Mod 1 lecture 3: antihyperlipidemia agents Flashcards

1
Q

what are lipids

A

hydrophobic molecules made from mostly hydrocarbon chains

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2
Q

what his hyperlipidemia

A

excess lipids in the blood

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3
Q

what are types of lipids

A

fats - triglycerides
sterols - cholesterol
phospholipids - emulsifiers, lipid bilayer

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4
Q

what are lipoproteins

A

serve as carriers to transport lipids (cholesterol, triglycerides) in the blood

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5
Q

what type of proteins carry lipids into the atery wall

A

Apolipoprotein (apo) B- 100

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6
Q

what is LDL

A

low density lipoprotein. - contains (apo) b100

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7
Q

what is VLDL

A

very-low density lipoprotein
secreted by liver and export triglycerides to peripheral tissues
contain (apo) b100

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8
Q

what is chylmicrons

A

formed in the intestine and carry triglycerides of dietary origin, unesterified cholesterol and cholesteryl esters
contain (apo) B100

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9
Q

what is HDL

A

produced by liver and intestine
cholesterol is primary component in core
act as scavengers to take up cholesterol from peripheral tissues and triglyceride from degradation of VLDL
DO NOT contain (apo) B-100

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10
Q

what is the decreasing order of atherogenicity

A

LCL
VLDH
Chylomicrons
HDL

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11
Q

what is cholesterol

A

lipid
responsible for proper cell membrane synthesis and formation of bile acids and steroid hormones
primarily produced in the liver
INSOLUBLE in water so must be bound to lipoproteins for transport

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12
Q

what are tyriglycerides

A

main lipid component of dietary fat and fat deposits of animals
excess stored primarily in fat cells (adipocytes)
source of energy for body
INSOLUBLE in water so must be bound to lipoproteins for transportation

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13
Q

what are the classification of hyperlipidemia

A

primary (familial;hereditary) hyperlipidemia: genetically determined - type 1, 2a,2b, 3,4,5
secondary (acquired) hyperlipidemia:
- hypercholesterolemia: hyperthyroidism, nephrotic syndrome and drugs
- hypertriglyceridemia: DM, alcohol, gout, chronic renal failure

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14
Q

what is optimal total cholesterol level

A

less than or equal to 200 mg/dL

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15
Q

what is the optimal LDL-C level

A

less than or equal to 100 mg/dL

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16
Q

what is the optimal triclyceride level

A

less than or equal to 150 mg/dL

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17
Q

what is the optimal HDL level

A

greater than or equal to 60 mg/dL

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18
Q

what is TLC diet

A

Therapeutic lifestyle change diet for hyperlipoporteinemia

vegetables, fruits, whole grains
legumes and nuts
low-fat dairy produces
low-fat poultry (without skin)
fish and seafoods
non-tropical vegetable oils

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19
Q

what are the main classes of drugs used to treat hyperlipidemia

A

HMG CoA Reductase Inhibitors
Bile Acide Sequestrates
Nicotinic Acid
Cholesterol Absoprtion Inhibitor
Fibric Acids
Omega-3 Fatty Acids

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20
Q

what are the different HMG CoA reductase inhibitors

A

Statins
Atorvastatin (lipitor)
Lovastatin (mevacor)
Pravastatin (pravachol)
Rosuvastatin (crestor)
Simvastatin (Zocor)

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21
Q

what is the MOA for HMG CoA Reductase Inhibitors

A

Inhibits hepatic HMG-CaA reductase -> decrease in cholesterol synthesis -> hepatocytes synthesis more LDL receptors, increase ability to remove LDL from blood

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22
Q

what is HMG CoA reductase

A

a rate of controlling enzyme of the metabolic pathway that produces cholesterol

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23
Q

when are HMG CoA reductase inhibitors usually taken

A

taken at night usually
rosuvastatin and atorvastatin CAN be taken in the morning

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24
Q

what are low intensity therapies used to lower LDL levels

A

Lovastatin
Pravastain
Simvastatin

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25
Q

when are HMG CoA reductase inhibitors usually taken

A

taken at night usually
rosuvastatin and atorvastatin CAN be taken in the morning

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26
Q

what are the high potent statin medications

A

Rosuvastatin
Atorvastatin

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27
Q

what are the indications for HMG CoA reductase inhibitors

A

used to lower the risk of atherosclerotic cardiovascular disease events
helps lower plasma cholesterol levels in all types of hyperlipidemias

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28
Q

what should be avoided when using HMG CoA reductase inhibitors

A

avoid grapefruit or grapefruit juice (increased bioavailability of lovastatin and atorvastatin)

29
Q

when is HMG CoA reductase inhibitors contraindicated?

A

pregnancy
lactation
active or chronic liver disease (liver function checked prior to starting)
Red yeast rice

30
Q

what are the adverse effects of HMG CoA reductase inhibitors

A

elevated liver enzymes
myopathy and rhabdomyolysis
photosensitivity
may increase affect of warfarin - check INR prior
GI upset (N/V, diarrhea, pain, dyspepsia)

31
Q

what statin is labeled by the FDA for decreasing triglycerides as well as LDL and total cholesterol

A

Atorvastatin (Lipitor)

32
Q

what is lovastatin (mevacor)

A

low potency HMG CoA reductase inhibitor
take with meals
immediate release
avoid grapefruit or grapefruit juice

33
Q

what are atorvastatin (lipitor) and Rosuvastatin (crestor)

A

HMG CoA reductase inhibitor
MOST potent LDL-C lowering statin
avoid grapefruit/gf juice

34
Q

what is simvastatin (zocor)

A

Medium potency HMG CoA reductase inhibitor
metabolized by CYP450
inhibitors of CYP450 may cause increased risk of rhabdomyolosis
labeled by the FDA to treat for triglycerides, LDL and total cholesterol

35
Q

what is pravastatin

A

low potency HMG CoA Reductase inhibitor
fully excreted in urine

36
Q

what is Nicotinic acid

A

niacin

37
Q

what is the MOA for Niacin

A

inhibits lipolysis in adipose tissues -> reduced production of FFA and TGs
reduces VLDL secretion from liver -> lowers LDL

38
Q

what are the therapeutic uses of Niacin

A

familial hyperlipidemia, sever hypercholesteremias
often with used with other agents
most effective agent for increased HDL
lowers Lip-A, LDL, and TG

39
Q

what are the adverse effects of Niacin

A

flush, N, abd pain, gout, impaired glucose toleracne, hepatotoxicity, hypotension

40
Q

when is Niacin contraindicated

A

hepatic disease
active peptic ulcer
low BP
severe gout
be cautions when prescribing to diabetics, individuals with high uric acid levels and peptic ulcer disease

41
Q

what are the effects of Niacin

A

increases HDL (most effective agent)
decreases lipoprotein (a)
decreases LDL
lowers triglycerides

42
Q

What are Fibric Acid medications

A

Gemfibrozil (lopid)
Fenofibrate (tricor)

43
Q

what is the MOA for fibric acid medications

A

activates peroxisome proliferator - activated receptors (PPAR) - > up regulate lipoprotein lipase, induce HDL synthesis and decrease liver production of apolipoprotein C

44
Q

what are the therapeutic uses of fibric acids

A

hypertriglyceridemia
treatment in type III hyperlipidemia (dysbetalipoproteinemia)
low HDL

45
Q

when are Fibric Acids contraindicated

A

co-administration with statin therapy increases risk for myopathy and rhabdomyolysis
avoid in renal and hepatic dysfunction
avoid in preexisting gallbladder disease or biliary chirrhosis

46
Q

what are the AE of fibric acid toxicity

A

Gi disturbances (most common)
gallstones
myopathy
hepatic dysfunction
increase effects on warfarin - INR check prior to starting

47
Q

what are the effects of fibric acids

A

decreases secretion of VLDL
increases lipoprotein lipase activity
increase HDL

48
Q

what are bile acid sequestrate medications

A

Cholestyramine (Questran, prevalite)
Colesevelam (Welchol)
Colestipol (colestid)

49
Q

what is the MOA for bile avid sequestrates

A

prevents resorption of bile acid salts in intestines -> increases excretion - > increase synthesis -> liver cells increase LDL receptors, increase LDL uptake and decrease circulating LDL levels

50
Q

what are the indications for bile acid sequestrates

A

type IIa and type IIb hyperlipidemias
elevated LDL
digitalis toxicity
chronic pruritis

51
Q

when are bile acid sequestrates contraindicated

A

Biliary cirrhosis, biliary obstruction
gallstones (cholelitheiasis)
hypertriglyceridemia
GI obstruction
preexisting coagulopathy (hemophilia)
caution in hypothyroid pateints
pregnangy, lactation
prolonged used caution in renal disases

52
Q

what are the AE of bile acid sequestrates

A

constipation
bloating
nausea
flatulence
interferes with absorption of some drugs/fat-soluble vitamin A,
d, E and K
reported to increase serum triglyceride concentration

53
Q

what are the effects of bile acid sequestrants

A

decrease LDL (significant but less than seen in statins)

54
Q

What is cholestyramine
(questran, prevalite)

A

bile acid sequestrate
anonion-exhange resin that binds negatively changed bile acids and salts in small intestines
resin/bile acid complex excreted in feces
can relieve prurutis caused by accumulation of bile aids in patients with biliary stasis

55
Q

What is cholesterol absorption inhibitor

A

Ezetimbie (zetia)

56
Q

What is the MOA of ezetimbie (zetia)

A

acts on cells of the brush border of the small intestine to inhibit dietary cholesterol absorption
also inhibits reabsorption of cholesterol secreted in the bile

57
Q

What is the inidcations for ezetimbe (zetia)

A

used as adjunct therapy to lower LDL
phytosterolemia
mono or combo therapy with statin

58
Q

what are the contraindications of zetia

A

severe hepatic insufficiency
pregnancy/lactation

59
Q

what are the AE of zetia

A

SE rare: hepatic dysfunction (low)
myositis

60
Q

what are the effects of zetia

A

inhibits reabsorption of cholesterol excreted in bile
decreased LDL and phytosterols

61
Q

what are the omega-3 fatty acids

A

alpha-linolenic acid (ALA)
eicosapentaenoic avid (EPA)
Docosahexaenoic acid (DHA)

62
Q

what is the MOA for omega 3 fatty acid

A

inhibit VLDL and triglycerides synthesis in liver

63
Q

what are the indications for omega 3 fatty acid

A

lowering triglycerides
(used as an adjunct to diet and exercise

64
Q

when is fish oil contraindicated

A

avoided if pt has a hx of fish hypersensitivity
pts on anticoagulant, thrombolytic or anti-platelet therapy as bleeding may be increased

65
Q

what are the AE of fish oil

A

GI upset - abd pain, N and diarrhea
fishy aftertaste
increased bleeding risk with those already on anticoags
need to monitor

66
Q

what is Vytorin

A

combination of Ezetimibe (zetia) and simvastatin (zocor)

67
Q

what is Advicor

A

combination of lovastatin and Niacin

68
Q

what is Caduet

A

combination of amlopdipine/atorvastatin

69
Q

what are the injectable medications (monoclonal antibodies)

A

alirocumab (praluent)
Evolocumab (repathya)