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Questions and Answers
What is considered a first-line treatment for patients at elevated risk of ASCVD?
What is considered a first-line treatment for patients at elevated risk of ASCVD?
Which of the following is NOT a therapeutic benefit of HMG CoA reductase inhibitors?
Which of the following is NOT a therapeutic benefit of HMG CoA reductase inhibitors?
What is the primary treatment goal for hypercholesterolemia?
What is the primary treatment goal for hypercholesterolemia?
Which therapeutic benefit is primarily associated with HMG CoA reductase inhibitors?
Which therapeutic benefit is primarily associated with HMG CoA reductase inhibitors?
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In the context of drug therapy for hyperlipidemia, which effect is crucial for preventing heart attacks?
In the context of drug therapy for hyperlipidemia, which effect is crucial for preventing heart attacks?
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Which lipoprotein is the most atherogenic?
Which lipoprotein is the most atherogenic?
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What mechanism do HMG CoA reductase inhibitors primarily employ?
What mechanism do HMG CoA reductase inhibitors primarily employ?
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In treating hyperlipidemia, what effect does combination therapy typically aim to achieve?
In treating hyperlipidemia, what effect does combination therapy typically aim to achieve?
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Which group is most likely to benefit from antihyperlipidemic drugs?
Which group is most likely to benefit from antihyperlipidemic drugs?
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Which of the following actions contributes to the efficacy of HMG CoA reductase inhibitors in cardiac health?
Which of the following actions contributes to the efficacy of HMG CoA reductase inhibitors in cardiac health?
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What is the significance of high HDL levels in relation to heart disease?
What is the significance of high HDL levels in relation to heart disease?
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What impact do HMG CoA reductase inhibitors have on platelet activity?
What impact do HMG CoA reductase inhibitors have on platelet activity?
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Which underlying condition is primarily targeted by treatments with HMG CoA reductase inhibitors?
Which underlying condition is primarily targeted by treatments with HMG CoA reductase inhibitors?
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How do lifestyle changes impact the treatment of hyperlipidemia?
How do lifestyle changes impact the treatment of hyperlipidemia?
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Which statement about HMG CoA reductase inhibitors is true?
Which statement about HMG CoA reductase inhibitors is true?
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What distinguishes heterozygous familial hypercholesterolemia from standard hyperlipidemia?
What distinguishes heterozygous familial hypercholesterolemia from standard hyperlipidemia?
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Which of the following is a key risk factor for requiring treatment with HMG CoA reductase inhibitors?
Which of the following is a key risk factor for requiring treatment with HMG CoA reductase inhibitors?
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What is the expected outcome of long-term antihyperlipidemic therapy?
What is the expected outcome of long-term antihyperlipidemic therapy?
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Which of the following lipoproteins are primarily associated with an increased risk of coronary heart disease?
Which of the following lipoproteins are primarily associated with an increased risk of coronary heart disease?
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What can lead to a significant reduction in mortality among individuals with hyperlipidemia?
What can lead to a significant reduction in mortality among individuals with hyperlipidemia?
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What is the main mechanism by which statins lower plasma cholesterol levels?
What is the main mechanism by which statins lower plasma cholesterol levels?
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Which adverse effect is commonly associated with statin therapy that necessitates monitoring?
Which adverse effect is commonly associated with statin therapy that necessitates monitoring?
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What is the primary action of niacin in lipid management?
What is the primary action of niacin in lipid management?
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What role do fibrates play in lipid management?
What role do fibrates play in lipid management?
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How do bile acid sequestrants lower LDL cholesterol?
How do bile acid sequestrants lower LDL cholesterol?
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What mechanism does ezetimibe utilize to lower LDL cholesterol?
What mechanism does ezetimibe utilize to lower LDL cholesterol?
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Which combination therapy has shown effectiveness in reducing LDL levels?
Which combination therapy has shown effectiveness in reducing LDL levels?
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Which of the following statements about statins is true?
Which of the following statements about statins is true?
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What is a primary benefit of using niacin in lipid therapy?
What is a primary benefit of using niacin in lipid therapy?
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What effect do HMG CoA reductase inhibitors have on LDL receptors?
What effect do HMG CoA reductase inhibitors have on LDL receptors?
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What is the primary treatment recommended for hypercholesterolemia?
What is the primary treatment recommended for hypercholesterolemia?
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Which statement about high-density lipoprotein cholesterol (HDL-C) levels is correct?
Which statement about high-density lipoprotein cholesterol (HDL-C) levels is correct?
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What does recent cholesterol guidelines emphasize regarding treatment?
What does recent cholesterol guidelines emphasize regarding treatment?
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Which combination is recommended for managing hyperlipidemia?
Which combination is recommended for managing hyperlipidemia?
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Which of the following is NOT classified as an antihyperlipidemic drug?
Which of the following is NOT classified as an antihyperlipidemic drug?
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What is the effect of HMG CoA reductase inhibitors?
What is the effect of HMG CoA reductase inhibitors?
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Statin therapy is specifically recommended for which of the following groups?
Statin therapy is specifically recommended for which of the following groups?
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What dietary modification is recommended alongside drug therapy for hyperlipidemia?
What dietary modification is recommended alongside drug therapy for hyperlipidemia?
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In what context is high HDL-C not considered protective?
In what context is high HDL-C not considered protective?
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Which of the following treatment strategies has been emphasized in the latest cholesterol management guidelines?
Which of the following treatment strategies has been emphasized in the latest cholesterol management guidelines?
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Study Notes
Lecture #30: Hyperlipidemia Pharmacology
- Julia Hum, PhD, is the Primary Course Instructor
- Course meets Monday/Wednesday/Friday, 2:00-2:50pm
- Office hours are Monday/Wednesday/Friday, 11:00am-12:00pm (317B or WebEx)
- Marian University, College of Osteopathic Medicine
L30: Learning Objectives
- Describe treatment goals for hyperlipidemia
- Recognize main treatment options and mechanisms of action
- Compare and contrast statin therapy regimens
- Differentiate between hyperlipidemia and heterozygous familial hypercholesterolemia
- Predict relevant drugs given a lipid panel and medical history
- Explain how combination therapy treats hyperlipidemia
ASCVD: Coronary Heart Disease
- Hyperlipidemia is an abnormally high concentration of fats or lipids (cholesterol and triglycerides) in the blood
- It results from a combination of genetic and lifestyle factors
- Appropriate lifestyle changes and drug therapy can reduce mortality by 30% to 40%
- Antihyperlipidemic drugs are often taken indefinitely to control plasma lipid levels
Treatment Goals of Hypercholesterolemia
- Clinically important lipoproteins (decreasing order of atherogenicity): LDL, VLDL/chylomicrons, HDL
- High total cholesterol and elevated LDL are positively associated with coronary heart disease (CHD) risk
- High levels of HDL correlate with a decreased risk of CHD
- Reducing LDL is the primary goal of cholesterol-lowering therapy
MPP in the News
- A study found that low HDL cholesterol increased heart disease risk in white adults but not black adults
- Current high-density lipoprotein cholesterol-based risk calculations may be inaccurate for black adults
Treatment Goals of Hypercholesterolemia: Effect of circulating LDL and HDL on risk of CHD
- Past guidelines recommended treating to specific LDL targets
- Recent guidelines emphasize high-intensity or moderate-intensity statin therapy
Treatment options for Hypercholesterolemia
- HMG CoA reductase inhibitors (statins) are the primary treatment option
- Statin therapy is recommended for four major groups
Drugs for Hyperlipidemia
- Antihyperlipidemic drugs include HMG-CoA reductase inhibitors (statins), niacin, fibrates, bile acid-binding resins, cholesterol absorption inhibitors, and omega-3 fatty acids
- These drugs may be used alone or in combination
- Drug therapy should always be accompanied by lifestyle modifications (exercise and a diet low in saturated fats)
Drugs for Hyperlipidemia: HMG CoA reductase inhibitors
- 3-Hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitors (statins) lower elevated LDL
- Resulting in a substantial reduction in coronary events and death from CHD
- Statins are first-line treatment for patients with elevated risk of atherosclerotic cardiovascular disease (ASCVD)
Drugs for Hyperlipidemia: HMG CoA reductase inhibitors (cont.)
- Therapeutic benefits include plaque stabilization, improved coronary endothelial function, inhibition of platelet thrombus formation, and anti-inflammatory activity
- The value of lowering LDL with statins has been demonstrated in patients with and without established CHD
- Mechanism of action: competitive inhibitors of HMG CoA reductase, the rate-limiting step in cholesterol synthesis
- Inhibits de novo cholesterol synthesis, depleting intracellular cholesterol supply
- Causes the cell to increase the number of surface LDL receptors, leading to decreased cholesterol synthesis and increased LDL catabolism
- Pharmacokinetics: variable absorption (30% to 85%) following oral administration; metabolized in the liver.
Drugs for Hyperlipidemia: HMG CoA reductase inhibitors (cont.)
- Adverse effects: elevated liver enzymes and myopathy may occur
- Liver function should be evaluated prior to starting therapy
- Hepatic insufficiency can cause drug accumulation
Inhibitors of Cholesterol Absorption
- Reduce cholesterol absorption in the small intestine
- Reduce reabsorption of biliary cholesterol
- Inhibitors of cholesterol absorption decrease LDL cholesterol by inhibiting hepatic production of VLDL (very-low-density lipoprotein)
Inhibitors of Cholesterol Absorption - Niacin
- MOA: strongly inhibits lipolysis in adipose tissue, reducing FFA production
- Reduced liver triglyceride levels decrease hepatic VLDL production, thus reducing LDL plasma concentrations
- Niacin reduces LDL by 10% to 20% and increases HDL
- It also lowers triglycerides by 20% to 35% at typical doses
Inhibitors of Cholesterol Absorption - Fibrates
- Fenofibrate and gemfibrozil are derivatives of fibric acid; lower triglycerides and increase HDL levels
- MOA: PPARs (peroxisome proliferator-activated receptors) are members of the nuclear receptor family regulating lipid metabolism; increased expression of lipoprotein lipase causes decreased triglyceride concentrations
- PPAR activation increases expression of apoAI (apolipoprotein AI) and apoAII
- Fibrates increase HDL cholesterol levels by increasing expression of apoAI and apoAII
Inhibitors of Bile Acid Absorption: Resins
- Bile acid sequestrants (resins) lower LDL cholesterol
- MOA: bind negatively charged bile acids and salts in the small intestine; this resin/bile acid complex is excreted in the feces, thus lowering bile acid concentration
- This causes hepatocytes to increase conversion of cholesterol to bile acids, which lowers intracellular cholesterol concentrations
- This activates increased hepatic uptake of cholesterol-containing LDL particles, leading to lowered plasma LDL concentration
- Mediated by up-regulation of cell surface LDL receptors
- Clinical uses: hyperlipidemia, often in combination with diet or niacin
Cholesterol absorption inhibitor: Ezetimibe
- Selectively inhibits absorption of dietary and biliary cholesterol in the small intestine by blocking Niemann-Pick C1-like 1 (NPC1L1)
- Leads to a decrease in the delivery of intestinal cholesterol to the liver
- Causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood
- Ezetimibe lowers LDL cholesterol by approximately 17%
Combination Therapy
- Often necessary to use two antihyperlipidemic drugs to achieve treatment goals in plasma lipid levels
- Combining an HMG CoA reductase inhibitor with a bile acid-binding agent has been shown to be very useful in lowering LDL levels
- Simvastatin and niacin are currently available as a combined medication.
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Description
Join this quiz to test your knowledge on hyperlipidemia pharmacology, where you'll explore crucial treatment goals, options, and mechanisms of action. You'll also dive into the comparison of statin therapies and the differentiation of hyperlipidemia types. Enhance your understanding of how lifestyle changes and drug therapy can impact coronary heart disease.
