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

Stem definition	Drug id	CAS RN
antihypertensive substances, prazosin derivatives	3584	63590-64-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: terazosin terazosin hydrochloride terazosin hydrochloride anhydrous terazosine terazosin hydrochloride hydrate terazosin HCl	induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia Molecular weight: 387.44 Formula: C19H25N5O4 CLOGP: 2.23 LIPINSKI: 0 HAC: 9 HDO: 1 TPSA: 103.04 ALOGS: -2.41 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

terazosin
terazosin hydrochloride
terazosin hydrochloride anhydrous
terazosine
terazosin hydrochloride hydrate
terazosin HCl

induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia

Molecular weight: 387.44
Formula: C19H25N5O4
CLOGP: 2.23
LIPINSKI: 0
HAC: 9
HDO: 1
TPSA: 103.04
ALOGS: -2.41
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
5	mg	O

ADMET properties:

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

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Approvals:

Date	Agency	Company	Orphan
Aug. 7, 1987	FDA

FDA Adverse Event Reporting System (Female)

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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
Hyperkalaemia	40.60	26.23	22	1581	54181	63433238
Sleep disorder due to a general medical condition	32.31	26.23	12	1591	12176	63475243

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FDA Adverse Event Reporting System (Male)

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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	44.33	15.10	139	8633	221510	34726649
Syncope	36.92	15.10	75	8697	91376	34856783
Dizziness	36.51	15.10	129	8643	218392	34729767
Orthostatic hypotension	33.88	15.10	37	8735	25882	34922277
Distributive shock	32.02	15.10	12	8760	1242	34946917
Asthenia	31.33	15.10	133	8639	245118	34703041
Pulseless electrical activity	29.88	15.10	20	8752	7191	34940968
Heart valve incompetence	26.77	15.10	11	8761	1453	34946706
Bradyarrhythmia	25.55	15.10	12	8760	2179	34945980
Non-cardiogenic pulmonary oedema	23.18	15.10	8	8764	653	34947506

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FDA Adverse Event Reporting System (Geriatric)

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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	67.47	15.89	151	8816	440166	79295255
Hyperkalaemia	50.09	15.89	63	8904	114335	79621086
Orthostatic hypotension	38.38	15.89	39	8928	56125	79679296
Bradycardia	34.85	15.89	58	8909	135499	79599922
Asthenia	33.80	15.89	130	8837	511559	79223862
Acute kidney injury	33.52	15.89	131	8836	519273	79216148
Coronary artery disease	33.44	15.89	39	8928	65435	79669986
Distributive shock	32.49	15.89	12	8955	2675	79732746
Pulseless electrical activity	32.22	15.89	20	8947	14140	79721281
Dizziness	31.75	15.89	130	8837	526311	79209110

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G04CA03	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY Alpha-adrenoreceptor antagonists
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
FDA EPC	N0000175553	alpha-Adrenergic Blocker
FDA MoA	N0000000099	Adrenergic alpha-Antagonists
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D058668	Adrenergic alpha-1 Receptor Antagonists
MeSH PA	D000317	Adrenergic alpha-Antagonists
MeSH PA	D018674	Adrenergic Antagonists

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

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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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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

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External reference:

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ID	Source
TZN	PDB_CHEM_ID
000638	NDDF
004492	NDDF
1269092006	SNOMEDCT_US
129484001	SNOMEDCT_US
1299927	RXNORM
31270	MMSL
387068008	SNOMEDCT_US
4019435	VANDF
4019940	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-1338	CAPSULE	2 mg	ORAL	ANDA	25 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-1339	CAPSULE	5 mg	ORAL	ANDA	25 sections
Terazosin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-289	CAPSULE	10 mg	ORAL	ANDA	22 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	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

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