Effects of amiodarone, thyroid hormones and CYP2C9 and VKORC1 polymorphisms on warfarin metabolism: a review of the literature

Endocr Pract. 2013 Nov-Dec;19(6):1043-9. doi: 10.4158/EP13093.RA.

Abstract

Objective: To review the literature regarding the interaction among amiodarone therapy, thyroid hormone levels, and warfarin metabolism.

Methods: A 73-year-old male with type 2 after describing an unusual case of amiodarone-induced thyrotoxicosis (AIT) who experienced a severe rise in international normalized ratio (INR) values after initiating warfarin therapy due to an unusual combination of excessive thyroid hormones, amiodarone therapy, and a genetic abnormality affecting warfarin metabolism.

Results: Genetic analysis revealed that the patient was CYP2C9*2 wild-type, CYP2C9*3/*3 homozygous mutant, and VKORC1*3/*3 homozygous mutant. A review of the literature revealed that both mutations can independently affect warfarin metabolism. In addition, amiodarone therapy and the presence of thyrotoxicosis per se can affect warfarin metabolism and reduce the dose needed to maintain INR in the therapeutic range. The association of the 2 genetic polymorphisms in a patient with AIT is extremely rare and strongly impairs warfarin metabolism, exposing the patient to a high risk of overtreatment.

Conclusions: In patients with AIT, warfarin therapy should be gradually introduced, starting with a very low dose, because of the significant risk of warfarin overtreatment. Whether the genetic analysis of CYP2C9 and VKORC1 polymorphisms should be routinely performed in AIT patients remains conjectural.

Publication types

  • Case Reports
  • Review

MeSH terms

  • Aged
  • Amiodarone / adverse effects*
  • Anti-Arrhythmia Agents / adverse effects*
  • Anticoagulants / metabolism*
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Cytochrome P-450 CYP2C9
  • DNA / genetics
  • Drug Interactions
  • Hemorrhage / chemically induced
  • Hemorrhage / epidemiology
  • Humans
  • International Normalized Ratio
  • Male
  • Polymorphism, Genetic / genetics
  • Risk
  • Thyroid Hormones / adverse effects*
  • Thyroid Hormones / blood
  • Thyroidectomy
  • Thyrotoxicosis / chemically induced
  • Thyrotoxicosis / metabolism
  • Thyrotoxicosis / surgery
  • Vitamin K Epoxide Reductases / genetics*
  • Warfarin / metabolism*

Substances

  • Anti-Arrhythmia Agents
  • Anticoagulants
  • Thyroid Hormones
  • Warfarin
  • DNA
  • CYP2C9 protein, human
  • Cytochrome P-450 CYP2C9
  • Aryl Hydrocarbon Hydroxylases
  • VKORC1 protein, human
  • Vitamin K Epoxide Reductases
  • Amiodarone