Keefe D L
Am J Cardiol. 1984 Aug 13;54(4):18B-21B. doi: 10.1016/0002-9149(84)90819-1.
Lorcainide is a new type 1 antiarrhythmic drug that is well absorbed orally, with bioavailability increasing with both dose and continued administration. It is metabolized through the liver, and patients with significant liver disease will require dosage reduction. The drug has an active metabolite, norlorcainide, whose activity is similar to that of lorcainide but whose half-life is 26 hours instead of 8 for the parent compound. The levels of this metabolite are nearly twice those of lorcainide at steady state. The long half-life of the metabolite and the changing bioavailability of lorcainide require that a given dose be administered for 1 week for the maximum effect to be demonstrated.
劳卡尼是一种新型的Ⅰ类抗心律失常药物，口服吸收良好，生物利用度随剂量增加和持续给药而提高。它通过肝脏代谢，患有严重肝脏疾病的患者需要减少剂量。该药物有一种活性代谢物，去甲劳卡尼，其活性与劳卡尼相似，但其半衰期为26小时，而母体化合物的半衰期为8小时。在稳态时，这种代谢物的水平几乎是劳卡尼的两倍。代谢物的长半衰期和劳卡尼不断变化的生物利用度要求给予一定剂量的药物1周，以显示出最大效果。
