Flecainide
(Synonyms: 氟卡尼) 目录号 : GC65416Flecainide is a common medication used to help restore and maintain sinus rhythm in patients with atrial fibrillation.
Cas No.:54143-55-4
Sample solution is provided at 25 µL, 10mM.
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Flecainide is a common medication used to help restore and maintain sinus rhythm in patients with atrial fibrillation.
[1] Barman M. et al. J Atr Fibrillation. 2015 Dec 31;8(4):1091.
Cas No. | 54143-55-4 | SDF | Download SDF |
别名 | 氟卡尼 | ||
分子式 | C17H20F6N2O3 | 分子量 | 414.34 |
溶解度 | 储存条件 | Store at -20°C | |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.4135 mL | 12.0674 mL | 24.1348 mL |
5 mM | 0.4827 mL | 2.4135 mL | 4.827 mL |
10 mM | 0.2413 mL | 1.2067 mL | 2.4135 mL |
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Flecainide
J Cardiovasc Electrophysiol 1994 Nov;5(11):964-81.PMID:7889236DOI:10.1111/j.1540-8167.1994.tb01136.x.
Flecainide is a Class IC antiarrhythmic agent whose primary electrophysiologic effect is a slowing of conduction in a wide range of cardiac tissues. It is well absorbed and effective in suppressing isolated premature ventricular contractions (PVCs) or nonsustained ventricular arrhythmia but has only a modest efficacy when electrophysiologic testing is used as an endpoint. Its adverse effect on mortality in the CAST trial suggested a propensity to proarrhythmia--a phenomenon to which the Class IC agents appear particularly prone. Despite the applicability of the CAST study only to patients with a prior myocardial infarction, there has been a shift away from Flecainide in ventricular arrhythmia, but the low noncardiac side effect profile of the agent allows for its continued use in a wide variety of supraventricular arrhythmias.
Flecainide: Electrophysiological properties, clinical indications, and practical aspects
Pharmacol Res 2019 Oct;148:104443.PMID:31493514DOI:10.1016/j.phrs.2019.104443.
Over the last 35 years, Flecainide proved itself one of the most commonly used arrhythmic drugs, expanding its original indication for ventricular arrhythmias and results nowadays as the cornerstone of the rhythm control strategy in atrial fibrillation management of patients without structural heart disease. While the increased mortality associated with Flecainide in the Cardiac Arrhythmia Suppression Trial (CAST) still casts his shadow over Flecainide clinical profile, this compound has subsequently demonstrated safe and is now used successfully for a plethora of indications, including pharmacological cardioversion of atrial fibrillation, cathecolaminergic polymorphic ventricular tachycardia, supraventricular tachyarrhythmias and ventricular pre-excitation. Moreover, the recent marketing of a controlled release formulation, along with the intravenous and immediate release formulations, increased the armamentarium to the clinician's disposal while improving patients' compliance. In the present paper, we offer a comprehensive review of the anti-arrhythmic effects of Flecainide, detailing its electrophysiological properties, its effects on the conduction system, its clinical use and the major side effects and contraindications in clinical practice.
Safety of Flecainide
Drug Saf 2012 Apr 1;35(4):273-89.PMID:22435343DOI:10.2165/11599950-000000000-00000.
Flecainide is a class Ic antiarrhythmic agent that has an important role as part of rhythm control strategies in patients with atrial fibrillation (AF). Early clinical data on the use of Flecainide showed an increase in arrhythmias and mortality compared with placebo in patients with a previous myocardial infarction and asymptomatic or mildly symptomatic ventricular arrhythmias. These findings only apply to a specific group of patients with left ventricular dysfunction and ischaemic heart disease, but had a negative impact on the use of class Ic antiarrhythmics across all indications and patient groups. The aim of this review was to evaluate the available safety data for Flecainide in the literature and to assess its current use in patients with AF. Current European guidelines now recommend the use of Flecainide in carefully selected groups of patients with AF who do not have structural heart disease. This includes for the cardioversion of recent-onset AF, pretreatment prior to direct current cardioversion, out-of-hospital acute oral therapy ('pill-in-the-pocket' approach) and for the ongoing maintenance of sinus rhythm. Potential cardiac adverse effects of Flecainide include proarrhythmia, conduction abnormalities and negative inotropic effects. Dizziness is the most frequent non-cardiac side effect, followed by blurred vision and difficulty focusing; these are almost all mild, transient and tolerable. Data from recent clinical trials in patients with supraventricular arrhythmias suggest that Flecainide has a good tolerability profile in groups of appropriately selected patients. Caution is required when using Flecainide in patients with renal dysfunction, and there are a number of drug interactions, but these are well documented and manageable. Overall, Flecainide is a good choice for the pharmacological management of AF. It has a good safety record and low incidence of adverse effects, rare end-organ toxicity and a low risk of ventricular proarrhythmia. To ensure that the benefits of treatment outweigh any potential risks, careful patient selection and monitoring is required.
Flecainide and encainide
Eur Heart J 1987 Mar;8 Suppl A:33-40.PMID:3107989DOI:10.1093/eurheartj/8.suppl_a.33.
Flecainide and encainide (class IC) are presently under clinical evaluation in Italy. They prolong the duration of the QRS but not the period of ventricular repolarisation: the prolongation of QT is due solely to the prolongation of the Q-J. Flecainide and encainide are extremely powerful and are suitable for the treatment of reciprocating supraventricular paroxysmal tachycardia and of persistent reciprocating tachycardia, the prophylaxis of WPW atrial fibrillation including cases with a short anterograde refractory period of the anomalous pathway and the treatment of ventricular ectopic beats and ventricular tachycardia. Both drugs are probably effective for the treatment of atrial fibrillation. However, in the case of atrial flutter they are of little effect of sinus rhythm cardioversion; on the other hand they significantly prolong the duration of the A-A interval, with variable results on ventricular rate. Flecainide and encainide have 'parodoxical' arrhythmogenic effects, related to administration dosages, severity of the arrhythmia and seriousness of cardiopathy. Encainide shows peculiar pharmacokinetics due to hepatic oxidating metabolisation and to production of metabolites; among these the O-demethylencainide and the 3-methoxy-O-demethylencainide have an antiarrhythmic activity, which is probably more important than the encainide parent and is longer-lasting. There are 'extensive', 'poor' and 'non-metaboliser' subjects. This results in wide pharmacokinetic inter- and intraindividual variability which must be taken into account during clinical treatment.(ABSTRACT TRUNCATED AT 250 WORDS)
Intravenous Flecainide for Emergency Department Management of Acute Atrial Fibrillation
J Emerg Med 2018 Mar;54(3):320-327.PMID:29269083DOI:10.1016/j.jemermed.2017.11.016.
Background: Atrial fibrillation (AF) is the most commonly encountered dysrhythmia in the emergency department, and its prevalence is increasing. A substantial proportion of these patients have recent-onset AF (<48 h). The poor prognosis associated with AF is being increasingly recognized, and there is some evidence for better outcomes in younger patients with recent-onset AF when sinus rhythm is restored. Flecainide is recommended in the latest international guidelines for cardioversion of recent-onset AF, but its safety and efficacy relative to other recommended agents are unclear. Objective: Our aim was to clarify the Level 1 evidence for the use of i.v. Flecainide in acute AF. Methods: We performed a systematic review and meta-analysis of the literature. Medline, Ovid, Embase, and Cochrane Central databases were searched for relevant studies. Only randomized controlled trials (RCTs) of i.v. Flecainide for acute conversion of recent-onset AF were selected for meta-analysis. Results: Four hundred and three studies were screened, of which 11 RCTs were eligible for meta-analysis. Flecainide had high efficacy for cardioversion within 2 h (number needed to treat [NNT] = 1.8). Efficacy was superior to propafenone, amiodarone, procainamide, ibutilide, and sotalol (NNT = 4.3). There was no statistically significant difference in pro-dysrhythmia compared to these anti-dysrhythmics or placebo. Conclusions: Intravenous Flecainide cardioversion could be a safe and effective option for emergency physicians to restore sinus rhythm in selected patients with acute AF.