paliperidone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antipsychotics, risperidone derivatives	4137	144598-75-4

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
6	mg	O
2.50	mg	P

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
June 25, 2007	EMA
Dec. 19, 2006	FDA	JANSSEN PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Galactorrhoea	1010.99	23.89	217	10863	3678	56277309
Blood prolactin abnormal	827.29	23.89	167	10913	2058	56278929
Anosognosia	740.15	23.89	153	10927	2136	56278851
Sexual dysfunction	696.75	23.89	156	10924	3232	56277755
Disturbance in social behaviour	674.66	23.89	149	10931	2892	56278095
Blood prolactin increased	667.57	23.89	150	10930	3159	56277828
Dystonia	658.64	23.89	194	10886	12227	56268760
Schizophrenia	641.05	23.89	183	10897	10316	56270671
Metabolic disorder	602.76	23.89	152	10928	5309	56275678
Personality change	563.94	23.89	146	10934	5671	56275316
Sedation	524.11	23.89	212	10868	34642	56246345
Suicide attempt	514.61	23.89	243	10837	57593	56223394
Dyskinesia	507.30	23.89	197	10883	28911	56252076
Amenorrhoea	342.49	23.89	109	10971	8877	56272110
Hyperprolactinaemia	316.75	23.89	84	10996	3577	56277410
Blood glucose increased	285.83	23.89	180	10900	74971	56206016
Extrapyramidal disorder	270.79	23.89	99	10981	12257	56268730
Psychotic disorder	224.56	23.89	104	10976	23454	56257533
Akathisia	162.74	23.89	62	11018	8590	56272397
Intentional self-injury	159.57	23.89	84	10996	24908	56256079
Treatment noncompliance	151.71	23.89	89	10991	32534	56248453
Breast discharge	145.69	23.89	34	11046	847	56280140
Insurance issue	144.41	23.89	46	11034	3746	56277241
Neuroleptic malignant syndrome	142.46	23.89	61	11019	11417	56269570
Hallucination, auditory	135.67	23.89	59	11021	11465	56269522
Intentional overdose	131.14	23.89	108	10972	68009	56212978
Catatonia	118.33	23.89	40	11040	3924	56277063
Delusion	114.61	23.89	52	11028	11163	56269824
Tardive dyskinesia	110.72	23.89	46	11034	7985	56273002
Adverse drug reaction	83.21	23.89	82	10998	65050	56215937
Agitation	72.40	23.89	71	11009	55965	56225022
Diarrhoea	71.30	23.89	19	11061	638488	55642499
Oculogyric crisis	68.54	23.89	21	11059	1503	56279484
Weight increased	68.47	23.89	144	10936	229559	56051428
Mania	65.85	23.89	36	11044	11484	56269503
Pain	61.48	23.89	27	11053	663157	55617830
Parkinsonism	60.64	23.89	32	11048	9514	56271473
Aggression	57.81	23.89	42	11038	21964	56259023
Arthralgia	55.80	23.89	15	11065	501654	55779333
Hospitalisation	53.85	23.89	70	11010	74930	56206057
Schizoaffective disorder	51.39	23.89	20	11060	2929	56278058
Salivary hypersecretion	48.69	23.89	25	11055	7025	56273962
Tremor	48.37	23.89	86	10994	121003	56159984
Nausea	48.07	23.89	48	11032	764130	55516857
Tachycardia	45.94	23.89	78	11002	105798	56175189
Psychotic symptom	45.57	23.89	15	11065	1354	56279633
Breast enlargement	44.61	23.89	15	11065	1446	56279541
Drug ineffective	43.16	23.89	318	10762	918671	55362316
Condition aggravated	42.88	23.89	157	10923	344741	55936246
Overdose	40.76	23.89	74	11006	105756	56175231
Abnormal behaviour	40.75	23.89	33	11047	20239	56260748
Completed suicide	36.46	23.89	81	10999	133752	56147235
Suicidal ideation	35.51	23.89	50	11030	57692	56223295
Drug hypersensitivity	35.07	23.89	6	11074	275199	56005788
Fatigue	34.89	23.89	64	11016	788488	55492499
Pain in extremity	34.74	23.89	8	11072	297423	55983564
Personality disorder	34.73	23.89	18	11062	5155	56275832
Psychotic behaviour	34.54	23.89	10	11070	588	56280399
Alopecia	34.06	23.89	8	11072	293450	55987537
Paranoia	34.03	23.89	23	11057	10721	56270266
Monocyte count decreased	33.12	23.89	13	11067	1947	56279040
Mental impairment	32.77	23.89	24	11056	12698	56268289
Anger	32.30	23.89	23	11057	11649	56269338
Somnolence	31.87	23.89	87	10993	163326	56117661
Blood creatine phosphokinase increased	31.65	23.89	33	11047	27919	56253068
Polydipsia	29.91	23.89	14	11066	3221	56277766
Metabolic syndrome	29.89	23.89	11	11069	1382	56279605
Joint swelling	29.73	23.89	10	11070	289790	55991197
Muscle rigidity	29.47	23.89	21	11059	10650	56270337
Electrocardiogram QT prolonged	28.83	23.89	44	11036	54544	56226443
Lactate pyruvate ratio increased	28.58	23.89	6	11074	90	56280897
Personality change due to a general medical condition	28.28	23.89	6	11074	95	56280892
Sinusitis	28.26	23.89	3	11077	197578	56083409
Sinus tachycardia	28.15	23.89	28	11052	22416	56258571
Peripheral swelling	28.03	23.89	6	11074	234720	56046267
Ovarian germ cell cancer stage II	27.94	23.89	5	11075	30	56280957
Headache	27.80	23.89	42	11038	559002	55721985
Epileptic encephalopathy	26.61	23.89	7	11073	288	56280699
Infection	26.31	23.89	4	11076	200202	56080785
Sopor	26.05	23.89	26	11054	20896	56260091
Eosinophilic pleural effusion	25.87	23.89	5	11075	48	56280939
Nasopharyngitis	25.67	23.89	6	11074	220953	56060034
Breast tenderness	25.29	23.89	11	11069	2134	56278853
Sluggishness	25.06	23.89	14	11066	4654	56276333
Pneumonia	25.00	23.89	26	11054	407072	55873915
Blood citric acid increased	24.93	23.89	5	11075	59	56280928
Psychiatric symptom	24.58	23.89	14	11066	4830	56276157
Rash	24.53	23.89	37	11043	493010	55787977
Anaemia	24.51	23.89	11	11069	267500	56013487
Diabetes insipidus	23.94	23.89	11	11069	2426	56278561

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Schizophrenia	476.84	23.62	170	11244	10660	31675270
Dystonia	436.91	23.62	157	11257	10068	31675862
Psychotic disorder	364.33	23.62	172	11242	22121	31663809
Gynaecomastia	333.39	23.62	125	11289	9029	31676901
Extrapyramidal disorder	285.95	23.62	120	11294	11658	31674272
Akathisia	271.20	23.62	101	11313	7152	31678778
Intentional self-injury	268.55	23.62	119	11295	13196	31672734
Treatment noncompliance	261.38	23.62	144	11270	25540	31660390
Neuroleptic malignant syndrome	215.15	23.62	110	11304	16759	31669171
Anosognosia	211.35	23.62	51	11363	782	31685148
Sedation	203.02	23.62	110	11304	18855	31667075
Weight increased	194.41	23.62	191	11223	82756	31603174
Sexual dysfunction	186.73	23.62	73	11341	5895	31680035
Blood prolactin abnormal	183.70	23.62	46	11368	828	31685102
Hallucination, auditory	175.39	23.62	82	11332	10278	31675652
Disturbance in social behaviour	169.06	23.62	50	11364	1713	31684217
Suicide attempt	159.07	23.62	121	11293	37127	31648803
Dyskinesia	151.16	23.62	94	11320	20816	31665114
Delusion	149.35	23.62	77	11337	11920	31674010
Blood prolactin increased	138.18	23.62	42	11372	1582	31684348
Hyperprolactinaemia	128.74	23.62	39	11375	1452	31684478
Metabolic disorder	118.64	23.62	47	11367	3927	31682003
Intentional overdose	107.49	23.62	101	11313	41288	31644642
Apathy	102.60	23.62	49	11365	6433	31679497
Mental impairment	101.12	23.62	55	11359	9477	31676453
Loss of libido	95.53	23.62	35	11379	2360	31683570
Suicidal ideation	89.11	23.62	86	11328	36320	31649610
Catatonia	84.22	23.62	39	11375	4775	31681155
Aggression	83.66	23.62	84	11330	37207	31648723
Parkinsonism	80.82	23.62	44	11370	7592	31678338
Tachycardia	73.28	23.62	112	11302	76095	31609835
Drug ineffective	72.40	23.62	307	11107	395266	31290664
Persecutory delusion	67.35	23.62	27	11387	2325	31683605
Abnormal behaviour	67.35	23.62	61	11353	23767	31662163
Tardive dyskinesia	64.35	23.62	34	11380	5525	31680405
Galactorrhoea	63.40	23.62	17	11397	404	31685526
Mania	63.11	23.62	40	11374	9137	31676793
Personality change	60.29	23.62	31	11383	4764	31681166
Emotional disorder	57.65	23.62	31	11383	5218	31680712
Hospitalisation	56.23	23.62	79	11335	49728	31636202
Myocarditis	55.94	23.62	41	11373	11859	31674071
Paranoia	55.66	23.62	39	11375	10516	31675414
Diarrhoea	55.52	23.62	29	11385	352380	31333550
Salivary hypersecretion	53.67	23.62	34	11380	7758	31678172
Pleurothotonus	51.38	23.62	18	11396	1065	31684865
Drooling	50.81	23.62	24	11390	3071	31682859
Inappropriate schedule of product administration	46.43	23.62	73	11341	50750	31635180
Sluggishness	44.83	23.62	22	11392	3062	31682868
Muscle rigidity	41.84	23.62	32	11382	9865	31676065
Sopor	41.63	23.62	34	11380	11518	31674412
Blood glucose increased	41.61	23.62	77	11337	61006	31624924
Anaemia	40.96	23.62	13	11401	213509	31472421
Tremor	40.82	23.62	87	11327	76333	31609597
Thinking abnormal	40.09	23.62	25	11389	5548	31680382
Somnolence	39.72	23.62	101	11313	99344	31586586
Priapism	39.09	23.62	23	11391	4597	31681333
Arthralgia	37.69	23.62	5	11409	151419	31534511
Hallucination	37.41	23.62	63	11351	46347	31639583
Obesity	36.53	23.62	31	11383	11069	31674861
Social avoidant behaviour	36.49	23.62	19	11395	2994	31682936
Blepharospasm	36.30	23.62	14	11400	1087	31684843
Sedation complication	35.81	23.62	15	11399	1444	31684486
Abnormal weight gain	34.30	23.62	13	11401	963	31684967
Sepsis	33.42	23.62	7	11407	151922	31534008
Agitation	32.84	23.62	65	11349	54104	31631826
Psychiatric symptom	32.07	23.62	18	11396	3293	31682637
Pain	31.40	23.62	14	11400	186745	31499185
Thrombocytopenia	30.53	23.62	7	11407	142740	31543190
Adverse drug reaction	29.95	23.62	41	11373	25160	31660770
Blood creatine phosphokinase increased	29.94	23.62	54	11360	41920	31644010
Emotional distress	29.73	23.62	31	11383	14325	31671605
Pneumonia	29.64	23.62	47	11367	335265	31350665
Inappropriate affect	28.54	23.62	10	11404	592	31685338
Housebound	28.38	23.62	8	11406	230	31685700
Psychotic symptom	28.32	23.62	13	11401	1559	31684371
Water intoxication	27.91	23.62	9	11405	412	31685518
Acute kidney injury	27.87	23.62	36	11378	279678	31406252
Restlessness	27.75	23.62	38	11376	23323	31662607
Anion gap increased	27.37	23.62	13	11401	1684	31684246
Erectile dysfunction	27.05	23.62	34	11380	19201	31666729
Hyperinsulinaemic hypoglycaemia	25.99	23.62	6	11408	75	31685855
Blood osmolarity decreased	25.52	23.62	9	11405	543	31685387
Hypometabolism	25.43	23.62	6	11408	83	31685847
Death	25.33	23.62	58	11356	360511	31325419
Pruritus	25.10	23.62	7	11407	125160	31560770
Insurance issue	24.61	23.62	11	11403	1239	31684691
Schizoaffective disorder	24.40	23.62	11	11403	1264	31684666
Completed suicide	24.01	23.62	80	11334	91434	31594496
Sinus tachycardia	23.87	23.62	29	11385	15820	31670110

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dystonia	904.92	23.81	289	16838	19417	70891900
Blood prolactin abnormal	849.49	23.81	184	16943	2612	70908705
Anosognosia	843.74	23.81	184	16943	2701	70908616
Schizophrenia	840.70	23.81	263	16864	16505	70894812
Sexual dysfunction	766.78	23.81	200	16927	6481	70904836
Disturbance in social behaviour	723.50	23.81	173	16954	3894	70907423
Metabolic disorder	633.65	23.81	179	16948	7861	70903456
Sedation	610.10	23.81	273	16854	46458	70864859
Personality change	572.19	23.81	169	16958	8701	70902616
Galactorrhoea	571.44	23.81	138	16989	3240	70908077
Suicide attempt	571.22	23.81	309	16818	79201	70832116
Dyskinesia	558.68	23.81	247	16880	40827	70870490
Intentional self-injury	442.08	23.81	194	16933	31456	70879861
Blood prolactin increased	395.20	23.81	105	17022	3649	70907668
Extrapyramidal disorder	379.18	23.81	154	16973	20596	70890721
Psychotic disorder	334.54	23.81	169	16958	37532	70873785
Neuroleptic malignant syndrome	313.91	23.81	144	16983	25863	70885454
Akathisia	308.88	23.81	115	17012	12178	70899139
Hyperprolactinaemia	288.50	23.81	85	17042	4328	70906989
Blood glucose increased	274.70	23.81	215	16912	102767	70808550
Treatment noncompliance	258.23	23.81	153	16974	46421	70864896
Gynaecomastia	255.99	23.81	86	17041	6737	70904580
Hallucination, auditory	219.60	23.81	101	17026	18227	70893090
Intentional overdose	208.91	23.81	180	16947	98255	70813062
Delusion	203.01	23.81	97	17030	19068	70892249
Amenorrhoea	167.37	23.81	63	17064	6867	70904450
Catatonia	164.55	23.81	65	17062	8068	70903249
Insurance issue	152.72	23.81	50	17077	3611	70907706
Parkinsonism	130.87	23.81	67	17060	15258	70896059
Adverse drug reaction	124.25	23.81	103	17024	53241	70858076
Weight increased	116.25	23.81	209	16918	242122	70669195
Mental impairment	109.67	23.81	62	17065	17193	70894124
Salivary hypersecretion	106.01	23.81	55	17072	12870	70898447
Drug ineffective	103.14	23.81	473	16654	939279	69972038
Tachycardia	97.64	23.81	153	16974	158393	70752924
Diarrhoea	97.51	23.81	34	17093	783307	70128010
Abnormal behaviour	91.35	23.81	72	17055	34637	70876680
Tardive dyskinesia	86.48	23.81	44	17083	9885	70901432
Mania	83.72	23.81	52	17075	17122	70894195
Myocarditis	79.42	23.81	52	17075	18741	70892576
Pain	76.95	23.81	28	17099	628788	70282529
Arthralgia	75.50	23.81	15	17112	503375	70407942
Agitation	74.69	23.81	102	17025	93273	70818044
Aggression	74.31	23.81	74	17053	48372	70862945
Sluggishness	71.93	23.81	33	17094	5910	70905407
Apathy	68.22	23.81	40	17087	11868	70899449
Sopor	67.88	23.81	58	17069	31209	70880108
Loss of libido	65.03	23.81	24	17103	2473	70908844
Muscle rigidity	63.13	23.81	45	17082	18605	70892712
Nausea	59.74	23.81	71	17056	852017	70059300
Suicidal ideation	55.60	23.81	76	17051	69520	70841797
Somnolence	54.81	23.81	144	16983	215462	70695855
Psychotic symptom	54.66	23.81	21	17106	2417	70908900
Hospitalisation	54.01	23.81	82	17045	82486	70828831
Anaemia	52.71	23.81	16	17111	403407	70507910
Sinus tachycardia	52.37	23.81	52	17075	33861	70877456
Paranoia	52.36	23.81	39	17088	17249	70894068
Pleurothotonus	51.69	23.81	20	17107	2346	70908971
Blood creatine phosphokinase increased	50.60	23.81	68	17059	61195	70850122
Oculogyric crisis	49.15	23.81	20	17107	2678	70908639
Tremor	48.05	23.81	112	17015	155512	70755805
Fatigue	47.47	23.81	79	17048	824240	70087077
Schizoaffective disorder	47.42	23.81	18	17109	2005	70909312
Hallucination	44.67	23.81	72	17055	76188	70835129
Condition aggravated	44.11	23.81	212	16915	427423	70483894
Dyspnoea	43.21	23.81	75	17052	769985	70141332
Pruritus	42.84	23.81	15	17112	345545	70565772
Peripheral swelling	42.57	23.81	4	17123	236559	70674758
Psychiatric symptom	42.55	23.81	24	17103	6620	70904697
Headache	42.05	23.81	47	17080	580358	70330959
Pain in extremity	39.38	23.81	15	17112	328067	70583250
Polydipsia	39.35	23.81	22	17105	5966	70905351
Breast enlargement	38.63	23.81	14	17113	1370	70909947
Drooling	38.55	23.81	21	17106	5415	70905902
Overdose	36.79	23.81	107	17020	169638	70741679
Myelocyte count increased	34.12	23.81	11	17116	756	70910561
Thinking abnormal	33.87	23.81	26	17101	12025	70899292
Pneumonia	33.46	23.81	58	17069	596174	70315143
Drug hypersensitivity	33.19	23.81	11	17116	262448	70648869
Joint swelling	33.11	23.81	10	17117	253201	70658116
Completed suicide	32.96	23.81	125	17002	227010	70684307
Metamyelocyte count increased	31.98	23.81	10	17117	622	70910695
Rhabdomyolysis	31.84	23.81	71	17056	95689	70815628
Abnormal weight gain	31.71	23.81	14	17113	2292	70909025
Alopecia	31.68	23.81	5	17122	198485	70712832
General physical health deterioration	31.45	23.81	9	17118	236022	70675295
Urinary tract infection	30.47	23.81	11	17116	248758	70662559
Drug abuse	30.16	23.81	91	17036	147165	70764152
Infection	30.07	23.81	7	17120	210778	70700539
Cough	29.96	23.81	21	17106	325356	70585961
Inappropriate antidiuretic hormone secretion	29.30	23.81	32	17095	23244	70888073
Restlessness	29.19	23.81	43	17084	42085	70869232
Accidental exposure to product by child	29.08	23.81	14	17113	2792	70908525
Thrombocytopenia	28.56	23.81	11	17116	239099	70672218
Rebound psychosis	28.24	23.81	7	17120	183	70911134
Lactate pyruvate ratio increased	28.09	23.81	6	17121	79	70911238
Persecutory delusion	28.07	23.81	16	17111	4501	70906816
Granulocytopenia	27.81	23.81	22	17105	10625	70900692
Emotional disorder	27.61	23.81	24	17103	13202	70898115
Personality disorder	27.54	23.81	17	17110	5531	70905786
Anion gap increased	27.27	23.81	14	17113	3202	70908115
Back pain	27.00	23.81	16	17111	271136	70640181
Nasopharyngitis	26.91	23.81	10	17117	222196	70689121
Antipsychotic drug level decreased	26.68	23.81	10	17117	1076	70910241
Housebound	26.13	23.81	8	17119	464	70910853
Torticollis	25.90	23.81	12	17115	2197	70909120
Electrocardiogram QT prolonged	25.63	23.81	60	17067	83457	70827860
Inappropriate schedule of product administration	25.43	23.81	70	17057	107485	70803832
Behaviour disorder	25.25	23.81	16	17111	5448	70905869
Blood osmolarity decreased	25.15	23.81	10	17117	1261	70910056
Hallucination, visual	24.88	23.81	33	17094	29304	70882013
Personality change due to a general medical condition	24.54	23.81	6	17121	148	70911169
Inappropriate affect	24.25	23.81	10	17117	1384	70909933
Hyperinsulinaemic hypoglycaemia	24.17	23.81	6	17121	158	70911159
Decreased appetite	23.92	23.81	23	17104	304757	70606560
Blood citric acid increased	23.91	23.81	5	17122	59	70911258

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.47	PDSP	DRUG LABEL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8.96	PDSP	DRUG LABEL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.39	PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	7.93	PDSP
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.89	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.43	PDSP
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.22	PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.21	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.32	PDSP
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.62	PDSP
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	8.57	PDSP
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8.55	WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.64	PDSP
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	9.05	PDSP
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	5.30	PDSP
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	8.25	PDSP
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.92	PDSP
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		Ki	5.06	PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	7.64	PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	7.72	PDSP
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	8.20	PDSP
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	7.27	PDSP
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	9.16	PDSP
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	6.56	PDSP
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	5.99	PDSP
Prostaglandin E2 receptor EP3 subtype	GPCR	P43115	PE2R3_HUMAN		Ki	5	PDSP
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN		Ki	7.54	PDSP
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.30	PDSP

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	10147-0951	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	10147-0952	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