Quiz #01 Flashcards

1
Q

Which are the only (3) CYP enzymes that exhibit polymorphisms?

A

2C9
2C19 (more common in Asians)
2D6 (more common in Caucasians)

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2
Q

Which of the following would have a rapid onset typically within 24 hrs?

A. Enzyme induction
B. Enzyme inhibition

A

B. Onset of enzyme inhibition is more rapid than enzyme induction.

Enzyme inhibition is faster b/c it involves the drug binding with the enzyme, thereby preventing its function, whereas enzyme induction requires increased synthesis of the enzyme (a slower process).

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3
Q

Carbamazepine

give the brand name, state whether it’s an inducer, inhibitor and/or substrate of any CYP enzyme

A

Tegretol®

3A4 inducer
2C9 inducer
1A2 inducer

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4
Q

Phenytoin

A

Dilantin®

3A4 inducer
2C9 inducer
2C9 substrate
2C19 substrate
1A2 inducer
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5
Q

Phenobarbital

A

Luminal®

3A4 inducer
2C9 inducer
1A2 inducer

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6
Q

Rifampin

A

Rifadin®

3A4 inducer
2C9 inducer
1A2 inducer

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7
Q

Nafcillin

A

3A4 inducer

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8
Q

Dexamethasone

A

3A4 inducer

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9
Q

St. John’s wort

A

3A4 inducer

1A2 inducer

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10
Q

Itraconazole

A

Sporanox®

3A4 inhibitor

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11
Q

Ketoconazole

A

Nizoral®

3A4 inhibitor
2C19 inhibitor

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12
Q

Voriconazole

A

Vfend®

3A4 inhibitor
2C9 inhibitor
2C19 inhibitor

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13
Q

Fluconazole

A

Diflucan®

3A4 inhibitor (only at high doses)
2C9 inhibitor
2C19 inhibitor

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14
Q

HIV Protease Inhibitors

Atazanavir
Nelfinavir
Ritonavir
Saquinavir

A

Atazanavir - Reyataz®
Nelfinavir - Viracept®
Ritonavir - Norvir®
Saquinavir - Invirase®, Fortovase®

3A4 inhibitors
2C9 inhibitor (ritonavir)
2D6 inhibitor (ritonavir)
1A2 inducer (ritonavir)
1A2 inhibitor (atazanavir)
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15
Q

Clarithromycin

A

Biaxin®

3A4 inhibitor
1A2 inhibitor

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16
Q

Erythromycin

A

Erythrocin®

3A4 inhibitor
1A2 inhibitor

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17
Q

Diltiazem

A

Cardizem®

3A4 inhibitor
3A4 substrate

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18
Q

Verapamil

A

Calan®

3A4 inhibitor
3A4 substrate

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19
Q

Amiodarone

actually the active metabolite of amiodarone - desethylamiodarone

A

Cordarone®, Pacerone®

3A4 inhibitor
2C9 inhibitor
2D6 inhibitor
P-gp inhibitor

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20
Q

Alprazolam

A

Xanax®

3A4 substrate

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21
Q

Midazolam

A

Versed®

3A4 substrate

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22
Q

Felodipine

A

Plendil®

3A4 substrate

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23
Q

Nifedipine

A

Procardia®

3A4 substrate

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24
Q

Triazolam

A

Halcion®

3A4 substrate

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25
Q

Simvastatin

A

Zocor®

3A4 substrate
2C9 inhibitor

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26
Q

Atorvastatin

A

Lipitor®

3A4 substrate

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27
Q

Lovastatin

A

Mevacor®

3A4 substrate
2C9 inhibitor

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28
Q

Cyclosporin

A

Neoral®, Sandimmune®

3A4 substrate

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29
Q

Tacrolimus

A

Prograf®

3A4 substrate

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30
Q

Rivaroxaban

A

Xarelto®

3A4 substrate

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31
Q

Apixaban

A

Eliquis®

3A4 substrate

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32
Q

Ticagrelor

A

Brilinta®

3A4 substrate

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33
Q

Which (3) statins are metabolized solely by CYP3A4?

A

Simvastatin, Atorvastatin, and Lovastatin

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34
Q

Which statin is not metabolized by any CYP enzymes?

A

Pravastatin (Pravachol®)

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35
Q

What (2) CYP enzymes metabolize Crestor®?

A

2C9 & 2C19

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36
Q

Which statin is metabolized by both glucuronidation and CYP2C9?

A

Pitavastatin (Livalo®)

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37
Q

Max dose of simvastatin is limited to 10mg while on which of the following concomitant medications?

A. Amiodarone
B. Calan®
C. Multaq®
D. B & C
E. All of the above
A

D. B & C (Verapamil-Calan® and dronedarone-Multaq®) are both CYP3A4 inhibitors and limit the maximum daily dose of simvastatin to 10mg.

Diltiazem is the 3rd drug that limits Zocor® max dose to 10mg

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38
Q

Concomitant use of which (3) medications while on Zocor® would limit the dose to 20mg?

A
  1. Amiodarone
  2. Norvasc®
  3. Ranolazine (Ranexa®)
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39
Q

True or False - Clopidogrel is a prodrug?

A

True - Plavix® is metabolized by several different CYP enzymes into its active metabolite

Prasugrel (Effient®), another antiplatelet prodrug, is also metabolized into an active metabolite by multiple CYP enzymes

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40
Q

Which is the more active enantiomer of warfarin?

A. R-warfarin
B. S-warfarin

A

B. S-warfarin is the more active enantiomer

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41
Q

True or False - polymorphisms can exist in VKORC1 which would lead to increased warfarin effect?

A

True - VKORC1 or vitamin K epoxide reductase complex makes activated (reduced) vitamin K-dependent clotting factors. A polymorphism is this enzyme would decrease production of vitamin-K dependent clotting factors thereby indirectly increasing warfarin’s effects which may put the patient at higher risk for bleeding.

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42
Q

Miconazole

A

Oravig®

2C9 inhibitor

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43
Q

Metronidazole

A

Flagyl®

2C9 inhibitor

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44
Q

SMZ/TMP

A

Bactrim®

2C9 inhibitor

45
Q

Fluvastatin

A

Lescol®

2C9 inhibitor
2C9 substrate

46
Q

Isoniazid

A

2C9 inhibitor

47
Q

Gemfibrozil

A

Lopid®

2C9 inhibitor

48
Q

Fenofibrate

A

Tricor®

2C9 inhibitor

49
Q

NSAIDS

A

2C9 substrates

50
Q

Glimepiride

A

Amaryl®

2C9 substrate

51
Q

Glipizide

A

Glucotrol®

2C9 substrate

52
Q

Glyburide®

A

Diabeta®, Micronase®

2C9 substrate

53
Q

Warfarin

A

Coumadin®

2C9 substrate

54
Q

Posaconazole

A

Noxafil®

3A4 inhibitor

55
Q

Empirically, what should be done to the dose of warfarin when amiodarone is initiated? Why?

A

Decrease dose of warfarin by 30-50%. Amiodarone is a 2C9 inhibitor and warfarin is a 2C9 substrate. Therefore, amiodarone will inhibit the metabolism of warfarin leading to increased concentration and effect and potential risk of bleeding.

If adding warfarin to a patient regimen that already includes amiodarone, initial dose of warfarin should be more conservative.

56
Q

Choose all of the true statements:

A. Hyperthyroidism increases effects of warfarin from increased catabolism of vit K dependent clotting factors
B. Hyperthyroidism decreases effects of warfarin from increased catabolism of vit K dependent clotting factors
C. Hypothyroidism increases effects of warfarin from decreased catabolism of vit K dependent clotting factors
D. Hypothyroidism decreases effects of warfarin from decreased catabolism of vit K dependent clotting factors

A

A & D are correct

57
Q

Digoxin

A

Lanoxin®

P-gp substrate

58
Q

Quinidine

A

Quinidex® (class IA anti-arrhythmic)

2D6 inhibitor

59
Q

Fluoxetine

A

Prozac®

2D6 inhibitor
2D6 substrate
2C19 inhibitor

60
Q

Paroxetine

A

Paxil®

2D6 inhibitor
2D6 substrate

61
Q

Duloxetine

A

Cymbalta®

2D6 inhibitor

62
Q

Bupropion

A

Wellbutrin®

2D6 inhibitor

63
Q

Flecainide

A

Tambocor® (class IC anti-arrhythmic)

2D6 substrate

64
Q

Mexiletine

A

Mexitil® (Class IB anti-arrhythmic)

2D6 substrate

65
Q

Metoprolol

A

Lopressor®, Toprol XL®

2D6 substrate

66
Q

Carvedilol

A

Coreg®

2D6 substrate

67
Q

Propranolol

A

Inderal®

2D6 substrate

68
Q

Timolol

A

2D6 substrate

69
Q

Amitriptyline

A

Elavil®

2D6 substrate
1A2 substrate

70
Q

Imipramine

A

Tofranil®

2D6 substrate

71
Q

Nortriptyline

A

Pamelor®

2D6 substrate
1A2 substrate

72
Q

Venlafaxine

A

Effexor®

2D6 substrate

73
Q

Thioridazine

A

2D6 substrate

74
Q

Haloperidol

A

Haldol®

2D6 substrate

75
Q

Risperidone

A

Risperdal®

2D6 substrate

76
Q

Tamoxifen

A

Nolvadex®

2D6 substrate

Prodrug so inhibiting its metabolism will actually DECREASE its effect (since it’s not being metabolized into its active metabolite)

77
Q

Codeine

A

2D6 substrate

Prodrug so inhibiting its metabolism will actually DECREASE its effect (since it’s not being metabolized into its active metabolite)

78
Q

Tramadol

A

Ultram®

2D6 substrate

Prodrug so inhibiting its metabolism will actually DECREASE its effect (since it’s not being metabolized into its active metabolite)

79
Q

Sertraline

A

Zoloft®

2D6 inhibitor

80
Q

Terbinafine

A

Lamisil®

2D6 inhibitor

81
Q

Omeprazole

A

Prilosec®

2C19 inhibitor
2C19 substrate

82
Q

Esomeprazole

A

Nexium®

2C19 inhibitor
2C19 substrate

83
Q

Lansoprazole

A

Prevacid®

2C19 substrate

84
Q

Pantoprazole

A

Protonix®

2C19 substrate

85
Q

Rabeprazole

A

Aciphex®

2C19 substrate

86
Q

Clopidogrel

A

Plavix®

2C19 substrate

87
Q

Diazepam

A

Valium®

2C19 substrate

88
Q

Escitalopram

A

Lexapro®

2C19 substrate

89
Q

Efavirenz

A

Sustiva®

2C19 inhibitor

90
Q

Etravirine

A

Intelence®

2C19 inhibitor

91
Q

Cimetidine

A

Tagamet®

2C19 inhibitor
1A2 inhibitor

92
Q

Fluvoxamine

A

Faverin®

2C19 inhibitor
1A2 inhibitor
1A2 substrate

93
Q

Which CYP enzyme does charbroiled foods affect? How does it affect it?

A

Charbroiled foods induce CYP1A2

94
Q

Primidone

A

Mysoline®

1A2 inducer

95
Q

Which CYP enzyme does smoking affect? How?

A

Smoking induces CYP1A2

96
Q

Ciprofloxacin

A

Cipro®

1A2 inhibitor

97
Q

Ethinyl estradiol

A

1A2 inhibitor

98
Q

Caffeine

A

1A2 substrate

99
Q

Theophylline

A

Theolair®

1A2 substrate
XO substrate (if used with allopurinol, a XO inhibitor, decrease dose of theophylline by 25-33%)
100
Q

Clozapine

A

Clozaril®

1A2 substrate

101
Q

Olanzapine

A

Zyprexa®

1A2 substrate

102
Q

Zolmitriptan

A

Zomig®

1A2 substrate

103
Q

Frovatriptan

A

Frova®

1A2 substrate

104
Q

Mirtazapine

A

Remeron®

1A2 substrate

105
Q

Tizanidine

A

Zanaflex®

1A2 substrate

106
Q

Melatonin

A

1A2 substrate

107
Q

Allopurinol (Zyloprim®) and febuxostat (Uloric®) inhibit which enzyme involved in the production of uric acid?

A

Xanthine oxidase

108
Q

Azathioprine

A

Imuran® Prodrug to 6-MP

XO substrate (allopurinol and febuxostat inhibit XO which would increase the active metabolite potentially leading to increased risk of myelosuppression.

(if used with allopurinol, a XO inhibitor, decrease dose of Azathioprine by 25-33%)

109
Q

Febuxostat

A

Uloric®

XO inhibitor

CI with Azathioprine (Imuran®) and 6-MP