Antihyperlipidaemia Quiz

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Questions and Answers

Which of the following is the primary characteristic of familial hypercholesterolemia?

  • Elevated levels of VLDL
  • Elevated levels of LDL (correct)
  • Elevated levels of chylomicrons
  • Elevated levels of HDL

Which class of antihyperlipidemic drugs directly inhibits cholesterol synthesis?

  • Nicotinic acid
  • Bile acid binding resins
  • Fibrates
  • HMG-CoA reductase inhibitors (correct)

Which of the following lipid profiles is characteristic of familial hypertriglyceridemia?

  • Increased chylomicrons, increased triglycerides, normal HDL
  • Increased LDL, increased cholesterol, decreased triglycerides
  • Increased HDL, decreased VLDL, normal triglycerides
  • Increased VLDL, increased triglycerides, decreased HDL (correct)

Which drug is classified as a bile acid binding resin?

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

Which of the following is a second-generation fibrate?

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

Which of the following is a potential side effect associated with the drug mentioned?

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

What is the clinical indication for prescribing the drug?

<p>Atherosclerotic cardiovascular disease (ASCVD) (A)</p> Signup and view all the answers

What is the status of the drug mentioned in the content?

<p>Currently not in the market, still in Phase 3 clinical trials (A)</p> Signup and view all the answers

What combined therapy is considered most efficacious and practical for familial combined hyperlipoproteinemia?

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

When statins are combined with nicotinic acid, what precaution should be taken?

<p>Maintain the statin dose to less than 25% of the maximal dose. (D)</p> Signup and view all the answers

What is a potential risk associated with combining statins and fibrates?

<p>Increased risk of rhabdomyolysis (myopathy) (B)</p> Signup and view all the answers

What is a potential risk associated with combining fibrates and resins?

<p>Increased risk of cholelithiasis (A)</p> Signup and view all the answers

What synergistic effect can be achieved by combining statins and resins?

<p>Reduced VLDL induced by resins (A)</p> Signup and view all the answers

Which of the following is a significant contraindication for using Niacin?

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

What is the primary mechanism of action of Niacin in lipid management?

<p>Inhibiting lipolysis in peripheral tissues (A)</p> Signup and view all the answers

Which of the following statins should be administered in the evening?

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

Which side effect is most commonly associated with Niacin use?

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

What is the likely effect on LDL levels after treatment with Niacin?

<p>Decrease by 10-15% (B)</p> Signup and view all the answers

Which of the following statins are considered inactive prodrugs?

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

What interaction poses an increased risk of myopathy when combining certain medications?

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

Which lipid parameter is expected to increase with Niacin therapy?

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

What effect do fibrates have on warfarin levels?

<p>Increase the warfarin effect by displacing it from albumin. (D)</p> Signup and view all the answers

Which of the following side effects is associated with probucol?

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

What is the primary mechanism of action for probucol in lowering plasma cholesterol levels?

<p>Inhibition of cholesterol oxidation. (C)</p> Signup and view all the answers

Which lipid level is NOT affected by probucol treatment?

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

In which condition is probucol indicated for use?

<p>Type II hypercholesterolemia. (D)</p> Signup and view all the answers

What should be considered when administering probucol along with other medications?

<p>Possibility of QT interval prolongation. (A)</p> Signup and view all the answers

What is the recommended action regarding probucol prior to attempting pregnancy?

<p>Discontinue at least 6 months before pregnancy. (B)</p> Signup and view all the answers

How does ezetimibe work as a lipid-lowering agent?

<p>Decreases intestinal absorption of cholesterol. (B)</p> Signup and view all the answers

Which drug is most commonly associated with flushing and itchiness, relieved by aspirin?

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

Which drug combination is effective at significantly lowering LDL levels?

<p>PCSK9i + Statins (C)</p> Signup and view all the answers

What adverse effect might a patient experience when taking a bile acid sequestrant?

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

In which patient scenario would a doctor likely prescribe bempedoic acid?

<p>For a patient with muscle pain from statins (C)</p> Signup and view all the answers

Which drug is known to increase HDL levels while reducing LDL and triglycerides?

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

What is the mechanism of action for PCSK9 inhibitors?

<p>Increase hepatic clearance of LDL (B)</p> Signup and view all the answers

Which of the following drugs specifically targets lipoprotein lipase activity?

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

Which statement is true regarding the effectiveness of using statins in combination with other drugs?

<p>Effective doses may be lower than using each drug alone (A)</p> Signup and view all the answers

What is the primary mechanism of action of bile acid binding resins?

<p>They bind to and excrete bile acids in the feces. (C)</p> Signup and view all the answers

Which of the following is a side effect associated with the use of bile acid binding resins?

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

What is the effect of bile acid binding resins on plasma LDL levels?

<p>Decreases by 20% (B)</p> Signup and view all the answers

In which condition are bile acid binding resins contraindicated?

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

What compensatory mechanism occurs due to the use of bile acid binding resins?

<p>Upregulation of HMG-CoA reductase activity (D)</p> Signup and view all the answers

Which drug is considered a bile acid binding resin?

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

What primarily causes increased plasma VLDL-TG when using bile acid binding resins?

<p>Increased hepatic triglyceride synthesis (B)</p> Signup and view all the answers

How should other orally administered drugs be taken when using bile acid binding resins?

<p>One hour before or four hours after the resins (D)</p> Signup and view all the answers

Which of the following conditions can be treated with bile acid binding resins?

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

What characterizes bile acid binding resins as a physical form?

<p>Hygroscopic powders and hydrophilic gels (A)</p> Signup and view all the answers

Flashcards

Familial hyperchylomicronemia

Condition with elevated chylomicrons, triglycerides, and cholesterol.

HMG-CoA reductase inhibitors

A class of drugs known as statins that lower LDL cholesterol.

Mixed hypertriglyceridemia

Elevated levels of chylomicrons and VLDL in the blood.

Bile acid binding resins

Drugs that bind bile acids to help reduce cholesterol levels.

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Dysbetalipoproteinemia

Condition marked by elevated VLDL and IDL cholesterol levels.

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Effects on Plasma Lipid

↓ Plasma LDL and ↑ Plasma HDL levels.

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Mild Gastrointestinal Symptoms

Common side effects include nausea and abdominal discomfort.

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Atherosclerotic Cardiovascular Disease (ASCVD)

A condition involving narrowed arteries due to plaque buildup, increasing heart disease risk.

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Dyslipidemia

Abnormal levels of lipids in blood, often involving high LDL or low HDL.

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Combination with Statins

Statins are commonly prescribed with other lipid-lowering therapies for synergistic effects.

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Nicotinic Acid Interaction

Nicotinic acid enhances statin effects but increases myopathy risk at higher doses.

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Statins and Ezetimibe

Combination has a synergistic effect, significantly reducing LDL levels in patients.

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Fibrates and Resins

Useful in patients with familial hyperlipidemia intolerant to niacin, but may increase gallstone risk.

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Fibrates

A class of drugs that can displace warfarin from albumin, increasing its effect.

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Warfarin interaction

Fibrates can increase the anticoagulant effect of warfarin.

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Probecol

A drug that reduces LDL and cholesterol through unclear mechanisms.

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QT interval prolongation

Probecol can cause cardiac arrhythmias by prolonging the QT interval.

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Contraindications for probecol

Patients with abnormal QT intervals should not use probecol.

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Ezetimibe

An intestinal sterol absorption inhibitor that lowers cholesterol.

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Adverse effects of probecol

Common side effects include gastrointestinal disturbances and prolonged QT interval.

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Antioxidant properties

Probecol may help block atherosclerosis via antioxidant effects.

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HMG-CoA Reductase

An enzyme vital for cholesterol biosynthesis, important in fetal development.

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Statins

Medications that lower cholesterol by inhibiting HMG-CoA reductase.

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Evening Administration of Statins

Statins should be taken in the evening due to night-time cholesterol biosynthesis.

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Inactive Prodrugs

Drugs like lovastatin and simvastatin that require activation inside the body.

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Niacin (Vitamin B3)

A drug that inhibits lipolysis and reduces LDL while increasing HDL.

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Niacin Side Effects

Common side effects include flushing, hyperglycemia, and hepatotoxicity.

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Contraindication in Pregnancy

Niacin is contraindicated in pregnancy due to potential birth defects.

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Clinical Indications for Niacin

Used for treating hypercholesterolemia and hyperlipidemia.

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Bile Acid Sequestrants

Drugs that bind bile acids in the intestine, preventing their reabsorption.

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Cholestyramine

A bile acid-binding resin used to lower LDL cholesterol levels.

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Mechanism of Action

Bile acid resins bind negatively charged bile acids, reducing cholesterol liver recirculation.

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Plasma LDL Reduction

Bile acid sequestrants can decrease plasma LDL levels by 20%.

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Uptake of LDL

Increased uptake of LDL and IDL from plasma due to enhanced LDL receptors.

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Side Effects

Common side effects include abdominal bloating, constipation, and nausea.

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Malabsorption Risks

Possible malabsorption of vitamins K and folate, affecting blood clotting.

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Clinical Indications

Used for hypercholesterolemia, pruritis, and digitalis toxicity.

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Contraindications

Severe hypertriglyceridemia is a contraindication for using bile acid resins.

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LDL Reduction Strategies

Combination therapies such as PCSK9i with statins reduce LDL cholesterol.

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PCSK9i Function

PCSK9 inhibitors increase hepatic clearance of LDL cholesterol.

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Statin Mechanism

Statins decrease cholesterol production in the liver.

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Ezetimibe Role

Ezetimibe works by reducing intestinal absorption of cholesterol.

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Niacin Effects

Niacin can cause flushing and itching, relieved by aspirin.

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Bempedoic Acid

Bempedoic acid is used when statins alone are insufficient for lowering LDL.

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Cholestyramine Symptoms

Cholestyramine can lead to constipation and bloating.

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Gemfibrozil Action

Gemfibrozil increases lipoprotein lipase activity, decreasing triglycerides.

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Study Notes

Antihyperlipidaemia

  • Antihyperlipidaemic drugs are used to treat high cholesterol and other lipid disorders.

Hyperlipoproteinemia Classifications

  • Familial hyperchylomicronemia: characterized by increased chylomicrons, leading to elevated triglycerides and cholesterol.
  • Familial hypercholesterolemia: characterized by elevated LDL cholesterol and reduced LDL receptor activity.
  • Combined hyperlipoproteinemia/hyperlipidemia: characterized by elevated triglycerides and LDL cholesterol.
  • Familial hyperlipidemia: encompasses various disorders with elevated lipid levels.
  • Familial hypertriglyceridemia: characterized by elevated triglycerides.
  • Mixed hypertriglyceridemia: characterized by elevated triglycerides and VLDL.
  • Familial hyperalphalipoproteinemia: characterized by elevated HDL cholesterol.
  • Dysbetalipoproteinemia: characterized by elevated IDL cholesterol.

Classification of Antihyperlipidemic Drugs

  • Bile acid binding resins: (e.g., cholestyramine, cholestipol, colesevelam) bind bile acids in the intestine, preventing their reabsorption, increasing bile acid synthesis from cholesterol, and lowering LDL cholesterol.
  • HMG-CoA reductase inhibitors (statins): (e.g., lovastatin, simvastatin, atorvastatin) inhibit cholesterol synthesis in the liver, lowering LDL cholesterol and potentially increasing HDL cholesterol.
  • Nicotinic acid (niacin): reduces VLDL production, lowers triglycerides, and raises HDL cholesterol.
  • Fibrates: (e.g., clofibrate, gemfibrozil, fenofibrate) increase lipoprotein lipase activity, lowering triglycerides and potentially raising HDL cholesterol.
  • Intestinal sterol absorption inhibitors (e.g., ezetimibe): inhibit intestinal cholesterol absorption, lowering LDL cholesterol.
  • Protein convertase subtilisin/kexin type 9 (PCSK9) inhibitors: (e.g., evolocumab, alirocumab) block the PCSK9 protein and increasing LDL receptors in the liver, leading to decreased LDL cholesterol.
  • ATP-citrate lyase inhibitors (e.g., bempedoic acid): reduce cholesterol synthesis and therefore lower LDL cholesterol.
  • Cholesteryl ester transfer protein (CETP) inhibitors (e.g., torcetrapib, anacetrapib, dalcetrapib): inhibit transfer of cholesteryl esters from HDL to LDL particles, potentially raising HDL and lowering LDL.

Bile Acid Binding Resins (Example)

  • Route of administration: Oral
  • Mechanism of action: Bind bile acids in the intestine preventing their reabsorption, increasing bile acid synthesis from cholesterol, and lowering LDL cholesterol.
  • Effects on plasma lipids: Lower LDL, may increase VLDL and possibly TG, no consistent effect on HDL.
  • Side effects: Constipation, nausea, abdominal bloating, dyspepsia, malabsorption of fat soluble vitamins (rare), decreased absorption of other drugs.
  • Clinical indications: Hypercholesterolemia.
  • Contraindications: Severe liver impairment.
  • Other: Insoluble in water.

Combination Therapy

  • Statins and resins: Synergistic effect on LDL lowering, but nicotinic acid may increase risk of myopathy with higher doses of statins
  • Statins and fibrates: Useful for patients with familial hyperlipidemia. Potential increased risk of myopathy, especially in combination with gemfibrozil/clofibrate.
  • Other combinations: Various combinations may be used depending on the patient's specific lipid profile and clinical needs.

Drugs Under Development

  • Many other drugs are being studied for the treatment of hyperlipidemia.

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