Dronedarone

Properties

Safety Information

Description

AF is the most common form of sustained cardiac arrhythmia, with an increasing prevalence in the aging population. AF accounts for 34.5% of arrhythmia-related hospital admissions in the United States. The most significant consequences of AF include congestive heart failure, a 5-fold increased risk of stroke, and increased rate of mortality. Although a 90% conversion rate from AF to normal sinus rhythm (NSR) can be achieved with electrical cardioversion, up to 70% of these patients require additional therapy with antiarrhythmic drugs in order to maintain NSR.
Dronedarone, a close analog of amiodarone, is structurally modified to provide improved safety and pharmacokinetic profile. With the introduction of a sulfonamide group, dronedarone is less lipophilic, has lower tissue accumulation, and has a much shorter serum half-life (～24 h) compared with amiodarone. Additionally, dronedarone lacks the iodine moieties that are responsible for thyroid dysfunctions associated with amiodarone. Dronedarone is specifically indicated to reduce the risk of cardiovascular hospitalization in patients with paroxysmal or persistent AF or AFL, with a recent episode of AF/AFL and associated cardiovascular risk factors, who are in sinus rhythm or who will be cardioverted. Similar to amiodarone, dronedarone is a potent blocker of multiple ion currents (including the rapidly activating delayed-rectifier potassium current, the slowly activating delayed-rectifier potassium current, the inward rectifier potassium current, the acetylcholine-activated potassium current, peak sodium current, and L-type calcium current) and exhibits antiadrenergic effects. Overall, dronedarone was well tolerated. The most common side effects were gastrointestinal in nature and included nausea, vomiting, and diarrhea.