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30 Cards in this Set
- Front
- Back
Draw the basic biochem synthesis of lipids in your head. Visualize where each of the drug classes work.
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Great job!
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List the drug classes that tx hyperlipidemia (5)
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Resins
Niacin Reductase Inhibitors Fibric Acid Derivatives Misc: Ezetimibe & Orlistat |
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Name the Bile Acid Binding Resin prototype
Name two others |
Cholestyramine
Colestipol, colesevelam |
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Cholestyramine
Drug class: Mech: |
Bile Acid Binding Resin
Binds bile acids, preventing their reabsorption from the gut to the liver. |
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Cholestyramine is useless in what two diseases?
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Homozygous Familial Hypercholesterolemia - no recs
Hypertriglyceridemia |
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Cholestyramine
PHKs (2) Adverse effects (2) Impairs abs of (5) [DATTA] |
Take with meals. Not absorbed.
Cause constipation and bloating. Digitalis, abx, thiazides, thyroxine, aspirin. |
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Niacin
Drug Class/Mech: Effects (3): PHK: |
Impairs synth of LPs.
Lowers plasma VLDL & LDL Inhibits hepatic chol synth. Increases HDL Oral abs & RExc |
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Niacin is most effective for:
Esp when combined with: |
Heterozygous Fam Hyperchol
Bile Acid Binding Resin (Cholestyramine) |
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Niacin might cause:
but it can be prevented with: because: |
Cutaneous sxs
Low dose aspirin It is PG dependent. |
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Niacin adverse effects (3):
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Cutaneous sxs
Intolerance for glucose Severe hepatotoxicity (rare) |
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Lovastatin/statins
Drug class: Mech: |
HMG CoA Reductase Inhibitor
This increases high affinity LDL recs, which decreases plasma TAGs and increases HDL. |
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Lovastatin additional benefits (5)
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Decreases CRP
Increases NO production Increases plaque stability Reduces LP Oxidation Decreases platelet aggregation |
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Lovastatin
PHK (2) Uses (2) |
Take at night
High first pass Best with elevated LDL - Heterozygous Fam Hyper - Combined hyperlipoproteinemia |
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Lovastatin Contraindications (3)
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Teratogenic
GF juice enhances bioavailability Gemfibrozil decreases metab |
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List the Fibric Acid Derivatives (3)
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Gemfibrozil
fenofibrate (Clofibrate) |
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Gemfibrozil & fenofibrate
PHKs (3) |
Oral abs
High PP bind RExc 70% |
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Gemfibrozil & fenofibrate
Drug Class: Mech: Effects: |
Fibric Acid Derivatives
They fcn as a ligand for PPAR-a, a nuclear transcription regulator. Increased LPL = decreased VLDL = decreased TAGs Decreased hepatic chol synth |
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Gemfibrozil & fenofibrate
Effective for (2): Useless for (2): |
Familial dysbetalipoproteinemia
Hypertriglyceridemia Primary chylomicronemia Familial hypercholesterolemia |
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Gemfibrozil & fenofibrate
Adverse Effects (3) |
Gallstones
Potentiate anticoagulants Inhibits statins |
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Ezetimibe
Drug class: Mech: Combined with: |
Cholesterol Absorption Inhibitor
Blocks abs of chol & phytosterols Statins: synergistic |
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Orlistat/Xenical
Drug Class: Mech: Adverse Effects (2) |
Weight loss drug
Decreased TAG breakdown = more TAG excretion steatorrhea & decreased vit abs |
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What is the best course of tx for high cholesterol?
High TAGs? High Choles & High TAGs? |
Cholestyramine, ezetimibe
Gemfibrozil Statins, niacin, ezetimibe |
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What is good total cholesterol?
What is good LDL? What is the tx plan? |
<200
<130 for no risk; <100 for risky Lifestyle modification |
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What is borderline total chol?
What is borderline LDL? What is the tx plan? |
200-239
130-159 No risk: lifestyle modification Risky: consider drugs |
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What is high total chol?
What is high LDL? What is the tx plan? |
>240
>160 No risk >190 LDL = drugs Risky = drugs |
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Lovestatin efficacy on LDL? On Total TAG?
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LDL - 20-40% dec
Total TAGs - 20% dec |
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Diet mod efficacy on LDL? On Total TAG? On HDL?
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LDL - 10-15%
Total TAGs - 20% HDL - none |
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Resin efficacy on LDL? On Total TAG? On HDL?
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Meh.
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Gemfibrozil efficacy on Total TAG?
Why? |
40-50%
Increases LPL very well |
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Niacin efficacy on Total TAG?
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20-80%
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