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

Stem definitionDrug idCAS RN
antihypertensive substances, prazosin derivatives 3584 63590-64-7

Description:

MoleculeDescription

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:

DoseUnitRoute
5 mg O

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
Aug. 7, 1987 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hyperkalaemia 35.46 25.86 19 1199 48070 50555836
Sleep disorder due to a general medical condition 30.54 25.86 10 1208 7361 50596545
Shock 26.76 25.86 12 1206 20638 50583268

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dizziness 41.72 15.54 126 7580 189558 29377263
Hypotension 40.79 15.54 127 7579 194227 29372594
Orthostatic hypotension 29.78 15.54 33 7673 22596 29544225
Syncope 28.03 15.54 64 7642 81307 29485514
Asthenia 24.62 15.54 116 7590 215134 29351687
Non-cardiogenic pulmonary oedema 23.30 15.54 8 7698 619 29566202
Heart valve incompetence 18.23 15.54 8 7698 1195 29565626
Sopor 18.05 15.54 18 7688 10916 29555905
Coronary artery disease 17.75 15.54 37 7669 44153 29522668
Pulseless electrical activity 17.40 15.54 14 7692 6420 29560401
Sinus bradycardia 17.15 15.54 18 7688 11585 29555236
Distributive shock 16.40 15.54 7 7699 978 29565843
Toxicity to various agents 16.10 15.54 13 7693 173648 29393173
Myocardial infarction 16.06 15.54 64 7642 110232 29456589

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypotension 64.35 15.40 140 7490 380834 64110268
Dizziness 37.68 15.40 124 7506 430039 64061063
Coronary artery disease 34.38 15.40 39 7591 60394 64430708
Hyperkalaemia 32.14 15.40 49 7581 101080 64390022
Orthostatic hypotension 31.53 15.40 33 7597 46705 64444397
Bradycardia 30.37 15.40 52 7578 118167 64372935
Acute kidney injury 29.55 15.40 118 7512 449122 64041980
Asthenia 26.21 15.40 110 7520 427934 64063168
Myocardial infarction 25.69 15.40 59 7571 165762 64325340
Syncope 24.32 15.40 56 7574 157579 64333523
Non-cardiogenic pulmonary oedema 23.72 15.40 8 7622 1300 64489802
Cerebrovascular accident 21.35 15.40 49 7581 137534 64353568
Presyncope 18.86 15.40 22 7608 35067 64456035
Pulseless electrical activity 18.72 15.40 14 7616 12725 64478377
Blood creatinine increased 18.52 15.40 46 7584 135736 64355366
Heart valve incompetence 17.83 15.40 8 7622 2785 64488317
Distributive shock 17.39 15.40 7 7623 1868 64489234
Gastrointestinal haemorrhage 16.16 15.40 43 7587 132269 64358833
Hyperhidrosis 15.66 15.40 41 7589 124879 64366223
Cardiac failure congestive 15.50 15.40 42 7588 130538 64360564

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 D018663 Adrenergic Agents
MeSH PA D058668 Adrenergic alpha-1 Receptor Antagonists
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D064804 Urological Agents
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:37890 alpha-adrenergic receptor blockaders

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

DiseaseRelationSNOMED_IDDOID
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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 9.08 WOMBAT-PK CHEMBL
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 8.95 WOMBAT-PK CHEMBL
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 9.20 WOMBAT-PK CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 6.93 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR Ki 6.88 WOMBAT-PK
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme WOMBAT-PK
Solute carrier family 22 member 1 Transporter IC50 4.63 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.26 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.75 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 5.45 PDSP
Alpha-1B adrenergic receptor GPCR Ki 8.72 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 9.09 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 8.11 CHEMBL
Alpha-1D adrenergic receptor GPCR Ki 9 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.59 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 9.16 CHEMBL

External reference:

IDSource
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
DB01162 DRUGBANK_ID
CHEMBL3989562 ChEMBL_ID
CHEMBL1256665 ChEMBL_ID
C041226 MESH_SUPPLEMENTAL_RECORD_UI
5401 PUBCHEM_CID
7302 IUPHAR_LIGAND_ID
4843 INN_ID
8L5014XET7 UNII
1299927 RXNORM
31270 MMSL
44696 MMSL
5546 MMSL
d00386 MMSL
000638 NDDF
004492 NDDF
129484001 SNOMEDCT_US
387068008 SNOMEDCT_US
412519000 SNOMEDCT_US
CHEMBL1201091 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Terazosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-1337 CAPSULE 1 mg ORAL ANDA 22 sections
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 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 Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24689-792 CAPSULE 1 mg ORAL ANDA 25 sections
Terazosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24689-855 CAPSULE 2 mg ORAL ANDA 25 sections
Terazosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24689-882 CAPSULE 5 mg ORAL ANDA 25 sections
Terazosin Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24689-961 CAPSULE 10 mg ORAL ANDA 25 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 Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 49999-227 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 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 50090-2371 CAPSULE 10 mg ORAL ANDA 25 sections