Pharm- Hyperlipidemia

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Pharm II, Exam III

Optimal LDL level

< 100 mg/dL

Optimal total cholesterol

< 200 mg/dL

minimum level for HDL

< 40 mg/dL

what to have at least 60 mg/dL

NL level for triglycerides

<150 mg/dL

What are the CHD risk equivalents?

CAD, PAD (PVD), AAA, DM

What is in the clinical def'n of CHD?

angina, MI, angioplasty or stent placement, CABG

what is the CHD risk equivalent in CAD?

history of stroke, TIA, carotid stenosis

what is the CHD risk equivalent in PAD?

claudication

Adequate lifestyle changes trial?

12 weeks

restrict cholesterol and sat fats
regular exercise
weight reduction
inc'd leafy green veggies
inc'd fiber intake

What are the Bile Acid Sequesterants? what do they specifically help with?

1. Cholestyramine Granules
2. Colestipol Granules and tablets
3. Colesevelam

Lowering LDL! - they bind bile acid in the intestines

Are the bile acid seq. systemically absorbed?

no (ADRs are GI)

ADRs for Bile Acid Seq?

GI!
flatulence, constipation, bloating, fullness, nausea

inc'd TGs

What is the problem with Bile Acid Seq?

You will poop out any other drug you take

bind to many drugs, vitamins, nutrients

HMG-CoA Reductase inhibitors ("statins")

Atorvastatin (lipitor)
Fluvastatin (Lescol)
Lovastatin
Pravastatin
Rosuvastatin
Pitavastatin

MOA: rate limiting step in cholesterol production is conversion of HMG-CoA to mevalonate

What is great about statins?

Affect All 3 lipid componenents!
HDL, LDL, TGs

What are the potencies of statins?

rosuva > atorva = pitava > simva = prava > lova > fluva

What is the most potent statin?

Rosuvastatin, then Atorvastatin

Which statin do we no longer dose to 80mg bc of inc'd adrs?

Simvastatin

Side Effects of Statins

inc'd LFTs
myopathy/myalgia/myositis/rhabdo
DM - may inc blood sugar, HgA1C

what is the MOA for the muscle aches? Risk factors

ubiquinone (coenzyme Q10) deficiency

advanced age, female, renal insuf, liver dysfunction, small body frame, frail, multiple meds

myopathy

general term for muscle complaint

myalgia

most common!
muscle complaints without elevation in CK

myositis

muscle complaints with elevation of CK

rhabdomyolysis

marked inc'd CK (> 10 x UL of NL)

usually w/ creatinine elevation, brown urine, urinary myoglobin

When do you d/c statin therapy?

if 10x upper limit of normal

or symptomatic and CK continues to rise

can consider switching to different statin- switch to a less lipophilic (fluva, rosuva, prava)

what should you not drink with a statin?

Grapefruit Juice!!!

not as big of problem with fluva, rosuva, prava - less lipophilic

Drug Interxns with Statins

Grapefruit juice (rhabdo)
Niacin, Fibric Acid Deriv. (hepatotox.)
BAS (dec'd absorption)

When should we not use statins?

pregnancy
chronic liver disease

Niacin (nicotinic acid)? MOA? max dose?

Niaspan (sustained release)

reduces production of VLDL in liver - primarily biotransformation in liver (dec'd syn of LDL, TGs, inc'd HDL!)

max dose 2 g/day due to hepatoxicity

Niacin side effects

cutaneous flushing
GI
Inc'd uric acid - gout attack
inc'd blood sugar
liver dysfunction
myopathy/myalgias/myositis/rhabdo

When should you not take niacin?

Gout, DM, PUD, chronic liver disease

which drug can cause a gout flare?

Niacin

Fibric Acid Derivatives? MOA?

Gemfibrozil
Fenofibrate
Fenofibric Acid

increase lipoprotein lipase = reduce VLDL - used to treat TGs only

dec'd TGs 20-50%!

which drug lowers TGs only?

Fibric acid derivatives

side effects of fibric acid derivatives?

gallstones
cholecystitis
myositis/myopathy - usually if combined with niacin or statin

what drug interaction is a problem with fibric acid derivatives?

Statins - inc'd hepatotoxicity and inc'd risk of rhabdomyolysis

When do you need to use caution with fibric acid derivatives?

gallstone patients

Cholesterol Absorption inhibitors? MOA?

Ezetimibe (Zetia)

inhibits cholesterol abs in small intestine, inc'd syn of LDL receptors decreasing LDL levels
- inhibs ~54% of all intestinal cholesterol absorption

what does Zetia primarily Lower?

LDL

what is the best combination therapy?

Simvastin + Ezetimibe (Vytorin)

can be controversial, we don't recommend right off the bat - inc'd risk of side effects

Red Yeast Rice has same MOA as what?

Statins

What do omega 3 fatty acids do?

prevent heard disease
decrease triglycerides
anti-inflammatory properties

Omega 3 FA agents

Eicosapentaenoid acid (EPA)
Docosahexaenoic acid (DHA)

Alpha-Linolenic acid (vegan option, not as good)

What is the RX only Omega 3 FA drug?

Lovaza

what is the recommended amount of omega 3?

1500-2000mg/day

What is a potential problem with too high of a dose of omega 3?

risk of bleeding (anticoagulant)

important to know before surgery if ppl are on these!

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