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 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 |
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Comment on dronedarone. | 2006 Dec |
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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 |
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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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Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter. | 2007 Apr |
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Effect of dronedarone on renal function in healthy subjects. | 2007 Dec |
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Dronedarone in atrial fibrillation. | 2007 Dec 6 |
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Dronedarone in atrial fibrillation. | 2007 Dec 6 |
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Dronedarone: in quest of the ideal antiarrhythmic drug. | 2007 Fall |
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Pharmacological inhibition of TRalpha1 receptor potentiates the thyroxine effect on body weight reduction in rats: potential therapeutic implications in controlling body weight. | 2007 Jan |
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Effect of amiodarone and dronedarone administration in rats on thyroid hormone-dependent gene expression in different cardiac components. | 2007 Jun |
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New antiarrhythmic drugs for establishing sinus rhythm in atrial fibrillation: what are our therapies likely to be by 2010 and beyond? | 2007 Nov |
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Antiarrhythmics for maintaining sinus rhythm after cardioversion of atrial fibrillation. | 2007 Oct 17 |
|
Maintaining sinus rhythm--making treatment better than the disease. | 2007 Sep 6 |
|
Dronedarone for maintenance of sinus rhythm in atrial fibrillation or flutter. | 2007 Sep 6 |
|
[Efficacy of dronedarone in cardiac failure due to severe left ventricular systolic dysfunction. Results of the ANDROMEDA]. | 2008 |
|
Atrial fibrillation after cardiac surgery: where are we now? | 2008 |
|
[Efficacy of dronedarone for maintenance of sinus rhythm in atrial fibrillation or flutter. Results of the EURIDIS and ADONIS]. | 2008 |
|
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 |
|
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 |
|
Pharmacotherapy for atrial arrhythmias: present and future. | 2008 Jun |
|
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 |
|
Is dronedarone effective for the prevention of recurrent atrial fibrillation? | 2008 Mar |
|
Dronedarone: a new treatment for atrial fibrillation. | 2008 Nov |
|
Amiodarone as paradigm for developing new drugs for atrial fibrillation. | 2008 Oct |
|
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 |
|
Clinical trials update from Heart Rhythm 2008 and Heart Failure 2008: ATHENA, URGENT, INH study, HEART and CK-1827452. | 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 |
|
Alternatives to amiodarone: search for the Holy Grail. | 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 |
|
Clinical trials update from the Heart Failure Society of America and the American Heart Association meetings in 2008: SADHART-CHF, COMPARE, MOMENTUM, thyroid hormone analogue study, HF-ACTION, I-PRESERVE, beta-interferon study, BACH, and ATHENA. | 2009 Feb |
|
Effect of dronedarone on cardiovascular events in atrial fibrillation. | 2009 Feb 12 |
|
Atrial-selective pharmacological therapy for atrial fibrillation: hype or hope? | 2009 Jan |
|
Benzofuran derivatives and the thyroid. | 2009 Jan |
|
Major recent trials in cardiovascular diseases. | 2009 Mar |
|
New pharmacological options for patients with atrial fibrillation: the ATHENA trial. | 2009 May |
|
The role of thyroid hormone nuclear receptors in the heart: evidence from pharmacological approaches. | 2010 Mar |
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
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on
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Record UNII |
JQZ1L091Y2
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Validated (UNII)
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WHO-VATC |
QC01BD07
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LIVERTOX |
NBK548208
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N0000175426
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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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100000081006
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208898
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C118667
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DTXSID3048653
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m4768
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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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N0000190114
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50659
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C65485
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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
|
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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