Punnam Sujeeth R, Goyal Sandeep K, Kotaru Veera P K, Pachika Ajay R, Abela George S, Thakur Ranjan K
Sparrow Health System, Division of Cardiology, Michigan State University, East Lansing, MI, USA.
Cardiovasc Hematol Disord Drug Targets. 2010 Mar;10(1):73-81. doi: 10.2174/187152910790780032.
Amiodarone, an iodinated benzofuran derivative, introduced in 1960's as an anti-anginal agent, emerged as a potent anti-arrhythmic agent by 1970's and is currently one of the most commonly prescribed drugs in US for ventricular and atrial arrhythmias. Although amiodarone is considered a class III anti-arrhythmic agent, it also has class I, II, IV actions, making it a unique and effective anti-arrhythmic agent. Because of its minimal negative inotropic activity and very low rate of pro-arrhythmia, it is considered safe in treating arrhythmias in patients with Coronary Artery Disease and Left ventricular systolic dysfunction. Despite these advantages, long term oral therapy with amiodarone is limited by side effect profile involving various organs like thyroid, lung, heart, liver, skin etc. Though the side effects can be decreased significantly by keeping the maintenance dose at 200 to 300 mg/day, patients on amiodarone should be followed closely. Amiodarone interacts with medications such as Warfarin, Digoxin, Macrolides, Floroquinolones etc., which share Cytochrome P450 metabolic pathway. Hence reducing their doses prior to starting amiodarone is recommended. Amiodarone, a category D drug, is contraindicated in pregnant and breast feeding women. This review discusses the pharmacokinetics of amiodarone, its evolving clinical indications, management of toxicity and drug interactions.
胺碘酮是一种碘化苯并呋喃衍生物，于20世纪60年代作为抗心绞痛药物引入，到20世纪70年代成为一种强效抗心律失常药物，目前是美国治疗室性和房性心律失常最常用的药物之一。尽管胺碘酮被认为是Ⅲ类抗心律失常药物，但它也具有Ⅰ类、Ⅱ类、Ⅳ类作用，使其成为一种独特而有效的抗心律失常药物。由于其负性肌力作用极小且促心律失常发生率极低，它被认为在治疗冠状动脉疾病和左心室收缩功能障碍患者的心律失常时是安全的。尽管有这些优点，但胺碘酮的长期口服治疗受到涉及甲状腺、肺、心脏、肝脏、皮肤等多个器官的副作用的限制。虽然将维持剂量保持在200至300毫克/天可显著降低副作用，但服用胺碘酮的患者仍应密切随访。胺碘酮与华法林、地高辛、大环内酯类、氟喹诺酮类等通过细胞色素P450代谢途径的药物相互作用。因此，建议在开始使用胺碘酮之前降低这些药物的剂量。胺碘酮是D类药物，孕妇和哺乳期妇女禁用。本综述讨论了胺碘酮的药代动力学、其不断演变的临床适应症、毒性管理和药物相互作用。
