[Clinical pharmacology and electrophysiological properties of dronedarone].

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Lewalter T, Pittrow D, Goette A, Kirch W, Hohnloser S

[Clinical pharmacology and electrophysiological properties of dronedarone].

Dtsch Med Wochenschr. 2010 Mar;135 Suppl 2:S43-7. doi: 10.1055/s-0030-1249208. Epub 2010 Mar 10.

PubMed ID

20221978 [ View in PubMed

]

Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Amiodarone	Voltage gated L-type calcium channel (Protein Group)	Protein group	Humans	Unknown	Inhibitor	Details
Amiodarone	Voltage-dependent T-type calcium channel subunit alpha-1I	Protein	Humans	Unknown	Inhibitor	Details