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Questions and Answers
Which antihyperlipidemic drug is primarily recognized as the treatment option for hypercholesterolemia?
Which antihyperlipidemic drug is primarily recognized as the treatment option for hypercholesterolemia?
What lifestyle modification is recommended alongside drug therapy for managing hyperlipidemia?
What lifestyle modification is recommended alongside drug therapy for managing hyperlipidemia?
Which of the following statements regarding HDL and its role in coronary artery disease (CAD) is accurate?
Which of the following statements regarding HDL and its role in coronary artery disease (CAD) is accurate?
Recent cholesterol guidelines recommend what type of treatment approach for statin therapy?
Recent cholesterol guidelines recommend what type of treatment approach for statin therapy?
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Which combination therapy option involves using two types of antihyperlipidemic drugs?
Which combination therapy option involves using two types of antihyperlipidemic drugs?
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What effect do statins have on LDL cholesterol levels?
What effect do statins have on LDL cholesterol levels?
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What is the recommended approach for drug therapy in managing hyperlipidemia?
What is the recommended approach for drug therapy in managing hyperlipidemia?
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What is the primary treatment goal of therapy for hyperlipidemia?
What is the primary treatment goal of therapy for hyperlipidemia?
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Which pharmacological approach is crucial for managing hyperlipidemia effectively?
Which pharmacological approach is crucial for managing hyperlipidemia effectively?
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Which type of therapy is NOT commonly recognized as a treatment option for hyperlipidemia?
Which type of therapy is NOT commonly recognized as a treatment option for hyperlipidemia?
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What role does lifestyle modification play in managing hyperlipidemia?
What role does lifestyle modification play in managing hyperlipidemia?
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Which lipoprotein is most strongly associated with an increased risk for coronary heart disease?
Which lipoprotein is most strongly associated with an increased risk for coronary heart disease?
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Identifying both LDL and HDL levels provides insight into what risk?
Identifying both LDL and HDL levels provides insight into what risk?
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Which of the following statements regarding HDL levels is accurate?
Which of the following statements regarding HDL levels is accurate?
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In what circumstance are antihyperlipidemic drugs typically prescribed?
In what circumstance are antihyperlipidemic drugs typically prescribed?
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What combination of cholesterol components constitutes total cholesterol?
What combination of cholesterol components constitutes total cholesterol?
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Which approach can help in achieving plasma lipid treatment goals?
Which approach can help in achieving plasma lipid treatment goals?
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What is the major effect of statins on LDL levels?
What is the major effect of statins on LDL levels?
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Which statement is true regarding the use of niacin in lipid management?
Which statement is true regarding the use of niacin in lipid management?
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What role do bile acid sequestrants play in cholesterol management?
What role do bile acid sequestrants play in cholesterol management?
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What is a common adverse effect associated with statin use?
What is a common adverse effect associated with statin use?
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What is the mechanism of action for ezetimibe in cholesterol management?
What is the mechanism of action for ezetimibe in cholesterol management?
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Fibrates primarily target which type of lipid?
Fibrates primarily target which type of lipid?
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Which of the following is a combination therapy example used to lower LDL cholesterol?
Which of the following is a combination therapy example used to lower LDL cholesterol?
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How do bile acid sequestrants impact cholesterol levels?
How do bile acid sequestrants impact cholesterol levels?
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Study Notes
Lecture #30: Hyperlipidemia Pharmacology
- Julia Hum, PhD is the course instructor
- Course meets Monday, Wednesday, and Friday from 2:00-2:50pm
- Office hours are Monday, Wednesday, and Friday from 11:00am-12:00pm (either in person in 317B or via WebEx)
- Website: marian.edu/medicalschool
Learning Objectives
- Describe the treatment goal(s) of hyperlipidemia
- Recognize the main treatment options for hyperlipidemia and identify their mechanism(s) of action
- Compare and contrast different types of statin therapy regimes
- Identify the difference between hyperlipidemia and heterozygous familial hypercholesterolemia
- Predict the most clinically relevant drug(s) for hyperlipidemia given a lipid panel and relevant medical history
- Explain how combination therapy helps treat hyperlipidemia
Hyperlipidemia
- Hyperlipidemia is an abnormally high concentration of fats or lipids (cholesterol and triglycerides) in the blood
- Caused by a combination of genetic and lifestyle factors
- Lifestyle changes and drug therapy can lead to a 30-40% reduction in mortality
- Antihyperlipidemic drugs are often taken indefinitely to control plasma lipid levels
Top 10 Drugs (Statins)
- Atorvastatin (Lipitor)
- Fluvastatin (Lescol)
- Lovastatin (Mevacor)
- Pitavastatin (Livalo)
- Pravastatin (Pravachol)
- Rosuvastatin (Crestor)
- Simvastatin (Zocor)
- Niacin (Niaspan, Slo-Niacin)
- Gemfibrozil (Lopid)
- Fenofibrate (TriCor, Lofibra, Triglide)
Treatment Goals of Hypercholesterolemia
- The clinically important lipoproteins (in 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 have been associated with decreased CHD risk.
- Reduction of LDL is the primary goal of cholesterol-lowering therapy
MPP in the News
- 'Good' cholesterol (HDL) may not protect against heart disease in white adults, but not in Black adults
- Low HDL-C was associated with increased CHD risk in White, but not Black adults. High HDL-C wasn't protective in either group.
- Current cholesterol-based risk calculations may be inaccurate for Black adults
Treatment Goals of Hypercholesterolemia
- Past guidelines recommended treating to specific LDL targets
- Recent guidelines emphasize high-intensity or moderate-intensity statin therapy without targets.
Treatment Options and HMG-CoA Reductase Inhibitors (Statins)
- Statins (HMG CoA reductase inhibitors) are the primary treatment for hypercholesterolemia
- Four groups receive statin treatment recommendation
- Statin therapy is recommended to four major groups; people with history of CVD, high LDL-C, people with Type 1 or 2 Diabetes 40-75 years old, 10-year ASCVD risk estimate more than or equal 7.5%
Drugs for Hyperlipidemia
- Antihyperlipidemic drugs: HMG CoA reductase inhibitors, niacin, fibrates, bile acid-binding resins, a cholesterol absorption inhibitor, and omega-3 fatty acids
- These can be used alone or in combination
- Drug therapy should always be accompanied by lifestyle modifications (exercise and a diet low in saturated fats).
HMG-CoA Reductase Inhibitors (Statins)
- 3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, also known as statins, are used to lower elevated LDL cholesterol in patients
- Resulting in a substantial reduction in coronary events and death from CHD
- First-line drug for patients with elevated risk of ASCVD
- Benefits include plaque stabilization, improvement of coronary endothelial function; inhibition of platelet thrombus formation; anti-inflammatory activity. Statins have shown value in lowering LDL in patients with (and without) established CHD
Mechanism of Action (Statins)
- Competitive inhibitors of HMG-CoA reductase in the liver.
- Inhibiting de novo cholesterol synthesis which depletes intracellular cholesterol
- Causes the cell to increase the number of cell surface LDL receptors that can bind and internalize LDLs
- Reducing cholesterol synthesis and increasing LDL catabolism
Pharmacokinetics (statins)
- Absorption is variable (30-85%) after oral administration
- Metabolized in the liver
Adverse Effects of Statins
- Elevated liver enzymes
- Liver function should be evaluated before starting therapy
- Hepatic insufficiency can cause drug accumulation
- Myopathy (muscle pain or weakness)
Inhibitors of Cholesterol Absorption
- Reduce cholesterol absorption by the small intestine, particularly dietary cholesterol, and the reabsorption of biliary cholesterol
Inhibitors of Cholesterol Absorption: Ezetimibe
- Selectively inhibits absorption of dietary and biliary cholesterol in the small intestine.
- Blocks the Niemann-Pick C1-like 1 (NPC1L1) transporter.
- Decreases cholesterol delivery to liver, reducing hepatic cholesterol stores, and increases the clearance of cholesterol from the blood.
- Lowers LDL cholesterol by approximately 17% and is used often as an adjunct to statin therapy
Combined Therapy
- Combination therapy, using two or more drugs, is sometimes necessary to achieve treatment goals for plasma lipid levels.
- Combination is useful in lowering LDLs (example: statin with bile acid-binding agent).
- Combining simvastatin and niacin is available in a combined pill form for those with elevated LDL cholesterol and triglycerides
Newer Combination Therapies
- FDA approved Althera's Roszet (Rovastatin and Ezetimibe) tablets for significant cholesterol reduction
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Description
Test your knowledge on antihyperlipidemic drugs and their role in managing hypercholesterolemia. This quiz covers recommended treatments, lifestyle modifications, and the guidelines surrounding statin therapy. Perfect for students and healthcare professionals interested in cardiovascular health.
