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超治疗窗瑞维伐沙班浓度:胺碘酮停药后持续的药物-药物相互作用。

Supratheraputic rivaroxaban levels: A persistent drug-drug interaction after discontinuation of amiodarone.

机构信息

Clinical Pharmacology Unit, Zealand University Hospital, Roskilde, Denmark.

Department of Cardiology, Zealand University Hospital, Roskilde, Denmark.

出版信息

Basic Clin Pharmacol Toxicol. 2020 Oct;127(4):351-353. doi: 10.1111/bcpt.13419. Epub 2020 May 4.

Abstract

We report the case of an 88-year old woman referred for evaluation of increased INR. Surprisingly supratherapeutic levels of rivaroxaban was detected. Upon scrutiny of the patient's medical history, a drug-drug interaction between amiodarone and rivaroxaban persisting 3 weeks after cessation of amiodaron remains the prime suspect causing the clinical picture. Both INR and rivaroxaban levels returned to normal within 3 days of cessation of rivaroxaban. The case highlights that rivaroxaban, although highly variably, does affect INR. Furthermore, it highlights that the potential for DDIs involving amiodarone may persists for weeks or months after discontinuation. Amiodarone is predicted to increase rivaroxaban exposure, through inhibition of rivaroxaban elimination via CYP3A4 and P-gp. Elderly patients and patients with declining renal function are especially at risk of increased rivaroxaban exposure when a DDI with amiodarone occurs.

摘要

我们报告了一例 88 岁女性因 INR 升高而就诊的病例。令人惊讶的是,检测到 rivaroxaban 的治疗剂量以上水平。仔细审查患者的病史后,胺碘酮和 rivaroxaban 之间的药物-药物相互作用在停用胺碘酮后持续 3 周,仍然是导致这种临床情况的主要原因。停止使用 rivaroxaban 3 天后,INR 和 rivaroxaban 水平均恢复正常。该病例强调了 rivaroxaban 虽然变化很大,但确实会影响 INR。此外,它还强调了涉及胺碘酮的药物相互作用在停药后可能会持续数周或数月。胺碘酮通过抑制 CYP3A4 和 P-gp 来消除 rivaroxaban,预计会增加 rivaroxaban 的暴露。当与胺碘酮发生药物相互作用时,老年患者和肾功能下降的患者尤其面临增加 rivaroxaban 暴露的风险。

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