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Pharm term 2 module 1 > Antihyperlipidemia > Flashcards

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
Q

What is the indication of nicotinic acid

A

-Familial hyperlipidemias, severe hypercholesteremias
-Often used w other agents
-Most effective agent for incr HDL
-Lowers lip-A, LDL, and TG

26
Q

What are the bile acid sequestrates

A

Colesevelam
Cholestyramine
Colestipol

27
Q

What is the MOA for the bile acid sequestrates

A

-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
Q

What food needs to be avoided when taking HMG CoA reductase drugs and why

A

Grapefruit / grapefruit juice

Increased bioavailability of lovastatin and atorvastatin

29
Q

What is the pharmacokinetics of pravastatin

A

-Oral admin
-Rapid hepatic metabolism

-Dose adjust in mod-severe renal impairment

30
Q

What is the pharmacokinetics of Lovastatin

A

-Oral admin, take w meals
-Rapid hepatic metabolism
-Metabolized by CYP3A4

-Dose adjust in severe renal impairment

31
Q

What is the pharmacokinetics of Simvastatin

A

Oral admin
-Rapid hepatic metabolism
-Metabolized by CYP3A4 (the 3A4 isoenzyme of cytochrome P450)

-Dose adjust in severe renal impairment

32
Q

What are the adverse reactions and contraindications of low potency HMG CoA reductase inhibitors

A

-HA, rash, dyspepsia, cramps, flatulence, constipation, abdominal pain
-Serious adverse effects: hepatotoxicity and myopathy
-Contra in pregnancy, avoid grapefruit juice

33
Q

What is the pharmacokinetics of Rosuvastatin

A

-Oral admin
-Rapid hepatic metabolism

-Dose adjust in severe renal impairment and w Asian pts

34
Q

What are the adverse reactions and contraindications of Rosuvastatin

A

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
Q

What is the pharmacokinetics of atorvastatin

A

-Oral admin
-Rapid hepatic metabolism
-Metabolized by CYP3A4 (the 3A4 isoenzyme of cytochrome P450)

-No dose adjustment needed

36
Q

What are the adverse reactions and contraindications of atorvastatin

A

-HA, rash, dyspepsia, cramps, flatulence, constipation, abdominal pain
-Serious adverse effects: hepatotoxicity and myopathy
-Contra in pregnancy, avoid grapefruit juice

37
Q

What is the indication of nicotinic acid

A

-Familial hyperlipidemias, severe hypercholesteremias
-Often used w other agents
-Most effective agent for incr HDL
-Lowers lip-A, LDL, and TG

38
Q

What is the MOA of nicotinic acid

A

-Inhibits lipolysis in adipose tissues = reduced production of free fatty acids and TGs
-Reduces VLDL secretion from liver = lowers LDL

39
Q

What are the pharmacokinetics of nicotinic acid

A

-Oral admin
-Comes in immediate, ER, and SR preparations

*SR reduces adverse effects

40
Q

What are the adverse effects and contraindications of nicotinic acid

A

-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
Q

What is the indication of colesevelam

A

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
Q

What are the adverse reactions and contraindications of Colesevelam

A

Constipation, bloating, indigestion, nausea
Contraindicated in biliary cirrhosis, gallstones, pregnancy, hypertryglyceridemia

43
Q

What are the indications for cholestyramine and colestipol

A

-Bile acid sequestrant
-Reduces LDL cholesterol: primary hypercholesterolemia
-Can be used alone but usu combined w a statin

44
Q

What are the adverse reactions and contraindications of Cholestyramine and colestipol

A

-Constipation, bloating, indigestion, and nausea
-Decr uptake of fat-soluble vitamins
-Can form insoluble complexes w other drugs

45
Q

What are the fibrate drugs

A

Gemfibrozil
Fenofibrate

46
Q

What is the indication for fenofibrate

A

-Principal indication is hypertriglyceridemia
-Lowers VLDL and raises HDL
-More effective than gemfibrozil in lowering TGs

47
Q

What are the adverse reaction and contraindications for Gemfibrozil

A

-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
Q

What are the contraindications and adverse reactions in Fenofibrate

A

-Rash and GI disturbances, gall stones, liver injury
-Contra in hepatic and gallbladder dz

49
Q

What is the indication for Ezetimibe

A

-Usu used as adjunct therapy to lower LDL
-Phytosterolemia
-Mono or combo therapy w a statin

50
Q

What is the MOA of Ezetimibe

A

-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
Q

What are the pharmacokinetics of Ezetimibe

A

-Absorption not affected by food

-Undergoes extensive conversion to ezetimibe glucuronide (active metabolite)

52
Q

What are the adverse reactions and contraindications of ezetimibe

A

SE are rare

Contraindicated in patients with hepatic insufficiency and pregnancy

53
Q

What is the indication of fish oil

A

Essential fatty acid used for dietary supplementation to lower TGs

54
Q

What is the MOA of fish oil

A

Inhibit VLDL and triglyceride synthesis in the liver

55
Q

What are the adverse effects and contraindications of fish oil

A

GI disturbances
Fishy aftertaste
**Contra indicated in fish allergies and patients on anticoags

56
Q

What is a cholesterol absorption inhibitor drug

A

Ezetimibe

Pharm term 2 module 1 (3 decks)

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