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
Molecular Formula | C31H44N2O5S |
Molecular Weight | 556.756 |
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 Date2009 |
|||
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 Date2009 |
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 |
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Dronedarone for prevention of atrial fibrillation: a dose-ranging study. | 2003 Aug |
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Effects of amiodarone and dronedarone on voltage-dependent sodium current in human cardiomyocytes. | 2003 Aug |
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Electrophysiologic characterization of dronedarone in guinea pig ventricular cells. | 2003 Feb |
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Old and new antiarrhythmic drugs for converting and maintaining sinus rhythm in atrial fibrillation: comparative efficacy and results of trials. | 2003 Mar 20 |
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Acute effects of dronedarone on both components of the cardiac delayed rectifier K+ current, HERG and KvLQT1/minK potassium channels. | 2003 Nov |
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IKr channel blockers: novel antiarrhythmic agents. | 2003 Oct |
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Trials of new antiarrhythmic drugs for maintenance of sinus rhythm in patients with atrial fibrillation. | 2004 |
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Dronedarone: an amiodarone analogue. | 2004 Apr |
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Effects of metabolites and analogs of amiodarone on alveolar macrophages: structure-activity relationship. | 2004 Aug |
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Involvement of nitric oxide in amiodarone- and dronedarone-induced coronary vasodilation in guinea pig heart. | 2004 Aug 2 |
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High affinity HERG K(+) channel blockade by the antiarrhythmic agent dronedarone: resistance to mutations of the S6 residues Y652 and F656. | 2004 Dec 17 |
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Pharmacokinetic and pharmacodynamic interactions between metoprolol and dronedarone in extensive and poor CYP2D6 metabolizers healthy subjects. | 2004 Feb |
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Theoretical possibilities for the development of novel antiarrhythmic drugs. | 2004 Jan |
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Oral class III antiarrhythmics: what is new? | 2004 Jan |
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[New anti-arrhythmics--hope or disappointment?]. | 2004 Nov |
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A benefit-risk assessment of class III antiarrhythmic agents. | 2004 Nov |
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[Atrial fibrillation: choice of the method of pharmacological cardioversion]. | 2005 |
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[Safety of new anti-arrhythmic drugs]. | 2005 Apr |
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In vivo and in vitro antiarrhythmic effects of SSR149744C in animal models of atrial fibrillation and ventricular arrhythmias. | 2005 Feb |
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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 |
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[Dronedarone establishes and maintains control of sinus rhythm]. | 2006 Aug 23 |
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[Dronedarone--a new therapeutic option for controlling atrial rhythm and ventricular frequency]. | 2006 Aug 25 |
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Do we need pharmacological therapy for atrial fibrillation in the ablation era? | 2006 Dec |
|
Comment on dronedarone. | 2006 Dec |
|
Dronedarone: a new antiarrhythmic agent. | 2006 Feb |
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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 |
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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 |
|
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 |
|
New antiarrhythmic treatment of atrial fibrillation. | 2007 Jul |
|
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 |
|
[Amiodaron for treatment of perioperative cardiac arrythmia: a broad spectrum antiarrythmetic agent?]. | 2008 Dec |
|
Rationale and design of ATHENA: A placebo-controlled, double-blind, parallel arm Trial to assess the efficacy of dronedarone 400 mg bid for the prevention of cardiovascular Hospitalization or death from any cause in patiENts with Atrial fibrillation/atrial flutter. | 2008 Jan |
|
Concurrent Chagas' disease and borderline disseminated cutaneous leishmaniasis: The role of amiodarone as an antitrypanosomatidae drug. | 2008 Jun |
|
Anti-arrhythmic drug therapy for atrial fibrillation: current anti-arrhythmic drugs, investigational agents, and innovative approaches. | 2008 Jun |
|
Is dronedarone effective for the prevention of recurrent atrial fibrillation? | 2008 Mar |
|
Dronedarone: a new treatment for atrial fibrillation. | 2008 Nov |
|
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 |
|
Benzofuran derivatives and the thyroid. | 2009 Jan |
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
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on
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Record UNII |
JQZ1L091Y2
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WHO-VATC |
QC01BD07
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NBK548208
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C01BD07
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NCI_THESAURUS |
C47793
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DRONEDARONE
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DB04855
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N0000185503
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233698
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m4768
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N0000182137
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141626-36-0
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N0000190114
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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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
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TRANSPORTER -> INHIBITOR |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE -> PARENT |
MAJOR
PLASMA
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE LESS ACTIVE -> PARENT |
Dronedarone is extensively metabolized, mainly by CYP 3A
MAJOR
PLASMA
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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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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