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etilefrine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sympathomimetic, phenethyl derivatives | 1101 | 709-55-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phenylephrine-related beta-1 adrenergic and alpha adrenergic agonist used as a cardiotonic and antihypotensive agent.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
| 50 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 3.94 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 38 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 2.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 14 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.77 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.20 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK2,PIK3CB,PIM2,PLK1,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ZAP70 | 38 | |||
| kinase-selectivity-class | AXL,EIF2AK3,EPHB4,GRK2,MAP2K6,TEK | 6 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1929 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Sulphaemoglobinaemia | 46.92 | 31.25 | 7 | 584 | 588 | 110588120 |
| Lip erosion | 45.56 | 31.25 | 8 | 583 | 1858 | 110586850 |
| Postoperative adhesion | 39.43 | 31.25 | 6 | 585 | 575 | 110588133 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C01CA01 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Adrenergic and dopaminergic agents |
| ATC | C01CA51 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Adrenergic and dopaminergic agents |
| MeSH PA | D000316 | Adrenergic alpha-Agonists |
| MeSH PA | D000318 | Adrenergic beta-Agonists |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D013566 | Sympathomimetics |
| MeSH PA | D014662 | Vasoconstrictor Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D058665 | Adrenergic beta-1 Receptor Agonists |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C01CA Adrenergic and dopaminergic agents 25 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.15 | acidic |
| pKa2 | 13.78 | acidic |
| pKa3 | 8.83 | 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 | AGONIST | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| N0000166808 | NUI |
| D01573 | KEGG_DRUG |
| 943-17-9 | SECONDARY_CAS_RN |
| C0015116 | UMLSCUI |
| CHEBI:748373 | CHEBI |
| CHEMBL86882 | ChEMBL_ID |
| DB08985 | DRUGBANK_ID |
| D005039 | MESH_DESCRIPTOR_UI |
| 3306 | PUBCHEM_CID |
| 2229 | INN_ID |
| 14324 | IUPHAR_LIGAND_ID |
| ZB6F8MY53V | UNII |
| 235960 | RXNORM |
| 004352 | NDDF |
| 004353 | NDDF |
| 734508002 | SNOMEDCT_US |
| 96255000 | SNOMEDCT_US |
| ZB6F8MY53V | INXIGHT DRUGS |
Pharmaceutical products:
None