胺碘酮的临床药物动力学。
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Latini R, Tognoni G,凯特
胺碘酮的临床药物动力学。
Pharmacokinet。1984; 3 - 4月9日(2):136 - 56。doi: 10.2165 / 00003088-198409020-00002。
- PubMed ID
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6370540 (在PubMed]
- 文摘
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胺碘酮是一个认可的碘化香豆酮衍生物抗心律失常的活动的人。到目前为止,其药代动力学行为没有得到令人满意的特征。特定的和敏感的高压液相色谱方法已经成为最近只有这部分解释了稀缺药物的药代动力学数据。现有证据表明,吸收后口服胺碘酮是不稳定和不可预测的;口服生物利用度从22 - 86%不等。该药物主要由代谢消除;不到1%的剂量不变排出尿液。胆汁排泄可能有作用的整体消除药物。Desethyl-amiodarone是唯一代谢物积极接受用胺碘酮治疗的患者血浆中标识;没有数据可在其可能的药理作用。 Since it is a highly lipophilic drug, amiodarone is extensively distributed into tissues. Adipose tissue and skeletal muscle accumulate large amounts of the drug during long term treatment. Myocardium/plasma ratios of amiodarone are high both in man and in animals; peak concentrations in the myocardium are reached within half an hour after administration of an intravenous bolus to dogs. Placental transfer of amiodarone has been demonstrated in humans, while its blood profile is not modified by dialysis treatment. In vitro protein binding of amiodarone has been reported to be 96.3 +/- 0.6%. The plasma half-life of amiodarone after single-dose administration has been reported to be in the range of 3.2 to 79.7 hours. However, after withdrawal of long term amiodarone treatment the half-life is as long as 100 days. Total body clearance ranges from 0.10 to 0.77 L/min after single-dose intravenous administration, and the apparent volume of distribution ranges between 0.9 and 148 L/kg. Amiodarone disposition kinetics in patients with cardiac arrhythmias are not different from those in healthy volunteers. However, the possible effects of liver and cardiac failure on the drug's kinetics have not been studied. Amiodarone potentiates the anticoagulant effect of warfarin, probably by inhibition of its metabolism. Increases of steady-state concentrations of digoxin, together with the appearance of signs of digitalis toxicity, have been reported when amiodarone was given to patients receiving long term treatment with digoxin. Amiodarone has also been shown to interact with other antiarrhythmic agents such as quinidine and procainamide. The time of onset of action of amiodarone after a single intravenous dose ranges between 1 and 30 minutes and its duration of effect between 1 and 3 hours.(ABSTRACT TRUNCATED AT 400 WORDS)
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