Canada A T, Lesko L J, Haffajee C I, Johnson B, Asdourian G K
Drug Intell Clin Pharm. 1983 Feb;17(2):100-4. doi: 10.1177/106002808301700203.
Amiodarone, although widely studied in Europe, is a recent addition to the investigational antiarrhythmics being used in the U.S. Pharmacologically, its primary cardiac effects are to increase coronary artery blood flow, increase the effective refractory period, and produce an atropine-resistant bradycardia. Amiodarone is incompletely (approximately 50 percent) and slowly (peak serum concentration approximately 6 h) absorbed. With chronic administration, it deposits both in adipose tissue and in organs with high blood perfusion. It has an apparent elimination half-life of 15-45 days, which presents unique dosing problems. The apparent therapeutic range is 0.6-3 microgram/ml. Amiodarone is 85-95 percent effective in the treatment of atrial tachyarrhythmias and 70-80 percent effective in ventricular tachyarrhythmias. It appears to be of particular value in chronic atrial fibrillation/flutter because it may be able to maintain sinus rhythm after cardioversion. Side effects, although uncommon, may prevent the drug from becoming a standard of therapy. Drug interactions, particularly with warfarin and digoxin, as well as pulmonary fibrosis are of concern.
胺碘酮尽管在欧洲已得到广泛研究,但在美国它是最近才被用于抗心律失常研究的药物。从药理学角度来看,它对心脏的主要作用是增加冠状动脉血流量、延长有效不应期,并产生对阿托品不敏感的心动过缓。胺碘酮吸收不完全(约50%)且缓慢(血清峰值浓度约6小时)。长期给药时,它会沉积在脂肪组织和血液灌注丰富的器官中。其表观消除半衰期为15 - 45天,这带来了独特的给药问题。表观治疗范围是0.6 - 3微克/毫升。胺碘酮治疗房性快速心律失常的有效率为85 - 95%,治疗室性快速心律失常的有效率为70 - 80%。在慢性心房颤动/扑动中,它似乎具有特殊价值,因为它可能能够在心脏复律后维持窦性心律。副作用虽然不常见,但可能会阻碍该药物成为治疗标准。药物相互作用,尤其是与华法林和地高辛的相互作用,以及肺纤维化令人担忧。