paliperidone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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) 0.01 mg/mL Benet LZ, Broccatelli F, Oprea TI
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

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
Galactorrhoea 1009.93 23.51 217 10261 3506 50591140
Blood prolactin abnormal 799.03 23.51 163 10315 2012 50592634
Anosognosia 712.99 23.51 149 10329 2085 50592561
Sexual dysfunction 666.25 23.51 151 10327 3141 50591505
Blood prolactin increased 664.40 23.51 149 10329 2950 50591696
Disturbance in social behaviour 652.49 23.51 145 10333 2749 50591897
Dystonia 634.98 23.51 189 10289 11737 50582909
Metabolic disorder 580.35 23.51 148 10330 5138 50589508
Personality change 541.70 23.51 142 10336 5503 50589143
Sedation 512.42 23.51 204 10274 30406 50564240
Suicide attempt 503.88 23.51 235 10243 51497 50543149
Dyskinesia 488.40 23.51 192 10286 27669 50566977
Amenorrhoea 330.88 23.51 106 10372 8378 50586268
Hyperprolactinaemia 295.72 23.51 79 10399 3286 50591360
Blood glucose increased 273.66 23.51 175 10303 71149 50523497
Extrapyramidal disorder 248.52 23.51 93 10385 11677 50582969
Schizophrenia 222.53 23.51 76 10402 7321 50587325
Psychotic disorder 181.16 23.51 89 10389 21723 50572923
Akathisia 162.72 23.51 62 10416 8167 50586479
Insurance issue 160.16 23.51 46 10432 2502 50592144
Intentional self-injury 147.56 23.51 79 10399 23033 50571613
Breast discharge 145.31 23.51 34 10444 813 50593833
Neuroleptic malignant syndrome 141.31 23.51 61 10417 11069 50583577
Treatment noncompliance 138.28 23.51 83 10395 30067 50564579
Hallucination, auditory 130.33 23.51 57 10421 10671 50583975
Intentional overdose 130.27 23.51 106 10372 62398 50532248
Catatonia 106.94 23.51 37 10441 3699 50590947
Tardive dyskinesia 106.05 23.51 44 10434 7235 50587411
Delusion 99.43 23.51 47 10431 10522 50584124
Adverse drug reaction 81.50 23.51 77 10401 55145 50539501
Weight increased 73.93 23.51 142 10336 201749 50392897
Diarrhoea 68.05 23.51 19 10459 588457 50006189
Agitation 66.75 23.51 68 10410 53316 50541330
Mania 63.21 23.51 35 10443 10881 50583765
Aggression 57.46 23.51 42 10436 21074 50573572
Oculogyric crisis 56.16 23.51 18 10460 1419 50593227
Hospitalisation 53.35 23.51 68 10410 67869 50526777
Pain 53.04 23.51 27 10451 578876 50015770
Parkinsonism 50.22 23.51 28 10450 8819 50585827
Arthralgia 49.10 23.51 15 10463 438687 50155959
Condition aggravated 46.51 23.51 151 10327 296907 50297739
Nausea 45.11 23.51 48 10430 705350 49889296
Tremor 44.67 23.51 83 10395 114820 50479826
Breast enlargement 44.34 23.51 15 10463 1400 50593246
Tachycardia 43.81 23.51 76 10402 99687 50494959
Salivary hypersecretion 43.35 23.51 23 10455 6568 50588078
Drug ineffective 39.76 23.51 297 10181 819036 49775610
Overdose 38.70 23.51 72 10406 99655 50494991
Abnormal behaviour 38.09 23.51 32 10446 19626 50575020
Psychotic symptom 34.67 23.51 12 10466 1200 50593446
Psychotic behaviour 34.47 23.51 10 10468 563 50594083
Personality disorder 33.95 23.51 17 10461 4307 50590339
Paranoia 33.75 23.51 23 10455 10325 50584321
Drug hypersensitivity 33.12 23.51 6 10472 251004 50343642
Pain in extremity 32.97 23.51 8 10470 272857 50321789
Monocyte count decreased 32.97 23.51 13 10465 1873 50592773
Completed suicide 31.29 23.51 78 10400 131811 50462835
Schizoaffective disorder 31.00 23.51 13 10465 2193 50592453
Fatigue 30.68 23.51 63 10415 707538 49887108
Mental impairment 30.61 23.51 23 10455 12021 50582625
Muscle rigidity 30.07 23.51 21 10457 9808 50584838
Metabolic syndrome 29.71 23.51 11 10467 1336 50593310
Polydipsia 29.70 23.51 14 10464 3110 50591536
Peripheral swelling 29.25 23.51 4 10474 205932 50388714
Somnolence 29.05 23.51 84 10394 154901 50439745
Blood creatine phosphokinase increased 28.33 23.51 31 10447 26336 50568310
Lactate pyruvate ratio increased 28.28 23.51 6 10472 90 50594556
Sinus tachycardia 28.13 23.51 28 10450 21326 50573320
Alopecia 28.05 23.51 8 10470 245039 50349607
Suicidal ideation 28.04 23.51 45 10433 55340 50539306
Personality change due to a general medical condition 27.98 23.51 6 10472 95 50594551
Ovarian germ cell cancer stage II 27.69 23.51 5 10473 30 50594616
Electrocardiogram QT prolonged 27.43 23.51 43 10435 51843 50542803
Anger 27.39 23.51 21 10457 11312 50583334
Epileptic encephalopathy 26.72 23.51 7 10471 269 50594377
Sopor 26.06 23.51 26 10452 19853 50574793
Eosinophilic pleural effusion 25.91 23.51 5 10473 45 50594601
Sluggishness 25.13 23.51 14 10464 4399 50590247
Breast tenderness 25.04 23.51 11 10467 2077 50592569
Sinusitis 24.97 23.51 3 10475 170555 50424091
Pneumonia 24.93 23.51 25 10453 378376 50216270
Blood citric acid increased 24.68 23.51 5 10473 59 50594587
Psychiatric symptom 24.68 23.51 14 10464 4556 50590090
Headache 24.63 23.51 42 10436 506493 50088153
Joint swelling 24.62 23.51 10 10468 245276 50349370
Death 24.43 23.51 19 10459 325360 50269286
Anaemia 24.21 23.51 11 10467 252445 50342201

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
Dystonia 430.48 22.82 153 10399 9596 29554379
Psychotic disorder 327.72 22.82 155 10397 20199 29543776
Extrapyramidal disorder 279.66 22.82 115 10437 10716 29553259
Akathisia 260.74 22.82 96 10456 6646 29557329
Intentional self-injury 241.49 22.82 108 10444 12353 29551622
Treatment noncompliance 220.91 22.82 126 10426 24101 29539874
Neuroleptic malignant syndrome 211.86 22.82 107 10445 16041 29547934
Anosognosia 207.59 22.82 50 10502 768 29563207
Sedation 201.44 22.82 106 10446 17299 29546676
Blood prolactin abnormal 179.87 22.82 45 10507 815 29563160
Suicide attempt 167.34 22.82 120 10432 33990 29529985
Disturbance in social behaviour 166.86 22.82 49 10503 1653 29562322
Weight increased 165.23 22.82 168 10384 76499 29487476
Sexual dysfunction 164.63 22.82 66 10486 5748 29558227
Hallucination, auditory 157.11 22.82 74 10478 9519 29554456
Gynaecomastia 155.25 22.82 70 10482 8147 29555828
Dyskinesia 150.43 22.82 92 10460 19969 29544006
Blood prolactin increased 136.59 22.82 41 10511 1493 29562482
Schizophrenia 130.63 22.82 58 10494 6507 29557468
Delusion 125.99 22.82 67 10485 11149 29552826
Metabolic disorder 115.27 22.82 45 10507 3650 29560325
Mental impairment 103.77 22.82 55 10497 9086 29554889
Intentional overdose 100.77 22.82 94 10458 38434 29525541
Apathy 99.16 22.82 47 10505 6124 29557851
Loss of libido 97.29 22.82 35 10517 2261 29561714
Hyperprolactinaemia 87.96 22.82 28 10524 1242 29562733
Catatonia 87.35 22.82 39 10513 4429 29559546
Suicidal ideation 85.61 22.82 82 10470 34634 29529341
Parkinsonism 83.20 22.82 44 10508 7234 29556741
Aggression 82.11 22.82 81 10471 35460 29528515
Tachycardia 71.21 22.82 107 10445 72303 29491672
Drug ineffective 67.99 22.82 282 10270 362888 29201087
Tardive dyskinesia 66.43 22.82 34 10518 5224 29558751
Personality change 58.62 22.82 30 10522 4608 29559367
Mania 58.00 22.82 37 10515 8626 29555349
Hospitalisation 57.08 22.82 76 10476 45912 29518063
Abnormal behaviour 55.79 22.82 54 10498 23073 29540902
Paranoia 53.58 22.82 37 10515 9840 29554135
Myocarditis 52.39 22.82 38 10514 10918 29553057
Pleurothotonus 52.29 22.82 18 10534 1020 29562955
Inappropriate schedule of product administration 51.40 22.82 71 10481 44401 29519574
Persecutory delusion 49.37 22.82 21 10531 2120 29561855
Diarrhoea 49.22 22.82 29 10523 332669 29231306
Drooling 48.49 22.82 23 10529 2998 29560977
Galactorrhoea 46.00 22.82 13 10539 381 29563594
Sopor 43.56 22.82 34 10518 10900 29553075
Blood glucose increased 42.78 22.82 76 10476 58908 29505067
Muscle rigidity 39.09 22.82 30 10522 9381 29554594
Priapism 37.27 22.82 22 10530 4466 29559509
Social avoidant behaviour 37.09 22.82 19 10533 2923 29561052
Blepharospasm 37.01 22.82 14 10538 1041 29562934
Anaemia 36.66 22.82 13 10539 200938 29363037
Thinking abnormal 36.63 22.82 23 10529 5213 29558762
Salivary hypersecretion 36.11 22.82 26 10526 7383 29556592
Hallucination 35.53 22.82 60 10492 44652 29519323
Agitation 34.51 22.82 64 10488 51240 29512735
Sedation complication 34.36 22.82 14 10538 1268 29562707
Arthralgia 33.42 22.82 5 10547 139612 29424363
Tremor 33.35 22.82 78 10474 73460 29490515
Psychiatric symptom 32.88 22.82 18 10534 3166 29560809
Somnolence 32.56 22.82 90 10462 93865 29470110
Blood creatine phosphokinase increased 31.57 22.82 54 10498 40590 29523385
Sluggishness 31.03 22.82 17 10535 2994 29560981
Sepsis 30.11 22.82 7 10545 142675 29421300
Restlessness 29.63 22.82 38 10514 22107 29541868
Housebound 28.65 22.82 8 10544 224 29563751
Anion gap increased 28.37 22.82 13 10539 1567 29562408
Thrombocytopenia 27.69 22.82 7 10545 134816 29429159
Adverse drug reaction 27.21 22.82 38 10514 23982 29539993
Pain 26.63 22.82 14 10538 171418 29392557
Erectile dysfunction 25.83 22.82 32 10520 17977 29545998
Pneumonia 25.71 22.82 47 10505 320125 29243850
Blood osmolarity decreased 25.65 22.82 9 10543 540 29563435
Insurance issue 24.24 22.82 10 10542 935 29563040
Water intoxication 24.18 22.82 8 10544 401 29563574
Acute kidney injury 24.01 22.82 36 10516 265231 29298744
Drug use disorder 23.86 22.82 15 10537 3407 29560568
Trismus 23.36 22.82 13 10539 2360 29561615

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 873.51 21.23 280 15673 18585 64464194
Blood prolactin abnormal 821.38 21.23 179 15774 2553 64480226
Anosognosia 816.68 21.23 179 15774 2626 64480153
Sexual dysfunction 715.50 21.23 189 15764 6282 64476497
Disturbance in social behaviour 701.28 21.23 168 15785 3719 64479060
Metabolic disorder 609.96 21.23 173 15780 7524 64475255
Sedation 602.54 21.23 263 15690 41199 64441580
Suicide attempt 574.34 21.23 301 15652 70706 64412073
Galactorrhoea 559.35 21.23 135 15818 3084 64479695
Personality change 551.68 21.23 164 15789 8429 64474350
Dyskinesia 540.42 21.23 240 15713 39148 64443631
Intentional self-injury 404.70 21.23 179 15774 28865 64453914
Blood prolactin increased 394.40 21.23 104 15849 3424 64479355
Extrapyramidal disorder 360.38 21.23 147 15806 19405 64463374
Neuroleptic malignant syndrome 306.67 21.23 141 15812 24855 64457924
Psychotic disorder 300.39 21.23 154 15799 34424 64448355
Akathisia 295.18 21.23 110 15843 11400 64471379
Schizophrenia 272.80 21.23 103 15850 11065 64471714
Blood glucose increased 266.44 21.23 209 15744 97864 64384915
Hyperprolactinaemia 240.98 21.23 73 15880 3992 64478787
Treatment noncompliance 220.32 21.23 136 15817 43346 64439433
Intentional overdose 200.69 21.23 171 15782 89773 64393006
Hallucination, auditory 196.64 21.23 92 15861 16847 64465932
Amenorrhoea 169.46 21.23 63 15890 6476 64476303
Delusion 164.40 21.23 83 15870 17931 64464848
Insurance issue 160.02 21.23 49 15904 2777 64480002
Catatonia 156.59 21.23 62 15891 7558 64475221
Parkinsonism 121.78 21.23 63 15890 14310 64468469
Adverse drug reaction 119.19 21.23 95 15858 45369 64437410
Mental impairment 108.70 21.23 61 15892 16282 64466497
Weight increased 101.66 21.23 186 15767 213162 64269617
Gynaecomastia 99.83 21.23 42 15911 5974 64476805
Drug ineffective 95.03 21.23 434 15519 839813 63642966
Tachycardia 91.80 21.23 146 15807 149433 64333346
Diarrhoea 88.99 21.23 34 15919 722670 63760109
Tardive dyskinesia 85.80 21.23 43 15910 9135 64473644
Mania 80.03 21.23 50 15903 16236 64466543
Salivary hypersecretion 79.97 21.23 45 15908 12068 64470711
Abnormal behaviour 77.07 21.23 65 15888 33557 64449222
Agitation 74.12 21.23 100 15853 88267 64394512
Myocarditis 73.03 21.23 48 15905 16995 64465784
Aggression 70.19 21.23 71 15882 46161 64436618
Sopor 69.34 21.23 58 15895 29603 64453176
Loss of libido 65.36 21.23 24 15929 2380 64480399
Arthralgia 64.87 21.23 15 15938 442245 64040534
Pain 64.84 21.23 28 15925 553483 63929296
Apathy 64.22 21.23 38 15915 11194 64471585
Muscle rigidity 60.16 21.23 43 15910 17430 64465349
Sluggishness 57.26 21.23 28 15925 5642 64477137
Nausea 53.36 21.23 70 15883 785730 63697049
Hospitalisation 52.52 21.23 78 15875 75129 64407650
Pleurothotonus 51.76 21.23 20 15933 2282 64480497
Oculogyric crisis 49.87 21.23 20 15933 2518 64480261
Anaemia 49.58 21.23 16 15937 378664 64104115
Paranoia 48.98 21.23 37 15916 16315 64466464
Blood creatine phosphokinase increased 48.67 21.23 66 15887 58492 64424287
Condition aggravated 48.32 21.23 201 15752 372225 64110554
Sinus tachycardia 48.06 21.23 49 15904 32139 64450640
Suicidal ideation 47.89 21.23 70 15883 66472 64416307
Somnolence 45.75 21.23 132 15821 203513 64279266
Psychiatric symptom 43.30 21.23 24 15929 6249 64476530
Psychotic symptom 42.53 21.23 17 15936 2121 64480658
Fatigue 41.88 21.23 76 15877 748654 63734125
Dyspnoea 41.04 21.23 72 15881 718602 63764177
Hallucination 40.45 21.23 68 15885 72720 64410059
Polydipsia 39.44 21.23 22 15931 5799 64476980
Breast enlargement 38.72 21.23 14 15939 1328 64481451
Pruritus 37.80 21.23 15 15938 312385 64170394
Peripheral swelling 37.56 21.23 4 15949 209149 64273630
Tremor 37.13 21.23 100 15853 148130 64334649
Headache 37.06 21.23 46 15907 529421 63953358
Pain in extremity 35.94 21.23 15 15938 303070 64179709
Myelocyte count increased 34.07 21.23 11 15942 741 64482038
Drooling 33.06 21.23 19 15934 5300 64477479
Metamyelocyte count increased 31.79 21.23 10 15943 619 64482160
Rhabdomyolysis 31.63 21.23 70 15883 91656 64391123
Overdose 31.63 21.23 99 15854 159467 64323312
Pneumonia 31.05 21.23 57 15896 559519 63923260
Cough 29.81 21.23 19 15934 302129 64180650
Drug hypersensitivity 29.45 21.23 11 15942 237804 64244975
Urinary tract infection 28.20 21.23 11 15942 231585 64251194
Completed suicide 28.16 21.23 120 15833 224294 64258485
Lactate pyruvate ratio increased 27.95 21.23 6 15947 79 64482700
General physical health deterioration 27.87 21.23 8 15945 204417 64278362
Thinking abnormal 27.83 21.23 23 15930 11533 64471246
Granulocytopenia 27.73 21.23 22 15931 10418 64472361
Personality disorder 27.09 21.23 16 15937 4695 64478084
Inappropriate schedule of product administration 26.96 21.23 66 15887 92220 64390559
Thrombocytopenia 26.64 21.23 11 15942 223790 64258989
Joint swelling 26.60 21.23 10 15943 215372 64267407
Inappropriate antidiuretic hormone secretion 26.36 21.23 30 15923 22259 64460520
Persecutory delusion 26.24 21.23 15 15938 4143 64478636
Schizoaffective disorder 26.06 21.23 11 15942 1576 64481203
Housebound 26.05 21.23 8 15945 457 64482322
Restlessness 25.96 21.23 40 15913 39745 64443034
Infection 25.64 21.23 7 15946 184873 64297906
Electrocardiogram QT prolonged 25.57 21.23 59 15894 79389 64403390
Alopecia 25.50 21.23 5 15948 165685 64317094
Blood osmolarity decreased 25.33 21.23 10 15943 1208 64481571
Anion gap increased 24.79 21.23 13 15940 3031 64479748
Disease progression 24.70 21.23 3 15950 141677 64341102
Personality change due to a general medical condition 24.40 21.23 6 15947 148 64482631
Back pain 24.30 21.23 16 15937 250155 64232624
Antipsychotic drug level decreased 24.10 21.23 9 15944 935 64481844
Blood citric acid increased 23.79 21.23 5 15948 59 64482720
Blepharospasm 23.53 21.23 13 15940 3362 64479417
Slow speech 23.43 21.23 11 15942 2026 64480753
Nasopharyngitis 22.75 21.23 10 15943 196063 64286716
Epileptic encephalopathy 22.74 21.23 7 15946 403 64482376
Torticollis 22.73 21.23 11 15942 2166 64480613
Monocyte count decreased 22.70 21.23 12 15941 2845 64479934
Behaviour disorder 22.68 21.23 14 15939 4448 64478331
Social avoidant behaviour 22.40 21.23 14 15939 4543 64478236
Metabolic syndrome 21.94 21.23 11 15942 2337 64480442

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 D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D065127 Dopamine D2 Receptor Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D058830 Serotonin 5-HT2 Receptor Antagonists
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:35471 psychotropic drugs
CHEBI has role CHEBI:37890 alpha-adrenergic receptor blockaders
CHEBI has role CHEBI:37955 H1 receptor antagonists
CHEBI has role CHEBI:48279 serotonin antagonists
CHEBI has role CHEBI:48561 dopaminergic antagonists
CHEBI has role CHEBI:49103 drug metabolites
CHEBI has role CHEBI:63726 neuroprotective agents
CHEBI has role CHEBI:65191 atypical antipsychotic agent

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
D(1A) dopamine receptor GPCR Ki 7.39 PDSP
Alpha-2A adrenergic receptor GPCR Ki 7.93 PDSP
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.89 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 5.43 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
5-hydroxytryptamine receptor 7 GPCR Ki 8.57 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
Beta-1 adrenergic receptor GPCR Ki 5.30 PDSP
Histamine H1 receptor GPCR Ki 8.25 PDSP
Histamine H2 receptor GPCR Ki 6.92 PDSP
Histamine H4 receptor GPCR Ki 5.06 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 7.64 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
D(1B) dopamine receptor GPCR Ki 7.54 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP

External reference:

IDSource
4025875 VUID
N0000176080 NUI
D05339 KEGG_DRUG
4025875 VANDF
C0753678 UMLSCUI
CHEBI:82978 CHEBI
CHEMBL1621 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
117004004 SNOMEDCT_US
425483000 SNOMEDCT_US
426276000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3978 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3978 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3979 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3979 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3980 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3980 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3981 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3981 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 33 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3692 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3692 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3693 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3693 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3694 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3694 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3695 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3695 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6935 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6935 TABLET, EXTENDED RELEASE 3 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6936 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6936 TABLET, EXTENDED RELEASE 6 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6937 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6937 TABLET, EXTENDED RELEASE 9 mg ORAL ANDA 31 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0951 TABLET, EXTENDED RELEASE 1.50 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0951 TABLET, EXTENDED RELEASE 1.50 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0952 TABLET, EXTENDED RELEASE 3 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0952 TABLET, EXTENDED RELEASE 3 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0953 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0953 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0954 TABLET, EXTENDED RELEASE 9 mg ORAL NDA 35 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0954 TABLET, EXTENDED RELEASE 9 mg ORAL NDA 35 sections