Drugs and Risk Factors for Atherosclerosis

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Questions and Answers

What is the primary mechanism of action for PCSK9 inhibitors?

  • They block absorption of dietary cholesterol in the intestines.
  • They increase HDL cholesterol production.
  • They inhibit triglyceride synthesis in adipose tissues.
  • They enhance the liver's ability to remove LDL cholesterol from the blood. (correct)

Which of the following is an adverse effect associated with Cholestyramine?

  • Diarrhea
  • Bloating (correct)
  • Heartburn
  • Nausea

How often are PCSK9 inhibitors typically administered?

  • Every four weeks
  • Every two weeks (correct)
  • Every month
  • Daily

What is a common limitation of using PCSK9 inhibitors?

<p>High cost (D)</p> Signup and view all the answers

Which effect can be expected from proper adherence to PCSK9 inhibitor therapy?

<p>Decrease in LDL levels by as much as 68-70% (A)</p> Signup and view all the answers

What type of drug is Cholestyramine?

<p>A bile acid sequestrant (A)</p> Signup and view all the answers

What is a potential adverse effect at the site of injection for PCSK9 inhibitors?

<p>Mild skin reactions (C)</p> Signup and view all the answers

What aspect of LDL cholesterol alteration is significant concerning PCSK9 inhibitors?

<p>They enhance the rate of LDL cholesterol clearance. (C)</p> Signup and view all the answers

Cholestyramine has which of the following side effects?

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

What is a characteristic of PCSK9 inhibitors?

<p>They are monoclonal antibodies. (C)</p> Signup and view all the answers

What is the primary therapeutic use of fibric acid derivatives like Gemfibrozil?

<p>To treat hypertriglyceridemia (A)</p> Signup and view all the answers

Which of the following is NOT a reported adverse effect of Gemfibrozil?

<p>Hypertension (D)</p> Signup and view all the answers

How does Gemfibrozil primarily affect triglycerides in the liver and adipose tissue?

<p>By promoting the breakdown of triglycerides (B)</p> Signup and view all the answers

Which of the following drugs is an example of a bile acid binding resin?

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

What role does Gemfibrozil play in the management of cholesterol levels?

<p>It significantly reduces triglycerides and VLDL levels (D)</p> Signup and view all the answers

Which of the following mechanisms is involved in the action of fibric acid derivatives?

<p>They enhance the breakdown of triglycerides via lipolysis (B)</p> Signup and view all the answers

What is a significant factor in the success of cholesterol-lowering drug therapy?

<p>Regular physical activity and behavioral modifications (C)</p> Signup and view all the answers

Which of the following statements about hypertriglyceridemia is correct?

<p>It primarily involves elevated triglycerides in the blood. (C)</p> Signup and view all the answers

What is the primary role of statins in treating hyperlipoproteinemia?

<p>To inhibit HMG-CoA reductase in the liver (C)</p> Signup and view all the answers

Which behavioral factor is known to contribute significantly to the risk of developing atherosclerosis?

<p>Cigarette smoking (D)</p> Signup and view all the answers

A patient presents with symptoms consistent with peripheral artery disease. Which of the following is a likely underlying cause?

<p>Narrowing of arteries due to plaque buildup (A)</p> Signup and view all the answers

What is the main consequence of plaque accumulation in the coronary arteries?

<p>Limitation of oxygen delivery to the heart (D)</p> Signup and view all the answers

Which of the following lipoproteins is known to help protect against heart disease?

<p>High-density lipoprotein (HDL) (D)</p> Signup and view all the answers

In the context of atherosclerosis, what eventually happens to lipid accumulation in the arteries?

<p>It results in calcium deposit formation in plaques (A)</p> Signup and view all the answers

What is the recommended first-line treatment strategy for managing high LDL cholesterol?

<p>Statin therapy combined with lifestyle changes (B)</p> Signup and view all the answers

Which metabolic disorder can lead to the development of secondary hyperlipoproteinemia?

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

What is a common symptom of angina pectoris?

<p>Chest pain during physical exertion (D)</p> Signup and view all the answers

What dietary change is recommended to improve LDL cholesterol levels?

<p>Reduce saturated fat intake (B)</p> Signup and view all the answers

How does obesity relate to the risk of atherosclerosis?

<p>It increases inflammation and promotes plaque buildup (A)</p> Signup and view all the answers

Why is blood lipid analysis important before starting drug therapy for hyperlipoproteinemia?

<p>To identify the type of lipid issue causing the problem (B)</p> Signup and view all the answers

Which of the following conditions is NOT related to atherosclerosis?

<p>High HDL cholesterol level (D)</p> Signup and view all the answers

Match the drug class with its mechanism of action:

Drug Class Mechanism of Action
Statins A. Inhibit HMG-CoA (rate-limiting step in cholesterol biosynthesis)
Sterol absorption inhibitors B. Inhibit transporter in GI tract responsible for cholesterol absorption
Fibric acid derivatives C. Reduce VLDL levels by:
breakdown of triglycerides
decrease VLDL secretion by liver
breakdown of fatty acids in adipose tissue
Bile acid binding resins D. Bind bile acids in intestine, inhibiting their reabsorption, ↑ synthesis of bile from cholesterol in liver
PCSK9 inhibitors E. Inhibit PCSK9, ↑ liver's ability to remove cholesterol from blood

<p>Statins = A Sterol Absorption Inhibitors = B Fibric Acid Derivatives = C Bile Acid Binding Resins = D PCSK9 Inhibitors = E</p> Signup and view all the answers

What is the primary therapeutic effect of statins?

<p>Lowering LDL and cholesterol levels (A)</p> Signup and view all the answers

Which of the following are potential adverse effects of statins?

<p>Liver enzyme elevation (A), Myopathy (E)</p> Signup and view all the answers

What is the primary therapeutic use of Fibric Acid Derivatives?

<p>Treating hypertriglyceridemia (D)</p> Signup and view all the answers

Which of the following are common adverse effects of bile acid binding resins?

<p>Bloating (B), Constipation (E)</p> Signup and view all the answers

Which drug class is typically used as a LAST resort for treating high LDL cholesterol?

<p>PCSK9 inhibitors (A)</p> Signup and view all the answers

Statins are the most effective drugs for lowering LDL cholesterol levels.

<p>True (A)</p> Signup and view all the answers

Fibric acid derivatives are primarily used to treat high cholesterol levels.

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

Bile acid binding resins are effective in lowering HDL levels.

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

What are the two main adverse effects associated with the use of PCSK9 inhibitors?

<p>Mild skin reactions at the site of injection and upper respiratory tract infections</p> Signup and view all the answers

Flashcards

Atherosclerosis

A buildup of plaque in the arteries, narrowing the blood vessel lumen and limiting blood flow.

Coronary Artery Disease (CAD)

A condition caused by atherosclerosis in the coronary arteries, which supply oxygenated blood to the heart.

Heart Failure

A condition where the heart can't pump enough blood to meet the body's needs due to restricted blood flow caused by atherosclerosis.

Peripheral Artery Disease

Atherosclerosis in arteries outside the heart (e.g., legs, arms), causing reduced blood flow to the affected areas.

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Lipoproteins

Protein-lipid complexes that carry cholesterol and triglycerides in the blood.

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HDL

High-density lipoprotein; considered "good" cholesterol, carrying cholesterol away from the arteries to the liver.

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LDL

Low-density lipoprotein; considered "bad" cholesterol as it contributes to plaque buildup in the arteries.

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Statins

Drugs that lower LDL and total cholesterol levels by inhibiting cholesterol production in the liver.

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Ezetimibe

A drug that inhibits cholesterol absorption from the intestines.

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Hyperlipoproteinemia

Blood disorders characterized by an inability to break down lipids/fats in the body.

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Behavioural Risk Factors

Lifestyle choices, such as obesity, smoking, lack of exercise, and high blood pressure, that increase the risk of atherosclerosis.

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Angina Pectoris

Chest pain caused by insufficient oxygen supply to the heart during exertion.

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Cholesterol

A type of fat-like substance that's essential for various body functions, but high levels in the blood can contribute to health problems.

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Cholesterol-Lowering Therapy

A combination of behavioral changes and drug therapy used to lower blood cholesterol and related lipids.

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Cholestyramine's adverse effects

Cholestyramine can cause constipation and bloating.

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Liver's cholesterol role

The liver produces proteins that manage cholesterol levels.

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PCSK9 Inhibitors

These drugs target a protein (PCSK9) to control LDL cholesterol.

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Monoclonal antibodies

Specialized proteins that are used in targeted drug therapies.

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LDL Cholesterol reduction

PCSK9 Inhibitors can significantly lower LDL cholesterol levels.

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PCSK9 Inhibitor administration

PCSK9 Inhibitors are usually given by injection every 2-4 weeks.

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Common side effects (PCSK9 Inhibitors)

Mild skin reactions, injection site reactions, and upper respiratory infections are potential side effects.

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Drug's limitations

PCSK9 Inhibitors might have limitations related to patient compliance.

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LDL cholesterol levels

LDL (low-density lipoprotein) cholesterol levels can be evaluated to assess the effectiveness of treatment.

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Cholesterol metabolism

The process by which the body regulates and manages cholesterol.

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Fibric Acid Derivatives

Drugs that lower triglycerides and VLDL in the blood.

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Mechanism of action (fibric acid)

Increased breakdown of triglycerides by reducing VLDL secretion.

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Hypertriglyceridemia

High levels of triglycerides in the blood.

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Gemfibrozil

Example of a Fibric Acid Derivative used to treat high triglycerides.

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Bile Acid Binding Resin

A medication that lowers cholesterol by binding to bile acids in the gut.

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Cholestyramine

Example of a Bile Acid Binding Resin.

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Adverse Effects (Fibric Acid)

Possible side effects include rashes, upset stomach, myopathy, and hyperkalemia.

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Mechanism of Action (Bile Acid Binding Resin)

Bind bile acids, preventing their reabsorption and therefore lowering cholesterol.

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HMG-CoA Reductase

An enzyme involved in the production of cholesterol in the liver.

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How do Statins work?

Statins inhibit HMG-CoA reductase, the enzyme that produces cholesterol in the liver, thus reducing LDL and total cholesterol levels.

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Stero Absorption Inhibitors

Drugs that prevent the absorption of cholesterol and bile acids in the gut.

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How do Fibric Acid Derivatives work?

They increase the breakdown of triglycerides by reducing the production and secretion of VLDL.

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How do Bile Acid Binding Resins work?

They bind to bile acids in the gut, preventing them from being absorbed back into the bloodstream, thus reducing cholesterol production in the liver.

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Alirocumab and Evolocumab

Examples of PCSK9 inhibitors.

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How do PCSK9 Inhibitors work?

They block the PCSK9 protein, which helps the liver remove LDL-cholesterol, resulting in a decrease in LDL levels.

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Adverse Effects of Statins

Muscle pain (myopathy), liver enzyme elevations, and potential for interactions with other drugs.

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Adverse Effects of Sterol Absorption Inhibitors

Generally well-tolerated, but some individuals may experience diarrhea or abdominal pain.

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Adverse Effects of Fibric Acid Derivatives

Possible side effects may include rashes, upset stomach, muscle problems (myopathy), and elevated potassium levels (hyperkalemia).

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Adverse Effects of Bile Acid Binding Resins

Common side effects include constipation, bloating, and gas.

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Adverse Effects of PCSK9 Inhibitors

Potential side effects include mild skin reactions, injection site reactions, and upper respiratory tract infections.

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When are PCSK9 Inhibitors used?

PCSK9 Inhibitors are typically used as a last resort for individuals with very high LDL cholesterol levels, particularly when other treatments haven't been effective.

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LDL Cholesterol

Low-Density Lipoprotein cholesterol, known as the 'bad' cholesterol as it contributes to plaque buildup in arteries.

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How do Statins lower LDL?

Statins lower LDL cholesterol by inhibiting the production of cholesterol in the liver, leading to a decrease in LDL levels.

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How do Sterol Absorption Inhibitors lower LDL?

They prevent the absorption of dietary cholesterol in the gut, reducing the amount of LDL cholesterol circulating in the blood.

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How do Bile Acid Binding Resins lower LDL?

They bind to bile acids in the gut, preventing their reabsorption, leading to increased cholesterol production and a decrease in LDL levels.

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How do PCSK9 Inhibitors lower LDL?

They block a protein (PCSK9) that prevents the liver from removing LDL cholesterol, allowing the body to clear more LDL from the blood.

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Why is it important to lower LDL?

Lowering high LDL cholesterol levels reduces the risk of atherosclerosis, heart disease, and other cardiovascular problems.

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What are the different types of cholesterol-lowering drugs?

There are statins, sterol absorption inhibitors, bile acid binding resins, and PCSK9 inhibitors, each with a unique mechanism of action.

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Study Notes

Drugs for Atherosclerosis Treatment and Prevention

  • Characterized by plaque buildup in arteries, narrowing blood vessels and limiting blood flow
  • Leading cause of coronary artery disease, peripheral artery disease, and chronic kidney disease.
  • Drugs used in combination with lifestyle changes improve blood cholesterol, triglycerides.
  • Coronary arteries are responsible for oxygenated blood supply to the heart
  • Atherosclerosis involves fatty sludge accumulation in coronary artery walls, leading to narrowed arteries.
  • Calcium deposits can cause stiffness in the hardened arteries.
  • The heart needs more oxygen during exertion, which can result in chest pain (angina pectoris) when inadequate oxygen supply occurs.

Behavioral Risk Factors for Atherosclerosis

  • Obesity (BMI >20%)
  • Cigarette smoking
  • Lack of exercise
  • Hypertension

Lipoproteins

  • Proteins that transport fats in the blood
  • Different types with varying roles.
  • Chylomicrons carry triglycerides from the intestine to the blood and transport dietary fats.
  • Very-low-density lipoproteins (VLDL) carry triglycerides synthesized in the liver.
  • Low-density lipoproteins (LDL) transport cholesterol from the liver to the cells (bad cholesterol).
  • High-density lipoproteins (HDL) transport cholesterol from cells to the liver (good cholesterol). High HDL levels are protective against heart disease.

Hyperlipoproteinemias

  • Blood disorders characterized by inability to break down lipids (especially cholesterol and triglycerides).
  • Primary arises from genetic defects, secondary as a result of medical conditions like diabetes or hypothyroidism.
  • Inherited disorders happen in a predictable pattern (Mendelian). Environmental factors can also contribute to primary.
  • Secondary occur as complications of other metabolic problems.
  • Hyperlipidemia can contribute to poor health
  • Calculation of HDL/LDL ratio is important.
  • Cholesterol is not the only marker to look at, and other substances (like triglycerides) are also relevant.

Therapeutic Measures for Hyperlipoproteinemia

  • Behavioral changes (diet and exercise)
  • Drug therapy
  • The choice of drug therapy depends on lipid analysis (blood test) results.
    • First-line treatment is usually statins.

Statins

  • Inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis.
  • Lower LDL cholesterol, but raise HDL.
  • Commonly used as a first-line therapy to lower cholesterol levels.

Inhibitors of Sterol Absorption (Ezetimibe)

  • Inhibit the absorption of cholesterol from the intestine
  • Often combined with statins to further reduce cholesterol
  • May be used in combination with other medications.

Fibric Acid Derivatives (Gemfibrozil)

  • Lower VLDL and triglycerides levels
  • Used for patients with high triglyceride levels
  • Adverse effects like rashes and muscle pain, but also other possible complications

Bile Acid Binding Resins (e.g., Cholestyramine)

  • Bind to bile acids in the intestine and prevent their reabsorption.
  • This forces the liver to convert more cholesterol into bile acids, which lowers cholesterol levels in the blood.
  • Side effects include constipation and bloating.

PCSK9 Inhibitors

  • Monoclonal antibodies that reduce LDL cholesterol.
  • Given by injection every few weeks.
  • Reduce LDL levels, improving cardiovascular health.

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