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Cardio Drugs > Hyperlipidemia Drugs > Flashcards

Hyperlipidemia Drugs Flashcards

1
Q

Statin indication

A

High LDL, hypercholesterolemia, treatment/prevention of heart disease. Choose Pravastatin if need to use Cyclosporins!

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2
Q

Statin effect on LDL

A

↓ 20-60%

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3
Q

Statin effect on HDL

A

↑ 5-10%

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4
Q

Statin effect on Trigly

A

↓ 10-20%

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5
Q

Statin MOA

A

Inhibits HMG Co-A reductase and triggers increased LDL-R expression resulting in increased LDL clearance

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6
Q

Statin Adverse Effects

A

mild GI, mm myalgia (pain)/myopathy (weakness), RHABDOMYOLYSIS, Hepatitis

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7
Q

Statin Contra-indications

A

Pregnancy or lactation, liver disease, gemfibrozil pts (increased risk of rhabdomyolysis)

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8
Q

Statin Drug interactions

A

CYP3A4 inhibitors (erythromycin, cyclosporin and grapefruit juice increase LSA).

CYP 3A4 inducers (phenytoin, rifampin) decrease LSA.

CYP2C9 inhibitors (ketoconazole/metroconazole) increase FR.

Decreased Glucoronidation (gemfibrozil, fibrates) increases ALL statins (LSA, FR and P)

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9
Q

Statin Notes/Reminder

A

LSA=Lovastatin, Simvastatin and Atrovastatin. FR=Fluvastatin and Rosuvastatin. P=Pravastatin. Simvastatin=Zocor Myositis (inflammation) and Rhabdomyolysis are rare but occur at higher doses and in pts with polymorphism of anion transporter.

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10
Q

Bile Acid Binding Resins Cholestyramine Colestipol Colesevelam effect on LDL

A

_ 10-25%

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11
Q

Bile Acid Binding Resins Cholestyramine Colestipol Colesevelam effect on HDL

A

minimal increase

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12
Q

Bile Acid Binding Resins Cholestyramine Colestipol Colesevelam type and indication

A

High LDL, hypercholesterolemia. Drug of choice for children and women of childbearing age or who are pregnant.

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13
Q

Bile Acid Binding Resins (Cholestyramine Colestipol Colesevelam) effect on Trigly

A

minimal to slight increase

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14
Q

Bile Acid Binding Resins (Cholestyramine Colestipol Colesevelam) MOA

A

Bind to bile acids, preventing reabsorption, which diverts hepatic cholesterol to synthesis of new bile acids, stimulates LDL-R production upon drop in hepatic cholesterol pool.

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15
Q

Bile Acid Binding Resins (Cholestyramine Colestipol Colesevelam) Adverse Effects

A

mild GI, bloating. Can INCREASE trigly levels if pt has hypertriglyceridemia

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16
Q

Bile Acid Binding Resins (Cholestyramine Colestipol Colesevelam) Contra-indications

A

type III dysbetalipoproteinemia (due to risk of increased triglys)

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17
Q

Bile Acid Binding Resins (Cholestyramine Colestipol Colesevelam) Notes/Reminder

A

treat cholestasis/bile salt accumulation pt’s pruritus (itch)

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18
Q

Ezetimibe (Zetia) type and indication

A

High LDL

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19
Q

Ezetimibe (Zetia) effect on LDL

A

↓ 18%

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20
Q

Ezetimibe (Zetia) effect on HDL

A

minimal effect

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21
Q

Ezetimibe (Zetia) effect on Trigly

A

minimal effect

22
Q

Ezetimibe (Zetia) MOA

A

Inhibits absorption of cholesterol (NPC1L1 txporter in intestine) and cholesterol excreted in bile, decrease tightly regulated hepatic pool, stimulate LDL-R production.

23
Q

Ezetimibe (Zetia) Adverse Effects

A

mild GI symptoms, low incidence of liver problems (reversible)

24
Q

Ezetimibe (Zetia) Contra-indications

A

pregnancy, mild to severe hepatitis, hypersensitivity to drug

25
Q

Ezetimibe (Zetia) Drug interactions

A

Bile acid resins interfere with absorption (decrease levels). Cyclosporin increases levels of Zetia. Fibrates increase active, glucuronide form.

26
Q

Ezetimibe (Zetia) Notes/Reminder

A

combination with HMG-CoA inhibitor makes more effective (Zetia+Zocor=Vytorin); converted in liver to active glucuronide form; NP is neimann-pick receptor

27
Q

Niacin type and indication

A

High VLDL High LDL Low HDL. Wide applications: Can be used for hypertriglyceridemia, hypercholesterolemia, to fix low HDL levels.

28
Q

Niacin effect on LDL

A

_ 10-20%

29
Q

Niacin effect on HDL

A

_ 10-30% *best at increasing HDLS!

30
Q

Niacin effect on Trigly

A

_ 30-80%

31
Q

Niacin MOA

A

THREE MOA situations: 1-block of HSTL causes decreased lipolysis in adipocytes which decreases FFA (decrease triglys) which decreases VLDL and then LDL.

2-increased apo A-1 needed to build HDL (increase HDL),

3-decreased thrombosis due to decreased lipoprotein (a)

32
Q

Niacin Adverse Effects

A

skin flushing, hepatitis (elevation of liver enzymes and severe hepatotoxicity), GOUT (hyperuricemia), hyperglycemia, peptic ulcers

33
Q

Niacin Contra-indications

A

diabetics (due to possible CHO intolerance), hx of Gout, impaired liver function, pregnancy (risk of gestational diabetes)

34
Q

Niacin Drug interactions

A

**use of Niacin is really limited by poor tolerability, many side effects**

35
Q

Niacin Notes/Reminder

A

pre-treatment with NSAIDS can reduce skin flushing (suggests a PG mechanism for the flushing). Elevated triglys are a risk factor for pancreatitis!

36
Q

Fibrates (Gemfibrozil Fenofibrate) type and indication

A

High VLDL, Low HDL. Good for pts. w/ very high triglys that may be at risk for pancreatitis. Drug of choice for Familial dysbetalipoproteinemia

37
Q

Fibrates (Gemfibrozil Fenofibrate) effect on LDL

A

may increase LDL in genetic pts.

38
Q

Fibrates (Gemfibrozil Fenofibrate) effect on HDL

A

↑ 10-20%

39
Q

Fibrates (Gemfibrozil Fenofibrate) effect on Trigly

A

↓ 40-80%

40
Q

Fibrates (Gemfibrozil Fenofibrate) MOA

A

drug is ligand for perioxisome proliferator activated receptor alpha (PPAR-alpha) protein, which regulates transcription of genes in lipid metabolism. Increases lipoprotein lipase (LPL) which metabolizes CyM, and increases FA oxidation in liver, decreasing VLDLs. Increases ApoA1 which increases HDLs. Decreases apoCIII synthesis (building block of LDL)

41
Q

Fibrates (Gemfibrozil Fenofibrate) Adverse Effects

A

nausea, skin rashes, increased cholesterol gallstones (block of bile acid production enzyme leads to more free cholesterol), hepatitis, myopathy, rhabdomyolysis (rare, more with Gemfib)

42
Q

Fibrates (Gemfibrozil Fenofibrate) Contra-indications

A

pt hx of cholelithiasis (gall stones). Gemfibrozil affects liver uptake of statins and metab/excretion. Fenofibrate is drug of choice for combo therapy b/c doesn’t interfere w/statins.

43
Q

Fibrates (Gemfibrozil Fenofibrate) Drug interactions

A

STRONG PROTEIN BINDERS, lots of interactions!! No statins (increased risk of rhabdomyolysis, must choose Feno if have to), Cyclosporin (risk of renal tox), Sulfonylureas (inc hypoglycemia) or Warfarin (inc risk of bleeding)

44
Q

Fibrates (Gemfibrozil Fenofibrate) Notes/Reminder

A

VLDL is very triglyceride rich and is precursor to LDL. CyM are expogenous form of triglys, metabolized by LPL in capillary. Elevated triglys are a risk factor for pancreatitis!

45
Q

Familial Hypercholesterolemia

A

Hyperlipoproteinemia Type IIa

0.2% frequency

LDL receptor defect

↑ LDL

Atherosclerosis +++

46
Q

Familial apoB100 defect

A

Hyperlipoproteinemia Type IIa

0.1% frequency

↓ Binding of LDL to LDLR

↑ LDL

Atherosclerosis +++

47
Q

Polygenic Hypercholesterolemia

A

Hyperlipoproteinemia Type IIa

Relatively common

Unknown defects result in impaired clearance of LDLs

↑ LDL

Atherosclerosis +++

47
Q

Familial Combined Hyperlipidemia

A

Type IIb

0.5% frequency

Unknown (polygenic): Overproduction of B100 & triglycerides (VLDL) and decreased clearance of LDL

↑ VLDL and ↑ LDL

Atherosclerosis +++ (insulin resistance w/obesity often)

48
Q

Familial Dysbetalipoproteinemia

A

Hyperlipoproteinemia Type III

0.02% frequency

Mutant ApoE: Increased production/decreased clearance of VLDL remnants

↑ IDL

Atherosclerosis +++

49
Q
A

Cardio Drugs (7 decks)

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