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CVS Pharmacology > Lipid Lowering > Flashcards

Lipid Lowering Flashcards

1
Q

What is the MOA of statins?

A

Statins are HMG-CoA reductase inhibitors, preventing the synthesis of cholesterol by HMG-CoA

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2
Q

What are 3 examples of statins?

A

Atorvastatin
Simvastatin
Fluvastatin

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3
Q

What is the clinical indication for statins?

A

Lowering LDL-C in all types of hyperlipidemias

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4
Q

When should statins be given?

A

In the evening as de novo synthesis of cholesterol is the predominant pathway at night

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5
Q

What are the adverse effects associated with the use of statins?

A
  1. Abnormalities in liver function
  2. Myopathy & rhabdomyolysis
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6
Q

What group of individuals are statins contraindicated in?

A

Pregnant, nursing mothers
Children & teenagers(Statins affect neurodevelopment of children & fetus)

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7
Q

Why are statins commonly given for hyperlipidemia?

A

Statins are effective in reducing LDL-C levels in all types of hyperlipidemias

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8
Q

What is the MOA of PCSK9 inhibitors?

A

They inhibit PCSK9, preventing the degradation of cell-surface LDL receptors.
This increases LDL uptake by the cells, reducing cirulating LDL.

PCSK9 degrades cell-surface LDL receptors

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9
Q

What are 2 examples of PCSK9 inhibitors?

A

Evolocumab
Alirocumab

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10
Q

What is the route of administration of evolocumab?

A

via injection

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11
Q

What is evolocumab indicated in?

A
  1. Lowering LDL-C levels in familial hypercholesterolaemias, especially those intolerant to statins
  2. Patients with significant atherosclerotic CVD even after being on maximally-tolerated statin therapy
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12
Q

What are the adverse effects associated with the use of PCSK9 inhibitors?

A
  1. Hypersensitivity
  2. Injection site inflammation
  3. Sinusitis & nasopharyngitis
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13
Q

Fibrates activate ________, resulting in increased activity of ________.More triglycerides are uptaken by the cells, reducing plasma triglyceride levels

A

Fibrates activate PPAR-alpha, resulting in increased activity of lipoprotein lipase.More triglycerides are uptaken by the cells, reducing plasma triglyceride levels

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14
Q

What are 2 examples of fibrates?

A

Gemfibrozil
Fenofibrate

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15
Q

What are gemfibrozil/fenofibrate indicated in?

A

Hypertriglyceridemias

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16
Q

What are the adverse effects associated with the use of gemfibrozil/fenofibrate?

A
  1. Nausea2. Rashes3. Gall-stones4. Myositis
17
Q

Omega-3 ethyl esters are functional inhibitors of ____________, preventing the synthesis of triglycerides
Omega-3 ethyl esters also increase free ____________ via ____________

A

Omega-3 ethyl esters are functional inhibitiors of diglyceride acyltransferase, preventing the synthesis of triglycerides
Omega-3 ethyl esters also increase free fatty acid breakdown via beta-oxidation

18
Q

What are the clinical indications for omega-3 acid ethyl esters?

A

Hypertriglyceridaemia (Type IV)Hyperlipidaemia (Type IIb) in combination with statins

19
Q

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

A
  1. GI effects
  2. Increased bleeding time - due to increased production of thromboxane A2
  3. Increase in LDL-C in some patients
20
Q

What class of drug is cholestyramine?

A

Bile acid binding resins

21
Q

What is the MOA of cholestyramine?

A

Binds bile acids in the small intestine, lowering the bile acid concentration.Hepatocytes hence increase conversion of cholesterol to bile acids, causing an increase in the hepatic uptake of LDL-C.

22
Q

What are the clinical indications for cholestyramine?

A

Hypercholesterolemia (IIa)Hyperlipidemia (IIb)

23
Q

What are the adverse effects associated with cholestyramine use?

A
  1. GI effects - nausea, flatulence
  2. Impaired absorption of fat solube vitamins A, D, E, K
24
Q

What class of drug is ezetimibe?

A

Inhibitor of intestinal sterol absorption

25
Q

What is the MOA of ezetimibe?

A

Reduces cholesterol absorption at the small intestine by inhibiting the sterol transport protein NPC1L1

26
Q

What is the clinical indication for ezetimibe?

A

Reduction of LDL

27
Q

What are the adverse effects associated with ezetimibe?

A
  1. GI effects
  2. Rhabdomyolysis
  3. Heptatotoxicity
28
Q

What are the 6 classes of lipid-lowering medications?

A
  1. HMG-CoA inhibitors (statins)
  2. PCSK9 inhibitors
  3. Fibrates
  4. Bile acid binding resins
  5. Omega-3 ethyl esters
  6. Inhibitors of intestinal sterol transporter NPC1L1

CVS Pharmacology (6 decks)

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