Drugs Used In Hyperlipidemia Flashcards

1
Q

The longer and lower the reduction in circulating LDL-C, the lower the incidence of

A

CHD

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2
Q

Cholesterol esters and triglycerides are insoluble in water and circulate in blood as

A

Lipoprotein particles

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3
Q

Low density lipoprotein ApoB is recognized by the

A

LDL receptor

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4
Q

The LDL receptor internalizes circulating

A

LDL

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5
Q

A transcription factor that serves as the master regulator of cholesterol levels in the cell

A

SREBP (Sterol Regulatory Element Binding Protein)

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6
Q

In a low cholesterol diet, SREBP is

A

Activated

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7
Q

Results in increase in cholesterol biosynthesis and increase in receptor-mediated LDL endocytosis from the plasma

A

SREBP activation

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8
Q

In a high-cholesterol diet, SREBP is not activated and thus we see a decrease in

A

Cholesterol biosynthesis and LDL receptors

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9
Q

The most effective and best tolerated agents for treating dyslipidemia

A

Statins

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10
Q

Statins function as

A

HMG-CoA reductase inhibitors

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11
Q

Competitive inhibitors of HMG-CoA reductase

  • Inhibits cholesterolgenesis
  • Increase expression of LDL receptor
A

Statins

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12
Q

Inactive lactose pro drugs hydrolysis to active drugs

A

Statins

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13
Q

Statin absorption varies from 40% to 75% except for

A

Fluvastatin (almost completely absorbed)

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14
Q

Statins have half-lives of 1-3 hours except for

  1. ) Atorvastatin?
  2. ) Rosuvastatin?
A
  1. ) 14 hours

2. ) 19 hours

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15
Q

Hepatic cholesterol biosynthesis is maximal from midnight-2 AM, so we want to take them in the

A

Evening (except for the ones w/ the long half-lives)

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16
Q

Contraindicated in women who are pregnant, lactating, or likely to become pregnant

A

Statins

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17
Q

Most efficacious agents for severe hypercholesterolemia

-More TG lowering activity compared to other statins

A

Atorvastatin and Rosuvastatin

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18
Q

Two toxic/adverse effects of Statins are

A
  1. ) Hepatotoxicity

2. ) Diabetes Mellitus

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19
Q

While statin therapy can reduce occlusive vascular events by 40-50%, many patients discontinue statins due to

A

Myopathies

20
Q

Monoclonal antibodies (mAbs) against PCSK9 protein

A

PCSK9 inhibitors

21
Q

Diverts LDLR from recycling pathway towards lysosome for degradation

A

PCSK9

22
Q

A cholesterol absorption inhibitor

A

Ezetimibe

23
Q

Ezetimibe’s site of action is at the

A

NPC1L1 cholesterol transporter

24
Q

Selectively inhibits intestinal cholesterol absorption and also plant sterols

A

Ezetimibe

25
Q

Increases expression of hepatic LDL receptors, decreases intestinal delivery of cholesterol to the liver, and decreases cholesterol content of atherogenic particles

A

Ezetimibe

26
Q

The average reduction in LDL-C with drug alone is

A

18%

27
Q

Ezetimibe is synergistic with

-Additional 25% decrease compared to statin alone

A

Statins

28
Q

Highly positively charged and bind negatively charged bile acids

-The bound bile acids are then excreted in stool

A

Bile acid sequestrants

29
Q

Decline hepatic cholesterol content, increase LDL receptors, increase clearance of LDL from plasma, and lower LDL-C

A

Bile acid sequestrants

30
Q

However, bile acid sequestrants do upregulate

A

HMG-CoA reductase

31
Q

Use with extreme caution or avoid completely in patients with severe hypertriglyceridemia

A

Bile Acid Sequestrants

32
Q

You must take with meals or there is no effect

A

Bile acid sequestrants

33
Q

Used to treat heterozygous FH

A

Bile acid sequestrants

34
Q

Can cause constipation, bloating, heart burn, and diarrhea

A

Bile acid sequestrants

35
Q

These side effects can be relieved by increasing fiber or by mixing bile acid sequestrant with

A

Psyllium Seed

36
Q

Can interfere with the absorption of many other drugs

-Should wait 3-4 hours after taking to take another drug

A

Bile acid sequestrants

37
Q

What’re soluble vitamin B3

A

Niacin (nicotinic acid)

38
Q

Has favorable effects on all lipid profiles, but there are a lot of adverse effects

A

Niacin

39
Q

Has the primary effect of inhibiting VLDL secretion, thereby decreasing production of LDL

A

Niacin

40
Q

Inhibits lipolysis of TG by hormone-sensitive lipase

A

Niacin

41
Q

Increased CHD risk associated with TG levels greater than 150 mg/dL

A

Hypertriglyceridemia

42
Q

Elevated triglycerides (greater than 500 mg/dL) can lead to

A

Pancreatitis

43
Q

Activated the peroxisome proliferator-activated receptor-alpha

A

Vibrates

44
Q

A transcription factor regulating genes that control lipid metabolism

A

Vibrates

45
Q

Primary effect is to reduce plasma TG

-Only a modest decrease in LDL

A

Fibrates