Pharmcogenetics Flashcards
The most well-documented examples of differences in drug effects are due to what? What branch is now starting to be heavily researched?
- Metabolism- liver enzymes
2. pharmocodynamic- mechanism of action
Phase I enzymes are associated with what? Phase II?
- CYP-oxidation, hydrolysis, reduction
2. Conjugating enzymes
What variant number is the most clinically important UGT variant?
28
Ultra rapid metabolizers with usually gene multiplication are usually associated with what enzyme?
CYP2D6
The extensive metabolizer is characterized as what?
Normal activity, two copies of normal gene
The intermediate metabolizer is characterized as what?
– Roughly half-normal enzyme activity– Usually one copy of low activity active gene
The poor metabolizer is characterized as what/
– Little or no enzyme activity– Two copies of low activity gene
Wat are the 4 most important CYP enzymes?which one does over half of prescription drugs? 25%?
- 2C9, 2C19, 2D6, 3A4
- 3A4
- 2D6
What enzyme converts tomoxifen to active metabolite?
CYP2D6
What converts codeine to morphine
CYP2D6
What are 3 major drug class metabolized by CYP 2 D6
- Anti-depressants (SSRIs, tricyclics)
- Anti-psychotics (aripiprazole, olanzapine)
- Adrenergic antagonists (carvedilol, metoprolol)
What converts azathioprine and 6 mercaptopurine?
Thiopurine methyltransferase TPMT
What metabolizes irinotecan?
UGT1A1- Gilbert’s syndrome
What metabolizes warfarin and phenytoin?
CYP2C9
What metabolizes isoniazid, hydalazine, procainamide?
N-acetyltransferase