Week 7: Antilipidemics Flashcards

1
Q

HMG CoA Reductase Inhibitors - “statins” (Atorvastatin/Rosuvastatin) MOA

A
  • block synthesis of cholesterol in the liver by competitively inhibiting the HMG CoA reductase activity - best at lowering LDL
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2
Q

HMG CoA Reductase Inhibitors - drug interactions

A
  • CYP 3A4 inhibitors - “azoles” - increase statin concentration
  • CYP 3A4 inducers - “rifampin” - decrease statin concentrations
    Pravastatin - not affected by grapefruit juice
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3
Q

HMG CoA reductase inhibitors cautions/ contraindications

A
  • Pregnancy Category X - not safe in pregnancy
  • Avoid in active liver disease
  • Avoid grapefruit juice with simvastatin, lovastatin and atorvastatin - can increase toxicity
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4
Q

HMG CoA reductase inhibitors ADRs

A
  • myalgias/myopathies –> increased CPK - rhabdo/metabolic acidosis
  • headache
  • fatigue
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5
Q

Statin Monitoring

A
  • check lipid levels 4 to 6 weeks after starting therapy and then every 3 to 4 months until control is established
  • LDL levels guide dose increases
  • LFTs before starting therapy and then 3 to 6 months later only is suspected issues or underlying hepatic disease
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6
Q

Niacin MOA

A
  • uncertain but appears to reduce VLDL synthesis - best at increasing HDL
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7
Q

Niacin cautions/ contraindications

A
  • avoid w/ hx of gout
  • avoid w/ hepatic dysfunction
  • avoid in uncontrolled diabetes
  • avoid w/ active peptic ulcers
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8
Q

Niacin ADRs

A
  • pruritis, flushing, hepatotoxicity
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9
Q

Niacin Pt education

A
  • take anti-inflammatory strength NSAID 30 minutes prior to dose to decrease ADRs
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10
Q

Fibrates (Gemfibrozil/Fenofibrate) MOA

A
  • Increased plasma and hepatic lipoprotein lipase (LPL) activity - inhibition of cholesterol and triglyceride synthesis - inhibition of lipolysis in adipose tissue - decreased production of VLDL
  • *best at decreasing triglyceride levels**
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11
Q

Fibrates ADRs

A

dyspepsia, abdominal pain - cholelithiasis

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12
Q

Fibrates cautions/ contraindications

A
  • avoid in liver or renal disease
  • avoid in pre-existing gallbladder disease
  • avoid in pregnancy and lactation
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13
Q

Bile Acid Sequestrants (Cholestyramine/Questran) MOA

A
  • indirectly blocks absorption of cholesterol by forming a nonabsorbable complex with bile acids in the intestine - increase the number of LDL receptors on the cell membrane for greater uptake in the liver and less in the bloodstream
  • *can increase triglycerides**
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14
Q

Bile Acid sequestrants ADRs

A

flatulence, bloating, abdominal pain, constipation

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15
Q

Bile Acid sequestrants cautions/ contraindications

A
  • avoid in pts w/ elevated triglycerides >300
  • safe in pregnancy and lactation
  • must take other medications and vitamins either 1 hour before or 4 hours after this medication
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16
Q

Cholesterol Absorption Inhibitors (Ezetimibe/Zetia) MOA

A
  • directly blocks endogenous absorption of cholesterol - leads to a decreased delivery of cholesterol to the liver, decreased hepatic cholesterol stores, and increased clearance of cholesterol from the bloodstream
  • can safely be used with -statins
17
Q

Ezetimibe/Zetia ADRs

A
  • fatigue
  • diarrhea
  • arthralgias/joint pain
18
Q

Ezetimibe/Zetia cautions/contraindications

A
  • avoid in liver dz

- avoid in pregnancy/lactation

19
Q

PCSK9 (Evolocumab/Repatha) MOA

A
  • subq injection - binds to circulating PCSK9 and inhibits the binding of PCSK9 to LDL receptors allowing for increased LDL receptors on the cell surface, decreasing LDL in the blood stream - 50 to 70% LDL reducation as monotherapy (can be used with statins)
    Indication: genetic DO: familial homozygous hypercholesteremia
20
Q

PCSK9 ADRs

A
  • pain at injection site

- anaphyslaxis

21
Q

PCSK9/Repatha cautions/ contraindications

A
  • avoid in pregnancy/lactation
22
Q

Four Major Statin Benefit Groups

A
  • Group 1: nave clinical ASCVD - use high intensity statin if = 75y/o - use moderate intensity statin is > 75 y/o
  • Group 2: No ASCVD but have LDL-C levels >/= 190 - high intensity statin unless contraindication/unable to tolerate
    Group 3: No ASCVD - age 40-75 w/ diabetes and LDL levels of 70-189 - moderate intensity statin if 10yr ASCVD risk is <7.5%; high intensity statin if 10yr ASCVD risk is > 7.5%
    Group 4: NO ASCVD or DM; age 40-75 w/ LDL-C 70-189 and 10yr ASCVD risk >/= 7.5%- moderate intensity statin