Week 2 Pharmodynamics Module

Question 1

define pharmodynamics

Answer 1

what a drug does to the body

Question 2

define pharmokinetics

Answer 2

what the body does to a drug

Question 3

what is a drug?

Answer 3

an exogenous chemical compound that effects a biochemical or physiological function in a specific way

Question 4

define receptor

Answer 4

a sensing element in a chemical communication system that coordinates the function of different cells in the body

Question 5

define inert binding site

Answer 5

an endogenous molecule that binds to a drug but does not lead to a response (ex drugs commonly bind with albumin, and that binding does not cause any physiologic effects)

Question 6

give an example of a drug that inhibits an enzyme

Answer 6

Statin: inhibits HMGCoA Reductase which decreases intra-hepatic cholesterol synthesis

Question 7

give an example of a drug that acts on a transport protein

Answer 7

Digitalis: inhibits Na/K ATPase

Question 8

give an example of a drug that acts on a structural protein

Answer 8

Colchicine: binds tubuline

Question 9

what are the four families of receptors. which are membrane receptors?

Answer 9

ligand-gated ion channels: membrane G protein coupled receptors: membrane Enzyme-linked receptors: membrane Intracellular receptros: not in the membrane (ligand is hydrophobic)

Question 10

what are three prototypes of statin?

Answer 10

simvastatin, lovastatin, atorvastatin

Question 11

what do glucocorticoid drugs do?

Answer 11

anti-inflammatory agents

Question 12

what are three prototypes of glucocorticoids?

Answer 12

dexamethasone, prednisone, hydrocortisone

Question 13

Drug affinity is directly proportional to what two factors?

Answer 13

bond strength and structural conformation

Question 14

what is an agonist?

Answer 14

substance that activates receptors. has affinity for receptor and intrinsic activity

Question 15

what is an antagonist

Answer 15

substance that prevents receptor activation. affinity for receptor but no intrinsic activity

Question 16

what is othrosteric binding of drugs

Answer 16

drug binds to active site

Question 17

what is allosteric binding of drugs

Answer 17

drug binds at a site other than the active site

Question 18

what is a full agonist?

Answer 18

produces 100% activation of a receptor at high concentrations

Question 19

what is a partial agonist

Answer 19

binding results in less than 100% activation even at very high concentrations

Question 20

what is an inverse agonist

Answer 20

binding results in a response below the basal activity

Question 21

what is a competitive antagonist. can they be overcome

Answer 21

binds to the same site as an agonist (reduce potency). overcome by increasing agonist concentration

Question 22

what is a noncompetitive antagonist. how can they be overcome?

Answer 22

binds to a different site than the agonist. prevent the binding of agonist or prevent the agonist from activating the receptor. reduce efficacy. cant be overcome

Question 23

define potency

Answer 23

amount of drug needed to reach a desired effect

Question 24

define efficacy

Answer 24

max effect a drug can produce

Question 25

what are physiological antagonists

Answer 25

opposing pathways that exist in the body

Question 26

what are chemical antagonists

Answer 26

receptors are not involved, activity based on chemical interactions

Question 27

what is selectivity

Answer 27

the degree to which a drug or chemical has an affinity for a particular type of receptor

Question 28

what is favorable about highly selective drugs?

Answer 28

they produce the intended or desired effect with minimal side effects

Question 29

give an example of a selective drug

Answer 29

some beta blockers selectively block Beta 1 receptors in the heart but not beta 2 receptors in the lungs

Question 30

a drug is selective if...

Answer 30

the drug interacts with only one type of receptor, and if that receptor type regulates just a few processes

Question 31

a drug is non-selective if...(2 options)

Answer 31

if a drug interacts with one receptor but that receptor regulates multiple processes. OR if a drug interacts with multiple receptors.

Question 32

which drugs are completely selective

Answer 32

none. increasing does of any drug will lead to side effects.

Question 33

does selectivity guarantee drug safety?

Answer 33

no. too much of a drug can still have a negative effect

Question 34

what is a graded dose-response curve? what can it tell you?

Answer 34

a curve that shows how different concentrations of a drug impact its effects. it can be used tom compare potency and efficacy of different drugs

Question 35

what is Emax?

Answer 35

the maximal response or effect. biggest response a drug can produce

Question 36

what is EC50

Answer 36

the concentration of the drug producing 50% of the maximal effect (Emax)

Question 37

what to quantal dose-response curves show?

Answer 37

these curves tell you how drugs effect the general population. Give you ED50, TD50, LD50

Question 38

what is ED50

Answer 38

the effective dose in which the desired effects are seen in 50% of people

Question 39

what is TD50

Answer 39

the toxic dose for 50% of popn

Question 40

what is LD50

Answer 40

the lethal dose for 50% of people

Question 41

how do you calculate therapeutic index? TI

Answer 41

TI=TD50/ED50

Question 42

how do you calculate the margin of safety?

Answer 42

MS=LD1/ED99

Question 43

when is it ok to use a drug with a narrow therapeutic window (small TI)

Answer 43

only when no other therapeutic options exist. routine monitoring of drug levels is necessary

Question 44

a wide therapeutic window has what TI?

Answer 44

large TI

Question 45

what is this?

Answer 45

Quantal dose response curve

Question 46

what is this?

Answer 46

graded dose response curve

Question 47

give an example of a non-slective beta blocker?

Answer 47

propanolol and sotolol

Question 48

what are examples of selective beta blockers

Answer 48

atenolol, metoprolol, esmolol