Pharmacodynamics

Question 1

what the BODY does to the the DRUG

Answer 1

pharmacoKINETICS

Question 2

what the DRUG does to the BODY

Answer 2

pharmacoDYNAMICS

Question 3

observed effect on the body

Answer 3

pharmacological effect

Question 4

functional modification

Answer 4

pharmacological action

Question 5

molecular modification

Answer 5

mechanism of action

Question 6

drug goes through the cell membranes

Answer 6

diffusional transfer

Question 7

drug goes through intercellular pores (between cells)

Answer 7

bulk flow transfer

Question 8

proportional to concentration gradient

Answer 8

lipid diffusion (size: 100 - 1,000 MW)

Question 9

inversely proportional to thickness of membrane

Answer 9

lipid diffusion

Question 10

drug goes through aquaporins

Answer 10

aqueous diffusion

Question 11

proportional to # of aquaporins AND concentration gradient

Answer 11

aqueous diffusion (size: less than or equal to 200 MW)

Question 12

MW = 2,000 - 100,000 REQUIRES ENERGY

Answer 12

endocytosis/exocytosis

Question 13

amount of drug in body compared to plasma concentration

Answer 13

volume of distribution (Vd)

Question 14

Vd is _____, NOT _____

Answer 14

CONSTANT

dose-dependent

Question 15

Vd formula

Answer 15

(D x F)/Cp

Question 16

Vd

• 3L =
• 13L =
• 42L =
• more than 42L =

Answer 16

• plasma
• ECF
• TBW
• tissues

Question 17

more protein-binding drugs cross placenta ____, and will NOT _____

Answer 17

SLOWLY

be filtered by glomeruli

Question 18

D x F =

Answer 18

Total drug inside body

Question 19

relates RATE of elimination to plasma concentration

Answer 19

clearance

Question 20

CL total =

Answer 20

CL(hepatic) + CL(renal) + CL(after)

Question 21

organ CL of a drug CANNOT exceed that of

Answer 21

MAXIMUM blood flow to that organ

Question 22

makes drug more POLAR

Answer 22

biotransformation

Question 23

phase I

Answer 23

CYP450 (oxidation, reduction, hydrolyses)

Question 24

phase II

Answer 24

conjugation (MC: glucuronidation; acetylation)

Question 25

CL(renal)

Answer 25

(F x U(drug))/P(drug)

Question 26

CL(renal) - 100-150mL/min = - more than 150mL/min - less than 100mL/min

Answer 26

- filtration - secretion - reabsorption (or protein binding)

Question 27

amount of time taken for the plasma concentration of a drug to fall by 1/2

Answer 27

t(1/2) of elimination

Question 28

t(1/2) is NOT dependent on?

Answer 28

DOSE

Question 29

T =

Answer 29

infusion time

Question 30

C(ss) is proportional to

Answer 30

D

Question 31

C(ss) is inversely proportional to

Answer 31

T

Question 32

C(ss) =

Answer 32

D/(T x CL)

Question 33

steady state =

Answer 33

rate of infusion = rate of elimination

Question 34

drug is considered eliminated after how many t(1/2)?

Answer 34

4.5

Question 35

if dosing interval is shorter than 4t(1/2), what will occur?

Answer 35

accumulation

Question 36

drug receptors include

Answer 36

1. regulatory proteins 2. iron channels 3. enzymes 4. carrier proteins 5. structural proteins

Question 37

properties of receptors

Answer 37

1. specificity 2. stereo-specific 3. SENSITIVITY 4. variability

Question 38

define affinity

Answer 38

tendency of drug to bind to receptor

Question 39

full agonist

Answer 39

activates receptor to MAXIMUM response

Question 40

partial agonist

Answer 40

activates receptor to BELOW max response

Question 41

inverse agonist

Answer 41

deactivates receptor's BASAL activity (decreases it)

Question 42

antagonist

Answer 42

prevent agonist-induced increase in basal activity, AND prevents inverse agonist-induced decrease in basal activity

Question 43

drug antagonism

Answer 43

1. chemical 2. pharmacokinetic 3. physiologic (functional) 4. pharmacological (receptor-block)

Question 44

drug binds w/ another drug to inactivate it

Answer 44

chemical

Question 45

drug to decreased absorption OR increases elimination reducing its concentration at SOA (site of action)

Answer 45

pharmacokinetic

Question 46

drug acts on DIFFERENT receptor to antagonize effect of a drug on its receptor

Answer 46

physiologic (functional)

Question 47

agonist and antagonist complete for the SAME receptor

Answer 47

pharmacological (receptor-block)

Question 48

receptor blockade w/ same efficacy; need increased dose (decreases potency)

Answer 48

competitive antagonist

Question 49

receptor blockade that decreases efficacy

Answer 49

noncompetitive antagonist

Question 50

receptor regulation: - desensitization

Answer 50

response diminishes over time (seconds to minutes)

Question 51

receptor regulation: - down-regulation

Answer 51

- response diminishes over time (hours to days) | - decrease in # of R's

Question 52

drug interaction: - 1 + 1 = 2 - 1 + 1 > 2 - 0 + 1 > 1 - 1 + 1 < 2 or 0 + 1 < 1

Answer 52

- addition - synergism - potentiation (drug which has no effect by itself increases effects of another drug) - antagonism