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?

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
statins drug interactions
grapefruit juice and verapamil increase serum statin [] because they inhibit CYP3A (which breaks statins down)
26
what two statins are not broken down by CYP3A (use different paths)
pravastatin and fluvastatin
27
which statin is least potent (only 3% reaches circulation as active drug) - begins as inactive drug
lovastatin
28
atorvastatin
lipitor active drug AS GIVEN 2nd MOST EFFECTIVE STATIN at reducing LDL cholesterol and TG
29
which statin is most effective at reducing LDL cholesterol and TG? 2nd?
1- rosuvastatin | 2-atorvastatin (lipitor)
30
ALL STATINS when in high doses can cause...
rhabdomyolysis
31
what type of hypolipidemic drug is not recomended for postmonopausal women? why?
estrogen replacement therapy | it increases HDL and decreases LDL BUT it causes an increased risk of heart disease and breast cancer
32
what is ezetimibe
a cholesterol absorption inhibitor | --> works on the brush border of the gut wall and prevents cholesterol absorption through villi
33
ezetimibe + ______
a statin --> LDL is lowered extra 25%
34
although ezetimibe lowers LDL, it does not...
prevent or reduce plaque build-up in arteries | or reduce coronary events/ischemic strokes
35
three types of agents that predominantly lower TG?
niacin (nicotinic acid) fibric acid derivatives fish oil
36
how does niacin work to lower TG?
decrease in hepatic synthesis of VLDL in response, IDL and LDL levels decrease as well -unknown mech: increases HDL
37
side effects of niacin?
flushing --> can be reduced by aspirin or laropiprant
38
fenofibrate and gemfibrozil
fibric acid derivatives - lower TG
39
how do fibric acid derivatives work?
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
gemfibrozil vs fenofibrate
fenofibrate isbetter in increasing HDL; reduces incidience of MI or CHD
41
side effects of fibric acid derivatives
rash, gallstones in obese people, | GI issues, rhabdomyolysis when gemfibrozil is + statin
42
gemfibrozil + statin =
NO! | rhabdomyolysis
43
fibric acid derivatives (gemfibrozil and fenofibrate) potentiate what?
actions of coumarin and indanedione anticoagulants by displacing them from bidning sites on albumin
44
FIsh oil contains...effects...
omega 3 polyunsaturated FA | decrease TG by suppressing VLDL production and increases HDL
45
neomycin
antimicrobial agent of aminoglycoside family | -when combined with niacin, helps to lower cholesterol levels
46
neomycin + niacin =
complementary --> lower cholesterol levels
47
IF one drug does not help lower blood lipids enough, three combination options:
1. statin + resin 2. niacin + resin (1 and 2 lower LDL-C) 3. gemfibrozil + fish oil (lower TG)
48
combination to treat chylomicronemia(too much chylomicrons and VLDL)
niacin and fibrate
49
combo for familial hypertriglyceridemia (high chylomicrons and VLDL)
niacin and fibrate
50
combo to treat familial combined hyperlipoproteinemia(high VLDL and LDL)
niacin and statin or resin
51
familial hypercholesterolemia
(homozygous is worse) hetero - statin+resin homo - niacin + atorvostatin or rosuvastatin
52
combo for lp(a) hyperlipoproteinemia (high Lp(a)
niacin and neomycin