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Pharm Block 1 > Drug metabolism > Flashcards

Drug metabolism Flashcards

1
Q

Processes that prevent continuous drug action

A

elimination/excreation

metabolism

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2
Q

Drug metabolites are usually more ________ then the drug ingested thus easliy excreated

A

poloar

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3
Q

most drugs enter the body _______ thus are difficult to excrete

A

lipophilic

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4
Q

In most cases metabolism will take active drug–>

A

inactive metabolite

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5
Q

A drug that is converted to active form by drug metabolizing enZ

A

prodrug

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6
Q

a prodrug is inactive until

A

metabolized

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7
Q

the more drugs we take the more at risk we are for

A

adverse affects

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8
Q

Drugs withdrawn from the market often d/t this reason

A

drug-drug interactions d/t drug metabolism

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9
Q

These guys do oxidation, reduction, dealkylation or hydrolysis

A

Phase I enZ

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10
Q

This enZ will often introdue or reaveal a functional group

A

Phase I enZ

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11
Q

Phase I enZ actions

A

oxidation, reduction, dealkylation or hyrolysis and introduce or reveal a functional group

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12
Q

These guys have conjugation of durg or durg metaboliet to endogenous substrate molecule

A

Phase II enZ

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13
Q

responsible for : Drug + conjugant–> Drug-conjugant

A

Phase II enZ

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14
Q

CYPs are examples of

A

Phase I enx

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15
Q

CYPs will often

A

make lipophilic drugs more soluble in water

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16
Q

These guys add large, polar conjugates to make drug super water soluble

A

phase II

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17
Q

Common location for drug metabolizing agents

A

portals of entry/exit
liver (HIGHEST)
GI, kidneys, lungs

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18
Q

Subcellularly where are the Phase I enZ located ?

A

In the SER microsomes

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19
Q

Subcellularly, where are phase II enZ located?

A

most are cytosilc

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20
Q

What venous system will take drugs to liver from the GI system

A

portal venous sytem

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21
Q

What drug administration is exposed to 1st pass effect

A

orally administered

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22
Q

Significant drug metabolism can occur before reaching general circulation d/t

A

first pass in intestines and liver

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23
Q

Drugs exposed to 1st pass will need _____ dose

A

higher

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24
Q

bioavialibty will ______ d/t first pass

A

lower F

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25
Q

F for IV administration

A

1 or 100%

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26
Q

What are two reasons for poor F

A

poor absorption or large first pass effect

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27
Q

Morphines’s F d/t first pass

A

.33

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28
Q

If i gave IV dose of 10 mg of morphine to relieve pain, what oral dose would i need to match that?

A

30 mg

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29
Q

Two key Phase I enZ

A

Cytochrome P450s = CYPs

Flavin-containing monooxygenases

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30
Q

Cytochrome P450s and Flavin-containing monooxygenases are examples of:

A

Phase I enZ

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31
Q

P450’s are anchored to:

A

outer face of ER

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32
Q

Core of P450’s

A

Fe

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33
Q

P450’s conjugate what to our substrates (drug)

A

O2 and we get S-OH +H20

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34
Q

P450 reductase use what to get the 2e- to add to our substrate?

A

NADPH –> NADP + 2e-

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35
Q

molecular ration of P450s per P450 reductase

A

10-20 P450s: 1 P450reductase

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36
Q

CYP stands for

A

cytochrome

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37
Q

CYP2B10: 2 stands for

A

gene family

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38
Q

CYP2B10: B stands for

A

Gene subfamliy

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39
Q

CYP2B10: 10 stands for

A

isoform

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40
Q

Human P450’s has _____ families

A

18

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41
Q

3 P450’s involved in drug metabolism

A

CYP1, CYP2, CYP3

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42
Q

There are _____ human P450 genes

with _____ of them involved in drug metabolism

A

57

15

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43
Q

Inidivudual differences in _____ result in big difference of catyltic activity and drub metabolism

A

isofrm

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44
Q

This CYP handles 50% of drug metabolism

A

CYP3A

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45
Q

CYP3A handles____ % drug metabolism

A

50

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46
Q

This cyp handles 25% drug metabolism

A

CYP2D6: DEPRESSENTS

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47
Q

This CYP handles 19% drug metabolizm

A

CYP2C19: includes warfarin, phenytoin

48
Q

Relative CYP isoform content does/does not equate to significance in role of drug metabolism

A

does not

49
Q

CYP 2D6 responsible for metabolism of _____%

and has ______% expression

A

25% drugs

1.5% is expressed

50
Q

FMO stands for

A

flavin-containig monooxygenase

51
Q

What are the substrates for flavin monooxygenase (FMO)

A

soft nucleophiles like N, SP or Se

52
Q

Does FMO react with endogenous soft nuecleophiles?

A

nope, just interacts with exogenous soft Nu’s

53
Q

what are expamples of endogenous soft nucelophiles

A

glutathione or cysteine

54
Q

FMO’s have broader or more specific substarte profile then P450’s

A

broader

55
Q

What type of products do Flavin-containing monooxygenases procude?

A

more polar and less toxic then CYPs

56
Q

What results in broad substrate range for FMO’s?

A

it’s hydorperoxyflavin intermediates

57
Q

What FMO is expressed in liver, brain and kidney?

A

FMO3

58
Q

FMO3 makes up 2-3% of protein in

A

kidney

59
Q

key FMO in liver

A

FMO3

60
Q

Glucuronidation, sulfination and Acetylation are exapmles of

A

phase II enZ

61
Q

UDP-glucoronic acid is example of

A

phase II enZ that does glucuronidation

62
Q

PAPS is used in

A

sulfination; a phase II enZ

63
Q

Acetyl Co-A involved in what?

A

acetylation in phase II enZ

64
Q

Gluthathione conjucation is type of

A

phase II enZ

65
Q

EnZ responsible for glucuronidation?

A

UDP-glucuronosyl transferase (UGT)

66
Q

EnZ responsible for acetylation

A

N-acetyltransferase (NAT)

67
Q

EnZ responsible for sulfination

A

Slufotransferases (SULT)

68
Q

EnZ responsible for Glutathione conjucation

A

Glutathione S- transfereases (GST)

69
Q

(NAT) stands for

A

N-acetyltransferase

70
Q

(SULT) stands for

A

Sulfotransferases

71
Q

(GST) stands for

A

Glutathione S- transfereases

72
Q

(UGT) stands for

A

UDP-glucuronosyl transferase

73
Q

IG, Phase II enZ makes metabolites more:

A

polar and less toxic

74
Q

NAT does what to metabolites

A

makes some more polar, others less polar but makes most less toxic

75
Q

Phase II enZ resposible for metabolism of almost half drugs

A

UGTs

76
Q

bilirubin is metabolized by which phse II enz

A

UGT’s

77
Q

What affects the Vmax of the Phase II enZ?

A

amount of conjugant available

78
Q

Glucuronidation has _____ conjugant capacity and ______ amt of raw materials for conjugation

A

High conjugation capacity

High amt of materials available

79
Q

Sulfonation has ______ conjugation capacity and ______ abundance of raw materials for conjucation available

A

Low conjucation capacity

low abundance of raw materials

80
Q

Gutathione conjucation has ______ conjucation capacity and _____ abundance of raw materials for conjucation

A 
low conjucgation capacity
low materials (humans have high GSH initially, but gets rapidly depleated)
81
Q

Two most common types of drug metabolism interactions:

A

EnZ induction

EnZ inhibition

82
Q

Exposure to certain drugs/enviro chemicals will upregulate durg metabolizing enZ amount and or activity via transcription increase:

A

EnZ Induction

83
Q

end result of enZ induction

A

more enZ d/t increased transcription = faster metabolism

84
Q

Ethanol is an inducer of:

A

CYP2E1

85
Q

Are Phase II enZ suseptible to enZ induction?

A

yes, UGTs and GST’s are induced by stuff like tobaccoo smoke, PAH or benzoapyrene

86
Q

A single inducer can affect _____ drugs handled by that enZ

A

many drugs

87
Q

EnZ indcuction increases

A

drug metabolism

88
Q

Induction has what sort of affect on drug effects

A

can increase or decrease them

–depends on if metabolite is inactive or active

89
Q

How long does induction take?

A

1-2 days

90
Q

Are inducers quantally equal?

A

no

91
Q

Inducers of specific isoforms (CYP isoforms) are substrates (T/F)

A

F: they may or may not be substrates

92
Q

T/F: all substartes are inducers

A

fales, NOT all substrates are inducers

93
Q

Some inducers are substartes (T/F)

A

true

94
Q

Inhibitors of drug metabolizing enZ will inhibit enZ activity, but not:

A

gene expression

95
Q

Drug inhibitors include:

A

competitive and non-competitive

96
Q

3 types of P450 Inhibitors

A

Competitive substrates
Bind CYP heme–distrupts catalytic activity (non-competitive)
Suicide inhibitors (irreversible and non-competitive)

97
Q

Major cauase of CYP releated drug interactions are due to:

A

competitive substrates

98
Q

By binding CYP heme, these P450 inhibitors will:

A

distrupt catalytic activity (non-competitive)

99
Q

How long does enZ inhibition take

A

immediate effect

100
Q

How much does inhibition affect drug metabolism

A

highly variabel: depends on enZ and inhibitor and could be small or large effect

101
Q

Serveral CYP2D6 inhibitors will reduce it’s activity to:

A

nearly zero

102
Q

Grapefruit juice will _______ drug absorption

A

INCREASE

103
Q

Grapefruit juice inhibits this intestinal CYP

A

CYP3A

104
Q

By inhibiting CYP3A, grapeftruit juice will

A

increase net amount abosorbed to general circulation

105
Q

the responsible ingrediant in grapefruit that inhibits intestinal CYP3A

A

furanocourmarin

106
Q

Grapefruit juice is a big no for this CYP that handles 50% of drug metabolizm

A

CYP3A

107
Q

FMO’s are _______induced or inhibited by clinically used drugs

A

NOT significantly

108
Q

These guys are less suseptible to competitive subtrate inhibition than P450’s

A

FMOs

109
Q

Whats the benefit to drugs that are handled by FMO’s

A

less potential for metabolic drug-drug interactions

110
Q

other factors that affect drug metabolism

A

age, genetics, disease states, gender

111
Q

most common cause of acute hepatic failure in US

A

acetaminophen use

112
Q

Second most common cause of liver fail requiring transplant

A

acetaminophen use

113
Q

First line Phase II’s that breakdown Acetaminiophen

A

SULT and UGT

114
Q

What CYP will act on acetaminophen

A

CYP2E1

115
Q

What will induce action of CYP2E1

A

ethenol

116
Q

Product of acetaminophen–> CYP2E1 is

A

toxic and needs to be broken down by GST

Pharm Block 1 (23 decks)

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