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 |
|---|---|
|
Synonyms:
|
induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mg | O |
ADMET properties:
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 7, 1987 | FDA |
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 |
|---|---|---|---|---|---|---|
| Hyperkalaemia | 33.84 | 26.02 | 19 | 1382 | 50846 | 56239820 |
| Sleep disorder due to a general medical condition | 31.99 | 26.02 | 11 | 1390 | 9079 | 56281587 |
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 |
|---|---|---|---|---|---|---|
| Hypotension | 45.40 | 14.83 | 135 | 8000 | 204483 | 31484726 |
| Dizziness | 40.99 | 14.83 | 128 | 8007 | 199019 | 31490190 |
| Syncope | 38.26 | 14.83 | 74 | 8061 | 85108 | 31604101 |
| Orthostatic hypotension | 31.88 | 14.83 | 35 | 8100 | 24084 | 31665125 |
| Distributive shock | 29.53 | 14.83 | 11 | 8124 | 1094 | 31688115 |
| Pulseless electrical activity | 28.31 | 14.83 | 19 | 8116 | 6708 | 31682501 |
| Asthenia | 24.37 | 14.83 | 118 | 8017 | 224637 | 31464572 |
| Heart valve incompetence | 24.12 | 14.83 | 10 | 8125 | 1320 | 31687889 |
| Non-cardiogenic pulmonary oedema | 23.22 | 14.83 | 8 | 8127 | 635 | 31688574 |
| Bradyarrhythmia | 22.77 | 14.83 | 11 | 8124 | 2080 | 31687129 |
| Sinus bradycardia | 18.55 | 14.83 | 19 | 8116 | 12068 | 31677141 |
| Myocardial infarction | 18.04 | 14.83 | 67 | 8068 | 113387 | 31575822 |
| Presyncope | 17.64 | 14.83 | 22 | 8113 | 17306 | 31671903 |
| Sopor | 17.44 | 14.83 | 18 | 8117 | 11534 | 31677675 |
| Coronary artery disease | 17.06 | 14.83 | 37 | 8098 | 46050 | 31643159 |
| Toxicity to various agents | 17.06 | 14.83 | 13 | 8122 | 181474 | 31507735 |
| Diffuse alveolar damage | 16.81 | 14.83 | 9 | 8126 | 2110 | 31687099 |
| Loss of consciousness | 15.18 | 14.83 | 49 | 8086 | 77306 | 31611903 |
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 |
|---|---|---|---|---|---|---|
| Hypotension | 68.94 | 15.21 | 147 | 8040 | 404234 | 70516023 |
| Dizziness | 36.52 | 15.21 | 127 | 8060 | 464014 | 70456243 |
| Orthostatic hypotension | 36.51 | 15.21 | 37 | 8150 | 51706 | 70868551 |
| Coronary artery disease | 33.97 | 15.21 | 39 | 8148 | 62697 | 70857560 |
| Hyperkalaemia | 33.92 | 15.21 | 51 | 8136 | 106540 | 70813717 |
| Syncope | 32.55 | 15.21 | 64 | 8123 | 165645 | 70754612 |
| Bradycardia | 30.60 | 15.21 | 53 | 8134 | 124562 | 70795695 |
| Distributive shock | 30.54 | 15.21 | 11 | 8176 | 2226 | 70918031 |
| Pulseless electrical activity | 30.47 | 15.21 | 19 | 8168 | 13196 | 70907061 |
| Acute kidney injury | 29.93 | 15.21 | 121 | 8066 | 474503 | 70445754 |
| Myocardial infarction | 28.65 | 15.21 | 62 | 8125 | 171583 | 70748674 |
| Asthenia | 27.53 | 15.21 | 115 | 8072 | 457551 | 70462706 |
| Bradyarrhythmia | 24.47 | 15.21 | 11 | 8176 | 3942 | 70916315 |
| Heart valve incompetence | 24.13 | 15.21 | 10 | 8177 | 2946 | 70917311 |
| Non-cardiogenic pulmonary oedema | 23.51 | 15.21 | 8 | 8179 | 1369 | 70918888 |
| Presyncope | 21.49 | 15.21 | 24 | 8163 | 37414 | 70882843 |
| Blood creatinine increased | 20.89 | 15.21 | 49 | 8138 | 142952 | 70777305 |
| Cerebrovascular accident | 20.78 | 15.21 | 49 | 8138 | 143421 | 70776836 |
| Prostatomegaly | 20.06 | 15.21 | 9 | 8178 | 3210 | 70917047 |
| Diffuse alveolar damage | 19.68 | 15.21 | 9 | 8178 | 3354 | 70916903 |
| Gastrointestinal haemorrhage | 17.84 | 15.21 | 45 | 8142 | 137363 | 70782894 |
| Prostatic disorder | 17.52 | 15.21 | 7 | 8180 | 1878 | 70918379 |
| Sinus bradycardia | 16.85 | 15.21 | 17 | 8170 | 23606 | 70896651 |
| Lactic acidosis | 16.40 | 15.21 | 28 | 8159 | 64996 | 70855261 |
| Cardiac failure congestive | 16.18 | 15.21 | 43 | 8144 | 135414 | 70784843 |
| Hyperhidrosis | 15.95 | 15.21 | 42 | 8145 | 131544 | 70788713 |
| Rheumatoid arthritis | 15.73 | 15.21 | 7 | 8180 | 291798 | 70628459 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| 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 | 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|
| 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 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| 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 |
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 | 24689-792 | 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 | 24689-855 | 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 | 24689-882 | CAPSULE | 5 mg | ORAL | ANDA | 25 sections |
| Terazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24689-961 | CAPSULE | 10 mg | ORAL | ANDA | 25 sections |
| Terazosin 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 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 |