Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PHARM 203 > Core Principles of Drug Action > Flashcards

Core Principles of Drug Action Flashcards

1
Q

what drugs do to your body

A

pharmacodynamics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what your body does to drugs

A

pharmacokinetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

_____ is the chemical control of physiology

A

pharmacology

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

binding of drug and protein results in a

A

complex

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

ligand refers to

A

any small molecule that binds to a protein

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

allosteric effect

A

a drug that binds to the target at a different site from the endogenous ligant and affects the protein’s ability to respond

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

NAMs

A

negative allosteric modulators

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

ligand that binds but doesn’t activate the receptor, just prevents agonist binding

A

antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

the majority of drugs that bind to receptors are

A

antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

almost all endogenous ligands are

A

agonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

most ligands bind ____ to proteins

A

reversibly

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

most irreversible drugs are

A

enzyme inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

aspirin targets

A

COX

irrev

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

omeprazol targets

A

H”K” ATPase

irrev

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

tranylcypromine targets

A

MAO- antidepressant

irrev

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

higher affinity means

A

tighter binding = effective at lower concentrations = more potent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

drugs with different affinities have ______ number of collisions

A

the same

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

drug concentration and target occupation have a _________ relationship

A

hyperbolic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

a lower Kd means

A

higher affinity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Hill-langmr equation

A

b/Bmax = [L]/(Kd+[L])

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

diphenhydramine is a

A

histamine antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

diphenhydramine has side effects due to

A

small affinity for ACh receptors (binds preferentially to H receptors (lower Kd))
- more side effects seen with higher concentratiosn

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

when there is competition for a common binding site, there is a _____ in collisions of each ligand, but an _____ in total number of collisions

A

decrease for each

increase for total

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

if the drug is an agonist, then the overall effect of natural agonist + drug is

A

increased receptor stimulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

if the drug is an antagonist then the overall effect of natural agonist + drug is

A

decreased receptor stimulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

drugs competing for binding site results in

A

increased levels of both drugs

- not being metabolised as fast because need to share binding site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

how can you reduce inactivation of an expensive drug

A

put in another drug that competes with it for the same enzyme

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

ability of agonist to evoke a response in a tissue

A

efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

angatonists have ___, while agonists have _____ and ____

A

affinity

affinity and efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

receptors that are not required are called

A

spare receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

what is the function of spare receptors

A

so that the cell can generate the same response with less endogenous ligand release = metabolic efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

agonist binds to receptor, isomerisation to form higher affinity bonds, then isomerised receptor is active

A

two state induced fit model

can also happen with antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

conformational selection

A

agonist binds preferentially to active conformation and shifts the equilibrium so that more receptor exists in the activated conformation
proteins are not static

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

tachyphylaxis is

A

receptor desensitisation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

rebound vasodilation is a result of

A

receptor desensitisation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

partial agonists elicits a ___ than maximal effect even when all receptors are occupied

A

smaller

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

partial agonists can behave as both

A

agonists and antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

inverse agonists have a higher affinity for the

A

inactive form of the receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

most drugs classed as antagonists at receptors that show conformational selection behaviour are probably

A

inverse agonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

prolonged therapeutic effects happen when

A

drugs are irreversible

typically TE mirrors amount of drug in the body

41
Q

net movement of drug frm site of admin into bloodstream

A

absorption

42
Q

net movement of drug from bloodstream into organs and tissues

A

distribution

43
Q

enteral

A

PO or PR

- has first pass loss

44
Q

parenteral

A

bypassing the intesting

IV, IM, SC, topical, transdermal, inhalation, buccal, sublingual

45
Q

drugs with high lipid solubility pass cell membranes quickly because of ___ law of ____

A

fick’s law of diffusion

- larger concentration gradient in cell membrane

46
Q

Pka is the pH at

A

which 50% of the drug is ionised

47
Q

formulation used to optimise absorption include

A

drug size
protective coatings
sustained release pellets
depot injections

48
Q

a formulation of larger # of small particles results in

A

faster higher peak

49
Q

all drugs absorbed from the stomach and intestines must enter the

A

portal vein to go to the liver

50
Q

after first pass metabolism, oral drugs may pass through the liver once every ___ circults

A

4

51
Q

the fraction of an oral dose of drug that reaches the systemic circulation as an intact drug

A

oral bioavailability

52
Q

what causes a higher apparent volume of blood

A

more drug distribution

53
Q

the larger the volume of distribution, or the smaller the fraction of the dose that remains in the blood, the ____ it takes to remove the drug from the body

A

longer

54
Q

AVd

A

apaprent volume of plasma

55
Q

plasma albumin has __ drug binding sites

A

2

56
Q

alpha1-acid glycoprotein has ___ drug binding site

A

1

57
Q

competition for plasma protein binding results in

A

drug-drug interactions + can’t diffuse into cell

- may cause side effects as less of singular drug can be bound when there’re 2

58
Q

majority of drug elimination is from

A

urine and feces

59
Q

3 parts of renal drug elimination

A
  1. bowman’s capsule
  2. acid/ base transporter pumps
  3. lipid soluble drug reabsorbed at descending loop onwards
60
Q

lipid soluble drug srequire metabolism by

A

helatic metabolism

61
Q

metabolism does deactivate/ detoxify drugs T or F

A

F- not necessarily

62
Q

phase 1 metabolism is

A

functionalization

63
Q

phase 2 metabolism is

A

connjugation

64
Q

where does hepatic metabolism occur

A

hepatocytes

65
Q

phase 1 reactions include

A

oxidations, reductions, hydrolysis, hydration, isomerisations, dealkylations

66
Q

cytochrome P450 enzymes are used in which phase

A

1

67
Q

most prominant cyp450 enzymes

A

3A4/5/7 and 2D6- most drugs metabolized

68
Q

conjugation reactions usually involve

A

attaching a large, water soluble molecule to a drug or phase 1 metabolite

69
Q

glucuronidation enzyme

A

UDP glucuronyl transferase- adds glucuronic acid (a sugar)

70
Q

sulfation enzyme

A

sulfotransferase - adds sulfate

71
Q

acetylation enzyme

A

N-acetyl transferase - adds acetyl

72
Q

glutathionylation enzyme

A

glutathione S transferase- adds glutathione (tripeptide)

73
Q

which predominantes at low [drug] glucuronidation or sulfation

A

sulfation

74
Q

where is UGT found

A

throughout body- high levels in liver smooth ER

75
Q

where are SULTs found

A

mainly in cytosol of hepatocytes

76
Q

N-acetyl transferases (NAT1 and NAT2 are found)

A

in Kupffer cells of the liver

77
Q

acetylation is a common conjugation pathway for

A

aromatic amines, hydrazines, and sulfonamide antibacterial drugs

78
Q

which NAT is an example of genetic polymorphism

A

NAT2

79
Q

which phase 2 metabolism makes drugs less water soluble

A

acetylation

80
Q

which phase 2 reaction is a protective mechanism against electrophilic species

A

glutathione conjugation

81
Q

glutathione is made of

A

glu-cys-gly

82
Q

NAPQI is the

A

hepatotoxic metabolite of acetaminophen

83
Q

what part of glutathione reacts with electrophilic species

A

thiol

84
Q

N acetyl cysteine and methionine are added with acetaminophen to

A

protect against overdose- reacts nonenzymatically at high concentrations with NAPQI

85
Q

elimination can be an unchanged drug or a drug’s enzymeatic metabolite

A

T

86
Q

efficacy of drug elimination is measured as

A

drug clearance

87
Q

first order drug elimination is ______ and has an ___ curve

A

concentration dependent

exponential

88
Q

Kel

A

first order elimination rate constant

89
Q

Kel=

A

Ln2/T1/2

90
Q

clearance =

A

ADv * Kel

91
Q

the ____ curve is a mirror image to the first order elimination curve for the same drug

A

infusion

92
Q

how many half lives to reach steady state

A

5

93
Q

Css is an ____

A

average

94
Q

IV injections have ___ where as smoothing is seen with ___ dosing

A

spikes

oral

95
Q

smoothing is exaggerated with

A

sustained release preparation

96
Q

a range of plasma concentratiosn within which a TR is obtained but without serious side effects

A

therapeutic window

97
Q

if cyp is irreversibly inhibited

A

increased bioavailability and Css

decreased clearance, Kel

98
Q

to reduce fluctuations without changing dosing rate

A

choose a different dosing regimen- shorter time between each dose + smaller doses

99
Q

drugs that are rapidly metabolized by the kidneys have a ____ clearance rate

A

higher

PHARM 203 (21 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions