Exam 1 - 1st half

Question 1

Pharmacokinetics

Answer 1

what the body does to the drug

absorption, distribution, metabolism, excretion

Question 2

Pharmacodynamics

Answer 2

what the drug does to the body

Question 3

Properties of drugs

Answer 3

drug size
shape (stereochemistry)
reactivity
hydrophobicity

Question 4

greater hydrophobicity means ____ ability to cross biological membranes

Answer 4

greater

Question 5

4 types of drug-receptor interactions

Answer 5

1. g protein couple receptors (main one)
2. ion channels
3. transmembrane with cytosolic domains
4. intracellular receptors

Question 6

g- protein coupled receptors act in ____ time

Answer 6

seconds to minutes

Question 7

examples of second messengers (2 of them)

Answer 7

cAMP

Ca2+ phosphoionisitide signaling

Question 8

ion channels act in ___ times

Answer 8

miliseconds (QUICK)

Question 9

3 KINDS of ion channels

Answer 9

ligand gated
voltage gated
second-messanger regulated

Question 10

ligand gated channels transmit signal across plasma membrane by _______ transmembrane conductance and changing ____ potential

Answer 10

ligand gated channels transmit signal across plasma membrane by increasing transmembrane conductance and changing membrane potential

Question 11

example of ligand-gated channels

Answer 11

nicotinic ACh receptor

Question 12

transmembrane receptors with cytosolic enzymatic domains (5 kinds)

Answer 12

1. receptor tyrosine kinase (insulin)
2. receptor tyrosine phosphatases (immunosuppression)
3. tyrosine kinase -associated
4. Ser/Thr kinases (cell growth)
5. guanylyl cyclases (smallest family)

Question 13

intracellular receptors (3 kinds)

Answer 13

1. enzymes
2. transcription factors
3. structural proteins

Question 14

actions of drugs NOT mediated by receptors (3 kinds)

Answer 14

1. antiacids
2. agents that affect osmolarity
3. chelatic agents

Question 15

greater potency the drug means the concentration needed for the response is

Answer 15

smaller

Question 16

what value does potency get associated with?

Answer 16

EC50

Question 17

the lower the EC50 the _____ the drug

Answer 17

more potent

Question 18

the higher the EC50 the ____ the drug

Answer 18

less potent

Question 19

Emax is known as

Answer 19

the maximum response

Question 20

partial agonists are ____ potent than standard agonsits

Answer 20

LESS

Question 21

antagonist is an agent that binds to a receptor but cannot produce the conformational change necessary to

Answer 21

trigger the downstream events

Question 22

competitive antagonists bind ____ to the receptor

Answer 22

REVERSIBLY

Question 23

With competitive antagonism what kind of shift in the curve do you see?

Answer 23

a shift to the right

Question 24

in competitive antagonist explain what happens to efficacy and potency

Answer 24

efficacy stays the same, potency goes DOWN

Question 25

non-competitive antagonists ____ the receptor, its a ____ action

Answer 25

non-competitive antagonists inactivates the receptor, its a non-reversible action

Question 26

in non-competitive antagonist explain what happens to efficacy and potency

Answer 26

potency stays the same and efficacy goes down

Question 27

physiological antagonism

Answer 27

agonist and antagonist acting at 2 independent sites, opposite effects

Question 28

chemical antagonism is caused by combination of

Answer 28

agonist with antagonist with resulting in inactivation of the agonist

Question 29

what are the advantages to the spar receptors

Answer 29

activation at low concentrations with faster turn of

Question 30

what is the most common mechanism that drugs pass membranes?

Answer 30

passive diffusion

Question 31

acidic drugs are better absorbed in the

Answer 31

stomach

Question 32

acids with accumulate in

Answer 32

basic compartments

Question 33

bases are absorbed in the

Answer 33

small intestine

Question 34

bases will accumulate in

Answer 34

acidic compartments

Question 35

bioavailability is the measure of the _____ of the orally administered drug that _____ systemic circulation

Answer 35

bioavailability is the measure of the percent of the orally administered drug that enters systemic circulation

Question 36

volume of distribution is related the blood _____ to the

Answer 36

blood concentration to the amount in the body

Question 37

what 2 properties determine Vd value

Answer 37

lipid solubility and binding to plasma proteins

Question 38

high lipid solubility means plasma concentration is low so the Vd is

Answer 38

a large value

Question 39

binding to plasma proteins typically results in a what Vd value?

Answer 39

a lower value

Question 40

what organ is the most important for excretion?

Answer 40

the kidney

Question 41

in renal golmerular filtration what drug is filtered?

Answer 41

only the unbound drug

Question 42

renal tubular secretion can be inhibited by what drug?

Answer 42

probenecid

Question 43

renal tubular reabsorption is influcened by what properties?

Answer 43

nonionized, lipid solubility

Question 44

adding sodium bicarbonate will allow trapping of what kind of drug in the urine ?

Answer 44

acidic drugs

Question 45

adding ammonium chloride will allow trapping of what kind of drug in the urine?

Answer 45

basic drugs

Question 46

phase 1 metabolism refers to what reactions?

Answer 46

oxidation, reduction, hydrolysis

Question 47

phase II metabolism referes to what?

Answer 47

functional groups being attached to the drug molecule

Question 48

zero order is constant ____ lost per unit time

Answer 48

constant amount lost per unit time

Question 49

first order is constant ___ is lost per unit time

Answer 49

constant fraction or % lost per unit time

Question 50

what is a good example of zero order

Answer 50

alcohol

Question 51

half life can only be determined for

Answer 51

1st order kinetics

Question 52

as 1/2 life increases what decreases?

Answer 52

ke (elimiation constant )

Question 53

the elimiation rate constant gives a measure of the

Answer 53

rapidity of the drug elimination

Question 54

steady state is when

Answer 54

rate of input and rate of ouptu per day are equal

Question 55

elimination kinetics control ____ kinetics

Answer 55

accumultion kinetics

Question 56

clearance is only for ____ order kinetics

Answer 56

1st order

Question 57

bioavailability is also known as the

Answer 57

area under the curve

Question 58

therapeutic index is an estimate of the ____ of the dose needed to produce ___ response from the dose that produces _____

Answer 58

therapeutic index is an estimate of the separation of the dose needed to produce desired response from the dose that produces toxicity

Question 59

problems with TI (4)

Answer 59

1. data must be collected in animals 2. applicability of animal data to humans is uncertain 3. ED50 is not a realistic dose, ED99 would be better 4. assumption is that ED and LD curves are parallel and this isn't always the case