Lecture 1: Pharmacodynamics

Question 1

actions of a drug on the body

Answer 1

pharmacodynamics

Question 2

actions of the body on a drug

Answer 2

pharmacokinetics

Question 3

normal function is to be a receptor for something naturally produced in the body

Answer 3

physiological receptor

Question 4

a protein that isn’t normally a receptor, but a drug binds to it and alters its function

Answer 4

generalized receptor

Question 5

what types of molecules can be drugs?

Answer 5

any chemical that interacts with a system to produce a physiological effect

Question 6

what are “biologicals”

Answer 6

peptides/proteins/antibodies

Question 7

the component of a cell or organism that interacts with a drug and initiates the biochemical events leading to its effects

Answer 7

receptor

Question 8

most common way drugs bind receptor

Answer 8

hydrogen bonds

Question 9

agonist

Answer 9

activate the receptor

Question 10

antagonist

Answer 10

block the endogenous ligand

Question 11

negative or posiitve allosteric modulator

Answer 11

cause the endogenous ligand to be weaker or stronger

Question 12

channel opens (allow ions to pass) when a signaling molecule binds

Answer 12

ligand-gated ion channels

Question 13

activates G proteins which activate second messenger cascades

Answer 13

G-protein coupled receptors

Question 14

activates signaling cascades through phosphorylation of substrates

Answer 14

receptor tyrosine kinase

Question 15

activates or inhibits gene expression

Answer 15

nuclear

Question 16

GPCR, RTK, and LGIC are located where

Answer 16

cell membrane m

Question 17

where are nuclear receptors located

Answer 17

cytosol

Question 18

the physical properties of a drug and structure of a receptor determines:

Answer 18

• binding
• selectivity
• affinity

Question 19

drug-receptor binding equation (agonist)

Answer 19

D + R <-> DR <-> DR* ->-> response

Question 20

ideal drug would function specifically on

Answer 20

desired organ system and receptor

Question 21

most drugs either: (selectivity)

Answer 21

• bind to the same receptors, but in multiple organs or
• bind to different receptors, especially as drug concentration increases

Question 22

the _ of a drug for a receptor described how readily and tightly that drug binds to the receptor

Answer 22

affinity

Question 23

the lower the Kd, the _ the affinity for a receptor

Answer 23

higher

Question 24

the higher the Kd, the _ the affinity of a drug for a receptor

Answer 24

lower

Question 25

high affinity =

Answer 25

good drug-receptor interaction; LESS drug needed to produce a response

Question 26

low affinity =

Answer 26

poor drug receptor interaction; MORE drug needed to produce a response

Question 27

Equilibrium dissociation constant

Answer 27

Kd

Question 28

X axis on ligand-receptor binding curves

Answer 28

concentration of drug (ligand)

Question 29

Y axis of ligand-receptor binding curves

Answer 29

fraction of receptors occupied by drug

Question 30

LR

Answer 30

ligand-receptor complexes

Question 31

R0:

Answer 31

total receptors

Question 32

Kd

Answer 32

concentration where half of receptors are occupied

Question 33

EC50 or ED50

Answer 33

concentration or dose needed to reach 50% of max effect

Question 34

Emax

Answer 34

maximal effect produced by the drug

Question 35

potency

Answer 35

how much of a drug is needed to produce a certain level of effect? * EC50 commonly used

Question 36

efficacy

Answer 36

how big is the effect

Question 37

EC50 < Kd when

Answer 37

there are spare receptors

Question 38

how can maximal effect be achieved with less than 100% of the receptors occupied?

Answer 38

signal amplification by second messenger pathways

Question 39

ED50

Answer 39

median effective dose

Question 40

TD50

Answer 40

median toxic dose

Question 41

LD50

Answer 41

median lethal dose

Question 42

therapeutic index equation

Answer 42

(TD50 OR LD50) / ED50

Question 43

margin of safety

Answer 43

(LD1 or TD1) / ED99

Question 44

The higher the TI of MOS, the _ the drug

Answer 44

safer

Question 45

competitive antagonist

Answer 45

more drug necessary to achieve effect

Question 46

competitive antagonist are surmountable or insurmountable

Answer 46

surmountable

Question 47

noncompetitive antagonist

Answer 47

bind covalently

Question 48

noncompetitive antagonists are surmountable or insurmountable

Answer 48

insurmountable

Question 49

partial agonist

Answer 49

not able to achieve 100% effect

Question 50

buprenorphine

Answer 50

partial agonist, most potent but less efficacious

Question 51

inverse agonist

Answer 51

promote the inactive (R) conformation and therefore eliminate baseline/constitutuve signaling thereby producing effects opposite those regular agonists

Question 52

orthosteric drugs

Answer 52

binds to the primary agonist site on a receptor

Question 53

allosteric modulators

Answer 53

bind to a secondary, allosteric site to positively or negatively regulate agonist binding or efficacy

Question 54

tachyphylaxis

Answer 54

decreased response when same dose is given multiple times

Question 55

desensitization

Answer 55

receptor is phosphorylated and binds beta-arrestin

Question 56

inactivation

Answer 56

receptor removed from membrane

Question 57

upregulation

Answer 57

chronic antagonist exposure can cause this, greater receptor number

Question 58

up/down regulation depend on _ and _ (longest time frame compared to other mechanisms

Answer 58

internalization, transcription

Question 59

receptor drug binding equation (antagonist)

Answer 59

D + R<-> DR <-x-> DR* ->-> response