Markos J, Veronese M E, Nicholson M R, McLean S, Shevland J E
Am J Cardiol. 1985 Jul 1;56(1):89-92. doi: 10.1016/0002-9149(85)90572-7.
Amiodarone therapy is difficult to monitor because of the poor correlation between plasma amiodarone levels and clinical efficacy or toxicity. Monitoring tissue levels may give a better measure of effectiveness, but tissue levels cannot be easily measured. The iodine-containing amiodarone and its major metabolite, desethylamiodarone (DA), are highly tissue-bound, and it has been shown that computerized tomographic (CT) scanning of the abdomen will detect drug deposition in the liver. Ten patients receiving chronic amiodarone therapy were studied by abdominal CT scanning. Liver CT density was increased in 6; 68 to 94 CT units (normal 50 to 65) and liver/spleen relative CT density increased in 5; 1.4 to 2.0 (normal 1.0 to 1.3). Estimates of liver drug levels (based on a calibration curve with inorganic iodide) gave values of up to 3 g of amiodarone and DA per kilogram weight of liver. Absolute and relative liver CT density correlated significantly with plasma levels of DA (r = 0.65, p less than 0.05), but not with amiodarone (r = 0.55, p less than 0.1). No significant correlation was found with QTc intervals. This indirect estimate of liver deposition of amiodarone and DA may prove useful in guiding antiarrhythmic therapy.
胺碘酮治疗难以监测，因为血浆胺碘酮水平与临床疗效或毒性之间的相关性较差。监测组织水平可能能更好地衡量疗效，但组织水平不易测量。含碘的胺碘酮及其主要代谢产物去乙基胺碘酮（DA）与组织结合紧密，并且已经表明腹部计算机断层扫描（CT）能检测到药物在肝脏中的沉积。对10例接受慢性胺碘酮治疗的患者进行了腹部CT扫描研究。6例患者肝脏CT密度增加；为68至94 CT单位（正常为50至65），5例患者肝脏/脾脏相对CT密度增加；为1.4至2.0（正常为1.0至1.3）。肝脏药物水平估计值（基于与无机碘化物的校准曲线）显示每千克肝脏重量中胺碘酮和DA的含量高达3 g。肝脏绝对和相对CT密度与血浆DA水平显著相关（r = 0.65，p < 0.05），但与胺碘酮不相关（r = 0.55，p < 0.1）。与QTc间期未发现显著相关性。这种对胺碘酮和DA在肝脏中沉积的间接估计可能对指导抗心律失常治疗有用。
