Cardiovascular Disease Prevention with Lipid Drugs

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Questions and Answers

What is the recommended dose of atorvastatin for primary prevention of cardiovascular disease in individuals with a 10% or greater 10-year risk of developing cardiovascular disease?

20 mg (correct)

10 mg

80 mg

40 mg

Statins are not recommended for individuals over 85 years old.

False (B)

What are the two primary categories of dyslipidemia?

Primary dyslipidemia and secondary dyslipidemia.

______ is a common non-pharmacological approach to manage dyslipidemia.

Cardioprotective diet Signup and view all the answers

Which of the following is NOT a type of lipid-lowering drug?

Antibiotics (B) Signup and view all the answers

Match the lipid-lowering drug with its corresponding mechanism of action:

Simvastatin = Blocks HMG-CoA reductase, a rate-limiting enzyme in cholesterol synthesis Ezetimibe = Inhibits cholesterol absorption in the small intestine Nicotinic acid = Reduces VLDL production, raises HDL levels Fibrates = Activates PPARα, decreasing triglyceride levels and increasing HDL levels Signup and view all the answers

What is the primary mechanism of action for HMG-CoA reductase inhibitors?

They block HMG-CoA reductase, a key enzyme in cholesterol synthesis. Signup and view all the answers

Atorvastatin is a short-acting HMG-CoA reductase inhibitor.

False (B) Signup and view all the answers

What is a significant clinical effect of HMG CoA reductase inhibitors?

Lowering LDL by 30% (B) Signup and view all the answers

Fibrates primarily reduce triglyceride levels by 20-30%.

True (A) Signup and view all the answers

What is the mechanism of action of fibrates?

Agonist at the peroxisome-activated receptor (PPAR-a) Signup and view all the answers

HMG CoA reductase inhibitors improve ____________ function.

endothelial Signup and view all the answers

Match the following drugs with their primary effects:

Gemofibrozil = Increases hepatic LDL uptake Fenofibrate = Reduces triglycerides Bezafibrate = Modest reduction in LDL Clofibrate = May cause gallstones Signup and view all the answers

What is the primary mechanism of action for Ezetimibe?

Inhibits intestinal absorption of cholesterol (D) Signup and view all the answers

Ezetimibe has a half-life of around 10 hours.

False (B) Signup and view all the answers

What adverse effect is commonly associated with Nicotinic acid (Niacin)?

Cutaneous flushing Signup and view all the answers

Colestipol prevents the reabsorption of bile acids, diverting hepatic cholesterol to ______.

bile acid synthesis Signup and view all the answers

Which condition is Nicotinic acid NOT primarily used to treat?

Hypertension (B) Signup and view all the answers

Match the following cholesterol absorption inhibitors with their characteristics:

Ezetimibe = Inhibits intestinal absorption of cholesterol Colestipol = Binds to bile acids to prevent reabsorption Cholestyramine = Reduces VLDL synthesis and increases HDL clearance Niacin = Reduces hormone-sensitive lipase activity Signup and view all the answers

Cholestyramine is contraindicated in breastfeeding.

True (A) Signup and view all the answers

What is the principal clinical use of Colestipol?

Primary Hypercholesterolemia Signup and view all the answers

Study Notes

Lipid Lowering Drugs for Cardiovascular Disease Prevention

Lipid-lowering drugs are used to treat cardiovascular disease.
People at risk of early death from cardiovascular disease should have lifestyle changes and lipid modification therapy.
Identifying and assessing cardiovascular disease risk is a key aspect of prevention.

Primary Prevention of Statins in Cardiovascular Disease

Offer atorvastatin 20 mg for primary prevention of cardiovascular disease to people with a 10% or greater 10-year risk of developing cardiovascular disease.
For people aged 85 and older, consider atorvastatin 20 mg, as statins may reduce the risk of non-fatal myocardial infarction.
Primary dyslipidemia is a combination of dietary and genetic factors. Familial hypercholesterolemia (FH) is a high risk for coronary heart disease (CHD).
Secondary dyslipidemia is a consequence of other conditions like diabetes, alcoholism, and renal disease.

Treating Dyslipidemia Pharmacologically and Non-Pharmacologically

Non-pharmacological methods include a cardioprotective diet, weight loss, physical activity, and reduced alcohol consumption and smoking cessation.
Pharmacologically, anti-hyperlipidaemic drugs are used.

Different Lipid Lowering Drugs

HMG-CoA reductase inhibitors
Fibrates
Cholesterol absorption inhibitors (Ezetimibe & Bile-acid binding resins)
Omega fatty acids
Nicotinic acid

HMG-CoA Reductase Inhibitors

Simvastatin, Pravastatin, Lovastatin, Atorvastatin, Rosuvastatin, and Fluvastatin are examples.
They block HMG-CoA reductase, a crucial enzyme in cholesterol synthesis.
Short-acting and specific inhibitors include Simvastatin and Lovastatin.
Long-lasting inhibitors include Atorvastatin.
These drugs increase LDL receptor synthesis and increase LDL clearance.
They are mostly short-acting and oral, typically taken at night.
Liver metabolism, primarily by CYP450s, is a key aspect, with some exceptions.
Clinical use includes preventing FH, reducing LDL (30%) and increasing HDL (20%), providing secondary prevention for MI and stroke.
Potential adverse effects include muscle pain and gastrointestinal problems.

Beneficial Effects of HMG-CoA Reductase Inhibitors

Improved endothelial function
Improved vascularisation of ischaemic tissue
Atherosclerotic plaque stabilisation
Reduction in vascular inflammatory response
Reduction in platelet activation
Enhanced fibrinolysis
Antithrombotic properties

Fibrates

Gemfibrozil, Fenofibrate, Bezafibrate are examples.
They act as agonists at peroxisome-activated receptor-alpha (PPAR-alpha).
They increase lipoprotein lipase synthesis, increase fatty acid oxidation, and increase LDL uptake.
They reduce VLDL and TG, with modest reduction in LDL.
They can be helpful for hypertriglyceridemia and mixed hyperlipidemia.
Metabolized by CYP450s and renal excretion is common.
Potential adverse effects include rash, gastrointestinal problems, and rare cases of rhabdomyolysis (muscle breakdown) potentially leading to kidney damage.

Cholesterol Absorption Inhibitors

Ezetimibe, is used to inhibit cholesterol absorption.
It works by affecting Niemann-Pick C1-like 1 (NPC1L1) transport protein.
It's absorbed into intestinal cells.
Clinical use for hyperlipidemia often in combination with statins.
Adverse effects include mild diarrhea and abdominal pain.

Colestipol and Cholestyramine, Cholesterol Absorption Inhibitors

These bind to bile acids in the gut, preventing reabsorption.
They increase LDL receptors, thus increasing LDL removal from the blood.
They are administered orally.
Clinical Use is for primary hypercholesterolemia.
Associated potential adverse effects include constipation, bloating, malabsorption of certain vitamins and minerals.

Nicotinic Acid (Niacin)

Reduces VLDL synthesis in the liver.
Reduces hormone-sensitive lipase activity in adipose tissue.
Increases HDL levels.
Increases VLDL and TG clearance.
It's readily absorbed, metabolized in the liver, and excreted via the kidneys.
Clinical use is for hypercholesterolemia and hypertriglyceridemia, particularly with low HDL levels.
Common adverse effects include flushing and pruritus (itchiness).

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Description

This quiz covers important aspects of lipid-lowering drugs used for preventing cardiovascular disease, focusing on the use of statins for primary prevention. It also discusses the significance of identifying cardiovascular disease risk and the role of lifestyle changes and lipid modification therapy. Test your understanding of dyslipidemia types and treatments.