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

Stem definition	Drug id	CAS RN
	2865	146939-27-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ziprasidone zaprasidone ziprasidone hydrochloride ziprasidone mesylate geodon ziprasidone HCl ziprasidone mesilate	a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone Molecular weight: 412.94 Formula: C21H21ClN4OS CLOGP: 4.86 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 48.47 ALOGS: -4.76 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ziprasidone
zaprasidone
ziprasidone hydrochloride
ziprasidone mesylate
geodon
ziprasidone HCl
ziprasidone mesilate

a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone

Molecular weight: 412.94
Formula: C21H21ClN4OS
CLOGP: 4.86
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 48.47
ALOGS: -4.76
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
80	mg	O
40	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.36 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.10 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Feb. 5, 2001	FDA	PFIZER

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
Dystonia	1007.55	18.62	298	15873	11628	50577325
Blood prolactin abnormal	894.76	18.62	193	15978	1982	50586971
Sexual dysfunction	878.18	18.62	205	15966	3087	50585866
Anosognosia	756.51	18.62	169	16002	2065	50586888
Sedation	715.38	18.62	293	15878	30317	50558636
Tardive dyskinesia	707.79	18.62	203	15968	7076	50581877
Disturbance in social behaviour	697.34	18.62	166	16005	2728	50586225
Dyskinesia	648.59	18.62	266	15905	27595	50561358
Metabolic disorder	621.16	18.62	171	16000	5115	50583838
Personality change	569.22	18.62	162	16009	5483	50583470
Suicide attempt	469.26	18.62	258	15913	51474	50537479
Extrapyramidal disorder	381.61	18.62	143	16028	11627	50577326
Completed suicide	333.01	18.62	300	15871	131589	50457364
Neuroleptic malignant syndrome	320.39	18.62	124	16047	11006	50577947
Akathisia	292.51	18.62	107	16064	8122	50580831
Blood glucose increased	249.46	18.62	196	15975	71128	50517825
Orthostatic hypertension	203.93	18.62	42	16129	336	50588617
Electrocardiogram QT prolonged	197.50	18.62	150	16021	51736	50537217
Parkinsonism	197.15	18.62	82	16089	8765	50580188
Metabolic syndrome	169.39	18.62	46	16125	1301	50587652
Insurance issue	160.90	18.62	51	16120	2497	50586456
Diabetes mellitus	142.35	18.62	121	16050	48912	50540041
Suicidal ideation	131.56	18.62	122	16049	55263	50533690
Psychotic disorder	127.28	18.62	82	16089	21730	50567223
Oculogyric crisis	121.52	18.62	36	16135	1401	50587552
Agitation	118.00	18.62	113	16058	53271	50535682
Tremor	108.29	18.62	157	16014	114746	50474207
Blood prolactin increased	101.63	18.62	38	16133	3061	50585892
Mania	100.26	18.62	55	16116	10861	50578092
Galactorrhoea	94.86	18.62	38	16133	3685	50585268
Hallucination, auditory	87.50	18.62	50	16121	10678	50578275
Obesity	83.19	18.62	57	16114	16718	50572235
Arthralgia	77.88	18.62	22	16149	438680	50150273
Cardio-respiratory arrest	74.56	18.62	89	16082	53803	50535150
Weight increased	72.75	18.62	183	15988	201708	50387245
Respiratory arrest	71.00	18.62	66	16105	29943	50559010
Impulse-control disorder	70.97	18.62	20	16151	650	50588303
Hyperprolactinaemia	70.96	18.62	30	16141	3335	50585618
Paranoia	70.66	18.62	43	16128	10305	50578648
Torsade de pointes	70.27	18.62	45	16126	11790	50577163
Posture abnormal	66.26	18.62	25	16146	2064	50586889
Anxiety	66.07	18.62	163	16008	177443	50411510
Pain	63.80	18.62	55	16116	578848	50010105
Somnolence	58.43	18.62	143	16028	154842	50434111
Type 2 diabetes mellitus	58.11	18.62	63	16108	34312	50554641
Delusion	57.39	18.62	38	16133	10531	50578422
Rapid eye movement sleep behaviour disorder	56.83	18.62	13	16158	177	50588776
Diarrhoea	55.55	18.62	64	16107	588412	50000541
Depression	54.44	18.62	145	16026	165278	50423675
Peripheral swelling	53.67	18.62	3	16168	205933	50383020
Catatonia	52.25	18.62	25	16146	3711	50585242
Pneumonia	50.78	18.62	29	16142	378372	50210581
Joint swelling	50.05	18.62	9	16162	245277	50343676
Dyslipidaemia	49.07	18.62	28	16143	5960	50582993
Adverse drug reaction	48.40	18.62	73	16098	55149	50533804
Rheumatoid arthritis	47.03	18.62	5	16166	202545	50386408
Abnormal behaviour	46.04	18.62	43	16128	19615	50569338
Condition aggravated	45.07	18.62	201	15970	296857	50292096
Substance abuse	44.10	18.62	23	16148	4101	50584852
Muscle rigidity	43.14	18.62	31	16140	9798	50579155
Cardiac arrest	42.51	18.62	87	16084	83564	50505389
Psychomotor hyperactivity	42.35	18.62	30	16141	9271	50579682
Insomnia	41.95	18.62	137	16034	174728	50414225
Overdose	40.76	18.62	95	16076	99632	50489321
Blood triglycerides increased	39.26	18.62	31	16140	11281	50577672
Arthropathy	39.06	18.62	3	16168	157903	50431050
Mental disorder	36.62	18.62	40	16131	21951	50567002
Product use issue	36.52	18.62	3	16168	149472	50439481
Reduced facial expression	36.26	18.62	15	16156	1579	50587374
Swollen tongue	35.88	18.62	45	16126	28585	50560368
Restlessness	35.49	18.62	42	16129	25131	50563822
Cardiac hypertrophy	31.96	18.62	12	16159	977	50587976
Rabbit syndrome	31.40	18.62	9	16162	311	50588642
Systemic lupus erythematosus	31.31	18.62	4	16167	140618	50448335
Aggression	31.05	18.62	36	16135	21080	50567873
Personality change due to a general medical condition	30.69	18.62	7	16164	94	50588859
Treatment failure	30.44	18.62	4	16167	137633	50451320
Toxicity to various agents	30.09	18.62	141	16030	212358	50376595
Alopecia	29.77	18.62	21	16150	245026	50343927
Product substitution issue	29.60	18.62	29	16142	14028	50574925
Intentional overdose	29.40	18.62	63	16108	62441	50526512
Off label use	29.30	18.62	68	16103	474358	50114595
Tachyphrenia	29.28	18.62	12	16159	1233	50587720
Abdominal discomfort	29.28	18.62	19	16152	231622	50357331
Mental status changes	29.04	18.62	46	16125	36226	50552727
Swelling	28.95	18.62	14	16157	200858	50388095
Seizure	28.82	18.62	93	16078	117781	50471172
Torticollis	28.56	18.62	13	16158	1723	50587230
Nasopharyngitis	28.49	18.62	13	16158	192914	50396039
Maternal exposure during pregnancy	28.29	18.62	8	16163	159770	50429183
Fatigue	27.95	18.62	124	16047	707477	49881476
Sinusitis	27.61	18.62	10	16161	170548	50418405
Infection	26.57	18.62	11	16160	172943	50416010
Echolalia	26.56	18.62	7	16164	176	50588777
Cough	26.37	18.62	23	16148	241241	50347712
Trismus	25.68	18.62	15	16156	3333	50585620
Drooling	25.54	18.62	15	16156	3369	50585584
Pyrexia	25.52	18.62	52	16119	380151	50208802
General physical health deterioration	25.46	18.62	7	16164	142427	50446526
Pain in extremity	25.29	18.62	30	16141	272835	50316118
Abdominal pain	25.24	18.62	23	16148	236205	50352748
Drug withdrawal syndrome	24.63	18.62	35	16136	25046	50563907
Bruxism	24.33	18.62	14	16157	3026	50585927
Back pain	24.01	18.62	21	16150	220009	50368944
Rhabdomyolysis	23.98	18.62	44	16127	38983	50549970
Thrombocytopenia	23.33	18.62	6	16165	127667	50461286
Haemoglobin decreased	23.21	18.62	6	16165	127210	50461743
Schizophrenia	22.97	18.62	19	16152	7378	50581575
Amenorrhoea	22.69	18.62	20	16151	8464	50580489
Drug ineffective	22.69	18.62	377	15794	818956	49769997
Irritability	22.68	18.62	36	16135	28390	50560563
Exposure via ingestion	22.68	18.62	13	16158	2790	50586163
Withdrawal syndrome	22.60	18.62	28	16143	17562	50571391
Cogwheel rigidity	22.17	18.62	11	16160	1766	50587187
Suicidal behaviour	22.09	18.62	12	16159	2322	50586631
Organ failure	22.02	18.62	12	16159	2336	50586617
Stereotypy	21.47	18.62	7	16164	375	50588578
Nausea	21.46	18.62	135	16036	705263	49883690
Wound	21.30	18.62	4	16167	105790	50483163
Headache	21.03	18.62	87	16084	506448	50082505
Diabetic coma	20.85	18.62	8	16163	691	50588262
Coprolalia	20.72	18.62	4	16167	22	50588931
Thinking abnormal	20.63	18.62	20	16151	9547	50579406
Apathy	20.60	18.62	18	16153	7530	50581423
Muscle twitching	20.53	18.62	25	16146	15406	50573547
Decreased eye contact	20.19	18.62	6	16165	236	50588717
Granulocytopenia	19.59	18.62	15	16156	5216	50583737
Sepsis	19.55	18.62	9	16162	132916	50456037
Obsessive thoughts	19.50	18.62	7	16164	502	50588451
Muscle tightness	19.42	18.62	20	16151	10260	50578693
Anaemia	19.16	18.62	32	16139	252424	50336529
Pituitary hyperplasia	19.07	18.62	3	16168	3	50588950
Pressure of speech	18.92	18.62	7	16164	547	50588406
Injection site pain	18.84	18.62	6	16165	111018	50477935
Pruritus	18.82	18.62	39	16132	283529	50305424
Coma	18.80	18.62	50	16121	56829	50532124
Female sexual dysfunction	18.71	18.62	4	16167	39	50588914

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
Dystonia	433.27	21.42	159	11841	9590	29552937
Neuroleptic malignant syndrome	308.31	21.42	144	11856	16004	29546523
Akathisia	281.17	21.42	105	11895	6637	29555890
Dyskinesia	278.63	21.42	144	11856	19917	29542610
Tardive dyskinesia	268.13	21.42	95	11905	5163	29557364
Anosognosia	241.95	21.42	58	11942	760	29561767
Blood prolactin abnormal	239.06	21.42	58	11942	802	29561725
Sedation	224.69	21.42	119	11881	17286	29545241
Antipsychotic drug level below therapeutic	221.74	21.42	65	11935	1909	29560618
Therapeutic product effect variable	216.10	21.42	63	11937	1814	29560713
Euphoric mood	211.62	21.42	78	11922	4747	29557780
Disturbance in social behaviour	208.71	21.42	60	11940	1642	29560885
Obsessive-compulsive disorder	204.48	21.42	75	11925	4501	29558026
Disinhibition	203.91	21.42	65	11935	2542	29559985
Suicide attempt	196.15	21.42	139	11861	33971	29528556
Weight increased	191.48	21.42	193	11807	76474	29486053
Extrapyramidal disorder	189.48	21.42	91	11909	10740	29551787
Sexual dysfunction	166.48	21.42	69	11931	5745	29556782
Increased appetite	163.67	21.42	69	11931	5995	29556532
Metabolic disorder	155.65	21.42	58	11942	3637	29558890
Priapism	127.59	21.42	53	11947	4435	29558092
Obesity	125.97	21.42	67	11933	9796	29552731
Aggression	120.22	21.42	106	11894	35435	29527092
Personality change	115.97	21.42	50	11950	4588	29557939
Electrocardiogram QT prolonged	114.74	21.42	104	11896	36033	29526494
Completed suicide	114.69	21.42	161	11839	90085	29472442
Psychotic disorder	105.61	21.42	78	11922	20276	29542251
Agitation	102.74	21.42	115	11885	51189	29511338
Suicidal ideation	100.69	21.42	95	11905	34621	29527906
Bruxism	97.60	21.42	33	11967	1554	29560973
Oppositional defiant disorder	94.09	21.42	25	11975	506	29562021
Decreased eye contact	91.51	21.42	24	11976	461	29562066
Homicidal ideation	89.68	21.42	35	11965	2489	29560038
Catatonia	88.74	21.42	41	11959	4427	29558100
Dyslipidaemia	79.71	21.42	42	11958	6019	29556508
Irritability	76.72	21.42	67	11933	22085	29540442
Oculogyric crisis	74.73	21.42	26	11974	1335	29561192
Trismus	70.75	21.42	29	11971	2344	29560183
Delusion	65.04	21.42	46	11954	11170	29551357
Blood prolactin increased	64.30	21.42	24	11976	1510	29561017
Hallucination, auditory	64.25	21.42	43	11957	9550	29552977
Swollen tongue	63.58	21.42	47	11953	12219	29550308
Mania	63.29	21.42	41	11959	8622	29553905
Serotonin syndrome	62.72	21.42	54	11946	17458	29545069
Drug ineffective	60.90	21.42	299	11701	362871	29199656
Anxiety	59.12	21.42	116	11884	85249	29477278
Psychomotor hyperactivity	57.87	21.42	38	11962	8175	29554352
Leukaemia	57.60	21.42	29	11971	3781	29558746
Crying	56.30	21.42	32	11968	5319	29557208
Paranoia	56.09	21.42	40	11960	9837	29552690
Diarrhoea	55.94	21.42	33	11967	332665	29229862
Choreoathetosis	54.13	21.42	19	11981	1001	29561526
Pneumonia	53.48	21.42	32	11968	320140	29242387
Therapeutic product effect incomplete	52.61	21.42	72	11928	39233	29523294
Leukopenia	50.92	21.42	85	11915	55118	29507409
Speech disorder	49.22	21.42	54	11946	23462	29539065
Schizoaffective disorder	49.14	21.42	18	11982	1074	29561453
Prescribed overdose	48.92	21.42	35	11965	8648	29553879
Coordination abnormal	47.90	21.42	32	11968	7082	29555445
Blood glucose increased	46.82	21.42	85	11915	58899	29503628
Anaemia	46.75	21.42	12	11988	200939	29361588
Dacryostenosis congenital	45.70	21.42	9	11991	42	29562485
Parkinsonism	44.87	21.42	31	11969	7247	29555280
Toxicity to various agents	43.68	21.42	162	11838	173499	29389028
Tic	43.31	21.42	19	11981	1816	29560711
Type 2 diabetes mellitus	42.88	21.42	39	11961	13542	29548985
Abnormal behaviour	41.44	21.42	49	11951	23078	29539449
Muscle rigidity	37.77	21.42	31	11969	9380	29553147
Somnolence	37.67	21.42	103	11897	93852	29468675
Diabetes mellitus	37.61	21.42	62	11938	39769	29522758
Blood creatine phosphokinase increased	36.68	21.42	62	11938	40582	29521945
Tremor	36.08	21.42	87	11913	73451	29489076
Schizophrenia	35.92	21.42	26	11974	6539	29555988
Granulocytopenia	35.71	21.42	25	11975	5969	29556558
Mood altered	35.26	21.42	28	11972	8083	29554444
Affect lability	34.86	21.42	20	11980	3382	29559145
Anger	33.84	21.42	31	11969	10859	29551668
Insomnia	33.31	21.42	95	11905	88666	29473861
Rhabdomyolysis	33.16	21.42	75	11925	60733	29501794
Hypotonia neonatal	33.09	21.42	14	11986	1225	29561302
Torticollis	31.34	21.42	13	11987	1082	29561445
Hyperkinesia	29.66	21.42	14	11986	1585	29560942
Blood triglycerides increased	29.54	21.42	31	11969	12803	29549724
Blunted affect	29.51	21.42	9	11991	303	29562224
Grandiosity	29.23	21.42	9	11991	313	29562214
Pruritus	29.08	21.42	6	11994	116843	29445684
Pyrexia	29.04	21.42	45	11955	287577	29274950
Feminisation acquired	28.28	21.42	6	11994	43	29562484
Acute kidney injury	27.25	21.42	41	11959	265226	29297301
Cough	26.81	21.42	9	11991	126718	29435809
Myopathy toxic	26.52	21.42	9	11991	428	29562099
Opisthotonus	26.19	21.42	9	11991	445	29562082
Asthenia	25.42	21.42	30	11970	215220	29347307
Bipolar disorder	25.06	21.42	16	11984	3279	29559248
Depressed mood	24.86	21.42	32	11968	16416	29546111
Thinking abnormal	24.76	21.42	19	11981	5217	29557310
Thrombocytopenia	24.58	21.42	12	11988	134811	29427716
Condition aggravated	23.27	21.42	119	11881	146176	29416351
Hyperprolactinaemia	23.19	21.42	11	11989	1259	29561268
Arthralgia	23.16	21.42	14	11986	139603	29422924
Neonatal respiratory depression	23.12	21.42	8	11992	404	29562123
Disease progression	23.06	21.42	3	11997	81913	29480614
Insurance issue	23.00	21.42	10	11990	935	29561592
Streptococcal infection	22.81	21.42	17	11983	4471	29558056
Off label use	22.61	21.42	56	11944	300744	29261783
Nervousness	21.99	21.42	25	11975	11281	29551246
Death	21.78	21.42	69	11931	342015	29220512
Sleep disorder	21.73	21.42	37	11963	24349	29538178
Posture abnormal	21.44	21.42	12	11988	1935	29560592

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	1107.57	18.18	359	20820	18506	64459047
Blood prolactin abnormal	1053.44	18.18	231	20948	2501	64475052
Sexual dysfunction	945.52	18.18	250	20929	6221	64471332
Anosognosia	921.25	18.18	208	20971	2597	64474956
Disturbance in social behaviour	838.46	18.18	205	20974	3682	64473871
Sedation	786.40	18.18	345	20834	41117	64436436
Dyskinesia	770.59	18.18	335	20844	39053	64438500
Metabolic disorder	717.30	18.18	209	20970	7488	64470065
Personality change	664.49	18.18	202	20977	8391	64469162
Neuroleptic malignant syndrome	509.46	18.18	219	20960	24777	64452776
Suicide attempt	499.24	18.18	303	20876	70704	64406849
Tardive dyskinesia	499.09	18.18	165	21014	9013	64468540
Completed suicide	489.56	18.18	476	20703	223938	64253615
Extrapyramidal disorder	361.50	18.18	160	21019	19392	64458161
Akathisia	302.52	18.18	121	21058	11389	64466164
Blood glucose increased	283.39	18.18	244	20935	97829	64379724
Electrocardiogram QT prolonged	234.18	18.18	200	20979	79248	64398305
Parkinsonism	219.50	18.18	103	21076	14270	64463283
Psychotic disorder	184.10	18.18	124	21055	34454	64443099
Suicidal ideation	180.86	18.18	160	21019	66382	64411171
Orthostatic hypertension	180.82	18.18	42	21137	597	64476956
Obesity	171.11	18.18	98	21081	20464	64457089
Insurance issue	170.51	18.18	55	21124	2771	64474782
Oculogyric crisis	163.84	18.18	52	21127	2486	64475067
Metabolic syndrome	159.43	18.18	50	21129	2298	64475255
Agitation	147.76	18.18	163	21016	88204	64389349
Aggression	143.54	18.18	120	21059	46112	64431441
Diabetes mellitus	125.87	18.18	131	21048	66343	64411210
Catatonia	120.63	18.18	56	21123	7564	64469989
Decreased eye contact	113.75	18.18	30	21149	735	64476818
Hallucination, auditory	112.94	18.18	70	21109	16869	64460684
Blood prolactin increased	110.00	18.18	42	21137	3486	64474067
Weight increased	108.16	18.18	225	20954	213123	64264430
Oppositional defiant disorder	106.60	18.18	26	21153	460	64477093
Type 2 diabetes mellitus	102.88	18.18	87	21092	33933	64443620
Respiratory arrest	99.53	18.18	104	21075	52881	64424672
Adverse drug reaction	95.89	18.18	95	21084	45369	64432184
Delusion	94.40	18.18	64	21115	17950	64459603
Dyslipidaemia	90.39	18.18	49	21130	9193	64468360
Psychomotor hyperactivity	89.51	18.18	57	21122	14394	64463159
Anxiety	89.28	18.18	202	20977	202447	64275106
Bruxism	87.96	18.18	36	21143	3588	64473965
Diarrhoea	85.00	18.18	68	21111	722636	63754917
Mania	83.29	18.18	57	21122	16229	64461324
Galactorrhoea	81.64	18.18	33	21146	3186	64474367
Homicidal ideation	81.26	18.18	33	21146	3224	64474329
Irritability	79.74	18.18	78	21101	36668	64440885
Pneumonia	78.76	18.18	43	21136	559533	63918020
Drug ineffective	77.44	18.18	505	20674	839742	63637811
Paranoia	76.07	18.18	54	21125	16298	64461255
Priapism	74.96	18.18	33	21146	3937	64473616
Condition aggravated	74.83	18.18	280	20899	372146	64105407
Cardiac arrest	70.53	18.18	156	21023	153908	64323645
Cardio-respiratory arrest	68.64	18.18	119	21060	98274	64379279
Trismus	68.32	18.18	33	21146	4868	64472685
Hyperprolactinaemia	67.86	18.18	31	21148	4034	64473519
Arthralgia	65.13	18.18	32	21147	442228	64035325
Posture abnormal	63.30	18.18	28	21151	3378	64474175
Tremor	63.28	18.18	146	21033	148084	64329469
Granulocytopenia	61.74	18.18	40	21139	10400	64467153
Muscle rigidity	59.74	18.18	48	21131	17425	64460128
Serotonin syndrome	59.68	18.18	69	21110	39213	64438340
Antipsychotic drug level below therapeutic	58.72	18.18	19	21160	966	64476587
Depression	57.85	18.18	161	21018	183130	64294423
Insomnia	56.84	18.18	168	21011	197668	64279885
Rhabdomyolysis	55.13	18.18	104	21075	91622	64385931
Impulse-control disorder	53.47	18.18	20	21159	1568	64475985
Pain	53.41	18.18	62	21117	553449	63924104
Torsade de pointes	51.65	18.18	44	21135	17319	64460234
Pyrexia	51.34	18.18	65	21114	558579	63918974
Abnormal behaviour	50.98	18.18	59	21120	33563	64443990
Peripheral swelling	50.67	18.18	5	21174	209148	64268405
Toxicity to various agents	50.19	18.18	244	20935	363269	64114284
Anaemia	49.11	18.18	32	21147	378648	64098905
Rapid eye movement sleep behaviour disorder	48.92	18.18	13	21166	328	64477225
Choreoathetosis	47.90	18.18	18	21161	1429	64476124
Joint swelling	47.63	18.18	7	21172	215375	64262178
Swollen tongue	47.49	18.18	58	21121	34896	64442657
Euphoric mood	45.86	18.18	28	21151	6563	64470990
Coordination abnormal	44.67	18.18	38	21141	14926	64462627
Blood triglycerides increased	44.61	18.18	42	21137	18824	64458729
Overdose	44.38	18.18	134	21045	159432	64318121
Nausea	42.86	18.18	125	21054	785675	63691878
Mental disorder	42.79	18.18	48	21131	26397	64451156
Cough	42.73	18.18	23	21156	302125	64175428
Blood creatine phosphokinase increased	42.36	18.18	72	21107	58486	64419067
Torticollis	40.79	18.18	18	21161	2159	64475394
Disinhibition	40.28	18.18	18	21161	2225	64475328
Exposure via ingestion	39.79	18.18	23	21156	4879	64472674
Abdominal pain	39.67	18.18	27	21152	312348	64165205
Rheumatoid arthritis	39.60	18.18	4	21175	164290	64313263
Speech disorder	38.30	18.18	62	21117	48379	64429174
Grandiosity	38.22	18.18	12	21167	553	64477000
Reduced facial expression	38.08	18.18	17	21162	2096	64475457
Obsessive-compulsive disorder	37.50	18.18	22	21157	4796	64472757
Haemoglobin decreased	37.46	18.18	9	21170	195054	64282499
Increased appetite	37.10	18.18	29	21150	10117	64467436
Crying	36.92	18.18	39	21140	20051	64457502
Mood altered	36.69	18.18	35	21144	15944	64461609
Somnolence	36.61	18.18	148	21031	203497	64274056
Malaise	36.45	18.18	46	21133	396201	64081352
Restlessness	35.74	18.18	54	21125	39731	64437822
Acute kidney injury	35.56	18.18	58	21121	449182	64028371
Therapeutic product effect variable	35.41	18.18	15	21164	1629	64475924
Hyperkinesia	35.05	18.18	17	21162	2529	64475024
Rabbit syndrome	34.83	18.18	10	21169	338	64477215
Tic	34.60	18.18	17	21162	2602	64474951
Nasopharyngitis	34.01	18.18	11	21168	196062	64281491
Pain in extremity	33.66	18.18	30	21149	303055	64174498
Affect lability	33.53	18.18	26	21153	8964	64468589
Thrombocytopenia	33.17	18.18	16	21163	223785	64253768
Dyspnoea	33.15	18.18	123	21056	718551	63759002
Schizophrenia	32.60	18.18	28	21151	11140	64466413
Febrile neutropenia	31.73	18.18	11	21168	187646	64289907
Renal impairment	30.75	18.18	4	21175	135013	64342540
Abdominal discomfort	30.29	18.18	11	21168	182311	64295242
General physical health deterioration	29.71	18.18	15	21164	204410	64273143
Off label use	29.35	18.18	108	21071	632698	63844855
Schizoaffective disorder	29.34	18.18	13	21166	1574	64475979
Arthropathy	29.00	18.18	3	21176	120964	64356589
Pruritus	28.99	18.18	36	21143	312364	64165189
Substance abuse	28.56	18.18	24	21155	9268	64468285
Thinking abnormal	27.84	18.18	26	21153	11530	64466023
Gastrointestinal haemorrhage	27.67	18.18	5	21174	132307	64345246
Personality change due to a general medical condition	27.56	18.18	7	21172	147	64477406
Headache	27.51	18.18	86	21093	529381	63948172
Tachyphrenia	27.26	18.18	13	21166	1863	64475690
Sepsis	26.54	18.18	22	21157	230319	64247234
Disease progression	26.30	18.18	7	21172	141673	64335880
Infection	26.22	18.18	14	21165	184866	64292687
Fatigue	26.17	18.18	142	21037	748588	63728965
Stereotypy	26.16	18.18	10	21169	832	64476721
Asthenia	25.56	18.18	65	21114	427979	64049574
Erythema	25.33	18.18	15	21164	187055	64290498
Feminisation acquired	25.11	18.18	5	21174	32	64477521
Mental status changes	24.70	18.18	59	21120	61103	64416450
Anger	24.49	18.18	28	21151	15713	64461840
Swelling	24.44	18.18	11	21168	160207	64317346
Alopecia	24.31	18.18	12	21167	165678	64311875
Depressed mood	24.00	18.18	46	21133	40966	64436587
Injection site pain	23.75	18.18	4	21175	111404	64366149
Sleep disorder	23.47	18.18	57	21122	59652	64417901
Drooling	23.44	18.18	17	21162	5302	64472251
Stomatitis	23.23	18.18	4	21175	109601	64367952
Cognitive disorder	23.18	18.18	54	21125	55033	64422520
Ventricular arrhythmia	22.48	18.18	19	21160	7396	64470157
Myopathy toxic	22.43	18.18	9	21170	852	64476701
Sinusitis	22.28	18.18	10	21169	145918	64331635
Treatment noncompliance	22.12	18.18	46	21133	43436	64434117
Sperm concentration decreased	21.94	18.18	5	21174	65	64477488
Corneal reflex decreased	21.90	18.18	7	21172	342	64477211
Echolalia	21.56	18.18	7	21172	360	64477193
Treatment failure	21.25	18.18	6	21173	116810	64360743
Pressure of speech	21.12	18.18	9	21170	992	64476561
Posturing	21.02	18.18	9	21170	1003	64476550
Obsessive thoughts	20.98	18.18	9	21170	1008	64476545
Muscle contractions involuntary	20.69	18.18	13	21166	3204	64474349
Streptococcal infection	20.32	18.18	18	21161	7461	64470092
Drug screen positive	20.14	18.18	16	21163	5713	64471840
Poisoning	20.08	18.18	30	21149	21849	64455704
Diabetic coma	20.06	18.18	9	21170	1122	64476431
Interstitial lung disease	19.78	18.18	4	21175	97728	64379825
Back pain	19.11	18.18	33	21146	250138	64227415
Intentional product use issue	19.10	18.18	4	21175	95360	64382193
Female sexual dysfunction	18.89	18.18	4	21175	36	64477517
Cardiac failure	18.80	18.18	10	21169	132363	64345190
Hyperkalaemia	18.76	18.18	5	21174	101124	64376429
Product substitution issue	18.59	18.18	26	21153	17835	64459718
Hallucination	18.24	18.18	59	21120	72729	64404824

FDA Adverse Event Reporting System (Pediatric)

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
Dacryostenosis congenital	38.95	29.56	8	116	8	84546
Opisthotonus	35.39	29.56	8	116	17	84537

Pharmacologic Action:

Source	Code	Description
ATC	N05AE04	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Indole derivatives
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	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
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:35476	neuroleptics
CHEBI has role	CHEBI:37956	antihistamines
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:48876	muscarinic antagonists

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

Disease	Relation	SNOMED_ID	DOID
Mixed bipolar I disorder	indication	16506000	DOID:3312
Schizophrenia	indication	58214004	DOID:5419
Bipolar disorder in remission	indication	85248005
Bipolar affective disorder, current episode manic	indication	191618007
Agitation associated with Schizophrenia	indication
Bipolar affective disorder, current episode depression	off-label use	191627008	DOID:3312
Depression Treatment Adjunct	off-label use
Tachyarrhythmia	contraindication	6285003
Suicidal thoughts	contraindication	6471006
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Agranulocytosis	contraindication	17182001	DOID:12987
Myocardial infarction	contraindication	22298006	DOID:5844
Hypovolemia	contraindication	28560003
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Dehydration	contraindication	34095006
Dysphagia	contraindication	40739000
Hypokalemia	contraindication	43339004
Conduction disorder of the heart	contraindication	44808001
Bradycardia	contraindication	48867003
Hyperlipidemia	contraindication	55822004	DOID:1168
Hepatic failure	contraindication	59927004
Cerebrovascular disease	contraindication	62914000	DOID:6713
Diabetes mellitus	contraindication	73211009	DOID:9351
Extrapyramidal disease	contraindication	76349003
Hyperglycemia	contraindication	80394007	DOID:4195
Heart failure	contraindication	84114007	DOID:6000
Epilepsy	contraindication	84757009	DOID:1826
Leukopenia	contraindication	84828003	DOID:615
Kidney disease	contraindication	90708001	DOID:557
Tardive dyskinesia	contraindication	102449007
Prolonged QT interval	contraindication	111975006
Hypomagnesemia	contraindication	190855004
Decompensated cardiac failure	contraindication	195111005
Metabolic syndrome X	contraindication	237602007	DOID:14221
Neutropenic disorder	contraindication	303011007	DOID:1227
Severe diarrhea	contraindication	409587002
Breastfeeding (mother)	contraindication	413712001
Myocardial ischemia	contraindication	414795007	DOID:3393
Obesity	contraindication	414916001	DOID:9970
Acquired torsion dystonia	contraindication	433493000
Congenital long QT syndrome	contraindication	442917000
Carcinoma of female breast	contraindication	447782002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.26	acidic
pKa2	7.35	Basic
pKa3	0.27	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 20MG BASE	GEODON	VIATRIS	N020825	Feb. 5, 2001	RX	CAPSULE	ORAL	Jan. 28, 2025	INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES
EQ 40MG BASE	GEODON	VIATRIS	N020825	Feb. 5, 2001	RX	CAPSULE	ORAL	Jan. 28, 2025	INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES
EQ 60MG BASE	GEODON	VIATRIS	N020825	Feb. 5, 2001	RX	CAPSULE	ORAL	Jan. 28, 2025	INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES
EQ 80MG BASE	GEODON	VIATRIS	N020825	Feb. 5, 2001	RX	CAPSULE	ORAL	Jan. 28, 2025	INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	9.40	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.32	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.30	PDSP
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	8.02	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.30	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.92	WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		IC50	7	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	7.36	PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.57	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	8.89	WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	7.22	WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	8.30	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8	WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.32	PDSP
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	ANTAGONIST	Ki	8.14	WOMBAT-PK
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN		Ki	6.82	PDSP
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	7.33	WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.46	PDSP
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.55	WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	5.52	PDSP
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	5	PDSP
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	5.80	PDSP
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	5.80	PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN	AGONIST	Ki	8.30	IUPHAR
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	8.70	WOMBAT-PK
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.11	PDSP
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN				WOMBAT-PK
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	ANTAGONIST	Ki	7.30	WOMBAT-PK
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN		Ki	6.40	WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	8.05	PDSP
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	6.54	PDSP
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	6.44	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		EC50	8.47	WOMBAT-PK
Histone H1.0	Nuclear other	P07305	H10_HUMAN		Ki	7.82	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	5.59	PDSP
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		Ki	9.30	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		Ki	7.80	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	8.32	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	9.38	CHEMBL
Histamine H1 receptor	GPCR		HRH1_RAT		IC50	6.82	CHEMBL
Transporter	Transporter		Q63380_RAT		Ki	7.32	CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		Ki	7.96	CHEMBL

External reference:

ID	Source
4021249	VUID
N0000148690	NUI
D02100	KEGG_DRUG
138982-67-9	SECONDARY_CAS_RN
199191-69-0	SECONDARY_CAS_RN
4021249	VANDF
4030214	VANDF
4030215	VANDF
C0380393	UMLSCUI
CHEBI:10119	CHEBI
CHEMBL708	ChEMBL_ID
CHEMBL1375743	ChEMBL_ID
CHEMBL1712	ChEMBL_ID
CHEMBL3989833	ChEMBL_ID
CHEMBL1200997	ChEMBL_ID
DB00246	DRUGBANK_ID
C092292	MESH_SUPPLEMENTAL_RECORD_UI
60854	PUBCHEM_CID
59	IUPHAR_LIGAND_ID
7155	INN_ID
6UKA5VEJ6X	UNII
115698	RXNORM
16791	MMSL
187736	MMSL
331404	MMSL
41113	MMSL
d04747	MMSL
009104	NDDF
009105	NDDF
009579	NDDF
129479007	SNOMEDCT_US
373389002	SNOMEDCT_US
409356003	SNOMEDCT_US
409357007	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0052	CAPSULE	20 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0052	CAPSULE	20 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0054	CAPSULE	40 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0054	CAPSULE	40 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0056	CAPSULE	60 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0056	CAPSULE	60 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0058	CAPSULE	80 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0058	CAPSULE	80 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0352	CAPSULE	20 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0352	CAPSULE	20 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0354	CAPSULE	40 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0354	CAPSULE	40 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0356	CAPSULE	60 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0356	CAPSULE	60 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0358	CAPSULE	80 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-0358	CAPSULE	80 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-1203	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20 mg	INTRAMUSCULAR	NDA	30 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-1203	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20 mg	INTRAMUSCULAR	NDA	30 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3920	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20 mg	INTRAMUSCULAR	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3920	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20 mg	INTRAMUSCULAR	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3960	CAPSULE	20 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3960	CAPSULE	20 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3980	CAPSULE	60 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3980	CAPSULE	60 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3990	CAPSULE	80 mg	ORAL	NDA	32 sections
Geodon	HUMAN PRESCRIPTION DRUG LABEL	1	0049-3990	CAPSULE	80 mg	ORAL	NDA	32 sections
ziprasidone hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7703	CAPSULE	80 mg	ORAL	ANDA	31 sections
ziprasidone hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0781-2164	CAPSULE	20 mg	ORAL	ANDA	30 sections
ziprasidone hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0781-2166	CAPSULE	40 mg	ORAL	ANDA	30 sections
ziprasidone hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0781-2167	CAPSULE	60 mg	ORAL	ANDA	30 sections