Drugs to Treat Hyperlipidemia Flashcards

1
Q

What is the MOA of statins?

A

Competibiley block HMG-CoA reductase

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2
Q

What is the most severe form of muscle damage that statins can cause which may lead to severe kidney damage?

A

Rhabdomyolysis

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3
Q

What non lipid lowering MOA do statins have?

A

1) Plaque stabilization

2) Reduced Inflammation

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4
Q

What contraindications do statins have?

A

1) Active hepatic disease
2) Unexplained persistent
elevations in aminotransferase levels
3) Pregnancy and while breastfeeding

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5
Q

A potential causal relationship between statin therapy and the risk of developing what condition has been noted?

A

Diabetes

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6
Q

What accounts for the low bioavailability of statins?

A

They undergo hepatic first pass metabolism

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7
Q

Which transaminase is higher in statin related liver dysfunction?

A

ALT greater than AST

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8
Q

Because of statins act on this particular organ, what may it cause?

A

Severe liver injury

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9
Q

Simvastatin and lovastatin the only two of the class administered as?

A

Prodrugs

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10
Q

The effect of statins in the body is almost universally affected by the concurrent metabolism of other pharmacologic agents which induce or inhibit?

A

CYP450

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11
Q

What needs to be done with warfarin prescription when

given alongside statins?

A

Dose reduction

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12
Q

What is the MOA of ezetimibe?

A

Impairs dietary and biliary cholesterol absorption at the brush border of the intestine

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13
Q

What protein does ezetimibe inhibit?

A

Niemann-Pick C1 like 1 (NPC1L1)

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14
Q

Ezetimibe is also used in combination with?

A

Statins and fenofibrate

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15
Q

What are the contraindications and adverse effects of ezetimibe?

A

Pretty much same as statins

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16
Q

Ezetimibe is primarily metabolized in the liver and the small intestine via?

A

Glucuronide conjugation

17
Q

What is the MOA of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors?

A

Cleaves LDL receptors at serine residues

18
Q

PCSK9-Inhibitors are indicated for patients with?

A

Heterozygous Familial Hypercholesterolemia

19
Q

What is the MOA of bile acid sequestrants (BAS)?

A

Bind bile salts at the intestine > decreased bile salts going back through enterohepatic circulation > liver must make more bile salts so they use up the cholesterol stores > utilize all the cholesterol stores in the body like absorbing from the blood > increase LDL receptors to absorb more LDL in the blood > Reduce low-density lipoprotein-cholesterol (LDL-C)

20
Q

What happens to BAS after oral administration?

A

They are not absorbed, but bind to bile acids in the intestine and prevent their reabsorption into the body

21
Q

Alirocumab and Evolocumab make up what class of drug?

A

PCSK9-Inhibitors

22
Q

Colesevelam, colestipol, and cholestyramine make up what class of drug?

A

Bile Acid Sequestrants

23
Q

What contraindications do BAS have?

A

Patients with dysbetalipoproteinemia

24
Q

BAS may decrease the absorption of?

A

Fat soluble vitamins (A,D,E,K) and folic acid

25
Q

What is the MOA of fibrates?

A

Activate Peroxisome Proliferator Antigen Receptor-alpha- (PPARɑ)

26
Q

What general side effects are noted with fibrates?

A

GI issues

27
Q

What should be done when prescribing fibrates?

A

1) Monitor liver enzymes

2) Monitor serum creatinine

28
Q

At what GFR should fenofibrates not be used?

A

GFR < 30 ml/min

29
Q

Why should gemfibrozil (fibrate) not be taken with statin?

A

Increased muscle toxicity risk

30
Q

What may occur because fibrates may increase the concentration of cholesterol in the gallbladder?

A

Gallstones

31
Q

Why does gemfibrozil have a lot of drug interactions?

A

It is a CYP2C8 strong inhibitor

32
Q

Can fibrates be taken by nursing mothers?

A

No it appears in breast milk

33
Q

What vitamin can be prescribed to reduce the levels of cholesterol and triglycerides (fatty substances) in your blood, and decrease your risk of a heart attack?

A

Niacin (vit B3)

34
Q

What may nancin inhibit release of form adipose tissue?

A

Free fatty acids

35
Q

What effect does niacin have with blood sugar and diabetes?

A

Raises blood sugar

36
Q

Why does niacin affect patients with gout?

A

May raise uric acid levels

37
Q

Why should niacin be used with caution in patients with active bleeding or bleeding disorders?

A

Prolongs prothrombin time