amrinone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| cardiac stimulants, amrinone derivatives | 201 | 60719-84-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.90 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 25 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.01 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 93 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 8.90 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.89 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 31, 1984 | FDA | SANOFI AVENTIS US |
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 | C01CE01 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Phosphodiesterase inhibitors |
| CHEBI has role | CHEBI:50218 | phosphodiesterase inhibitors |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D058987 | Phosphodiesterase 3 Inhibitors |
| MeSH PA | D010726 | Phosphodiesterase Inhibitors |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D014665 | Vasodilator Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Decompensated cardiac failure | indication | 195111005 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Hypovolemia | contraindication | 28560003 | |
| Hypokalemia | contraindication | 43339004 | |
| Low blood pressure | contraindication | 45007003 | |
| Pulmonic valve stenosis | contraindication | 56786000 | DOID:6420 |
| Aortic valve stenosis | contraindication | 60573004 | DOID:1712 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Hypertrophic cardiomyopathy | contraindication | 233873004 | DOID:11984 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Idiopathic hypertrophic subaortic stenosis | contraindication | 360465008 | |
| Myocardial infarction in recovery phase | contraindication | 418044006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.6 | acidic |
| pKa2 | 6.6 | Basic |
| pKa3 | 2.8 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Enzyme | INHIBITOR | IC50 | 4.78 | WOMBAT-PK | CHEMBL | |||
| Dual specificity protein kinase TTK | Kinase | Ki | 4.09 | CHEMBL | |||||
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Enzyme | INHIBITOR | IC50 | 4.51 | IUPHAR | ||||
| Phosphodiesterase 4 | Enzyme | IC50 | 4.39 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021234 | VUID |
| N0000148678 | NUI |
| D00231 | KEGG_DRUG |
| 75898-90-7 | SECONDARY_CAS_RN |
| 738 | RXNORM |
| C0002697 | UMLSCUI |
| CHEBI:2686 | CHEBI |
| CHEMBL12856 | ChEMBL_ID |
| DB01427 | DRUGBANK_ID |
| CHEMBL2096642 | ChEMBL_ID |
| D000676 | MESH_DESCRIPTOR_UI |
| 3698 | PUBCHEM_CID |
| 7202 | IUPHAR_LIGAND_ID |
| 11852 | MMSL |
| 16093 | MMSL |
| 41572 | MMSL |
| 4196 | MMSL |
| d00172 | MMSL |
| 412411004 | SNOMEDCT_US |
| 412412006 | SNOMEDCT_US |
| 60018006 | SNOMEDCT_US |
| 4310 | INN_ID |
| 4018237 | VANDF |
| 4019612 | VANDF |
| 4021233 | VANDF |
| 4021234 | VANDF |
| I229274Y5B | UNII |
| 000616 | NDDF |
| 006203 | NDDF |
Pharmaceutical products:
None