Details
Stereochemistry | ACHIRAL |
Molecular Formula | C31H44N2O5S |
Molecular Weight | 556.756 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCN(CCCC)CCCOC1=CC=C(C=C1)C(=O)C2=C(CCCC)OC3=CC=C(NS(C)(=O)=O)C=C23
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
DescriptionCurator'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
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.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1914276 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25182566 |
|||
Target ID: CHEMBL1250417 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21279331 |
1.0 µM [IC50] | ||
Target ID: CHEMBL340 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MULTAQ Approved UseMULTAQ® 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 Date1.24640638E12 |
|||
Primary | MULTAQ Approved UseMULTAQ® 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 Date1.24640638E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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%) Sources: QT interval prolonged (1.5%) |
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 Health Status: healthy Age Group: 21-40 years Sex: M Sources: |
|
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%) Sources: Page: p. 103Nausea (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%) |
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... Other AEs: Heart failure (grade 5) Sources: |
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%) Sources: Page: p. 103Vomiting (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%) |
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%) Sources: Page: p. 103Nausea (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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022425s000_ClinPharm_P1.pdf#page=76 Page: 76,89 |
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% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022425s000_ClinPharm_P1.pdf#page=76 Page: 76,89 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022425s000_ClinPharm_P1.pdf#page=76 Page: 76.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022425s000_ClinPharm_P1.pdf#page=76 Page: 76.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022425s000_ClinPharm_P1.pdf#page=76 Page: 76.0 |
unlikely |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022425s000_Pharm_P1.pdf#page=59 Page: 59.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Dronedarone (Sanofi-Synthélabo). | 2001 May |
|
Five novel single nucleotide polymorphisms in the CYP2C8 gene, one of which induces a frame-shift. | 2002 |
|
IKr channel blockers: novel antiarrhythmic agents. | 2003 Oct |
|
Involvement of nitric oxide in amiodarone- and dronedarone-induced coronary vasodilation in guinea pig heart. | 2004 Aug 2 |
|
High affinity HERG K(+) channel blockade by the antiarrhythmic agent dronedarone: resistance to mutations of the S6 residues Y652 and F656. | 2004 Dec 17 |
|
[New anti-arrhythmics--hope or disappointment?]. | 2004 Nov |
|
A benefit-risk assessment of class III antiarrhythmic agents. | 2004 Nov |
|
Antiarrhythmic drugs in patients with implantable cardioverter-defibrillators. | 2005 |
|
[Atrial fibrillation: choice of the method of pharmacological cardioversion]. | 2005 |
|
[Safety of new anti-arrhythmic drugs]. | 2005 Apr |
|
The novel antiarrhythmic drug dronedarone: comparison with amiodarone. | 2005 Fall |
|
In vivo and in vitro antiarrhythmic effects of SSR149744C in animal models of atrial fibrillation and ventricular arrhythmias. | 2005 Feb |
|
Dronedarone administration prevents body weight gain and increases tolerance of the heart to ischemic stress: a possible involvement of thyroid hormone receptor alpha1. | 2005 Jan |
|
This DAFNE is definitely not that DAFNE. | 2005 May 25 |
|
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 |
|
Comment on dronedarone. | 2006 Dec |
|
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 |
|
Dose-dependent effects of oral dronedarone on the circadian variation of RR and QT intervals in healthy subjects: implications for antiarrhythmic actions. | 2006 Sep |
|
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: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. | 2007 Apr |
|
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 quest of the ideal antiarrhythmic drug. | 2007 Fall |
|
Pharmacological inhibition of TRalpha1 receptor potentiates the thyroxine effect on body weight reduction in rats: potential therapeutic implications in controlling body weight. | 2007 Jan |
|
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 |
|
Na+/Ca2+ exchange inhibitors: a new class of calcium regulators. | 2007 Sep |
|
Acute in vitro effects of dronedarone, an iodine-free derivative, and amiodarone, on the rabbit sinoatrial node automaticity: a comparative study. | 2007 Sep |
|
Maintaining sinus rhythm--making treatment better than the disease. | 2007 Sep 6 |
|
Relationship among amiodarone, new class III antiarrhythmics, miscellaneous agents and acquired long QT syndrome. | 2008 |
|
[Amiodaron for treatment of perioperative cardiac arrythmia: a broad spectrum antiarrythmetic agent?]. | 2008 Dec |
|
Anti-arrhythmic drug therapy for atrial fibrillation: current anti-arrhythmic drugs, investigational agents, and innovative approaches. | 2008 Jun |
|
Increased mortality after dronedarone therapy for severe heart failure. | 2008 Jun 19 |
|
Dronedarone: a new treatment for atrial fibrillation. | 2008 Nov |
|
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 |
|
Dronedarone for the control of ventricular rate in permanent atrial fibrillation: the Efficacy and safety of dRonedArone for the cOntrol of ventricular rate during atrial fibrillation (ERATO) study. | 2008 Sep |
|
New horizons in antiarrhythmic therapy: will novel agents overcome current deficits? | 2008 Sep 22 |
|
Trial watch: novel antiarrhythmic agent shows promise in Phase III trial. | 2009 Apr |
|
Major recent trials in cardiovascular diseases. | 2009 Mar |
|
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 Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12548079
In isolated ventricular myocytes, dronedarone inhibited rapidly activating delayed-rectifier K+ current (I(Kr)) (median inhibitory concentration [IC50] = 3 uM voltage-independent); slowly activating delayed-rectifier K+ current (I(Ks)) (IC50 approximately/= 10 uM voltage-dependent and time-, frequency-, or use-independent); and inward rectifier potassium current (I(K1)) (IC50 >/= 30 uM).
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QC01BD07
Created by
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LIVERTOX |
NBK548208
Created by
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NDF-RT |
N0000175426
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WHO-ATC |
C01BD07
Created by
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NCI_THESAURUS |
C47793
Created by
admin on Fri Dec 16 19:51:32 UTC 2022 , Edited by admin on Fri Dec 16 19:51:32 UTC 2022
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Code System | Code | Type | Description | ||
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DRONEDARONE
Created by
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DB04855
Created by
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PRIMARY | |||
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N0000185503
Created by
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
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233698
Created by
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PRIMARY | RxNorm | ||
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208898
Created by
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PRIMARY | |||
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C118667
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PRIMARY | |||
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DTXSID3048653
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7928
Created by
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PRIMARY | |||
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M4768
Created by
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PRIMARY | Merck Index | ||
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N0000182137
Created by
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PRIMARY | Cytochrome P450 2D6 Inhibitors [MoA] | ||
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7465
Created by
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PRIMARY | |||
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141626-36-0
Created by
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PRIMARY | |||
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SUB06408MIG
Created by
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PRIMARY | |||
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JQZ1L091Y2
Created by
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PRIMARY | |||
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CHEMBL184412
Created by
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PRIMARY | |||
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N0000190114
Created by
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PRIMARY | Cytochrome P450 3A Inhibitors [MoA] | ||
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50659
Created by
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PRIMARY | |||
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C65485
Created by
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7382
Created by
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JQZ1L091Y2
Created by
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4112
Created by
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PRIMARY |
ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE LESS ACTIVE (PARENT)
SALT/SOLVATE (PARENT)