thioridazine

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	35.89 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	3.580		Moderate	0.72
caco2-efflux	Caco-2 efflux ratio (BA/AB)	2.028		Moderate	0.72
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	10.471	10^-6 cm/s	Moderate	0.72
dh-clint	Dog hepatocyte intrinsic clearance	52.481	uL/min/10^6 cells	Moderate	0.72
dppb	Dog plasma protein binding (% unbound)	0.840	%	Moderate	0.72
fcs-ppb	Fetal calf serum protein binding (% unbound)	3.310	%	Moderate	0.72
herg	hERG pIC50	6.071	pIC50	Moderate	0.72
hh-clint	Human hepatocyte intrinsic clearance	9.683	uL/min/10^6 cells	Moderate	0.72
hlm-clint	Human liver microsomal intrinsic clearance	40.551	uL/min/mg protein	Moderate	0.72
hppb	Human plasma protein binding (% unbound)	0.790	%	Moderate	0.72
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	0.615		Moderate	0.72
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	1.189		Moderate	0.72
mh-clint	Mouse hepatocyte intrinsic clearance	145.881		Moderate	0.72
mppb	Mouse plasma protein binding (% unbound)	1.340		Moderate	0.72
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	6.998		Moderate	0.72
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	6.770	%	Moderate	0.72
rat-kpuu-brain	Rat brain Kpuu	0.291	%	Moderate	0.72
rh-clint	Rat hepatocyte intrinsic clearance	243.220	uL/min/10^6 cells	Moderate	0.72
rh-fuinc	Rat hepatocyte fraction unbound in incubation	6.100	%	Moderate	0.72
rppb	Rat plasma protein binding (% unbound)	1.560	%	Moderate	0.72
solubility-dd	Solubility at pH 7.4 in DMSO	73.621	uM	Moderate	0.72

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
Polydipsia	122.13	73.02	22	663	4209	90623553
Tardive dyskinesia	118.35	73.02	25	660	10905	90616857
Head titubation	110.40	73.02	17	668	1251	90626511
Apraxia	107.52	73.02	18	667	2244	90625518
Parkinsonism	101.16	73.02	23	662	14042	90613720
Dystonia	86.70	73.02	21	664	16798	90610964

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
Antipsychotic drug level below therapeutic	653.39	179.46	117	2095	3087	42616036
Disinhibition	630.57	179.46	117	2095	3778	42615345
Therapeutic product effect variable	630.41	179.46	113	2099	2996	42616127
Obsessive-compulsive disorder	601.86	179.46	123	2089	6620	42612503
Euphoric mood	571.63	179.46	117	2095	6336	42612787
Increased appetite	534.06	179.46	117	2095	8789	42610334
Akathisia	520.85	179.46	118	2094	10333	42608790
Suicide attempt	343.53	179.46	117	2095	45983	42573140
Leukaemia	307.71	179.46	69	2143	5703	42613420
Therapeutic product effect incomplete	280.35	179.46	113	2099	70826	42548297
Leukopenia	257.64	179.46	108	2104	74638	42544485
Weight increased	246.99	179.46	117	2095	107866	42511257
Dyslipidaemia	239.62	179.46	62	2150	9356	42609767
Obesity	214.02	179.46	64	2148	16395	42602728
Prescribed overdose	193.14	179.46	56	2156	12871	42606252
Toxicity to various agents	181.51	179.46	124	2088	229012	42390111

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
Antipsychotic drug level below therapeutic	272.51	69.60	43	1763	1692	110585801
Therapeutic product effect variable	253.23	69.60	43	1763	2675	110584818
Disinhibition	247.11	69.60	43	1763	3091	110584402
Obsessive-compulsive disorder	211.17	69.60	43	1763	7198	110580295
Euphoric mood	202.68	69.60	43	1763	8784	110578709
Akathisia	189.63	69.60	46	1760	17067	110570426
Increased appetite	180.04	69.60	43	1763	14934	110572559
Dyslipidaemia	177.31	69.60	43	1763	15922	110571571
Schizoaffective disorder	155.12	69.60	29	1777	3107	110584386
Irritability	122.64	69.60	41	1765	47768	110539725
Leukaemia	108.20	69.60	25	1781	7493	110580000
Tardive dyskinesia	107.91	69.60	28	1778	13551	110573942
Head titubation	102.71	69.60	18	1788	1339	110586154
Suicide attempt	98.37	69.60	43	1763	103351	110484142
Obesity	97.76	69.60	44	1762	113307	110474186
Leukopenia	95.21	69.60	47	1759	148744	110438749
Prescribed overdose	95.09	69.60	40	1766	87541	110499952
Polydipsia	91.91	69.60	22	1784	7666	110579827
Apraxia	85.48	69.60	18	1788	3522	110583971
Toxicity to various agents	70.66	69.60	60	1746	480495	110106998

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

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Source	Code	Description
ATC	N05AC02	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with piperidine structure
FDA CS	M0016525	Phenothiazines
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018492	Dopamine Antagonists
FDA EPC	N0000175746	Phenothiazine
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35474	anxiolytic drug
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:37890	α-adrenergic antagonist
CHEBI has role	CHEBI:37955	H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role	CHEBI:48279	serotonergic antagonist
CHEBI has role	CHEBI:48561	dopaminergic antagonist
CHEBI has role	CHEBI:65190	first generation antipsychotic
CHEBI has role	CHEBI:76779	EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
CHEBI has role	CHEBI:77402	EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
CHEBI has role	CHEBI:176497	geroprotector

Disease	Relation	SNOMED_ID	DOID
Treatment-Resistant Schizophrenia	indication
Hyperkalemia	contraindication	14140009
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Orthostatic hypotension	contraindication	28651003
Hypokalemia	contraindication	43339004
Epilepsy	contraindication	84757009	DOID:1826
Stupor	contraindication	89458003
Tardive dyskinesia	contraindication	102449007
Prolonged QT interval	contraindication	111975006
Disease of blood AND/OR blood-forming organ	contraindication	191124002	DOID:74
Coma	contraindication	371632003
Breastfeeding (mother)	contraindication	413712001
Congenital long QT syndrome	contraindication	442917000
Predisposed to Torsades de Pointes Cardiac Arrhythmias	contraindication

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	IC50	7.40	WOMBAT-PK	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	8.57	PDSP
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	7.85	PDSP
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	7.60	PDSP
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	ANTAGONIST	IC50	7.30	WOMBAT-PK
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN	ANTAGONIST	Ki	5.60	IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		IC50	7.90	WOMBAT-PK
Nuclear receptor subfamily 1 group I member 3	Nuclear hormone receptor	Q14994	NR1I3_HUMAN				WOMBAT-PK
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		IC50	7.10	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.87	PDSP
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.82	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	7	WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.90	PDSP
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.81	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	ANTAGONIST	Ki	7.10	IUPHAR
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	EC50	8	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.09	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	7.30	IUPHAR
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN	ANTAGONIST	Ki	7.20	IUPHAR
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.15	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.70	IUPHAR
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.87	PDSP
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		Ki	5.62	PDSP
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	8.05	PDSP
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	7.89	PDSP
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	6.80	WOMBAT-PK
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	6.96	PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	6.24	PDSP
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.13	PDSP
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	5.77	PDSP
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5.75	DRUG MATRIX
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	ANTAGONIST	Ki	7.98	PDSP
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	8.69	DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	8.62	PDSP
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	6.00	DRUG MATRIX
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.18	CHEMBL
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	6.44	PDSP
Cytochrome P450 1A2	Enzyme	P05177	CP1A2_HUMAN		IC50	5.03	DRUG MATRIX
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	6.71	PDSP
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	5.53	DRUG MATRIX
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	5.20	DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		IC50	5.30	DRUG MATRIX
Serine/threonine-protein kinase pim-1	Kinase	P11309	PIM1_HUMAN		IC50	5.16	CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	5.19	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.47	PDSP
Mucosa-associated lymphoid tissue lymphoma translocation protein 1	Enzyme	Q9UDY8	MALT1_HUMAN		IC50	5.46	CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	8.59	DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	6.28	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	8.29	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		IC50	8.55	CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT	ANTAGONIST	Ki	7.20	IUPHAR
D(1A) dopamine receptor	GPCR		DRD1_RAT		IC50	7.76	CHEMBL
Histamine H1 receptor	GPCR		HRH1_RAT		IC50	7	CHEMBL
5-hydroxytryptamine receptor 6	GPCR		5HT6R_RAT	ANTAGONIST	Ki	8.20	IUPHAR
Pleiotropic ABC efflux transporter of multiple drugs	Transporter		PDR5_YEAST		IC50	5.89	CHEMBL
Muscarinic acetylcholine receptor	GPCR		ACM1_RAT ACM3_RAT ACM4_RAT ACM5_RAT ACM2_RAT		IC50	8.70	CHEMBL
Serotonin 1 (5-HT1) receptor	GPCR		5HT1A_RAT 5HT1B_RAT 5HT1D_RAT 5HT1F_RAT		IC50	5.06	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		IC50	5.89	CHEMBL
Dopamine receptor	GPCR		DRD1_RAT DRD3_RAT DRD5_RAT DRD4_RAT DRD2_RAT		IC50	7.07	CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT2B_RAT		IC50	7.74	CHEMBL
G protein-activated inward rectifier potassium channel 2	Ion channel		KCNJ6_MOUSE	GATING INHIBITOR	EC50	4.20	IUPHAR

ID	Source
4019946	VUID
N0000148031	NUI
D00373	KEGG_DRUG
130-61-0	SECONDARY_CAS_RN
4017892	VANDF
4019946	VANDF
C0039943	UMLSCUI
CHEBI:9566	CHEBI
LZU	PDB_CHEM_ID
CHEMBL479	ChEMBL_ID
DB00679	DRUGBANK_ID
CHEMBL1200916	ChEMBL_ID
D013881	MESH_DESCRIPTOR_UI
5452	PUBCHEM_CID
100	IUPHAR_LIGAND_ID
818	INN_ID
N3D6TG58NI	UNII
10502	RXNORM
2125	MMSL
5571	MMSL
5572	MMSL
d00389	MMSL
001482	NDDF
004591	NDDF
18550006	SNOMEDCT_US
33588000	SNOMEDCT_US
372706001	SNOMEDCT_US
N3D6TG58NI	INXIGHT DRUGS

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0612	TABLET, FILM COATED	10 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0614	TABLET, FILM COATED	25 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0616	TABLET, FILM COATED	50 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0618	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	48433-095	TABLET, FILM COATED	10 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	48433-096	TABLET, FILM COATED	25 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	48433-097	TABLET, FILM COATED	50 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	48433-098	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-565	TABLET, FILM COATED	10 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-565	TABLET, FILM COATED	10 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-566	TABLET, FILM COATED	25 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-566	TABLET, FILM COATED	25 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-567	TABLET, FILM COATED	50 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-567	TABLET, FILM COATED	50 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-580	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51079-580	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53489-148	TABLET, FILM COATED	10 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53489-149	TABLET, FILM COATED	25 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53489-150	TABLET, FILM COATED	50 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53489-500	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62135-934	TABLET, FILM COATED	10 mg	ORAL	ANDA	13 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62135-936	TABLET, FILM COATED	25 mg	ORAL	ANDA	13 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62135-938	TABLET, FILM COATED	50 mg	ORAL	ANDA	13 sections
Thioridazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62135-939	TABLET, FILM COATED	100 mg	ORAL	ANDA	13 sections

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.22	Basic
pKa2	3.45	Basic