Mechanisms/Drug Class Flashcards by Melissa V | Brainscape

Q

What is the mechanism of action of cholesterol synthesis inhibitors?

A

Inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis; LDL decreases up to 60%, HDL increases 10% and triglycerides decrease up to 40%

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Q

lovastatin

A

Inhibitor of cholesterol synthesis

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Q

pravastatin

A

Inhibitor of cholesterol synthesis

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Q

simvastatin

A

Inhibitor of cholesterol synthesis

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Q

fluvastatin

A

Inhibitor of cholesterol synthesis

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Q

atorvastatin

A

Inhibitor of cholesterol synthesis

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Q

rosuvastatin

A

Inhibitor of cholesterol synthesis

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Q

pitvastatin

A

Inhibitor of cholesterol synthesis

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Q

What is the mechanism of action of bile acid absorption inhibitors?

A

They bind to bile acids, preventing enterohepatic circulation; LDL decreases up to 28%, HDL increases 5%

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Q

cholestyramine

A

Inhibitor of bile acid absorption

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Q

colesevelam

A

Inhibitor of bile acid absorption

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Q

colestipol

A

Inhibitor of bile acid absorption

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Q

What is the mechanism of action of inhibitors of cholesterol absorption?

A

They decrease cholesterol transport from micelles into the enterocyte by inhibiting uptake through brush border protein NCP1L1; LDL decreases up to 20%, HDL increases 3%, triglycerides decrease 8%

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Q

ezetimibe

A

Inhibitor of cholesterol absorption

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Q

What is the mechanism of action of fibrates?

A

They are agonists of peroxisome proliferator-activity receptor α (PPARα); triglycerides decrease up to 50%, HDL increases up to 20%, DLD decreases up to 15%

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Q

gemfibrozil

A

Fibrate

Q

fenofibrate

A

Fibrate

Q

What is the mechanism of action of niacin?

A

It reduces free fatty acid release from adipose tissue, increases plasma residence time for apoA1; triglycerides decrease up to 45%, LDL decreases up to 20%, HDL increases up to 30%

Q

What is the mechanism of action of omega-3 fatty acids?

A

They regulate nuclear transcription factors including SREBP-1c and PPARα to reduce triglyceride biosynthesis and increase fatty acid oxidation; reduces plasma triglycerides by up to 50%

Q

Eicosapenaenoic acid

A

Omega-3 fatty acid

Q

docosahexaenoic acid

A

Omega-3 fatty acid