paliperidone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antipsychotics, risperidone derivatives 4137 144598-75-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • RO76477
  • RO 76477
  • paliperidone
  • invega
  • xeplion
  • Molecular weight: 426.49
  • Formula: C23H27FN4O3
  • CLOGP: 1.87
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 82.17
  • ALOGS: -3.16
  • ROTB: 4
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
6 mg O
2.50 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.03 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 59 % Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability) 28 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance) 1.18 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.24 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 24.60 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class EIF2AK3,GRK2,PDK1,PDK2,PDK4 5
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 4.656 Moderate 0.76
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
rat-kpuu-brain Rat brain Kpuu 0.062 % Moderate 0.76

Approvals:

DateAgencyCompanyOrphan
June 25, 2007 EMA
Dec. 19, 2006 FDA JANSSEN PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood prolactin abnormal 1265.10 25.33 246 14579 3020 90610602
Dystonia 1246.50 25.33 328 14497 16491 90597131
Anosognosia 1155.95 25.33 231 14594 3291 90610331
Sexual dysfunction 1101.57 25.33 234 14591 4570 90609052
Disturbance in social behaviour 1092.74 25.33 227 14598 3961 90609661
Dyskinesia 1060.04 25.33 344 14481 36190 90577432
Galactorrhoea 1056.59 25.33 225 14600 4447 90609175
Metabolic disorder 977.65 25.33 230 14595 7240 90606382
Personality change 919.31 25.33 218 14607 7103 90606519
Sedation 865.31 25.33 317 14508 47854 90565768
Suicide attempt 773.70 25.33 331 14494 75068 90538554
Blood prolactin increased 742.18 25.33 161 14664 3476 90610146
Blood glucose increased 486.59 25.33 259 14566 94987 90518635
Hyperprolactinaemia 465.11 25.33 119 14706 5314 90608308
Extrapyramidal disorder 437.75 25.33 145 14680 16158 90597464
Amenorrhoea 412.19 25.33 128 14697 11594 90602028
Tardive dyskinesia 341.20 25.33 109 14716 10821 90602801
Psychotic disorder 261.18 25.33 119 14706 31111 90582511
Parkinsonism 249.92 25.33 92 14733 13973 90599649
Akathisia 205.68 25.33 75 14750 11084 90602538
Treatment noncompliance 196.55 25.33 116 14709 51611 90562011
Neuroleptic malignant syndrome 187.09 25.33 76 14749 15020 90598602
Schizophrenia 181.12 25.33 74 14751 14840 90598782
Hallucination, auditory 176.20 25.33 74 14751 15901 90597721
Intentional self-injury 175.95 25.33 89 14736 29245 90584377
Drug ineffective 160.92 25.33 542 14283 1383756 89229866
Delusion 158.99 25.33 66 14759 13774 90599848
Catatonia 151.08 25.33 51 14774 6005 90607617
Breast discharge 144.99 25.33 35 14790 1224 90612398
Intentional overdose 144.56 25.33 121 14704 93713 90519909
Insurance issue 142.08 25.33 57 14768 10901 90602721
Personality change due to a general medical condition 107.01 25.33 21 14804 269 90613353
Apraxia 106.68 25.33 31 14794 2231 90611391
Tremor 101.29 25.33 125 14700 153048 90460574
Adverse drug reaction 100.26 25.33 109 14716 116592 90497030
Head titubation 95.03 25.33 25 14800 1243 90612379
Hospitalisation 93.62 25.33 110 14715 127990 90485632
Mania 90.99 25.33 45 14780 14079 90599543
Diarrhoea 83.80 25.33 25 14800 939165 89674457
Polydipsia 83.80 25.33 30 14795 4201 90609421
Pain 81.13 25.33 31 14794 996310 89617312
Agitation 80.25 25.33 75 14750 67023 90546599
Completed suicide 76.61 25.33 106 14719 144952 90468670
Schizoaffective disorder 74.51 25.33 29 14796 5118 90608504
Aggression 73.95 25.33 49 14776 26619 90587003
Arthralgia 72.60 25.33 19 14806 778503 89835119
Myocarditis 71.57 25.33 38 14787 13768 90599854
Salivary hypersecretion 70.81 25.33 33 14792 9059 90604563
Oculogyric crisis 66.28 25.33 22 14803 2457 90611165
Movement disorder 63.28 25.33 46 14779 28973 90584649
Condition aggravated 60.47 25.33 224 14601 595321 90018301
Weight increased 58.24 25.33 175 14650 417752 90195870
Paranoia 57.13 25.33 32 14793 12876 90600746
Myoclonus 55.04 25.33 36 14789 19132 90594490
Abnormal behaviour 54.24 25.33 38 14787 22590 90591032
Somnolence 54.08 25.33 111 14714 208973 90404649
Tachycardia 53.51 25.33 94 14731 157579 90456043
Overdose 53.50 25.33 94 14731 157615 90456007
Nausea 52.40 25.33 63 14762 1110253 89503369
Alopecia 52.39 25.33 9 14816 495062 90118560
Psychotic symptom 52.35 25.33 18 14807 2238 90611384
Metabolic syndrome 51.51 25.33 17 14808 1865 90611757
Drug hypersensitivity 50 25.33 8 14817 463601 90150021
Joint swelling 49.36 25.33 11 14814 503289 90110333
Breast enlargement 48.63 25.33 16 14809 1739 90611883
Sinus tachycardia 48.53 25.33 39 14786 28474 90585148
Depressive symptom 46.87 25.33 21 14804 5264 90608358
Drug interaction 46.51 25.33 124 14701 276329 90337293
Suicidal ideation 45.14 25.33 58 14767 73797 90539825
Sinusitis 44.43 25.33 3 14822 343085 90270537
Pain in extremity 43.86 25.33 10 14815 450519 90163103
Headache 42.75 25.33 47 14778 862699 89750923
Rash 42.11 25.33 41 14784 796059 89817563
Infection 41.97 25.33 5 14820 362089 90251533
Muscle rigidity 41.39 25.33 27 14798 14282 90599340
Psychiatric decompensation 39.32 25.33 14 14811 1929 90611693
Rhabdomyolysis 39.04 25.33 45 14780 51211 90562411
Fatigue 38.79 25.33 82 14743 1153941 89459681
Abdominal discomfort 38.47 25.33 15 14810 477313 90136309
Nasopharyngitis 37.74 25.33 10 14815 407094 90206528
Personality disorder 37.27 25.33 24 14801 12420 90601202
Blood creatine phosphokinase increased 36.81 25.33 36 14789 33987 90579635
Wound 35.56 25.33 4 14821 302976 90310646
Psychiatric symptom 35.23 25.33 19 14806 7099 90606523
Psychotic behaviour 35.16 25.33 10 14815 666 90612956
Peripheral swelling 34.94 25.33 12 14813 413094 90200528
Pneumonia 34.72 25.33 32 14793 638027 89975595
Hypersensitivity 33.91 25.33 16 14809 454661 90158961
Discomfort 33.82 25.33 3 14822 274332 90339290
Altered state of consciousness 33.43 25.33 33 14792 31499 90582123
Pruritus 33.38 25.33 24 14801 541501 90072121
Anger 32.78 25.33 23 14802 13697 90599925
Monocyte count decreased 31.93 25.33 13 14812 2578 90611044
Psychomotor hyperactivity 31.83 25.33 22 14803 12791 90600831
Abdominal pain upper 31.15 25.33 8 14817 332666 90280956
Electrocardiogram QT prolonged 31.03 25.33 48 14777 72408 90541214
Mental impairment 30.88 25.33 24 14801 16696 90596926
Ovarian germ cell cancer stage II 30.86 25.33 6 14819 73 90613549
Drooling 30.81 25.33 15 14810 4531 90609091
Lactate pyruvate ratio increased 30.42 25.33 6 14819 79 90613543
Mobility decreased 30.22 25.33 3 14822 250731 90362891
Lower respiratory tract infection 30.21 25.33 3 14822 250656 90362966
Restlessness 30.00 25.33 33 14792 35687 90577935
Regressive behaviour 30.00 25.33 7 14818 211 90613411
Hepatic enzyme increased 29.61 25.33 11 14814 360725 90252897
Swelling 29.36 25.33 16 14809 419042 90194580
Trichoglossia 29.36 25.33 8 14817 455 90613167
Diabetes insipidus 29.24 25.33 13 14812 3199 90610423
Decreased appetite 28.45 25.33 13 14812 376527 90237095
Sopor 28.40 25.33 27 14798 24617 90589005
Wheezing 28.30 25.33 3 14822 238077 90375545
Contusion 27.82 25.33 4 14821 251212 90362410
Dyspnoea 27.57 25.33 65 14760 880890 89732732
General physical health deterioration 27.24 25.33 12 14813 355103 90258519
Gender dysphoria 26.48 25.33 4 14821 8 90613614
Blood citric acid increased 26.35 25.33 5 14820 53 90613569
Epileptic encephalopathy 25.97 25.33 7 14818 382 90613240

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Gynaecomastia 773.15 23.97 257 15996 12310 42592772
Dystonia 515.48 23.97 191 16062 12599 42592483
Treatment noncompliance 446.08 23.97 238 16015 37434 42567648
Akathisia 420.79 23.97 156 16097 10295 42594787
Extrapyramidal disorder 391.79 23.97 168 16085 16244 42588838
Psychotic disorder 369.66 23.97 193 16060 29015 42576067
Sedation 331.23 23.97 182 16071 30293 42574789
Weight increased 297.75 23.97 279 15974 107704 42497378
Neuroleptic malignant syndrome 295.00 23.97 150 16103 21322 42583760
Anosognosia 241.43 23.97 60 16193 984 42604098
Intentional self-injury 240.74 23.97 117 16136 15085 42589997
Hyperprolactinaemia 229.81 23.97 67 16186 2056 42603026
Sexual dysfunction 221.76 23.97 87 16166 6688 42598394
Emotional disorder 216.99 23.97 84 16169 6230 42598852
Blood prolactin abnormal 206.17 23.97 53 16200 1002 42604080
Disturbance in social behaviour 191.18 23.97 56 16197 1747 42603335
Delusion 188.05 23.97 98 16155 14636 42590446
Suicide attempt 185.42 23.97 148 16105 45952 42559130
Dyskinesia 184.59 23.97 117 16136 25273 42579809
Hallucination, auditory 178.72 23.97 95 16158 14769 42590313
Schizophrenia 166.40 23.97 81 16172 10469 42594613
Blood prolactin increased 165.38 23.97 53 16200 2245 42602837
Myocarditis 141.96 23.97 89 16164 18849 42586233
Metabolic disorder 134.20 23.97 55 16198 4733 42600349
Tachycardia 133.47 23.97 178 16075 100909 42504173
Aggression 125.00 23.97 116 16137 44047 42561035
Mental impairment 123.94 23.97 70 16183 12247 42592835
Drug ineffective 123.36 23.97 519 15734 629678 41975404
Intentional overdose 122.72 23.97 123 16130 51333 42553749
Sedation complication 118.96 23.97 44 16209 2875 42602207
Salivary hypersecretion 117.76 23.97 65 16188 10878 42594204
Loss of libido 116.80 23.97 44 16209 3026 42602056
Obesity 115.00 23.97 74 16179 16385 42588697
Apathy 110.35 23.97 57 16196 8349 42596733
Tardive dyskinesia 105.69 23.97 52 16201 6872 42598210
Galactorrhoea 101.75 23.97 26 16227 479 42604603
Psychotic symptom 100.99 23.97 37 16216 2353 42602729
Suicidal ideation 93.19 23.97 103 16150 48058 42557024
Hospitalisation 92.11 23.97 127 16126 74203 42530879
Parkinsonism 89.99 23.97 54 16199 10569 42594513
Diarrhoea 88.18 23.97 33 16220 460816 42144266
Catatonia 86.80 23.97 44 16209 6195 42598887
Abnormal weight gain 85.26 23.97 28 16225 1282 42603800
Mania 82.63 23.97 51 16202 10496 42594586
Tremor 81.07 23.97 138 16115 96791 42508291
Persecutory delusion 80.09 23.97 35 16218 3529 42601553
Hallucination 80.02 23.97 104 16149 57403 42547679
Agitation 79.84 23.97 110 16143 64204 42540878
Personality change 75.69 23.97 39 16214 5680 42599402
Abnormal behaviour 73.87 23.97 69 16184 26382 42578700
Drooling 73.81 23.97 35 16218 4264 42600818
Paranoia 71.69 23.97 52 16201 13974 42591108
Anaemia 64.69 23.97 14 16239 280264 42324818
Emotional distress 63.19 23.97 51 16202 16042 42589040
Psychiatric symptom 56.35 23.97 29 16224 4212 42600870
Priapism 55.38 23.97 33 16220 6374 42598708
Overweight 55.22 23.97 24 16229 2388 42602694
Arthralgia 54.52 23.97 7 16246 205231 42399851
Muscle rigidity 53.34 23.97 41 16212 12018 42593064
Blood creatine phosphokinase increased 53.06 23.97 78 16175 48260 42556822
Febrile neutropenia 52.70 23.97 5 16248 185698 42419384
Sepsis 52.47 23.97 7 16246 199327 42405755
Blepharospasm 49.84 23.97 19 16234 1349 42603733
Jaw clicking 49.43 23.97 10 16243 59 42605023
Pleurothotonus 48.41 23.97 18 16235 1193 42603889
Rhabdomyolysis 46.35 23.97 96 16157 77923 42527159
Death 45.99 23.97 68 16185 471117 42133965
Somnolence 45.06 23.97 137 16116 140968 42464114
Thrombocytopenia 44.90 23.97 9 16244 190270 42414812
Pneumonia 44.10 23.97 58 16195 422091 42182991
Sinus tachycardia 43.10 23.97 46 16207 20607 42584475
Blood osmolarity decreased 42.75 23.97 14 16239 635 42604447
Thinking abnormal 42.27 23.97 29 16224 7132 42597950
Anion gap increased 42.03 23.97 19 16234 2075 42603007
Acute kidney injury 40.93 23.97 48 16205 367289 42237793
Blood glucose increased 40.66 23.97 88 16165 73611 42531471
Conversion disorder 40.63 23.97 13 16240 547 42604535
Pruritus 40.44 23.97 11 16242 188760 42416322
Disease progression 40.39 23.97 4 16249 143652 42461430
Hypometabolism 39.94 23.97 10 16243 169 42604913
Sopor 39.88 23.97 36 16217 13166 42591916
Social avoidant behaviour 39 23.97 21 16232 3343 42601739
Sluggishness 38.79 23.97 22 16231 3874 42601208
Antipsychotic drug level increased 37.66 23.97 23 16230 4643 42600439
Painful erection 37.64 23.97 11 16242 340 42604742
Cough 35.21 23.97 12 16241 178091 42426991
Restlessness 34.72 23.97 49 16204 29200 42575882
Nephrogenic diabetes insipidus 33.88 23.97 15 16238 1559 42603523
Intentional product misuse 31.97 23.97 72 16181 61828 42543254
Nausea 31.62 23.97 65 16188 396734 42208348
Myelocyte count increased 31.53 23.97 10 16243 409 42604673
Water intoxication 31.51 23.97 10 16243 410 42604672
Drug use disorder 30.86 23.97 28 16225 10305 42594777
Dyspnoea 30.83 23.97 78 16175 442543 42162539
Drug interaction 29.96 23.97 189 16064 266810 42338272
Paradoxical drug reaction 29.90 23.97 20 16233 4718 42600364
Inappropriate affect 29.35 23.97 11 16242 745 42604337
Bruxism 29.30 23.97 15 16238 2154 42602928
Troponin I increased 29.28 23.97 17 16236 3129 42601953
Yawning 28.99 23.97 11 16242 771 42604311
Housebound 27.89 23.97 8 16245 231 42604851
Pancytopenia 26.87 23.97 6 16247 117737 42487345
Eye movement disorder 26.79 23.97 19 16234 4926 42600156
Gastrointestinal haemorrhage 26.74 23.97 3 16250 97723 42507359
Olfactory nerve disorder 26.52 23.97 6 16247 64 42605018
Completed suicide 26.50 23.97 89 16164 96376 42508706
Metamyelocyte count increased 26.47 23.97 9 16244 459 42604623
Increased appetite 26.34 23.97 24 16229 8882 42596200
Renal failure 26.20 23.97 11 16242 143715 42461367
Illusion 26.06 23.97 11 16242 1018 42604064
Trismus 25.30 23.97 15 16238 2869 42602213
Delusional perception 25.18 23.97 7 16246 180 42604902
Blood bicarbonate decreased 25.06 23.97 15 16238 2920 42602162
Infection 25.00 23.97 6 16247 112062 42493020
Arrhythmia 24.38 23.97 50 16203 40267 42564815
Troponin increased 24.22 23.97 33 16220 19029 42586053
Inappropriate schedule of product administration 24.19 23.97 86 16167 95816 42509266
Protein total increased 24.17 23.97 14 16239 2564 42602518
Pain 24.13 23.97 35 16218 244813 42360269
Drug level below therapeutic 24.13 23.97 20 16233 6525 42598557
Pyrexia 24.03 23.97 74 16179 393968 42211114

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dystonia 1389.47 23.35 418 23837 25387 110539657
Blood prolactin abnormal 1198.60 23.35 254 24001 3581 110561463
Anosognosia 1188.96 23.35 255 24000 3819 110561225
Sexual dysfunction 1100.77 23.35 275 23980 8255 110556789
Disturbance in social behaviour 1063.52 23.35 242 24013 4816 110560228
Dyskinesia 988.20 23.35 385 23870 51061 110513983
Sedation 943.97 23.35 406 23849 69277 110495767
Metabolic disorder 920.46 23.35 249 24006 10261 110554783
Personality change 839.94 23.35 234 24021 10768 110554276
Suicide attempt 788.14 23.35 405 23850 102989 110462055
Galactorrhoea 627.13 23.35 152 24103 4003 110561041
Extrapyramidal disorder 585.71 23.35 225 24030 28642 110536402
Gynaecomastia 576.73 23.35 169 24086 9321 110555723
Akathisia 517.18 23.35 179 24076 16934 110548110
Blood prolactin increased 468.02 23.35 123 24132 4519 110560525
Hyperprolactinaemia 466.00 23.35 132 24123 6443 110558601
Neuroleptic malignant syndrome 462.43 23.35 199 24056 33860 110531184
Treatment noncompliance 448.72 23.35 248 24007 72742 110492302
Intentional self-injury 438.00 23.35 197 24058 37232 110527812
Blood glucose increased 403.01 23.35 288 23967 132208 110432836
Psychotic disorder 391.79 23.35 201 24054 50736 110514308
Parkinsonism 302.27 23.35 130 24125 22057 110542987
Delusion 274.54 23.35 124 24131 23631 110541413
Tardive dyskinesia 272.27 23.35 105 24150 13474 110551570
Hallucination, auditory 268.20 23.35 126 24129 26271 110538773
Schizophrenia 255.63 23.35 115 24140 21711 110543333
Drug ineffective 252.54 23.35 816 23439 1519724 109045320
Intentional overdose 243.04 23.35 214 24041 132287 110432757
Myocarditis 226.38 23.35 117 24138 29938 110535106
Amenorrhoea 212.61 23.35 79 24176 9152 110555892
Salivary hypersecretion 207.85 23.35 93 24162 17328 110547716
Catatonia 197.09 23.35 79 24176 11221 110553823
Tachycardia 169.65 23.35 228 24027 226417 110338627
Weight increased 149.80 23.35 302 23953 419342 110145702
Insurance issue 140.63 23.35 61 24194 10551 110554493
Diarrhoea 135.72 23.35 41 24214 1139464 109425580
Psychotic symptom 134.60 23.35 45 24210 3822 110561222
Mental impairment 130.98 23.35 74 24181 22565 110542479
Tremor 125.41 23.35 186 24069 202046 110362998
Agitation 120.53 23.35 136 24119 112915 110452129
Aggression 119.32 23.35 101 24154 59109 110505935
Adverse drug reaction 117.70 23.35 130 24125 105429 110459615
Mania 117.68 23.35 67 24188 20729 110544315
Hospitalisation 116.83 23.35 150 24105 142343 110422701
Arthralgia 108.55 23.35 20 24235 779612 109785432
Abnormal behaviour 105.21 23.35 79 24176 38960 110526084
Polydipsia 101.24 23.35 44 24211 7644 110557400
Emotional disorder 96.67 23.35 54 24201 16106 110548938
Loss of libido 95.48 23.35 33 24222 3100 110561944
Sinus tachycardia 93.98 23.35 78 24177 44415 110520629
Apraxia 91.53 23.35 33 24222 3507 110561537
Hallucination 91.44 23.35 112 24143 101320 110463724
Somnolence 88.55 23.35 199 24056 297250 110267794
Blood creatine phosphokinase increased 88.44 23.35 94 24161 72983 110492061
Rhabdomyolysis 88.25 23.35 120 24135 120281 110444763
Personality change due to a general medical condition 87.80 23.35 19 24236 296 110564748
Paranoia 87.75 23.35 57 24198 22317 110542727
Muscle rigidity 86.43 23.35 58 24197 23973 110541071
Sedation complication 86.36 23.35 54 24201 19801 110545243
Head titubation 86.08 23.35 25 24230 1332 110563712
Pain 85.51 23.35 52 24203 954903 109610141
Drug interaction 82.51 23.35 269 23986 499914 110065130
Apathy 80.45 23.35 48 24207 16191 110548853
Nausea 80.29 23.35 92 24163 1235598 109329446
Suicidal ideation 75.56 23.35 98 24157 93839 110471205
Drooling 75.33 23.35 35 24220 7104 110557940
Sopor 70.87 23.35 61 24194 36485 110528559
Headache 69.73 23.35 55 24200 882322 109682722
Pruritus 68.90 23.35 21 24234 581539 109983505
Sluggishness 67.35 23.35 33 24222 7534 110557510
Alopecia 64.14 23.35 4 24251 364749 110200295
Peripheral swelling 63.98 23.35 7 24248 404027 110161017
Dyspnoea 63.94 23.35 90 24165 1106782 109458262
Completed suicide 63.17 23.35 154 24101 242227 110322817
Anaemia 62.59 23.35 21 24234 547065 110017979
Joint swelling 62.32 23.35 11 24244 442834 110122210
Pain in extremity 56.94 23.35 18 24237 487100 110077944
Drug abuse 56.47 23.35 122 24133 177289 110387755
Rash 55.53 23.35 59 24196 820905 109744139
Myelocyte count increased 54.28 23.35 16 24239 898 110564146
Overdose 54.09 23.35 142 24113 233652 110331392
Oculogyric crisis 53.97 23.35 23 24232 3809 110561235
Metamyelocyte count increased 53.76 23.35 15 24240 691 110564353
Movement disorder 53.46 23.35 52 24203 36352 110528692
Psychiatric symptom 52.97 23.35 30 24225 9183 110555861
Pleurothotonus 52.51 23.35 20 24235 2478 110562566
Pneumonia 51.86 23.35 70 24185 876644 109688400
Infection 50.94 23.35 9 24246 362191 110202853
Metabolic syndrome 50.78 23.35 21 24234 3226 110561818
Fatigue 50.51 23.35 121 24134 1215837 109349207
Condition aggravated 49.87 23.35 303 23952 734533 109830511
Drug hypersensitivity 49.25 23.35 19 24236 454071 110110973
Nasopharyngitis 48.97 23.35 13 24242 394348 110170696
Abnormal weight gain 48.75 23.35 21 24234 3570 110561474
Stomatitis 47.39 23.35 3 24252 270239 110294805
Febrile neutropenia 46.49 23.35 7 24248 316760 110248284
Emotional distress 46.14 23.35 53 24202 44794 110520250
Persecutory delusion 45.94 23.35 24 24231 6267 110558777
Intentional product misuse 45.30 23.35 94 24161 132810 110432234
General physical health deterioration 44.16 23.35 19 24236 425276 110139768
Drug resistance 44.05 23.35 58 24197 56316 110508728
Blood osmolarity decreased 42.85 23.35 15 24240 1463 110563581
Restlessness 42.61 23.35 57 24198 56202 110508842
Abdominal pain upper 42.42 23.35 12 24243 349099 110215945
Abdominal discomfort 41.85 23.35 17 24238 393841 110171203
Electrocardiogram QT prolonged 41.84 23.35 81 24174 108879 110456165
Arrhythmia 41.64 23.35 63 24192 69512 110495532
Thinking abnormal 41.59 23.35 31 24224 15109 110549935
Breast enlargement 40.89 23.35 15 24240 1674 110563370
Antipsychotic drug level increased 40.76 23.35 23 24232 6992 110558052
Mobility decreased 40.56 23.35 3 24252 237419 110327625
Thrombocytopenia 40.56 23.35 13 24242 348872 110216172
Swelling 39.21 23.35 14 24241 351027 110214017
Wheezing 38.95 23.35 5 24250 255225 110309819
Hypersensitivity 38.94 23.35 20 24235 403978 110161066
Nephrogenic diabetes insipidus 38.87 23.35 16 24239 2429 110562615
Anion gap increased 38.82 23.35 19 24236 4325 110560719
Cough 38.68 23.35 27 24228 461614 110103430
Schizoaffective disorder 38.22 23.35 17 24238 3119 110561925
Wound 37.25 23.35 4 24251 234433 110330611
Acute psychosis 36.34 23.35 19 24236 4968 110560076
Back pain 36.30 23.35 18 24237 370978 110194066
Priapism 36.19 23.35 20 24235 5841 110559203
Antipsychotic drug level decreased 35.90 23.35 13 24242 1399 110563645
Myoclonus 35.65 23.35 40 24215 32958 110532086
Vomiting 35.12 23.35 94 24161 910581 109654463
Contusion 34.60 23.35 5 24250 233356 110331688
Hypometabolism 34.06 23.35 8 24247 183 110564861
Hypertension 34.05 23.35 37 24218 510047 110054997
Asthma 33.53 23.35 7 24248 250284 110314760
Increased appetite 33.17 23.35 27 24228 14950 110550094
Hyponatraemia 33.06 23.35 114 24141 217539 110347505
Toxicity to various agents 33.06 23.35 199 24056 480356 110084688
Altered state of consciousness 32.82 23.35 51 24204 57575 110507469
Hypoaesthesia 32.67 23.35 14 24241 314209 110250835
Lower respiratory tract infection 32.15 23.35 7 24248 243099 110321945
Erythema 31.90 23.35 12 24243 291435 110273609
Psychomotor hyperactivity 31.73 23.35 30 24225 20247 110544797
Olfactory nerve disorder 31.72 23.35 6 24249 45 110564999
Urinary tract infection 31.66 23.35 16 24239 326266 110238778
Decreased appetite 31.23 23.35 35 24220 475811 110089233
Drug use disorder 30.71 23.35 28 24227 18046 110546998
Troponin increased 30.32 23.35 35 24220 29731 110535313
Abdominal pain 30.23 23.35 41 24214 512948 110052096
Musculoskeletal pain 29.39 23.35 3 24252 183020 110382024
Death 29.35 23.35 69 24186 698800 109866244
Lactate pyruvate ratio increased 29.18 23.35 6 24249 72 110564972
Monocyte count decreased 29.00 23.35 15 24240 3836 110561208
Breast discharge 28.92 23.35 10 24245 940 110564104
Diabetes insipidus 28.90 23.35 18 24237 6552 110558492
Torticollis 28.52 23.35 14 24241 3207 110561837
Hallucination, visual 28.28 23.35 39 24216 39566 110525478
Inappropriate antidiuretic hormone secretion 28.28 23.35 36 24219 33815 110531229
Regressive behaviour 27.73 23.35 7 24248 218 110564826
Housebound 27.04 23.35 8 24247 455 110564589
Seizure 27.02 23.35 108 24147 221077 110343967
Social avoidant behaviour 26.93 23.35 16 24239 5353 110559691
Discomfort 26.78 23.35 7 24248 214700 110350344
Inflammation 26.72 23.35 5 24250 193233 110371811
Troponin I increased 26.70 23.35 16 24239 5436 110559608
Inappropriate affect 26.61 23.35 11 24244 1688 110563356
Influenza 26.57 23.35 3 24252 169098 110395946
Granulocytopenia 26.24 23.35 22 24233 12693 110552351
Psychiatric decompensation 25.88 23.35 16 24239 5749 110559295
Blood bicarbonate decreased 25.80 23.35 16 24239 5781 110559263
Drug level below therapeutic 25.76 23.35 21 24234 11652 110553392
Accidental exposure to product by child 25.66 23.35 13 24242 3185 110561859
Maternal exposure during pregnancy 25.48 23.35 12 24243 254871 110310173
Irritability 25.41 23.35 41 24214 47768 110517276
Drug dependence 25.37 23.35 42 24213 49978 110515066
Hepatic enzyme increased 25.27 23.35 20 24235 320872 110244172
Sepsis 25.03 23.35 21 24234 327325 110237719
Water intoxication 25.02 23.35 9 24246 950 110564094
Blood citric acid increased 24.88 23.35 5 24250 53 110564991
Behaviour disorder 24.83 23.35 19 24236 9628 110555416
Intentional product use issue 24.28 23.35 12 24243 247894 110317150
Hyperammonaemic encephalopathy 24.18 23.35 15 24240 5419 110559625
Trismus 23.90 23.35 16 24239 6580 110558464
Psychomotor retardation 23.77 23.35 17 24238 7775 110557269
Asthenia 23.69 23.35 75 24180 688924 109876120
Blast cell count increased 23.63 23.35 10 24245 1627 110563417
Disease progression 23.62 23.35 12 24243 244022 110321022
Rebound psychosis 23.44 23.35 7 24248 411 110564633

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX13 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
FDA EPC N0000175430 Atypical Antipsychotic
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D012702 Serotonin Antagonists
MeSH PA D014150 Antipsychotic Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D058830 Serotonin 5-HT2 Receptor Antagonists
MeSH PA D065127 Dopamine D2 Receptor Antagonists
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35471 psychotropic drug
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:37890 α-adrenergic antagonist
CHEBI has role CHEBI:37955 H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:49103 drug metabolite
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:65191 second generation antipsychotic

Related Drugs by ATC class:

N05AX Other antipsychotics 11 drugs
aripiprazolebrexpiprazolecariprazineiloperidonemosapraminepimavanserinprothipendylrisperidonetrospiumxanomelinezotepine

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419
Schizoaffective disorder indication 68890003 DOID:5418
Psychotic disorder indication 69322001
Mixed bipolar I disorder off-label use 16506000 DOID:3312
Bipolar disorder in remission off-label use 85248005
Bipolar affective disorder, current episode manic off-label use 191618007
Bipolar affective disorder, current episode depression off-label use 191627008 DOID:3312
Infantile autism off-label use 408857007
Depression Treatment Adjunct off-label use
Priapism contraindication 6273006 DOID:9286
Suicidal thoughts contraindication 6471006
Weight gain finding contraindication 8943002
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Lowered convulsive threshold contraindication 19260006
Myocardial infarction contraindication 22298006 DOID:5844
Stenosis of intestine contraindication 23065003
Short bowel syndrome contraindication 26629001 DOID:10605
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Parkinsonism contraindication 32798002
Crohn's disease contraindication 34000006
Dehydration contraindication 34095006
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Hyperlipidemia contraindication 55822004 DOID:1168
Cerebrovascular disease contraindication 62914000 DOID:6713
Substance abuse contraindication 66214007
Diabetes mellitus contraindication 73211009 DOID:9351
Extrapyramidal disease contraindication 76349003
Diffuse Lewy body disease contraindication 80098002
Hyperglycemia contraindication 80394007 DOID:4195
Leukopenia contraindication 84828003 DOID:615
Tardive dyskinesia contraindication 102449007
Increased intestinal motility contraindication 102624003
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Hypomagnesemia contraindication 190855004
Angina pectoris contraindication 194828000
Impaired renal function disorder contraindication 197663003
Metabolic syndrome X contraindication 237602007 DOID:14221
Hyperprolactinemia contraindication 237662005 DOID:12700
Esophageal dysmotility contraindication 266434009 DOID:9192
Neutropenic disorder contraindication 303011007 DOID:1227
At risk for aspiration contraindication 371736008
Impaired cognition contraindication 386806002
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Gastrointestinal hypomotility contraindication 421807004
Acquired torsion dystonia contraindication 433493000
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002
Esophageal Compression contraindication
Intestinal Cystic Fibrosis contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.78 Basic
pKa2 2.73 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.47 PDSP DRUG LABEL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8.96 PDSP DRUG LABEL
Histamine H4 receptor GPCR Ki 5.06 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 7.64 PDSP
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.89 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 5.43 PDSP
Beta-1 adrenergic receptor GPCR Ki 5.30 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
D(1A) dopamine receptor GPCR Ki 7.39 PDSP
Alpha-2A adrenergic receptor GPCR Ki 7.93 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 6.22 PDSP
5-hydroxytryptamine receptor 2B GPCR Ki 7.21 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 7.32 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 5.62 PDSP
Histamine H1 receptor GPCR Ki 8.25 PDSP
Alpha-1A adrenergic receptor GPCR Ki 8.55 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 7.64 PDSP
D(3) dopamine receptor GPCR Ki 9.05 PDSP
D(1B) dopamine receptor GPCR Ki 7.54 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 7.72 PDSP
Alpha-2C adrenergic receptor GPCR Ki 8.20 PDSP
D(4) dopamine receptor GPCR Ki 7.27 PDSP
Alpha-1B adrenergic receptor GPCR Ki 9.16 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 6.56 PDSP
5-hydroxytryptamine receptor 1E GPCR Ki 5.99 PDSP
Prostaglandin E2 receptor EP3 subtype GPCR Ki 5 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 8.57 PDSP
Histamine H2 receptor GPCR Ki 6.92 PDSP

External reference:

IDSource
4025875 VUID
N0000176080 NUI
D05339 KEGG_DRUG
4025875 VANDF
C0753678 UMLSCUI
CHEBI:82978 CHEBI
CHEMBL1621 ChEMBL_ID
CHEMBL2107360 ChEMBL_ID
D000068882 MESH_DESCRIPTOR_UI
DB01267 DRUGBANK_ID
7258 IUPHAR_LIGAND_ID
7977 INN_ID
838F01T721 UNII
115237 PUBCHEM_CID
679314 RXNORM
23004 MMSL
92090 MMSL
d06297 MMSL
011888 NDDF
425483000 SNOMEDCT_US
426276000 SNOMEDCT_US
838F01T721 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6935 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6936 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6937 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 31 sections
Paliperidone Human Prescription Drug Label 1 16714-866 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 31 sections
Paliperidone Human Prescription Drug Label 1 16714-867 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 31 sections
Paliperidone Human Prescription Drug Label 1 16714-868 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 31 sections
Paliperidone Human Prescription Drug Label 1 16714-869 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 31 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 21695-455 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 34 sections
Paliperidone Human Prescription Drug Label 1 27241-276 TABLET, EXTENDED RELEASE 1.50 mg ORAL ANDA 32 sections
Paliperidone Human Prescription Drug Label 1 27241-277 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 32 sections
Paliperidone Human Prescription Drug Label 1 27241-278 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 32 sections
Paliperidone Human Prescription Drug Label 1 27241-279 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 32 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 27808-222 TABLET, EXTENDED RELEASE 1.50 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 27808-223 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 27808-224 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 27808-225 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 33 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 31722-317 TABLET, EXTENDED RELEASE 1.50 mg ORAL ANDA 20 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 31722-318 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 20 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 31722-319 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 20 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 31722-320 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 20 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 42291-915 TABLET, EXTENDED RELEASE 1.50 mg ORAL ANDA 30 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 42291-916 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 30 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 42291-917 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 30 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 42291-918 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 30 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 43602-294 TABLET, EXTENDED RELEASE 1.50 mg ORAL ANDA 19 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 43602-295 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 19 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 43602-296 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 19 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 43602-297 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 19 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 43975-349 TABLET, EXTENDED RELEASE 1.50 mg ORAL ANDA 34 sections
PALIPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 43975-350 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 34 sections