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

Stem definition	Drug id	CAS RN
antiarrhythmics	4112	141626-36-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: dronedarone multaq dronedarone hydrochloride SR33598B dronedarone HCl	Dronedarone has antiarrhythmic properties belonging to all four Vaughan-Williams classes, but the contribution of each of these activities to the clinical effect is unknown. Molecular weight: 556.76 Formula: C31H44N2O5S CLOGP: 8.57 LIPINSKI: 2 HAC: 7 HDO: 1 TPSA: 88.85 ALOGS: -5.44 ROTB: 17 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

dronedarone
multaq
dronedarone hydrochloride
SR33598B
dronedarone HCl

Dronedarone has antiarrhythmic properties belonging to all four Vaughan-Williams classes, but the contribution of each of these activities to the clinical effect is unknown.

Molecular weight: 556.76
Formula: C31H44N2O5S
CLOGP: 8.57
LIPINSKI: 2
HAC: 7
HDO: 1
TPSA: 88.85
ALOGS: -5.44
ROTB: 17

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.80	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	33.33 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	20.53 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	20 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	16 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.02 %	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
July 1, 2009	FDA	SANOFI AVENTIS US

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
Atrial fibrillation	189.64	21.66	127	6185	116509	63366201
Blood creatinine increased	180.77	21.66	111	6201	87733	63394977
Drug interaction	172.25	21.66	158	6154	228973	63253737
International normalised ratio increased	125.29	21.66	70	6242	46355	63436355
Dyspnoea	109.71	21.66	217	6095	661096	62821614
Torsade de pointes	101.10	21.66	41	6271	13310	63469400
Cardiac failure	94.39	21.66	75	6237	89067	63393643
Cardiac failure congestive	79.58	21.66	69	6243	92364	63390346
Gastrointestinal haemorrhage	74.77	21.66	63	6249	81113	63401597
Ventricular tachycardia	64.63	21.66	34	6278	19945	63462765

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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
Blood creatinine increased	141.49	21.41	120	5616	94856	34856339
Atrial fibrillation	126.46	21.41	126	5610	122267	34828928
Drug interaction	110.89	21.41	159	5577	225787	34725408
Dyspnoea	101.94	21.41	203	5533	376579	34574616
Ventricular tachycardia	86.45	21.41	54	5682	26525	34924670
International normalised ratio increased	85.46	21.41	67	5669	47260	34903935
Cardiac failure	66.06	21.41	78	5658	91170	34860025
Gastrointestinal haemorrhage	61.35	21.41	74	5662	88403	34862792
Glomerular filtration rate decreased	48.96	21.41	29	5707	12932	34938263
Bradycardia	45.72	21.41	59	5677	75359	34875836

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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
Blood creatinine increased	262.54	20.09	191	10029	154866	79579302
Drug interaction	254.29	20.09	288	9932	414895	79319273
Atrial fibrillation	205.24	20.09	183	10037	197703	79536465
Dyspnoea	167.16	20.09	349	9871	856676	78877492
International normalised ratio increased	158.39	20.09	111	10109	84610	79649558
Gastrointestinal haemorrhage	119.18	20.09	119	10101	147600	79586568
Cardiac failure congestive	97.35	20.09	105	10115	142297	79591871
Torsade de pointes	96.89	20.09	48	10172	19264	79714904
Ventricular tachycardia	90.28	20.09	60	10160	41875	79692293
Cardiac failure	88.47	20.09	104	10116	154738	79579430

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01BD07	CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class III
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:78298	environmental contaminants
FDA EPC	N0000175426	Antiarrhythmic
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D002317	Cardiovascular 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
Atrial fibrillation	indication	49436004	DOID:0060224
Paroxysmal atrial fibrillation	indication	282825002
Complete atrioventricular block	contraindication	27885002
Torsades de pointes	contraindication	31722008
Sick sinus syndrome	contraindication	36083008	DOID:13884
Hypokalemia	contraindication	43339004
Chronic heart failure	contraindication	48447003
Bradycardia	contraindication	48867003
Hepatic failure	contraindication	59927004
Prolonged QT interval	contraindication	111975006

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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	7.65	acidic
pKa2	9.7	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 400MG BASE	MULTAQ	SANOFI AVENTIS US	N022425	July 1, 2009	RX	TABLET	ORAL	8410167	April 16, 2029	REDUCTION IN RISK OF HOSPITALIZATION IN PATIENTS WITH A HISTORY OF PAROXYSMAL OR PERSISTENT AF WITHOUT SEVERE HEART FAILURE AND WITH ONE OR MORE RISK FACTORS BY ADMINISTRATION TWICE A DAY WITH MORNING AND EVENING MEALS
EQ 400MG BASE	MULTAQ	SANOFI AVENTIS US	N022425	July 1, 2009	RX	TABLET	ORAL	8410167	April 16, 2029	TREATMENT OF PATIENTS WITH A HISTORY OF PAROXYSMAL OR PERSISTENT AF WITHOUT SEVERE HEART FAILURE AND WITH ONE OR MORE RISK FACTORS BY ADMINISTRATION TWICE A DAY WITH MORNING AND EVENING MEALS
EQ 400MG BASE	MULTAQ	SANOFI AVENTIS US	N022425	July 1, 2009	RX	TABLET	ORAL	9107900	April 16, 2029	REDUCTION IN RISK OF HOSPITALIZATION IN PATIENTS WITH CORONARY HEART DISEASE AND A HISTORY OF PAROXYSMAL OR PERSISTENT AF AND WITH ONE OR MORE RISK FACTORS BY ADMINISTRATION TWICE A DAY WITH MORNING AND EVENING MEALS
EQ 400MG BASE	MULTAQ	SANOFI AVENTIS US	N022425	July 1, 2009	RX	TABLET	ORAL	9107900	April 16, 2029	REDUCTION IN RISK OF HOSPITALIZATION IN PATIENTS WITH STABLE NYHA CLASS III HEART FAILURE AND A HISTORY OF PAROXYSMAL OR PERSISTENT AF AND WITH ONE OR MORE RISK FACTORS BY ADMINISTRATION TWICE A DAY WITH MORNING AND EVENING MEALS
EQ 400MG BASE	MULTAQ	SANOFI AVENTIS US	N022425	July 1, 2009	RX	TABLET	ORAL	8602215	June 30, 2031	MANAGEMENT OF RISK OF DRONEDARONE/BETA-BLOCKER INTERACTION IN PATIENTS IN SINUS RHYTHM WITH A HISTORY OF PAROXYSMAL OR PERSISTENT AF

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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/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1	Ion channel	O60741	HCN1_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2	Ion channel	Q9UL51	HCN2_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 3	Ion channel	Q9P1Z3	HCN3_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4	Ion channel	Q9Y3Q4	HCN4_HUMAN	BLOCKER			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily A member 5	Ion channel	P22460	KCNA5_HUMAN		IC50	5.63	CHEMBL
Thyroid hormone receptor alpha	Nuclear hormone receptor	P10827	THA_HUMAN		IC50	4.23	WOMBAT-PK
THAP domain-containing protein 1	Unclassified	Q9NVV9	THAP1_HUMAN		IC50	4.23	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.50	CHEMBL
Voltage-dependent calcium channel gamma-1 subunit	Ion channel	Q06432	CCG1_HUMAN		IC50	6.70	WOMBAT-PK
Potassium voltage-gated channel subfamily KQT member 2	Ion channel	O43526	KCNQ2_HUMAN	BLOCKER	IC50	8	WOMBAT-PK

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External reference:

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ID	Source
013186	NDDF
013187	NDDF
141625-93-6	SECONDARY_CAS_RN
166180	MMSL
208898	PUBCHEM_CID
233698	RXNORM
26593	MMSL
33190	MMSL
4028918	VUID
4028918	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Multaq	HUMAN PRESCRIPTION DRUG LABEL	1	0024-4142	TABLET, FILM COATED	400 mg	ORAL	NDA	29 sections
Multaq	HUMAN PRESCRIPTION DRUG LABEL	1	54868-3086	TABLET, FILM COATED	400 mg	ORAL	NDA	30 sections
Multaq	HUMAN PRESCRIPTION DRUG LABEL	1	55154-8104	TABLET, FILM COATED	400 mg	ORAL	NDA	29 sections
Multaq	HUMAN PRESCRIPTION DRUG LABEL	1	55154-8104	TABLET, FILM COATED	400 mg	ORAL	NDA	29 sections

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