Antihyperlipidemics Flashcards

1
Q

With statin therapy, how long does it usually take to see significant LDL reduction?

A

about 2 weeks

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2
Q

How long does it take for statin therapy to lower BP?

A

2 days. This occurs due to the stimulation of eNOS.

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3
Q

What are antihyperlipidemics or hypolipidemics?

A

drugs used to treat hyperlipoproteinemias that cause atherosclerosis/ coronary artery disease (CAD) and reduce risk of mortality to heart disease and stroke.
Also treat hypertriglyceridemia that may also cause acute pancreatitis when triglycerides (TGs) are markedly elevated.

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4
Q

What are the major lipids?

A

cholesterol and TGs that are transported via lipoproteins

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5
Q

What are apoproteins?

A

surface proteins on lipoproteins that interact with tissue membrane receptors to assist transport/ uptake to/from tissues (ex. apoB-100 is a ligand for LDL recepors=BAD)

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6
Q

How are lipoproteins correlated to CAD?

A

increased LDL and low HDL :(
These are associated with plaques (oxidized LDLs), foam cells, atherosclerosis, calcification, endothelial rupture, thrombosis, and MI.

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7
Q

What is Lp(a)?

A

atherogenic lipoprotein, genetically determined, related to LDL, and a risk factor for CAD.

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8
Q

What should normal LDL be?

A

Less than 100 mg/dL (2.59 mmol/L) — Optimal.

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9
Q

What should your LDL be if you have vascular disease?

A
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10
Q

How do you calculate LDL?

A

LDL= Total cholesterol - HDL - (TG/5)

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11
Q

What is a normal LDL/HDL ratio?

A

3 - 3.5. Anything above 3.5= increased risk for CAD.

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12
Q

What are the nonpharmacologic strategies to lowering LDL?

A
  • eliminate smoking
  • eliminate excess alcohol
  • diet (fish oils, omega-3s)
  • lose excess weight
  • aerobic exercise
  • control diabetes
  • control thyroid function
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13
Q

**What are bile acid binding resins?

A

inhibit bile acid reabsorption from the gut and the result is compensatory increase in liver bile acid sythesis from cholesterol by increasing LDL receptors on the liver to remove LDL-cholesterol form the plasma, thus lowering cholesterol.
Usually second-line drugs, or used in combination with statins, fibrates, or niacin.

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14
Q

What are the 3 bile acid binding resins?

A
  1. Cholestyramine
  2. Colestipol
  3. Colesevelam
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15
Q

**What are the ADRs of bile acid resins?

A
  • bloating, belching, gas, heartburn, and constipation.
  • impairs absorption of fat soluble vitamins (A, D, E, K)
  • may INCREASE VLDL-triglyceride levels due to increased liver TG synthesis. :(
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16
Q

**What are statins?

A
  • Competitive inhibitors of HMG CoA reductase. This is the rate limiting step and significantly reduces liver cholesterol synthesis. This decrease in LDL forces the liver cells to up-regulate more LDL receptors and import more LDL from the bloodstream.
  • Also have anti-inflammatory effects and increased eNOS activity.
17
Q

What are the more common statins?

A

Rosuvastatin, Atorvastatin, Simvastatin

18
Q

Do statins increase HDL?

A

very slightly

19
Q

**What are the ADRs of statins?

A
  • increased liver alanine and aspartate aminotransferase (LFTs) as well as metabolized via CYP450.
  • increased CPK and MYOPATHY
  • CONTRAINDICATED in PREGNANCY
20
Q

**What is ezetimibe?

A

inhibits jejunal enterocyte uptake of cholesterol. It is usually used with a statin or bile acid resin.

21
Q

**What is Niacin (vitamin B3)?

A
  • Inhibits intracellular lipase, decreasing free fatty acid supply to liver, decreasing synthesis of VLDL, plasma VLDL, and decrease LDLs, while increasing HDL.
  • It also improves endothelial function, enhancing the function of t-PA and decreases fibrinogen; keeps the pipes clean.
  • It is sometimes combined with a statin.
22
Q

**What are the ADRs of Niacin (vitamin B3)?

A
  • intense vasomotor flushing and pruritis.
  • increased LFTs (AST and ALT)
  • hyperglycemia intolerance and may increase insulin resistance
  • hyperuricemia (GOUT)
  • peptic ulcers
  • Thus don’t use in diabetics, those with liver disease, pregnant, or if they have gout.
23
Q

What are the fibric acid derivates?

A
  • Gemfibrozil= activates nuclear receptor in liver and muscle that increases LPL/ fatty acid oxidation, lowering TGs and it increases HDL (due to increased ApoI/II).
  • Considered first line drug for increased TGs.
  • Fenofibrate= newer drug that decreases LDL more the gemfibrozil but doesn’t increase HDL as much.
24
Q

What are the ADRs of fibric acid derivatives?

A

cholecystitis (GALLSTONES), myopathy, and increased liver enzymes.

25
Q

Consumption of alcohol is associated with what change in serum lipid concentration?

A

increased triglycerides.