DGIdb - AMIODARONE Drug Record

AMIODARONE chembl:CHEMBL633 Approved

Alternate Names:

CORDARONE
L-3428
AMIODARONE
PACERONE
SKF-33134A
AMIODARONE HYDROCHLORIDE
2-BUTYL-3-(3,5-DIIODO-4-(2-DIETHYLAMINOETHOXY)BENZOYL)BENZOFURAN
2-N-BUTYL-3',5'-DIIODO-4'-N-DIETHYLAMINOETHOXY-3-BENZOYLBENZOFURAN
CORDARONE®
AMIODARONA
AMIODARONUM
2-BUTYL-3-BENZOFURANYL 4-(2-(DIETHYLAMINO)ETHOXY)-3,5-DIIODOPHENYL KETONE
drugbank:01118
pubchem.compound:2157
rxcui:703
chembl:CHEMBL633
chemidplus:1951-25-3

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antiarrhytmic agent
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (strong)
Drug Categories	antiarrhythmics, class iii
Drug Class	vasodilator agents
Year of Approval	1985
Drug Class	anti-arrhythmia agents
Drug Categories	agents causing hyperkalemia
Drug Categories	agents causing muscle toxicity
Drug Categories	alpha-galactosidase, antagonists & inhibitors
Drug Categories	antiarrhythmic agents
Drug Categories	bsep/abcb11 inhibitors
Drug Categories	bsep/abcb11 substrates
Drug Categories	bsep/abcb11 substrates with narrow therapeutic index
Drug Categories	calcium channel blockers
Drug Categories	cytochrome p-450 cyp1a2 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2a6 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp2c19 inhibitors
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp2c19 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp2c8 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp2d6 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs causing inadvertant photosensitivity
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	narrow therapeutic index drugs
Drug Categories	oct2 inhibitors
Drug Categories	p-glycoprotein inducers
Drug Categories	p-glycoprotein inhibitors
Drug Categories	photosensitizing agents
Drug Categories	qtc prolonging agents
Drug Categories	vasodilating agents

(5 More Sources)

Publications:

Yang P et al., 2002, Allelic variants in long-QT disease genes in patients with drug-associated torsades de pointes., Circulation
Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med
Waldhauser et al., 2008, Interaction with the hERG channel and cytotoxicity of amiodarone and amiodarone analogues., Br. J. Pharmacol.
Varró et al., 2004, Theoretical possibilities for the development of novel antiarrhythmic drugs., Curr. Med. Chem.
Wang et al., 2008, Potassium channel currents in rat mesenchymal stem cells and their possible roles in cell proliferation., Clin. Exp. Pharmacol. Physiol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Doggrell et al., 2002, Present and future pharmacotherapy for heart failure., Expert Opin Pharmacother
Disatnik MH et al., 1991, Regulation of beta-adrenoceptors by thyroid hormone and amiodarone in rat myocardiac cells in culture., Biochem Pharmacol
Drvota V et al., 1999, The effect of amiodarone on the beta-adrenergic receptor is due to a downregulation of receptor protein and not to a receptor-ligand interaction., Biochem Biophys Res Commun
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Ricaurte et al., 2006, Simvastatin-amiodarone interaction resulting in rhabdomyolysis, azotemia, and possible hepatotoxicity., Ann Pharmacother
Cappiello et al., 1995, Ultrastructural evidence of thyroid damage in amiodarone-induced thyrotoxicosis., J. Endocrinol. Invest.
Baritussio et al., 2001, Amiodarone inhibits lung degradation of SP-A and perturbs the distribution of lysosomal enzymes., Am. J. Physiol. Lung Cell Mol. Physiol.
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
Benaim G et al., 2006, Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole., J Med Chem
Lee CA et al., 2010, Identification of novel substrates for human cytochrome P450 2J2., Drug Metab Dispos
Lewalter et al., 2010, [Clinical pharmacology and electrophysiological properties of dronedarone]., Dtsch. Med. Wochenschr.
Cohen et al., 1992, Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists., J. Gen. Physiol.
Watanabe Y et al., 2000, Inhibitory effect of amiodarone on Na(+)/Ca(2+) exchange current in guinea-pig cardiac myocytes., Br J Pharmacol
Lubic SP et al., 1994, Antiarrhythmic agent amiodarone possesses calcium channel blocker properties., J Cardiovasc Pharmacol
Szalowska E et al., 2014, Model steatogenic compounds (amiodarone, valproic acid, and tetracycline) alter lipid metabolism by different mechanisms in mouse liver slices., PLoS One
Song M et al., 2011, Phospholipidosis induced by PPARγ signaling in human bronchial epithelial (BEAS-2B) cells exposed to amiodarone., Toxicol Sci
McCarthy TC et al., 2004, Disruption of hepatic lipid homeostasis in mice after amiodarone treatment is associated with peroxisome proliferator-activated receptor-alpha target gene activation., J Pharmacol Exp Ther

AMIODARONE PPARGC1B

Interaction Score: 4.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
24489787

Sources:
DrugBank
AMIODARONE SQLE

Interaction Score: 0.7

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16451055

Sources:
DTC
AMIODARONE SFTPA1

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11597911

Sources:
NCI
AMIODARONE CYP2J2

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19923256

Sources:
PharmGKB
AMIODARONE NOS1AP

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
AMIODARONE KCNE1

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
AMIODARONE CACNA1I

Interaction Score: 0.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
1281221 7532747 20221978

Sources:
DrugBank
AMIODARONE KCNA7

Interaction Score: 0.26

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
AMIODARONE TG

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8778159

Sources:
NCI
AMIODARONE CACNA1C

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
20221978 1281221 10960072 7532747

Sources:
DrugBank
AMIODARONE ADRB1

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

negative modulator (inhibitory)

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

PMIDs:
12083991 1672592 10049740

Sources:
DrugBank TdgClinicalTrial TEND
AMIODARONE CALCA

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
AMIODARONE PPARA

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
15265979 24489787

Sources:
DrugBank
AMIODARONE KCNH2

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

PMIDs:
11997281 14999113 18604229 14754422 18505444 11752352

Sources:
DrugBank TdgClinicalTrial TEND PharmGKB
AMIODARONE CYP3A5

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
AMIODARONE PPARG

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
24489787 21123845

Sources:
DrugBank
AMIODARONE ADRA1A

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
AMIODARONE SCN5A

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
AMIODARONE MTOR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AMIODARONE CBX1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AMIODARONE CYP2C9

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
AMIODARONE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528 16537817

Sources:
NCI PharmGKB
AMIODARONE CYP2C19

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
AMIODARONE ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
AMIODARONE CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
AMIODARONE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC PharmGKB
AMIODARONE GMNN

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01118

Version: 5.1.7

Alternate Names:

PHL-amiodarone Drug Brand

PMS-amiodarone Drug Brand

Pacerone Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Lewalter et al., 2010, [Clinical pharmacology and electrophysiological properties of dronedarone]., Dtsch. Med. Wochenschr.

Lubic SP et al., 1994, Antiarrhythmic agent amiodarone possesses calcium channel blocker properties., J Cardiovasc Pharmacol

Watanabe Y et al., 2000, Inhibitory effect of amiodarone on Na(+)/Ca(2+) exchange current in guinea-pig cardiac myocytes., Br J Pharmacol

TEND: AMIODARONE
- Version: 01-August-2011
Alternate Names:

AMIODARONE Primary Drug Name

Drug Info:

Drug Class anti-arrhythmia agents

Year of Approval 1985

Drug Class vasodilator agents

Publications:
TdgClinicalTrial: AMIODARONE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antiarrhytmic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: AMIODARONE

Version: 14-September-2017

Alternate Names:

C236 NCI drug code

Drug Info:

Publications:

Ricaurte et al., 2006, Simvastatin-amiodarone interaction resulting in rhabdomyolysis, azotemia, and possible hepatotoxicity., Ann Pharmacother

Baritussio et al., 2001, Amiodarone inhibits lung degradation of SP-A and perturbs the distribution of lysosomal enzymes., Am. J. Physiol. Lung Cell Mol. Physiol.

Cappiello et al., 1995, Ultrastructural evidence of thyroid damage in amiodarone-induced thyrotoxicosis., J. Endocrinol. Invest.

DTC: AMIODARONE

Version: 02-September-2020

Alternate Names:

CHEMBL633 ChEMBL Drug ID

Drug Info:

Publications:

Benaim G et al., 2006, Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole., J Med Chem

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

PharmGKB: amiodarone

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Lee CA et al., 2010, Identification of novel substrates for human cytochrome P450 2J2., Drug Metab Dispos

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

TTD: Amiodarone
- Version: 2020.06.01
Alternate Names:

D0L5WM TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 135649937
- Version: 29-September-2020
Alternate Names:

AMIODARONE GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL633
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	amiodarone HCl,Amio-Aqueous IV
Novel drug target	Established target

PHL-amiodarone	Drug Brand
PMS-amiodarone	Drug Brand
Pacerone	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

Specific Action of the Ligand	None
Endogenous Drug?	False

antagonist (inhibitory)
inhibitor (inhibitory)
negative modulator (inhibitory)

AMIODARONE Drug Record

AMIODARONE chembl:CHEMBL633 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 24489787

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16451055

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11597911

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19923256

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 1281221 7532747 20221978

Sources: DrugBank

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8778159

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 20221978 1281221 10960072 7532747

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory) negative modulator (inhibitory)

Interaction Info: Trial Name amiodarone HCl,Amio-Aqueous IV Novel drug target Established target

PMIDs: 12083991 1672592 10049740

Sources: DrugBank TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 15265979 24489787

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name amiodarone HCl,Amio-Aqueous IV Novel drug target Established target

PMIDs: 11997281 14999113 18604229 14754422 18505444 11752352

Sources: DrugBank TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 24489787 21123845

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info: Trial Name amiodarone HCl,Amio-Aqueous IV Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

agonist (activating)

PMIDs:
24489787

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
16451055

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
11597911

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
19923256

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
1281221 7532747 20221978

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
8778159

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
20221978 1281221 10960072 7532747

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

negative modulator (inhibitory)

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

PMIDs:
12083991 1672592 10049740

Sources:
DrugBank TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
15265979 24489787

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

PMIDs:
11997281 14999113 18604229 14754422 18505444 11752352

Sources:
DrugBank TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

PMIDs:
24489787 21123845

Sources:
DrugBank

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
9187528 16537817

Sources:
NCI PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a