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amrinone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.308 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.855 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 11.402 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 0.998 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 74.520 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 84.210 | % | High | 1 |
| herg | hERG pIC50 | 4.010 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.059 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.388 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 76.140 | % | High | 1 |
| kinase-safety-class | ACVR1B,ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK19,CDK5,CDK7,CDK9,CHEK1,CLK2,CLK4,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EIF2AK3,ERBB2,FLT3,GRK1,GRK2,GRK3,GSK3B,HASPIN,IKBKB,IRAK1,IRAK3,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAPK1,MAPK12,MAPK3,MAPK7,MAPK9,MARK4,MELK,MET,MINK1,MKNK2,MTOR,NTRK2,PDK1,PDK4,PIM2,PRKAA2,PRKCD,PRKDC,ROCK1,ROCK2,SGK1,SIK2,SIK3,STK33,SYK,TEK,TNIK,TTK,ULK1,ULK2 | 79 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK9,CLK4,DYRK1A,DYRK1B,EGFR,ERBB2,ERBB4,GRK2,GRK3,HASPIN,IRAK1,MAP2K6,MAP3K10,MAP3K14,MAP3K21,MAP4K3,MAPK7,MARK4,MINK1,PRKAA1,PRKAA2,PRKCD,ROCK1,ROCK2,SGK1,SIK2,SIK3,STK33,TGFBR1,TNIK,ULK1,ULK2 | 39 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.812 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.228 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 82.650 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.581 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 74.170 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.239 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 92.070 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 72.820 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 874.984 | uM | High | 1 |
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:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:50218 | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D010726 | Phosphodiesterase Inhibitors |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D058987 | Phosphodiesterase 3 Inhibitors |
Related Drugs by ATC class:
C01CE Phosphodiesterase inhibitors 3 drugs
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 |
| 11852 | MMSL |
| 16093 | MMSL |
| 41572 | MMSL |
| 4196 | MMSL |
| d00172 | MMSL |
| 7202 | IUPHAR_LIGAND_ID |
| 4310 | INN_ID |
| 4018237 | VANDF |
| 4019612 | VANDF |
| 4021233 | VANDF |
| 4021234 | VANDF |
| I229274Y5B | UNII |
| 000616 | NDDF |
| 006203 | NDDF |
| 412411004 | SNOMEDCT_US |
| 412412006 | SNOMEDCT_US |
| 60018006 | SNOMEDCT_US |
| I229274Y5B | INXIGHT DRUGS |
Pharmaceutical products:
None