Warfarin dose requirement in patients having severe thrombosis or thrombophilia

Br J Clin Pharmacol. 2019 Aug;85(8):1684-1691. doi: 10.1111/bcp.13948. Epub 2019 Jun 17.

Abstract

Aims: Warfarin dose requirement varies significantly. We compared the clinically established doses based on international normalized ratio (INR) among patients with severe thrombosis and/or thrombophilia with estimates from genetic dosing algorithms.

Methods: Fifty patients with severe thrombosis and/or thrombophilia requiring permanent anticoagulation, referred to the Helsinki University Hospital Coagulation Center, were screened for thrombophilias and genotyped for CYP2C9*2 (c.430C>T, rs1799853), CYP2C9*3 (c.1075A>C, rs1057910) and VKORC1 c.-1639G>A (rs9923231) variants. The warfarin maintenance doses (target INR 2.0-3.0 in 94%, 2.5-3.5 in 6%) were estimated by the Gage and the International Warfarin Pharmacogenetics Consortium (IWPC) algorithms. The individual warfarin maintenance dose was tailored, supplementing estimates with comprehensive clinical evaluation and INR data.

Results: Mean patient age was 47 years (range 20-76), and BMI 27 (SD 6), 68% being women. Forty-six (92%) had previous venous or arterial thrombosis, and 26 (52%) had a thrombophilia, with 22% having concurrent aspirin. A total of 40% carried the CYP2C9*2 or *3 allele and 54% carried the VKORC1-1639A allele. The daily mean maintenance dose of warfarin estimated by the Gage algorithm was 5.4 mg (95% CI 4.9-5.9 mg), and by the IWPC algorithm was 5.2 mg (95% CI 4.7-5.7 mg). The daily warfarin maintenance dose after clinical visits and follow-up was higher than the estimates, mean 6.9 mg (95% CI 5.6-8.2 mg, P < 0.006), with highest dose in patients having multiple thrombophilic factors (P < 0.03).

Conclusions: In severe thrombosis and/or thrombophilia, variation in thrombin generation and pharmacodynamics influences warfarin response. Pharmacogenetic dosing algorithms seem to underestimate dose requirement.

Keywords: CYP2C9; VKORC1; dosing algorithm; thrombophilia; thrombosis; warfarin.

MeSH terms

  • Adult
  • Aged
  • Algorithms
  • Alleles
  • Anticoagulants / administration & dosage*
  • Anticoagulants / pharmacokinetics
  • Biological Variation, Population / genetics*
  • Blood Coagulation / drug effects
  • Blood Coagulation / genetics
  • Cytochrome P-450 CYP2C9 / genetics
  • Cytochrome P-450 CYP2C9 / metabolism
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • International Normalized Ratio
  • Male
  • Middle Aged
  • Polymorphism, Genetic
  • Retrospective Studies
  • Severity of Illness Index
  • Thrombin / analysis
  • Thrombin / metabolism
  • Thrombophilia / blood
  • Thrombophilia / diagnosis
  • Thrombophilia / drug therapy*
  • Thrombophilia / genetics
  • Thrombosis / blood
  • Thrombosis / diagnosis
  • Thrombosis / drug therapy*
  • Thrombosis / genetics
  • Vitamin K Epoxide Reductases / antagonists & inhibitors
  • Vitamin K Epoxide Reductases / genetics
  • Warfarin / administration & dosage*
  • Warfarin / pharmacokinetics
  • Young Adult

Substances

  • Anticoagulants
  • Warfarin
  • CYP2C9 protein, human
  • Cytochrome P-450 CYP2C9
  • VKORC1 protein, human
  • Vitamin K Epoxide Reductases
  • Thrombin