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Does amiodarone impact on apixaban levels?

Nov 11，2024

Yes. Apixaban and amiodarone are drugs used for non-valvular atrial fibrillation (NVAF) in routine practice. Based on its pharmacokinetic data, amiodarone is a substrate of CYP3A4 and CYP2C8. Likewise, amiodarone is an inhibitor of CYP3A4 and P-gp. CYP3A4 is an important metabolite of apixaban; approximately 20-25% of apixaban is used as a substrate of P-gp. Therefore, the combination of amiodarone with apixaban may affect plasma levels of apixaban and increase the risk of bleeding.

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In a prospective, observational, single-center study comparing apixaban monotherapy with apixaban plus amiodarone for the treatment of NVAF, amiodarone may increase the peak and trough plasma levels of apixaban. The combination was generally well tolerated. However, to ensure safety, it is necessary to carefully observe bleeding symptoms in individual cases.

In addition, many factors affect the plasma level of apixaban, such as age, weight, renal function, and potential drug interactions (especially azole antifungal drugs). Therefore, it is recommended to adjust the dose of apixaban in patients with NVAF according to the following factors: age ≥ 80 years, weight ≥ 60 kg, and SCr ≥ 1.5 mg/dL. Patients who meet the above two criteria can reduce the dose of apixaban (2.5 mg twice daily). Approximately 27% of apixaban is excreted through the renal system. Many studies have reported that renal insufficiency can increase the plasma level of apixaban and the AUC of apixaban. In the latest study, it was also shown that the difference in ALT between apixaban combined with amiodarone therapy and apixaban monotherapy was statistically significant. Similarly, mild and moderate hepatic impairment (Child-Pugh A and B) did not significantly alter apixaban exposure, but apixaban is contraindicated in patients with Child-Pugh class C.

References:

[1] SUTEE LIMCHAROEN. Does amiodarone impact on apixaban levels? The effect of amiodarone on apixaban level among Thai patients with non-valvular Atrial Fibrillation.[J]. PLoS ONE, 2024. DOI:10.1371/journal.pone.0295511.

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