胺碘酮及其活性代谢物的血浓度与临床效应相关性评价  

Relationship between plasma levels of amiodarone/its active metabolite desethylamiodarone and clinical effects

作　　者：刘学红[1] 郭瑞臣[2] 李丕宝[3] 宿连玲 史明[1] 肖少华[1] 

机构地区：[1]山东省交通医院药剂科,济南250031 [2]山东大学齐鲁医院临床药理研究所,济南250012 [3]山东省交通医院内科,济南250031

出　　处：《中国临床药学杂志》2006年第4期240-242,共3页Chinese Journal of Clinical Pharmacy

基　　金：山东省交通厅科技计划项目(200324A22)

摘　　要：目的探讨胺碘酮（AM）治疗心律失常的临床疗效与AM及其活性代谢物单N-去乙基胺碘酮（MDEA）血浓度间的相关性。方法住院心律失常患者37例，给予负荷量AM（600mg·d^-1）达临床疗效后渐减至最小维持量（25—100）mg·d^-1治疗8wk。门诊心律失常患者36例，长期服用AM（≥3mo），维持量50—200mg·d^-1。HPLC法监测AM和MDEA血浓度。结果AM、MDEA、AM＋MDEA和AM／MDEA值与临床效应相关系数分别为0．8123（P〉0．05）、0．7033（P〉0．05）、0．9079（P〈0．05）、0．4969（P〉0．05）。AM＋MDEA有效、无效和中毒浓度值分别为（1．2860±0．7459）、（0．6364±0．2086）和（2．3130±1．6824）mg·L^-1。结论AM最小维持量为25．100mg·d^-1；AM＋MDEA血浓度值可作为评价AM疗效，制定、修饰、调整AM治疗方案的参考指标。A/M To study the relationship between plasma level of amiodarone（AM）/desethylamiodarone （MDEA） and clinical effects for cardiac arrhythmia patients when treated with AM after a given dose at a period of time. METHODS The patients were divided into 2 groups. In groupⅠ, 37 hospitalized patients took a loading dose （600 mg·d^-1） of AM and eventually reduced to a minimum maintaining dose of （25 - 100 mg·d^-1） for 8wk, and 36 outpatients treated with AM for more than 3 months at a maintaining dose of （50 - 200）mg·d^-1 in group Ⅱ . The plasma concentrations of AM and MDEA were determined and the data were statistically analysed. RESULTS The total effective, ineffective and poisoning plasma levels of AM plus MDEA were（1.286 0±0.745 9）,（0.636 4 ± 0.208 6） and （2.313 0 ± 1.682 4）mg·L^-1, respectively. The coefficient of between AM, MDEA, AM ＋ MDEA, AM/MDEA and clinical effects were 0. 812 3 （P〉0.05）, 0.7033（P〉0.05）, 0.9079（P〈0.05）, 0.4969（P〉0.05） respectively. CONCLUSION AM is effective and safe at maintaining dose of 25 - 100 mg·d^- 1 in cardiac arrhythmia patients. The plasma concentrations of AM plus MDEA, rather than AM, MDEA or AM/MDEA, can be used as a index to evaluate clinical effects and to formulate, modify and adjust dosage regimen of AM therapy.

关 键 词：胺碘酮 单N-去乙基胺碘酮 心律失常 血浓度 

分 类 号：R96[医药卫生—药理学]