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Details

Stereochemistry ACHIRAL
Molecular Formula C31H44N2O5S
Molecular Weight 556.7587
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DRONEDARONE

SMILES

CCCCc1c(c2cc(ccc2o1)NS(=O)(=O)C)C(=O)c3ccc(cc3)OCCCN(CCCC)CCCC

InChI

InChIKey=ZQTNQVWKHCQYLQ-UHFFFAOYSA-N
InChI=1S/C31H44N2O5S/c1-5-8-12-29-30(27-23-25(32-39(4,35)36)15-18-28(27)38-29)31(34)24-13-16-26(17-14-24)37-22-11-21-33(19-9-6-2)20-10-7-3/h13-18,23,32H,5-12,19-22H2,1-4H3

HIDE SMILES / InChI

Molecular Formula C31H44N2O5S
Molecular Weight 556.7587
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: description was created based on several sources, including: https://www.drugs.com/ppa/dronedarone.html | https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7fa41601-7fb5-4155-8e50-2ae903f0d2d6 | http://www.rxlist.com/multaq-drug.htm

Dronedarone is an antiarrhythmic that is FDA approved for the treatment of atrial fibrillation in patients in sinus rhythm with a history of paroxysmal or persistent atrial fibrillation (AF). Dronedarone is multichannel blocker. Common adverse reactions include abdominal pain, diarrhea, indigestion, nausea, vomiting, asthenia and raised serum creatinine. Dronedarone has potentially important pharmacodynamics interactions: Digoxin: Consider discontinuation or halve dose of digoxin before treatment and monitor; Calcium channel blockers (CCB): Initiate CCB with low dose and increase after ECG verification of tolerability; Beta-blockers: May provoke excessive bradycardia, Initiate with low dose and increase after ECG verification of tolerability.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
MULTAQ

Approved Use

MULTAQ® is indicated to reduce the risk of hospitalization for atrial fibrillation in patients in sinus rhythm with a history of paroxysmal or persistent atrial fibrillation (AF) [see Clinical Studies (14)

Launch Date

1.24640638E12
Primary
MULTAQ

Approved Use

MULTAQ® is indicated to reduce the risk of hospitalization for atrial fibrillation in patients in sinus rhythm with a history of paroxysmal or persistent atrial fibrillation (AF) [see Clinical Studies (14)

Launch Date

1.24640638E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
96.2 ng/mL
1600 mg single, oral
dose: 1600 mg
route of administration: Oral
experiment type: SINGLE
co-administered: METOPROLOL
DRONEDARONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1386 ng × h/mL
1600 mg single, oral
dose: 1600 mg
route of administration: Oral
experiment type: SINGLE
co-administered: METOPROLOL
DRONEDARONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
12 h
1600 mg single, oral
dose: 1600 mg
route of administration: Oral
experiment type: SINGLE
co-administered: METOPROLOL
DRONEDARONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 20-97 years
n = 3282
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: 20-97 years
Sex: M+F
Population Size: 3282
Sources:
Disc. AE: Gastrointestinal disorders, QT interval prolonged...
AEs leading to
discontinuation/dose reduction:
Gastrointestinal disorders (3.2%)
QT interval prolonged (1.5%)
Sources:
1600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 1600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1600 mg, 2 times / day
Sources:
healthy, 21-40 years
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Disc. AE: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (6.7%)
Nausea (3.9%)
Abdominal pain upper (2%)
Abdominal pain (1.9%)
Vomiting (1.7%)
Dyspepsia (1.3%)
Nasopharyngitis (3.7%)
Upper respiratory tract infection (2.9%)
Dizziness (3.4%)
Blood creatinine increased (2.5%)
Hepatic enzyme increased (1.2%)
Blood urea increased (0.4%)
Bradycardia (2.6%)
Palpitations (1.1%)
Cardiac failure congestive (1.3%)
Cardiac failure (0.8%)
Fatigue (2.7%)
Oedema peripheral (4.2%)
Back pain (3.3%)
Arthralgia (3.1%)
Pain in extremity (2.1%)
Cough (2.2%)
Dyspnoea (2.3%)
Vertigo (1.3%)
Sources: Page: p. 103
400 mg 2 times / day steady, oral
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: NYHA Class IV heart failure | NYHA Class II - III heart failure
Age Group: adult
Sources:
Other AEs: Heart failure...
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Disc. AE: Diarrhea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Diarrhea (7.6%)
Vomiting (1.5%)
Dyspepsia (3%)
Abdominal pain (1.5%)
Nasopharyngitis (4.5%)
Electrocardiogram QT prolonged (1.5%)
Blood creatinine increased (1.5%)
Hepatic enzyme increased (4.5%)
Blood urea increased (3%)
Bradycardia (1.5%)
Palpitations (6.1%)
Cardiac failure congestive (4.5%)
Cardiac failure (4.5%)
Fatigue (4.5%)
Cough (1.5%)
Hypokalemia (3%)
Vertigo (4.5%)
Sources: Page: p. 103
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Disc. AE: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (29%)
Nausea (8.1%)
Vomiting (3.2%)
Abdominal pain (3.2%)
Influenza (3.2%)
Upper respiratory tract infection (1.6%)
Dizziness (4.8%)
Electrocardiogram QT prolonged (3.2%)
Hepatic enzyme increased (1.6%)
Blood urea increased (3.2%)
Bradycardia (6.5%)
Palpitations (4.8%)
Cardiac failure congestive (1.6%)
Cardiac failure (1.6%)
Fatigue (3.2%)
Atrial tachycardia (4.8%)
Cough (4.8%)
Vertigo (3.2%)
Sources: Page: p. 103
AEs

AEs

AESignificanceDosePopulation
QT interval prolonged 1.5%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 20-97 years
n = 3282
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: 20-97 years
Sex: M+F
Population Size: 3282
Sources:
Gastrointestinal disorders 3.2%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 20-97 years
n = 3282
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: 20-97 years
Sex: M+F
Population Size: 3282
Sources:
Blood urea increased 0.4%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Cardiac failure 0.8%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Palpitations 1.1%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Hepatic enzyme increased 1.2%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Cardiac failure congestive 1.3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Dyspepsia 1.3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Vertigo 1.3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Vomiting 1.7%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Abdominal pain 1.9%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Abdominal pain upper 2%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Pain in extremity 2.1%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Cough 2.2%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Dyspnoea 2.3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Blood creatinine increased 2.5%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Bradycardia 2.6%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Fatigue 2.7%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Upper respiratory tract infection 2.9%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Arthralgia 3.1%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Back pain 3.3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Dizziness 3.4%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Nasopharyngitis 3.7%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Nausea 3.9%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Oedema peripheral 4.2%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Diarrhea 6.7%
Disc. AE
400 mg 2 times / day steady, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 989
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 989
Sources: Page: p. 103
Heart failure grade 5
400 mg 2 times / day steady, oral
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: NYHA Class IV heart failure | NYHA Class II - III heart failure
Age Group: adult
Sources:
Abdominal pain 1.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Blood creatinine increased 1.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Bradycardia 1.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Cough 1.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Electrocardiogram QT prolonged 1.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Vomiting 1.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Blood urea increased 3%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Dyspepsia 3%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Hypokalemia 3%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Cardiac failure congestive 4.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Cardiac failure 4.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Fatigue 4.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Hepatic enzyme increased 4.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Nasopharyngitis 4.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Vertigo 4.5%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Palpitations 6.1%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Diarrhea 7.6%
Disc. AE
600 mg 2 times / day multiple, oral
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 66
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 66
Sources: Page: p. 103
Cardiac failure congestive 1.6%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Cardiac failure 1.6%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Hepatic enzyme increased 1.6%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Upper respiratory tract infection 1.6%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Diarrhea 29%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Abdominal pain 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Blood urea increased 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Electrocardiogram QT prolonged 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Fatigue 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Influenza 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Vertigo 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Vomiting 3.2%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Atrial tachycardia 4.8%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Cough 4.8%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Dizziness 4.8%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Palpitations 4.8%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Bradycardia 6.5%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
Nausea 8.1%
Disc. AE
800 mg 2 times / day multiple, oral
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: p. 103
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: atrial fibrillation | atrial flutter
Age Group: adult
Sex: M+F
Population Size: 62
Sources: Page: p. 103
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
likely
likely
moderate [Ki 8.12 uM]
yes (co-administration study)
Comment: dronedarone increased verapamil exposure by 1.4- fold, and nisoldipine exposure by 1.5- fold; dronedarone increased simvastatin, a sensitive CYP3A substrate, and simvastatin acid exposure by 4- fold and 2- fold, respectively;
Page: 76,89,194
no
no
no
no
no
no
not significant
not significant
not significant
not significant
not significant
not significant
not significant
weak (co-administration study)
Comment: dronedarone increased S-warfarin exposure by 1.2- fold
Page: 76.0
strong [IC50 0.97 uM]
yes (co-administration study)
Comment: IC50 value obtained using vincristine as substrate; increased S-warfarin exposure by 1.2- fold
Page: 76,90
weak [Ki 4.37 uM]
yes (co-administration study)
Comment: dronedarone increased metoprolol exposure by 1.6- and 2.3- fold, respectively; increased propranolol exposure by 1.3- fold;
Page: 76,89,194
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: administration of ketoconazole resulted in a 17- to 25- fold increase in dronedarone exposure; administration with rifampicin decreased dronedarone exposure by 80%
Page: 76,89
no
no
unlikely
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Mechanisms of action of antiarrhythmic drugs relative to the origin and perpetuation of cardiac arrhythmias.
2001 Jan
Electrophysiological effects of dronedarone (SR 33589), a noniodinated amiodarone derivative in the canine heart: comparison with amiodarone.
2001 Jul
The JT-area indicates dispersion of repolarization in dogs with atrioventricular block.
2002 Jun
Involvement of nitric oxide in amiodarone- and dronedarone-induced coronary vasodilation in guinea pig heart.
2004 Aug 2
Pharmacokinetic and pharmacodynamic interactions between metoprolol and dronedarone in extensive and poor CYP2D6 metabolizers healthy subjects.
2004 Feb
Pharmacological treatment of atrial fibrillation: mechanisms of action and efficacy of class III drugs.
2006
[Dronedarone establishes and maintains control of sinus rhythm].
2006 Aug 23
[Dronedarone--a new therapeutic option for controlling atrial rhythm and ventricular frequency].
2006 Aug 25
Dronedarone: a new antiarrhythmic agent.
2006 Feb
Amiodarone inhibits thyroidal iodide transport in vitro by a cyclic adenosine 5'-monophosphate- and iodine-independent mechanism.
2006 Jun
Drug evaluation: dronedarone, a novel non-iodinated anti-arrhythmic agent.
2006 Sep
Topics on the Na+/Ca2+ exchanger: pharmacological characterization of Na+/Ca2+ exchanger inhibitors.
2006 Sep
Amiodarone: a multifaceted antiarrhythmic drug.
2006 Sep
Medical management of atrial fibrillation: state of the art.
2006 Sep
Dronedarone: an emerging agent with rhythm- and rate-controlling effects.
2006 Sep
Dronedarone: drondarone, SR 33589, SR 33589B.
2007
Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin.
2007 Aug 1
In vitro effects of acute amiodarone and dronedarone on epicardial, endocardial, and M cells of the canine ventricle.
2007 Dec
Effect of dronedarone on renal function in healthy subjects.
2007 Dec
Dronedarone in atrial fibrillation.
2007 Dec 6
New antiarrhythmic treatment of atrial fibrillation.
2007 Jul
Effect of amiodarone and dronedarone administration in rats on thyroid hormone-dependent gene expression in different cardiac components.
2007 Jun
Comparative antiarrhythmic efficacy of amiodarone and dronedarone during acute myocardial infarction in rats.
2007 Jun 14
A review of the investigational antiarrhythmic agent dronedarone.
2007 Mar
Antiarrhythmics for maintaining sinus rhythm after cardioversion of atrial fibrillation.
2007 Oct 17
Dronedarone for maintenance of sinus rhythm in atrial fibrillation or flutter.
2007 Sep 6
Atrial fibrillation after cardiac surgery: where are we now?
2008
Acute inhibitory effect of dronedarone, a noniodinated benzofuran analogue of amiodarone, on Na+/Ca2+ exchange current in guinea pig cardiac ventricular myocytes.
2008 Jun
Increased mortality after dronedarone therapy for severe heart failure.
2008 Jun 19
Update on atrial fibrillation: part II.
2008 Mar
New antiarrhythmic drugs for atrial fibrillation: focus on dronedarone and vernakalant.
2008 Oct
[Current pharmacological management of atrial fibrillation management by practice cardiologists - news from congress in Munich].
2008 Sep
Trial watch: novel antiarrhythmic agent shows promise in Phase III trial.
2009 Apr
A preliminary assessment of the effects of ATI-2042 in subjects with paroxysmal atrial fibrillation using implanted pacemaker methodology.
2009 Apr
Dronedarone for atrial fibrillation--an odyssey.
2009 Apr 30
New pharmacological options for patients with atrial fibrillation: the ATHENA trial.
2009 May
Patents

Sample Use Guides

One tablet of 400 mg twice a day with morning and evening meals.
Route of Administration: Oral
In isolated ventricular myocytes, dronedarone inhibited rapidly activating delayed-rectifier K+ current (I(Kr)) (median inhibitory concentration [IC50] /= 30 uM).
Substance Class Chemical
Created
by admin
on Fri Jun 25 22:36:13 UTC 2021
Edited
by admin
on Fri Jun 25 22:36:13 UTC 2021
Record UNII
JQZ1L091Y2
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DRONEDARONE
EMA EPAR   INN   MART.   MI   VANDF   WHO-DD  
INN  
Official Name English
DRONEDARONE [INN]
Common Name English
METHANESULFONAMIDE, N-(2-BUTYL-3-(4-(3-(DIBUTYLAMINO)PROPOXY)BENZOYL)-5-BENZOFURANYL)-
Systematic Name English
SR33589
Code English
SR-33589
Code English
DRONEDARONE [VANDF]
Common Name English
N-(2-BUTYL-3-(4-(3-(DIBUTYLAMINO)PROPROXY)BENZOYL)BENZOFURAN-5-YL)METHANESULFONAMIDE
Common Name English
DRONEDARONE [EMA EPAR]
Common Name English
DRONEDARONE [MI]
Common Name English
DRONEDARONE [MART.]
Common Name English
DRONEDARONE [WHO-DD]
Common Name English
Classification Tree Code System Code
WHO-VATC QC01BD07
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
LIVERTOX 331
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
NDF-RT N0000175426
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
WHO-ATC C01BD07
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
NCI_THESAURUS C47793
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
Code System Code Type Description
WIKIPEDIA
DRONEDARONE
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
DRUG BANK
DB04855
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
NDF-RT
N0000185503
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
RXCUI
233698
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY RxNorm
PUBCHEM
208898
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
MESH
C118667
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
EPA CompTox
141626-36-0
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
HSDB
7928
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
MERCK INDEX
M4768
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY Merck Index
NDF-RT
N0000182137
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY Cytochrome P450 2D6 Inhibitors [MoA]
IUPHAR
7465
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
CAS
141626-36-0
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
EVMPD
SUB06408MIG
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
ChEMBL
CHEMBL184412
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
NDF-RT
N0000190114
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NCI_THESAURUS
C65485
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
INN
7382
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
FDA UNII
JQZ1L091Y2
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
DRUG CENTRAL
4112
Created by admin on Fri Jun 25 22:36:14 UTC 2021 , Edited by admin on Fri Jun 25 22:36:14 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
MINOR
TRANSPORTER -> INHIBITOR
EXCRETED UNCHANGED
Mass balance indicates that orally administered dronedarone is ultimately excreted in the urine (6 %) and feces (84 %) primarily as metabolites. Dronedarone was extensively metabolized; only low amounts of dronedarone were detected in feces and dronedarone was non-existent in urine.
AMOUNT EXCRETED
URINE
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> INHIBITOR
LOW
Ki
METABOLIC ENZYME -> INHIBITOR
LOW
Ki
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Related Record Type Details
METABOLITE -> PARENT
FECAL; URINE
METABOLITE LESS ACTIVE -> PARENT
Dronedarone is extensively metabolized, mainly by CYP 3A
MAJOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC IN HEPATICALLY IMPAIRED PATIENTS

DOSE

Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC IN HEALTHY SUBJECTS

DOSE