Ibutilide fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm. Ibutilide at concentrations ranging between 10 nM and 100 µM inhibited IKr (rectifier potassium currents) in dose-dependent manner with a half maximal effective concentration of 2.03 ± 0.74 µM (n = 5-10). The amplitude of tail currents activated by prepulse to + 20 mV was decreased from 253 ± 52 to 130 ± 25 pA (n = 8, p < 0.01) in the presence of 1 µM ibutilide. The slow IKs persisted to greater extent even at 100 μM ibutilide revealing a distinguishable selectivity toward the IKr component[3]. Ibutilide is a Vaughan-Williams class III antiarrhythmic agent approved for intravenous use for the rapid termination of recent-onset AF or AFl (atrial fibrillation or atrial flutter). The drug is extensively metabolized by the liver, has a volume of distribution of 11 - 15 L/kg, is 40% protein bound, and has an elimination half-life of 6 hours in patients[4]. Intravenous ibutilide 0.01 to 0.025 mg/kg or 1 to 2 mg successfully converted atrial flutter or fibrillation to sinus rhythm in 33 to 49% of patients in 2 placebo-controlled trials involving 439 patients with sustained arrhythmia[5]. Ibutilide is also safe and efficient in the treatment of atrial fibrillation in patients who have had cardiac surgery, and in accessory pathway-mediated atrial fibrillation Where the conversion rate of ibutilide is as high as 95%[6].
Ibutilide fumarate/富马酸伊布利特 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Canine right atrial cells
20 nmol/L
To investigate the effect of Ibutilide alone and in combination with Flecainide on atrial and ventricular action potential duration (APD), results showed that Ibutilide significantly prolonged APD in both atria and ventricles.
Prolonged QT Interval in EKG a... 展开 >>nd Sudden Death 收起 <<
Phase 2
Completed
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United States, Indiana
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Indiana Clinical Research Center
Indianapolis, Indiana, United States, 46202
Purdue University
Indianapolis, Indiana, United States, 46202 收起 <<
Prolonged QT Interval in EKG a... 展开 >>nd Sudden Death 收起 <<
Phase 2
Completed
-
United States, Indiana
... 展开 >>
Indiana Clinical Research Center
Indianapolis, Indiana, United States, 46202
Purdue University
Indianapolis, Indiana, United States, 46202 收起 <<
United States, California
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Regional Cardiology Associates
Sacramento, California, United States, 95823
United States, Massachusetts
Massachusetts General Hospital
Boston, Massachusetts, United States, 02114
Brigham and Women's Hospital
Boston, Massachusetts, United States, 02115
United States, New York
Icahn School of Medicine at Mount Sinai
New York, New York, United States, 10029
United States, Virginia
University Of Virginia Health System
Charlottesville, Virginia, United States, 22908
Canada, Ontario
Sunnybrook Health Sciences Centre
Toronto, Ontario, Canada, M4N 3M5
Korea, Republic of
Republic of Korea University Medical Center
Seoul, Korea, Republic of 收起 <<
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