Treatment of Hyperlipidemia
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Questions and Answers

What is the effect of niacin-extended-release and lovastatin tablets on LDL-C?

  • Reduces (correct)
  • Unknown
  • No effect
  • Increases

Ezetimibe is a statin.

False (B)

What is the brand name of niacin-extended-release and lovastatin tablets?

Advicor

Ezetimibe acts within the __________ to reduce cholesterol absorption.

<p>intestine</p> Signup and view all the answers

What is the primary use of Gemfibrozil?

<p>Reducing triglycerides (C)</p> Signup and view all the answers

Statins are used to reduce triglycerides.

<p>False (B)</p> Signup and view all the answers

What is the effect of Ezetimibe on cholesterol absorption?

<p>Reduces</p> Signup and view all the answers

Match the following drugs with their primary use:

<p>Cholestyramine = Reducing cholesterol Ezetimibe = Reducing triglycerides Gemfibrozil = Reducing cholesterol Niacin = Reducing triglycerides and cholesterol</p> Signup and view all the answers

What is the available dosage of niacin-extended-release and lovastatin tablets?

<p>All of the above (D)</p> Signup and view all the answers

Ezetimibe blocks one or more of __________ transporters.

<p>cholesterol</p> Signup and view all the answers

Flashcards

Statins: Mechanism of Action

Statins block the enzyme HMG-CoA reductase, which leads to a decrease in cholesterol synthesis and an increase in LDL receptors to clear more cholesterol from the blood.

Statins: Clinical Effects

Statins lower LDL cholesterol, lower triglycerides, and raise HDL cholesterol.

Bile Acid Sequestrants: Mechanism of Action

Bile acid sequestrants bind to bile acids in the gut, preventing them from being reabsorbed into the bloodstream. This forces the liver to use more cholesterol to make new bile acids, lowering cholesterol levels.

Fibrates: Mechanism of Action

Fibrates activate PPARα, a protein that regulates gene expression related to lipid metabolism, leading to changes in triglyceride and cholesterol levels.

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Nicotinic Acid (Niacin): Mechanism of Action

Niacin reduces VLDL synthesis in the liver by inhibiting fatty acid synthesis and esterification, and by reducing lipolysis in adipose tissue.

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Inhibitors of Intestinal Sterol Absorption: Mechanism of Action

These medications block cholesterol absorption in the intestines by inhibiting specific cholesterol transporters.

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Statins: Adverse Effects

Statins can cause muscle pain (myositis), liver enzyme elevation, and rarely, muscle breakdown (rhabdomyolysis).

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Bile Acid Sequestrants: Adverse Effects

These drugs can cause constipation, heartburn, and malabsorption of fat-soluble vitamins.

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Fibrates: Adverse Effects

Fibrates can cause digestive problems like diarrhea and bloating, and can also prolong the QT interval on an EKG.

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Nicotinic Acid (Niacin): Adverse Effects

Niacin can cause flushing, headache, and digestive problems, and may worsen gout or peptic ulcers.

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Study Notes

Treatment of Hyperlipidemia

  • Certain drugs should be avoided in pregnant and lactating women, and those likely to become pregnant.
  • All drugs that alter plasma lipoprotein concentrations may require adjustment of warfarin doses.

Treatment of Children with Hyperlipidemia

  • Children with heterozygous familial hypercholesterolemia may be treated with resins or statins after 7 or 8 years of age, when myelination of the CNS is complete.
  • The decision to treat a child should be based on the level of LDL, other risk factors, the family history, and the child's age.
  • Drugs are rarely indicated before age 16.

HMG-CoA Reductase Inhibitors (Statins)

  • Mechanism of action: Inhibit the synthesis/activity of HMG-CoA reductase, leading to increased LDL receptors and decreased secretion of VLDL.
  • Clinical effects:
    • Decrease LDL cholesterol by 30-40%.
    • Decrease plasma triglycerides by 10-30%.
    • Increase HDL cholesterol by 5-15%.
  • Therapeutic uses:
    • Familial and non-familial hypercholesterolemias.
    • May reduce the incidence of some cancers.
    • May reduce osteoporosis.
    • May have weak anti-inflammatory activity.
  • Adverse effects:
    • Nausea, epigastric fullness, distension, constipation, and headache.
    • Mild increase in transaminases.
    • Myositis (0.1-0.2%).
    • Rarely, rhabdomyolysis.
    • Hypotension.
  • Combination regimens: Statins/bile acid sequestrants combination exerts an additive effect on LDL cholesterol.

Bile Acid Sequestrants

  • Mechanism of action: Bind bile acids, preventing enterohepatic recycling of bile acids, leading to increased synthesis of bile acids from endogenous cholesterol.
  • Clinical effects:
    • Decrease LDL cholesterol by 10-30% in patients with normal LDL receptors.
    • Do not affect HDL cholesterol levels.
  • Dosage and administration: Powder taken with water or fruit juice, starting with one sachet daily and increasing as needed.
  • Adverse effects:
    • Constipation, heartburn, abdominal pain, bloating, and nausea.
    • Impair absorption of fat-soluble vitamins and other substances.
    • Bind other acidic drugs.

Fibrates

  • Mechanism of action: Stimulate the activity of peroxisome proliferating activating receptors alpha (PPARα), altering transcription of genes involved in triglyceride metabolism.
  • Clinical effects:
    • Decrease total serum cholesterol and LDL-C levels by about 10-20%.
    • No change in triglyceride levels.
    • Increase serum HDL-cholesterol concentrations by 15-20%.
  • Adverse effects:
    • Diarrhea, bloating, indigestion, and heartburn.
    • Headache, arthralgia.
    • Increase the QT interval on the electrocardiogram.

Nicotinic Acid (Niacin, B3)

  • Mechanism of action: Reduces VLDL synthesis in the liver, hence LDL, by inhibiting the synthesis and esterification of fatty acids in the liver and reducing lipolysis in adipose tissue.
  • Clinical effects:
    • At high doses, affects all plasma lipid subtypes.
    • Lowers plasma total and LDL cholesterol by 10-25%.
    • Decreases triglycerides by 5-30%.
    • Increases plasma HDL cholesterol by 10-20%.
  • Adverse effects:
    • Flushing, tingling, and headache.
    • Nausea, flatulence, and diarrhea.
    • May exacerbate peptic ulceration and gout.
    • Relatively contraindicated in gout and in diabetics.

Inhibitors of Intestinal Sterol Absorption

  • Mechanism of action: Acts within the intestine to reduce cholesterol absorption by blocking one or more of cholesterol transporters.
  • Examples: Ezetimibe (Zetia).
  • Used alone or combined with a statin.
  • Adverse effects: Fatigue, abdominal pain, and diarrhea.

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Description

This quiz covers the treatment of hyperlipidemia, including avoiding certain drugs in pregnant women and adjusting doses of warfarin, as well as treating children with familial hypercholesterolemia. Learn about the guidelines for treatment and risk assessment.

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