principles of pharmacology

Question 1

efficacy

Answer 1

ability to produce therapeutic effect (% response)

Question 2

potency

Answer 2

how much of the drug is required to cause therapeutic effect (i.e. 50% effect) (drug concentration)

Question 3

how do you determine efficacy from a graph

Answer 3

Emax

Question 4

how do you determine potency from a graph

Answer 4

EC50

Question 5

if less drug concentration is required, the ___(more/less) potent it is

Answer 5

more potent

Question 6

which drug is safer? a drug with a wider therapeutic ratio or shorter?

Answer 6

wider

Question 7

steep dose-response curves are higher or lower risk for toxicity

Answer 7

higher risk

Question 8

what is considered a narrow therapeutic ratio

Answer 8

<= 2

Question 9

therapeutic index or therapeutic ratio

Answer 9

TD50/ED50

Question 10

an antagonist that has reversible binding can be displaced if

Answer 10

increase concentration of agonist

Question 11

is Emax still achieved for an irreversible antagonist with agonist

Answer 11

no

Question 12

*describe the graph of a reversible antagonist with agonist

Answer 12

curves are shifted to the right and parallel but still achieve Emax

Question 13

can an antagonist that has irreversible binding be displaced

Answer 13

no. the antagonist doesnt leave the site even when the conc of agonist increases

Question 14

*describe the graph of a irreversible antagonist with agonist

Answer 14

curves have decreased Emax

Question 15

what are 3 adaptive mechanisms in response to repeated exposure to agonist (not involving receptors)?

Answer 15

1. increased metabolism of drug
2. decreased biotransformation of prodrug
3. physiological adaptation

Question 16

which pump excludes drugs from the endothelium of capillaries in the brain?

Answer 16

p-glycoprotein

Question 17

steps for voltage-gated channels

Answer 17

1. activation gate closed; inactivation gate open
2. threshold reached
3. activation gates open; inactivation gate still open
4. ion passes through channel
5. inactivation gate closes; activation gate closes

Question 18

3 mechanisms targeting receptors when repeated exposure to agonist

Answer 18

1. desensitization (phosphorylation)
2. internalization (decrease # of available receptors)
3. downregulation (decrease # of receptors - destruction)

Question 19

what determines if the endosome will downregulate receptor or recycle it back to the membrane?

Answer 19

zip proteins

Question 20

t/f: dimerization can occur between different GPCR

Answer 20

true

Question 21

t/f: G-proteins can activate 2 effector proteins

Answer 21

true (one by alpha-GTP, the other by beta-gamma)