Disease relevance of nifekalant

• Nifekalant (NF) is a novel class III antiarrhythmic agent that is effective in preventing life-threatening ventricular tachycardia/fibrillation (VT/VF) [1].
• Nifekalant is a class III antiarrhythmic drug that has been shown to be effective against ventricular tachyarrhythmias in experimental animals and humans [2].
• Nifekalant for shock-resistant atrial fibrillation [3].
• Nifekalant (NF), a pure K(+) channel blocker developed in Japan, has been reported to be effective in the treatment of life-threatening ventricular arrhythmias [4].
• Defibrillation effects of intravenous nifekalant in patients with out-of-hospital ventricular fibrillation [4].

High impact information on nifekalant

• Nifekalant concentration-dependently increased the force, peak [Ca(2+)](i), and the amplitude of RCCs in Ctr rats but not in MCT rats with identical prolongation of the action potential [5].
• Nifekalant administration significantly decreased the heart rate and increased systolic blood pressure during AF (P<0.001), and successful cardioversion rapidly further ameliorated these parameters (P<0.001) [3].
• Nifekalant inhibited HERG channels in a frequency-dependent manner [2].
• Nifekalant inhibited the HERG current in a concentration-dependent manner with an IC(50) value of 7.9 microM although the drug did not inhibit the minK current in Xenopus oocytes, suggesting selective inhibition of the rapid component of the delayed rectifier K(+) current (I(Kr)) in cardiomyocytes [2].
• We examined the detailed electrophysiological effects of nifekalant on human-ether-a-go-go-related gene (HERG) channels expressed in Xenopus oocytes [2].

Chemical compound and disease context of nifekalant

• Anti-arrhythmic efficacy of nifekalant hydrochloride, a pure class III anti-arrhythmic agent, in patients with healed myocardial infarction and inducible sustained ventricular tachycardia [6].
• Cardiovascular effects of Nifekalant were examined using halothane-anesthetized dogs, and its proarrhythmic potential was estimated with chronic complete atrioventricular block dogs [7].
• CONCLUSIONS: As compared with lidocaine, nifekalant may improve short-term survival in patients with out-of-hospital cardiac arrest due to shock-refractory ventricular fibrillation [8].

Biological context of nifekalant

• Nifekalant modified the voltage dependence and kinetics of HERG channel gating [2].
• CONCLUSIONS: Nifekalant, even at a therapeutic concentration, can increase muscle contraction, but may worsen triggered arrhythmias because of the acceleration of Ca2+ waves under Ca2+-overloaded conditions [9].
• By using representatives of 5 different categories of antiarrhythmic drugs, that is, pilsicainide, propranolol, nifekalant, verapamil, and amiodarone, we investigated whether these ion channel blockers or beta-antagonists affect cardiac apoptosis in cell cultures [10].

Anatomical context of nifekalant

• METHODS: Twelve mongrel dogs subjected to rapid stimulation (400 beats/min) at left atrial appendage (LAA) for 24 hours, were randomized into the control group (rapid pacing only, n = 6) and the nifekalant group (intravenous nifekalant therapy immediately after RAP, n = 6) [11].
• BACKGROUND: Because nifekalant hydrochloride (NIF) displayed a superior defibrillating effect on ventricular tachycardia/fibrillation (VT/VF) in cardiopulmonary arrest (CPA) patients, despite some QT prolongation, its effect on transmural dispersion of repolarization (TDR) in the left ventricle (LV) in an animal model of CPA was investigated [12].

Associations of nifekalant with other chemical compounds

• BACKGROUND: Some patients with an implantable cardioverter-defibrillator (ICD) suffer from burst of inappropriate multiple discharges (severe electrical storm), and because the current therapeutic options are limited, the effect of nifekalant hydrochloride, a new class III drug, on severe electrical storm was investigated in the present study [13].
• As intravenous administration of nifekalant terminated VT, we started oral administration of amiodarone (day 1) [14].
• Combined effects of nifekalant and lidocaine on the spiral-type re-entry in a perfused 2-dimensional layer of rabbit ventricular myocardium [15].
• However, one month after switching over nifekalant to sotalol, a short duration of ST elevation was documented in ECG monitoring at almost the same time for three consecutive days [16].

Gene context of nifekalant

• In control patients, RAMAP was recorded at CLs of 600 and 350 ms before and after administration of nifekalant [17].
• Prevention of Life-Threatening Ventricular Tachyarrhythmia by a Novel and Pure Class-III Agent, Nifekalant Hydrochloride [18].
• Experience with nifekalant hydrochloride in a patient with ischemic cardiomyopathy and severe ventricular dysfunction after dor operation [19].

Analytical, diagnostic and therapeutic context of nifekalant

• In 18 patients (75%), sinus rhythm was restored and maintained after nifekalant infusion (6 patients) or subsequent transthoracic cardioversion (12 patients) [3].
• The study included 18 patients with paroxysmal AF who underwent electrophysiological study before and after intravenous infusion of nifekalant [20].
• The rates of survival until hospital discharge were significantly higher in the nifekalant group (57%, 17/30) than in the control group (30%, 10/33; P < 0.03) [21].
• Multivariate analysis showed that treatment with nifekalant and early initiation of cardiopulmonary resuscitation were independent predictors of 24-h survival [8].
• As a control group, we also included 33 IHD patients with VT/VF that had been resistant to DC countershock upon or during hospitalization between January 1996 and May 2000 before nifekalant became commercially available [21].

References