CVS - Lipids Lowering Medication Flashcards
What is the correlation between coronary artery disease and plasma lipoproteins?
Coronary artery disease is correlated with the levels of plasma cholesterol and/or triacylglycerol-containing lipoproteins.
What are chylomicrons?
Chylomicrons are lipoproteins formed in the intestinal mucosa, transporting dietary triglycerides, cholesterol, and other lipids.
What role does VLDL play in the body?
VLDL transports endogenously synthesized triglycerides from the liver to adipose tissue and skeletal muscle.
What is the primary role of LDL?
LDL primarily transports cholesterol to peripheral tissues and is involved in the formation of cholesterol plaques in arteries.
How does HDL contribute to lipid metabolism?
HDL is involved in reverse cholesterol transport, carrying cholesterol away from the plasma and tissues to the liver for excretion.
What is the exogenous pathway of cholesterol transport?
The exogenous pathway involves the absorption and transport of dietary cholesterol and triglycerides from the intestines to the liver.
Describe the endogenous pathway of cholesterol transport.
The endogenous pathway transports endogenously synthesized cholesterol and triglycerides from the liver to peripheral tissues.
What is Type I hyperlipoproteinemia?
Type I hyperlipoproteinemia is characterized by elevated chylomicrons due to a deficiency in lipoprotein lipase or its co-factor.
Which lipoprotein is elevated in Type IIa hyperlipoproteinemia?
In Type IIa hyperlipoproteinemia, LDL is elevated.
What causes Type IV hyperlipoproteinemia?
Type IV is caused by an overproduction or decreased clearance of VLDL.
What dietary changes are recommended for dyslipidemia treatment?
Recommendations include reducing saturated fats, trans fats, and cholesterol, and increasing fibre intake.
What is the mechanism of action of PCSK9 inhibitors?
PCSK9 inhibitors block the protein PCSK9, increasing the number of LDL receptors in the liver and lowering LDL cholesterol levels in the plasma.
How do fibrates lower lipid levels?
Fibrates decrease triglyceride levels by activating PPAR-?, enhancing lipolysis and elimination of triglyceride-rich particles.
What is the role of omega-3 acid ethyl esters in lipid lowering?
Omega-3 acid ethyl esters reduce hepatic triglyceride synthesis, lowering VLDL and triglyceride levels.
How do bile acid binding resins lower cholesterol?
They bind bile acids in the intestine, preventing their reabsorption and causing the liver to use more cholesterol to make bile acids.
What is the action of ezetimibe in cholesterol lowering?
Ezetimibe inhibits intestinal absorption of cholesterol, leading to reduced plasma cholesterol levels.
What is the primary action of HMG-CoA reductase inhibitors (Statins)?
Statins inhibit HMG-CoA reductase, reducing cholesterol synthesis in the liver and increasing hepatic LDL receptor expression.
How do PCSK9 inhibitors differ from statins?
PCSK9 inhibitors block a protein that degrades LDL receptors, while statins inhibit cholesterol synthesis in the liver.
What are the clinical uses of fibrates?
Fibrates are primarily used to lower triglyceride levels and increase HDL cholesterol levels.
In which condition are omega-3 acid ethyl esters particularly effective?
They are effective in lowering triglycerides in hypertriglyceridemia.
When are bile acid binding resins prescribed?
They are used in hypercholesterolemia, particularly when statins are contraindicated or insufficient.
What is the pharmacokinetic property of ezetimibe?
Ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide.
What are the common adverse effects of statins?
Common adverse effects include myalgia, increased liver enzymes, and a risk of diabetes.
Name a significant adverse effect of PCSK9 inhibitors.
PCSK9 inhibitors can cause injection site reactions.
What are the adverse effects of fibrates?
Fibrates can cause gastrointestinal disturbances, gallstones, and myopathy.
What adverse effects are associated with omega-3 acid ethyl esters?
Common adverse effects include eructation, dyspepsia, and taste perversion.
What is a major side effect of bile acid binding resins?
They can cause gastrointestinal side effects like constipation and bloating.
What is a unique side effect of ezetimibe?
Ezetimibe can cause rare cases of myopathy and rhabdomyolysis.
How does the liver respond to reduced cholesterol synthesis by statins?
The liver increases LDL receptor expression to uptake more LDL from the blood.
What is the impact of PCSK9 inhibitors on LDL receptors?
PCSK9 inhibitors increase the number of LDL receptors available to clear LDL from the bloodstream.
How do fibrates activate PPAR-??
Fibrates are ligands for PPAR-?, activating gene transcription for fatty acid oxidation.
Why are omega-3 acid ethyl esters beneficial in hypertriglyceridemia?
They reduce hepatic triglyceride synthesis and VLDL secretion.
What is the primary function of bile acid binding resins in cholesterol metabolism?
They interrupt the enterohepatic circulation of bile acids, forcing the liver to make more bile by using more cholesterol.
How does ezetimibe specifically target cholesterol absorption?
Ezetimibe selectively inhibits the intestinal absorption of cholesterol and related phytosterols by inhibiting the NPC1L1 transport protein in enterocytes .
What is the relationship between HMG-CoA reductase and cholesterol synthesis?
HMG-CoA reductase is a key enzyme in the mevalonate pathway that produces cholesterol.
How does blocking PCSK9 affect cholesterol levels?
Blocking PCSK9 increases LDL receptor levels, leading to decreased blood LDL cholesterol levels.
What is the primary effect of fibrates on lipid profiles?
Fibrates primarily lower triglycerides and can modestly increase HDL cholesterol.
How do omega-3 acid ethyl esters affect triglyceride-rich lipoproteins?
They reduce the synthesis and secretion of VLDL, thereby lowering triglyceride levels.
What is the consequence of binding bile acids in the intestine?
It reduces their reabsorption and increases cholesterol utilization for bile acid synthesis.
How does ezetimibe complement statin therapy?
Ezetimibe adds to the cholesterol-lowering effect of statins by inhibiting intestinal cholesterol absorption.
What is the effect of statins on hepatic LDL receptor expression?
Statins increase the expression of LDL receptors on hepatocytes.
Why is the inhibition of PCSK9 beneficial in cholesterol management?
Inhibiting PCSK9 leads to increased degradation of blood LDL cholesterol via upregulated LDL receptors.
Describe the mechanism by which fibrates lower triglycerides.
Fibrates activate PPAR-?, leading to increased oxidation of fatty acids and decreased triglyceride synthesis.
What role do omega-3 acid ethyl esters play in VLDL metabolism?
They reduce the hepatic synthesis of triglycerides, thus lowering VLDL production.
How do bile acid binding resins indirectly reduce cholesterol levels?
By binding bile acids, they decrease their reabsorption, forcing the liver to use cholesterol to produce more bile acids.
What is the mechanism of action of HMG-CoA Reductase Inhibitors (Statins)?
Statins inhibit HMG-CoA reductase, upregulating LDL receptors on the liver surface.
How do PCSK9 Inhibitors work?
They inhibit hepatic PCSK9, reducing LDL receptor degradation and lowering LDL cholesterol.
What is the action of Fibrates/Fibric Acid Derivatives?
They activate lipoprotein lipase via PPAR-?, decreasing plasma triglycerides and VLDL, and moderately increasing HDL.
Describe the actions of Omega-3-acid Ethyl Esters.
They reduce hepatic triglyceride productionand increase fatty acid beta-oxidation.
How do Bile Acid Binding Resins function?
They bind bile acids in the intestine, lowering bile acid concentration, and activating increased hepatic uptake of LDL.
What is the action of Ezetimibe in lipid management?
Ezetimibe reduces cholesterol absorption in the small intestine by inhibiting the sterol transporter NPC1L1.
What are the adverse effects of Statins?
Statins may cause abnormalities in liver function, myopathy, and rhabdomyolysis.
What are the contraindications for using Statins?
Statins are contraindicated in pregnancy, nursing mothers, and children or teenagers due to potential neurodevelopmental effects.
What is the role of chylomicrons in lipid metabolism?
Chylomicrons transport dietary triglycerides and cholesterol from the intestines to peripheral tissues.
What is the significance of LDL in cardiovascular health?
LDL, often referred to as “bad” cholesterol, is crucial in plaque formation in arteries, leading to atherosclerosis.
Why is HDL considered “good” cholesterol?
HDL helps in transporting cholesterol away from the plasma to the liver for excretion, reducing atherosclerosis risk.
What is the exogenous lipid transport pathway?
It involves the absorption and transport of dietary lipids from the intestines to the liver.
Describe the endogenous lipid transport pathway.
This pathway transports lipids synthesized in the liver to peripheral tissues.
What is hyperlipoproteinemia type IIb?
It is characterized by elevated levels of both LDL and VLDL.
What lifestyle modifications are recommended for managing dyslipidemia?
Modifications include a diet low in saturated fats and cholesterol, regular exercise, and weight management.
What is the clinical use of PCSK9 inhibitors?
PCSK9 inhibitors are used to lower LDL cholesterol, especially in patients with familial hypercholesterolemia or statin intolerance.
What is the significance of bile acid binding resins in cholesterol management?
These resins lower LDL cholesterol by binding bile acids in the intestine, reducing their reabsorption.
How do fibrates affect HDL cholesterol?
Fibrates can increase HDL cholesterol levels by reducing the catabolism of apolipoprotein AI and AII.
