hypolipidemic drugs Flashcards

1
Q

Cholestin and Evolve

A

dietary supplements that inhibit HMGCoA reductase

almost as effective as lovastatin

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2
Q

HMG coa reductase

A

enzyme that controls the rate of cholesterol production

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3
Q

effects of omega 3 FA?

A

like fish oil
decrease LDL and TG
increase HDL

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4
Q

effects of omega 6 FA?

A

like veg oil
decrease LDL
BUT increases TG and decreases HDL

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5
Q

how does diet increase VLDL synthesis and secretion

A

excess caloric intake and not necessarily fat

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6
Q

risk factors for CHD

A
age
low HDL
high cholesterol
high BP
cigarettes
obesity, diabetes
history of CHD/sudden death
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7
Q

when should dietary aid be passed and go right to drugs?

A

if patient has 2 or more risk factors OR history of CHD death OR just diabetes

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8
Q

three bile acid binding resins

and what do they do?

A

cholestyramine
colestipol
colesevelam
–> lower cholesterol(especially LDL)

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9
Q

which bile acid binding resin is best to lower LDL/cholesterol?

A

colesevelam (less GI side effects and less interference with other drugs)

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10
Q

bile acid binding resins are used to treat:

A
  • combined hyperlipidemia

- heterozygous familial hypercholesterolemia

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11
Q

mechanism of cholesyramine/colestipol/colesevelam

A

bile acid binding resin

  • > binds bile acids in intestines and inhibits its reabsorption
  • cholesterol is the precursor to bile acid so more cholesterol is channeled to bile
  • decrease in serum cholesterol, increase in LDL receptors, clearance of lipoproteins
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12
Q

adverse effects of bile acid binding resins

A

reduced intrahepatic cholesterol can cause secondary cholesterol production –> constipation and bloating(fix with fiber)
–resins can bind other drugs(warfarin/anticoagulants, vitamin K, B blockers)

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13
Q

when should bile acid resins be taken?

A

with or just before meals

–any other drugs should be taken 2 hrs before the resins or 4 hrs after to prevent resin binding

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14
Q

are resins safe to use in pregnancy?

A

yes

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15
Q

what type of drug are bileacidbinding resins usually combined with?

A

HMGcoareductase (like lovastatin)

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16
Q

HMGcoa reductase inhibitors

A

any drugs that ends in -statin

lovastatin, simvastatin

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17
Q

what to use HMGcoareductase inhibitors for?

A

use statins for familial hypercholersterolemia, and combined hyperlipidemia

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18
Q

what do statins do?

A
they competitively inhibit HMGcoa reductase, decreasing cholesterol synthesis
causing upregulation(more ) of LDL receptors --> clearance of apoB and apoE lipoproteins (IDL, LDL, VLDL)
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19
Q

which statins reduce TG up to 40%?

A

simvastatin and atorvastatin

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20
Q

why are statins/reductase inhibitors usually given at night?

A

due to the diurnal pattern of cholesterol biosynthesis

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21
Q

side effects of statins

A

usually safe

-high doses plus fibric acid derivative = rhabdomyolysis and renal failure

22
Q

can pregnant women use statins?

A

NEVER

23
Q

statins and normal levels of blood cholesterol…

A

can reduce risk of heart attack and stroke

24
Q

statins are excreted…

A

by CYP3A in the liver

25
Q

statins drug interactions

A

grapefruit juice and verapamil increase serum statin [] because they inhibit CYP3A (which breaks statins down)

26
Q

what two statins are not broken down by CYP3A (use different paths)

A

pravastatin and fluvastatin

27
Q

which statin is least potent (only 3% reaches circulation as active drug) - begins as inactive drug

A

lovastatin

28
Q

atorvastatin

A

lipitor
active drug AS GIVEN
2nd MOST EFFECTIVE STATIN at reducing LDL cholesterol and TG

29
Q

which statin is most effective at reducing LDL cholesterol and TG? 2nd?

A

1- rosuvastatin

2-atorvastatin (lipitor)

30
Q

ALL STATINS when in high doses can cause…

A

rhabdomyolysis

31
Q

what type of hypolipidemic drug is not recomended for postmonopausal women? why?

A

estrogen replacement therapy

it increases HDL and decreases LDL BUT it causes an increased risk of heart disease and breast cancer

32
Q

what is ezetimibe

A

a cholesterol absorption inhibitor

–> works on the brush border of the gut wall and prevents cholesterol absorption through villi

33
Q

ezetimibe + ______

A

a statin –> LDL is lowered extra 25%

34
Q

although ezetimibe lowers LDL, it does not…

A

prevent or reduce plaque build-up in arteries

or reduce coronary events/ischemic strokes

35
Q

three types of agents that predominantly lower TG?

A

niacin (nicotinic acid)
fibric acid derivatives
fish oil

36
Q

how does niacin work to lower TG?

A

decrease in hepatic synthesis of VLDL
in response, IDL and LDL levels decrease as well
-unknown mech: increases HDL

37
Q

side effects of niacin?

A

flushing –> can be reduced by aspirin or laropiprant

38
Q

fenofibrate and gemfibrozil

A

fibric acid derivatives - lower TG

39
Q

how do fibric acid derivatives work?

A

bind to PPAR alpha (peroxisome proliferator activated receptor alpha) in liver and regulates gene transcription which:
-increases lipoprotein lipase activity, decreased VLDL synthesis, increased HDL chol.

40
Q

gemfibrozil vs fenofibrate

A

fenofibrate isbetter in increasing HDL; reduces incidience of MI or CHD

41
Q

side effects of fibric acid derivatives

A

rash, gallstones in obese people,

GI issues, rhabdomyolysis when gemfibrozil is + statin

42
Q

gemfibrozil + statin =

A

NO!

rhabdomyolysis

43
Q

fibric acid derivatives (gemfibrozil and fenofibrate) potentiate what?

A

actions of coumarin and indanedione anticoagulants by displacing them from bidning sites on albumin

44
Q

FIsh oil contains…effects…

A

omega 3 polyunsaturated FA

decrease TG by suppressing VLDL production and increases HDL

45
Q

neomycin

A

antimicrobial agent of aminoglycoside family

-when combined with niacin, helps to lower cholesterol levels

46
Q

neomycin + niacin =

A

complementary –> lower cholesterol levels

47
Q

IF one drug does not help lower blood lipids enough, three combination options:

A
  1. statin + resin
  2. niacin + resin
    (1 and 2 lower LDL-C)
  3. gemfibrozil + fish oil (lower TG)
48
Q

combination to treat chylomicronemia(too much chylomicrons and VLDL)

A

niacin and fibrate

49
Q

combo for familial hypertriglyceridemia (high chylomicrons and VLDL)

A

niacin and fibrate

50
Q

combo to treat familial combined hyperlipoproteinemia(high VLDL and LDL)

A

niacin and statin or resin

51
Q

familial hypercholesterolemia

A

(homozygous is worse)
hetero - statin+resin
homo - niacin + atorvostatin or rosuvastatin

52
Q

combo for lp(a) hyperlipoproteinemia (high Lp(a)

A

niacin and neomycin