Antihyperlipidemia Flashcards

1
Q

What are the main lipids that are important for medications

A

Triglycerides
Cholesterol

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2
Q

What is the purpose of lipoproteins

A

Serve as carriers to transport lipids in the blood

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3
Q

What type of lip are responsible for carrying lipids into the artery wall

A

Apolipoprotein (apo)B-100

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4
Q

What type of lipid is apo B100

A

LDL
*mutations in it cause a familial hypercholesterolemia

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5
Q

What is VLDL and where is it found

A

Very low density lipoprotein

Secreted by liver and export triglycerides to peripheral tissue

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6
Q

What are chylomicrons

A

Formed in the intestine and carry triglycerides from diet, unesterfied cholesterol, and cholesteryl esters

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7
Q

What produces HDL

A

Liver and intestines

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8
Q

What is the only lipoprotein that DOES NOT contain apo B100

A

HDL

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9
Q

What is the purpose of HDL

A

Acts as scavenger to take up cholesterol from peripheral tissue and triglycerides from degradation of VLDL

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10
Q

What is the role of cholesterol

A

Responsible for proper cell membrane synthesis and formation of bile acids / steroid hormones

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11
Q

What is the function of triglycerides

A

source of energy for the body

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12
Q

What is primary hyperlipidemia

A

Genetically determined
(Increase chylomicrons)

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13
Q

What is secondary hyperlipidemia

A

Acquired
(Increase in LDL / VLDL)

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14
Q

What causes hypercholesterolemia

A

hypothyroidism
nephrotic syndrome
drugs

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15
Q

What causes hypertriglyceridemia

A

DM
Gout
Alcohol
Chronic renal failure

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16
Q

What are the low potency statin medications

A

Lovastatin
Pravastatin

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17
Q

What is a medium potency statin

A

Simvastatin

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18
Q

What are high potency statins

A

Rosuvastatin
Atorvastatin

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19
Q

When is Lovastatin used

A

Low / moderate intensity therapy to lower LDL levels

Primary & secondary prevention of coronary events

Prevention of MI/Stroke in T2 diabetes

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20
Q

When is Pravastatin used

A

Low / moderate intensity therapy to lower LDL levels

Primary & secondary prevention of coronary events

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21
Q

What is the MOA for statins (Low, Medium, or high potency)

A

Inhibits hepatic HMG-CoA reductase=
decrease in cholesterol synthesis =
Hepatocytes synthesize more LDL receptors = increase ability to remove LDL from blood

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22
Q

When is Simvastatin used

A

-Low/ mod intensity therapy to lower LDL levels
-Primary & secondary prevention of coronary events
-Approved for decr TGs, LDL, and total cholesterol

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23
Q

What is the use of rosuvastatin

A

-Most potent statin
-Mod or high intensity therapy to lower LDL levels
-Primary prevention of coronary events
-Approved for reducing risk of CV events in people w normal LDL levels

24
Q

What is the use of atorvastatin

A

-Most potent statin
-Mod or high intensity therapy
-Primary & secondary prevention of coronary events, prevention of MI/stroke in T2 diabetes
-Approved for decr TGs, LDL, and total cholesterol

25
What is the indication of nicotinic acid
-Familial hyperlipidemias, severe hypercholesteremias -Often used w other agents -Most effective agent for incr HDL -Lowers lip-A, LDL, and TG
26
What are the bile acid sequestrates
Colesevelam Cholestyramine Colestipol
27
What is the MOA for the bile acid sequestrates
-Prevent resorption of bile acid salts in intestines = incr excretion = incr synth = liver cells incr LDL receptors, incr LDL uptake and decr circulating LDL levels
28
What food needs to be avoided when taking HMG CoA reductase drugs and why
Grapefruit / grapefruit juice Increased bioavailability of lovastatin and atorvastatin
29
What is the pharmacokinetics of pravastatin
-Oral admin -Rapid hepatic metabolism -Dose adjust in mod-severe renal impairment
30
What is the pharmacokinetics of Lovastatin
-Oral admin, take w meals -Rapid hepatic metabolism -Metabolized by CYP3A4 -Dose adjust in severe renal impairment
31
What is the pharmacokinetics of Simvastatin
Oral admin -Rapid hepatic metabolism -Metabolized by CYP3A4 (the 3A4 isoenzyme of cytochrome P450) -Dose adjust in severe renal impairment
32
What are the adverse reactions and contraindications of low potency HMG CoA reductase inhibitors
-HA, rash, dyspepsia, cramps, flatulence, constipation, abdominal pain -Serious adverse effects: hepatotoxicity and myopathy -Contra in pregnancy, avoid grapefruit juice
33
What is the pharmacokinetics of Rosuvastatin
-Oral admin -Rapid hepatic metabolism -Dose adjust in severe renal impairment and w Asian pts
34
What are the adverse reactions and contraindications of Rosuvastatin
HA, rash, dyspepsia, cramps, flatulence, constipation, abdominal pain -Serious adverse effects: hepatotoxicity and myopathy -Highest risk for rhabdomyolysis -Contra in pregnancy, avoid grapefruit juice
35
What is the pharmacokinetics of atorvastatin
-Oral admin -Rapid hepatic metabolism -Metabolized by CYP3A4 (the 3A4 isoenzyme of cytochrome P450) -No dose adjustment needed
36
What are the adverse reactions and contraindications of atorvastatin
-HA, rash, dyspepsia, cramps, flatulence, constipation, abdominal pain -Serious adverse effects: hepatotoxicity and myopathy -Contra in pregnancy, avoid grapefruit juice
37
What is the indication of nicotinic acid
-Familial hyperlipidemias, severe hypercholesteremias -Often used w other agents -Most effective agent for incr HDL -Lowers lip-A, LDL, and TG
38
What is the MOA of nicotinic acid
-Inhibits lipolysis in adipose tissues = reduced production of free fatty acids and TGs -Reduces VLDL secretion from liver = lowers LDL
39
What are the pharmacokinetics of nicotinic acid
-Oral admin -Comes in immediate, ER, and SR preparations *SR reduces adverse effects
40
What are the adverse effects and contraindications of nicotinic acid
-Flush, nausea, adb pain, gout, impaired glucose tolerance, hepatotoxicity, hypotension -Contra in hepatic dz, peptic ulcer dz, low BP, severe gout -Caution in diabetics, high uric acid levels, peptic ulcer dz
41
What is the indication of colesevelam
Bile acid sequestrate DOC -Lowers LDL: primary hypercholesterolemia -Can help control hyperglycemia in patients with T2 diabetes -Chronic pruritus, digitalis toxicity -Can be alone but usu combo w statin
42
What are the adverse reactions and contraindications of Colesevelam
Constipation, bloating, indigestion, nausea Contraindicated in biliary cirrhosis, gallstones, pregnancy, hypertryglyceridemia
43
What are the indications for cholestyramine and colestipol
-Bile acid sequestrant -Reduces LDL cholesterol: primary hypercholesterolemia -Can be used alone but usu combined w a statin
44
What are the adverse reactions and contraindications of Cholestyramine and colestipol
-Constipation, bloating, indigestion, and nausea -Decr uptake of fat-soluble vitamins -Can form insoluble complexes w other drugs
45
What are the fibrate drugs
Gemfibrozil Fenofibrate
46
What is the indication for fenofibrate
-Principal indication is hypertriglyceridemia -Lowers VLDL and raises HDL -More effective than gemfibrozil in lowering TGs
47
What are the adverse reaction and contraindications for Gemfibrozil
-Rash and GI disturbances -Gall stones, myopathy, liver injury -Incr risk of bleeding in pts taking warfarin, incr risk of myopathy in combo w statin -Contra in renal, hepatic, and gallbladder dz
48
What are the contraindications and adverse reactions in Fenofibrate
-Rash and GI disturbances, gall stones, liver injury -Contra in hepatic and gallbladder dz
49
What is the indication for Ezetimibe
-Usu used as adjunct therapy to lower LDL -Phytosterolemia -Mono or combo therapy w a statin
50
What is the MOA of Ezetimibe
-Acts on cells of the brush border of the sm intestine to inhibit dietary cholesterol absorption -Also inhibits reabsorption of cholesterol secreted in the bile
51
What are the pharmacokinetics of Ezetimibe
-Absorption not affected by food -Undergoes extensive conversion to ezetimibe glucuronide (active metabolite)
52
What are the adverse reactions and contraindications of ezetimibe
SE are rare Contraindicated in patients with hepatic insufficiency and pregnancy
53
What is the indication of fish oil
Essential fatty acid used for dietary supplementation to lower TGs
54
What is the MOA of fish oil
Inhibit VLDL and triglyceride synthesis in the liver
55
What are the adverse effects and contraindications of fish oil
GI disturbances Fishy aftertaste **Contra indicated in fish allergies and patients on anticoags
56
What is a cholesterol absorption inhibitor drug
Ezetimibe