フレカイニド 化學(xué)特性,用途語(yǔ),生産方法
効能
抗不整脈薬, ナトリウムチャネル遮斷薬
説明
From the chemical point, flecainide is an analog of procainamide, to which a 2.2.2-trifluoroethoxyl
group was added at C2 and C3 of the benzene ring, and a diaminoethyl side
chain is ended in the piperidine ring.
化學(xué)的特性
White Crystalline Powder
使用
Flecainide, as with other local anesthetics, is used for naturally occurring ventricular arrhythmia.
定義
ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prev
nt and treat tachyarrhythmia (abnormal fast rhythm of the heart).
世界保健機(jī)関（WHO）
The membrane-stabilizing antiarrhythmic agent flecainide was
introduced into medicine in 1982. The decision to delete the indications for
patients with asymptomatic and less severe symptomatic ventricular arrhythmias
was taken on the basis of the results of a trial (CAST study) that showed a two-fold
increase in deaths in post-myocardiac patients taking flecainide compared with the
placebo group.
危険性
Human systemic effects.
臨床応用
Flecainide (Tambocor) is a fluorinated aromatic hydrocarbon
examined initially for its local anesthetic
action and subsequently found to have antiarrhythmic
effects. Flecainide inhibits the sodium channel, leading
to conduction slowing in all parts of the heart, but
most notably in the His-Purkinje system and ventricular
myocardium. It has relatively minor effects on repolarization.
Flecainide also inhibits abnormal automaticity.
Flecainide is effective in treating most types of atrial arrhythmias.
It is also used for life-threatening ventricular
arrhythmias. However, flecainide should be used with extreme
caution in any patient with structural heart disease.
Flecainide crosses the placenta, with fetal levels reaching
approximately 70% of maternal levels. In many centers,
it is the second-line drug after digoxin for therapy of fetal
arrhythmias. Because of the high incidence of proarrhythmia,
initiation of therapy or significant increases in
dosing should be performed only on inpatients.
副作用
Most adverse effects occur within a few days of initial
drug administration. The most frequently reported effects
are dizziness, light-headedness, faintness, unsteadiness,
visual disturbances, blurred vision (e.g., spots before
the eyes, difficulty in focusing), nausea, headache,
and dyspnea.
Worsening of heart failure and prolongation of the PR
and QRS intervals are likely to occur with flecainide, and
an increased risk of proarrhythmia has been reported.
薬物相互作用
In patients whose condition has been stabilized by flecainide,
the addition of cimetidine may reduce the rate
of flecainide’s hepatic metabolism, increasing the potential
for toxicity. Flecainide may increase digoxin concentrations
on concurrent administration.
予防処置
Flecainide is contraindicated in patients with preexisting
second- or third-degree heart block or with bundle
branch block unless a pacemaker is present to maintain
ventricular rhythm. It should not be used in patients
with cardiogenic shock.
フレカイニド 上流と下流の製品情報(bào)
原材料
ピペリジン-2-メタンアミン
Desiccant
ゲンチシン酸
2-ピコリルアミン
硫酸マグネシウム (無(wú)水)
塩酸
2,5-ビス(2,2,2-トリフルオロエトキシ)安息香酸
2,5-ビス(2,2,2-トリフルオロエトキシ)安息香酸2,2,2-トリフルオロエチル
2,5-ビス(2,2,2-トリフルオロエトキシ)安息香酸メチル
準(zhǔn)備製品