penbutolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 2078 | 38363-40-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A nonselective beta-blocker used as an antihypertensive and an antianginal agent.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 40 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 3.92 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 93 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 7 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 30, 1987 | FDA |
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 | C07AA23 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective |
| ATC | C07CA23 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, non-selective, and other diuretics |
| FDA MoA | N0000000161 | Adrenergic beta-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:35530 | beta-adrenergic blockers |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Angina pectoris | off-label use | 194828000 | |
| Bronchospasm | contraindication | 4386001 | |
| Complete atrioventricular block | contraindication | 27885002 | |
| Depressive disorder | contraindication | 35489007 | |
| Anaphylaxis | contraindication | 39579001 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Cardiogenic shock | contraindication | 89138009 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Partial atrioventricular block | contraindication | 195039008 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Raynaud's phenomenon | contraindication | 266261006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Severe chronic obstructive pulmonary disease | contraindication | 313299006 | |
| Right ventricular failure | contraindication | 367363000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.31 | 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 | 8.80 | WOMBAT-PK | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | ANTAGONIST | Ki | 9 | WOMBAT-PK | CHEMBL | |||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.92 | WOMBAT-PK | |||||
| Alpha-1-acid glycoprotein 1 | Secreted | WOMBAT-PK | |||||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.62 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019879 | VUID |
| N0000147964 | NUI |
| D00602 | KEGG_DRUG |
| 38363-32-5 | SECONDARY_CAS_RN |
| 4019466 | VANDF |
| 4019879 | VANDF |
| C0030812 | UMLSCUI |
| CHEBI:7954 | CHEBI |
| CHEMBL1290 | ChEMBL_ID |
| DB01359 | DRUGBANK_ID |
| CHEMBL2361370 | ChEMBL_ID |
| CHEMBL1200363 | ChEMBL_ID |
| D010394 | MESH_DESCRIPTOR_UI |
| 37464 | PUBCHEM_CID |
| 7263 | IUPHAR_LIGAND_ID |
| 3017 | INN_ID |
| 78W62V43DY | UNII |
| 7973 | RXNORM |
| 5241 | MMSL |
| d00332 | MMSL |
| 001862 | NDDF |
| 004746 | NDDF |
| 108542009 | SNOMEDCT_US |
| 372505004 | SNOMEDCT_US |
| 386865000 | SNOMEDCT_US |
Pharmaceutical products:
None