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Dronedarone
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| Systematic (IUPAC) name | |
| N-(2-Butyl-3-(p-(3-(dibutylamino)propoxy)benzoyl)- 5-benzofuranyl)methanesulfonamide |
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| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C31H44N2O5S |
| Mol. mass | 556.758 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 24 hours |
| Excretion | feces |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | ? |
Dronedarone (also known as SR33589 or Multaq) is a drug under development by Sanofi-Aventis, mainly for the indication of cardiac arrhythmias (irregular heartbeat). It is currently in phase III trials for atrial fibrillation and in patients with an implantable cardioverter-defibrillator (ICD); a trial in heart failure was stopped as an interim analysis showed a possible increase in heart failure deaths.[1]
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Chemistry
Chemically it is a benzofuran derivative related to amiodarone, a popular antiarrhythmic the use of which is limited to toxicity due its high iodine content (pulmonary fibrosis, thyroid disease) as well as by liver disease. Dronedarone lacks the iodine, and is expected to have less toxicity, yet it displays amiodarone-like class III antiarrhythmic activity in vitro[2] and in clinical trials.[1]
Pharmacokinetics
Dronedarone is less lipophilic than amiodarone, has a much smaller volume of distribution, and has an elimination half-life of 24 hours-- this stands in contrast to amiodarone's half-life of several weeks.[3] As a result of these pharmacokinetic characteristics, dronedarone dosing may be less complicated than amiodarone.
Clinical trials
In a 2007 trial in atrial fibrillation, dronedarone was significantly more effective than placebo in maintaining sinus rhythm, with no difference in lung and thyroid function in the short term.[4]
References
- ^ a b Køber L, Torp-Pedersen C, McMurray JJ et al (June 2008). "Increased mortality after dronedarone therapy for severe heart failure". N Engl J Med 358 (25): 2678-87.
- ^ Sun W, Sarma JS, Singh BN (November 1999). "Electrophysiological effects of dronedarone (SR33589), a noniodinated benzofuran derivative, in the rabbit heart : comparison with amiodarone". Circulation 100 (22): 2276–81. PMID 10578003.
- ^ Dale KM, White CM (April 2007). "Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter". Ann Pharmacother 41 (4): 599–605. doi:. PMID 17389667.
- ^ Singh BN, Connolly SJ, Crijns HJ et al (Sept 2007). "Dronedarone for maintenance of sinus rhythm in atrial fibrillation or flutter". N Engl J Med 357: 987–999. doi:. PMID 17804843.
Wikipedia content modification information:
- This page was last modified on 17 August 2008, at 23:04.
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