Clinical pharmacology of dronedarone: implications for the therapy of atrial fibrillation.

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Dorian P

Clinical pharmacology of dronedarone: implications for the therapy of atrial fibrillation.

J Cardiovasc Pharmacol Ther. 2010 Dec;15(4 Suppl):15S-8S. doi: 10.1177/1074248410367792. Epub 2010 May 14.

PubMed ID

20472816 [ View in PubMed

]

Abstract

Dronedarone, a recently approved antiarrhythmic agent, is a chemical analog of amiodarone. It has an approximately 15% bioavailability, with plasma concentrations markedly increasing after a high-fat meal; it is recommended to be taken with food. The primary metabolic clearance pathway for dronedarone is via the hepatic enzyme system (primarily cytochrome P450 3A4 [CYP3A4]); the half-life of dronedarone is 27 to 31 hours. Strong CYP3A4 inhibitors, such as ketoconazole, are associated with a marked increase in dronedarone maximum concentration and are thus contraindicated; inducers of CYP3A4 will conversely decrease dronedarone exposure. Dronedarone is a substrate for P-glycoprotein (P-gp) and will lead to an increase in concentration of P-gp substrates such as digoxin. Dronedarone will cause a small increase in creatinine concentrations, without a change in glomerular filtration rate (GFR). Gender, renal dysfunction, weight, and age have little effect on the pharmacokinetics of dronedarone, and dose adjustment for these variables is not required.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Dronedarone	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate Inhibitor	Details

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
Integrate drug-drug interactions in your software
Dronedarone Midostaurin	The metabolism of Dronedarone can be decreased when combined with Midostaurin.
Dronedarone Clarithromycin	The metabolism of Dronedarone can be decreased when combined with Clarithromycin.
Dronedarone Efavirenz	The metabolism of Dronedarone can be decreased when combined with Efavirenz.
Dronedarone Boceprevir	The metabolism of Dronedarone can be decreased when combined with Boceprevir.
Dronedarone Voriconazole	The metabolism of Dronedarone can be decreased when combined with Voriconazole.

Pharmaco-metabolomics

Drug	Drug Groups	Metabolite	Change	Description
Dronedarone	Approved	Creatinine	increased	Dronedarone increases the level of Creatinine in the blood