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
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
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 |
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 |
---|---|---|
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 |
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Topics on the Na+/Ca2+ exchanger: pharmacological characterization of Na+/Ca2+ exchanger inhibitors. | 2006 Sep |
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Amiodarone: a multifaceted antiarrhythmic drug. | 2006 Sep |
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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 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).
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 22:36:13 UTC 2021
by
admin
on
Fri Jun 25 22:36:13 UTC 2021
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Record UNII |
JQZ1L091Y2
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Record Status |
Validated (UNII)
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QC01BD07
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LIVERTOX |
331
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NDF-RT |
N0000175426
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WHO-ATC |
C01BD07
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NCI_THESAURUS |
C47793
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Code System | Code | Type | Description | ||
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DRONEDARONE
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DB04855
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N0000185503
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
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233698
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PRIMARY | RxNorm | ||
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208898
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C118667
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141626-36-0
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PRIMARY | |||
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7928
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PRIMARY | |||
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M4768
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PRIMARY | Merck Index | ||
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N0000182137
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PRIMARY | Cytochrome P450 2D6 Inhibitors [MoA] | ||
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7465
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141626-36-0
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SUB06408MIG
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CHEMBL184412
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N0000190114
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PRIMARY | Cytochrome P450 3A Inhibitors [MoA] | ||
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C65485
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PRIMARY | |||
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7382
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JQZ1L091Y2
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4112
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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TRANSPORTER -> INHIBITOR | |||
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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
|
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|
SALT/SOLVATE -> PARENT | |||
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> INHIBITOR |
LOW
Ki
|
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METABOLIC ENZYME -> INHIBITOR |
LOW
Ki
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
MAJOR
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
FECAL; URINE
|
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|
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 |
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Tmax | PHARMACOKINETIC |
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IN HEPATICALLY IMPAIRED PATIENTS |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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IN HEALTHY SUBJECTS |
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