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Statins

Total questions: 70

Worksheet time: 48mins

Name
Class
Date
1.

Statins target de novo cholesterol biosynthesis in liver

a)

true

b)

false

2.

Liver compensates by

a)

increasing LDLR

b)

clears LDL and VDLDS from blood

c)

decrease LDLR

3.

PJ is a 4.5 year old boy. At his checkup, the pediatrician notices cutaneous xanthomas and orders a lipid panel. Repeated measures confirm that the patient's serum cholesterol levels are high (936 mg/dL). Further testing confirms a diagnosis of homozygous familial hypercholesterolemia. Which of the following interventions will be LEAST effective in this patient?

a)

Atorvastatin

b)

Ezetimibe

c)

Lomitapide

d)

Mipomersen

e)

Niacin

4.

Which of the following are enzymes involved in cholesterol biosynthesis that are good targets for drugs?

a)

HMG CoA Reductase

b)

Squalene Synthase

c)

PCDK9

d)

NPC1L1

5.

Which of the following are enzymes that serve as targets to statins?

a)

HMG CoA Reductase

b)

Squalene Synthase

c)

PCDK9

d)

NPC1L1

6.

Inhibitors were designed based on the intermediate in cholesterol biosynthesis

a)

true

b)

false

7.

3,5 dihydroxy acid in statins mimics the tetrahedral intermediate produced by

a)

HMG CoA Reductase

b)

Squalene Synthase

8.

Statins are transition state inhibitors

a)

true

b)

false

9.

Plasma cholesterol can be lowered by

a)

decrease liver cholesterol biosynthesis

b)

increase in LDL receptors leading to increase uptake in liver

c)

decrease VLDL precursors

d)

increase liver cholesterol biosynthesis

10.

Stereochemistry in the pharmacophore is required in which positions?

a)

3R

b)

5R

c)

3S

d)

5S

11.

Which of the following functional groups are present in Ring A?

a)

two cyclohexane rings

b)

hydroxyl group at R1

c)

Metyl substitution at R2

d)

5-6 member heterocyclic ring attached with floro-phenyl

e)

R= Aryl groups/hydrocarbon chains/amides/DO2/NH2

12.

Which of the following functional groups are present in Ring B?

a)

two cyclohexane rings

b)

hydroxyl group at R1

c)

Metyl substitution at R2

d)

5-6 member heterocyclic ring attached with floro-phenyl

e)

R= Aryl groups/hydrocarbon chains/amides/DO2/NH2

13.

Essential for anchoring the compound to enzyme active site

a)

two cyclohexane rings

b)

hydroxyl group at R1

c)

Metyl substitution at R2

14.

Increase hydrophilicity and may provide some cellular specificity

a)

two cyclohexane rings

b)

hydroxyl group at R1

c)

Metyl substitution at R2

15.

Increase activity

a)

two cyclohexane rings

b)

hydroxyl group at R1

c)

Metyl substitution at R2

16.

Lovastatin is more potent that Simvastatin

a)

true

b)

false

17.

Which of the following have a short duration of action (2 hours)?

a)

Lovastatin

b)

Simvastatin

c)

Pravastatin

d)

Atorvastatin

e)

Fluvastatin

18.

Which of the following does not have to be taken at bedtime?

a)

Lovastatin

b)

Simvastatin

c)

Pravastatin

19.

Which of the following are true about Pravastatin?

a)

neutral

b)

lipophilic

c)

acidic

d)

hydrophilic

e)

less muscle penetration

20.

Which of the following are true about Lovastatin and Simvastatin?

a)

neutral

b)

lipophilic

c)

acidic

d)

hydrophilic

e)

less muscle penetration

21.

Which structure is a hydrophilic statin and most likely to have less muscle penetration?

a)
b)
22.

According to these structures, which drug is more potent?

a)
b)
23.

Which of the following is true about Simvastatin and Lovastatin?

a)

active metabolite is the acid form

b)

further metabolized in liver (CYP3A4)

c)

excreted mainly in feces (84%)

d)

extensive first pass metabolism

e)

metabolized into active metabolite (less activity): CYP3A4 substrate minor

24.

Which of the following is true about Pravastatin?

a)

active metabolite is the acid form

b)

further metabolized in liver (CYP3A4)

c)

excreted mainly in feces (84%)

d)

extensive first pass metabolism

e)

metabolized into active metabolite (less activity): CYP3A4 substrate minor

25.

Which of the following drugs belong to the Ring B group?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

e)

Simvastatin

26.

This drug belongs to the Ring B group, but has a short duration of action, similar to Ring A

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

e)

Simvastatin

27.

Which of the following have a long duration of action and can be taken any time of the day?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

e)

Simvastatin

28.

Which of the following lipophilic statins?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

e)

Simvastatin

29.

Which is the MOST lipophilic statin?

a)

Atorvastatin

b)

Fluvastatin

30.

Which is a racemic mixture?

a)

Atorvastatin

b)

Fluvastatin

31.

Which of the following are acidic statins?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

32.

Which of the following are true about Rosuvastatin?

a)

it's amphoteric

b)

most hydrophilic statin

c)

less muscle pain

d)

most potent

e)

more muscle pain

33.

Which of the following is 99% protein bound?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

34.

Which of the following has an extensive first pass metabolism?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

35.

Which of the following does not have an extensive first pass metabolism and is excretes unchanged in feces?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

36.

Which of the following has least first pass metabolism (high bioavailability) and is excreted in feces?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

37.

Which of the following are excreted in feces?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

38.

Which of the following is excreted in bile (less by kidneys)?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

39.

Which of the following is metabolized to an equipotent metabolite (CYP3A4) that has an increased half life of 20-30 hours?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

40.

Which of the following has a strong affinity for CYP2DC6?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

41.

Which of the following has some metabolism by CYP2C9 (~10%)?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

42.

Which of the following is majorly metabolized by UDP-glucuronosyltransferase (UGT1A3 & UGT2B7)?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

43.

Which of the following is less likely to interact with drugs metabolized by 3A4 and is good in geriatric patients?

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

44.

Which of the following require OAT?

a)

anionic form (free acid) to be transported into hepatocytes

b)

active from (not prodrugs) of all statins

c)

cationic form (free acid) to be transported into hepatocytes

45.

Which functional group is responsible for making Pravastatin the second most hydrophilic statin?

a)

A

b)

B

46.

Rosuvastatin is the most hydrophilic because of

a)

A

b)

B

c)

C

47.

Atorvastatin is more potent than Rosuvastatin

a)

true

b)

false

48.

Pitavastatin has the least first pass metabolism because of

a)

A

b)

B

c)

C

49.

Which structure represents a Ring B statin?

a)
b)
50.

Atorvastatin and Rosuvastatin have long half lives but, Atorvastatin lasts longer

a)

true

b)

false

51.

Significant interactions with drugs affecting CYP3A4, PgP and OAT1B1

a)

Atorvastatin

b)

Fluvastatin

c)

Rosuvastatin

d)

Pitavastatin

52.

Atorvastatin causes more muscle problems because it's the most lipophilic

a)

true

b)

false

53.

Not all statins can interact with OAT1B1 hepatocytes

a)

true

b)

false

54.

Which statins can be taken at any time at any time of the day?

a)

Atorvastatin

b)

Rosuvastatin

c)

Pitavastatin

d)

Pravastatin

55.

Which of the following are true about drug-drug interactions of statins with OATPB1 inhibitors?

a)

Gemfibrozil and Cyclosporin

b)

Fluvastatin and Rosuvastatin can be used with cyclosporin and gemfibrozil at reduced doses

c)

Fluvastatin and Rosuvastatin can't be used with OATP1B1 inhibitors

56.

Fluvastatin + Gemfibozil recommended dose

a)

avoid

b)

20mg max

57.

Fluvastatin + Ciclosporin recommended dose

a)

avoid

b)

20mg max

58.

Which of the following are true about the drug-drug interactions of statins with CYP3A4 inhibitors?

a)

macrolide antibiotics

b)

azole antifungals like ketoconazole

c)

HIV protease inhibitors

d)

interaction with Atorvastatin, Simvastatin and Lovastatin

e)

Naproxen, Aspirin, Acetaminophen

59.

Which of the following are metabolized by CYP3A4?

a)

Simvstatin

b)

Lovastatin

c)

Atorvastatin

d)

Pravastatin (minor)

e)

Pitavastatin

60.

Which of the following are metabolized by CYP2C9?

a)

Fluvastatin

b)

Rosuvastatin

c)

Atorvastatin

d)

Pitavastatin

61.

Which of the following are metabolized by glucorination?

a)

Fluvastatin

b)

Rosuvastatin

c)

Atorvastatin

d)

Pitavastatin

62.

Rosuvastatin + Gemfibrozil recommended dose

a)

10mg max

b)

5mg max

c)

avoid

63.

Rosuvastatin + Cyclosporine recommended dose

a)

10mg max

b)

5mg max

c)

avoid

64.

Which of the following are true about statins?

a)

can decrease LDL cholesterol levels dramatically

b)

effective and well tolerated

c)

decrease risk of coronary events and mortality in patients with ischemic heart disease (IHD)

d)

can increase LDL cholesterol levels dramatically

65.

Which of the following are true about toxicity of statins?

a)

mild increase of serum aminotransferases (check ALT and AST)

b)

severe muscle pain and even rhabdomyolysis

c)

increase creatinine kinase (CK)

d)

CYP inhibitors increase risk for hepatotoxicity and myopathy

e)

decrease creatinine kinase (CK)

66.

Statins are safe to use during pregnancy

a)

true

b)

false

67.

Patients taking statins should not take grapefruit juice because it increases risk for hepatotoxicity and myopathy

a)

true

b)

false

68.

Fluvastatin is the most potent drug and Rosuvastatin is the least

a)

true

b)

false

69.

Which statin would not be prescribed to a patient who has myopathy?

a)

Fluvastatin

b)

Rosuvastatin

c)

Atorvastatin

d)

Pitavastatin

70.

Which of the following are lactone derivates?

a)

Lovastatin

b)

Simvastatin

c)

Pravastatin

d)

Rosuvastatin

e)

Pitavastatin