Literature DB >> 10730550

Azimilide.

D Clemett1, A Markham.   

Abstract

Azimilide is a potassium channel antagonist that, in contrast to existing class III antiarrhythmic agents, blocks both the rapidly (I(Kr)) and slowly (I(Ks)) activating components of the delayed rectifier potassium current. In animal and clinical studies, azimilide prolonged repolarisation by increasing the action potential duration and effective refractory period. In animal models, azimilide was effective in terminating both atrial and ventricular arrhythmias. Azimilide also demonstrated antifibrillatory efficacy in a canine model of sudden cardiac death. In patients with a history of atrial fibrillation/flutter, oral azimilide controlled arrhythmias more effectively than placebo in a 6-month randomised double-blind study. At a dosage of 125 mg once daily, azimilide significantly increased the time to first symptomatic recurrence of atrial fibrillation/flutter. However, no significant difference between placebo and azimilide was found in another study. Oral azimilide 100 mg once daily demonstrated clinically significant treatment effects in patients with paroxysmal supraventricular tachycardia. In clinical trials, azimilide was generally well tolerated and headache was the most commonly occurring adverse event. Azimilide is associated with a low incidence of proarrhythmic events, such as torsades de pointes, and few serious adverse events have been reported.

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Year:  2000        PMID: 10730550     DOI: 10.2165/00003495-200059020-00016

Source DB:  PubMed          Journal:  Drugs        ISSN: 0012-6667            Impact factor:   9.546


  18 in total

1.  Suppression of inducible ventricular arrhythmias by intravenous azimilide in dogs with previous myocardial infarction.

Authors:  A P Drexler; J M Micklas; R R Brooks
Journal:  J Cardiovasc Pharmacol       Date:  1996-12       Impact factor: 3.105

Review 2.  Emerging class III antiarrhythmic agents: mechanism of action and proarrhythmic potential.

Authors:  L A Nair; A O Grant
Journal:  Cardiovasc Drugs Ther       Date:  1997-04       Impact factor: 3.727

3.  The novel class III antiarrhythmics NE-10064 and NE-10133 inhibit IsK channels expressed in Xenopus oocytes and IKs in guinea pig cardiac myocytes.

Authors:  A E Busch; K Malloy; W J Groh; M D Varnum; J P Adelman; J Maylie
Journal:  Biochem Biophys Res Commun       Date:  1994-07-15       Impact factor: 3.575

4.  Class III antiarrhythmic agents have a lot of potential but a long way to go. Reduced effectiveness and dangers of reverse use dependence.

Authors:  L M Hondeghem; D J Snyders
Journal:  Circulation       Date:  1990-02       Impact factor: 29.690

5.  Effects of azimilide and d,l-sotalol on the heart rate and blood pressure response to isoproterenol in anesthetized rats.

Authors:  S W Mittelstadt; A E Maynard; D R Benn; E R Lowe; D R Kostreva
Journal:  Cardiovasc Drugs Ther       Date:  1997-09       Impact factor: 3.727

6.  The azimilide post-infarct survival evaluation (ALIVE) trial.

Authors:  A J Camm; R Karam; C M Pratt
Journal:  Am J Cardiol       Date:  1998-03-19       Impact factor: 2.778

7.  Effects of azimilide dihydrochloride on circus movement atrial flutter in the canine sterile pericarditis model.

Authors:  M Restivo; M Hegazy; E B Caref; M J Avitable; M A Assadi; M el-Hamami; H Yin; M Piracha; R R Brooks; N el-Sherif
Journal:  J Cardiovasc Electrophysiol       Date:  1996-07

8.  Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents.

Authors:  B Fermini; N K Jurkiewicz; B Jow; P J Guinosso; E P Baskin; J J Lynch; J J Salata
Journal:  J Cardiovasc Pharmacol       Date:  1995-08       Impact factor: 3.105

Review 9.  Effects of Class III drugs on atrial fibrillation.

Authors:  A Capucci; G Q Villani; D Aschieri; M Piepoli
Journal:  J Cardiovasc Electrophysiol       Date:  1998-08

10.  Protection against programmed electrical stimulation-induced ventricular tachycardia and sudden cardiac death by NE-10064, a class III antiarrhythmic drug.

Authors:  S C Black; J L Butterfield; B R Lucchesi
Journal:  J Cardiovasc Pharmacol       Date:  1993-12       Impact factor: 3.105

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