Pharmacodynamics

Question 1

pharmacology

Answer 1

study of drugs that interact with living beings through chemical processes

Question 2

pharmacodynamics

Answer 2

drugs acting on body

Question 3

pharmacokinetics

Answer 3

body acting on drug (metabolism)

Question 4

receptors

Answer 4

interacts with drug and initiates the biochemical events leading to effects

Question 5

physiological receptor

Answer 5

receptor for something naturally made in body (muscarinic, adrenergic)

Question 6

agonists

Answer 6

activate receptor

Question 7

antagonists

Answer 7

block endogenous ligand

Question 8

negative or positive allosteric modulator

Answer 8

endogenous ligand to be weaker / stronger (bind somewhere else besides active site)

Question 9

generalized receptors

Answer 9

not normally a receptor, drug binds to it and alters function (voltage-gated Na+ channels)

Question 10

how do drugs bind to receptors?

Answer 10

hydrogen bonds

Question 11

what can be drugs

Answer 11

anything that produces a physiological effect (most small molecules)

large amount of drugs deviate (biologics)

Question 12

ligand gated ion channels

Answer 12

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

Question 13

G-protein coupled receptors

Answer 13

activates G protein with activate secondary messenger (cAMP) cascades

Question 14

enzyme-linked (receptor tyrosine kinase)

Answer 14

activates signaling cascades through phosphorylation of substrates

Question 15

nuclear receptor

Answer 15

steroid hormone are lipid soluble - allows to enter cell through lipid bilayer

activates or inhibits gene expression after binds to response elements

Question 16

other receptors

Answer 16

no endogenous molecule acts on them, but affected by drugs

ex. proton pump, voltage gated ion channels, enzymes

Question 17

physical properties of drug and structure determine (3 things)

Answer 17

binding
selectivity
affinity

Question 18

selectivity

Answer 18

1 or many receptors

Question 19

NOT ideal conditions of selectivity

Answer 19

bind to same receptor in multiple organs

bind to different receptors, especially when drug concentration in creases (more undesirable side effects)

Question 20

when are drugs more specific?

Answer 20

at low concentrations

Question 21

affinity

Answer 21

how readily and tightly does it bind

Question 22

high affinitiy

Answer 22

good drug receptor interaction, less drug needed to produce a response

Question 23

low affinity

Answer 23

poor drug receptor interaction, more drug needed to produce a response

Question 24

affinity is measured through

Answer 24

equilibrium dissociation constant (Kd)

Question 25

equilibrium dissociation constant

Answer 25

drug concentration for which 50% of that receptor is bound by the drug

Question 26

lower Kd

Answer 26

higher affinity

Question 27

higher Kd

Answer 27

lower affinity

Question 28

law of mass action

Answer 28

drug effects are reversible interactions - can tilt equilibrium

Question 29

when drug receptor complex is activated

Answer 29

conformational change

Question 30

potency

Answer 30

how much drug needed to produce certain effect

Question 31

efficacy

Answer 31

how big is the effect

Question 32

quantal dose response

Answer 32

yes or no situation

Question 33

therapeutic index

Answer 33

want high, so likelihood of toxicity is not reachable

Question 34

margin of safety

Answer 34

the higher the TI of MOS, the safer the drug

Question 35

antagonists

Answer 35

bind to receptor but don't cause conformational change or biological response

Question 36

competitive antagonist

Answer 36

more drug necessary to achieve effect (surmountable) -compete for active site but doesn't activate it -decrease in potency but no decrease in efficacy

Question 37

noncompetitive antagonist

Answer 37

antagonist that bind covalently (insurmountable) -irreversibly bind to allosteroic site on receptor to prevent activation of receptor -decrease in efficacy

Question 38

partial agonist

Answer 38

can't achieve 100% decrease effects of full agonist when given together

Question 39

inverse agonists

Answer 39

promotes inactive conformation - produce opposite effects of regular agonists

Question 40

allosteric modulators

Answer 40

bind to secondary, allosteric site to + or - regulate agonist binding / efficacy

Question 41

orthosteric drugs

Answer 41

bind to primary agonist site on receptor (no effect on signalling)

Question 42

tachyphylaxis

Answer 42

decrease response when same does is given repeatbly

Question 43

desensitization

Answer 43

receptor phosphorylated and binds B-arrestin

Question 44

inactivation

Answer 44

receptor removed from membrane (reversible) membrane forms endosome so receptor is embedded in it can lead to degradation

Question 45

pharmacodynamic tolerance

Answer 45

chronic exposure to agonist can cause decrease in receptor number due to degradation of receptor or decrease in gene expression

Question 46

upregulation

Answer 46

greater receptor number

Question 47

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