lec7 pharmacodynamics

Question 1

categories of drug effects

Answer 1

therapeutic
nontherapeutic
placebo

Question 2

dose intensity curves measures

Answer 2

how much effect

Question 3

dose frequency curves measures

Answer 3

hoe many affected

Question 4

application of the law of mass action to the kinetics of the binding of drug and receptor creates the equation

Answer 4

drug + receptor bound-receptor –> effect

Question 5

dissociation constant (Kd) for the drug from the receptor is measured by (2 equations for it)

Answer 5

=Kr/Kf
K reverse / K forward
or
= drug + receptor / bound-receptor

Question 6

the curve for durg conc v fraction of bound receptors (i.e. bound / total receptors) is what shape

Answer 6

hyperbolic

Question 7

the conc at which half of the receptors are bound is the

Answer 7

Kd = dissociation constant

Question 8

Bmax is the

Answer 8

totality of the receptors bound by the drug

Question 9

why are semilogarithmic plots used instead of linear (hyperbola)

Answer 9

linear plots at point near zero, the effect changes rapidly
semi log curve has large middle portion close to EC50 which is linear and easier to work with so easier to make accurate determination

Question 10

Emax =

Answer 10

maximum effect

Question 11

what is used as a measure of Kd

Answer 11

EC50

Question 12

lower EC50 means what to the affinity for binding to the receptor

Answer 12

lower EC50 –> lower Kd –> higher affinity for binding to the receptor

Question 13

drug conc producing an effect that’s 50% of the max effect

Answer 13

EC50

Question 14

EC50 provides what important characteristic of drugs

Answer 14

potency

Question 15

Emax provides what important characteristic of drugs

Answer 15

efficacy

Question 16

define efficacy

Answer 16

max effect of a drug achieveable at a high dose

Question 17

lower EC50 = ____ potency

Answer 17

higher

Question 18

lower Emax = ____ efficacy

Answer 18

lower

Question 19

when comparing 2 drugs you want the one with the lower or higher Emax

Answer 19

higher

Question 20

how well the drug binds the receptor

Answer 20

potency

Question 21

how well the drug produces the effect

Answer 21

efficacy

Question 22

t/f potency and efficacy are related

Answer 22

f: unrelated

Question 23

potency is ___ related to EC50

Answer 23

inversely

lower potency = higher EC50

Question 24

ability of a drug to affect one tissue or receptor in prefereance to another

Answer 24

selectivity

Question 25

a highly selective drug is one which

Answer 25

affects only a receptor or tissue without affecting others

Question 26

what curve is needed to measure selectivity

Answer 26

concentration - response

Question 27

what type of agonist: drug that has efficacy greater than zero but less than a full agonist

Answer 27

partial agonist

Question 28

what type of agonist: drug that binds to a receptor and produces max bio response

Answer 28

full agonist

Question 29

what type of agonist: drug that induces pharm response opposite of agonist

Answer 29

inverse agonist

Question 30

what is a neutral antagonist

Answer 30

drug that does NOT induce a bio response and reduces/blocks response induced by agonist

Question 31

order the 3 agonists from highest emax to lowest

Answer 31

full > partial > inverse

Question 32

process where a drug decr or opposes action of another drug or endogenous ligand

Answer 32

antagonism

Question 33

what are the 4 types of antagonisms

Answer 33

chemical pharmacokinetic physiological pharmacological

Question 34

type of antagonism where antagonist accelerates the metabolism or the elimination of the agonist

Answer 34

pharmacokinetic

Question 35

type of antagonism where antagonist binds directly to agonistto make it inactive

Answer 35

chemical

Question 36

type of antagonism where theres 3 types | reversible competitive, noncompetitive, irreversible

Answer 36

pharmacological

Question 37

type of antagonismwhere antagonist activates a diff mechanism that opposes the effects of the agonist

Answer 37

physiological

Question 38

what happens to potency and efficacy in reversible competitive

Answer 38

right shift of dose-response curve higher EC50 --> lower potency no change in efficacy

Question 39

competitive antagonism can be overcome by

Answer 39

incr the conc of agonist to achieve the same effect as before

Question 40

can a noncompetitive antagonism be overcome

Answer 40

no cant restory to original response by incr conc of agonist

Question 41

what happens to potency and efficacy in noncompetitive

Answer 41

lower emax --> decr efficacy | unchanged potency

Question 42

what happens to potency and efficacy in irreversible competitive

Answer 42

lower emax --> decr effcacy | no change potency

Question 43

joint effect of 2 drugs is the sum of their individual effects

Answer 43

summation

Question 44

joint effect of 2 drugs is greater than sum of their effects

Answer 44

synergism

Question 45

inert drug enhances the effect of another drug

Answer 45

potentiation

Question 46

drug effect loss over time

Answer 46

tolerance

Question 47

mechanism for decreased effect (includes tachyphylaxis)

Answer 47

desensitization

Question 48

what curve is all or nothing i.e. their effect is scored on whether present or absent

Answer 48

quantal dose-response curves

Question 49

diff bn incremental and cumulative quantal curves

Answer 49

incremental - as dose incr, number responders incr (bell curve) cumulative - as dose incr, number responders adds up

Question 50

which curve has more variability? shallow, wider taller, narrow

Answer 50

shallow, wide

Question 51

dose producing effect in 50% of subject

Answer 51

ED50

Question 52

dose making death in 50% of subjects

Answer 52

LD 50 = lethal dose

Question 53

what do different slopes in quantal curves imply

Answer 53

diff sources of variability, suggesting diff in route or mechanism of action

Question 54

therapeutic index equation

Answer 54

LD50 / ED50

Question 55

the higher the therapeutic index

Answer 55

the safer the drug

Question 56

why is pop variability important in quantal curves

Answer 56

bc can have same therapeutic index but different risk

Question 57

standardized safety margin equation

Answer 57

(LD1-ED99) / ED99 * 100

Question 58

the more positive the ED99 or the greater the diff bn LD1 and ED99 , the ___ the drug

Answer 58

safer