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Pharmacology - Test #4 > Anti-hyperlipidemic Drugs > Flashcards

Anti-hyperlipidemic Drugs Flashcards

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1
Q

Ways that statin treatment improves patient outcomes

A

Less mortality, CVD disease, stroke

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2
Q

Normal significance of cholesterol and triglycerides?

A

Cholesterol – Essential to cell membranes, sterol/steroid precursor
Triglyceride – Storage form of fuel to support high energy compound generation, in structural lipids

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3
Q

What are lipoproteins all about?

A

Lipoproteins transport cholesterol and triglycerides in blood. Exterior phospholipid, cholesterol, and protein. Interior triglycerides and cholesterol. Regulated by apoproteins.

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4
Q

Signiificance of Chylomicrons

A

Involved in transport of dietary lipids from gut to liver and adipose tissue

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5
Q

Importance of apoliprotein A-1

A

Structural in HDL, ligand of ABCA1 receptor
Mediates reverse cholesterol transport
Made in liver and intestine

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6
Q

Importance of apoliprotein B-100

A

Structural VLDL, IDL, LDL, LDL receptor ligand in liver

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7
Q

Importance of apoliprotein B-48

A

Structural in chylomicrons

Produced in Intestine

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8
Q

Importance of apoliprotein E

A

Ligand for LDL receptor
Reverse cholesterol transport with HDL
Produced in liver

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9
Q

Importance of apoliprotein CIII

A

Foudn in chylomicrons, VLDL, HDL>LDL

Inhibits Lipoprotein lipase and interferes with ApoB and ApoE binding to hepatic receptors

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10
Q

Lipoprotein Lipase is an important part of what conversion

A

Chylomicrons –> Chylo remnant

VLDL –> IDL

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11
Q

Enzyme that converts from HDL to IDL

A

CETP

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12
Q

Most important enzyme in the synthesis of cholesterol in the liver

A

HMG CoA Reductase

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13
Q

Lipoprotein disorders are detected by measuring….

A

serum lipid after a 10 hr fast

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14
Q

Key measurements in assessing risk of CVD

A

Ratio of Total Cholesterol to HDL-Cholesterol

Ratio over 4.5 is associated with risk, under 3.5 desired

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15
Q

Important details on hyperlipoproteinemia

A

Elevated Cholesterol/LDL Levels
Atherosclerosis – Excess accumulation of cholesterol in vascular smooth muscle
Prematures CAD
Stroke Risk

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16
Q

Hypertriglyceridemia is associated with…

A

Pancreatitis
Xanthomas
CHD risk

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17
Q

Subendothelial uptake of cholesterol by mps is largely facilitated by…

A

Scavenger Receptos
LDLR
mLDL – SR-A, CD36

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18
Q

Mp recetors that allow mature HDL to withdrawl cholesterol

A

SR-B1

ABCG1

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19
Q

Mp receptor associated with giving cholesterol to an immature HDL

A

ABCA1

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20
Q

Three types of drugs used primarily for high cholesterol

A

HMG CoA Reductase Inhibitors
Bile Acid Binding Resins
Inhibitors of Cholesterol Absorption

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21
Q

Drugs used mainl for high triglycerides

A

Fibrates
Niacin
Omega 3 FAs

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22
Q

Mechanism of Bile Acid Binding Resins

A
  • Inhibit the reabsorption of bile acids from intestine by binding bile acids to form insoluble complex that is excreted in feces
  • Loss upregulates LDL receptors in the Liver
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23
Q

Examples of Bile Acid Binding Resins

A

Cholestyramine (Queastran)

Colestipol (Colestid)

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24
Q

Important therapeutic data abotu Bile Acid Binding Resins

A

Treatment of hypercholesterolemia, 20% drop in 2-4 weeks
Taken before meals
Can increase HDL

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25
Q

Side effects of Bile Acid Binding Resins

A

Constipation and Bloating aided by high fiber diet and water

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26
Q

Major drug groups that interfere with Bile Acid Binding Resins absorption

A 
Acetaminophen
Thiazides
Warfarin, Digoxin
Fibrates
Oral Contraceptives
27
Q

Mechanism of Action of Ezetimbe (Zetia)

A

Inhibits intestinal absorption of cholesterol from dietary sources and reabsorption of cholesterol excreted in bile by inhibiting NPC1L1

28
Q

What is NPC1L1’s function?

A

Expressed on the apical surface of enterocytes of the SI.

It senses levels of sterol in the lumen. When there is plenty, triggers a large internal absorption via clathrin)

29
Q

Adverse effects of Ezetimibe

A

Low incidence of liver/skeletal muscle damage

Usually pretty well tolerated tho

30
Q

How to distinguish between a stain and a statin prodrug

A

All the statins have a mevalonic acid ring, which is open. If the ring is closed, it is a prodrug and metabolism will open it.

31
Q

Name three non-prodrug statins

A

Fluvastatin
Rosuvastain (Crestor)
Atorvastatin (Lipitor)

32
Q

Name two statin prodrugs

A

Lovastatin and Simvastatin

33
Q

How do HMG-CoA Reductase inhibitors work

A

Competitively inhibit HMG CoA Reductase, the rate-limiting enzyme in cholesterol biosynthesis
- Also upregulates LD receptors in the liber, reducing plasma cholesterol

34
Q

Explain the mechanism of hepatic LDL receptor upregulation

A

Statins help bind sterols and SCAP in the ER. The lower levels of free statins allow SREBP to be moved to the golgi, where it is cleaved by SCAP to send bHLH to the nucleus. This will upregulate LDL expression in the liver

35
Q

Why give an HMG-CoA Reductase Inhibitor

A

Hypercholesterolemia

Standard practive to initiate after MI

36
Q

Details on Dosing Statins..

A
  • Short half-life ones are takin in evenings, because nighttime is the biggest cholesterol synthesis time.
  • Take lovastatin w/ food
  • Otherwise, a single dose whenever
37
Q

Lovastatin, Simvastatin, and Atorvastatin are broken down by _________. This makes them tend to accumulate in patients taking…

A

CYP3A4

Macrolides, Cyclosporine, Ketoconazole, Grapefruit Juice

38
Q

Fluvastatin and Rosuvastatin are broken down by _____. They tend to accumulate with ……

A

CYP2C9

Cimetidine, Metronidazole, Amiodarone

39
Q

Adverse effects of Statins….

A

Rhabdomyolysis (which will cause renal dysfxn)

Hepatotoxicity

40
Q

statin rhabdomyolysis is especially associated with coadministration wtih…

A

Gemfibrozil

41
Q

Drugs that work by inhibiting ApoB Lipoprotein synthesis?

A

Juxtapid

Mipomersen

42
Q

How does Juxtapid work?

A

Small molecule inhibitor of microsomal TG transfer protein, which stopds assembly of ApoB lipoproteins in the liver and intestine (decreasing absorption).

43
Q

Who should you prescribe Juxtapid or Mipomersen for?

A

Homozygous Familial Hypercholesterolemia

High risk of liver damage, only use if desperate

44
Q

How are Juxtapid and Mipomerson dosed?

A

Jux – Oral

Mipo – SubQ Injection

45
Q

How does Mipomersen work?

A

Hybridized ApoB100 mRNA in the liver to promote its degredation

46
Q

Name same important Fibric Acid Derivatives

A

Gemfibrozil, Fenofibrate

Clofibrate, Ciprofibrate, Benzafibrate

47
Q

Fibric Acid Derivative mechanism of action

A

bind to PPAR-alpha and regulate gene transcription w/ retinoic acid receptor. Cause a complex set of effects, but include reduced LDL, serum TGs, and elevated HDL.

48
Q

What are some important mecahnisms by which PPARs have their effect on blood lipids

A

Increased in Lipoprotein Lipase
Decreased ApoCIII synth –> lower VLDL
Increased ApoA1, AIII synthesis –> higher HDL

49
Q

Therapeutic indications fo Fibric Acid Derivatives

A

Hypertriglyceridemia in which VLDL predominate

Second line for mixed hyperlipidemia

50
Q

Side effects of Fibric Acid Derivatives

A

Gall Stones

Skeletal Muscle Effects (Rhabdo) – ESPECIALYL W/ Statins

51
Q

Importna tdrug interaction of Fibric Acid Derivatives

A

Potentiates the effects of Warfarin

52
Q

What is Lovaza? Mechanism of Action?

A

Combo of Ethyl Esters from Omega 3 Fatty Acids

Reduced TG synthesis in liver, inhibit esterification of other FAs

53
Q

Therapeutic indications for Lovaza

A 
Following a Lipid Lowering Diet
Severe hypertriglyceridemia (over 500)
54
Q

Adverse effects of Lovaza

A

Can increase LDL (usually OK if you combine with a statin)

55
Q

Potential way that Omega 3 FAs may promote CV health

A

Very similar structure to PGI3, which is a potent inhibitor of platelet aggregation

56
Q

In order for Niacin to influence lipids, doses must be…

A

1-3 g/day

Typically a supplement beyond any dietary level

57
Q

How does Nicain decrease TG levels? (conceptually)

A

It reduces them, increasing lipase activity and thus increasing their clearance. It also drops levels of liver VLDL production while typically increasing HDL levels.

58
Q

How does Niacin decrease TG levels (molecularly)?

A

Hits GPR 109A of adipocytes, which drops cAMP and inhibits the conversion of TGs to FFAs. Fewer FFAs will cause lower production of TGs/VLDL In the liver, and thus systemically lower LDL.

59
Q

What is niacin doing specifically in the adipocyte (I know these questions fuckin suck)

A

Acts on GPR109A to inhibit TG lipolysis by hormone sensitive lipase, decreasing FA transport to the liver.

60
Q

What is niacin doing in the liver

A

Inhibits FA synthesis and Esterification

Reduced clearance of apoA-1, but not CEs (inc. HDL)

61
Q

What does niacin do to macrophages?

A

Increased CD36 and ABCA1 expression

Decreases CE content via HDL mediated reverse transport

62
Q

Indications for Niacin

A

Effective for mixed hyperlipidemia
HyperTG w/ risk f pancreatitis
Low HDL
Usually combined with resins

63
Q

Adverse effects of Niacin

A
  • Marked vasodilation (flushing), itching, tingling of Upper body, Headache (too much PG, treat w/ ASA or ibu)
  • Hepatotoxicity

Pharmacology - Test #4 (9 decks)

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