Pharmacology/Part 10/10.1 Pharmacogenomics

10.1 Pharmacogenomics

Pharmacogenomics studies how genetic variations affect drug response, enabling personalized medicine through tailored drug selection and dosing based on individual genetic profiles.

CYP450 Polymorphisms

CYP2D6

  • Substrates: Codeine, tamoxifen, metoprolol, tricyclics
  • Poor metabolizers: No codeine analgesia (not converted to morphine)
  • Ultra-rapid: Codeine toxicity, tamoxifen inefficacy

CYP2C19

  • Substrates: Clopidogrel, PPIs, SSRIs
  • Poor metabolizers: Clopidogrel ineffective (prodrug); ↑ PPI efficacy
  • • Common in Asian populations

Clinical Applications

Warfarin Dosing

  • CYP2C9: Metabolism polymorphisms (↓ dose if slow metabolizer)
  • VKORC1: Target enzyme variations (↓ dose if sensitive variant)
  • • FDA-approved pharmacogenetic dosing algorithms

Thiopurine Methyltransferase (TPMT)

  • • Metabolizes azathioprine, 6-MP
  • Low activity: Severe myelosuppression
  • • FDA recommends testing before starting

HLA-B*5701 & Abacavir

  • Positive: High risk of hypersensitivity reaction
  • Mandatory screening before abacavir (HIV therapy)
  • • Prevents life-threatening reactions

G6PD Deficiency

  • Avoid: Primaquine, dapsone, nitrofurantoin, sulfonamides
  • • Risk of hemolytic anemia
  • • Common in Mediterranean, African, Asian populations