General Information of Drug (ID: DM7NPJS)

Drug Name
Paliperidone
Synonyms
Xeplion; Invega Sustenna; Paliperidone palmitate; JNS-010; Paliperidone (depot injection, NanoCrystal); Paliperidone (injectable, NanoCrystal), Elan; Paliperidone (depot injection, NanoCrystal), Johnson & Johnson
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Approved [1], [2], [3]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 426.5
Topological Polar Surface Area (xlogp) 2.2
Rotatable Bond Count (rotbonds) 4
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 4: low solubility and low permeability [4]
Bioavailability
The bioavailability of drug is 28% [5]
Clearance
The drug present in the plasma can be removed from the body at the rate of 1.18 mL/min/kg [6]
Elimination
59% of drug is excreted from urine in the unchanged form [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 23 hours [6]
Metabolism
The drug is not metabolised [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.24% [6]
Vd
The volume of distribution (Vd) of drug is 487 L [7]
Water Solubility
The ability of drug to dissolve in water is measured as 0.01125 mg/mL [4]
Chemical Identifiers
Formula
C23H27FN4O3
IUPAC Name
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
Canonical SMILES
CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
InChI
InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3
InChIKey
PMXMIIMHBWHSKN-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
115237
ChEBI ID
CHEBI:83804
CAS Number
144598-75-4
DrugBank ID
DB01267
TTD ID
D0B3UJ
VARIDT ID
DR00159
INTEDE ID
DR1230
ACDINA ID
D00505

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT receptor (5HTR) TT85JO3 NOUNIPROTAC Antagonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [9]
Cytochrome P450 2D6 (CYP2D6)
Main DME
DECB0K3 CP2D6_HUMAN Substrate [10]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [11]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Paliperidone
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Paliperidone and Iloperidone. Schizophrenia [6A20] [50]
Molindone DMAH70G Moderate Additive anticholinergic effects by the combination of Paliperidone and Molindone. Schizophrenia [6A20] [51]
Thiothixene DMDINC4 Moderate Additive anticholinergic effects by the combination of Paliperidone and Thiothixene. Schizophrenia [6A20] [51]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Paliperidone and Amisulpride. Schizophrenia [6A20] [52]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Asenapine. Schizophrenia [6A20] [50]
Coadministration of a Drug Treating the Disease Different from Paliperidone (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Paliperidone and Ivosidenib. Acute myeloid leukaemia [2A60] [53]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Midostaurin. Acute myeloid leukaemia [2A60] [50]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Arn-509. Acute myeloid leukaemia [2A60] [54]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Gilteritinib. Acute myeloid leukaemia [2A60] [55]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Paliperidone and Oliceridine. Acute pain [MG31] [56]
Mepyramine DMB4SFH Moderate Additive anticholinergic effects by the combination of Paliperidone and Mepyramine. Allergic/hypersensitivity disorder [4A80-4A8Z] [57]
Phenyltoloxamine DMKAEQW Moderate Additive anticholinergic effects by the combination of Paliperidone and Phenyltoloxamine. Allergic/hypersensitivity disorder [4A80-4A8Z] [57]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Paliperidone and Ivabradine. Angina pectoris [BA40] [54]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Paliperidone and Dronedarone. Angina pectoris [BA40] [50]
Amyl nitrite DMJKO05 Moderate Additive hypotensive effects by the combination of Paliperidone and Amyl nitrite. Angina pectoris [BA40] [58]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Paliperidone and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [59]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Paliperidone and Levalbuterol. Asthma [CA23] [60]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Pirbuterol. Asthma [CA23] [61]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Retigabine. Behcet disease [4A62] [50]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Eribulin. Breast cancer [2C60-2C6Y] [50]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [62]
Olodaterol DM62B78 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Olodaterol. Chronic obstructive pulmonary disease [CA22] [61]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Paliperidone and Vilanterol. Chronic obstructive pulmonary disease [CA22] [60]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Indacaterol. Chronic obstructive pulmonary disease [CA22] [61]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Paliperidone and Arformoterol. Chronic obstructive pulmonary disease [CA22] [61]
Dihydrocodeine DMB0FWL Major Additive CNS depression effects by the combination of Paliperidone and Dihydrocodeine. Chronic pain [MG30] [63]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Probucol. Coronary atherosclerosis [BA80] [50]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Paliperidone and Pasireotide. Cushing syndrome [5A70] [50]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Osilodrostat. Cushing syndrome [5A70] [54]
Cyclandelate DMO0R76 Moderate Additive hypotensive effects by the combination of Paliperidone and Cyclandelate. Dementia [6D80-6D8Z] [58]
OPC-34712 DMHG57U Moderate Additive anticholinergic effects by the combination of Paliperidone and OPC-34712. Depression [6A70-6A7Z] [51]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Paliperidone and Esketamine. Depression [6A70-6A7Z] [64]
Mepenzolate DM8YU2F Moderate Additive anticholinergic effects by the combination of Paliperidone and Mepenzolate. Digestive system disease [DE2Z] [51]
Tetrabenazine DMYWQ0O Major Increased risk of prolong QT interval by the combination of Paliperidone and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [65]
Deutetrabenazine DMUPFLI Major Increased risk of prolong QT interval by the combination of Paliperidone and Deutetrabenazine. Dystonic disorder [8A02] [66]
Ingrezza DMVPLNC Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Ingrezza. Dystonic disorder [8A02] [67]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Solifenacin. Functional bladder disorder [GC50] [50]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Sunitinib. Gastrointestinal stromal tumour [2B5B] [50]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [68]
Lopinavir DMITQS0 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Lopinavir. Human immunodeficiency virus disease [1C60-1C62] [50]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [50]
Penbutolol DM4ES8F Moderate Additive hypotensive effects by the combination of Paliperidone and Penbutolol. Hypertension [BA00-BA04] [58]
Nebivolol DM7F1PA Moderate Additive hypotensive effects by the combination of Paliperidone and Nebivolol. Hypertension [BA00-BA04] [58]
Levamlodipine DM92S6N Moderate Additive hypotensive effects by the combination of Paliperidone and Levamlodipine. Hypertension [BA00-BA04] [58]
TAK-491 DMCF6SX Moderate Additive hypotensive effects by the combination of Paliperidone and TAK-491. Hypertension [BA00-BA04] [58]
Hydralazine DMU8JGH Moderate Additive hypotensive effects by the combination of Paliperidone and Hydralazine. Hypertension [BA00-BA04] [58]
Clevidipine butyrate DMW4M97 Moderate Additive hypotensive effects by the combination of Paliperidone and Clevidipine butyrate. Hypertension [BA00-BA04] [58]
Belladonna DM2RBWK Moderate Additive anticholinergic effects by the combination of Paliperidone and Belladonna. Infectious gastroenteritis/colitis [1A40] [51]
ITI-007 DMUQ1DO Moderate Additive anticholinergic effects by the combination of Paliperidone and ITI-007. Insomnia [7A00-7A0Z] [51]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Paliperidone and Polyethylene glycol. Irritable bowel syndrome [DD91] [50]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Paliperidone and Phenolphthalein. Irritable bowel syndrome [DD91] [50]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Paliperidone caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [54]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Paliperidone and Crizotinib. Lung cancer [2C25] [69]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Paliperidone and Ceritinib. Lung cancer [2C25] [50]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Paliperidone and Osimertinib. Lung cancer [2C25] [70]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Paliperidone and Selpercatinib. Lung cancer [2C25] [54]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Paliperidone and Lumefantrine. Malaria [1F40-1F45] [64]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Paliperidone and Hydroxychloroquine. Malaria [1F40-1F45] [71]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [54]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Paliperidone and Vemurafenib. Melanoma [2C30] [50]
LGX818 DMNQXV8 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and LGX818. Melanoma [2C30] [72]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Paliperidone and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [73]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Paliperidone and Lasmiditan. Migraine [8A80] [74]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Paliperidone and Flibanserin. Mood disorder [6A60-6E23] [75]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Paliperidone and Panobinostat. Multiple myeloma [2A83] [76]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Paliperidone and Siponimod. Multiple sclerosis [8A40] [64]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Paliperidone and Fingolimod. Multiple sclerosis [8A40] [50]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Paliperidone and Ozanimod. Multiple sclerosis [8A40] [77]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Romidepsin. Mycosis fungoides [2B01] [50]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Paliperidone and Nilotinib. Myeloproliferative neoplasm [2A20] [50]
Phenindamine DMDTC7R Moderate Additive anticholinergic effects by the combination of Paliperidone and Phenindamine. Nasopharyngitis [CA00] [51]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Entrectinib. Non-small cell lung cancer [2C25] [64]
Lorcaserin DMG6OYJ Moderate Increased risk of hyperprolactinemic effects by the combination of Paliperidone and Lorcaserin. Obesity [5B80-5B81] [78]
Polythiazide DMCH80F Moderate Increased risk of ventricular arrhythmias by the combination of Paliperidone and Polythiazide. Oedema [MG29] [64]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Paliperidone and Lofexidine. Opioid use disorder [6C43] [50]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Rucaparib. Ovarian cancer [2C73] [50]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Triclabendazole. Parasitic worm infestation [1F90] [50]
Opicapone DM1BKA6 Moderate Antagonize the effect of Paliperidone when combined with Opicapone. Parkinsonism [8A00] [79]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Pimavanserin. Parkinsonism [8A00] [80]
Methylscopolamine DM5VWOB Moderate Additive anticholinergic effects by the combination of Paliperidone and Methylscopolamine. Peptic ulcer [DA61] [51]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Paliperidone and Macimorelin. Pituitary gland disorder [5A60-5A61] [81]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Paliperidone and Lefamulin. Pneumonia [CA40] [82]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Degarelix. Prostate cancer [2C82] [54]
ABIRATERONE DM8V75C Moderate Increased risk of prolong QT interval by the combination of Paliperidone and ABIRATERONE. Prostate cancer [2C82] [54]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Enzalutamide. Prostate cancer [2C82] [54]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Relugolix. Prostate cancer [2C82] [54]
Levomepromazine DMIKFEL Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Levomepromazine. Psychotic disorder [6A20-6A25] [50]
Neupro DMHEAB1 Moderate Additive CNS depression effects by the combination of Paliperidone and Neupro. Restless legs syndrome [7A80] [79]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Paliperidone and LEE011. Solid tumour/cancer [2A00-2F9Z] [50]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Paliperidone and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [50]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [54]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Pitolisant. Somnolence [MG42] [50]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [50]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Paliperidone and Lenvatinib. Thyroid cancer [2D10] [50]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Paliperidone and Cabozantinib. Thyroid cancer [2D10] [54]
Acrivastine DMTIGA0 Moderate Additive anticholinergic effects by the combination of Paliperidone and Acrivastine. Vasomotor/allergic rhinitis [CA08] [51]
⏷ Show the Full List of 91 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
Allura red AC dye E00338 33258 Colorant
Butylated hydroxytoluene E00336 31404 Antioxidant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Sodium stearyl fumarate E00545 23665634 lubricant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Ammonia E00007 222 Alkalizing agent
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
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
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium chloride E00077 5234 Diluent; Tonicity agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
⏷ Show the Full List of 19 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Paliperidone 9 mg tablet 9 mg 24 HR Extended Release Oral Tablet Oral
Paliperidone 1.5 mg tablet 1.5 mg 24 HR Extended Release Oral Tablet Oral
Paliperidone 3 mg tablet 3 mg 24 HR Extended Release Oral Tablet Oral
Paliperidone 6 mg tablet 6 mg 24 HR Extended Release Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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56 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.".
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62 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
63 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.".
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66 Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
67 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
68 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
69 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
70 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
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72 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
73 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
74 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
75 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
76 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
77 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
78 Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
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80 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
81 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
82 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.