Sloskey G E
Clin Pharm. 1983 Jul-Aug;2(4):330-40.
The chemistry, pharmacology, pharmacokinetics, clinical use and efficacy, adverse effects, and dosage of amiodarone, an investigational antiarrhythmic agent, are reviewed. Amiodarone hydrochloride (L3428, Cordarone; Labaz Laboratories) is a benzofuran derivative and contains iodine. Amiodarone is a noncompetitive antagonist of alpha- and beta-adrenergic receptors. It is a type III antiarrhythmic agent and causes prolongation of the action potential of atrial and ventricular tissue. The drug is incompletely and variably absorbed following oral administration; bioavailability ranges from 22 to 86%. Peak serum concentrations occur 2-10 hours after an oral dose. Amiodarone has a large volume of distribution and is widely distributed in body tissues. It is metabolized by the liver; half-life following a single dose is 5-20 hours, but terminal half-lives of 14-58 days have been found following discontinuation of long-term therapy. Amiodarone has been effective in treating supraventricular tachycardias in patients with Wolff-Parkinson-White syndrome whose arrhythmias are refractory to other drugs. Preliminary data suggest a potential use for amiodarone in treating atrial fibrillation/flutter and bradycardia-tachycardia syndrome. The drug has also been tested in patients with ventricular arrhythmias with promising results. Amiodarone has many side effects, some of them serious. The cardiovascular, pulmonary, neurologic, and hepatic systems may be affected; the drug also has deleterious effects on the eyes, thyroid gland, and skin. The usual oral adult dose of amiodarone hydrochloride is 600 mg daily for seven days followed by maintenance doses of 200-400 mg daily during initial therapy. Intravenous initial doses of amiodarone hydrochloride 5 or 10 mg/kg via a central line have been used; these are often followed by infusions of 10 mg/kg/day for three to five days. Amiodarone is an effective antiarrhythmic agent whose use is limited by numerous and sometimes serious side effects. Until more clinical data are available, its use should be restricted to treatment of serious arrhythmias refractory to other agents.
对一种研究中的抗心律失常药物胺碘酮的化学性质、药理学、药代动力学、临床应用与疗效、不良反应及剂量进行了综述。盐酸胺碘酮（L3428，可达龙；拉巴兹实验室）是一种苯并呋喃衍生物，含有碘。胺碘酮是α和β肾上腺素能受体的非竞争性拮抗剂。它是Ⅲ类抗心律失常药物，可使心房和心室组织的动作电位延长。口服给药后，该药物吸收不完全且存在个体差异；生物利用度范围为22%至86%。口服一剂后，血清峰值浓度在2至10小时出现。胺碘酮分布容积大，广泛分布于身体组织中。它在肝脏代谢；单次给药后的半衰期为5至20小时，但长期治疗停药后发现终末半衰期为14至58天。胺碘酮对预激综合征患者的室上性心动过速有效，这些患者的心律失常对其他药物难治。初步数据表明胺碘酮在治疗心房颤动/扑动和心动过缓-心动过速综合征方面有潜在用途。该药物也已在室性心律失常患者中进行测试，结果令人鼓舞。胺碘酮有许多副作用，其中一些很严重。心血管、肺、神经和肝脏系统可能受到影响；该药物对眼睛、甲状腺和皮肤也有有害影响。成人盐酸胺碘酮的常用口服剂量为每日600毫克，连用7天，初始治疗期间维持剂量为每日200至400毫克。已采用通过中心静脉给予盐酸胺碘酮5或10毫克/千克的静脉初始剂量；随后通常以10毫克/千克/天的速度输注3至5天。胺碘酮是一种有效的抗心律失常药物，但其使用受到众多且有时严重的副作用限制。在获得更多临床数据之前，其使用应限于治疗对其他药物难治的严重心律失常。
