モリシジン 化学特性,用途語,生産方法
効能
抗不整脈薬, 心抑制薬, ナトリウムチャネル遮断薬
使用
Moricizine, is Phenothiazine (P318040) derivative, which It was used as an Antiarrhythmic agent. It is also shown that moracizine is effective in suppressing premature ventricular contractions, couplets, and nonsustained ventricular tachycardia.
定義
ChEBI: A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group.
一般的な説明
Moricizine, ethyl 10-(3-morpholinopropionyl)phenothiazine-2-carbamate (Ethmozine), is aphenothiazine derivative used for the treatment of malignantventricular arrhythmias. It is categorized as a class ICantiarrhythmic agent, blocking the Na
+ channel with 1:1stochiometry. The drug has higher affinity for the inactivatedstate than the activated or resting states. It appearsto bind to a site on the external side of the Na channelmembrane. It has been used to suppress life-threateningventricular arrhythmias.
臨床応用
Moricizine (Ethmozine) is an antiarrhythmic used to
treat documented life-threatening arrhythmias.
Moricizine is indicated for the treatment of documented
ventricular arrhythmias, particularly sustained ventricular
tachycardia. Moricizine was evaluated in the CAST
II clinical trial for the prevention of postinfarction ventricular
premature complexes. It was ineffective and
found to be proarrhythmic. Patients in the moricizine
arm of the trial exhibited a greater incidence of sudden
cardiac death than did controls.
副作用
The principal adverse gastrointestinal effect of moricizine
is nausea (7%). Abdominal discomfort has also
been reported. Dizziness (11%) is the most frequently
reported CNS-related adverse effect. Such reactions
increase in frequency with prolonged drug administration.
As with other antiarrhythmic drugs, moricizine has
proarrhythmic activity, which may manifest as new ventricular
ectopic beats or a worsening of preexisting ventricular
arrhythmias. These effects are most common in
patients with depressed left ventricular function and a
history of congestive heart failure. Cardiovascular effects requiring drug withdrawal include conduction defects,
sinus pauses, junctional rhythm, and A-V block.
薬物相互作用
Clinically significant interactions with moricizine do not
appear to exist.
予防処置
Patients with preexisting second- or third-degree A-V
block, cardiogenic shock, or drug hypersensitivity should
not be treated with moricizine.
モリシジン 上流と下流の製品情報
原材料
準備製品