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Dronedarone


General


Pronunciation

(droe NE da rone)


Brand Names: U.S.

  • Multaq

Indications


Use: Labeled Indications

Paroxysmal or persistent atrial fibrillation: To reduce the risk of hospitalization for atrial fibrillation (AF) in patients in sinus rhythm with a history of paroxysmal or persistent AF


Contraindications


Hypersensitivity to dronedarone or any component of the formulation; permanent AF (patients in whom normal sinus rhythm will not or cannot be restored); symptomatic heart failure (heart failure with recent decompensation requiring hospitalization or NYHA Class IV symptoms); liver or lung toxicity related to previous amiodarone use; second-degree or third-degree atrioventricular block or sick sinus syndrome (except when used in conjunction with a functioning artificial pacemaker); bradycardia <50 bpm; concomitant use of strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, voriconazole, cyclosporine, telithromycin, clarithromycin, nefazodone, ritonavir); concomitant use of drugs or herbal products known to prolong the QT interval increasing the risk for torsade de pointes (eg, phenothiazine antipsychotics, tricyclic antidepressants, certain oral macrolide antibiotics, class I and III antiarrhythmics); QTc (Bazett) interval ≥500 msec or PR interval >280 msec; severe hepatic impairment; pregnancy; breast-feeding

Canadian labeling: Additional contraindications (not in U.S. labeling): Permanent atrial fibrillation of any duration where sinus rhythm cannot be restored and further attempts to restore it are no longer considered; history of or current heart failure regardless of NYHA class; left ventricular systolic dysfunction; complete bundle branch block, distal block, sinus node dysfunction, or atrial conduction defects (except when used in conjunction with a functioning pacemaker); unstable hemodynamic condition


ALERT: U.S. Boxed Warning

Increased risk of death, stroke, and heart failure:

Dronedarone is contraindicated in patients with symptomatic heart failure with recent decompensation requiring hospitalization or New York Heart Association (NYHA) class IV heart failure. Dronedarone doubles the risk of death in these patients.

Dronedarone is contraindicated in patients in atrial fibrillation (AF) who will not or cannot be cardioverted into normal sinus rhythm. In patients with permanent AF, dronedarone doubles the risk of death, stroke, and hospitalization for heart failure.


Dosing and Administration


Dosing: Adult

Note: Prior to initiation of dronedarone, class I or III antiarrhythmics (eg, amiodarone, flecainide, propafenone, quinidine, disopyramide, dofetilide, sotalol) or drugs that are strong inhibitors of CYP3A (eg, ketoconazole) must be stopped.

Paroxysmal or persistent atrial fibrillation: Oral: 400 mg twice daily.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Renal Impairment

No dosage adjustment necessary.


Dosing: Hepatic Impairment

Mild-to-moderate impairment: No dosage adjustment necessary.

Severe impairment: Use is contraindicated.


Administration

Administer with morning and evening meal. Avoid coadministration with grapefruit/grapefruit juice.

Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).


Dietary Considerations

Take with a meal. Avoid coadministration with grapefruit/grapefruit juice.


Storage

Store at 25 ‚ °C (77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Multaq: 400 mg


Drug Interactions

Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Afatinib. Management: Per US labeling: reduce afatinib by 10mg if not tolerated. Per Canadian labeling: avoid combination if possible; if used, administer the P-gp inhibitor simultaneously with or after the dose of afatinib. Consider therapy modification

Antipsychotic Agents (Phenothiazines): May enhance the arrhythmogenic effect of Dronedarone. Avoid combination

Apixaban: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Apixaban. Monitor therapy

Aprepitant: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Aprepitant. Avoid combination

Asunaprevir: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Asunaprevir. Avoid combination

AtorvaSTATin: Dronedarone may increase the serum concentration of AtorvaSTATin. Monitor therapy

Avanafil: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Avanafil. Management: The maximum avanafil adult dose is 50 mg per 24-hour period when used together with a moderate CYP3A4 inhibitor. Patients receiving such a combination should also be monitored more closely for evidence of adverse effects. Consider therapy modification

Beta-Blockers: Dronedarone may enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6. Management: Use lower initial beta-blocker doses; adequate tolerance of the combination, based on ECG findings, should be confirmed prior to any increase in beta-blocker dose. Consider therapy modification

Blonanserin: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Blonanserin. Monitor therapy

Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Bosentan: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bosentan. Management: Concomitant use of both a CYP2C9 inhibitor and a CYP3A inhibitor or a single agent that inhibits both enzymes with bosentan is likely to cause a large increase in serum concentrations of bosentan and is not recommended. See monograph for details. Monitor therapy

Bosutinib: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bosutinib. Avoid combination

Bosutinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Bosutinib. Avoid combination

Bradycardia-Causing Agents: May enhance the bradycardic effect of other Bradycardia-Causing Agents. Monitor therapy

Brentuximab Vedotin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased. Monitor therapy

Bretylium: May enhance the bradycardic effect of Bradycardia-Causing Agents. Bretylium may also enhance atrioventricular (AV) blockade in patients receiving AV blocking agents. Monitor therapy

Brexpiprazole: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Brexpiprazole. Management: The brexpiprazole dose should be reduced to 25% of usual if used together with both a moderate CYP3A4 inhibitor and a strong or moderate CYP2D6 inhibitor, or if a moderate CYP3A4 inhibitor is used in a CYP2D6 poor metabolizer. Monitor therapy

Bromocriptine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bromocriptine. Management: The bromocriptine dose should not exceed 1.6 mg daily with use of a moderate CYP3A4 inhibitor. The Cycloset brand specifically recommends this dose limitation, but other bromocriptine products do not make such specific recommendations. Consider therapy modification

Budesonide (Systemic): CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Budesonide (Systemic). Avoid combination

Budesonide (Topical): CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Budesonide (Topical). Management: Per US prescribing information, avoid this combination. Canadian product labeling does not recommend strict avoidance. If combined, monitor for excessive glucocorticoid effects as budesonide exposure may be increased. Consider therapy modification

Calcium Channel Blockers (Nondihydropyridine): May enhance the AV-blocking effect of Dronedarone. Other electrophysiologic effects of Dronedarone may also be increased. Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Dronedarone. Dronedarone may increase the serum concentration of Calcium Channel Blockers (Nondihydropyridine). Management: Use lower starting doses of the nondihydropyridine calcium channel blockers (i.e., verapamil, diltiazem), and only consider increasing calcium channel blocker dose after obtaining ECG-based evidence that the combination is being well-tolerated. Exceptions: Bepridil. Consider therapy modification

Cannabis: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cannabis. More specifically, tetrahydrocannabinol and cannabidiol serum concentrations may be increased. Monitor therapy

Ceritinib: Bradycardia-Causing Agents may enhance the bradycardic effect of Ceritinib. Management: If this combination cannot be avoided, monitor patients for evidence of symptomatic bradycardia, and closely monitor blood pressure and heart rate during therapy. Avoid combination

Cilostazol: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol. Management: Consider reducing the cilostazol dose to 50 mg twice daily in adult patients who are also receiving moderate inhibitors of CYP3A4. Consider therapy modification

Cobimetinib: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cobimetinib. Management: Avoid the concomitant use of cobimetinib and moderate CYP3A4 inhibitors. If concurrent short term (14 days or less) use cannot be avoided, reduce the cobimetinib dose to 20 mg daily. Avoid combination

Colchicine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Colchicine. Management: Reduce colchicine dose as directed when using with a moderate CYP3A4 inhibitor, and increase monitoring for colchicine-related toxicity. Use extra caution in patients with impaired renal and/or hepatic function. Consider therapy modification

Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: Colchicine is contraindicated in patients with impaired renal or hepatic function who are also receiving a p-glycoprotein inhibitor. In those with normal renal and hepatic function, reduce colchicine dose as directed. Consider therapy modification

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CycloSPORINE (Systemic): May increase the serum concentration of Dronedarone. Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Dronedarone. Avoid combination

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Dronedarone. Avoid combination

CYP3A4 Substrates: CYP3A4 Inhibitors (Moderate) may decrease the metabolism of CYP3A4 Substrates. Exceptions: Alitretinoin (Systemic); Praziquantel; Vinorelbine. Monitor therapy

Dabigatran Etexilate: Dronedarone may increase the serum concentration of Dabigatran Etexilate. Management: Dose reductions and/or avoidance of this combination may be necessary. Specific recommendations vary by U.S. vs. Canadian labeling, renal function, and indication for dabigatran. Refer to full monograph or dabigatran labeling. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dapoxetine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dapoxetine. Management: The dose of dapoxetine should be limited to 30 mg/day when used together with a moderate inhibitor of CYP3A4. Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Digoxin: May enhance the AV-blocking effect of Dronedarone. Digoxin may also enhance the other electrophysiologic effects of Dronedarone. Dronedarone may increase the serum concentration of Digoxin. Management: Avoid concurrent use of digoxin when possible. If concurrent use is necessary, reduce adult digoxin dose by 50%, monitor digoxin concentration closely, and increase monitoring for both clinical response to therapy and the occurrence of adverse effects. Consider therapy modification

DOCEtaxel: Dronedarone may increase the serum concentration of DOCEtaxel. Management: Avoid this combination whenever possible. If this combination must be used, consider using a reduced docetaxel dose, and/or increase monitoring for evidence of serious docetaxel toxicity (e.g., neutropenia, mucositis, etc.). Consider therapy modification

Domperidone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Domperidone. Avoid combination

DOXOrubicin (Conventional): CYP3A4 Inhibitors (Moderate) may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to moderate CYP3A4 inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided. Consider therapy modification

DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to P-glycoprotein inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided. Consider therapy modification

Dronabinol: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dronabinol. Monitor therapy

Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Edoxaban. Management: See full monograph for details. Reduced doses are recommended for patients receiving edoxaban for venous thromboembolism in combination with certain inhibitors. Similar dose adjustment is not recommended for edoxaban use in atrial fibrillation. Consider therapy modification

Eletriptan: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eletriptan. Management: The use of eletriptan within 72 hours of a moderate CYP3A4 inhibitor should be avoided. Consider therapy modification

Eplerenone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eplerenone. Management: When used concomitantly with moderate inhibitors of CYP3A4, eplerenone dosing recommendations vary by indication and international labeling. See full drug interaction monograph for details. Consider therapy modification

Everolimus: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Everolimus. Management: Everolimus dose reductions are required for patients being treated for subependymal giant cell astrocytoma or renal cell carcinoma. See prescribing information for specific dose adjustment and monitoring recommendations. Consider therapy modification

Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Everolimus. Management: Everolimus dose reductions are required for patients being treated for subependymal giant cell astrocytoma or renal cell carcinoma. See prescribing information for specific dose adjustment and monitoring recommendations. Consider therapy modification

FentaNYL: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of FentaNYL. Management: Monitor patients closely for several days following initiation of this combination, and adjust fentanyl dose as necessary. Consider therapy modification

Fingolimod: May enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III). Avoid combination

Flibanserin: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Flibanserin. Avoid combination

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Grapefruit Juice: May increase the serum concentration of Dronedarone. Avoid combination

GuanFACINE: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of GuanFACINE. Management: Reduce the guanfacine dose by 50% when initiating this combination. Consider therapy modification

Highest Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of other Highest Risk QTc-Prolonging Agents. Avoid combination

HYDROcodone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of HYDROcodone. Monitor therapy

Ibrutinib: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ibrutinib. Management: If a moderate CYP3A inhibitor must be used, consider reducing the dose of ibrutinib to 140mg daily and monitor closely for signs of toxicity. Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ifosfamide: CYP3A4 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Ifosfamide. Monitor therapy

Imatinib: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Imatinib. Monitor therapy

Ivabradine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ivabradine. Avoid combination

Ivabradine: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Ivacaftor: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ivacaftor. Management: Ivacaftor dose reductions are required; consult prescribing information for specific age- and weight-based recommendations. Consider therapy modification

Lacosamide: Bradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide. Monitor therapy

Lidocaine (Topical): May enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III). Antiarrhythmic Agents (Class III) may increase the serum concentration of Lidocaine (Topical). This mechanism specifically applies to amiodarone and dronedarone. Monitor therapy

Lomitapide: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lomitapide. Avoid combination

Lovastatin: Dronedarone may increase the serum concentration of Lovastatin. Management: Limit lovastatin to a maximum of 20 mg/day (in adults). Increase monitoring for signs of lovastatin toxicity (e.g., myopathy, rhabdomyolysis). Consider therapy modification

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Lurasidone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lurasidone. Management: U.S. labeling: start at 20 mg/day and limit to max of 80 mg/day with moderate CYP3A4 inhibitor. Canadian labeling: limit to max of 40 mg/day with moderate CYP3A4 inhibitor; avoid concomitant use of grapefruit products. Consider therapy modification

MiFEPRIStone: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Mirodenafil: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Mirodenafil. Monitor therapy

Moderate Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Naloxegol: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Naloxegol. Avoid combination

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

NiMODipine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of NiMODipine. Monitor therapy

Nintedanib: Combined Inhibitors of CYP3A4 and P-glycoprotein may increase the serum concentration of Nintedanib. Monitor therapy

Olaparib: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Olaparib. Management: Avoid use of moderate CYP3A4 inhibitors in patients being treated with olaparib. If such concurrent use cannot be avoided, the dose of olaparib should be reduced to 200 mg twice daily. Avoid combination

OxyCODONE: CYP3A4 Inhibitors (Moderate) may enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Moderate) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite Oxymorphone may also be increased. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of PAZOPanib. Avoid combination

Perhexiline: CYP2D6 Inhibitors (Weak) may increase the serum concentration of Perhexiline. Monitor therapy

P-glycoprotein/ABCB1 Substrates: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

Pimecrolimus: CYP3A4 Inhibitors (Moderate) may decrease the metabolism of Pimecrolimus. Monitor therapy

Pimozide: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide. Avoid combination

Propafenone: May enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III). Management: Concurrent use of propafenone with quinidine, amiodarone, or other class IA or class III antiarrhythmics should be avoided. Treatment with such agents should be withheld for at least 5 half-lives prior to initiation of propafenone. Avoid combination

Prucalopride: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Prucalopride. Monitor therapy

QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying): May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Ranolazine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ranolazine. Management: Limit the ranolazine adult dose to a maximum of 500 mg twice daily in patients concurrently receiving moderate CYP3A4 inhibitors (e.g., diltiazem, verapamil, erythromycin, etc.). Consider therapy modification

Red Yeast Rice: Dronedarone may increase the serum concentration of Red Yeast Rice. In particular, concentrations of the lovastatin-like components may be increased. Monitor therapy

RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RifAXIMin. Monitor therapy

Rivaroxaban: Inhibitors of CYP3A4 (Moderate) and P-glycoprotein may increase the serum concentration of Rivaroxaban. Management: No action is needed in patients with normal renal function. US labeling recommends avoidance in patients with estimated creatinine clearance 15 to 80 mL/min unless prospective benefits outweigh the risks. See monograph for details of Canadian labeling. Consider therapy modification

Rosuvastatin: Dronedarone may increase the serum concentration of Rosuvastatin. Monitor therapy

Ruxolitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Management: Ruxolitinib Canadian product labeling recommends avoiding use with bradycardia-causing agents to the extent possible. Monitor therapy

SAXagliptin: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of SAXagliptin. Monitor therapy

Sildenafil: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Sildenafil. Monitor therapy

Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Silodosin. Avoid combination

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Simeprevir: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Simeprevir. Avoid combination

Simvastatin: Dronedarone may increase the serum concentration of Simvastatin. Management: Limit simvastatin to a max of 10 mg/day (in adults). Increase monitoring for signs of simvastatin toxicity (e.g., myositis, rhabdomyolysis). Consider therapy modification

Sonidegib: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Sonidegib. Management: Avoid concomitant use of sonidegib and moderate CYP3A4 inhibitors when possible. When concomitant use cannot be avoided, limit CYP3A4 inhibitor use to less than 14 days and monitor for sonidegib toxicity (particularly musculoskeletal adverse reactions). Consider therapy modification

St Johns Wort: May decrease the serum concentration of Dronedarone. Avoid combination

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Suvorexant: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Suvorexant. Consider therapy modification

Tacrolimus (Systemic): May enhance the QTc-prolonging effect of Dronedarone. Dronedarone may increase the serum concentration of Tacrolimus (Systemic). Management: Monitor for increased serum tacrolimus concentrations, tacrolimus toxicity, and QTc interval prolongation if combined with dronedarone. Tacrolimus dose adjustments may be needed. Consider therapy modification

Tetrahydrocannabinol: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tetrahydrocannabinol. Monitor therapy

Ticagrelor: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ticagrelor. Monitor therapy

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Tofacitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Monitor therapy

Tolvaptan: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tolvaptan. Avoid combination

Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Topotecan. Avoid combination

Trabectedin: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Trabectedin. Avoid combination

Tricyclic Antidepressants: May enhance the arrhythmogenic effect of Dronedarone. Avoid combination

Udenafil: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Udenafil. Monitor therapy

Ulipristal: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ulipristal. Management: This is specific for when ulipristal is being used for signs/symptoms of uterine fibroids (Canadian indication). When ulipristal is used as an emergency contraceptive, patients receiving this combination should be monitored for ulipristal toxicity. Avoid combination

Venetoclax: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring these combinations. Consider therapy modification

Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring these combinations. Consider therapy modification

Vilazodone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Vilazodone. Monitor therapy

VinCRIStine (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of VinCRIStine (Liposomal). Avoid combination

Vindesine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Vindesine. Monitor therapy

Vinflunine: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Vitamin K Antagonists (eg, warfarin): Dronedarone may increase the serum concentration of Vitamin K Antagonists. Monitor therapy

Zopiclone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Zopiclone. Management: The starting adult dose of zopiclone should not exceed 3.75 mg if combined with a moderate CYP3A4 inhibitor. Monitor patients for signs and symptoms of zopiclone toxicity if these agents are combined. Consider therapy modification


Monitoring Parameters

ECG (at least every 3 months), blood pressure, heart rate and rhythm throughout therapy; assess patient for signs of lethargy, edema of the hands or feet; monitor serum electrolytes, especially potassium and magnesium; serum liver enzymes and bilirubin (periodically, especially during the first 6 months of therapy)

Patients with implantable cardiac devices: Monitor pacing or defibrillation thresholds with initiation of dronedarone and during treatment.

Canadian labeling: Additional monitoring recommendations: ECG at least every 6 months during therapy; serum creatinine 1 week after initiating therapy followed by periodic renal function tests; periodic pulmonary function assessment


Adverse Reactions


>10%:

Cardiovascular: Prolonged Q-T interval on ECG (Bazett; 28% [placebo: 19%]; defined as >450 msec in males or >470 msec in female)

Renal: Increased serum creatinine (51%; increased >10%; occurred 5 days after initiation)

1% to 10%:

Cardiovascular: Bradycardia (3%)

Dermatologic: Allergic dermatitis ( ≤5%), dermatitis ( ≤5%), eczema ( ≤5%), pruritus ( ≤5%), skin rash ( ≤5%; described as generalized, macular, maculopapular, erythematous)

Gastrointestinal: Diarrhea (9%), nausea (5%), abdominal pain (4%), dyspepsia (2%), vomiting (2%)

Neuromuscular & skeletal: Weakness (7%)

<1%, postmarketing, and/or case reports: Acute hepatic failure (requiring transplant), anaphylaxis, angioedema, atrial flutter (with 1:1 atrioventricular conduction), cardiac failure (new or worsened), dysgeusia, hepatic injury, hyperbilirubinemia, hypersensitivity angiitis, increased blood urea nitrogen, increased liver enzymes, interstitial pulmonary disease, pneumonitis, pulmonary fibrosis, skin photosensitivity, vasculitis


Warnings/Precautions


Special Populations: Hepatic Function Impairment

Dronedarone mean exposure increased 1.3-fold and mean exposure of the N-debutyl metabolite decreased by 50% in patients with moderate hepatic impairment.


Special Populations: Elderly

Dronedarone exposure is 23% higher in patients 65 years and older.


Special Populations: Gender

Dronedarone exposure is 30% higher in females than in males.


Special Populations: Race

Asian (Japanese) males have about a 2-fold higher exposure than white males.


Warnings/Precautions

Concerns related to adverse effects:

- Heart failure (HF): New-onset or worsening HF symptoms have been observed. If patient develops new or worsening HF symptoms (eg, weight gain, dependent edema, or increasing shortness of breath) requiring hospitalization while on therapy, discontinue dronedarone.

- Hepatic effects: Severe liver injury, including acute liver failure leading to liver transplant, has been reported. If liver injury is suspected, discontinue therapy and evaluate liver enzymes/bilirubin. Appropriate treatment should be started and therapy should not be reinitiated if liver injury is confirmed. Advise patients to report any signs or symptoms of hepatic injury (anorexia, malaise, fatigue, jaundice, dark urine, itching, right upper quadrant pain, nausea, vomiting, abdominal pain, and/or fever). Consider periodic monitoring of serum liver enzymes and bilirubin, especially during the first 6 months of therapy.

- QTc interval prolongation: Dronedarone induces a moderate prolongation of the QT interval (average ~10 msec); much greater effects have been observed. Use in patients with QTc (Bazett) interval ≥500 msec is contraindicated; discontinue use of dronedarone if this occurs during therapy.

- Renal effects: Dronedarone may produce a slight increase in serum creatinine (~0.1 mg/dL) within 7 days of initiation due to inhibition of tubular secretion; glomerular filtration rate is not affected. Effect is reversible upon discontinuation. Marked increase in serum creatinine, prerenal azotemia and acute renal failure have been reported; usually in the setting of heart failure or hypovolemia. The effects appear to be reversible upon drug discontinuation and with appropriate medical treatment; monitor renal function periodically. Discontinue use in the setting of heart failure as this is a contraindication.

- Respiratory effects: Interstitial lung disease (including pulmonary fibrosis and pneumonitis) has been reported. Evaluate patients with onset of dyspnea or nonproductive cough for pulmonary toxicity. Discontinue therapy with confirmed pulmonary toxicity. Use is contraindicated in patients with previous pulmonary toxicity with amiodarone.

Disease-related concerns:

- Cardiac devices (eg, implanted defibrillators): One trial conducted during ischemia in a closed-chest animal (porcine) model demonstrated that dronedarone does not affect defibrillation threshold of implantable cardioverter defibrillators (ICD) compared to amiodarone (Chevalier, 2012). However, prospective human studies are necessary to confirm these results in humans. Assess defibrillation threshold when initiating dronedarone and during therapy.

- Electrolyte imbalance: Correct electrolyte disturbances, especially hypokalemia or hypomagnesemia, prior to use and throughout therapy.

- Heart failure (HF): [U.S. Boxed Warning]: The risk of death is doubled when used in patients with symptomatic HF with recent decompensation requiring hospitalization or NYHA Class IV symptoms; use is contraindicated in these patients. Canadian labeling contraindicates use of dronedarone in patients with a history of or current heart failure, regardless of NYHA class.

- Hepatic impairment: Use with caution in patients with mild-to-moderate hepatic impairment; use is contraindicated in severe hepatic impairment. Use is also contraindicated in patients with previous liver toxicity with amiodarone.

- Permanent atrial fibrillation (AF): [U.S. Boxed Warning]: Use in patients with permanent atrial fibrillation doubles the risk of death, stroke (especially within the first 2 weeks of therapy), and hospitalization for heart failure. Use is contraindicated in patients with permanent AF who will not or cannot be converted to normal sinus rhythm. Monitor ECG at least every 3 months. Cardiovert patients who are in AF (if clinically indicated) or discontinue dronedarone.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

- Elderly: In the treatment of atrial fibrillation, avoid antiarrhythmics as first-line treatment. In older adults, data suggests rate control may provide more benefits than risks compared to rhythm control for most patients.

- Women of childbearing potential: Should use effective contraceptive methods during treatment.

Special handling:

- Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

Other warnings/precautions:

- Appropriate use: Initiate only in patients in sinus rhythm who are receiving appropriate antithrombotic therapy.


Pregnancy Risk Factor

X


Pregnancy Considerations

Studies in animals have shown evidence of fetal abnormalities and use is contraindicated in women who are or may become pregnant


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Pharmacology

A noniodinated antiarrhythmic agent structurally related to amiodarone exhibiting properties of all 4 antiarrhythmic classes. Dronedarone inhibits sodium (INa) and potassium (Ikr, IkS, Ik1, and Ik-ACh) channels resulting in prolongation of the action potential and refractory period in myocardial tissue without reverse-use dependent effects; decreases AV conduction and sinus node function through inhibition of calcium (ICa-L) channels and beta1-receptor blocking activity. Similar to amiodarone, dronedarone also inhibits alpha1-receptor mediated increases in blood pressure.


Distribution

Vd: ~1400 L


Metabolism

Hepatic via CYP3A4 to active N-debutyl metabolite (1/10 to 1/3 as potent as dronedarone) and other inactive metabolites


Excretion

Feces (84% mainly as metabolites); urine (~6% mainly as metabolites)


Time to Peak

Plasma: 3-6 hours


Half-Life Elimination

13-19 hours


Protein Binding

>98%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience diarrhea, nausea, vomiting, loss of strength and energy, or abdominal pain. Have patient report immediately to prescriber signs of signs of kidney problems (urinary retention, blood in urine, change in amount of urine passed, weight gain), signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), signs of a severe pulmonary disorder (lung or breathing problems like trouble breathing, shortness of breath, or a cough that is new or worse), excessive weight gain, swelling of arm or leg, bradycardia, or arrhythmia (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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