Sunday, September 24, 2023

Causes of Subtherapeutic INR despite Full-Dose Warfarin Administration

  • Hereditary 
    • Mutations of VKORC1 Gene → Warfarin resistance 
    • Duplication or multiplication of Cyt P450 enzyme genes (P450 CYP2D6 & CYP2A6)
    • ↑ metabolic clearance of Warfarin

  • Acquired 
    • Poor patient compliance 
    • High consumption of Vitamin K
    • Decreased absorption of Warfarin 
      • Gastroenteritis
      • Coeliac disease
      • Chronic pancreatitis
      • Short gut syndrome
    • Increased clearance of Warfarin 
      • Hypoalbuminemia → ↑ free fraction of Warfarin → ↑ clearance and ↓ plasma half-life
      • Hyperalbuminemia → Paradoxical effect by increased binding of Warfarin 
    • Hyperlipidemia 
      • ↑ Lipids → ↑ Vitamin K pool → Warfarin resistance 
    • Drugs decreasing the effect of Warfarin 
      • Azathioprine
      • Barbiturates 
      • Carbamazepine 
      • Cholestyramine
      • Corticosteroids 
      • Dicloxacillin & Nafcillin 
      • Estrogen preparations
      • Spironolactone → ↓ Plasma volume → ↑ Coagulation factor levels  
      • Griseofulvin 
      • Rifampicin 
      • Contraceptive pill  
      • Ritonavir
      • Saint John's wort
      • Sucralfate
    • Tobacco smoking 
      • Powerful inducer of P450 (CYP1A1 & CYP1A2)
      • Tobacco leaves are rich in Phylloquinone (vitamin K1)
      • Each gram of Tobacco → 50 μg Vitamin K1 (exceeds the amount found in food sources) 


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