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44 Cards in this Set
- Front
- Back
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What is the primary aim of lipid-lowering drugs? |
Reduce plasma CH |
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How do these drugs act? 2 ways |
Control dietary intake of CH and other fats Direct pharmacological intervention |
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What dietary changes are implicated to reduce lipid levels? |
consume <200 mg/day of CH (overall weight) Maintain total fat to <30% of total calories ±30% of fat should mono/polyunsaturated |
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Under which circumstances is drug treatment required? |
Suffers CAD/at risk of developing it Primary = lack of LDLR expr |
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3 main types of drug |
HMG CoA reductase inhibitors Fibrates Bile acid binding resins |
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what are statins? |
HMG CoA reductase inhibitors |
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What do statins inhibit? |
Endogenous CH synth, inhibits the enzyme that constantly makes CH |
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Eg.s of statins? 3 |
Atorvastatin Simvastatin Pravastatin |
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For which type of lipoprotein are statins used? |
High LDL (apo a) and high LDL + VLDL |
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If you have primary conditions --> what are you not expressing? |
Not expressing enough receptors to clear CH |
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What is the mechanism of action do statins work by? |
Rate limiting step involves HMG CoA reductase Converts HMG CoA to mevalonate (endogenous pway) act as false substrates, competitive anatagonism |
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How do statins reduced CH? |
Low CH levels stimulate LDL receptor production and uptake of LDLs Upreg of expression of LDLRs and transports more of it into cells Increased LDL clearance |
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Possible side-effects of statins? 2 |
GIT: abdominal pain, nausea Muscle pain possible ot weakness (decreased blood flow, breakdown of muscle at increased rate) |
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Additional benefits of statins?
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Improved endothelial function via mech of action Reduced platelet aggregability Increased neovascularisation of ischaemic tissue Antithrombotic actions Atherosclerotic plaque stabilisation Immunesuppresion |
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Contraindications of statins? |
Caution if history of liver disease Contraindicated in active liver disease use with caution if high alcohol intake Contraindicated in pregnancy and breast-feeding |
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Name 2 Fibric acids (fibrates)? When are these used? |
Gemfibrozil Fenofibrate when statins are contraindicated |
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What are fibrates used to combat? |
High levels of VLDL |
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What are fibrates agonists at? |
PPAR alpha (peroxisome proliferator-activated receptor alpha) |
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Mechanism of action of fibrates? |
Increase act of lipoprotein lipase Increases catabolism of TG rich VLDL + IDL |
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What happens if VLDL is reduced what occurs? |
CH of HD cannot be exchanged thus reduced LDL-CH |
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GEMFIBROZIL: How is it administered? What does it reduce? What does it increase? When can it be used? |
Orally TG and CH levels HDL-CH when statins are contraindicated |
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Side-effects of fibrates? |
Generally well-tolerated Rare May cause muscular damage, can lead to kidney disease |
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Contraindication of fibrates? |
Don't use if history of renal impairment |
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2 e.gs of bile acid resins? |
Cholestyramine Colestipol |
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Where do bile acid resins act? |
Not working systemically do not absorb into it |
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What are bile acid resins used against? |
High LDL (2 alpha) |
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Often used with which other drug type? |
Statins |
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Mechanism of action of bile acid resins? |
Act as ion-exchange resins Bind to bile acids = elimination High conc of bile acids inhibits the enzyme controlling this process NEGATIVE FEEDBACK |
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What are bile acids needed for? |
Absorption of CH |
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What does removal of bile acids do? What problem does this cause? How does this organ respond? |
Less CH absorbed liver needs CH increased HMG CoA reductase activity and increased LDL receptors to clear from plasma |
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Side effects of BABRs? 3 |
Not absorbed Can cause nausea, constipation, diarrhoea and severe flatulence Can decrease absorp of fat-sol vits (K, folic acid and other drugs) |
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Name an adjunct to statins? What does it do? |
Ezetimbe (azetidione) CH absorption inhibitor |
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How does ezetimibe work? |
Binds to NPC1L1 in brush border of enterocytes |
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Benefit of ezetemibe? |
No effect on K absorption |
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Side effects of ezetimibe? |
Well tolerated |
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What does nictotinic acid reduce? |
VLDL and to some extent IDL =ldl |
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How does nicotinic acid work? 2 ways |
1) decreased TG adn VLDL secretion by liver 2) increased lipoprotein lipase activity (breaks down VLDL) |
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What does nicotinic acid increase? |
HDL |
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Side effects of nicotinic acid? 4 |
1) GIT disturbances 2) liver function 3) palpitations 4) Flushing PGD2 |
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What do fish oils tend to reduce? |
TG |
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Unwanted effects of fish oils? 2 |
Flatulence and nausea |
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Name 2 plant sterols?
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Beta-sitosterol
sitosterol (benecol) |
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How do plant sterols work? What do they reduce? |
Inhibit absorption of dietary endogenous CH Total LDL-CH in plasma |
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Problem with plant sterols? |
Needed in large amounts to see an effect |
