[Clinical pharmacology and electrophysiological properties of dronedarone].
Dronedarone is a benzofuran derivative structurally similar to amiodarone but non-iodinated. The agent was systematically developed with the aim to maintain the antiarrhythmic potency of amiodarone while reducing the extracardiac side effects of the drug. Dronedarone is less lipophilic compared to the mother compound, which manifests in a substantial lower time to steady state (4-8 days compared to 1-3 weeks with amiodarone), and a more rapid elimination (half life 25-30 hours). Dronedarone has antiarrhythmic properties of all Vaughan-Williams classes. Among other channel blocking effects, It blocks sodium ion channels at higher stimulation frequency, prolongs the cardiac action potential, and has properties of a calcium channel blocker. Further, dronedarone has non-competitive antiadrenegic effects. No reverse use dependence has been documented at higher heart rate. These effects explain the antiarrhythmic and rate control properties of dronedarone in patients with atrial fibrillation.
Lewalter
T
T
Medizinische Klinik und Poliklinik II, Universitätsklinikum Bonn. thorsten.lewalter@marien-hospital-bonn.de
Pittrow
D
D
Goette
A
A
Kirch
W
W
Hohnloser
S
S
D018674:Adrenergic Antagonists / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use; D000638:Amiodarone / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001281:Atrial Fibrillation / Q000097:blood* / Q000188:drug therapy*; D001682:Biological Availability; D015220:Calcium Channels / Q000187:drug effects; D004195:Disease Models, Animal; D000077764:Dronedarone; D004562:Electrocardiography / Q000187:drug effects*; D006207:Half-Life; D006801:Humans; D008657:Metabolic Clearance Rate / Q000502:physiology; D015222:Sodium Channels / Q000187:drug effects
D018674:Adrenergic Antagonists; D000889:Anti-Arrhythmia Agents; D015220:Calcium Channels; D015222:Sodium Channels; D000077764:Dronedarone; D000638:Amiodarone