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Pharmacology Test #4 > Anti-hyperlipidemic Drugs > Flashcards

Anti-hyperlipidemic Drugs Flashcards

1
Q

Cholesterol

A

essential component of cell membranes; precursor to sterols and steroids

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2
Q

Triglyceride

A

storage form of fuel to support generation of high energy compounds; component of structural lipids

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3
Q

Lipoproteins transport

A

cholesterol and triglycerides in the blood

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4
Q

Describe the structure of lipoproteins

A

spherical particles with phospholipid, free cholesterol and protein making up surface; core made up of triglyceride and cholesterol ester

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5
Q

Apoproteins on surface of lipoproteins are critical in

A

regulating transport and metabolism

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6
Q

Lipoprotein lipase system

A

release free fatty acids from lipoproteins

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7
Q

Chylomicrons

A

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

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8
Q

VLDL

A

secreted by liver into blood as a source of triglycerides

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9
Q

IDL

A

triglyceride-depleted VLDLs

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10
Q

LDL

A

main transport form in blood

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11
Q

HDL

A

secreted by liver and acquire cholesterol from peripheral tissues and atheromas (reverse cholesterol transport)

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12
Q

ApoA-1

A

structural in HDL; ligand of ABCA1 receptor; mediates reverse cholesterol transport; produced in liver and intestine

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13
Q

ApoB-100

A

structural in VLDL

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14
Q

ApoB-48

A

structural in chylomicrons; produced in intestine

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15
Q

ApoE

A

ligand for LDL receptor remnant receptor; reverse cholesterol transport with HDL; produced in liver and other tissues

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16
Q

ApoCIII

A

found in chylomicrons, VLDL, HDL > LDL; inhibits LPL and interferes with ApoB and ApoE binding to hepatic receptors

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17
Q

LPL-Lipoprotein lipase

A

in capillaries of fat, cardiac and skeletal muscle

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18
Q

LCAT

A

lethicin-cholesterol acyltransferase

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19
Q

CETP

A

cholesterol ester transfer protein

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20
Q

Hyperlipoproteinemia is related to

A

atherosclerosis; premature coronary artery disease; neurologic disease

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21
Q

Hypertriglyceridemia is related to

A

pancreatitis; xanthomas; increased risk of CHD

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22
Q

Goals of hyperlipidemia drug therapy

A

decrease reabsorption of excreted bile acids; decrease secretion of VLDL from liver; decrease synthesis of cholesterol; increase hydrolysis of lipoprotein triglycerides

23
Q

Drugs mainly for high cholesterol

A

HMG-CoA reductase inhibitors
Bile acid binding resins
Inhibitors of cholesterol absorption

24
Q

Drugs mainly for high triglycerides

A

Fibrates
Niacin
Omega 3 fatty acids

25
Q

Ezetimibe (Zetia)

A

cholesterol absorption inhibitor; inhibits intestinal absorption of cholesterol from dietary sources and reabsorption of cholesterol excreted in bile (inhibits NPC1L1)

26
Q

Indication for Ezetimibe

A

primary clinical effect is reduction of LDL levels; usually used in combination with statins

27
Q

Adverse effects of Ezetimibe

A

low incidence of liver/skeletal muscle damage; generally well tolerated

28
Q

HMG-CoA reductase inhibitor/Statins

A

Fluvastatin (Lescol), Rosuvastatin (Crestor), Atorvastatin (Lipitor); Lovastatin (Mevacor), Simvastatin (Zocor), Pravastatin (Pravachol)

29
Q

MOA of statins

A

competitively inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis

30
Q

Indications for HMG-CoA reductase inhibitors

A

hypercholesterolemia: elevated LDL; elevated LDL with slightly elevated TGs
standard to initiate therapy immediately after MI, irrespective of lipid levels

31
Q

Dosing of Lovastatin

A

should be taken with evening meal to facilitate absorption

32
Q

Dosing of Rosuvastatin, Atorvastatin, and Pravachol

A

taken as a single dose any time of the day

33
Q

Dosing of Fluvastatin XL

A

can be taken as a single dose any time of the day

34
Q

Metabolism of Lovastatin, Simvastatin and Atorvastatin

A

CYP3A4; tends to accumulate in presence of drugs that inhibit or compete for CYP 3A4 (macrolide antibiotics, cyclosporine, ketoconazole; grapefruit juice)

35
Q

Prodrug statins

A

Lovastatin and Simvastatin

36
Q

Metabolism of Fluvastatin and Rosuvastatin

A

inhibitors may increase plasma levels: cimetidine, metronidazole and amiodarone

37
Q

Metabolism of Pravastatin

A

sulfation

38
Q

Adverse effects of HMG-CoA reductase inhibitors

A

Rhabdomyolysis with renal dysfunction secondary to myoglobinuria; dose related phenomenon; monitor serum creatinine phosphokinase; increased incidence when co-administered with CYP inhibitors; may occur with gemfibrozil
Hepatotoxicity: monitor serum transaminase activity

39
Q

Juxtapid (Lomitapide)

A

inhibits assembly of ApoB containing lipoproteins in liver and intestine; interferes with the ability to absorb dietary lipids and fat-soluble vitamins

40
Q

Indications for Juxtapid

A

indicated as adjunct to other treatments for patients with homozygous familial hypercholesterolemia - LDLR mutation

41
Q

Mipomersen (Kynamro)

A

phosphorothioate anti-sense oligonucleotide inhibitor of apoB 100; hybridizes Apo B100 mRNA in liver and promotes degradation

42
Q

Indications for Mipomersen

A

indicated as adjunct to other treatments for patients with homozygous familial hypercholesterolemia

43
Q

Fibrates bind to

A

PPAR-alpha and regulted gene transcription along with the retinoic acid receptor (RXR)

44
Q

Therapeutic indications for fibric acid derivates

A

hypertriglyceridemia in which VLDL predominate; second line drug for mixed hyperlipidemia

45
Q

Side effects of fibric acid derivatives

A

gallstones; skeletal muscle effects - rhabdomyolysis

46
Q

Lovaza

A

combination of ethyl esters of omega-3-fatty acid

47
Q

Lovaza MOA

A

reduce synthesis of triglyceride in liver: omega-3 fatty acids are poor substrates for enzymes responsible for TG synthesis; inhibit esterification of other fatty acids

48
Q

Therapeutic indications for omega-3 fatty acids

A

lipid lowering diet is initiated before Lovaza therapy is started; severe hypertriglyceridemia >500 mg/dl

49
Q

MOA of Niacin

A

reduces serum triglycerides; increases lipase activity to increase clearance of VLDL; decreases hepatic VLDL production; may significantly reduce serum LDL and TG; usually increases HDL levels

50
Q

What does Niacin do in adipose tissue?

A

inhibits TG lipolysis by hormone-sensitive lipase; decreaseing FA transport to liver; via activation of GPR109A

51
Q

What does Niacin do in the liver?

A

inhibits FA synthesis and esterification; reducing TG export via VLDL;
reduces clearance of apoA-1 but no CEs; increases HDL levels and reverse transport

52
Q

What does Niacin do to macrophages?

A

increases expression of CD36 and ABCA1; decreasing CE content via HDL0mediated reverse transport

53
Q

Indications for Niacin

A

effective for mixed hyperlipidemias; effective drug for raising HDL levels; used in combo with resin drugs to treat severe cases of hyperlipidemia; also combined with statins

54
Q

Adverse effects of Niacin

A 
marked vasodilation (cutaneous flushing), itching, tingling of upper body and headache may occur with initial dosing - prostaglandins mediate these (treat with aspirin or ibuprofen)
hepatotoxicity

Pharmacology Test #4 (9 decks)

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