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Master YLL Pharmacology > CVS - Lipids Lowering Medication > Flashcards

CVS - Lipids Lowering Medication Flashcards

1
Q

What is the correlation between coronary artery disease and plasma lipoproteins?

A

Coronary artery disease is correlated with the levels of plasma cholesterol and/or triacylglycerol-containing lipoproteins.

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2
Q

What are chylomicrons?

A

Chylomicrons are lipoproteins formed in the intestinal mucosa, transporting dietary triglycerides, cholesterol, and other lipids.

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3
Q

What role does VLDL play in the body?

A

VLDL transports endogenously synthesized triglycerides from the liver to adipose tissue and skeletal muscle.

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4
Q

What is the primary role of LDL?

A

LDL primarily transports cholesterol to peripheral tissues and is involved in the formation of cholesterol plaques in arteries.

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5
Q

How does HDL contribute to lipid metabolism?

A

HDL is involved in reverse cholesterol transport, carrying cholesterol away from the plasma and tissues to the liver for excretion.

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6
Q

What is the exogenous pathway of cholesterol transport?

A

The exogenous pathway involves the absorption and transport of dietary cholesterol and triglycerides from the intestines to the liver.

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7
Q

Describe the endogenous pathway of cholesterol transport.

A

The endogenous pathway transports endogenously synthesized cholesterol and triglycerides from the liver to peripheral tissues.

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8
Q

What is Type I hyperlipoproteinemia?

A

Type I hyperlipoproteinemia is characterized by elevated chylomicrons due to a deficiency in lipoprotein lipase or its co-factor.

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9
Q

Which lipoprotein is elevated in Type IIa hyperlipoproteinemia?

A

In Type IIa hyperlipoproteinemia, LDL is elevated.

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10
Q

What causes Type IV hyperlipoproteinemia?

A

Type IV is caused by an overproduction or decreased clearance of VLDL.

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11
Q

What dietary changes are recommended for dyslipidemia treatment?

A

Recommendations include reducing saturated fats, trans fats, and cholesterol, and increasing fibre intake.

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12
Q

What is the mechanism of action of PCSK9 inhibitors?

A

PCSK9 inhibitors block the protein PCSK9, increasing the number of LDL receptors in the liver and lowering LDL cholesterol levels in the plasma.

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13
Q

How do fibrates lower lipid levels?

A

Fibrates decrease triglyceride levels by activating PPAR-?, enhancing lipolysis and elimination of triglyceride-rich particles.

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14
Q

What is the role of omega-3 acid ethyl esters in lipid lowering?

A

Omega-3 acid ethyl esters reduce hepatic triglyceride synthesis, lowering VLDL and triglyceride levels.

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15
Q

How do bile acid binding resins lower cholesterol?

A

They bind bile acids in the intestine, preventing their reabsorption and causing the liver to use more cholesterol to make bile acids.

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16
Q

What is the action of ezetimibe in cholesterol lowering?

A

Ezetimibe inhibits intestinal absorption of cholesterol, leading to reduced plasma cholesterol levels.

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17
Q

What is the primary action of HMG-CoA reductase inhibitors (Statins)?

A

Statins inhibit HMG-CoA reductase, reducing cholesterol synthesis in the liver and increasing hepatic LDL receptor expression.

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18
Q

How do PCSK9 inhibitors differ from statins?

A

PCSK9 inhibitors block a protein that degrades LDL receptors, while statins inhibit cholesterol synthesis in the liver.

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19
Q

What are the clinical uses of fibrates?

A

Fibrates are primarily used to lower triglyceride levels and increase HDL cholesterol levels.

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20
Q

In which condition are omega-3 acid ethyl esters particularly effective?

A

They are effective in lowering triglycerides in hypertriglyceridemia.

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21
Q

When are bile acid binding resins prescribed?

A

They are used in hypercholesterolemia, particularly when statins are contraindicated or insufficient.

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22
Q

What is the pharmacokinetic property of ezetimibe?

A

Ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide.

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23
Q

What are the common adverse effects of statins?

A

Common adverse effects include myalgia, increased liver enzymes, and a risk of diabetes.

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24
Q

Name a significant adverse effect of PCSK9 inhibitors.

A

PCSK9 inhibitors can cause injection site reactions.

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25
Q

What are the adverse effects of fibrates?

A

Fibrates can cause gastrointestinal disturbances, gallstones, and myopathy.

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26
Q

What adverse effects are associated with omega-3 acid ethyl esters?

A

Common adverse effects include eructation, dyspepsia, and taste perversion.

27
Q

What is a major side effect of bile acid binding resins?

A

They can cause gastrointestinal side effects like constipation and bloating.

28
Q

What is a unique side effect of ezetimibe?

A

Ezetimibe can cause rare cases of myopathy and rhabdomyolysis.

29
Q

How does the liver respond to reduced cholesterol synthesis by statins?

A

The liver increases LDL receptor expression to uptake more LDL from the blood.

30
Q

What is the impact of PCSK9 inhibitors on LDL receptors?

A

PCSK9 inhibitors increase the number of LDL receptors available to clear LDL from the bloodstream.

31
Q

How do fibrates activate PPAR-??

A

Fibrates are ligands for PPAR-?, activating gene transcription for fatty acid oxidation.

32
Q

Why are omega-3 acid ethyl esters beneficial in hypertriglyceridemia?

A

They reduce hepatic triglyceride synthesis and VLDL secretion.

33
Q

What is the primary function of bile acid binding resins in cholesterol metabolism?

A

They interrupt the enterohepatic circulation of bile acids, forcing the liver to make more bile by using more cholesterol.

34
Q

How does ezetimibe specifically target cholesterol absorption?

A

Ezetimibe selectively inhibits the intestinal absorption of cholesterol and related phytosterols by inhibiting the NPC1L1 transport protein in enterocytes .

35
Q

What is the relationship between HMG-CoA reductase and cholesterol synthesis?

A

HMG-CoA reductase is a key enzyme in the mevalonate pathway that produces cholesterol.

36
Q

How does blocking PCSK9 affect cholesterol levels?

A

Blocking PCSK9 increases LDL receptor levels, leading to decreased blood LDL cholesterol levels.

37
Q

What is the primary effect of fibrates on lipid profiles?

A

Fibrates primarily lower triglycerides and can modestly increase HDL cholesterol.

38
Q

How do omega-3 acid ethyl esters affect triglyceride-rich lipoproteins?

A

They reduce the synthesis and secretion of VLDL, thereby lowering triglyceride levels.

39
Q

What is the consequence of binding bile acids in the intestine?

A

It reduces their reabsorption and increases cholesterol utilization for bile acid synthesis.

40
Q

How does ezetimibe complement statin therapy?

A

Ezetimibe adds to the cholesterol-lowering effect of statins by inhibiting intestinal cholesterol absorption.

41
Q

What is the effect of statins on hepatic LDL receptor expression?

A

Statins increase the expression of LDL receptors on hepatocytes.

42
Q

Why is the inhibition of PCSK9 beneficial in cholesterol management?

A

Inhibiting PCSK9 leads to increased degradation of blood LDL cholesterol via upregulated LDL receptors.

43
Q

Describe the mechanism by which fibrates lower triglycerides.

A

Fibrates activate PPAR-?, leading to increased oxidation of fatty acids and decreased triglyceride synthesis.

44
Q

What role do omega-3 acid ethyl esters play in VLDL metabolism?

A

They reduce the hepatic synthesis of triglycerides, thus lowering VLDL production.

45
Q

How do bile acid binding resins indirectly reduce cholesterol levels?

A

By binding bile acids, they decrease their reabsorption, forcing the liver to use cholesterol to produce more bile acids.

46
Q

What is the mechanism of action of HMG-CoA Reductase Inhibitors (Statins)?

A

Statins inhibit HMG-CoA reductase, upregulating LDL receptors on the liver surface.

47
Q

How do PCSK9 Inhibitors work?

A

They inhibit hepatic PCSK9, reducing LDL receptor degradation and lowering LDL cholesterol.

48
Q

What is the action of Fibrates/Fibric Acid Derivatives?

A

They activate lipoprotein lipase via PPAR-?, decreasing plasma triglycerides and VLDL, and moderately increasing HDL.

49
Q

Describe the actions of Omega-3-acid Ethyl Esters.

A

They reduce hepatic triglyceride productionand increase fatty acid beta-oxidation.

50
Q

How do Bile Acid Binding Resins function?

A

They bind bile acids in the intestine, lowering bile acid concentration, and activating increased hepatic uptake of LDL.

51
Q

What is the action of Ezetimibe in lipid management?

A

Ezetimibe reduces cholesterol absorption in the small intestine by inhibiting the sterol transporter NPC1L1.

52
Q

What are the adverse effects of Statins?

A

Statins may cause abnormalities in liver function, myopathy, and rhabdomyolysis.

53
Q

What are the contraindications for using Statins?

A

Statins are contraindicated in pregnancy, nursing mothers, and children or teenagers due to potential neurodevelopmental effects.

54
Q

What is the role of chylomicrons in lipid metabolism?

A

Chylomicrons transport dietary triglycerides and cholesterol from the intestines to peripheral tissues.

55
Q

What is the significance of LDL in cardiovascular health?

A

LDL, often referred to as “bad” cholesterol, is crucial in plaque formation in arteries, leading to atherosclerosis.

56
Q

Why is HDL considered “good” cholesterol?

A

HDL helps in transporting cholesterol away from the plasma to the liver for excretion, reducing atherosclerosis risk.

57
Q

What is the exogenous lipid transport pathway?

A

It involves the absorption and transport of dietary lipids from the intestines to the liver.

58
Q

Describe the endogenous lipid transport pathway.

A

This pathway transports lipids synthesized in the liver to peripheral tissues.

59
Q

What is hyperlipoproteinemia type IIb?

A

It is characterized by elevated levels of both LDL and VLDL.

60
Q

What lifestyle modifications are recommended for managing dyslipidemia?

A

Modifications include a diet low in saturated fats and cholesterol, regular exercise, and weight management.

61
Q

What is the clinical use of PCSK9 inhibitors?

A

PCSK9 inhibitors are used to lower LDL cholesterol, especially in patients with familial hypercholesterolemia or statin intolerance.

62
Q

What is the significance of bile acid binding resins in cholesterol management?

A

These resins lower LDL cholesterol by binding bile acids in the intestine, reducing their reabsorption.

63
Q

How do fibrates affect HDL cholesterol?

A

Fibrates can increase HDL cholesterol levels by reducing the catabolism of apolipoprotein AI and AII.

Master YLL Pharmacology (36 decks)

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