PK/PD

Question 1

CYP2D6

Answer 1

variations turn into poor/normal/ultrarapid metabolizers 100x variability in enzyme activity

PRODRUGS may be more effective in UMs, but can increase toxicity risk (UMs), less effective in PMs

Question 2

CYP2D6 PRODRUGS

Answer 2

Tamoxifen

Codeine

Tramadol

Nortriptyline

Fluoxetine

Metoprolol/carvedilol

Question 3

CYP2C9

Answer 3

mainly in the liver, on chromosome 10, very polymorphic

Question 4

CYP2C9 substrates

Answer 4

ARB, NSAIDS, celecoxib

Question 5

Drugs with small therapeutic window

Answer 5

warfarin, phenytoin, tolbutamide, glipizide

Question 6

Warfarin

Answer 6

PM; increase risk of bleeding

Question 7

Phenytoin

Answer 7

PM; increased risk of ataxia, other toxicity

Question 8

Tolb, gly, glim

Answer 8

PM; increase risk of hypoglycemia

Question 9

CYP2C19

Answer 9

mainly in the liver; metabolism of clinically important drugs

Omeprazole, lansoprazole, diazepam, clopidogrel

Question 10

CYP3A4

Answer 10

Major CYP in humans, in the liver, genetic polymorphisms are rare

Question 11

CYP3A5

Answer 11

in kidney, highly polymorphic

6/7 cause loss of 3A5 activity

*1 in 50% of AA pop and 33% in hispanic/asian causes increased activity

Question 12

CYP2A6