T3

Question 1

pharmacodynamics

Answer 1

what the drug does to the body and how it does it

Question 2

ligand/substrate

Answer 2

any substance that binds a drug target

Question 3

endogenous

Answer 3

originating from within the body

Question 4

exogenous

Answer 4

originating from outside the body

Question 5

orthosteric

Answer 5

drug ligand binds to the same site as the endogenous signaling substance to exert its effects
direct competition between ligands for the binding site

Question 6

allosteric

Answer 6

drug ligand binds to a different site as the endogenous signaling substance to exert its effects
no competition between ligands for the binding site

Question 7

constitutive activity

Answer 7

activity in the absence of a ligand

Question 8

types of binding

Answer 8

covalent: very strong bond, irreversible
electrostatic: strong bond but weaker than covalent bonds and reversible
hydrophobic: weakest bond, reversible

Question 9

agonism

Answer 9

capacity of a ligand to activate a drug target

Question 10

antagonism

Answer 10

blocks the action of an agonist

Question 11

efficacy (Emax)

Answer 11

maximal effect an agonist can produce
determined primarily by the drug dose and the ability of the drug to activate receptors

Question 12

potency (EC50)

Answer 12

concentration or amount of drug required to produce a defined effect
determined by the affinity of the receptor for the drug and the total number of receptors available

Question 13

ideal drug target

Answer 13

appropriate physical characteristics to bind the drug substance (MW, shape, solubility)
high affinity for the drug substance (drug binds strongly to the desired site)
high selectivity for the drug substance (drug not competing with numerous other molecules for the targeted binding site)
unique from other drug targets (few or no other targets with similar structure or function)

Question 14

methods of target validation: chemical probe

Answer 14

small substance is developed which binds that target and the biological effects are closely studied

Question 15

methods of target validation: gene silencing

Answer 15

small interfering RNA (siRNA) block production of target protein to mimic the effect of inhibition

Question 16

methods of target validation: genetic modification of animals

Answer 16

gene coding for the target is disabled

Question 17

small molecule drug targets

Answer 17

receptors, enzymes, ion channels, and membrane transporters

Question 18

large molecule drug targets

Answer 18

inflammatory mediators
immunological checkpoint inhibitors
cell surface molecules
genetic replication

Question 19

signal transduction

Answer 19

when a drug binds to a receptor and initiates a series of events
transmission of signals from the drug receptor complex to various cellular components leading to changes in cell function

Question 20

full agonist

Answer 20

activates target fully and produces maximal response
ligand has high affinity for the target receptor

Question 21

partial agonist

Answer 21

produced less than full effect even when target is saturated
ligand has less of an affinity for the target receptor

Question 22

inverse agonist

Answer 22

produces opposite effect of agonist by selectively binding receptors in the inactive state
reduces constitutive activity

Question 23

competitive antagonism

Answer 23

orthosteric - competes with the agonist for binding site
non-covalent bonding (reversible)
decreases potency of the agonist

Question 24

non-competitive antagonism

Answer 24

orthosteric - binds regardless of whether another ligand is bound
covalent bonding (irreversible)
decreases the efficacy of the agonist

Question 25

positive allosteric modulator

Answer 25

amplify response of the receptor to its endogenous ligand and enhances activity may enhance potency and/or efficacy

Question 26

negative allosteric modulator

Answer 26

inhibit response of the receptor to its endogenous ligand thereby reducing activity reduced potency and efficacy

Question 27

beta adrenergic receptor

Answer 27

metoprolol class: beta blocker inhibits beta-1 adrenergic receptors to lower heart rate

Question 28

mu opioid receptor

Answer 28

morphine class: opioid activates mu opioid receptors to inhibit nerve activity

Question 29

drug action on enzymes demonstrate

Answer 29

demonstrate lock and key fit to enzyme active sites and form enzyme substrate complexes when bound

Question 30

enzymes that are drug targets are almost always those

Answer 30

that are rate-limiting

Question 31

enzymes typically demonstrate _____ binding

Answer 31

orthosteric agonism - reversible antagonism competitive - reversible antagonism non-competitive - irreversible

Question 32

drug action on enzyme synthesis induction

Answer 32

increasing production of certain enzymes causes higher enzyme levels which in turn can alter physiologic processes

Question 33

drug action on enzyme synthesis inhibition

Answer 33

reducing production of certain enzymes causes decreased enzyme levels and can alter physiologic processes

Question 34

hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase

Answer 34

atorvastatin class: HMG-CoA reductase inhibitor blocks the activation of the rate limiting enzyme in cholesterol synthesis

Question 35

angiotensin converting enzyme (ACE)

Answer 35

lisinopril class: ACE inhibitor competitive inhibitor of ACE, which converts angiotensin I to angiotensin II thereby lowering blood pressure

Question 36

ion channel types

Answer 36

voltage-gated ion channels: depolarized gates open and hyperpolarized gates close, regulates flow of ions ligand-gated ion channels: a specific signaling molecule binds to a site on the channel protein which causes it to change shape (opens pore)

Question 37

drug action on ion channel agonist

Answer 37

directly bind and induce opening of the ion channel

Question 38

drug action on ion channel antagonist

Answer 38

directly bind to prevent ion channel opening

Question 39

drug action on ion channel positive modulator

Answer 39

amplify response of the ion channel to its endogenous ligand to enhance activity

Question 40

drug action on ion channel negative modulator

Answer 40

inhibit response of the ion channel to its endogenous thereby reducing ion channel activity

Question 41

voltage gated calcium channel

Answer 41

verapamil class: calcium channel blocker inhibit ion conductance in the heart and vascular smooth muscle to provide anti arrhythmic and blood pressure lowering effects

Question 42

gamma-aminobutyric acid (GABAA) ligand gated ion channel

Answer 42

lorazepm class: benzodiazepine activate GABAA receptor, increasing neuronal permeability to chloride causing sedative

Question 43

sodium-potassium chloride cotransporter

Answer 43

furosemide class: loop diuretic competes with chloride ions for binding in the renal tubule thereby increasing natiuresis

Question 44

serotonin transporter (SERT)

Answer 44

sertraline class: selective serotonin reuptake inhibitor (SSRI) block serotonin transporter, increasing serotonin levels in the synaptic cleft and enhancing neurotransmission