Brainscape's Knowledge GenomeTM

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


See full index

FMS > FMS week #4 > Flashcards

FMS week #4 Flashcards

1
Q

Which routes of drug administration might have 1st pass metabolism

A

oral, rectal, sublingual

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

Route of drug administration with most rapid onset of action

A

IV

also 100% bioavailable

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

What are pros and cons of intrathecal drug administration

A

bypass blood-CSF & blood-brain barriers

risks of infection & headache

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

bioavailability is influenced by (3 categories)

A

physiological, physiochemical, and biopharmaceutical factors

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

Fick’s law determines

A

Rate of diffusion

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

When pH

A

protonated form (HA and BH+)

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

When pH>pKa, ______ form predominate

A

unprotonated (A- and B)

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

What is the partition coefficient?

A

states how soluble a drug is in a lipid membrane

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

ABC family of transporters

A

ATP-Binding Cassettes. family of transporters (ie. P-glycoproteins - oppose drugs from entering cells)

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

4 physiological factors that affect GI absorption

A
  1. Surface area
  2. GI pH
  3. GI motility/gastric emptying]
  4. Blood flow
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Where is the primary site of biotransformation

A

liver

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

Microsomal hepatic sites of drug metabolism

A

vesicles rich in smooth ER; contain enzymes that catalyze oxidation reactions and glucorinide conjugation

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

Non-microsomal hepatic sites of drug metabolism

A

occurs mostly in cytosol; some enzymes display important genetic polymorphisms

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

Enterohepatic cycling

A

when drugs are excreted into the gut via bile and are reabsorbed

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

Only (bound/unbound) drugs in plasma can penetrate cell membranes

A

unbound

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

What type of drugs tend to bind to albumin

A

neutral acid & base

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

Basic drugs commonly bind to:

A

globulins

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

What are 2 physiochemical characteristics of drugs affected distribution?

A

pKa & partition coefficient

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

What are 2 cardiovascular factors that affect drug distribution?

A

cardiac output & regional blood flow

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

What are some tissue-dependent factors that affect drug distribution?

A

pH gradient, active transport, non-specific binding, dissolution in fat, drug reservoirs

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

Why is drug distribution different across the blood brain barrier?

A

a. CNA capillaries are not fenestrated
b. tight junctions & basal lamina of cerrebal endothelial cells resist the movement of water-soluble and ionized drugs into CNS
c. brain capillary endothelial cells express ATP-driven drug efflux pumps
d. CSF proteins do not function as drug reservoir

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

Why is drug distribution different across the placenta?

A

distribution by simple simple diffusion; nutrients & drugs of abuse readily cross placenta

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

Elimination is ______ related to stead state concentration in blood

A

inversely

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

Volume of distribution

A

the volume of fluid that would be needed to contain the administered amount of drug at the concentration measured in blood or plasma

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

Volume of distribution is _____ proportional to the concentration of the drug measured in the blood

A

inversely

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

Volume of distribution is _____ proportional to the total amount of drug administered

A

directly

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

What is first-pass metabolism?

A

biotransformation of a drug prior to its entry into the systemic circulation (usually to a less active compound)

usually in liver, sometimes SI

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

What occurs in Phase I metabolism?

A

introduce/unmask a polar functional group

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

Mixed Function Oxidases (MFOs) are found in Phase I/II?

A

Phase I

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

Cytochrome P450 is found in Phase I/II?

A

Phase I

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

Glucuronidation reactions occur in Phase I/II?

A

Phase II

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

What occurs in Phase II metabolism?

A

conjugation and synthetic reactions; addition of an acid or amino acid; glucuronidation

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

How does inhibition modify metabolism of drug

A

competitive inhibition

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

How does induction modify metabolism of drug?

A

either increases synthesis or blocks breakdown

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

How do hepatitis, cirrhosis, liver cancer affect drug metabolism?

A

They impair microsomal oxidases

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

How does cardiac dysfunction affect drug metabolism?

A

leads to reduced hepatic blood flow, which affects metabolism of drugs that are flow-limited

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

As renal function decreases, plasma 1/2-life ______

A

increases

38
Q

Therapeutic window is

A

the range of concentrations between the therapeutic concentration and the toxic concentration

39
Q

In a first order reaction, rate of metabolism is _____ proportional to concentration

A

directly

40
Q

First order reactions generally occur when relatively low/high substrates

A

low

41
Q

How are first order reactions eliminated?

A

at a fixed percentage per time

42
Q

Zero order reactions occur when drug concentration is relatively low/high

A

high

43
Q

How are zero-order reactions eliminated?

A

at a fixed amount/time

44
Q

How do calculate maintenance dose? (not the actual equation detials)

A

loading dose - amount that’s been eliminated

45
Q

elimination 1/2-life is (dependent/independent) of dose/concentration?

A

independent

46
Q

1/2-life is ______ proportional to clearance

A

inversely

47
Q

1/2-life is ______ proportional to Vd/Cl,

A

directly

48
Q

decreased hepatic/renal function will increase/decrease rate of elimination

A

decrease

49
Q

Concentration of drug present is ____ related to volume of distribution in an IV administration

A

inversely

50
Q

dose, dosage interval, and 1/2-life determine

A

Drug plateau level

51
Q

T/F dose determines time it takes to reach plateau

A

FALSE

52
Q

Define agonist

A

a drug that mimics the effects of the endogenous ligand for a receptor

53
Q

A full agonist has an intrinsic value of _

A

1

54
Q

A _____ agonist cannot elicit the maximum response of tissue

A

partial

55
Q

What is an inverse agonist

A

it causes inhibtion of agonist-independent activity; long term treatment with inverse agonists may lead to receptor up-regulation

56
Q

A drug (which does not itself have intrinsic activity) that interferes with binding of endogenous ligand (or an agonist) to a receptor

A

antagonist

57
Q

Antagonists have an intrinsic activity of _

A

0

58
Q

What does a competitive antagonist do?

A

binds to same site so agonist cannot bind

changes Kd but NOT maximum response

59
Q

What does a noncompetitive antagonist do?

A

binds to non-binding site but makes it so agonist cannot bind

decreased maximum response, but Kd stays the same

60
Q

Affinity is determined by

A

interacting sites and types of forces involved in binding interactions

61
Q

Kd is the?

A

concentration of drug when 1/2 total # receptors are bound b drug

62
Q

Lower molar concentration value of Kd, the higher/lower affinity for the receptor

A

higher

63
Q

ability of a receptor to elicit a response without outside factors

A

intrinsic activity

64
Q

strongest

A

correct

65
Q

Receptor down-regulation occurs in hours-days or secs-mins?

A

hours-days

66
Q

Receptor _________ involves receptor phosphorylation

A

desensitization

67
Q

receptor desensitization _____ affinity and ____ # receptors

A

decreases and does not change

68
Q

in sigmoid concentration curves, drugs with higher affinity are shifted to the left/right

A

left

69
Q

T/F a partial agonist will reach the maximum response

A

F

70
Q

T/F a competitive antagonist will change the Kd

A

F; will change Kd though

71
Q

T/F noncompetitive antagonist will change the Kd

A

F; will decrease maximum response though

72
Q

The influence of genetic variability on drug responses (both therapeutic and toxic drug responses)

A

pharmacogenetics

73
Q

the use of genetic information to predict drug responses

A

pharmacogenomics

74
Q

Which Cytochrome P450 is involved in metabolism of 20-25% of all meds?

A

2D6

75
Q

Described poor metabolizers

A

PM’s have deceased metabolism & clearance, increased elimination 1/2-life

will get higher drug plasma levels, increased risk fo drug-related side effects

need reduced drug dose

76
Q

Describe intermediate metabolizers

A

might need slightly lower dose

77
Q

describe intermediate metablizors

A

Usually ok with standard dose of drug

78
Q

Describe ultrarapid metabolizers

A

Have increased metabolism & clearance; decreased elimination 1/2-life

have low plasma drug levels, risk losing drug efficacy

Need a higher dose

79
Q

What is Tamoxifen?

A

Pro-drug that treats Estrogen positive tumors

Converted to Endoxifen via CYP2D6 & CYP3A4/5

PM’s have reduced drug efficacy of tamoxifen bc can’t convert as well to endoxifen

80
Q

codeine is a pro-drug for ______ via which CYP?

A

morphine;n 2D6

81
Q

Normally, __% of administered codeine gets converted to morphine

A

5-10%

82
Q

UM’s are at an increased/decreased risk for drowsiness and respiratory depression

A

increased

83
Q

What is Isoniazid?

A

drug used in TB treatment

84
Q

How is Isonizid metabolized?

A

via N-Acetyletransferase (NAT)

[phase II enzyme]

85
Q

Slow/fast acetylators are more likely to suffer from isoniazid toxicity (ie. peripheral neuropathy)

A

slow

86
Q

Thiopurine drugs are used for….

A

autoimmune conditions, acute, lymphoblastic anemia, preventing organ rejection

87
Q

Which forms of thiopurine drugs have desired effect?

A

6-TGNs

88
Q

Thiopurine drugs are inactivated by

A

TMPT

89
Q

If TMPT activity too high, might have to…

A

give higher dose of thiopurine drugs

90
Q

if individual has reduced undetectable TMPT activity, what will happen?

A

increased potential for life threatening adverse events (myelosuppression, bleeding, severe infection)

91
Q

Why is G6PD important?

A

only source of NADPH and GSH in RBC’s, which are necessary for reduction

no reduction–> increased risk for hemolysis when exposed to oxidative stress

92
Q

Why do you get hemolysis in those that are G6PD deficient?

A

products of rasburicase breakdown include allantoin and hydrogen peroxide, which the body cannot handle if no antioxidants such has NADPH and GSH around

FMS (3 decks)

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