Week 3b Protein Binding

Question 1

albumin

Answer 1

major blood protein that binds drugs

binds to acidic and neutral drugs

Question 2

protein binding is reversible

Answer 2

protein + drug (free or unbound drug) (equilibrium) drug protein complex (bound drug)

Question 3

alpha1-Acid glycoprotein

Answer 3

binds to basic drugs

Question 4

lipoproteins

Answer 4

binds to hydrophobic drugs

Question 5

The Dynamics of Drug Movement
only free (unbound) drug molecules

Answer 5

• can move around between different compartments and elicit pharmacological effect
• act on a target or be removed by a clearance organ

Question 6

tissue binding

Answer 6

amount of drug in body located in plasma depends on the degree of binding to plasma and tissue components

Question 7

• fraction of unbound drug, fu
Cu?
C?

Answer 7

– Cu is the concentration of unbound drug

– C is the total drug concentration

Question 8

equilibrium association constant, Ka
Cbd?
P?

Answer 8

– Drug + Protein (left/right arrow) Drug-Protein
– Cbd is the concentration of bound drug
– P is the concentration of unbound protein

Question 9

Pt stands for

Answer 9

total protein concentration

Question 10

Kd (dissociation) =

Answer 10

1/Ka

Question 11

lithium

Answer 11

mostly unbound. free to move around body and leave plasma

Question 12

naproxen

Answer 12

strongly protein bound. not available to diffuse into clearance organs. 99.8% bound

Question 13

drugs bound > 90% are said to be

Answer 13

highly protein bound

Question 14

unbound drug is considered to be the

Answer 14

pharmacologically active species