37 Questions
What is the mechanism of action of ezetimibe?
Inhibits the selective-cholesterol transporter NPC1L1
Which drug is used as monotherapy in mild cases of hypercholesterolemia?
Ezetimibe
What is the main effect of fibrates on HDL-C levels?
Increase HDL-C
In what type of patients are statins never given?
Pregnant patients
Which drug is used cautiously in patients under 18 years of age?
Ezetimibe
What is the net effect of fibrates on triglycerides and VLDL?
Decrease triglycerides and VLDL
Which drug is mainly given as an adjuvant to statins in resistant cases of hypercholesterolemia?
Ezetimibe
'PPAR-α Agonists' like fibrates modulate gene expression of all the following EXCEPT:
Adhesion molecules
What is the main classification method for statins based on lipid solubility?
Into hydrophilic, lipophilic, or mixed
Which type of statins has a higher tendency to induce myopathy?
Lipophilic statins
How do statins mainly modulate the lipid profile?
By decreasing total cholesterol and LDL-C
Which of the following is a major concern when taking lipophilic statins?
Hepatic enzyme elevation
What is the primary method of diagnosis for myopathy induced by statins?
Serum creatine kinase (CK) level measurement
How are hydrophilic statins eliminated from the body?
By filtration through the kidneys
What is the primary impact of statins on total cholesterol and LDL-C levels?
Decrease in total cholesterol and LDL-C levels
Which aspect of lipid profile is mainly increased by statins?
HDL-C levels
Which of the following is true about Omega-3 Fatty Acids?
They inhibit platelet aggregation.
What is the mechanism of action of Niacin (Nicotinic Acid) in adipose tissue?
Decreases availability of free fatty acids for triglyceride synthesis.
What is a characteristic of Adjuvant therapy in Hypertriglyceridemia?
It can inhibit platelet aggregation.
Which statement about Cholestyramine is correct?
It decreases HDL levels.
Why should Fibrates be used cautiously in renal impairment?
They can suppress serum uric acid if elevated.
What effect does Omega-3 Fatty Acids have on the cell membrane?
Protects against oxidative stress.
What are the common side effects of Niacin?
Pruritus and flushing
How can the side effects of Niacin, such as pruritus and flushing, be avoided?
By taking a low dose of aspirin an hour before its intake
In what condition is Niacin better avoided?
Diabetes
How does Cholestyramine help in lowering hypertriglyceridemia and hypercholesterolemia?
By adsorbing bile acids and eliminating them in stools
What is a major drawback in using Cholestyramine for treatment?
It adsorbs to fat-soluble vitamins and steroids
Which lipid parameter does Cholestyramine primarily target for reduction?
LDL cholesterol
What can be a potential solution to the issue of Cholestyramine adsorbing to fat-soluble vitamins?
Taking fat-soluble vitamin supplements separately from Cholestyramine
What is a common side effect that Niacin can induce when combined with statins or fibrates?
Myalgia
Which of the following is NOT classified as an anti-hypercholesterolemic agent according to the text?
Fibrates
What is the mechanism of action of statins according to the text?
Inhibition of liver cholesterol synthesis
Which drug is classified as a mixed anti-dyslipidemic agent?
Niacin
How do statins reduce blood cholesterol levels according to the text?
Upregulating LDL-Receptors
Which agent exerts its action by inhibiting PPAR- according to the text?
Omega-3 fatty acids
When considering adjuvant therapy in hypertriglyceridemia, what drug class can be used with statins according to the text?
Statins + Fibrates
Which agent aims to elevate HDL levels based on the text?
Niacin
Study Notes
Anti-Dyslipidemic Agents
- Classified into three groups: anti-hypercholesterolemic agents, anti-hypertriglyceridemic agents, and mixed anti-dyslipidemic agents
Statins
- Inhibit cholesterol synthesis in the liver by reversible competitive inhibition of the rate-limiting step of its formation
- Upregulate LDL-Receptors, reducing circulating cholesterol levels
- Classified according to lipid solubility into hydrophilic, lipophilic, or mixed
- Hydrophilic agents are eliminated by the kidney and have minimal drug interactions
- Lipophilic agents are metabolized by the liver and have many drug interactions
- Can cause dose-dependent elevation in hepatic enzymes and induce myopathy
- Used to treat dyslipidemia, especially hypercholesterolemia
- Can improve glucose tolerance and suppress serum uric acid
Ezetimibe
- Selective cholesterol absorption inhibitor
- Inhibits exogenous cholesterol intake, stimulating the liver to upregulate LDL-R
- Given as monotherapy in mild cases of hypercholesterolemia or as an adjuvant to statins in resistant cases
- Has a safe profile
Fibrates
- PPAR-α agonists
- Modulate gene expression, decreasing triglycerides and VLDL, and increasing HDL-C
- Involved in inflammatory reactions, especially those linked to cholesterol accumulation
- Classified according to lipid solubility and duration of action
- Can be used in combination with statins, but caution is needed to avoid myopathy
- Fibrates are never given during pregnancy and are used cautiously in renal and hepatic impairment
Omega-3 Fatty Acids
- Polyunsaturated fatty acids derived from fatty fish oil
- Possess a weak PPAR-α agonistic effect
- Inhibit platelet aggregation and are cardio-protective
- Used as adjuvant therapy in hypertriglyceridemia
Niacin
- Vitamin B3 that acts on a specific receptor in adipose tissue to inhibit hormone-sensitive lipase
- Decreases lipolysis and availability of FFA for TG synthesis in the liver
- Activates lipoprotein lipase to increase VLDL circulatory clearance
- Increases HDL-C by decreasing clearance of Apo A from plasma
- Used as mono therapy or in combination with other anti-dyslipidemic agents
- Can cause pruritus, sensation of warmth, and flushing, which can be avoided by using aspirin or slow-release formulations
Cholestyramine
- Bile acid sequestrant that adsorbs bile acids and eliminates them in stools
- Enhances uptake of circulating LDL to eliminate endogenous cholesterol
- Used to lower hypertriglyceridemia, hypercholesterolemia, or in mixed dyslipidemia
- Can be given as monotherapy or in combination with other anti-dyslipidemic agents
- Has a drawback of adsorbing steroids and fat-soluble vitamins, which must be replaced as supplements
Test your knowledge on pharmacological agents used to lower lipid levels in patients with hypertriglyceridemia and atherosclerosis. This quiz covers the mechanism of action and considerations when prescribing statins and ezetimibe.
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