Antihyperlipidaemia and Drug Classifications
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How does the reduction of bile acid concentration affect hepatic cholesterol levels?

  • Decreases hepatic cholesterol due to decreased de novo production of bile acids.
  • Decreases hepatic cholesterol due to increased de novo production of bile acids. (correct)
  • Increases hepatic cholesterol due to increased de novo production of bile acids.
  • Increases hepatic cholesterol due to decreased de novo production of bile acids.

Which of the following best describes the mechanism of action of bile acid binding resins?

  • Binding to bile acids in the small intestine and preventing their reabsorption. (correct)
  • Binding to bile acids in renal tubules and promoting their excretion.
  • Enhancing the enterohepatic circulation of bile acids.
  • Inhibiting the synthesis of bile acids in the liver.

What is the primary reason bile acid binding resins are contraindicated in patients with severe hypertriglyceridemia?

  • They interfere with the metabolism of triglycerides in the liver.
  • They increase plasma LDL levels, exacerbating the condition.
  • They decrease plasma HDL levels, worsening the lipid profile.
  • They can further elevate plasma VLDL-TG levels, worsening the condition. (correct)

A patient taking cholestyramine complains of indigestion and abdominal discomfort. Which of the following side effects is MOST likely responsible for these symptoms?

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

What compensatory mechanism is triggered by the action of bile acid sequestrants?

<p>Increased HMG-CoA reductase activity (A)</p> Signup and view all the answers

Which of the following is a clinical application of bile acid sequestrants unrelated to hypercholesterolemia?

<p>Alleviation of pruritus in cholestatic patients (C)</p> Signup and view all the answers

Why should other orally administered drugs be taken either one hour before or four hours after taking bile acid resins?

<p>To prevent the resin from impairing the absorption of the other drugs (B)</p> Signup and view all the answers

Which of the following is a potential effect of bile acid sequestrants on plasma lipids?

<p>Decrease in plasma LDL (B)</p> Signup and view all the answers

A patient presents with symptoms of easy bruising and prolonged bleeding times. Which of the following side effects of bile acid sequestrants could be contributing to these findings?

<p>Vitamin K malabsorption (A)</p> Signup and view all the answers

Which classification of hyperlipoproteinemia is characterized by elevated levels of chylomicrons, triglycerides, and cholesterol?

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

What is the primary action of HMG-CoA reductase inhibitors in managing hyperlipidemia?

<p>Inhibits cholesterol synthesis (A)</p> Signup and view all the answers

Which drug class includes medications that are effective in increasing HDL levels?

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

What is a common outcome when statins are combined with resins?

<p>Reduction of LDL to nearly 80% (A)</p> Signup and view all the answers

What are the main features of combined hyperlipoproteinemia?

<p>Increased VLDL and LDL (A)</p> Signup and view all the answers

What side effect is commonly associated with the new treatment being studied in clinical trials?

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

Which of the following is a first-generation fibrate?

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

Which of the following combinations increases the risk of myopathy when statin doses exceed 25% of the maximum?

<p>Nicotinic acid and statins (C)</p> Signup and view all the answers

What is the current status of the new lipid-modifying treatment mentioned?

<p>Undergoing Phase 3 clinical trials (B)</p> Signup and view all the answers

In dysbetalipoproteinemia, what lipoprotein is primarily elevated?

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

Which medication is classified as a bile acid binding resin?

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

Which combination is noted for being particularly effective for familial combined hyperlipoproteinemia?

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

What effect does Ezetimibe have on plasma Total Cholesterol (TC)?

<p>It decreases plasma TC. (C)</p> Signup and view all the answers

Which of the following represents a side effect of Ezetimibe?

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

In patients with which condition should Ezetimibe be used with caution?

<p>Active liver disease (C)</p> Signup and view all the answers

How does Ezetimibe primarily lower plasma LDL levels?

<p>By selectively inhibiting intestinal absorption of cholesterol (D)</p> Signup and view all the answers

Which group of patients would most commonly be prescribed Ezetimibe?

<p>Patients with hypercholesterolemia (B)</p> Signup and view all the answers

What is a noted effect of Ezetimibe on plasma HDL levels?

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

Why might Ezetimibe be contraindicated in pregnant or breastfeeding women?

<p>It crosses the placenta and poses risks to the fetus. (A)</p> Signup and view all the answers

Which effect is not associated with the use of Ezetimibe?

<p>Enhanced reabsorption of dietary cholesterol (B)</p> Signup and view all the answers

What additional treatment is Ezetimibe commonly combined with?

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

In which age group is Ezetimibe indicated for use in children?

<p>Children above 6 years (B)</p> Signup and view all the answers

What is the primary effect of fibrates on warfarin?

<p>They displace warfarin from albumin, increasing its effect. (C)</p> Signup and view all the answers

Which side effect is specifically associated with probucol?

<p>Prolongation of the QT interval (D)</p> Signup and view all the answers

What is the mechanism of action of probucol related to cholesterol?

<p>It reduces the oxidation of cholesterol and promotes its uptake by macrophages. (C)</p> Signup and view all the answers

What is a notable contraindication for the use of probucol?

<p>Individuals having abnormal long QT intervals (D)</p> Signup and view all the answers

In which condition is probucol primarily indicated?

<p>Hypercholesterolemia, particularly type IIA (D)</p> Signup and view all the answers

Which of the following does NOT describe an effect of probucol on plasma lipids?

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

Ezetimibe is classified primarily as which type of drug?

<p>Intestinal sterol absorption inhibitor (B)</p> Signup and view all the answers

What effect do fibrates have on antithrombotic properties?

<p>They inhibit coagulation. (D)</p> Signup and view all the answers

How long before attempting pregnancy should probucol be discontinued due to its half-life?

<p>At least 6 months (A)</p> Signup and view all the answers

What effect does probucol have on HDL as per the provided information?

<p>It decreases HDL levels. (A)</p> Signup and view all the answers

Flashcards

Familial hyperchylomicronemia

A condition characterized by very high levels of chylomicrons, triglycerides (TG), and cholesterol in the blood.

Familial hypercholesterolemia

A genetic disorder that results in elevated levels of Low-Density Lipoprotein (LDL) cholesterol in the blood.

Combined hyperlipoproteinemia

A condition involving increased levels of both VLDL and LDL lipoproteins in the blood.

HMG-CoA reductase inhibitors

A class of drugs also known as statins, used to lower cholesterol levels by inhibiting cholesterol production in the liver.

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Fibrates

Medications primarily used to lower triglyceride levels and increase HDL cholesterol levels.

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Nicotinic acid (niacin)

A form of vitamin B3 used to treat dyslipidemia by lowering LDL and triglycerides and raising HDL cholesterol.

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Dysbetalipoproteinemia

A condition where there are elevated levels of VLDL and IDL, leading to increased cholesterol levels.

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Ezetimibe

An intestinal sterol absorption inhibitor that reduces cholesterol absorption.

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Bile Acid Binding Resins

Drugs that bind bile acids in the intestine, preventing reabsorption and lowering cholesterol.

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Common Bile Acid Resins

Cholestyramine, Cholestipol, Colesevelam are examples of bile acid resins.

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Mechanism of Action of Resins

Resins bind bile acids, preventing enterohepatic circulation, leading to decreased cholesterol levels.

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Effects on Plasma Lipids

Resins lower plasma LDL by ~20% but increase VLDL-TG by 15-20%.

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Side Effects of Resins

Includes abdominal bloating, nausea, constipation, and malabsorption of vitamins.

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Clinical Indications for Resins

Used for hypercholesterolemia and pruritis in cholestatic patients.

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Contraindications of Resins

Not recommended for patients with severe hypertriglyceridemia.

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Hygroscopic Nature of Resins

Bile acid resins are hygroscopic powders and can absorb water.

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Plasma LDL

Low-Density Lipoprotein; a type of cholesterol that can build up in arteries.

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Plasma HDL

High-Density Lipoprotein; known as 'good cholesterol' that helps remove LDL from arteries.

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Atherosclerotic cardiovascular disease (ASCVD)

A disease caused by the buildup of plaque in arteries, leading to heart problems.

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Combination therapy

Using multiple medications together for a synergistic effect on lipid levels.

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Side effects of lipid-lowering therapy

Common mild effects include nausea or abdominal discomfort from treatment.

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Mechanism of action

Selectively inhibits intestinal absorption of dietary cholesterol and phytosterols.

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Effect on plasma TC

Lowers total cholesterol (TC) levels in plasma.

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Effect on plasma LDL

Decreases LDL cholesterol levels by approximately 19%.

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Effect on plasma HDL

Causes a minimal increase in HDL cholesterol.

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Side effect: hepatic function

Low incidence of impaired liver function, higher with statins.

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Side effect: muscle weakness

Muscle weakness reported as a side effect.

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Contraindication: pregnancy

Use cautiously in pregnancy and breastfeeding; risks vs. benefits must be evaluated.

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Contraindication: liver disease

Not recommended for patients with active liver disease or abnormal liver tests.

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Clinical indication: Hypercholesterolemia

Used to treat individuals with high cholesterol levels.

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Clinical indication: phytosterolemia

Used to treat phytosterolemia, a condition of elevated plant sterols.

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Warfarin

An oral anticoagulant that is displaced by fibrates, increasing its effectiveness.

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Antiatherothrombotic effects

Effects that inhibit coagulation and increase fibrinolysis, reducing the risk of thrombosis.

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Probucol

A drug that lowers cholesterol by inhibiting cholesterol oxidation and ingestion by macrophages.

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Prolonged QT interval

An abnormality that can lead to cardiac arrhythmias; a side effect of probucol.

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Hypercholesterolemia

Condition of having high cholesterol, particularly type IIA treated by probucol.

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Adipose tissue accumulation

The storage of drugs like probucol in fat tissue, which can affect drug action.

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QT interval caution

A caution for drugs that prolong the QT interval; important when combining medications.

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Cholesterol oxidation

A process inhibited by probucol, preventing the ingestion of oxidized LDL by macrophages.

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Study Notes

Antihyperlipidaemia

  • Antihyperlipidaemic drugs are used to treat high cholesterol and related conditions.
  • Different types of drugs target different aspects of lipid metabolism.

Hyperlipoproteinemia Classifications

  • Different forms of hyperlipoproteinemia exist; each is characterized by specific lipid elevations.
  • Familial hyperchylomicronemia shows elevated chylomicrons, while familial hypercholesterolemia shows high LDL.
  • Other classifications feature elevated IDL, VLDL, and HDL levels.

Classification of Antihyperlipidemic Drugs

  • Bile acid binding resins: These resins bind bile acids in the intestine, preventing their reabsorption. This leads to higher cholesterol production.
  • HMG-CoA reductase inhibitors (statins): These drugs reduce cholesterol production by inhibiting the enzyme HMG-CoA reductase.
  • Nicotinic acid (niacin): This reduces VLDL and LDL production, while increasing HDL.
  • Fibrates: These drugs mainly affect VLDL and TG (Triglyceride) levels. They increase lipoprotein lipase activity and thus hydrolysis of triglycerides.
  • Intestinal sterol absorption inhibitors: These drugs block cholesterol absorption in the intestines. Ezetimibe is an example.
  • Probucol: This drug's exact mechanism in cholesterol reduction isn't fully understood, but it may reduce cholesterol oxidation.
  • PCSK9 Inhibitors: These drugs prevent LDL receptors from being removed by the liver.

Bile Acid Binding Resins (BA BRs)

  • Mechanism of action: BA BRs are cationic resins that bind bile acids in the intestine, preventing their reabsorption and forcing the liver to produce more bile acids from cholesterol.
  • Effects on plasma lipids: Decrease LDL, with a possible increase in VLDL and triglycerides.

HMG-CoA Reductase Inhibitors (Statins)

  • Mechanism: Inhibit HMG-CoA reductase, the enzyme key to cholesterol synthesis.
  • Effect on plasma lipids: Significantly reduce LDL, possible increase in HDL.
  • Side effects: Myopathy or rhabdomyolysis (muscle damage) in some cases, liver damage.

Nicotinic acid (niacin)

  • Mechanism: Inhibits lipolysis in peripheral tissues, reducing VLDL secretion and increasing HDL.
  • Side Effects: Cutaneous flush (redness), pruritus (itching), and possibly liver damage.

Fibrates

  • Mechanism: Activate PPAR-alpha receptors affecting lipoprotein lipase and VLDL production.
  • Side effects: Gastrointestinal issues, rashes, or myopathy.

Intestinal Sterol Absorption Inhibitors (e.g., Ezetimibe)

  • Mechanism: Blocks cholesterol absorption in the intestines.
  • Effects on plasma lipids: Reduce LDL.

Probucol

  • Mechanism: Reduces cholesterol oxidation, possibly by reducing the ingestion of oxidized LDL by macrophages.

PCSK9 Inhibitors

  • Mechanism: Inhibiting PCSK9 reduces the removal of LDL receptors from the cell surface, resulting in more LDL removed from the blood.
  • Effects on Lipids: Significantly reduce LDL, moderate increase in HDL.

ATP-Citrate Lyase Inhibitors (e.g., Bempedoic acid).

  • Mechanism: Inhibit ATP-citrate lyase, a key enzyme in cholesterol synthesis, leading to a reduction in LDL.
  • Side effects: Some muscle complaints.

Cholesteryl Ester Transfer Protein (CETP) Inhibitors

  • Mechanism: Inhibit CETP, which transfers lipids between lipoproteins, increasing HDL levels and reducing LDL levels.
  • Effects on Lipids: Decrease LDL, increase HDL.

Combination Therapy

  • Combining different types of antihyperlipidaemic drugs can provide more extensive effects on plasma lipids.
  • Synergistic effects can be achieved by optimizing the combination strategies for more effective lipid profile modification and achieving better cardiovascular results.

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Description

This quiz covers the essential aspects of antihyperlipidaemic drugs and their classifications. It details various types of hyperlipoproteinemia and their characteristics, along with the specific mechanisms of different drug classes like statins and fibrates. Test your knowledge on how these medications target lipid metabolism and cholesterol levels.

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