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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.
Great job!
List the drug classes that tx hyperlipidemia (5)
Resins
Niacin
Reductase Inhibitors
Fibric Acid Derivatives
Misc: Ezetimibe & Orlistat
Name the Bile Acid Binding Resin prototype

Name two others
Cholestyramine

Colestipol, colesevelam
Cholestyramine

Drug class:

Mech:
Bile Acid Binding Resin

Binds bile acids, preventing their reabsorption from the gut to the liver.
Cholestyramine is useless in what two diseases?
Homozygous Familial Hypercholesterolemia - no recs

Hypertriglyceridemia
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.
Niacin

Drug Class/Mech:

Effects (3):

PHK:
Impairs synth of LPs.

Lowers plasma VLDL & LDL
Inhibits hepatic chol synth.
Increases HDL

Oral abs & RExc
Niacin is most effective for:

Esp when combined with:
Heterozygous Fam Hyperchol

Bile Acid Binding Resin (Cholestyramine)
Niacin might cause:

but it can be prevented with:

because:
Cutaneous sxs

Low dose aspirin

It is PG dependent.
Niacin adverse effects (3):
Cutaneous sxs

Intolerance for glucose

Severe hepatotoxicity (rare)
Lovastatin/statins

Drug class:

Mech:
HMG CoA Reductase Inhibitor

This increases high affinity LDL recs, which decreases plasma TAGs and increases HDL.
Lovastatin additional benefits (5)
Decreases CRP
Increases NO production
Increases plaque stability
Reduces LP Oxidation
Decreases platelet aggregation
Lovastatin

PHK (2)

Uses (2)
Take at night
High first pass

Best with elevated LDL
- Heterozygous Fam Hyper
- Combined hyperlipoproteinemia
Lovastatin Contraindications (3)
Teratogenic
GF juice enhances bioavailability
Gemfibrozil decreases metab
List the Fibric Acid Derivatives (3)
Gemfibrozil
fenofibrate

(Clofibrate)
Gemfibrozil & fenofibrate

PHKs (3)
Oral abs
High PP bind
RExc 70%
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
Gemfibrozil & fenofibrate

Effective for (2):

Useless for (2):
Familial dysbetalipoproteinemia
Hypertriglyceridemia

Primary chylomicronemia
Familial hypercholesterolemia
Gemfibrozil & fenofibrate

Adverse Effects (3)
Gallstones
Potentiate anticoagulants
Inhibits statins
Ezetimibe

Drug class:

Mech:

Combined with:
Cholesterol Absorption Inhibitor

Blocks abs of chol & phytosterols

Statins: synergistic
Orlistat/Xenical

Drug Class:

Mech:

Adverse Effects (2)
Weight loss drug

Decreased TAG breakdown = more TAG excretion

steatorrhea & decreased vit abs
What is the best course of tx for high cholesterol?

High TAGs?

High Choles & High TAGs?
Cholestyramine, ezetimibe

Gemfibrozil

Statins, niacin, ezetimibe
What is good total cholesterol?

What is good LDL?

What is the tx plan?
<200

<130 for no risk; <100 for risky

Lifestyle modification
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
What is high total chol?

What is high LDL?

What is the tx plan?
>240

>160

No risk >190 LDL = drugs
Risky = drugs
Lovestatin efficacy on LDL? On Total TAG?
LDL - 20-40% dec
Total TAGs - 20% dec
Diet mod efficacy on LDL? On Total TAG? On HDL?
LDL - 10-15%
Total TAGs - 20%
HDL - none
Resin efficacy on LDL? On Total TAG? On HDL?
Meh.
Gemfibrozil efficacy on Total TAG?

Why?
40-50%

Increases LPL very well
Niacin efficacy on Total TAG?
20-80%