Drugs for Hyperlipidemia
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Questions and Answers

What type of cholesterol is primarily considered 'bad cholesterol' and is correlated with coronary heart disease?

  • Cholesterol absorption inhibitors
  • Low-density lipoprotein (LDL-C) (correct)
  • High-density lipoprotein (HDL-C)
  • Triglycerides

Which of the following is NOT classified as an antihyperlipidemic drug?

  • Fibrates
  • Beta-blockers (correct)
  • Omega-3 fatty acids
  • HMG CoA reductase inhibitors (statins)

What lifestyle factor can contribute to elevated cholesterol levels according to the overview provided?

  • Mediterranean diet
  • Excess saturated fat in diet (correct)
  • Regular physical activity
  • Low carbohydrate intake

Statin therapy is primarily recommended for which of the following conditions?

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

Which of the following drugs is an example of a fibrate used for treating hyperlipidemia?

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

What is the recommended effect of lifestyle changes when combined with drug therapy for lipid control?

<p>A 30-40% reduction in CHD mortality (A)</p> Signup and view all the answers

Elevated triglycerides are primarily linked to which of the following health conditions?

<p>Coronary heart disease (A)</p> Signup and view all the answers

Which of the following treatments is suggested for managing hypertriglyceridemia?

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

What is the primary reason patients who are homozygous for familial hypercholesterolemia benefit less from certain cholesterol treatments?

<p>They lack LDL receptors. (A)</p> Signup and view all the answers

What is the absorption rate of statins following oral administration?

<p>Variable at 30-85% (C)</p> Signup and view all the answers

What adverse effect related to liver function should be monitored before and during statin therapy?

<p>Elevated liver enzymes. (C)</p> Signup and view all the answers

Which condition may increase the risk of rhabdomyolysis in patients taking simvastatin?

<p>Renal insufficiency. (A)</p> Signup and view all the answers

What is the typical dose range of niacin for lowering triglycerides?

<p>1.5-3 g/d. (B)</p> Signup and view all the answers

How does niacin primarily reduce LDL-C levels?

<p>By inhibiting lipolysis in adipose tissue. (D)</p> Signup and view all the answers

Which enzyme metabolizes simvastatin, increasing the risk of interactions when inhibited?

<p>Cytochrome P450 3A4. (A)</p> Signup and view all the answers

What is a common side effect of statins that may necessitate monitoring plasma creatine kinase levels?

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

What is a primary therapeutic use of niacin?

<p>Treating familial hyperlipidemias (B)</p> Signup and view all the answers

How is niacin processed in the body after oral administration?

<p>It is converted to nicotinamide (C)</p> Signup and view all the answers

What side effect is commonly associated with niacin use?

<p>Intense cutaneous flush (C)</p> Signup and view all the answers

Which of the following statements is true regarding the use of aspirin with niacin?

<p>Aspirin prevents cutaneous flushing (B)</p> Signup and view all the answers

Which of the following is a mechanism of action for fibrates?

<p>Activation of peroxisome proliferator activated receptors (PPARs) (B)</p> Signup and view all the answers

Which of the following is true about fenofibrate compared to gemfibrozil?

<p>Fenofibrate is more effective than gemfibrozil in lowering triglyceride levels (B)</p> Signup and view all the answers

What effect does niacin have on uric acid levels?

<p>It inhibits tubular secretion of uric acid (A)</p> Signup and view all the answers

What potential risk is associated with the use of niacin in patients with hepatic disease?

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

Which drugs are primarily effective in lowering triglyceride levels?

<p>Niacin and fibric acid derivatives (B)</p> Signup and view all the answers

What is the primary benefit of statins in hyperlipidemia treatment?

<p>Reduction of LDL-C (A)</p> Signup and view all the answers

Which of the following statins is considered the most potent in lowering LDL cholesterol?

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

How do HMG CoA reductase inhibitors primarily decrease LDL cholesterol levels?

<p>By inhibiting cholesterol synthesis and increasing LDL receptor numbers (A)</p> Signup and view all the answers

Which statement about the therapeutic uses of statins is accurate?

<p>They lower cholesterol levels in all types of hyperlipidemias. (D)</p> Signup and view all the answers

Which of these drugs is known for a secondary benefit of triglyceride reduction?

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

Which of the following is NOT a mechanism by which statins exert their therapeutic effects?

<p>Inhibition of diastolic blood pressure (C)</p> Signup and view all the answers

What is the mechanism behind the increased LDL receptor numbers when using statins?

<p>Decreased intracellular cholesterol levels (C)</p> Signup and view all the answers

What is the primary therapeutic use of fibrates?

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

What is the primary effect of bile acid binding resins on cholesterol metabolism?

<p>They enhance the conversion of cholesterol to bile acids. (D)</p> Signup and view all the answers

Which of the following is a common adverse effect of fibrates?

<p>Mild gastrointestinal disturbances (C)</p> Signup and view all the answers

Which conditions are indicated for the use of bile acid binding resins?

<p>Type IIA and type IIB hyperlipidemias (C)</p> Signup and view all the answers

What is the fate of fenofibrate after oral administration?

<p>It is converted to fenofibric acid, the active moiety (B)</p> Signup and view all the answers

Which condition is a contraindication for fibrates?

<p>Severe hepatic dysfunction (C)</p> Signup and view all the answers

What is a common adverse effect associated with bile acid sequestrants?

<p>GI disturbances such as constipation (B)</p> Signup and view all the answers

What effect do fibrates have on HDL cholesterol levels?

<p>They increase HDL cholesterol levels (C)</p> Signup and view all the answers

How do bile acid binding resins affect the absorption of other drugs?

<p>They impair the absorption of many drugs. (B)</p> Signup and view all the answers

Which of the following statements about colesevelam is true?

<p>It is used for glucose-lowering effects in type 2 diabetes. (D)</p> Signup and view all the answers

Which substance is primarily responsible for the formation of glucuronide conjugates during the metabolism of fibrates?

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

What is the mechanism of action of ezetimibe?

<p>It inhibits the absorption of dietary and biliary cholesterol. (B)</p> Signup and view all the answers

What is the mechanism of action of bile acid sequestrants?

<p>They bind negatively charged bile acids in the intestine (A)</p> Signup and view all the answers

What should be monitored more frequently when a patient is taking both gemfibrozil and warfarin?

<p>INR (International Normalized Ratio) (B)</p> Signup and view all the answers

What is the ideal time to take other medications in relation to bile acid binding resins?

<p>1 to 2 hours before or 4 to 6 hours after (B)</p> Signup and view all the answers

What is a contraindication for the use of bile acid sequestrants?

<p>Significant hypertriglyceridemia over 400 mg/dL (D)</p> Signup and view all the answers

Flashcards

Hyperlipidemia

Elevated levels of lipids in the blood, including cholesterol and triglycerides.

Statins

Drugs that lower LDL cholesterol by inhibiting HMG-CoA reductase, an enzyme in cholesterol production.

Hypercholesterolemia

High levels of cholesterol in the blood; a type of hyperlipidemia.

LDL-C

Low-density lipoprotein cholesterol, considered "bad" cholesterol, linked to heart disease.

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HDL-C

High-density lipoprotein cholesterol, considered "good" cholesterol, helps remove cholesterol.

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Hypertriglyceridemia

Elevated levels of triglycerides in the blood; a type of hyperlipidemia.

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Lifestyle Modifications

Changes in diet and exercise habits to improve health, for some cases.

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Primary Treatment for Hypercholesterolemia

Statins are the initially recommended treatment option for high cholesterol.

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Statins' Primary Benefit

Statins primarily lower LDL-C (bad cholesterol), reducing the risk of heart disease.

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Statins' Secondary Benefit

Statins also help lower triglycerides, although this isn't their main function.

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Mechanism of Statins in Lowering Cholesterol

Statins block an enzyme (HMG-CoA reductase) that makes cholesterol, and this then leads to cells making more receptors for taking LDL-C from the blood.

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Niacin and Fibric Acids

These drugs are effective in lowering triglycerides.

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Omega-3 Fatty Acids

Omega-3 fatty acids (like those in fish oil) can also help lower triglycerides to a varying extent.

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HMG CoA Reductase

An enzyme that plays a crucial role in cholesterol production.

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Homozygous Familial Hypercholesterolemia & Statins

Patients with this genetic condition lack LDL receptors, making them less responsive to statin treatment.

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Statin Metabolism

Most statins are metabolized in the liver, with some metabolites retaining their activity. Excretion occurs primarily through bile and feces.

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Statin Adverse Effects

Statins can cause elevated liver enzymes and muscle problems like myopathy and rhabdomyolysis.

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Statin Interactions

Statins can interact with other medications, such as erythromycin, gemfibrozil, niacin, and warfarin, increasing the risk of side effects.

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Niacin's Effect on Lipids

Niacin reduces LDL-C (10-20%), increases HDL-C, and lowers triglycerides (20-35%).

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Niacin's Mechanism of Action

Niacin inhibits lipolysis in adipose tissue, reducing free fatty acid production, which in turn reduces triglyceride synthesis and LDL-C.

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Niacin and Statins

Niacin can be used alongside statins, improving the effectiveness of cholesterol management.

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Fixed-Dose Combination

A specific combined drug containing lovastatin and long-acting niacin is available.

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Niacin's Lipid-Lowering Effect

Niacin (vitamin B3) reduces both cholesterol and triglyceride levels in the blood. It's used to treat high lipid levels, especially in combination with other medications.

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Niacin's Side Effects

Niacin can cause flushing (redness), itching, nausea, and abdominal pain. Aspirin can reduce flushing. Long-term use could lead to gout, glucose intolerance, and liver problems.

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PPARs: Lipid Regulators

Peroxisome proliferator-activated receptors (PPARs) are proteins in the body that control lipid metabolism. They respond to fatty acids and medications like fibrates.

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Fibrates' Action on Triglycerides

Fibrates (like fenofibrate and gemfibrozil) lower triglyceride levels and increase HDL ('good') cholesterol. They activate PPARs to increase lipoprotein lipase and decrease apoCII.

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Lipoprotein Lipase (LPL)

An enzyme essential for breaking down triglycerides in the blood. Fibrates increase its activity, leading to lower triglyceride levels.

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ApoCII and Fibrates

Fibrates decrease the concentration of apolipoprotein CII (apoCII), a protein that inhibits lipoprotein lipase activity. This helps lower triglycerides.

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Fenofibrate vs. Gemfibrozil

Both are fibrates, but fenofibrate is more effective at lowering triglycerides than gemfibrozil.

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Niacin and Fibrates: Complementary

Niacin and fibrates are often used together to target both cholesterol and triglyceride levels in individuals with hyperlipidemia.

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Fibrates: What do they do?

Fibrates are medications that primarily help reduce triglycerides (fat) in the blood, thereby improving cholesterol levels. They work by increasing the activity of an enzyme (lipoprotein lipase) that breaks down triglycerides.

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Fibrate's Effect on HDL?

Fibrates not only decrease triglycerides but also increase the levels of 'good' cholesterol (HDL) by boosting the production of proteins (apo AI and apo AII) that help form HDL.

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How are fibrates used therapeutically?

Fibrates are used to treat high triglyceride levels (hypertriglyceridemia) and a specific type of cholesterol disorder called type III hyperlipidemia where 'bad' cholesterol accumulates.

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What's a prodrug?

A prodrug is a medication that's inactive when taken but gets converted into an active form within the body. Fenofibrate is a prodrug that transforms into fenofibric acid to become effective.

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Common side effects of fibrates?

The most common side effects of fibrates are mild stomach issues that often lessen as the treatment continues. However, they can also increase the risk of gallstones and muscle problems, so careful monitoring is needed.

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Fibrates and Warfarin:

Fibrates can increase the effects of warfarin (a blood thinner), making the chances of bleeding higher. Therefore, close monitoring of the blood-thinning effect is crucial when taking both drugs.

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Bile acid sequestrants: What are they?

Bile acid sequestrants are medications that help lower cholesterol by binding to bile acids in the gut, preventing their reabsorption and causing them to be excreted in the stool. This action triggers the liver to use more cholesterol to make new bile acids, thus lowering overall cholesterol.

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What are bile acid sequestrants good for?

Bile acid sequestrants, primarily cholestyramine, colestipol, and colesevelam, are medications that can lower 'bad' cholesterol (LDL) levels, although their effectiveness is less than other cholesterol-lowering drugs like statins.

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Bile Acid Sequestrants

Drugs that bind to bile acids in the gut, preventing their reabsorption and increasing their excretion. This leads to lower cholesterol levels by stimulating the liver to produce more bile acids, which uses up more cholesterol.

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Bile Acid Sequestrants: How They Work

They bind to bile acids in the gut, preventing their reabsorption and increasing their excretion. This triggers the liver to produce more bile acids, which uses up more cholesterol. This process ultimately leads to a decrease in blood cholesterol levels.

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Bile Acid Sequestrants: Uses

Used to treat type IIA and IIB hyperlipidemias (high cholesterol) often alongside diet or niacin. They can also relieve itching (pruritus) caused by bile acid buildup in patients with blocked bile ducts.

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Bile Acid Sequestrants: Absorption

These drugs are not absorbed from the intestines. They are not broken down by the body but instead, are excreted in the feces.

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Bile Acid Sequestrants: Side Effects

Common side effects include GI disturbances like constipation, nausea, and gas. These drugs can also interfere with the absorption of fat-soluble vitamins and some medications.

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Ezetimibe: What it Does

This drug specifically blocks the absorption of cholesterol from food and bile in the small intestine. This helps to lower cholesterol levels by reducing the amount reaching the liver.

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Ezetimibe: Benefit

By preventing cholesterol from entering the liver, Ezetimibe lowers the amount of cholesterol available for the body to use. This ultimately leads to lower cholesterol levels in the blood.

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Ezetimibe: Where it Works

It works primarily in the small intestine, blocking the absorption of dietary and biliary cholesterol. This means it targets cholesterol before it reaches the liver.

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Study Notes

Drugs for Hyperlipidemia

  • Coronary heart disease (CHD) is the leading cause of death worldwide, correlated with high levels of low-density lipoprotein cholesterol (LDL-C), triglycerides, and low levels of high-density lipoprotein cholesterol (HDL-C).
  • Other risk factors for CHD include smoking, hypertension, obesity, and diabetes.
  • Elevated cholesterol levels can be caused by lifestyle factors, such as a lack of exercise or a diet high in saturated fats.
  • Hyperlipidemias can also result from a combination of genetic and lifestyle factors.
  • Appropriate lifestyle changes, along with drug therapy, can lead to a 30-40% reduction in CHD mortality.
  • Antihyperlipidemic drugs are often taken indefinitely to control plasma lipid levels.

Types of Drugs for Hyperlipidemia

  • HMG CoA Reductase Inhibitors (Statins): Lower LDL-C, reducing coronary events and death from CHD.
    • Atorvastatin (Lipitor)
    • Fluvastatin (Lescol)
    • Lovastatin (Mevacor)
    • Pitavastatin (Livalo)
    • Pravastatin (Pravachol)
    • Rosuvastatin (Crestor)
    • Simvastatin (Zocor)
  • Fibrates: Lower triglycerides and increase HDL levels.
    • Gemfibrozil
    • Fenofibrate
  • Niacin: Reduces LDL-C, increases HDL-C, and lowers triglycerides.
  • Cholesterol Absorption Inhibitors: Selectively inhibit cholesterol absorption
    • Ezetimibe (Zetia)
  • Bile Acid Sequestrants: Bind bile acids, lowering LDL-C.
    • Colesevelam (Welchol)
    • Colestipol (Colestid)
    • Cholestyramine (Questran, Prevalite)
  • Omega-3 Fatty Acids: Lower triglycerides.
    • Docosahexaenoic and eicosapentaenoic acids (Lovaza)
    • Icosapent ethyl (Vascepa)

Mechanism of Action and Therapeutic Uses

  • Drugs work through various mechanisms to lower cholesterol, including inhibiting cholesterol synthesis, increasing LDL receptors, and affecting triglyceride production.
  • These drugs are used to treat a variety of hyperlipidemias, types I, IIA, IIB, III, IV, and V, affecting different lipoprotein profiles.
  • Patients with homozygous familial hypercholesterolemia respond less well to the drugs.

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Description

This quiz covers the types and functions of antihyperlipidemic drugs, focusing on their role in managing cholesterol levels and reducing the risk of coronary heart disease (CHD). It includes specific classes of drugs such as statins and their impact on LDL and HDL cholesterol. Test your understanding of how lifestyle factors contribute to hyperlipidemia and the importance of drug therapy.

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