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Questions and Answers
How does the reduction of bile acid concentration affect hepatic cholesterol levels?
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?
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?
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?
A patient taking cholestyramine complains of indigestion and abdominal discomfort. Which of the following side effects is MOST likely responsible for these symptoms?
What compensatory mechanism is triggered by the action of bile acid sequestrants?
What compensatory mechanism is triggered by the action of bile acid sequestrants?
Which of the following is a clinical application of bile acid sequestrants unrelated to hypercholesterolemia?
Which of the following is a clinical application of bile acid sequestrants unrelated to hypercholesterolemia?
Why should other orally administered drugs be taken either one hour before or four hours after taking bile acid resins?
Why should other orally administered drugs be taken either one hour before or four hours after taking bile acid resins?
Which of the following is a potential effect of bile acid sequestrants on plasma lipids?
Which of the following is a potential effect of bile acid sequestrants on plasma lipids?
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?
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?
Which classification of hyperlipoproteinemia is characterized by elevated levels of chylomicrons, triglycerides, and cholesterol?
Which classification of hyperlipoproteinemia is characterized by elevated levels of chylomicrons, triglycerides, and cholesterol?
What is the primary action of HMG-CoA reductase inhibitors in managing hyperlipidemia?
What is the primary action of HMG-CoA reductase inhibitors in managing hyperlipidemia?
Which drug class includes medications that are effective in increasing HDL levels?
Which drug class includes medications that are effective in increasing HDL levels?
What is a common outcome when statins are combined with resins?
What is a common outcome when statins are combined with resins?
What are the main features of combined hyperlipoproteinemia?
What are the main features of combined hyperlipoproteinemia?
What side effect is commonly associated with the new treatment being studied in clinical trials?
What side effect is commonly associated with the new treatment being studied in clinical trials?
Which of the following is a first-generation fibrate?
Which of the following is a first-generation fibrate?
Which of the following combinations increases the risk of myopathy when statin doses exceed 25% of the maximum?
Which of the following combinations increases the risk of myopathy when statin doses exceed 25% of the maximum?
What is the current status of the new lipid-modifying treatment mentioned?
What is the current status of the new lipid-modifying treatment mentioned?
In dysbetalipoproteinemia, what lipoprotein is primarily elevated?
In dysbetalipoproteinemia, what lipoprotein is primarily elevated?
Which medication is classified as a bile acid binding resin?
Which medication is classified as a bile acid binding resin?
Which combination is noted for being particularly effective for familial combined hyperlipoproteinemia?
Which combination is noted for being particularly effective for familial combined hyperlipoproteinemia?
What effect does Ezetimibe have on plasma Total Cholesterol (TC)?
What effect does Ezetimibe have on plasma Total Cholesterol (TC)?
Which of the following represents a side effect of Ezetimibe?
Which of the following represents a side effect of Ezetimibe?
In patients with which condition should Ezetimibe be used with caution?
In patients with which condition should Ezetimibe be used with caution?
How does Ezetimibe primarily lower plasma LDL levels?
How does Ezetimibe primarily lower plasma LDL levels?
Which group of patients would most commonly be prescribed Ezetimibe?
Which group of patients would most commonly be prescribed Ezetimibe?
What is a noted effect of Ezetimibe on plasma HDL levels?
What is a noted effect of Ezetimibe on plasma HDL levels?
Why might Ezetimibe be contraindicated in pregnant or breastfeeding women?
Why might Ezetimibe be contraindicated in pregnant or breastfeeding women?
Which effect is not associated with the use of Ezetimibe?
Which effect is not associated with the use of Ezetimibe?
What additional treatment is Ezetimibe commonly combined with?
What additional treatment is Ezetimibe commonly combined with?
In which age group is Ezetimibe indicated for use in children?
In which age group is Ezetimibe indicated for use in children?
What is the primary effect of fibrates on warfarin?
What is the primary effect of fibrates on warfarin?
Which side effect is specifically associated with probucol?
Which side effect is specifically associated with probucol?
What is the mechanism of action of probucol related to cholesterol?
What is the mechanism of action of probucol related to cholesterol?
What is a notable contraindication for the use of probucol?
What is a notable contraindication for the use of probucol?
In which condition is probucol primarily indicated?
In which condition is probucol primarily indicated?
Which of the following does NOT describe an effect of probucol on plasma lipids?
Which of the following does NOT describe an effect of probucol on plasma lipids?
Ezetimibe is classified primarily as which type of drug?
Ezetimibe is classified primarily as which type of drug?
What effect do fibrates have on antithrombotic properties?
What effect do fibrates have on antithrombotic properties?
How long before attempting pregnancy should probucol be discontinued due to its half-life?
How long before attempting pregnancy should probucol be discontinued due to its half-life?
What effect does probucol have on HDL as per the provided information?
What effect does probucol have on HDL as per the provided information?
Flashcards
Familial hyperchylomicronemia
Familial hyperchylomicronemia
A condition characterized by very high levels of chylomicrons, triglycerides (TG), and cholesterol in the blood.
Familial hypercholesterolemia
Familial hypercholesterolemia
A genetic disorder that results in elevated levels of Low-Density Lipoprotein (LDL) cholesterol in the blood.
Combined hyperlipoproteinemia
Combined hyperlipoproteinemia
A condition involving increased levels of both VLDL and LDL lipoproteins in the blood.
HMG-CoA reductase inhibitors
HMG-CoA reductase inhibitors
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Fibrates
Fibrates
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Nicotinic acid (niacin)
Nicotinic acid (niacin)
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Dysbetalipoproteinemia
Dysbetalipoproteinemia
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Ezetimibe
Ezetimibe
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Bile Acid Binding Resins
Bile Acid Binding Resins
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Common Bile Acid Resins
Common Bile Acid Resins
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Mechanism of Action of Resins
Mechanism of Action of Resins
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Effects on Plasma Lipids
Effects on Plasma Lipids
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Side Effects of Resins
Side Effects of Resins
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Clinical Indications for Resins
Clinical Indications for Resins
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Contraindications of Resins
Contraindications of Resins
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Hygroscopic Nature of Resins
Hygroscopic Nature of Resins
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Plasma LDL
Plasma LDL
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Plasma HDL
Plasma HDL
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Atherosclerotic cardiovascular disease (ASCVD)
Atherosclerotic cardiovascular disease (ASCVD)
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Combination therapy
Combination therapy
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Side effects of lipid-lowering therapy
Side effects of lipid-lowering therapy
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Mechanism of action
Mechanism of action
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Effect on plasma TC
Effect on plasma TC
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Effect on plasma LDL
Effect on plasma LDL
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Effect on plasma HDL
Effect on plasma HDL
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Side effect: hepatic function
Side effect: hepatic function
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Side effect: muscle weakness
Side effect: muscle weakness
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Contraindication: pregnancy
Contraindication: pregnancy
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Contraindication: liver disease
Contraindication: liver disease
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Clinical indication: Hypercholesterolemia
Clinical indication: Hypercholesterolemia
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Clinical indication: phytosterolemia
Clinical indication: phytosterolemia
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Warfarin
Warfarin
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Antiatherothrombotic effects
Antiatherothrombotic effects
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Probucol
Probucol
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Prolonged QT interval
Prolonged QT interval
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Hypercholesterolemia
Hypercholesterolemia
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Adipose tissue accumulation
Adipose tissue accumulation
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QT interval caution
QT interval caution
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Cholesterol oxidation
Cholesterol oxidation
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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.