Pharmacology-Hyperlipidemic Drugs

Question 1

What are the cholesterol levels standards after an overnight fast?

Answer 1

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Question 2

What are risk factors for coronary heart disease? At what point should you start treating someone aggressively for CHD?

Answer 2

You treat aggressively when your patient has two or more of these factors or just one of the red factors.

Question 3

An elevated level of what apolipoprotein is associated with decreased risk of coronary heart disease?

Answer 3

Apo A1. It is on HDL which pulls cholesterol out of plaques.

Question 4

List 4 primary hypercholesterolemias.

Answer 4

Familial hypercholesterolemia, familial ligand-defective apolipoprotein B, familial combined hyperlipoproteinemia, Lp(a) hyperlipoproteinemia.

Question 5

List 4 primary hypertriglyceridemias.

Answer 5

Primary chylomicronemia, familial hypertriglyceridemia, familial combined hyperlipoproteinemia and familial dysbetalipoproteinemia.

Question 6

What are some secondary causes of hyperlipidemia?

Answer 6

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Question 7

How can you decrease cholesterol levels by 10-20% by just changing your diet?

Answer 7

Reduce intake of fats and cholesterol. Eat oat and rice (reduces LDL). Reduce sugar intake (sugar increases VLDL synthesis). Eat nuts (reduces LDL). Omega-3 oil in fish (increases HDL and reduces LDL).

Question 8

What drugs can you prescribe to a patient with high cholesterol that are bile-acid sequestrates (resins)? What is the mechanism by which these drugs work?

Answer 8

Cholestyramine, colestipol and colesevelam (best one). They bind bile acids and inhibit reabsorption of bile acid. This increases channeling of cholesterol to bile acid production and decreases intra-hepatic cholesterol levels. As these levels decrease, the liver upregulates LDL (apoB and E) receptors and increases clearance of LDL, IDL and VLDL.

Question 9

How effective are resins at decreasing CHD events (fatal and nonfatal)? Who are these drugs particularly good for?

Answer 9

They decrease them by 19%, decreasing LDL cholesterol levels by 15-30% and increasing HDL levels by 3-5%. These drugs are safe for pregnant women as statins are not. They are used in conjunction with statins in heterozygous familial hypercholesterolemia and combined hyperlipidemia.

Question 10

What are adverse effects and interactions you need to keep in mind with bile-acid sequestrates?

Answer 10

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Question 11

What are the main statins you will use and how do they work?

Answer 11

Simvastatin, atorvastatin and rosuvastatin. The look like mevalonate, bind to HMG-CoA reductase, inhibit it and thus reduce cholesterol synthesis. Decreasing synthesis, results in up regulation of LDL receptors and incidentally more LDLs are taken up by the liver.

Question 12

How effective are statins?

Answer 12

Rosuvastatin might be slightly better because it increases HDL more than atorvastatin.

Question 13

What are contraindications to consider with statins?

Answer 13

Myopathy (they can cause it and possibly lead to rhabdomyolysis). Asians (don’t metabolize them as well). Mild hepatotoxicity. Pregnant women (teratogenic). Memory loss. Increased blood sugar levels.

Question 14

What are drug interactions you need to consider when prescribing lovastatin, simvastatin and atorvastatin? Why is rosuvastatin not considered?

Answer 14

Drugs that interact with CYP3A4. Rosuvastatin is not metabolized by CYP3A4.

Question 15

Why are statins so good for patients that just survived an MI?

Answer 15

Induce endothelial production of NO and vasodilate. Stabilize plaques. Reduce CRP (reducing inflammation). Reduces thrombotic events.

Question 16

What other chronic conditions aside from heart disease can benefit from statin therapy?

Answer 16

Multiple sclerosis (anti-inflammatory effect). Alzheimer’s. Rheumatoid arthritis.

Question 17

What groups of people should receive moderate to high intensity statin therapy?

Answer 17

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Question 18

What apolipoprotein was found in people in Italy that significantly decreased their incidence of CHD events?

Answer 18

Apo A1-Milano

Question 19

Why is estrogen-replacement therapy a controversial topic in cholesterol management?

Answer 19

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Question 20

What drug prevents cholesterol absorption in your GI tract? What happens when you combine it with a statin?

Answer 20

Ezetimibe. It actually increases plaque formation when combined with statins.

Question 21

What happens when your triglycerides (VLDL) get too high? What drug do you use treat this that causes the largest increase in HDL levels?

Answer 21

Pancreatitis and xanthomas. Niacin increases lipoprotein lipase activity (decreasing VLDL) and raises HDL.

Question 22

What drugs are used to lower triglyceride (VLDL) levels in patients with familial hypertriglyceridemia and familial dysbetalipoproteinemia?

Answer 22

Fenofibrate (fibrin acid derivative). This drug binds to PPAR-alpha receptors, increasing LPL activity, increasing HDL and decreasing VLDL synthesis and excretion by the liver.

Question 23

Why should you not use fenofibrate in patients with renal failure?

Answer 23

It is excreted by the kidneys

Question 24

Why should you be wary prescribing gemfibrozil when a patient is on a statin?

Answer 24

Rhabdomyolysis

Question 25

What drug is used in combination with niacin to treat Lp(a) hyperlipoproteinemia?

Answer 25

Neomycin. It is an antimicrobial that actually inhibits resorption of cholesterol and bile salts.