terazosin

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	24.20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.86 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.98 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	9 hours	Lombardo F, Berellini G, Obach RS

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	1.038		Moderate	0.70
caco2-efflux	Caco-2 efflux ratio (BA/AB)	30.832		Moderate	0.70
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	3.776	10^-6 cm/s	Moderate	0.70
dh-clint	Dog hepatocyte intrinsic clearance	0.834	uL/min/10^6 cells	Moderate	0.70
dppb	Dog plasma protein binding (% unbound)	58.880	%	Moderate	0.70
fcs-ppb	Fetal calf serum protein binding (% unbound)	81.600	%	Moderate	0.70
herg	hERG pIC50	4.655	pIC50	Moderate	0.70
hh-clint	Human hepatocyte intrinsic clearance	1.052	uL/min/10^6 cells	Moderate	0.70
hlm-clint	Human liver microsomal intrinsic clearance	3.013	uL/min/mg protein	Moderate	0.70
hppb	Human plasma protein binding (% unbound)	33.590	%	Moderate	0.70
kinase-safety-class	ACVR2B,EIF2AK3,GRK2,MAPK7,PDK2,PDK4,PIK3CD,PRKDC	8
kinase-selectivity-class	PRKDC,TTK	2
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	11.194		Moderate	0.70
mh-clint	Mouse hepatocyte intrinsic clearance	9.036		Moderate	0.70
mppb	Mouse plasma protein binding (% unbound)	59.880		Moderate	0.70
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	16.749		Moderate	0.70
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	0		Moderate	0.70
pppb	Pig plasma protein binding (% unbound)	74.390	%	Moderate	0.70
rh-clint	Rat hepatocyte intrinsic clearance	2.099	uL/min/10^6 cells	Moderate	0.70
rh-fuinc	Rat hepatocyte fraction unbound in incubation	81.150	%	Moderate	0.70
rppb	Rat plasma protein binding (% unbound)	57.430	%	Moderate	0.70
solubility-dd	Solubility at pH 7.4 in DMSO	749.894	uM	Moderate	0.70

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
Neoplasm skin	68.12	24.57	16	2409	3126	90622896
Vulvovaginal mycotic infection	61.62	24.57	17	2408	6297	90619725
Haemorrhoidal haemorrhage	59.74	24.57	16	2409	5307	90620715
Chest discomfort	49.80	24.57	36	2389	138329	90487693
Hypovolaemia	46.36	24.57	16	2409	12415	90613607
Hyperkalaemia	46.20	24.57	26	2399	64938	90561084
Blood pressure increased	34.79	24.57	34	2391	197183	90428839
Haemorrhoids	34.50	24.57	16	2409	26686	90599336
Clostridium difficile colitis	34.50	24.57	16	2409	26690	90599332
Cardiomegaly	33.02	24.57	14	2411	18911	90607111
Transplant dysfunction	32.75	24.57	10	2415	5272	90620750
Transient ischaemic attack	27.25	24.57	16	2409	43160	90582862
Iliac artery stenosis	26.04	24.57	4	2421	78	90625944
Dyspnoea	25.90	24.57	66	2359	880889	89745133
Forced expiratory flow decreased	24.62	24.57	4	2421	113	90625909

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
Hypotension	41.99	15.46	147	10142	257484	42353562
Dizziness	40.43	15.46	142	10147	249112	42361934
Syncope	38.08	15.46	78	10211	99328	42511718
Asthenia	35.67	15.46	148	10141	280645	42330401
Orthostatic hypotension	31.70	15.46	38	10251	30532	42580514
White coat hypertension	28.40	15.46	8	10281	346	42610700
Pulseless electrical activity	27.74	15.46	20	10269	8417	42602629
Blood alkaline phosphatase abnormal	27.71	15.46	9	10280	633	42610413
Heart valve incompetence	26.11	15.46	11	10278	1608	42609438
Myasthenic syndrome	25.54	15.46	9	10280	812	42610234
Distributive shock	24.51	15.46	12	10277	2484	42608562
Myocardial infarction	23.92	15.46	75	10214	123934	42487112
Bradyarrhythmia	23.72	15.46	12	10277	2663	42608383
Toxicity to various agents	23.58	15.46	13	10276	229123	42381923
Non-cardiogenic pulmonary oedema	20.77	15.46	8	10281	927	42610119
Dysuria	20.50	15.46	31	10258	31065	42579981
Chest pain	18.80	15.46	75	10214	139455	42471591
Presyncope	18.72	15.46	25	10264	22362	42588684
Diffuse alveolar damage	18.34	15.46	10	10279	2582	42608464
Prostatic disorder	17.55	15.46	11	10278	3678	42607368
Fall	16.59	15.46	105	10184	234415	42376631
Sopor	16.36	15.46	18	10271	13184	42597862
Sinus bradycardia	16.28	15.46	19	10270	14834	42596212
Coronary artery disease	15.85	15.46	38	10251	53682	42557364

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
Hypotension	67.96	15.36	159	11159	523690	110054291
Hyperkalaemia	60.48	15.36	72	11246	135724	110442257
Neoplasm skin	46.54	15.36	16	11302	3188	110574793
Acute kidney injury	42.42	15.36	152	11166	635278	109942703
Vulvovaginal mycotic infection	41.88	15.36	17	11301	5360	110572621
Myocardial infarction	38.67	15.36	70	11248	192013	110385968
Bradycardia	38.32	15.36	62	11256	155455	110422526
Orthostatic hypotension	37.82	15.36	40	11278	66209	110511772
Syncope	34.81	15.36	69	11249	202467	110375514
Dizziness	34.48	15.36	152	11166	698041	109879940
Coronary artery disease	33.54	15.36	39	11279	71651	110506330
Asthenia	33.26	15.36	149	11169	688850	109889131
Blood pressure increased	32.94	15.36	78	11240	258295	110319686
Haemorrhoidal haemorrhage	32.22	15.36	16	11302	8077	110569904
Pulseless electrical activity	30.86	15.36	20	11298	16737	110561244
Myasthenic syndrome	29.23	15.36	9	11309	1267	110576714
Chest pain	27.63	15.36	93	11225	376282	110201699
Prostatic disorder	26.88	15.36	10	11308	2499	110575482
Bradyarrhythmia	26.53	15.36	12	11306	4922	110573059
Heart valve incompetence	25.59	15.36	11	11307	3998	110573983
Cardiovascular disorder	25.35	15.36	20	11298	22740	110555241
Prostatomegaly	24.99	15.36	11	11307	4231	110573750
Chest discomfort	24.93	15.36	55	11263	173793	110404188
Distributive shock	24.47	15.36	12	11306	5892	110572089
Hypovolaemia	24.04	15.36	19	11299	21655	110556326
Cerebrovascular accident	23.38	15.36	55	11263	181229	110396752
Renal failure	23.23	15.36	63	11255	226511	110351470
Blood creatinine increased	23.06	15.36	55	11263	182834	110395147
Cardiomegaly	22.99	15.36	21	11297	29109	110548872
Diffuse alveolar damage	22.26	15.36	10	11308	4037	110573944
Dysuria	22.10	15.36	29	11289	60202	110517779
Presyncope	21.87	15.36	26	11292	48861	110529120
Non-cardiogenic pulmonary oedema	21.60	15.36	8	11310	1976	110576005
Blood alkaline phosphatase abnormal	20.95	15.36	7	11311	1280	110576701
Transient ischaemic attack	20.73	15.36	29	11289	63953	110514028
White coat hypertension	20.71	15.36	7	11311	1324	110576657
Atrial fibrillation	19.80	15.36	60	11258	229582	110348399
Dyspnoea	19.75	15.36	186	11132	1106686	109471295
Drug intolerance	18.87	15.36	9	11309	406503	110171478
Treatment failure	18.66	15.36	3	11315	277231	110300750
Alopecia	18.65	15.36	7	11311	364746	110213235
Cardiac failure congestive	18.59	15.36	45	11273	150955	110427026
Hepatic enzyme increased	18.46	15.36	5	11313	320887	110257094
Death	18.16	15.36	128	11190	698741	109879240
Transplant dysfunction	17.99	15.36	11	11307	8317	110569664
COVID-19 immunisation	17.05	15.36	6	11312	1280	110576701
Postoperative hypertension	16.95	15.36	3	11315	35	110577946
Gastrointestinal haemorrhage	16.93	15.36	46	11272	165472	110412509
Maternal exposure during pregnancy	16.62	15.36	3	11315	254880	110323101
Systemic lupus erythematosus	16.57	15.36	3	11315	254335	110323646
Iliac artery stenosis	16.57	15.36	4	11314	226	110577755
Hospitalisation	16.00	15.36	41	11277	142452	110435529
Sinus bradycardia	15.42	15.36	17	11301	29466	110548515
Forced expiratory flow decreased	15.38	15.36	4	11314	306	110577675

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terazosin 🐶 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	G04CA03	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
FDA MoA	N0000000099	Adrenergic alpha-Antagonists
FDA EPC	N0000175553	alpha-Adrenergic Blocker
MeSH PA	D000317	Adrenergic alpha-Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D058668	Adrenergic alpha-1 Receptor Antagonists
MeSH PA	D064804	Urological Agents
CHEBI has role	CHEBI:35526	hypoglycemic agent
CHEBI has role	CHEBI:35554	cardiovascular drug
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:35674	antihypertensive agent
CHEBI has role	CHEBI:37890	α-adrenergic antagonist
CHEBI has role	CHEBI:48407	antiparkinson drug
CHEBI has role	CHEBI:145947	antiatherosclerotic agent

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Benign prostatic hyperplasia	indication	266569009
Priapism	contraindication	6273006	DOID:9286
Orthostatic hypotension	contraindication	28651003
Cataract surgery	contraindication	110473004
Syncope	contraindication	271594007
Intraoperative floppy iris syndrome	contraindication	418801006

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 1MG BASE/ML	TEZRULY	NOVITIUM PHARMA	N218139	July 29, 2024	DISCN	SOLUTION	ORAL	11224572	Feb. 1, 2041	TREATMENT OF HYPERTENSION IN PATIENTS WHO ARE IN NEED OF A LIQUID COMPOSITION OF TERAZOSIN
EQ 1MG BASE/ML	TEZRULY	NOVITIUM PHARMA	N218139	July 29, 2024	DISCN	SOLUTION	ORAL	11224572	Feb. 1, 2041	TREATMENT OF SYMPTOMATIC BENIGN PROSTATIC HYPERPLASIA (BPH) IN PATIENTS WHO ARE IN NEED OF A LIQUID COMPOSITION OF TERAZOSIN
EQ 1MG BASE/ML	TEZRULY	NOVITIUM PHARMA	N218139	July 29, 2024	DISCN	SOLUTION	ORAL	12427108	Feb. 1, 2041	TREATMENT OF HYPERTENSION IN PATIENTS WHO ARE IN NEED OF A LIQUID COMPOSITION OF TERAZOSIN
EQ 1MG BASE/ML	TEZRULY	NOVITIUM PHARMA	N218139	July 29, 2024	DISCN	SOLUTION	ORAL	12427108	Feb. 1, 2041	TREATMENT OF SYMPTOMATIC BENIGN PROSTATIC HYPERPLASIA (BPH) IN PATIENTS WHO ARE IN NEED OF A LIQUID COMPOSITION OF TERAZOSIN

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	9.08	WOMBAT-PK	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	8.95	WOMBAT-PK	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	9.20	WOMBAT-PK	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.93	WOMBAT-PK
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.88	WOMBAT-PK
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN				WOMBAT-PK
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.63	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.26	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.75	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	5.45	PDSP
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	8.72	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		Ki	9.09	CHEMBL
Alpha-2B adrenergic receptor	GPCR		ADA2B_RAT		Ki	8.11	CHEMBL
Alpha-1D adrenergic receptor	GPCR		ADA1D_RAT		Ki	9	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		Ki	7.59	CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_MESAU		Ki	9.16	CHEMBL

ID	Source
4019940	VUID
N0000179262	NUI
D00610	KEGG_DRUG
70024-40-7	SECONDARY_CAS_RN
63074-08-8	SECONDARY_CAS_RN
4019435	VANDF
4019940	VANDF
C0076107	UMLSCUI
CHEBI:9445	CHEBI
TZN	PDB_CHEM_ID
CHEMBL611	ChEMBL_ID
CHEMBL3989562	ChEMBL_ID
DB01162	DRUGBANK_ID
CHEMBL1201091	ChEMBL_ID
C041226	MESH_SUPPLEMENTAL_RECORD_UI
5401	PUBCHEM_CID
7302	IUPHAR_LIGAND_ID
4843	INN_ID
8L5014XET7	UNII
1299927	RXNORM
31270	MMSL
36586	MMSL
44696	MMSL
5546	MMSL
d00386	MMSL
000638	NDDF
004492	NDDF
1269092006	SNOMEDCT_US
129484001	SNOMEDCT_US
387068008	SNOMEDCT_US
412519000	SNOMEDCT_US

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-289	CAPSULE	10 mg	ORAL	ANDA	22 sections
Terazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-812	CAPSULE	2 mg	ORAL	ANDA	24 sections
Terazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-813	CAPSULE	5 mg	ORAL	ANDA	24 sections
terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	23155-735	CAPSULE	1 mg	ORAL	ANDA	20 sections
terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	23155-736	CAPSULE	2 mg	ORAL	ANDA	20 sections
terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	23155-737	CAPSULE	5 mg	ORAL	ANDA	20 sections
terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	23155-738	CAPSULE	10 mg	ORAL	ANDA	20 sections
Terazosin	Human Prescription Drug Label	1	27241-288	CAPSULE	1 mg	ORAL	ANDA	12 sections
Terazosin	Human Prescription Drug Label	1	27241-289	CAPSULE	2 mg	ORAL	ANDA	12 sections
Terazosin	Human Prescription Drug Label	1	27241-290	CAPSULE	5 mg	ORAL	ANDA	12 sections
Terazosin	Human Prescription Drug Label	1	27241-291	CAPSULE	10 mg	ORAL	ANDA	12 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	33261-211	CAPSULE	1 mg	ORAL	ANDA	22 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	33261-212	CAPSULE	2 mg	ORAL	ANDA	22 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	33261-870	CAPSULE	10 mg	ORAL	ANDA	22 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	42291-820	CAPSULE	1 mg	ORAL	ANDA	26 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	42291-821	CAPSULE	2 mg	ORAL	ANDA	26 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	42291-822	CAPSULE	5 mg	ORAL	ANDA	26 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	42291-823	CAPSULE	10 mg	ORAL	ANDA	26 sections
TERAZOSIN HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	42549-666	CAPSULE	5 mg	ORAL	ANDA	24 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	50090-0657	CAPSULE	1 mg	ORAL	ANDA	25 sections
Terazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-0659	CAPSULE	10 mg	ORAL	ANDA	25 sections
Terazosin	Human Prescription Drug Label	1	50090-1559	CAPSULE	5 mg	ORAL	ANDA	25 sections
Terazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-1943	CAPSULE	5 mg	ORAL	ANDA	25 sections
Terazosin	Human Prescription Drug Label	1	50090-2371	CAPSULE	10 mg	ORAL	ANDA	25 sections
Terazosin	Human Prescription Drug Label	1	50090-2623	CAPSULE	2 mg	ORAL	ANDA	25 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	50268-764	CAPSULE	1 mg	ORAL	ANDA	26 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	50268-765	CAPSULE	2 mg	ORAL	ANDA	26 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	50268-766	CAPSULE	5 mg	ORAL	ANDA	26 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	50268-767	CAPSULE	10 mg	ORAL	ANDA	26 sections
terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	51655-915	CAPSULE	2 mg	ORAL	ANDA	20 sections

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.22	Basic
pKa2	0.72	Basic