Exam 1 - 1st half Flashcards Preview

Intro to Pharm > Exam 1 - 1st half > Flashcards

Flashcards in Exam 1 - 1st half Deck (59):
1

Pharmacokinetics

what the body does to the drug
absorption, distribution, metabolism, excretion

2

Pharmacodynamics

what the drug does to the body

3

Properties of drugs

drug size
shape (stereochemistry)
reactivity
hydrophobicity

4

greater hydrophobicity means ____ ability to cross biological membranes

greater

5

4 types of drug-receptor interactions

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

6

g- protein coupled receptors act in ____ time

seconds to minutes

7

examples of second messengers (2 of them)

cAMP
Ca2+ phosphoionisitide signaling

8

ion channels act in ___ times

miliseconds (QUICK)

9

3 KINDS of ion channels

ligand gated
voltage gated
second-messanger regulated

10

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

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

11

example of ligand-gated channels

nicotinic ACh receptor

12

transmembrane receptors with cytosolic enzymatic domains (5 kinds)

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)

13

intracellular receptors (3 kinds)

1. enzymes
2. transcription factors
3. structural proteins

14

actions of drugs NOT mediated by receptors (3 kinds)

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

15

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

smaller

16

what value does potency get associated with?

EC50

17

the lower the EC50 the _____ the drug

more potent

18

the higher the EC50 the ____ the drug

less potent

19

Emax is known as

the maximum response

20

partial agonists are ____ potent than standard agonsits

LESS

21

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

trigger the downstream events

22

competitive antagonists bind ____ to the receptor

REVERSIBLY

23

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

a shift to the right

24

in competitive antagonist explain what happens to efficacy and potency

efficacy stays the same, potency goes DOWN

25

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

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

26

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

potency stays the same and efficacy goes down

27

physiological antagonism

agonist and antagonist acting at 2 independent sites, opposite effects

28

chemical antagonism is caused by combination of

agonist with antagonist with resulting in inactivation of the agonist

29

what are the advantages to the spar receptors

activation at low concentrations with faster turn of

30

what is the most common mechanism that drugs pass membranes?

passive diffusion

31

acidic drugs are better absorbed in the

stomach

32

acids with accumulate in

basic compartments

33

bases are absorbed in the

small intestine

34

bases will accumulate in

acidic compartments

35

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

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

36

volume of distribution is related the blood _____ to the

blood concentration to the amount in the body

37

what 2 properties determine Vd value

lipid solubility and binding to plasma proteins

38

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

a large value

39

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

a lower value

40

what organ is the most important for excretion?

the kidney

41

in renal golmerular filtration what drug is filtered?

only the unbound drug

42

renal tubular secretion can be inhibited by what drug?

probenecid

43

renal tubular reabsorption is influcened by what properties?

nonionized, lipid solubility

44

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

acidic drugs

45

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

basic drugs

46

phase 1 metabolism refers to what reactions?

oxidation, reduction, hydrolysis

47

phase II metabolism referes to what?

functional groups being attached to the drug molecule

48

zero order is constant ____ lost per unit time

constant amount lost per unit time

49

first order is constant ___ is lost per unit time

constant fraction or % lost per unit time

50

what is a good example of zero order

alcohol

51

half life can only be determined for

1st order kinetics

52

as 1/2 life increases what decreases?

ke (elimiation constant )

53

the elimiation rate constant gives a measure of the

rapidity of the drug elimination

54

steady state is when

rate of input and rate of ouptu per day are equal

55

elimination kinetics control ____ kinetics

accumultion kinetics

56

clearance is only for ____ order kinetics

1st order

57

bioavailability is also known as the

area under the curve

58

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

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

59

problems with TI (4)

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