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Flashcards in HLD drugs Deck (77)
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31

Bile acid-bindign resins: adverse effects?

  • Generally safe
  • Can increase TG levels in hypertriglyceridemia
  • At high concentrations, Cholestyramine and Colestipol, but not Colesevelam, impair the absorption of the fat soluble vitamins A, D E & K

32

Bile acid-binding resins: contraindications?

TG > 400 mg/dL

Type III Dysbetalipoproteinemia

33

Bile acid-binding resins: effects on serum lipids?

 v LDL (10-25%)

Small increase in TG

34

What's the name of the drug that inhibits cholesterol absorption?

Ezetimibe

35

Ezetimibe: effects on serum lipids?

How is this the same/different compared to bile acid-binding resins?

Effect on serum lipids: v LDL (~18%)

Note: unlike Bile acid-binding resins, Ezetimibe does not raise triglyceride levels

36

Bile acid-binding resins: indications?

High LDL

37

Ezetimibe: indications?

High LDLs

38

Ezetimibe: MoA?

Inhibits intestinal absorption of chol (via NPCL1, small int) --> decreased hepatic chol (therefore reduced VLDLs, LDLs) --> increased LDL-R expression --> increased LDL clearance

39

What are the therapeutic uses for ezetimibe?

  1. Reduces LDL-C in patients with primary hypercholesterolemia
    1. i.e. not completely dependent upon intact LDLR
  2. Can induce a significant further LDL-C lowering effect when combined with a STATIN
    1. Allows the use of a lower STATIN dose to avoid adverse effects

40

Ezetimibe: toxicity?

Generally well-tollerated

41

Name 2 PCSK9 inhibitors.

Alirocumab

Evolocumab

42

PCSK9 inhibitors: MoA?

Inhibits PCSK9 (secreted) --> blocks nl targeting of LDL-R to lysosome --> increased LDL-R expression --> increased LDL clearance

43

PCSK9 inhibitors (alirocumab, evolocumab): indications?

Hetero FH

High LDL not controlled w/statins or statin-intollerant

44

PCSK9 inhibitors: effect on serum lipids?

v LDL (> 50%)

45

Name 2 drugs that are indicated for homozygous familial hypercholesterolemia (FH).

Lomitapide

Mipomersen

46

Lomitapide: MoA?

Inhibits MTP (microsomal triglyceride transfer protein) in both erythrocytes and liver --> decreased production of chylomicrons, VLDL, and LDL

47

Mipomersen: MoA?

Antisense oligonucleotide specific for apoB48/100 --> decreased expression of apoB48/100 --> decreased VLDL & LDLs.

48

Lomitpide: toxicity?

Mipomersen: toxicity?

Hepatotoxicity

Hepatotocity

49

Lomitpide: contraindications?

Mipomersen: contraindications?

Lomitipide: pregnancy

Mipomersen: Mild/mod hepatic impairment

50

Lomitapide: effect on serum lipids?

Mipomersen: effect on serum lipids?

Lomitapide: v chylomicrons, v VLDL, v LDL

Mipomersen: v VLDL, v LDL

51

Elevated serum triglycerides are often a/w what other lipoprotein?

Decrease in HDLs ("good cholesterol")

52

Name all 3 of the drugs whose main action is to lower triglycerides.

Niacin, fibrates (gemfibrozil + fenofibrate)

53

Treatment options for Hypercholesterolemia

1. For moderate hypercholesterolemia with low cardiovascular risk:

Therapeutic lifestyle change

  - Dietary reduction of cholesterol intake

  - Exercise/Weight reduction (improves lipoprotein metabolism)

54

Treatment options for Hypercholesterolemia

2. For severe hypercholesterolemia and/or a high cardiovascular risk

  i.e.   - LDL levels > 190 mg/dL (or > 70 mg/dL with Diabetes)

  - Current clinical evidence of CVD

  - New: 10 yr CVD risk > 7.5% (controversial)

  Answer: 

  Drug therapy is indicated.

  - the initial goal is to reduce LDL - decrease risk of atherosclerosis

  - the initial drug of choice is typically a STATIN

55

Treatment Options for Hypertriglyceridemia:

1. When serum triglycerides are borderline high (150-199 mg/dL)

- Lifestyle change is indicated

- Low fat diet, exercise & cessation of smoking/alcohol

56

Treatment Options for Hypertriglyceridemia:

2. When serum triglycerides are very high (>500 mg/dL)

  - The initial goal is to to prevent pancreatitis by lowering triglyceride levels with either niacin or a fibrate

  - Once triglycerides are <500 mg/dL then any LDL-C goals should be addressed

57

What are 2 other names for niacin?

Nicotinic acid/vitamin B3

58

Niacin: effects on serum lipids?

v TG (30-80%), v LDL (10-20%), ^ HDL (10-30%)

59

Niacin: indications?

High VLDL, high LDL, low HDL

  • Lowers both plasma cholesterol and triglycerides--Useful in the treatment of familial combined hyperlipidemias (­VLDL & ­LDL) and familial dysbetalipoproteinemia (­IDL), i.e. where both cholesterol and triglycerides are elevated.
  • Low HDLs
  • In patients with a history of previous MI, NIACIN has been shown to reduce the incidence of:
    • Re-infarctions, CVAs, overall mortality
  • Combo therapy w/statins (esp. if low HDLs)

60

What's the most effective drug at reducing HDL levels?

Niacin