Nitsch J, Lüderitz B
Dtsch Med Wochenschr. 1986 Aug 15;111(33):1241-4. doi: 10.1055/s-2008-1068613.
In eleven patients serum levels of amiodarone and its desethyl metabolite were determined after a single dose of 400 mg amiodarone given with and without subsequent administration of colestyramine. In addition, the elimination half-life was measured in three patients after discontinuation of long-term amiodarone therapy. Mean serum levels of amiodarone at 7 1/2 hours after dosing (n = 11) were 0.42 +/- 0.11 micrograms/ml without colestyramine and 0.21 +/- 0.14 micrograms/ml with colestyramine (P less than 0.01). Elimination half-life after discontinuing long-term amiodarone therapy (n = 3) was 23 1/2, 29 and 32 days, respectively (half-life in eight controls: 35-58 days). The results indicate that colestyramine significantly reduces the enterohepatic circulation of amiodarone. Therefore, colestyramine should be capable of accelerating the regression of dose-dependent side-effects of amiodarone by enhancing its elimination.
对11名患者在单次服用400毫克胺碘酮（无论后续是否给予考来烯胺）后测定了胺碘酮及其去乙基代谢物的血清水平。此外，在3名患者停用长期胺碘酮治疗后测量了消除半衰期。给药后7.5小时时胺碘酮的平均血清水平（n = 11），未服用考来烯胺时为0.42±0.11微克/毫升，服用考来烯胺时为0.21±0.14微克/毫升（P<0.01）。停用长期胺碘酮治疗后（n = 3）的消除半衰期分别为23.5天、29天和32天（8名对照者的半衰期为35 - 58天）。结果表明，考来烯胺可显著减少胺碘酮的肠肝循环。因此，考来烯胺应该能够通过增强胺碘酮的消除来加速其剂量依赖性副作用的消退。
