Class #1 to #4

Question 1

Effect of intra cellular receptors?

Answer 1

Alter gene transcription

Question 2

Kd=

Answer 2

50% receptors bound

Question 3

AVD

Answer 3

Vd=Dose / Drug [] in blood. High = more tissue binding. Low = more protein binding in blood

Question 4

Efficacy=

Answer 4

How strong response after Dx bound to receptors

Question 5

Eg of competitive partial agonist?

Answer 5

Oxymetazoline with Epi in nasal spray

Question 6

therapeutic index=

Answer 6

LD50/ED50

Question 7

Therapeutic window=

Answer 7

Concentration range where most people have therapeutic effect and very little have TD

Question 8

Affinity vs Efficacy?

Answer 8

1. Binding 2. USefullness

Question 9

P Glycoprotein =

Answer 9

transport drug out of body

Question 10

Metabolism two steps?

Answer 10

1)Hydrolysis/reduction/oxidation making compound less active or inactive. (Now lipid soluble)(Eg. AAS made into salicylic acid) 2) Conjugation of metabolite to make it more water soluble, transferases make rise to those conjugates (Eg. Gluthatione-s-transferase, glucoronic acid transferases).

Question 11

P450 found where in hepatocytes?

Answer 11

ER

Question 12

Family of CYP that metabolize drugs?

Answer 12

CYP1 CYP2 CYP3

Question 13

Polymorphic distribution? Eg?

Answer 13

More than 1% of pop. has trait that cause differential expression of enz. metabolism.
Eg: CYP 2D6 - codeine, B-blockers, tricyclic antidepressants. CYP 2D6 inhibited by fluoexitine, haloperidol, paroxetine, quinidine

Question 14

Excretion, mostly kidney?

Answer 14

Filtration (small molecules), secretion, reabsorption (lipid soluble are reabsorbed), water soluble are excreted.

Question 15

Drug clearance?

Answer 15

Quantity eliminated in a given amount of time