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Patho > Exam 3 metabolism > Flashcards

Exam 3 metabolism Flashcards

1
Q

CYP3A4 substrates

A

midazolam, indinavir

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2
Q

CYP3A4 inhibitors

A

ritonavir, ketoconazole

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3
Q

CYP3A4 inducers

A

rifampin and St. Johns Wort

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4
Q

CYP2D6 substrates

A

codeine, fluoxetine

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5
Q

CYP2D6 inhibitors

A

fluoxetine, quinidine

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6
Q

CYP2D6 inducers

A

clinical relevance

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7
Q

CYP2C9 substrates

A

S-warfarin, ibuprofen

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8
Q

CYP2C9 inhibitors

A

fluconazole, amiodarone

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9
Q

CYP2C9 inducers

A

rifampin, secobarbital

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10
Q

what are the 6 sites for drug metabolism

A

liver, GI tract, lungs, kidneys, brain and skin

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11
Q

what is the most important site for drug metabolism

A

liver

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12
Q

what makes the liver the most important site for drug metabolism

A

the high concentration of drug metabolizing enzymes

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13
Q

what is Phase I of drug metabolism

A

chemical modification to introduce new functional groups or expose a group for Phase II

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14
Q

what is Phase II of drug metabolism

A

conjugation of polar group with drug

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15
Q

what is the most common reactions in Phase I of drug metabolism

A

oxidation

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16
Q

what catalyzes the drugs in Phase I

A

cytochrome P450 (CYP), NADPH and oxygen

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17
Q

what causes the metabolite to be excreted out of Phase I

A

highly polar

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18
Q

what membrane anchored protein is needed before P450 is utilized

A

P450 reductase

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19
Q

what other potential protein is involved in electron transfer to P450

A

cytochrome b5

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20
Q

CYPs are subdivided according to their amino acid identity into

A

families and subfamilies

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21
Q

what order do you name CYPs

A

CYP-family-subfamily-individual gene

22
Q

how many CYP genes do humans have

A

57

23
Q

T/F P450 enzymes are able to metabolize a vast spectrum of structurally diverse compounds

A

TRUE

24
Q

what does the active site of CYP contain

A

an iron-heme cofactor

25
Q

what is reversible inhibition

A

reversible inhibitors compete with other substrates for occupancy of active site

26
Q

what are the factors that determine binding strength

A

coordination strength with heme, hydrophobic contact with binding site, and specific contact with binding site residues

27
Q

what molecule allows stronger affinity to heme

A

nitrogen

28
Q

what is an example of the metabolite being the inhibitor

A

erythromycin

29
Q

what is an example of a metabolite that inhibits one drug but not the other in the same gene

A

cimetidine inhibits warfarin but not ibuprofen

30
Q

what is mechanism based inhibition

A

metabolite of substrate generates reactive metabolite that irreversibly interacts with the heme

31
Q

increased CYP450 does what to metabolism

A

increases it

32
Q

what does cross talk mean

A

it can induce multiple genes

33
Q

once a drug reaches initial plateau the concentration declines after continued use why

A

production of P450s is increased and metabolizes the drug faster

34
Q

the consequences of inhibition or metabolism is determined by which species is

A

active

35
Q

what are the 3 most important CYP genes

A

CYP2C8/9, CYP2D6 and CYP3A4/5

36
Q

CYP1A subfamily metabolizes

A

PAHs, arylamines and nitrosamines

37
Q

which CYP subfamily metabolizes 20-25% of clinically important drugs

A

CYP2C

38
Q

T/F CYP2C9 has a bigger pocket so more variety of substrate can bind

A

TRUE

39
Q

T/F CYP3A4 has the biggest pocket

A

TRUE

40
Q

CYP3A has an inhibitor that will not inhibit all the substrates due to

A

multiple binding spots due to largest pocket

41
Q

CYP2D6 metabolizes about what percent of clinically important drugs

A

20

42
Q

CYP3A4 metabolizes what percent of clinically important drugs

A

50

43
Q

T/F CYP3A4 has low substrate specificity

A

TRUE

44
Q

Phase II reactions couples drugs or activates drugs with

A

conjugates

45
Q

Drug conjugates of Phase II display

A

increase water solubility and decreased lipid solubility

46
Q

what are the most common Phase II metabolites

A

UGTs, SULTs, GSTs, NATs, and TPMTs

47
Q

UGT conjugates glucuronic acid a component of

A

UDPGA

48
Q

UGT and CYP450 are spatially co-localized on the ER why

A

to move from Phase I to II fast

49
Q

SULTs are for

A

steroid hormones

50
Q

GSTs are for

A

anticancer drugs

51
Q

what would be the consequence of pretreatment with a drug that consumed PAP followed by administration of a drug undergoing sulfation

A

no sulation

Patho (11 decks)

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