Barbieri E, Conti F, Zampieri P, Trevi G P, Zardini P, d'Aranno V, Latini R
J Am Coll Cardiol. 1986 Jul;8(1):210-3. doi: 10.1016/s0735-1097(86)80114-0.
The time to onset of action of amiodarone is often long in patients treated for arrhythmias; one reason might be a slow entry of the drug into the target organ, the heart. Amiodarone and desethylamiodarone, its active metabolite, were measured in the plasma, atrial tissue and pericardial fat of patients undergoing cardiac surgery. Two groups were studied: patients treated with amiodarone for less than 28 days (short-term group) and those treated for 28 days or more (long-term group). Plasma levels of amiodarone in the two groups were not different, whereas levels of desethylamiodarone were significantly higher in the long-term group. Average concentrations of amiodarone in the atrium were higher with longer treatment periods (30.2 +/- 5.6 versus 13.2 +/- 2.5 micrograms/g wet weight of tissue); the same was true for desethylamiodarone (40.3 +/- 7.7 versus 15.7 +/- 3.7 micrograms/g). Amiodarone concentrations in fat were also significantly higher in the long-term than in the short-term group. Atrium/plasma concentration ratios of desethylamiodarone were higher than those of amiodarone, whereas fat plasma concentration ratios of desethylamiodarone were lower. In conclusion, the equilibration of amiodarone and desethylamiodarone concentrations between myocardium and plasma appears to occur slowly in patients undergoing long-term treatment with amiodarone.(ABSTRACT TRUNCATED AT 250 WORDS)
在接受心律失常治疗的患者中，胺碘酮起效时间通常较长；一个原因可能是药物进入靶器官——心脏的速度较慢。对接受心脏手术患者的血浆、心房组织和心包脂肪中的胺碘酮及其活性代谢产物去乙基胺碘酮进行了测定。研究了两组患者：接受胺碘酮治疗少于28天的患者（短期组）和接受治疗28天或更长时间的患者（长期组）。两组患者的胺碘酮血浆水平无差异，而去乙基胺碘酮水平在长期组中显著更高。随着治疗时间延长，心房中胺碘酮的平均浓度更高（分别为30.2±5.6与13.2±2.5微克/克组织湿重）；去乙基胺碘酮情况相同（分别为40.3±7.7与15.7±3.7微克/克）。长期组脂肪中的胺碘酮浓度也显著高于短期组。去乙基胺碘酮的心房/血浆浓度比高于胺碘酮，而去乙基胺碘酮的脂肪/血浆浓度比更低。总之，在接受胺碘酮长期治疗的患者中，心肌与血浆之间胺碘酮和去乙基胺碘酮浓度的平衡似乎出现得较慢。（摘要截短于250字）
