Pharm 1.

Question 1

drug action vs drug effects

Answer 1

drug action: molecular - invisible. drug effect - pharmacologic - visible

Question 2

How do we measure drugs?

Answer 2

drug effect

Question 3

pharmacokinetics

Answer 3

time course of drug absorption, actions and elimination

Question 4

pharmacodynamics

Answer 4

types of drug actions

Question 5

How are drugs created?

Answer 5

to mimic endogenous agonists

Question 6

How are doses measured?

Answer 6

by weight (mg, mcg)

Question 7

Where do pharmacodynamics and pharmacokinetics event occur?

Answer 7

at the molecular level

Question 8

How much is a mole?

Answer 8

6.022 x 10^23 molecules

Question 9

How many L of total body water?

Answer 9

40

Question 10

How do you induce a change in tissue function with drugs?

Answer 10

affect the receptor which causes molecule events - enough of these events causes change in cell function

Question 11

What is the effect of drug/receptor interaction?

Answer 11

production of a small change in the biochemical or electrochemical homeostasis of the cell - cumulative effects lead to change in function of cell

Question 12

eMax

Answer 12

maximal response that is eventually achieved which is related to the number of drug-receptor interactions and the physiologic capacity of the tissue

Question 13

What are reversible receptor bonds?

Answer 13

ionic, van der waals, hydrogen

Question 14

What are irreversible receptor bonds?

Answer 14

covalent

Question 15

G protein activity

Answer 15

lasts only for seconds before being turned off - stimulation by drugs can cause amplification of signals

Question 16

Second messengers

Answer 16

produces amplification of the drug receptor interaction

Question 17

How does the structure of the drug affect the activity of the drug?

Answer 17

structure determines how it will fit into the receptor - better the fit, the better the stimulation

Question 18

How do stereoisomers affect drug interaction? (epi as example)

Answer 18

(-) form of epic more active than the (+) epic because hydroxyl group is facing towards the receptor as opposed to the -H in the (-) form

Question 19

Why are stereoisomers a bad thing?

Answer 19

the “bad” stereoisomer can block the good isomer (competition)

Question 20

How do we measure dose-response relationships?

Answer 20

log of drug concentration because it is easier to pick up EC50

Question 21

What is the Michaelis Menten equation?

Answer 21

Effect = Emax [Dose] / Kd (dissociation constant = EC50) + [D]

Question 22

threshold

Answer 22

the beginning of the curve - dose of agonist at which a response begins

Question 23

maximal asymptote

Answer 23

top of the curve - represents EMax for a particular agonist

Question 24

slope

Answer 24

rate of rise of the response on the steep portion of the curve, log of EC50 also relates to affinity

Question 25

intrinsic activity

Answer 25

ability to stimulate the receptor once bound - relates to structure and influences efficacy and potency - greater intrinsic activity = greater efficacy

Question 26

spare receptors

Answer 26

not all receptors need to be occupied to achieve Emax

Question 27

secondary receptors

Answer 27

outside target tissuemay mediate other effects of the drug “side effects”

Question 28

receptor regulation

Answer 28

a cell can up or down regulate a population of receptors by changing the total number of receptors or their sensitivity

Question 29

agonists drugs

Answer 29

bing to the receptor and produce a pharmacologic effect - activate after binding

Question 30

If the best agonist produces 100% effect at lowest dose, why do we sometimes use weak agonists?

Answer 30

the doses of the weak agonists can be less dangerous because harder to reach toxic levels - can still reach 100% effect as well

Question 31

antagonist

Answer 31

receptor blocker - blocks effects of receptor and other drugs

Question 32

How do weak agonists work?

Answer 32

only fits one of two binding sites - either effector site or binding site 1. fits binding site, but effector site not well = weak agonist or 2. only binds effector site, not binding sit, binds only briefly

Question 33

Best agonists intrinsic activity

Answer 33

only some receptors are occupied to get 100% effect

Question 34

two agonists with different intrinsic activity but same affinity

Answer 34

have same affinity for receptors but different intrinsic activity - know they are binding the receptor in the same way because the have the same E50

Question 35

two agonists with different intrinsic activity AND different affinity

Answer 35

different e50, different effect (one doesn’t reach Emax)

Question 36

efficacy

Answer 36

the ability of the drug to activate the effector portion of the receptor once the drug is bound to the receptor. depends upon structure of drug

Question 37

potency

Answer 37

relates to the amount of drug needed for effect. depends on receptor density, efficiency of stimulus-response mechanisms of the tissue

Question 38

relative potency

Answer 38

horizontal relationship (both reach eMax)

Question 39

relative efficacy

Answer 39

vertical relationship (one doesn’t reach eMax)

Question 40

competitive antagonists

Answer 40

antagonist effect can be overcome by increasing the dose of the agonist (weak bond)

Question 41

noncompetitive antagonists

Answer 41

can’t be overcome by increasing doses of agonist (strong bond) - can change effector site or binding site