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PFM: Biweekly Exam 3 > ILA: Drug Metabolism CYTP450 > Flashcards

ILA: Drug Metabolism CYTP450 Flashcards

1
Q

2 ways a drug can be inactivated

A
  1. metabolism
  2. excretion
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2
Q

primary site for metabolism of drugs

A

hepatocyte

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3
Q

T or F: Drugs are toxins

A

True

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4
Q

what induces metabolism that handles drug elimination

A

enzymes

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5
Q

Phase 1 of detoxification in hepatocyte

A

oxidation/reduction, hydrolysis

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6
Q

goal of phase I of detoxification:

A

water solubility!!!! (always) + drug activation (sometimes)

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7
Q

Phase 2 of detoxification in hepatocytes

A

conjugation

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8
Q

goal of phase 2 of detoxification:

A

drug inactivation!!!! + water solubility

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9
Q

Phase 3 of detoxification in hepatocytes

A

excretion (into bile)

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10
Q

in phase 1, what does making drugs water soluble mean

A

drugs will stay longer in the bloodstream; increase effectiveness and minimize SE

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11
Q

in phase 1, bile acid oxidation happens by what

A

CYPs (cytochrome P450) enzymes

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12
Q

one CYP often can metabolize______ drugs

A

many

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13
Q

one drug can be metabolized by _______ CYPs

A

several

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14
Q

CYP2C9
CYP2C19
CYP2D6
CYP34A

A

CYPs in Phase 1

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15
Q

substrate for CYP2C9 enzyme

A

warfarin (anti-coagulant)

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16
Q

substrate for CYP2C19

A

omeprazole (PPI)

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17
Q

substrate for CYP2D6

A

codeine

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18
Q

substrate for CYP34A

A

amiodarone (slows HR)

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19
Q

location of CYP450s in phase 1

A

smooth ER

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20
Q

in phase 1, activation of codeine to morphine is done by what enzyme

A

CYP2D6

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21
Q

in phase 1, activation of clopidogrel is done by what enzyme

A

CYP2C19

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22
Q

simvastatin is a substrate of what CYP enzyme

23
Q

this enzyme is responsible for simvastatin’s elimination

24
Q

what juice inhibits CYP3A4

A

grapefruit juice

25
Q

if someone drinks grapefruit juice while taking a simvastatin, what happens

A

simvastatin elimination will be lower, and its plasma concentration will exceed MTC—–causing toxicity

26
Q

inducer of CYP3A4

A

St. John’s Wort

27
Q

what happens when someone take St. John’s Wort (antidepressant) while on simvastatin

A

simvastatin elimination will be higher, and its plasma concentration will not even reach MEC, meaning the drug will not work

28
Q

St. John’s Wort
Rifampin
Griseofulvin

Phenobarbital
Phenytoin
Carbamazepine

A

CYP3A4 inducers (decrease effectiveness of drug)

29
Q

grapefruit juice
cimetidine

ciprofloxacin
erythromycin

ketoconazole

A

CYP3A4 inhibitors (increase toxicity)

30
Q

Warfarin metabolized by

31
Q

what inactivates CYP2C9

A

Cimetidine

32
Q

Warfarin + Cimeditine=

33
Q

erythromycin inhibits what

34
Q

erythromycin + warfarin=

35
Q

basically, if warfarin (anticoagulant) is unable to be eliminated, it reaches MTC and has what toxic effect

36
Q

what two drugs raise each other’s levels (they do the same thing)

A

erythromycin and ketoconazole

37
Q

erythromycin and ketoconazole together increase the risk of long what

A

long QT (ventricular depolarization)

38
Q

long QT + long QT=

A

Torsades de Pointes (ventricular tachycardia)

39
Q

what happens before heart goes into V-fib

A

Torsades de Pointes (ventricular tachycardia)

40
Q

clopidogrel is bioactivated by what

41
Q

CYP2C19 is inactivated by its substrate

A

omeprazole

42
Q

omeprazole + clopidogrel=

A

platelet aggregation (no active form of clopidogrel—blood thinner)

43
Q

grapefruit juice + statins=

A

myopathy, including rhabdomyolysis (muscle breakdown)

44
Q

rifampin induces what

45
Q

hormones in birth control pills are degraded by what

46
Q

rifampin + oral contraceptive=

47
Q

phase 2 deals with conjugation by what enzyme

A

transferases

48
Q

major transferase in phase 2 that is located in ER

A

glucuronidation

49
Q

what is (UDP-glucuronosyltransferases, UGTs)

A

another name for glucuronidation that is used to inactivate drugs in phase 2

50
Q

how does glucuronidation make drug inactivated

A

basically makes the drug extremely water soluble, so it can be excreted

51
Q

Gemfibrozil inhibits uptake of ______ into hepatocytes in phase 2

52
Q

when statin levels rise in plasma, it leads to ______

A

rhabdomyolysis

53
Q

gemfribrozil + simvastatin=

A

myoglobinuria

PFM: Biweekly Exam 3 (20 decks)

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