Stem definition | Drug id | CAS RN |
---|---|---|
antiarrhythmics | 176 | 1951-25-3 |
Dose | Unit | Route |
---|---|---|
0.20 | g | O |
0.20 | g | P |
Property | Value | Reference |
---|---|---|
t_half (Half-life) | 820 hours | Lombardo F, Berellini G, Obach RS |
Vd (Volume of distribution) | 60 L/kg | Lombardo F, Berellini G, Obach RS |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 41.37 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
CL (Clearance) | 1.90 mL/min/kg | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 0.72 mg/mL | Bocci G, Oprea TI, Benet LZ |
BA (Bioavailability) | 0.50 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
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 |
---|---|---|---|---|---|---|
Drug interaction | 1228.21 | 12.53 | 1241 | 54489 | 227890 | 63205402 |
Bradycardia | 840.93 | 12.53 | 615 | 55115 | 72612 | 63360680 |
Torsade de pointes | 838.00 | 12.53 | 346 | 55384 | 13005 | 63420287 |
Electrocardiogram QT prolonged | 752.19 | 12.53 | 530 | 55200 | 59000 | 63374292 |
Atrial fibrillation | 701.50 | 12.53 | 674 | 55056 | 115962 | 63317330 |
Hyperthyroidism | 683.39 | 12.53 | 308 | 55422 | 14365 | 63418927 |
Acute kidney injury | 470.41 | 12.53 | 834 | 54896 | 262581 | 63170711 |
Interstitial lung disease | 398.83 | 12.53 | 372 | 55358 | 61536 | 63371756 |
International normalised ratio increased | 393.37 | 12.53 | 326 | 55404 | 46099 | 63387193 |
Myxoedema coma | 364.12 | 12.53 | 83 | 55647 | 352 | 63432940 |
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 |
---|---|---|---|---|---|---|
Hyperthyroidism | 1996.08 | 11.67 | 792 | 79529 | 9774 | 34866836 |
Pulmonary toxicity | 690.13 | 11.67 | 319 | 80002 | 5828 | 34870782 |
Drug interaction | 563.92 | 11.67 | 1450 | 78871 | 224496 | 34652114 |
Interstitial lung disease | 537.96 | 11.67 | 705 | 79616 | 64577 | 34812033 |
Ventricular tachycardia | 526.85 | 11.67 | 458 | 79863 | 26121 | 34850489 |
Bradycardia | 524.20 | 11.67 | 750 | 79571 | 74668 | 34801942 |
Cardiac failure | 491.24 | 11.67 | 806 | 79515 | 90442 | 34786168 |
Thyroiditis | 380.22 | 11.67 | 158 | 80163 | 2204 | 34874406 |
Electrocardiogram QT prolonged | 369.70 | 11.67 | 463 | 79858 | 40489 | 34836121 |
Atrial fibrillation | 349.22 | 11.67 | 828 | 79493 | 121565 | 34755045 |
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 |
---|---|---|---|---|---|---|
Hyperthyroidism | 2561.45 | 11.00 | 1044 | 121989 | 21165 | 79600190 |
Drug interaction | 1653.58 | 11.00 | 2568 | 120465 | 412615 | 79208740 |
Bradycardia | 1287.40 | 11.00 | 1299 | 121734 | 134258 | 79487097 |
Torsade de pointes | 1043.76 | 11.00 | 536 | 122497 | 18776 | 79602579 |
Electrocardiogram QT prolonged | 1013.01 | 11.00 | 949 | 122084 | 89437 | 79531918 |
Pulmonary toxicity | 998.50 | 11.00 | 458 | 122575 | 12456 | 79608899 |
Interstitial lung disease | 949.72 | 11.00 | 1013 | 122020 | 111587 | 79509768 |
Atrial fibrillation | 888.42 | 11.00 | 1297 | 121736 | 196589 | 79424766 |
Ventricular tachycardia | 847.14 | 11.00 | 620 | 122413 | 41315 | 79580040 |
Cardiac failure | 785.11 | 11.00 | 1076 | 121957 | 153766 | 79467589 |
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 arrest neonatal | 41.28 | 40.06 | 11 | 86 | 83 | 89612 |
Source | Code | Description |
---|---|---|
ATC | C01BD01 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class III |
CHEBI has role | CHEBI:35554 | cardiovascular agent |
FDA EPC | N0000175426 | Antiarrhythmic |
FDA MoA | N0000182137 | Cytochrome P450 2D6 Inhibitors |
FDA MoA | N0000182138 | Cytochrome P450 1A2 Inhibitors |
FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
FDA MoA | N0000185504 | Cytochrome P450 2C9 Inhibitors |
FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
MeSH PA | D000889 | Anti-Arrhythmia Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Ventricular fibrillation | indication | 71908006 | |
Prevention of Ventricular Fibrillation | indication | ||
Life-Threatening Ventricular Tachycardia | indication | ||
Atrial fibrillation | off-label use | 49436004 | DOID:0060224 |
Cardioversion of Atrial Fibrillation | off-label use | ||
Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation | off-label use | ||
Complete atrioventricular block | contraindication | 27885002 | |
Torsades de pointes | contraindication | 31722008 | |
Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
Extrinsic allergic alveolitis | contraindication | 37471005 | DOID:841 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.72 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Potassium voltage-gated channel subfamily H member 2 | Ion channel | BLOCKER | IC50 | 5 | WOMBAT-PK | CHEMBL | |||
Sodium channel protein type 5 subunit alpha | Ion channel | BLOCKER | IC50 | 7.10 | WOMBAT-PK | ||||
Mu-type opioid receptor | GPCR | Ki | 5.11 | DRUG MATRIX | |||||
D(1A) dopamine receptor | GPCR | Ki | 5.34 | DRUG MATRIX | |||||
D(2) dopamine receptor | GPCR | Ki | 5.18 | DRUG MATRIX | |||||
Alpha-2A adrenergic receptor | GPCR | IC50 | 6.30 | WOMBAT-PK | |||||
Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7 | WOMBAT-PK | |||||
Thyroid hormone receptor alpha | Nuclear hormone receptor | IC50 | 5.64 | WOMBAT-PK | |||||
Thyroid hormone receptor beta | Nuclear hormone receptor | IC50 | 6.22 | WOMBAT-PK | |||||
Cytochrome P450 3A4 | Enzyme | Ki | 6.22 | WOMBAT-PK |
ID | Source |
---|---|
000629 | NDDF |
004484 | NDDF |
13960 | MMSL |
19774-82-4 | SECONDARY_CAS_RN |
2012 | INN_ID |
203114 | RXNORM |
2157 | PUBCHEM_CID |
2566 | IUPHAR_LIGAND_ID |
372821002 | SNOMEDCT_US |
4018065 | VANDF |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Amiodarone HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-307 | TABLET | 100 mg | ORAL | ANDA | 29 sections |
Amiodarone HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-307 | TABLET | 100 mg | ORAL | ANDA | 29 sections |
Amiodarone HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-308 | TABLET | 200 mg | ORAL | ANDA | 29 sections |
Amiodarone HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-308 | TABLET | 200 mg | ORAL | ANDA | 29 sections |
Amiodarone HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-309 | TABLET | 400 mg | ORAL | ANDA | 29 sections |
Amiodarone Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9875 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 26 sections |
Amiodarone Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9875 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 26 sections |
Amiodarone Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0185-0144 | TABLET | 200 mg | ORAL | ANDA | 27 sections |
Amiodarone Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9815 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 16 sections |
Amiodarone Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9815 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 16 sections |