PKPD

Question 1

oral absorption changes

Answer 1

net effect- no significant effect on rate or extent

Question 2

transdermal absorption changes

Answer 2

↓ absorption of hydrophilic drugs due to drying of the skin (no change for lipophilic drugs)

Question 3

mucosal absorption changes

Answer 3

sublingual, buccal, rectal all stay intact

Question 4

distribution changes

Answer 4

● ↓ lean body mass (weaker), ↑ fat (fatter), ↓ water (dryer)
● more drug held in fat stores
● ↓ albumen in severe illness

Question 5

elimination changes

Answer 5

↓ volume and weight, ↓ renal blood flow, ↓ glomerular function, ↓ tubular function

Question 6

metabolism changes

Answer 6

↓ liver mass and volume, ↓ phase 1 (hydroxylation and demethylation), ↓ CYP3A4, no changes in CYP2D6

Question 7

*types of drugs that may not be metabolized well

Answer 7

benzos, NSAIDs, CCBs

Question 8

*medications with significant renal elimination

Answer 8

beta-blockers, ACEi, AGs, Vanco

Question 9

*distribution changes implications

Answer 9

↓ Vd and ↑ plasma conc. for hydrophilic drugs
↑ Vd and t1/2 in lipophilic drugs

Question 10

*metabolism and excretion summary

Answer 10

↓ clearance and ↑ t1/2

Question 11

*PD changes

Answer 11

increase in baseline effect and sensitivity

Question 12

*PD CNS effects

Answer 12

↓ BBB: ↑ CNS drug conc and time in CNS (BZDs ↑ CNS depression)

Question 13

*PD anticoagulant effects (warfarin)

Answer 13

↓ clearance of warfarin and ↑ intrinsic sensitivity