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KG - Pharmacology 2 > KG - Pharm 2 Exam 2, Hyperlipidemia > Flashcards

KG - Pharm 2 Exam 2, Hyperlipidemia Flashcards

1
Q

list bile acid binding resins

A

Cholestyramine
colestipol
colesevelam

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2
Q

bile acid binding resins MOA

A
  • bind bile acids and prevent intestinal reabsorption

- decreases bile acids, which increases uptake of LDL (lower LDL decreases plasma cholesterol)

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3
Q

bile acid binding resins indications/therapeutic effects

A
  • effective WHEN LDL IS ELEVATED
  • NO EFFECT in HOMOZYGOUS familial hypercholesterolemia (no functional LDL receptors)
  • NO EFFECT HYPERTRIGLYCERIDEMIA (may increase VLDL)
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4
Q

bile acid binding resins pharmacokinetics

A
  • not absorbed

- take w/ meals (need to produce bile for effect)

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5
Q

bile acid binding resins adverse effects

A
  • safe!
  • CONSTIPATION, BLOATING
  • steatorrhea w/ cholestasis
  • rare = gallstones (esp obese pts)
  • rare = HYPERPROTHROMBINEMIA due to Vit K malabsorption
  • can impair absorption of certain drugs (digitalis, thiazides, statins, tetracycline, thyroxine, aspirin)
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6
Q

niacin MOA

A
  • lowers VLDL/LDL by INHIBITING VLDL SECRETION

- inhibits hepatic cholesterologenesis

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7
Q

niacin indications/therapeutic effects

A
  • increased clearance LDL pathway
  • INCREASED LEVELS HDL (most effective agent)
  • most effective for hypercholesterolemia
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8
Q

niacin pharmacokinetics

A
  • oral
  • renal excretion
  • doses = gram range (vitamins = mg)
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9
Q

niacin adverse effects

A
  • mild effects
  • cutaneous VASODILATION, warm sensation, pruritis, dry skin
  • NAUSEA & ABDOMINAL DISCOMFORT
  • IMPAIRS GLUCOSE INTOLERANCE
  • hyperuricemia
  • rarely, but possible HEPATOTOXICITY
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10
Q

what are two hallmark effects of niacin?

A

VASODILATION & IMPAIRS GLUCOSE INTOLERANCE

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11
Q

list of statins (HMG CoA Reductase Inhibitors

A 
Atorvastatin
fluvastatin
lovastatin
pravastatin
simvastatin
rosuvastatin
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12
Q

statins MOA

A
  • active forms = analogs of HMG CoA reductase

- reduce plasma LDL by INHIBITING REDUCTASE TO INCREASE HIGH AFFINITY LDL RECEPTOR

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13
Q

statins indications/therapeutic effects

A
  • DECREASE LDL - MOST EFFECTIVE DRUG!
  • decr plasma triglycerides
  • increase HDL
  • DECREASE CRP in pts w/ CHD
  • enhance production of NO
  • INCREASE PLAQUE STABILITY
  • DECREASE LIPOPROTEIN OXIDATION
  • DECREASE PLATELET AGGREGATION
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14
Q

when are statins most effective?

A

when LDL IS ELEVATED!

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15
Q

statins pharmacokinetics

A
  • high first pass
  • liver metabolism
  • GI excretion
  • GIVE IN THE EVENING (diurnal pattern cholesterol synthesis)
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16
Q

which two statins are inactive?

A

LOVASTATIN & SIMVASTATIN - must be hydrolyzed to active form

17
Q

statins - adverse effects

A
  • INCREASED levels serum aminotransferase (reversible)
  • LIVER DAMAGE in alcoholics, pts w/ liver probs
  • SERUM Cr KINASE ACTIVITY - associated w/ phys activity
  • Rhabdomyolysis
18
Q

statins contraindications/precautions

A
  • contraindicated in PREGNANCY
  • ACTIVE HEPATIC DZ
  • p450 inhibitors (increase statin concentration)
  • p450 activators (decrease plasma concentrations of statins
19
Q

which fibrate inhibits metabolism of statins?

A

Gemfibrozil

20
Q

fibrates MOA

A

PPAR alpha ligand - upregulates LPL and other genes involved in fatty acid oxidation

21
Q

list fibrates

A

gemfibrizol
fenofibrate
fenofibric acid

22
Q

fibrates indications/therapeutic effects

A
  • increase LPL –> incr catabolism VLDL
  • DECREASE TRIGLYCERIDES by lowering VLDL conc
  • decrease cholesterol by inhibiting hepatic cholesterologenesis
23
Q

fibrates adverse effects

A
  • skin rashes, GI symptoms, arrhythmias, hypokalemia, myopathy
  • incr blood aminotransferases, alkaline phosphatase
  • INCREASED INCIDENCE CHOLELITHIASIS OR GALLSTONES = HALLMARK EFFECT
  • potentiate effect warfarin
  • may increase LDL
24
Q

Ezetimibe MOA

A

selectively BLOCKS INTESTINAL ABSORPTION of cholesterol and phytosterols

25
Q

Ezetimibe indications/therapeutic effects

A
  • moderate decr LDL
26
Q

with which drug would you combine Ezetimibe to get synergistic effects?

A

STATIN!

- can produce reductions 25% beyond if using drug alone

27
Q

Ezetimibe pharmacokinetics

A
  • metabolized by liver

- enterohepatically recirculated

28
Q

Ezetimibe adverse effects

A

NONE!

29
Q

drug used for high cholesterol?

A

cholestyramine
cholestipol
ezetimibe

30
Q

drug used for high triglycerides?

A

gemfibrozil

31
Q

drug used for high cholesterol AND triglycerides?

A

statins + niacin, ezetimibe

KG - Pharmacology 2 (10 decks)

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