Pharmacodynamics

Question 1

what is pharmacodynamics

Answer 1

biochemical and physiological effects of drug on body and mechanism of action

Question 2

what is EDTA

Answer 2

chelator with an afinity for lead

Question 3

how do antacids work

Answer 3

they are basic and work to neutralize stomach acid

Question 4

how does mannitol work

Answer 4

it is inert and doesn’t get absorbed in the body so it works in the urine as an osmotic diuretic

Question 5

what are the 4 types of receptors/proteins that drugs can act on

Answer 5

enzymes, transporters, ion channels, and proteins

Question 6

molecules that bind to receptors are called

Answer 6

ligands

Question 7

ligands include _____ as well as ______ signaling molecules such as hormones and neurotransmitters

Answer 7

drugs(exogenous) as well as endogenous

Question 8

if a drug causes the receptor to respond in the same way as the naturally occuring substance the drug is called a(n)

Answer 8

agonist

Question 9

If a drug binds to the receptor and doesnt produce a response it’s called a(n)

Answer 9

antagonist (prevents binding of endogenous NT or hormones)

Question 10

what are the 4 major classes of receptors

Answer 10

ligand-gated ion channels (nicotinic Ach receptors musc)
protein receptors (tyrosine-kinase, insulin)
g-protein coupled receptors(beta adrenergic)
ligand activated transcription factors (estrogen receptors, hormones)

Question 11

how do transmembrane ion channels work/ex

Answer 11

ligand or voltage gated –> nicotinic Ach receptors Na+ flux

Question 12

what is the most common pathway affected by drugs

Answer 12

transmembrane ion channel linked to intracellular G proteins (signal transduction to a 2nd messenger)

Question 13

what do alpha1 and alpha2 adrenergic receptors do?

Answer 13

1 - activation of lipase

2 - inhib adenylyl cyclase

Question 14

what does the beta adrenergic receptor do?

Answer 14

stimulates adenylyl cyclase

Question 15

what does the muscarinic receptor do?

Answer 15

activates phospholipase

Question 16

give an example of a transmembrane receptor with a cytosolic domain

Answer 16

insulin receptor and growth factor

Question 17

Intracellular receptor binding causes ______. ex of ligands that bind (3)

Answer 17

ligand binding causes a change in gene expression (transcription factors)
steroids, hormones, VitD

Question 18

give 2 examples of extracellular receptors

Answer 18

ACE and Ach-esterase

Question 19

give an example of an adhesion receptor

Answer 19

integrins

Question 20

desctribe a transmem ion receptor

Answer 20

a ligand binds to the receptor on the channel which opens the channel and the change in ion concentration triggers a cellular response

Question 21

________ gated ion channels are activated by changed in membrane voltage

Answer 21

voltage

Question 22

_______ gated ion channels are activated after binding of a ligand occurs …. where can the binding domain be found

Answer 22

ligand gated; intra, extracellular, or within the ion channel

Question 23

________ and ___________ drug classes work by alt the conductance of ion channels

Answer 23

local anesthetics

benzodiazepines

Question 24

G-protein coupled receptors are good for….

Answer 24

amplification of the signal

Question 25

what are secondary messengers

Answer 25

small nonprotein, water-soluable molecules or ions

Question 26

Increases in CA2+ can cause... (3)

Answer 26

musc cell contraction, cell division, and secretion of various substances

Question 27

protein linked receptors often involve ________

Answer 27

phosphorylation (tyrosine kinase)

Question 28

some proteins/receptors are located in the ___ or _____ of the target cell

Answer 28

cytoplasm or nucleus

Question 29

strong chemical bonds aka _______,

Answer 29

covalent (usually undesirable.

Question 30

what is a partial agonist, what are they good for?

Answer 30

when bound to receptor only produce a slight activation, a smaller response than an agonist. good for pts with withdrawl... help ween (can act as a competative antagonist)

Question 31

Buprenorphine is used to treat _____ addiction because...

Answer 31

morphine, bc it is a partial agonist

Question 32

Pindolol is used to _______, often categorized as a Beta blocker, but is in fact a _______

Answer 32

HTN, but it is a partial agonist -- prevents dangerous inc from sympathetic response

Question 33

antagonists do what?

Answer 33

have no action at all they inhib action of an agonist --- binds to either active or allosteric site

Question 34

physiologic vs chemical antagonist

Answer 34

phys: cause opposite effect of agonist chem: inactivates agonist before it has the opportunity to bind to the receptor

Question 35

a competative antagonist shifts the dose curve to the right which means...

Answer 35

it dec agonist potency without dec efficacy

Question 36

with noncompetative antagonists, the _______ is effected... additionally if it binds to the active site...._____

Answer 36

efficacy | if binds the active site, this is IRREVERSIBLE

Question 37

Describe the idea of spare receptors in a full response

Answer 37

ligand may be able to elicit a 50% response with <50% recpetors bound... if there are more receptors in the membrane than is needed fro a full response(like it's been upregulated) -common with hormones and NTs

Question 38

receptor mediated drug desensitization results in ____(fast/slow) change in the receptor via _____. Usually happens after taking _____(agonist/antagonist)

Answer 38

rapid change in receptor conformation agonist

Question 39

Slow longterm Desensitization can happen as a result of.....

Answer 39

a change in the number of receptors

Question 40

Non-drug mediated drug desnesitization can be dt ___ or _____

Answer 40

depletion of intracell 2nd messengers or signaling molecules | Increased rate of drug metabolism (P450 inducers met by P450 are met more quickly)

Question 41

_______ tend to desensitize receptors and _______ sensitize receptors/upregulate

Answer 41

agonists=desense | antagonists=upreg

Question 42

2 types of responses (drug responses)

Answer 42

quantal(all or none) and graded

Question 43

dose response curves plot ______ and ______

Answer 43

potency and efficacy

Question 44

define potency

Answer 44

amount of drug needed to ellict a response

Question 45

define efficacy

Answer 45

maximal response produced by a drug

Question 46

define affinity

Answer 46

probab of drug occupying a receptor at any given instance

Question 47

_____ and _____ are determined base don biofeedback and structure

Answer 47

affinity and efficacy

Question 48

what is the therapuedic window?

Answer 48

range of doses that the drug ellicits response without toxicity

Question 49

what does it mean if a drug has a narrow therapeudic index?

Answer 49

the toxic dose is close to the effective dose (digoxin)

Question 50

what is the therapeudic index(calc)

Answer 50

toxic dose in 50%/effective dose in 50%

Question 51

drugs with similar effects produce a ______ response

Answer 51

exaggerated

Question 52

drugs with opposing effects cause

Answer 52

diminshed or no response

Question 53

what are 3 changes seen in the elderly w/drug metabolism

Answer 53

``` inc sensitivity of receptor top drug (need to dec dose) dec capacity to respond to drug (need in dose) # or affinity of receptors may be reduced ```