2F9Z] [91]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Perphenazine and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [91]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [94]
Doxorubicin DMVP5YE Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [91]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Pitolisant. Somnolence [MG42] [91]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Lenvatinib. Thyroid cancer [2D10] [91]
Papaverine DMCA9QP Moderate Additive hypotensive effects by the combination of Perphenazine and Papaverine. Tonus and reflex abnormality [MB47] [100]
Tacrolimus DMZ7XNQ Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Tacrolimus. Transplant rejection [NE84] [91]
Methdilazine DMAUHQX Moderate Additive anticholinergic effects by the combination of Perphenazine and Methdilazine. Vasomotor/allergic rhinitis [CA08] [92]
Trimeprazine DMEMV9D Moderate Additive anticholinergic effects by the combination of Perphenazine and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [97]
Acrivastine DMTIGA0 Moderate Additive anticholinergic effects by the combination of Perphenazine and Acrivastine. Vasomotor/allergic rhinitis [CA08] [92]
Procainamide DMNMXR8 Major Increased risk of prolong QT interval by the combination of Perphenazine and Procainamide. Ventricular tachyarrhythmia [BC71] [91]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Propafenone. Ventricular tachyarrhythmia [BC71] [91]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Perphenazine and Flecainide. Ventricular tachyarrhythmia [BC71] [91]
Amiodarone DMUTEX3 Major Increased risk of prolong QT interval by the combination of Perphenazine and Amiodarone. Ventricular tachyarrhythmia [BC71] [91]
⏷ Show the Full List of 193 DDI Information of This Drug

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

DIG
DIG Name DIG ID PubChem CID Functional Classification
Calcium carbonate E00198 10112 Binding agent; Buffering agent; Diluent; Opacifying agent
Isopropyl alcohol E00070 3776 Antimicrobial preservative; Solvent
Sodium benzoate E00432 517055 Antimicrobial preservative; lubricant
Acetone E00004 180 Solvent
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Saccharose E00091 5988 Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
⏷ Show the Full List of 16 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Perphenazine 2 mg tablet 2 mg Oral Tablet Oral
Perphenazine 8 mg tablet 8 mg Oral Tablet Oral
Perphenazine 16 mg tablet 16 mg Oral Tablet Oral
Perphenazine 4 mg tablet 4 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 209).
2 Methamphetamine Addiction and Abuse - Perphenazine.
3 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.
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
6 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
7 A cross-validation study on the relationship between central D2 receptor occupancy and serum perphenazine concentration. Psychopharmacology (Berl). 2004 Sep;175(2):148-53.
8 Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J Med Chem. 2013 Sep 26;56(18):7232-42.
9 Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates. J Pharm Pharmacol. 2004 Aug;56(8):967-75.
10 Identification of the human cytochrome P450 isoforms mediating in vitro N-dealkylation of perphenazine. Br J Clin Pharmacol. 2000 Dec;50(6):563-71.
11 Use of antidepressant drugs in schizophrenic patients with depression. Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9.
12 Effect of antipsychotic drugs on human liver cytochrome P-450 (CYP) isoforms in vitro: preferential inhibition of CYP2D6. Drug Metab Dispos. 1999 Sep;27(9):1078-84.
13 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.
14 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
15 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.
16 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
17 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.
18 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.
19 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
20 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.
21 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.
22 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
23 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
24 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
25 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
26 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
27 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
28 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
29 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
30 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
31 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
32 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.
33 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
34 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.
35 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
36 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
37 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
38 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
39 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
40 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
41 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
42 Identification of human cytochrome P450s involved in the formation of all-trans-retinoic acid principal metabolites. Mol Pharmacol. 2000 Dec;58(6):1341-8.
43 Targeted antipeptide antibodies to cytochrome P450 2C18 based on epitope mapping of an inhibitory monoclonal antibody to P450 2C51. Arch Biochem Biophys. 1997 Feb 15;338(2):157-64.
44 Involvement of cytochrome P450 3A4 enzyme in the N-demethylation of methadone in human liver microsomes. Chem Res Toxicol. 1996 Mar;9(2):365-73.
45 CYP2C8/9 mediate dapsone N-hydroxylation at clinical concentrations of dapsone. Drug Metab Dispos. 2000 Aug;28(8):865-8.
46 Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metab Dispos. 2001 Mar;29(3):242-51.
47 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
48 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
49 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
50 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
51 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
52 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.
53 Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
54 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.
55 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
56 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
57 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.
58 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
59 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
60 High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8.
61 Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91.
62 CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6.
63 Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21.
64 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
65 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
66 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
67 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.
68 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
69 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
70 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
71 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.
72 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
73 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
74 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
75 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
76 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
77 Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma
78 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
79 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
80 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
81 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
82 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
83 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
84 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
85 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: 3639).
86 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
87 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
88 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
89 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
90 Randomized clinical comparison of perospirone and risperidone in patients with schizophrenia: Kansai Psychiatric Multicenter Study. Psychiatry Clin Neurosci. 2009 Jun;63(3):322-8.
91 Canadian Pharmacists Association.
92 Cohen MA, Alfonso CA, Mosquera M. Development of urinary retention during treatment with clozapine and meclizine [published correction appears in Am J Psychiatry 1994 Jun;151(6):952]. Am J Psychiatry. 1994;151(4):619-620. [PMID: 8147469]
93 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
94 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
95 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
96 US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
97 Kulik AV, Wilbur R "Delirium and stereotypy from anticholinergic antiparkinson drugs." Prog Neuropsychopharmacol Biol Psychiatry 6 (1982): 75-82. [PMID: 7202232]
98 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]
99 Cerner Multum, Inc. "Australian Product Information.".
100 Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
101 Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.
102 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
103 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
104 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
105 Achor MB, Extein I "Diet aids, mania, and affective illness" Am J Psychiatry 138 (1981): 392. [PMID: 7468847]
106 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
107 Multum Information Services, Inc. Expert Review Panel.
108 Cole JM, Sheehan AH, Jordan JK "Concomitant use of ipratropium and tiotropium in chronic obstructive plmonary disease." Ann Pharmacother 46 (2012): 1717-21. [PMID: 23170031]
109 US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
110 Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
111 Bock JL, Nelson JC, Gray S, Jatlow PI "Desipramine hydroxylation: variability and effect of antipsychotic drugs." Clin Pharmacol Ther 33 (1983): 322-8. [PMID: 6130865]
112 Lee BS "Possibility of hyperpyrexia with antipsychotic and anticholinergic drugs." J Clin Psychiatry 47 (1986): 571. [PMID: 3771507]
113 Burke RE, Fahn S, Mayeux R, Weinberg H, Louis K, Willner JH "Neuroleptic malignant syndrome caused by dopamine-depleting drugs in a patient with Huntington disease." Neurology 31 (1981): 1022-5. [PMID: 6115336]
114 Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
115 Product Information. Zonegran (zonisamide) Elan Pharmaceuticals, S. San Francisco, CA.
116 Hvizdos AJ, Bennett JA, Wells BG, Rappaport KB, Mendel SA "Anticholinergic psychosis in a patient receiving usual doses of haloperidol." Clin Pharm 2 (1983): 174-8. [PMID: 6883947]
117 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
118 AbdelRahman SM, Gotschall RR, Kauffman RE, Leeder JS, Kearns GL "Investigation of terbinafine as a CYP2D6 inhibitor in vivo." Clin Pharmacol Ther 65 (1999): 465-72. [PMID: 10340911]
119 Product Information. Stribild (cobicistat/elvitegravir/emtricitabine/tenofov). Gilead Sciences, Foster City, CA.
120 Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475]
121 Postma JU, van Tilburg W "Visual hallucinations and delirium during treatment with amantadine (Symmetrel)." J Am Geriatr Soc 23 (1975): 212-5. [PMID: 123540]
122 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
123 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
124 Product Information. Vizimpro (dacomitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
125 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
126 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
127 Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
128 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]
129 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
130 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
131 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
132 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
133 Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ.
134 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
135 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
136 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
137 Bateman DN, Rawlins MD, Simpson JM "Extrapyramidal reactions with metoclopramide." Br Med J (Clin Res Ed) 291 (1985): 930-2. [PMID: 3929968]
138 Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
139 Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
140 Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200]
141 Mims RB, Scott CL, Modebe O, Bethune JE "Inhibition of L-dopa-induced growth hormone stimulation by pyridoxine and chlorpromazine." J Clin Endocrinol Metab 40 (1975): 256-9. [PMID: 1117978]
142 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
143 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
144 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
145 Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]