Lec 4 Protein Binding concepts

Question 1

what gives the therapeutic effect in body

Answer 1

Cu

Question 2

why is C a good estimate for Cu? (e.g. if C increases, Cu increases as well)

Answer 2

as fu is usually constant in a healthy individual

Question 3

which drugs bind exclusively to albumin

Answer 3

anionic drugs (NSAIDS, coumarin anticoagulants, anticonvulsant)

Question 4

which drugs have affinity for a1-AGP

Answer 4

cationic (lipophilic amines): BB, antiarrhythmics, antidepressants

Question 5

when does fu changes V?

Answer 5

when have large V (>1L/kg)

Question 6

which eqn works well for low V?

Answer 6

Oie and tozer model

Question 7

what does oie and tozer model account for?

Answer 7

albumin and plasma proteins present in interstitial fluid

Question 8

basic drugs tend to have stronger _____ than acidic drugs that causes them to have larger V?

Answer 8

extensive tissue protein binding

Question 9

(1) in what situation, Cu remains unchanged when fu increases? (2) and what ensures Cu remains unchanged?

Answer 9

(1) drugs with high V and low E (both factors sensitive to fu changes)
(2) tissue distribution increases (V) and clearance (CL) sensitive to fu increases