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amiodarone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antiarrhythmics	176	1951-25-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: amiodarone amidorone sedacoron amiodarone hydrochloride amiodarone HCl	An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance. Molecular weight: 645.32 Formula: C25H29I2NO3 CLOGP: 8.95 LIPINSKI: 2 HAC: 4 HDO: 0 TPSA: 42.68 ALOGS: -5.13 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

amiodarone
amidorone
sedacoron
amiodarone hydrochloride
amiodarone HCl

An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.

Molecular weight: 645.32
Formula: C25H29I2NO3
CLOGP: 8.95
LIPINSKI: 2
HAC: 4
HDO: 0
TPSA: 42.68
ALOGS: -5.13
ROTB: 11

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.20	g	O
0.20	g	P

ADMET properties:

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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 µM/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

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Approvals:

Date	Agency	Company	Orphan
Dec. 24, 1985	FDA	WYETH PHARMS INC

FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

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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

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Pharmacologic Action:

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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

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Drug Use | Suggest Off label Use Form| |View source of the data|

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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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.72	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN	BLOCKER	IC50	5	WOMBAT-PK	CHEMBL
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	IC50	7.10	WOMBAT-PK
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	5.11	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.34	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.18	DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		IC50	6.30	WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	7	WOMBAT-PK
Thyroid hormone receptor alpha	Nuclear hormone receptor	P10827	THA_HUMAN		IC50	5.64	WOMBAT-PK
Thyroid hormone receptor beta	Nuclear hormone receptor	P10828	THB_HUMAN		IC50	6.22	WOMBAT-PK
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		Ki	6.22	WOMBAT-PK

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External reference:

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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

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Pharmaceutical products:

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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

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