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metildigoxin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1761 | 30685-43-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A semisynthetic digitalis glycoside with the general properties of DIGOXIN but more rapid onset of action. Its cardiotonic action is prolonged by its demethylation to DIGOXIN in the liver. It has been used in the treatment of congestive heart failure (HEART FAILURE).
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | mg | O |
| 0.20 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.01 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.690 | Moderate | 0.79 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 22.387 | Moderate | 0.79 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 11.194 | 10^-6 cm/s | Moderate | 0.79 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.344 | uL/min/10^6 cells | Moderate | 0.79 |
| dppb | Dog plasma protein binding (% unbound) | 48.500 | % | Moderate | 0.79 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 45.010 | % | Moderate | 0.79 |
| herg | hERG pIC50 | 4.363 | pIC50 | Moderate | 0.79 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.560 | uL/min/10^6 cells | Moderate | 0.79 |
| hlm-clint | Human liver microsomal intrinsic clearance | 5.984 | uL/min/mg protein | Moderate | 0.79 |
| hppb | Human plasma protein binding (% unbound) | 50.230 | % | Moderate | 0.79 |
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 15.885 | High | 0.88 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 22.594 | Moderate | 0.79 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.458 | Moderate | 0.79 | |
| mppb | Mouse plasma protein binding (% unbound) | 33.330 | Moderate | 0.79 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 41.783 | Moderate | 0.79 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 0.88 | |
| pppb | Pig plasma protein binding (% unbound) | 47.300 | % | Moderate | 0.79 |
| rat-kpuu-brain | Rat brain Kpuu | 0.019 | % | High | 0.88 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.767 | uL/min/10^6 cells | Moderate | 0.79 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 70.630 | % | Moderate | 0.79 |
| rppb | Rat plasma protein binding (% unbound) | 41.730 | % | Moderate | 0.79 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 774.462 | uM | Moderate | 0.79 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Bradycardia | 71.42 | 35.44 | 31 | 1263 | 83816 | 90543337 |
| Cardiac failure | 69.59 | 35.44 | 33 | 1261 | 109463 | 90517690 |
| Wound haemorrhage | 67.80 | 35.44 | 14 | 1280 | 2853 | 90624300 |
| Toxic neuropathy | 61.58 | 35.44 | 10 | 1284 | 538 | 90626615 |
| Troponin T increased | 50.74 | 35.44 | 10 | 1284 | 1613 | 90625540 |
| Refractory anaemia with an excess of blasts | 49.17 | 35.44 | 8 | 1286 | 435 | 90626718 |
| Renal impairment | 44.16 | 35.44 | 24 | 1270 | 105397 | 90521756 |
| Haematoma | 41.76 | 35.44 | 17 | 1277 | 39031 | 90588122 |
| Congestive cardiomyopathy | 35.71 | 35.44 | 10 | 1284 | 7344 | 90619809 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Cardiac failure chronic | 55.08 | 34.74 | 17 | 1095 | 9584 | 42610639 |
| Cardiac failure | 44.40 | 34.74 | 30 | 1082 | 106826 | 42513397 |
| N-terminal prohormone brain natriuretic peptide increased | 37.23 | 34.74 | 10 | 1102 | 3443 | 42616780 |
| Micturition disorder | 35.52 | 34.74 | 9 | 1103 | 2471 | 42617752 |
| Dyspnoea at rest | 35.18 | 34.74 | 10 | 1102 | 4239 | 42615984 |
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 |
|---|---|---|---|---|---|---|
| Cardiac failure | 108.44 | 29.94 | 61 | 2357 | 187565 | 110399316 |
| Cardiac failure chronic | 68.47 | 29.94 | 21 | 2397 | 13790 | 110573091 |
| Wound haemorrhage | 54.83 | 29.94 | 14 | 2404 | 4724 | 110582157 |
| Toxic neuropathy | 50.14 | 29.94 | 10 | 2408 | 1113 | 110585768 |
| Bradycardia | 47.88 | 29.94 | 34 | 2384 | 155483 | 110431398 |
| Cerebral infarction | 44.47 | 29.94 | 22 | 2396 | 51816 | 110535065 |
| N-terminal prohormone brain natriuretic peptide increased | 42.12 | 29.94 | 12 | 2406 | 6109 | 110580772 |
| Refractory anaemia with an excess of blasts | 40.58 | 29.94 | 8 | 2410 | 839 | 110586042 |
| Congestive cardiomyopathy | 39.65 | 29.94 | 14 | 2404 | 14205 | 110572676 |
| Aortic stenosis | 36.96 | 29.94 | 13 | 2405 | 13046 | 110573835 |
| Troponin T increased | 36.77 | 29.94 | 10 | 2408 | 4296 | 110582585 |
| Dyspnoea | 35.73 | 29.94 | 76 | 2342 | 1106796 | 109480085 |
| Renal impairment | 33.82 | 29.94 | 30 | 2388 | 188415 | 110398466 |
| Embolic stroke | 33.79 | 29.94 | 11 | 2407 | 8732 | 110578149 |
| Micturition disorder | 31.38 | 29.94 | 9 | 2409 | 4689 | 110582192 |
| Dyspnoea at rest | 30.24 | 29.94 | 10 | 2408 | 8336 | 110578545 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C01AA08 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC GLYCOSIDES Digitalis glycosides |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D020011 | Protective Agents |
Related Drugs by ATC class:
C01AA Digitalis glycosides 7 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
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium/potassium-transporting ATPase subunit alpha-1 | Transporter | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000168450 | NUI |
| D02587 | KEGG_DRUG |
| C0025132 | UMLSCUI |
| CHEMBL1697843 | ChEMBL_ID |
| DB13401 | DRUGBANK_ID |
| 2876 | INN_ID |
| I7GG1YUC5V | UNII |
| 443946 | PUBCHEM_CID |
| 6686 | RXNORM |
| 006744 | NDDF |
| 317911001 | SNOMEDCT_US |
| 418574005 | SNOMEDCT_US |
| D008520 | MESH_DESCRIPTOR_UI |
| CHEBI:135885 | CHEBI |
Pharmaceutical products:
None