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) 0.03 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

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 1166.69 25.43 234 12044 2845 63473899
Anosognosia 1075.04 25.43 220 12058 2976 63473768
Sexual dysfunction 1023.76 25.43 223 12055 4136 63472608
Galactorrhoea 1017.49 25.43 220 12058 3935 63472809
Disturbance in social behaviour 1003.57 25.43 216 12062 3777 63472967
Metabolic disorder 914.21 25.43 219 12059 6284 63470460
Dystonia 908.07 25.43 254 12024 13565 63463179
Personality change 838.06 25.43 207 12071 6766 63469978
Sedation 787.89 25.43 292 11986 38517 63438227
Dyskinesia 743.32 25.43 266 12012 31736 63445008
Suicide attempt 712.58 25.43 308 11970 60610 63416134
Blood prolactin increased 694.19 25.43 156 12122 3347 63473397
Blood glucose increased 444.34 25.43 247 12031 83509 63393235
Amenorrhoea 358.26 25.43 115 12163 9799 63466945
Hyperprolactinaemia 341.45 25.43 90 12188 3810 63472934
Extrapyramidal disorder 287.60 25.43 105 12173 13179 63463565
Schizophrenia 212.92 25.43 78 12200 9874 63466870
Psychotic disorder 178.81 25.43 91 12187 25621 63451123
Akathisia 171.20 25.43 65 12213 9081 63467663
Intentional self-injury 158.77 25.43 84 12194 25603 63451141
Insurance issue 153.60 25.43 54 12224 6067 63470677
Treatment noncompliance 149.67 25.43 92 12186 37233 63439511
Breast discharge 146.81 25.43 35 12243 976 63475768
Neuroleptic malignant syndrome 143.88 25.43 62 12216 11994 63464750
Hallucination, auditory 136.98 25.43 61 12217 12763 63463981
Catatonia 129.79 25.43 44 12234 4433 63472311
Intentional overdose 126.79 25.43 109 12169 74043 63402701
Tardive dyskinesia 125.91 25.43 51 12227 8451 63468293
Delusion 121.46 25.43 55 12223 11962 63464782
Adverse drug reaction 100.82 25.43 99 12179 79615 63397129
Drug ineffective 93.63 25.43 423 11855 1044342 62432402
Diarrhoea 82.21 25.43 19 12259 715347 62761397
Personality change due to a general medical condition 73.44 25.43 15 12263 199 63476545
Pain 70.07 25.43 28 12250 740600 62736144
Agitation 69.60 25.43 71 12207 59686 63417058
Mania 69.54 25.43 38 12240 12329 63464415
Weight increased 67.66 25.43 153 12125 260639 63216105
Condition aggravated 67.28 25.43 200 12078 402017 63074727
Parkinsonism 66.91 25.43 35 12243 10404 63466340
Oculogyric crisis 66.39 25.43 21 12257 1700 63475044
Arthralgia 63.67 25.43 16 12262 569694 62907050
Aggression 60.50 25.43 44 12234 23454 63453290
Hospitalisation 59.99 25.43 78 12200 85003 63391741
Completed suicide 55.07 25.43 100 12178 145573 63331171
Nausea 54.83 25.43 51 12227 854420 62622324
Salivary hypersecretion 47.13 25.43 25 12253 7641 63469103
Breast enlargement 47.10 25.43 16 12262 1620 63475124
Tremor 46.48 25.43 88 12190 132151 63344593
Personality disorder 44.58 25.43 22 12256 5789 63470955
Tachycardia 44.49 25.43 81 12197 118075 63358669
Fatigue 44.05 25.43 65 12213 887963 62588781
Psychotic symptom 43.90 25.43 15 12263 1546 63475198
Abnormal behaviour 43.87 25.43 35 12243 21391 63455353
Overdose 43.47 25.43 79 12199 114999 63361745
Alopecia 40.62 25.43 8 12270 337528 63139216
Drug hypersensitivity 40.38 25.43 6 12272 310681 63166063
Metabolic syndrome 39.79 25.43 14 12264 1574 63475170
Pain in extremity 39.59 25.43 8 12270 331478 63145266
Paranoia 37.38 25.43 25 12253 11654 63465090
Suicidal ideation 36.08 25.43 52 12226 62369 63414375
Joint swelling 35.02 25.43 10 12268 327656 63149088
Headache 34.72 25.43 43 12235 633198 62843546
Psychotic behaviour 34.69 25.43 10 12268 590 63476154
Muscle rigidity 32.97 25.43 23 12255 11477 63465267
Sinusitis 32.86 25.43 3 12275 226650 63250094
Somnolence 32.78 25.43 92 12186 178593 63298151
Sinus tachycardia 32.25 25.43 31 12247 24237 63452507
Monocyte count decreased 32.16 25.43 13 12265 2140 63474604
Polydipsia 31.90 25.43 15 12263 3549 63473195
Anger 31.32 25.43 23 12255 12433 63464311
Mental impairment 30.87 25.43 24 12254 14127 63462617
Rash 30.81 25.43 38 12240 560833 62915911
Infection 30.77 25.43 4 12274 229169 63247575
Ovarian germ cell cancer stage II 29.86 25.43 6 12272 73 63476671
Blood creatine phosphokinase increased 29.81 25.43 33 12245 30397 63446347
Pneumonia 29.49 25.43 27 12251 456740 63020004
Schizoaffective disorder 28.86 25.43 14 12264 3548 63473196
Lactate pyruvate ratio increased 28.69 25.43 6 12272 90 63476654
Peripheral swelling 28.62 25.43 8 12270 265934 63210810
Nasopharyngitis 28.60 25.43 7 12271 254250 63222494
Anaemia 27.78 25.43 11 12267 293419 63183325
Abdominal discomfort 27.30 25.43 14 12264 320871 63155873
Death 26.78 25.43 20 12258 374361 63102383
Epileptic encephalopathy 26.68 25.43 7 12271 290 63476454
Electrocardiogram QT prolonged 26.55 25.43 44 12234 59486 63417258
Psychiatric symptom 26.49 25.43 15 12263 5208 63471536
Diabetes insipidus 26.47 25.43 12 12266 2613 63474131
Eosinophilic pleural effusion 25.96 25.43 5 12273 48 63476696
General physical health deterioration 25.90 25.43 4 12274 201398 63275346

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 564.71 23.27 190 12429 9990 34934322
Dystonia 472.30 23.27 169 12450 10676 34933636
Psychotic disorder 348.68 23.27 172 12447 24280 34920032
Treatment noncompliance 309.10 23.27 166 12453 27934 34916378
Extrapyramidal disorder 304.94 23.27 129 12490 12751 34931561
Akathisia 295.93 23.27 111 12508 7998 34936314
Intentional self-injury 258.02 23.27 117 12502 13654 34930658
Weight increased 255.45 23.27 234 12385 92799 34851513
Anosognosia 248.93 23.27 60 12559 913 34943399
Sedation 241.91 23.27 128 12491 20878 34923434
Neuroleptic malignant syndrome 234.43 23.27 119 12500 17815 34926497
Sexual dysfunction 221.67 23.27 84 12535 6219 34938093
Blood prolactin abnormal 218.59 23.27 54 12565 915 34943397
Disturbance in social behaviour 197.23 23.27 57 12562 1794 34942518
Suicide attempt 173.24 23.27 130 12489 38986 34905326
Hallucination, auditory 170.18 23.27 84 12535 11833 34932479
Emotional disorder 168.41 23.27 67 12552 5649 34938663
Dyskinesia 167.48 23.27 103 12516 22310 34922002
Delusion 165.53 23.27 84 12535 12551 34931761
Hyperprolactinaemia 164.95 23.27 48 12571 1548 34942764
Blood prolactin increased 147.43 23.27 45 12574 1715 34942597
Metabolic disorder 146.68 23.27 56 12563 4227 34940085
Schizophrenia 138.53 23.27 66 12553 8600 34935712
Intentional overdose 112.08 23.27 106 12513 43568 34900744
Mental impairment 110.59 23.27 60 12559 10262 34934050
Apathy 108.37 23.27 52 12567 6880 34937432
Aggression 106.59 23.27 98 12521 38866 34905446
Loss of libido 104.32 23.27 38 12581 2514 34941798
Drug ineffective 89.94 23.27 363 12256 456388 34487924
Suicidal ideation 88.62 23.27 90 12529 40298 34904014
Catatonia 85.61 23.27 40 12579 4985 34939327
Personality change 84.75 23.27 40 12579 5099 34939213
Tachycardia 80.45 23.27 124 12495 84648 34859664
Persecutory delusion 78.63 23.27 31 12588 2549 34941763
Parkinsonism 78.09 23.27 44 12575 8094 34936218
Galactorrhoea 76.44 23.27 20 12599 430 34943882
Myocarditis 70.76 23.27 50 12569 13632 34930680
Obesity 68.78 23.27 48 12571 12830 34931482
Hospitalisation 68.20 23.27 93 12526 56809 34887503
Paranoia 66.85 23.27 46 12573 12022 34932290
Abnormal behaviour 66.69 23.27 62 12557 24907 34919405
Diarrhoea 66.44 23.27 29 12590 389883 34554429
Mania 64.17 23.27 41 12578 9470 34934842
Tardive dyskinesia 62.96 23.27 34 12585 5756 34938556
Salivary hypersecretion 60.16 23.27 38 12581 8606 34935706
Psychotic symptom 56.84 23.27 22 12597 1721 34942591
Abnormal weight gain 56.06 23.27 19 12600 1015 34943297
Hallucination 52.59 23.27 78 12541 51420 34892892
Drooling 51.73 23.27 25 12594 3357 34940955
Pleurothotonus 49.46 23.27 18 12601 1187 34943125
Emotional distress 49.44 23.27 42 12577 14984 34929328
Tremor 48.62 23.27 98 12521 82489 34861823
Blood glucose increased 47.70 23.27 86 12533 66632 34877680
Anaemia 45.30 23.27 14 12605 233321 34710991
Priapism 45.21 23.27 26 12593 4968 34939344
Muscle rigidity 44.37 23.27 34 12585 10484 34933828
Somnolence 44.36 23.27 113 12506 111003 34833309
Rhabdomyolysis 43.88 23.27 84 12535 68079 34876233
Hypometabolism 43.82 23.27 10 12609 118 34944194
Sluggishness 43.25 23.27 22 12597 3295 34941017
Thinking abnormal 42.75 23.27 27 12592 6110 34938202
Sedation complication 42.67 23.27 18 12601 1759 34942553
Sopor 42.15 23.27 35 12584 12101 34932211
Blood creatine phosphokinase increased 41.63 23.27 65 12554 44792 34899520
Inappropriate schedule of product administration 41.62 23.27 78 12541 62218 34882094
Arthralgia 41.55 23.27 6 12613 170035 34774277
Social avoidant behaviour 38.71 23.27 20 12599 3094 34941218
Sepsis 38.19 23.27 7 12612 166554 34777758
Sinus tachycardia 36.80 23.27 38 12581 17322 34926990
Pneumonia 36.04 23.27 47 12572 362580 34581732
Blepharospasm 35.82 23.27 14 12605 1124 34943188
Thrombocytopenia 34.89 23.27 7 12612 156240 34788072
Agitation 34.82 23.27 69 12550 57330 34886982
Death 32.46 23.27 59 12560 397990 34546322
Water intoxication 31.86 23.27 10 12609 418 34943894
Psychiatric symptom 31.03 23.27 18 12601 3495 34940817
Adverse drug reaction 30.73 23.27 45 12574 29297 34915015
Restlessness 29.51 23.27 41 12578 25441 34918871
Antipsychotic drug level increased 29.44 23.27 18 12601 3847 34940465
Acute kidney injury 28.79 23.27 41 12578 304947 34639365
Pruritus 28.47 23.27 8 12611 141973 34802339
Housebound 28.36 23.27 8 12611 230 34944082
Drug use disorder 28.10 23.27 18 12601 4173 34940139
Dyspnoea 27.97 23.27 59 12560 376723 34567589
Postoperative respiratory failure 27.14 23.27 7 12612 142 34944170
Inappropriate affect 27.00 23.27 10 12609 693 34943619
Erectile dysfunction 26.63 23.27 35 12584 20602 34923710
Hyperinsulinaemic hypoglycaemia 26.20 23.27 6 12613 72 34944240
Delusional perception 26.02 23.27 7 12612 168 34944144
Anion gap increased 25.96 23.27 13 12606 1883 34942429
Disease progression 25.95 23.27 4 12615 108073 34836239
Blood osmolarity decreased 25.20 23.27 9 12610 562 34943750
General physical health deterioration 24.32 23.27 8 12611 128261 34816051
Hallucination, visual 24.25 23.27 31 12588 17760 34926552
Cough 24.18 23.27 12 12607 150128 34794184
Pain 24.15 23.27 23 12596 204652 34739660
Completed suicide 24.03 23.27 84 12535 98084 34846228
Delirium 23.27 23.27 50 12569 43941 34900371

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
Blood prolactin abnormal 1146.80 23.13 246 18881 3355 79721906
Anosognosia 1141.57 23.13 247 18880 3517 79721744
Dystonia 1131.83 23.13 349 18778 21050 79704211
Sexual dysfunction 1052.57 23.13 265 18862 7498 79717763
Disturbance in social behaviour 1009.34 23.13 235 18892 4735 79720526
Metabolic disorder 899.29 23.13 242 18885 8928 79716333
Sedation 846.64 23.13 354 18773 51541 79673720
Personality change 805.81 23.13 227 18900 9943 79715318
Dyskinesia 752.29 23.13 312 18815 44461 79680800
Suicide attempt 731.77 23.13 369 18758 82563 79642698
Galactorrhoea 592.37 23.13 144 18983 3502 79721759
Intentional self-injury 432.31 23.13 192 18935 32227 79693034
Blood prolactin increased 422.09 23.13 112 19015 3899 79721362
Extrapyramidal disorder 414.42 23.13 168 18959 22511 79702750
Blood glucose increased 393.58 23.13 278 18849 114697 79610564
Gynaecomastia 387.57 23.13 121 19006 7560 79717701
Akathisia 344.86 23.13 127 19000 13132 79712129
Neuroleptic malignant syndrome 338.03 23.13 154 18973 27405 79697856
Hyperprolactinaemia 328.07 23.13 95 19032 4581 79720680
Psychotic disorder 312.09 23.13 166 18961 41236 79684025
Treatment noncompliance 304.85 23.13 177 18950 52091 79673170
Schizophrenia 267.04 23.13 110 19017 15330 79709931
Delusion 221.99 23.13 105 19022 20318 79704943
Hallucination, auditory 217.62 23.13 104 19023 20589 79704672
Intentional overdose 208.31 23.13 185 18942 105775 79619486
Amenorrhoea 175.64 23.13 67 19060 7625 79717636
Catatonia 170.68 23.13 68 19059 8688 79716573
Drug ineffective 168.39 23.13 603 18524 1080310 78644951
Insurance issue 160.49 23.13 58 19069 5675 79719586
Adverse drug reaction 142.63 23.13 122 19005 66270 79658991
Weight increased 141.75 23.13 245 18882 277141 79448120
Parkinsonism 134.84 23.13 70 19057 16514 79708747
Mental impairment 117.64 23.13 67 19060 18969 79706292
Diarrhoea 115.92 23.13 34 19093 880455 78844806
Salivary hypersecretion 112.66 23.13 59 19068 14165 79711096
Tachycardia 104.04 23.13 167 18960 177601 79547660
Tardive dyskinesia 98.70 23.13 49 19078 10522 79714739
Aggression 98.09 23.13 88 19039 50870 79674391
Abnormal behaviour 95.11 23.13 75 19052 36346 79688915
Myocarditis 91.89 23.13 60 19067 21673 79703588
Mania 88.62 23.13 55 19072 18205 79707056
Arthralgia 87.16 23.13 16 19111 571787 79153474
Psychotic symptom 81.95 23.13 29 19098 2668 79722593
Agitation 77.41 23.13 107 19020 99608 79625653
Pain 76.11 23.13 37 19090 703765 79021496
Loss of libido 74.53 23.13 27 19100 2658 79722603
Apathy 73.06 23.13 43 19084 12934 79712327
Nausea 71.31 23.13 75 19052 957121 78768140
Muscle rigidity 69.98 23.13 49 19078 19833 79705428
Sluggishness 68.97 23.13 33 19094 6539 79718722
Sopor 67.49 23.13 59 19068 32951 79692310
Hospitalisation 67.04 23.13 97 19030 94139 79631122
Sinus tachycardia 65.66 23.13 61 19066 36847 79688414
Paranoia 64.02 23.13 46 19081 19386 79705875
Blood creatine phosphokinase increased 63.84 23.13 79 19048 66011 79659250
Emotional disorder 61.50 23.13 40 19087 14347 79710914
Somnolence 60.81 23.13 159 18968 238822 79486439
Anaemia 58.72 23.13 17 19110 444998 79280263
Condition aggravated 58.23 23.13 256 18871 500868 79224393
Personality change due to a general medical condition 57.41 23.13 13 19114 229 79725032
Hallucination 56.29 23.13 85 19042 85660 79639601
Fatigue 55.55 23.13 86 19041 929641 78795620
Rhabdomyolysis 55.02 23.13 93 19034 103038 79622223
Suicidal ideation 54.90 23.13 79 19048 76261 79649000
Tremor 54.83 23.13 124 19003 169959 79555302
Headache 52.30 23.13 48 19079 653724 79071537
Dyspnoea 51.44 23.13 79 19048 856946 78868315
Oculogyric crisis 50.90 23.13 21 19106 2931 79722330
Pleurothotonus 50.63 23.13 20 19107 2496 79722765
Pruritus 50.38 23.13 16 19111 394632 79330629
Peripheral swelling 49.63 23.13 4 19123 269613 79455648
Pain in extremity 46.13 23.13 15 19112 364523 79360738
Psychiatric symptom 44.09 23.13 25 19102 7010 79718251
Completed suicide 43.75 23.13 144 18983 245623 79479638
Polydipsia 42.83 23.13 24 19103 6581 79718680
Drooling 42.43 23.13 23 19104 5911 79719350
Pneumonia 41.37 23.13 59 19068 660187 79065074
Breast enlargement 40.48 23.13 15 19112 1574 79723687
Drug hypersensitivity 40.17 23.13 11 19116 298905 79426356
Joint swelling 39.98 23.13 10 19117 288636 79436625
Overdose 39.32 23.13 115 19012 184091 79541170
Metabolic syndrome 38.97 23.13 17 19110 2723 79722538
Alopecia 38.52 23.13 5 19122 231350 79493911
Thinking abnormal 38.49 23.13 29 19098 13132 79712129
General physical health deterioration 37.23 23.13 10 19117 275228 79450033
Infection 36.25 23.13 7 19120 241705 79483556
Drug abuse 36.10 23.13 103 19024 162588 79562673
Hypometabolism 35.94 23.13 8 19119 130 79725131
Cough 35.60 23.13 22 19105 366767 79358494
Myelocyte count increased 34.16 23.13 11 19116 758 79724503
Personality disorder 33.64 23.13 20 19107 6126 79719135
Thrombocytopenia 33.39 23.13 11 19116 265248 79460013
Abnormal weight gain 33.09 23.13 15 19112 2629 79722632
Nasopharyngitis 32.90 23.13 10 19117 253871 79471390
Obesity 32.33 23.13 41 19086 35084 79690177
Persecutory delusion 32.27 23.13 18 19109 4891 79720370
Metamyelocyte count increased 31.92 23.13 10 19117 630 79724631
Urinary tract infection 31.83 23.13 13 19114 274499 79450762
Restlessness 31.80 23.13 47 19080 46445 79678816
Electrocardiogram QT prolonged 31.47 23.13 68 19059 90318 79634943
Torticollis 31.33 23.13 14 19113 2373 79722888
Back pain 31.28 23.13 17 19110 304163 79421098
Monocyte count decreased 30.36 23.13 15 19112 3186 79722075
Rash 30.32 23.13 58 19069 578300 79146961
Sedation complication 30.01 23.13 27 19100 15642 79709619
Inappropriate antidiuretic hormone secretion 29.59 23.13 34 19093 26279 79698982
Antipsychotic drug level increased 29.04 23.13 18 19109 5939 79719322
Hallucination, visual 28.24 23.13 37 19090 32692 79692569
Lactate pyruvate ratio increased 28.13 23.13 6 19121 79 79725182
Decreased appetite 27.48 23.13 25 19102 342393 79382868
Postoperative respiratory failure 27.21 23.13 7 19120 215 79725046
Abdominal pain upper 26.93 23.13 10 19117 223809 79501452
Breast discharge 26.89 23.13 9 19118 700 79724561
Erythema 26.83 23.13 10 19117 223280 79501981
Emotional distress 26.75 23.13 40 19087 39929 79685332
Vomiting 26.71 23.13 77 19050 665751 79059510
Granulocytopenia 26.57 23.13 22 19105 11409 79713852
Housebound 26.11 23.13 8 19119 468 79724793
Accidental exposure to product by child 25.65 23.13 13 19114 2913 79722348
Behaviour disorder 25.63 23.13 17 19110 6296 79718965
Antipsychotic drug level decreased 25.58 23.13 10 19117 1214 79724047
Anion gap increased 25.44 23.13 14 19113 3706 79721555
Death 25.38 23.13 62 19065 566452 79158809
Abdominal pain 25.16 23.13 34 19093 389535 79335726
Stomatitis 24.84 23.13 3 19124 146754 79578507
Blood osmolarity decreased 24.77 23.13 10 19117 1321 79723940
Social avoidant behaviour 24.62 23.13 15 19112 4799 79720462
Disease progression 24.35 23.13 7 19120 184355 79540906
Hyperinsulinaemic hypoglycaemia 24.13 23.13 6 19121 160 79725101
Blood citric acid increased 23.95 23.13 5 19122 59 79725202
Increased appetite 23.65 23.13 21 19106 11957 79713304
Rebound psychosis 23.59 23.13 7 19120 367 79724894
Antipsychotic drug level above therapeutic 23.53 23.13 11 19116 2069 79723192
Diabetes insipidus 23.46 23.13 15 19112 5222 79720039
Inappropriate affect 23.38 23.13 10 19117 1526 79723735
Schizoaffective disorder 23.17 23.13 11 19116 2141 79723120

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
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
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
5-hydroxytryptamine receptor 1E GPCR Ki 5.99 PDSP
D(1B) dopamine receptor GPCR Ki 7.54 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
Prostaglandin E2 receptor EP3 subtype GPCR Ki 5 PDSP
D(3) dopamine receptor GPCR Ki 9.05 PDSP
Beta-1 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
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 0378-3978 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 0378-3979 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 0378-3980 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 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 10147-0951 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