oxprenolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 2027 | 6452-71-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.16 | g | O |
| 0.16 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 30.86 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 3 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 15.14 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 44 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.72 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 7.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.19 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.09 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | NOVARTIS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C07AA02 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective |
| ATC | C07BA02 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, non-selective, and thiazides |
| ATC | C07CA02 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, non-selective, and other diuretics |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D013565 | Sympatholytics |
| MeSH PA | D014149 | Tranquilizing Agents |
| MeSH PA | D014665 | Vasodilator Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Ventricular arrhythmia | indication | 44103008 | |
| Anxiety | indication | 48694002 | |
| Angina pectoris | indication | 194828000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.19 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.11 | WOMBAT-PK | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | ANTAGONIST | Ki | 8 | WOMBAT-PK | CHEMBL | |||
| Solute carrier family 22 member 1 | Transporter | IC50 | 4.54 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.03 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01806 | KEGG_DRUG |
| 6452-73-9 | SECONDARY_CAS_RN |
| C0030040 | UMLSCUI |
| CHEBI:31949 | CHEBI |
| CHEMBL546 | ChEMBL_ID |
| CHEMBL1200745 | ChEMBL_ID |
| DB01580 | DRUGBANK_ID |
| D010096 | MESH_DESCRIPTOR_UI |
| 4631 | PUBCHEM_CID |
| 7255 | IUPHAR_LIGAND_ID |
| 2506 | INN_ID |
| 519MXN9YZR | UNII |
| 203131 | RXNORM |
| 003463 | NDDF |
| 004748 | NDDF |
| 387583006 | SNOMEDCT_US |
| 395817005 | SNOMEDCT_US |
| 96299009 | SNOMEDCT_US |
Pharmaceutical products:
None