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TYPES OF LIPIDS
Triglycerides: 90% lipids in body
o Major storage form of fat
o Only lipid that serves impt E source
Phospholipids: build plasma membranes
o Lecithins: egg yolk, soy beans
Steroids: sterol nucleus/ring structure
o Cholesterol: hi level = atherosclerosis
Fxn: building block for biochem Vitamin D, bile acids, cortisol,
estrogen, testosterone
Body makes 75%; diet provides 25%
AHA: limit dietary chol to 300mg/day
LIFESTYLE CHANGES: goal should be maintain normal lipid values w/o pharmacotx
Diet:
o Fat <30% total caloric intake
o Chol reduced, <300mg/day
Liver reacts to lo-chol by making more chol, inhibt excretion when saturated fats
present
o SO pt must reduce BOTH saturdated and chol to reduce [chol blood]
Eating plant sterols leads to chol excretion
o Less chol delivered to liver, LDL uptake increases, decrease LDL serum level
o Ex) nuts, wheat, corn, rye, oats, rice, olive oil
CHAPTER 22: Drugs for Lipid Disorders
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HMG-CoA REDUCTASE INHIBITORS / STATINS
First line antihyperlipidemics
Effectiveness
o Reduce LDL levels 20-40%; raise HDL
o Reduce CV-related events 25-30%
Mechanism:
o Chol made in liver
o HMG-CoA reductase is primary regulatory site for chol biosyn
Normal cond: enzyme controlled via neg feedback
i.e. hi LDL shuts down HMG-CoA reductase & stops prod of chol
o Statins: inhibit HMG-CoA reductase less chol biosyn
Less chol prod, more LDL receptors made on surface of liver cells
So increase removal LDL from blood
o NOT permanent pt must remain on drugs until hyperlipidemia controlled by
diet, lifestyle changes
AEs: oral, mostly well-tolerated
o Minor: headache, fatigue, muscle/joint pain, heartburn
o Rare SAE: myopathy (musc weakness), rhabdomyolysis (breakdown of musc
fibers into systemic circulation acute renal failure)
Admin:
o Statins w/ short half lives should be given @ night because chol biosyn higher @
night
o Combine with bile acid sequestrants, niacin to boost effectiveness
o Admin with food to decrease GI discomfort
o Most preg category X!!!
Prototype: Atorvastatin (Lipitor)
Note: takes 2 wk for therapeutic effects
HMG-CoA reductase Inhibit HMG-CoA enzyme Headaches, GI complaints, Serious Preg category X!! X
inhibitor less chol synthesis, incr musc/joint pain, fatigue liver dx
LDL receptors NO grapefruit juice, red yeast rice.
Atorvastatin Rhabdomyolysis, myopathy,
Take w food! hepatic damage Take w/ CoQ10 to prevent deficiency