Details of the Drug

General Information of Drug (ID: DMBHMOX)

Drug Name
Palonosetron
Synonyms Aloxi; Onicit; Palonosetron [INN]; Aloxi (TN); RS 25233-197; RS 25259-197; RS-25233-197; RS-25259-197; (S-(R*,R*))-2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one
Indication
Disease Entry ICD 11 Status REF
Nausea MD90 Approved [1], [2]
Therapeutic Class
Antiemetics
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 296.4
Topological Polar Surface Area (xlogp) 2.8
Rotatable Bond Count (rotbonds) 1
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [3]
Bioavailability
The bioavailability of drug is poor [4]
Clearance
The clearance of drug is 160 +/- 35 mL/h/kg [5]
Elimination
40% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 40 hours [6]
Metabolism
The drug is metabolized via the hepatic [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.01205 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.38% [6]
Vd
The volume of distribution (Vd) of drug is 8.3 +/- 2.5 L/kg [5]
Chemical Identifiers
Formula
C19H24N2O
IUPAC Name
(3aS)-2-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3a,4,5,6-tetrahydro-3H-benzo[de]isoquinolin-1-one
Canonical SMILES
C1C[C@@H]2CN(C(=O)C3=CC=CC(=C23)C1)[C@@H]4CN5CCC4CC5
InChI
InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1
InChIKey
CPZBLNMUGSZIPR-NVXWUHKLSA-N
Cross-matching ID
PubChem CID
6337614
ChEBI ID
CHEBI:85161
CAS Number
135729-61-2
DrugBank ID
DB00377
TTD ID
D04FVU
VARIDT ID
DR00394
INTEDE ID
DR1232
ACDINA ID
D00506

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Antagonist [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [9]
Cytochrome P450 2D6 (CYP2D6)
Main DME 		DECB0K3 CP2D6_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 Nausea
ICD Disease Classification MD90
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
5-HT 3A receptor (HTR3A) DTT HTR3A 6.60E-01 1.08E-02 0.04
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.20E-01 -1.63E-03 -1.13E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.40E-01 -2.17E-02 -4.03E-02
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 Palonosetron
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Droperidol DM0DXA8 Major Increased risk of prolong QT interval by the combination of Palonosetron and Droperidol. Nausea/vomiting [MD90] [37]
Prochlorperazine DM53SRA Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Prochlorperazine. Nausea/vomiting [MD90] [37]
Promethazine DM6I5GR Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Promethazine. Nausea/vomiting [MD90] [37]
Dolasetron DMMG26Z Major Increased risk of prolong QT interval by the combination of Palonosetron and Dolasetron. Nausea/vomiting [MD90] [37]
Ondansetron DMOTQ1I Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Ondansetron. Nausea/vomiting [MD90] [37]
Coadministration of a Drug Treating the Disease Different from Palonosetron (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Methylene blue DMJAPE7 Major Additive serotonergic effects by the combination of Palonosetron and Methylene blue. Acquired methaemoglobinaemia [3A93] [37]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Palonosetron and Ivosidenib. Acute myeloid leukaemia [2A60] [38]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Midostaurin. Acute myeloid leukaemia [2A60] [37]
Idarubicin DMM0XGL Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Idarubicin. Acute myeloid leukaemia [2A60] [37]
Daunorubicin DMQUSBT Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Daunorubicin. Acute myeloid leukaemia [2A60] [37]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Arn-509. Acute myeloid leukaemia [2A60] [39]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Gilteritinib. Acute myeloid leukaemia [2A60] [40]
Oliceridine DM6MDCF Major Additive serotonergic effects by the combination of Palonosetron and Oliceridine. Acute pain [MG31] [37]
Tacrine DM51FY6 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Tacrine. Alzheimer disease [8A20] [37]
Galantamine DMEO794 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Galantamine. Alzheimer disease [8A20] [37]
Rivastigmine DMG629M Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Rivastigmine. Alzheimer disease [8A20] [37]
Metronidazole DMTIVEN Minor Increased risk of prolong QT interval by the combination of Palonosetron and Metronidazole. Amoebiasis [1A36] [41]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Palonosetron and Ivabradine. Angina pectoris [BA40] [39]
Bepridil DM0RKS4 Major Increased risk of prolong QT interval by the combination of Palonosetron and Bepridil. Angina pectoris [BA40] [37]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Palonosetron and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [42]
Promazine DMZAL7W Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Promazine. Appearance/behaviour symptom [MB23] [37]
Cilostazol DMZMSCT Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Cilostazol. Arterial occlusive disease [BD40] [37]
Voriconazole DMAOL2S Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Voriconazole. Aspergillosis [1F20] [37]
Posaconazole DMUL5EW Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Posaconazole. Aspergillosis [1F20] [37]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Levalbuterol. Asthma [CA23] [43]
Terbutaline DMD4381 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Terbutaline. Asthma [CA23] [44]
Pirbuterol DMI5678 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Pirbuterol. Asthma [CA23] [44]
Salbutamol DMN9CWF Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Salbutamol. Asthma [CA23] [43]
Formoterol DMSOURV Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Formoterol. Asthma [CA23] [44]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [39]
Desipramine DMT2FDC Major Increased risk of prolong QT interval by the combination of Palonosetron and Desipramine. Attention deficit hyperactivity disorder [6A05] [37]
Ofloxacin DM0VQN3 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Ofloxacin. Bacterial infection [1A00-1C4Z] [45]
Ciprofloxacin XR DM2NLS9 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Ciprofloxacin XR. Bacterial infection [1A00-1C4Z] [37]
Clarithromycin DM4M1SG Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Clarithromycin. Bacterial infection [1A00-1C4Z] [37]
Sulfamethoxazole DMB08GE Minor Increased risk of prolong QT interval by the combination of Palonosetron and Sulfamethoxazole. Bacterial infection [1A00-1C4Z] [37]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Palonosetron and Sparfloxacin. Bacterial infection [1A00-1C4Z] [45]
Linezolid DMGFPU2 Major Additive serotonergic effects by the combination of Palonosetron and Linezolid. Bacterial infection [1A00-1C4Z] [37]
Gemifloxacin DMHT34O Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Gemifloxacin. Bacterial infection [1A00-1C4Z] [45]
Norfloxacin DMIZ6W2 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Norfloxacin. Bacterial infection [1A00-1C4Z] [45]
Levofloxacin DMS60RB Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Levofloxacin. Bacterial infection [1A00-1C4Z] [45]
Lomefloxacin DMVRH9C Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Lomefloxacin. Bacterial infection [1A00-1C4Z] [37]
Telithromycin DMZ4P3A Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Telithromycin. Bacterial infection [1A00-1C4Z] [37]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Retigabine. Behcet disease [4A62] [37]
Loperamide DMOJZQ9 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Loperamide. Bowel habit change [ME05] [46]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Eribulin. Breast cancer [2C60-2C6Y] [37]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Lapatinib. Breast cancer [2C60-2C6Y] [37]
Tamoxifen DMLB0EZ Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Tamoxifen. Breast cancer [2C60-2C6Y] [37]
Toremifene DMQYUWG Major Increased risk of prolong QT interval by the combination of Palonosetron and Toremifene. Breast cancer [2C60-2C6Y] [37]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Bosutinib. Breast cancer [2C60-2C6Y] [39]
Sotalol DML60TN Major Increased risk of prolong QT interval by the combination of Palonosetron and Sotalol. Cardiac arrhythmia [BC9Z] [37]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [47]
Olodaterol DM62B78 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Olodaterol. Chronic obstructive pulmonary disease [CA22] [44]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Vilanterol. Chronic obstructive pulmonary disease [CA22] [43]
Salmeterol DMIEU69 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Salmeterol. Chronic obstructive pulmonary disease [CA22] [44]
Indacaterol DMQJHR7 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Indacaterol. Chronic obstructive pulmonary disease [CA22] [44]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Arformoterol. Chronic obstructive pulmonary disease [CA22] [44]
Dihydrocodeine DMB0FWL Moderate Additive serotonergic effects by the combination of Palonosetron and Dihydrocodeine. Chronic pain [MG30] [48]
Levomilnacipran DMV26S8 Major Additive serotonergic effects by the combination of Palonosetron and Levomilnacipran. Chronic pain [MG30] [37]
Oxaliplatin DMQNWRD Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Oxaliplatin. Colorectal cancer [2B91] [37]
Isoproterenol DMK7MEY Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Isoproterenol. Conduction disorder [BC63] [43]
Halothane DM80OZ5 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Halothane. Corneal disease [9A76-9A78] [37]
Propofol DMB4OLE Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Propofol. Corneal disease [9A76-9A78] [49]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Sevoflurane. Corneal disease [9A76-9A78] [37]
Alfentanil DMVO0UB Major Additive serotonergic effects by the combination of Palonosetron and Alfentanil. Corneal disease [9A76-9A78] [37]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Probucol. Coronary atherosclerosis [BA80] [37]
Dextromethorphan DMUDJZM Major Additive serotonergic effects by the combination of Palonosetron and Dextromethorphan. Cough [MD12] [37]
Clofazimine DMEBOFW Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Clofazimine. Crohn disease [DD70] [50]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Palonosetron and Pasireotide. Cushing syndrome [5A70] [37]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Osilodrostat. Cushing syndrome [5A70] [39]
Trimipramine DM1SC8M Major Increased risk of prolong QT interval by the combination of Palonosetron and Trimipramine. Depression [6A70-6A7Z] [37]
Imipramine DM2NUH3 Major Increased risk of prolong QT interval by the combination of Palonosetron and Imipramine. Depression [6A70-6A7Z] [37]
Nortriptyline DM4KDYJ Major Increased risk of prolong QT interval by the combination of Palonosetron and Nortriptyline. Depression [6A70-6A7Z] [37]
Nefazodone DM4ZS8M Major Additive serotonergic effects by the combination of Palonosetron and Nefazodone. Depression [6A70-6A7Z] [37]
Paroxetine DM5PVQE Major Increased risk of prolong QT interval by the combination of Palonosetron and Paroxetine. Depression [6A70-6A7Z] [37]
Vortioxetine DM6F1PU Major Additive serotonergic effects by the combination of Palonosetron and Vortioxetine. Depression [6A70-6A7Z] [37]
Duloxetine DM9BI7M Major Additive serotonergic effects by the combination of Palonosetron and Duloxetine. Depression [6A70-6A7Z] [37]
Isocarboxazid DMAF1NB Major Additive serotonergic effects by the combination of Palonosetron and Isocarboxazid. Depression [6A70-6A7Z] [37]
Milnacipran DMBFE74 Major Additive serotonergic effects by the combination of Palonosetron and Milnacipran. Depression [6A70-6A7Z] [37]
Escitalopram DMFK9HG Major Increased risk of prolong QT interval by the combination of Palonosetron and Escitalopram. Depression [6A70-6A7Z] [37]
Tranylcypromine DMGB5RE Major Additive serotonergic effects by the combination of Palonosetron and Tranylcypromine. Depression [6A70-6A7Z] [37]
Desvenlafaxine DMHD4PE Major Additive serotonergic effects by the combination of Palonosetron and Desvenlafaxine. Depression [6A70-6A7Z] [37]
Phenelzine DMHIDUE Major Additive serotonergic effects by the combination of Palonosetron and Phenelzine. Depression [6A70-6A7Z] [37]
Clomipramine DMINRKW Major Increased risk of prolong QT interval by the combination of Palonosetron and Clomipramine. Depression [6A70-6A7Z] [37]
Trazodone DMK1GBJ Major Increased risk of prolong QT interval by the combination of Palonosetron and Trazodone. Depression [6A70-6A7Z] [37]
Amoxapine DMKITQE Major Additive serotonergic effects by the combination of Palonosetron and Amoxapine. Depression [6A70-6A7Z] [37]
Doxepin DMPI98T Major Additive serotonergic effects by the combination of Palonosetron and Doxepin. Depression [6A70-6A7Z] [41]
Maprotiline DMPWB7T Major Increased risk of prolong QT interval by the combination of Palonosetron and Maprotiline. Depression [6A70-6A7Z] [37]
5-hydroxy-L-tryptophan DMDWZGJ Major Additive serotonergic effects by the combination of Palonosetron and 5-hydroxy-L-tryptophan. Discovery agent [N.A.] [41]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [37]
Ingrezza DMVPLNC Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Ingrezza. Dystonic disorder [8A02] [51]
Stiripentol DMMSDOY Moderate Decreased metabolism of Palonosetron caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [52]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Solifenacin. Functional bladder disorder [GC50] [37]
Pentamidine DMHZJCG Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Pentamidine. Fungal infection [1F29-1F2F] [37]
Ketoconazole DMPZI3Q Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Ketoconazole. Fungal infection [1F29-1F2F] [37]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Sunitinib. Gastrointestinal stromal tumour [2B5B] [37]
Procarbazine DMIK367 Major Additive serotonergic effects by the combination of Palonosetron and Procarbazine. Hodgkin lymphoma [2B30] [37]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [53]
Efavirenz DMC0GSJ Major Increased risk of prolong QT interval by the combination of Palonosetron and Efavirenz. Human immunodeficiency virus disease [1C60-1C62] [54]
Saquinavir DMG814N Major Increased risk of prolong QT interval by the combination of Palonosetron and Saquinavir. Human immunodeficiency virus disease [1C60-1C62] [55]
Lopinavir DMITQS0 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Lopinavir. Human immunodeficiency virus disease [1C60-1C62] [37]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [37]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Polyethylene glycol. Irritable bowel syndrome [DD91] [39]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Phenolphthalein. Irritable bowel syndrome [DD91] [37]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Palonosetron and Crizotinib. Lung cancer [2C25] [56]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Palonosetron and Ceritinib. Lung cancer [2C25] [37]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Palonosetron and Osimertinib. Lung cancer [2C25] [57]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Palonosetron and Selpercatinib. Lung cancer [2C25] [39]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Palonosetron and Lumefantrine. Malaria [1F40-1F45] [41]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Palonosetron and Halofantrine. Malaria [1F40-1F45] [58]
Chloroquine DMSI5CB Major Increased risk of prolong QT interval by the combination of Palonosetron and Chloroquine. Malaria [1F40-1F45] [59]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Palonosetron and Hydroxychloroquine. Malaria [1F40-1F45] [59]
Quinine DMSWYF5 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Quinine. Malaria [1F40-1F45] [37]
Primaquine DMWQ16I Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Primaquine. Malaria [1F40-1F45] [37]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [39]
Arsenic trioxide DM61TA4 Major Increased risk of prolong QT interval by the combination of Palonosetron and Arsenic trioxide. Mature B-cell lymphoma [2A85] [60]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Palonosetron and Vemurafenib. Melanoma [2C30] [37]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and LGX818. Melanoma [2C30] [61]
Almogran DM7I64Z Major Additive serotonergic effects by the combination of Palonosetron and Almogran. Migraine [8A80] [37]
Frovatriptan DM7RE8P Major Additive serotonergic effects by the combination of Palonosetron and Frovatriptan. Migraine [8A80] [37]
Rizatriptan DMDJMA3 Major Additive serotonergic effects by the combination of Palonosetron and Rizatriptan. Migraine [8A80] [37]
Naratriptan DMO50U2 Major Additive serotonergic effects by the combination of Palonosetron and Naratriptan. Migraine [8A80] [37]
Sumatriptan DMVYXR8 Major Additive serotonergic effects by the combination of Palonosetron and Sumatriptan. Migraine [8A80] [37]
Lasmiditan DMXLVDT Major Additive serotonergic effects by the combination of Palonosetron and Lasmiditan. Migraine [8A80] [37]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Palonosetron and Panobinostat. Multiple myeloma [2A83] [62]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Thalidomide. Multiple myeloma [2A83] [41]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Palonosetron and Siponimod. Multiple sclerosis [8A40] [41]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Palonosetron and Fingolimod. Multiple sclerosis [8A40] [37]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Romidepsin. Mycosis fungoides [2B01] [37]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Palonosetron and Nilotinib. Myeloproliferative neoplasm [2A20] [37]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Dasatinib. Myeloproliferative neoplasm [2A20] [63]
Bupropion DM5PCS7 Major Additive serotonergic effects by the combination of Palonosetron and Bupropion. Nicotine use disorder [6C4A] [37]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Entrectinib. Non-small cell lung cancer [2C25] [41]
Sibutramine DMFJTDI Major Additive serotonergic effects by the combination of Palonosetron and Sibutramine. Obesity [5B80-5B81] [37]
Dexfenfluramine DMJ7YDS Major Additive serotonergic effects by the combination of Palonosetron and Dexfenfluramine. Obesity [5B80-5B81] [37]
Levomethadyl Acetate DM06HG5 Major Increased risk of prolong QT interval by the combination of Palonosetron and Levomethadyl Acetate. Opioid use disorder [6C43] [39]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Palonosetron and Lofexidine. Opioid use disorder [6C43] [37]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Rucaparib. Ovarian cancer [2C73] [37]
Pentazocine DM1XBHS Major Additive serotonergic effects by the combination of Palonosetron and Pentazocine. Pain [MG30-MG3Z] [37]
Dextropropoxyphene DM23HCX Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Dextropropoxyphene. Pain [MG30-MG3Z] [64]
Butorphanol DM5KYPJ Moderate Additive serotonergic effects by the combination of Palonosetron and Butorphanol. Pain [MG30-MG3Z] [48]
Oxymorphone DM65AGJ Moderate Additive serotonergic effects by the combination of Palonosetron and Oxymorphone. Pain [MG30-MG3Z] [48]
Levorphanol DMGS80V Moderate Additive serotonergic effects by the combination of Palonosetron and Levorphanol. Pain [MG30-MG3Z] [48]
Dezocine DMJDB0Y Moderate Additive serotonergic effects by the combination of Palonosetron and Dezocine. Pain [MG30-MG3Z] [48]
Nalbuphine DMOSQGU Moderate Additive serotonergic effects by the combination of Palonosetron and Nalbuphine. Pain [MG30-MG3Z] [48]
Buprenorphine DMPRI8G Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Buprenorphine. Pain [MG30-MG3Z] [37]
Hydrocodone DMQ2JO5 Moderate Additive serotonergic effects by the combination of Palonosetron and Hydrocodone. Pain [MG30-MG3Z] [48]
Meperidine DMX4GND Major Additive serotonergic effects by the combination of Palonosetron and Meperidine. Pain [MG30-MG3Z] [37]
Oxycodone DMXLKHV Moderate Additive serotonergic effects by the combination of Palonosetron and Oxycodone. Pain [MG30-MG3Z] [48]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Triclabendazole. Parasitic worm infestation [1F90] [37]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Pimavanserin. Parkinsonism [8A00] [65]
Famotidine DMRL3AB Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Famotidine. Peptic ulcer [DA61] [41]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Palonosetron and Macimorelin. Pituitary gland disorder [5A60-5A61] [66]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Palonosetron and Lefamulin. Pneumonia [CA40] [67]
Ritodrine DM4V6RL Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Ritodrine. Preterm labour/delivery [JB00] [44]
ABIRATERONE DM8V75C Moderate Increased risk of prolong QT interval by the combination of Palonosetron and ABIRATERONE. Prostate cancer [2C82] [39]
Nilutamide DMFN07X Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Nilutamide. Prostate cancer [2C82] [39]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Enzalutamide. Prostate cancer [2C82] [39]
Flutamide DMK0O7U Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Flutamide. Prostate cancer [2C82] [39]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Relugolix. Prostate cancer [2C82] [39]
Bicalutamide DMZMSPF Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Bicalutamide. Prostate cancer [2C82] [39]
Levomepromazine DMIKFEL Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Levomepromazine. Psychotic disorder [6A20-6A25] [37]
Fluphenazine DMIT8LX Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Fluphenazine. Psychotic disorder [6A20-6A25] [37]
Triflupromazine DMKFQJP Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Triflupromazine. Psychotic disorder [6A20-6A25] [37]
Sorafenib DMS8IFC Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Sorafenib. Renal cell carcinoma [2C90] [37]
Gatifloxacin DMSL679 Major Increased risk of prolong QT interval by the combination of Palonosetron and Gatifloxacin. Respiratory infection [CA07-CA4Z] [68]
Quetiapine DM1N62C Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Quetiapine. Schizophrenia [6A20] [37]
Mesoridazine DM2ZGAN Major Increased risk of prolong QT interval by the combination of Palonosetron and Mesoridazine. Schizophrenia [6A20] [37]
Thioridazine DM35M8J Major Increased risk of prolong QT interval by the combination of Palonosetron and Thioridazine. Schizophrenia [6A20] [37]
Aripiprazole DM3NUMH Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Aripiprazole. Schizophrenia [6A20] [41]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Palonosetron and Iloperidone. Schizophrenia [6A20] [37]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Paliperidone. Schizophrenia [6A20] [37]
Haloperidol DM96SE0 Major Increased risk of prolong QT interval by the combination of Palonosetron and Haloperidol. Schizophrenia [6A20] [37]
Perphenazine DMA4MRX Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Perphenazine. Schizophrenia [6A20] [37]
Chlorpromazine DMBGZI3 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Chlorpromazine. Schizophrenia [6A20] [37]
Trifluoperazine DMKBYWI Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Trifluoperazine. Schizophrenia [6A20] [37]
Risperidone DMN6DXL Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Risperidone. Schizophrenia [6A20] [37]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Palonosetron and Amisulpride. Schizophrenia [6A20] [69]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Asenapine. Schizophrenia [6A20] [37]
Pimozide DMW83TP Major Increased risk of prolong QT interval by the combination of Palonosetron and Pimozide. Schizophrenia [6A20] [39]
Fentanyl DM8WAHT Major Additive serotonergic effects by the combination of Palonosetron and Fentanyl. Sensation disturbance [MB40] [37]
Sufentanil DMU7YEL Major Additive serotonergic effects by the combination of Palonosetron and Sufentanil. Sensation disturbance [MB40] [37]
Vardenafil DMTBGW8 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Vardenafil. Sexual dysfunction [HA00-HA01] [37]
Epirubicin DMPDW6T Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Epirubicin. Solid tumour/cancer [2A00-2F9Z] [37]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Palonosetron and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [37]
Doxorubicin DMVP5YE Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [37]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Pitolisant. Somnolence [MG42] [37]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [37]
Adenosine DMM2NSK Moderate Increased risk of ventricular arrhythmias by the combination of Palonosetron and Adenosine. Supraventricular tachyarrhythmia [BC81] [37]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Lenvatinib. Thyroid cancer [2D10] [37]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Palonosetron and Cabozantinib. Thyroid cancer [2D10] [39]
Papaverine DMCA9QP Major Increased risk of prolong QT interval by the combination of Palonosetron and Papaverine. Tonus and reflex abnormality [MB47] [70]
Tizanidine DMR2IQ4 Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Tizanidine. Tonus and reflex abnormality [MB47] [37]
Tacrolimus DMZ7XNQ Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Tacrolimus. Transplant rejection [NE84] [37]
Astemizole DM2HN6Q Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Astemizole. Vasomotor/allergic rhinitis [CA08] [37]
Trimeprazine DMEMV9D Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [64]
Procainamide DMNMXR8 Major Increased risk of prolong QT interval by the combination of Palonosetron and Procainamide. Ventricular tachyarrhythmia [BC71] [37]
Propafenone DMPIBJK Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Propafenone. Ventricular tachyarrhythmia [BC71] [37]
Flecainide DMSQDLE Moderate Increased risk of prolong QT interval by the combination of Palonosetron and Flecainide. Ventricular tachyarrhythmia [BC71] [37]
Amiodarone DMUTEX3 Major Increased risk of prolong QT interval by the combination of Palonosetron and Amiodarone. Ventricular tachyarrhythmia [BC71] [37]
⏷ Show the Full List of 194 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
Butylhydroxyanisole E00308 24667 Antimicrobial preservative; Antioxidant
Glycerin E00026 753 Antimicrobial preservative; Emollient; Flavoring agent; Humectant; Lubricant; Plasticizing agent; Solvent; Suppository base; Tonicity agent; Viscosity-controlling agent
Water E00035 962 Solvent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Palonosetron 0.5 mg capsule 0.5 mg Oral Capsule 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: 7486).
2 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
3 BDDCS applied to over 900 drugs
4 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.
5 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
6 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
7 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
8 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
9 Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37.
10 Cytochrome P450 2D6 metabolism and 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting. Med Sci Monit. 2005 Oct;11(10):RA322-8.
11 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.
12 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
13 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.
14 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
15 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.
16 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.
17 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
18 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.
19 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.
20 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
21 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.
22 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
23 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.
24 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
25 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
26 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
27 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
28 Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, do... Lancet Oncol. 2009 Feb;10(2):115-24.
29 Efficacy of 5-HT3 antagonists and 5-HT4 agonists in irritable bowel syndrome: systematic review and meta-analysis. Am J Gastroenterol. 2009 Jul;104(7):1831-43; quiz 1844.
30 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
31 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
32 Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors. Reg Anesth Pain Med. 2007 Nov-Dec;32(6):462-70.
33 Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
34 Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9.
35 mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83.
36 Effect of serotonin (5-HT)3-receptor antagonists YM060, YM114 (KAE-393), ondansetron and granisetron on 5-HT4 receptors and gastric emptying in rodents. Jpn J Pharmacol. 1995 Nov;69(3):205-14.
37 Canadian Pharmacists Association.
38 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
39 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
40 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
41 Cerner Multum, Inc. "Australian Product Information.".
42 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
43 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
44 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
45 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
46 Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747]
47 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
48 Vizcaychipi MP, Walker S, Palazzo M "Serotonin syndrome triggered by tramadol." Br J Anaesth 99 (2007): 919. [PMID: 18006535]
49 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]
50 Product Information. Lamprene (clofazimine). Novartis Pharmaceuticals, East Hanover, NJ.
51 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
52 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
53 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
54 Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE.
55 Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475]
56 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
57 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
58 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]
59 Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
60 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]
61 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
62 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
63 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
64 Iannini PB "Cardiotoxicity of macrolides, ketolides and fluoroquinolones that prolong the QTc interval." Expert Opin Drug Saf 1 (2002): 121-8. [PMID: 12904146]
65 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
66 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
67 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
68 Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]
69 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
70 Goto M, Sato M, Kitzazawa H, et.al "Papaverine-induced QT interval prolongation and ventricular fibrillation in a patient with a history of drug-induced QT prolongation." Intern Med 53 (2014): 1629-31. [PMID: 25088875]