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 UnknownSubstrateInhibitorDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareDronedaroneMidostaurin The metabolism of Dronedarone can be decreased when combined with Midostaurin. DronedaroneClarithromycin The metabolism of Dronedarone can be decreased when combined with Clarithromycin. DronedaroneEfavirenz The metabolism of Dronedarone can be decreased when combined with Efavirenz. DronedaroneBoceprevir The metabolism of Dronedarone can be decreased when combined with Boceprevir. DronedaroneVoriconazole 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