プロパフェノン

用途ナトリウムチャネル抑制薬（Ⅰc群）抗不整脈薬

使用Cardiac depressant (anti-arrhythmic).

一般的な説明Propafenone, 2-[2＇-hydroxy-3-(propylamino)propoxy]-3-phenylpropiophenone (Rythmol), a classIC antiarrhythmic drug, contains a chiral center and is marketedas the racemic mixture. Therapy with the racemicmixture of propafenone produces effects that can be attributedto both (S) and (R) enantiomers. Although (R) and (S)enantiomers exert similarNa+channel–blocking effects, the(S) enantiomer also produces aβ-adrenergic blockade. As aresult, the (S) enantiomer is reported to be 40-fold morepotent than the (R) enantiomer as an antiarrhythmic agent.The enantiomers also display stereoselective dispositioncharacteristics. The (R) enantiomer is cleared more quickly.Hepatic metabolism is polymorphic and determined genetically.Ten percent of Caucasians have a reduced capacity tohydroxylate the drug to form 5-hydroxypropafenone. Thispolymorphic metabolism accounts for the interindividualvariability in the relationships between dose and concentrationand, thus, variability in the pharmacodynamic effects ofthe drug. The 5-hydroxy metabolites of both enantiomersare as potent as the parent compound in blocking Na+channels.Propafenone also depresses the slow inward current ofCa2+ions.

定義ChEBI: An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydroch oride salt in the management of supraventricular and ventricular arrhythmias.