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Pharm > hypolipidemic drugs > Flashcards

hypolipidemic drugs Flashcards

1
Q

LDL

A

low density lipoproteins

  • transports cholesterol from liver to the blood stream
  • aka “bad cholesterol”
  • high levels in the blood are associated with an increased risk of atherosclerosis and coronary artery disease
  • normal 100 start treatment
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2
Q

HDL

A

High density lipoprotein
- “good cholesterol”
- HDLs acquire cholesterol from peripheral tissue i.e. arterial walls
- low HDL levels = risk factor for cardiovascular disease
-

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3
Q

LP(a) Lipoprotein

A

formed from a LDL-like moiety and LP(a) protein

  • highly homologous to plasminogen but lacks the ability to be activated by tPA
  • repair of vessels
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4
Q

competitive inhibition

A

has same Vmax different Km

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5
Q

noncompetitive inhibition

A

has same Km different Vmax (squashed graph)

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6
Q

Cholesterol metabolism

A

?

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7
Q

statins

A 
simvastatin
fluvastatin
atorvastatin
pravastatin
lovastatin
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8
Q

statins use and MOA

A
  • lower LDL levels (by almost 60% ; TG down 40%)
    MOA: competitive inhibitors of HMC-CoA reductase
  • leads to an induction of high affinity LDL receptors–> thus lowering serum LDL levels
  • increasing LDL receptors is the important part of the mechanism!!

clinically all statins have the same efficacy

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9
Q

statin side effects

A
  1. elevations of serum aminotransferase and hepatotoxicity (increase in liver enzymes ALT/AST)
  2. myositis (muscle pain), marked by elevated creatine kinase activity
    - if drug is not discontinued, rhabdomyolysis may occur–> producing myoglobinemia –> may lead to acute renal failure

*always monitor liver enzymes and creatine kinase when giving statins!

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10
Q

statin drug interactions

A
  • drugs that may inhibit CYP enzymes (erythromycin, ketoconazole) will increase the plasma concentrations of statins
  • concomitant use of amiodarone (class 3) or verapamil (class 4) or fibrates causes an increased risk of myopathy
  • statin + BABR/ezetimibe (which works better in conjunction with statins)
  • never use statins + fibrate bc toxicity! (myositis)
  • never combine statins + niacin bc toxicity! (myositis)
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11
Q

niacin

A

aka nicotinic acid

when used in high doses

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12
Q

Niacin MOA and use

A
  • water soluble VB3 which is converted in the body into nicotinamide adenine dinucleotide (NAD) but in high [ ]
  • decreases plasma LDL levels and VLDL **
  • markledly decreases plasma TG levels
    mechanism primarily involves the inhibition of VLDL synthesis and esterification of Fatty Acids in the liver
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13
Q

Niacin Side Effects

A
  • flushing (PGE2–> vasodilation–> flushing…..treated by aspirin or other NSAIDS)
  • diarrhea
  • hyperuricemia (can precipitate gout)
  • hyperglycemia (so statins are preferred in diabetics)
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14
Q

Fabric Acid Derivatives and use

A

Gemfibrozil
Fenofibrate

Use: Increases the activity of LPL and Reduces VLDL levels, especially TG!!!

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15
Q

Fenofibrate MOA and use and A/E and drug interactions

A

MOA: agonist at peroxisome proliferator-activated receptor alpha (PPARalpha) which is a nuclear receptor

  • PPARalpha affects genes necessary for carb and fat metabolism –> activation –> increase plasma HDL and decrease plasma TG
  • increases the activity of lipoprotein lipase!!
  • reduces VLDL levels esp lowers triglycerides

Use: typically used to treat hypertriglyceridemias
(preferred over statins)

A/E:

  • GI symptoms
  • myopathy (increased with given with statins)
  • risk of cholesterol gallstones

Major Drug Interactions:
- fabric acid derivatives can displace other albumin bound drugs like warfarin–> thereby increase the anticoagulant effect of warfarin and sulfonyl ureas

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16
Q

Bile Acid Binding Resins and use

A

Colestipol
Cholestyramine
Colesevelam

Use: DECREASE LDL levels and INCREASE HDL

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17
Q

drugs that may inhibit CYP enzymes

A 
erythromycin (macrolide antibiotics)
ketoconazole
cimetidine
SSRIs
fluoroquinolones
HIV protease inhibitors
grapefruit juice
18
Q

CYP450 enzyme INDUCERS

A 
rifampicin
barbiturates
phenytoin
carbamazepine
glucocorticoids
chronic alcohol administration
19
Q

Gemfibrozil MOA and use and A/E and drug interactions

A

MOA: agonist at peroxisome proliferator-activated receptor alpha (PPARalpha) which is a nuclear receptor

  • PPARalpha affects genes necessary for carb and fat metabolism –> activation –> increase plasma HDL and decrease plasma TG
  • increases the activity of lipoprotein lipase!!
  • reduces VLDL levels esp lowers triglycerides

Use: typically used to treat hypertriglyceridemias
(preferred over statins)

A/E:

  • GI symptoms
  • myopathy (increased with given with statins)
  • risk of cholesterol gallstones

Major Drug Interactions:
- fabric acid derivatives can displace other albumin bound drugs like warfarin–> thereby increase the anticoagulant effect of warfarin and sulfonyl ureas

20
Q

Colestipol: use, MOA, A/E and drug interactions

A

**Decreases LDL levels and increases HDL

MOA:

  • bind bile acids in the intestine forming a complex that is excreted in the feces
  • this leads to an increased oxidation of cholesterol to bile acids in the liver
  • this results in an increase in the number of low-density lipoprotein receptors –> thereby decreasing serum LDL levels

Side Effects:

  • constipation
  • bad taste (may lead to compliance issues)
  • deficiency of fat-soluble vitamins (as these resins bind bile acids they may interfere with normal fit digestion and absorption and thus may prevent absorption of fat soluble vitamin such as A, D, E and K)
  • side effects can even be seen at therapeutic doses compared to toxicities which are seen at higher than therapeutic doses*

Drug Interactions:
- may delay or reduce the absorption of other concomitant oral medications i.e. digitalis, warfarin

21
Q

Side Effects vs Toxicities

A
  • side effects can even be seen at therapeutic doses compared to toxicities which are seen at higher than therapeutic doses*
22
Q

patient has flushing. what drug did you give the patient and how do you treat it

A

the patient was given Niacin to lower LDL and VLDL

you treat this with aspirin or other NSAIDs

23
Q

cholestyramine: use, MOA, A/E and drug interactions

A

**Decreases LDL levels and increases HDL

MOA:

  • bind bile acids in the intestine forming a complex that is excreted in the feces
  • this leads to an increased oxidation of cholesterol to bile acids in the liver
  • this results in an increase in the number of low-density lipoprotein receptors –> thereby decreasing serum LDL levels

Side Effects:

  • constipation
  • bad taste (may lead to compliance issues)
  • deficiency of fat-soluble vitamins (as these resins bind bile acids they may interfere with normal fit digestion and absorption and thus may prevent absorption of fat soluble vitamin such as A, D, E and K)
  • side effects can even be seen at therapeutic doses compared to toxicities which are seen at higher than therapeutic doses*

Drug Interactions:
- may delay or reduce the absorption of other concomitant oral medications i.e. digitalis, warfarin

24
Q

Ezetimibe: use & toxicity

A

(zetia*)

  • Prodrug
  • lowers serum LDL and TG*
  • decreases GI absorption of cholesterol
  • used alone reduces LDL by 18% but MUCH more effective when given with statins (72%)

Toxicity: well-tolerated, MC side effect = diarrhea, abdominal pain

25
Q

MOA = decrease synthesis of VLDL

name that drug!

A

Niacin

26
Q

MOA = decrease cholesterol synthesis and increase LDL receptors

name that drug!

A

statins

27
Q

MOA = interrupts enterohepatic circulation of bile acids and increases synthesis of bile acids and LDL receptors

name that drug!

A

Bile acid binding resins

Colestipol
Cholestyramine
colesevelam

28
Q

colesevelam: use, MOA, A/E and drug interactions

A

**Decreases LDL levels and increases HDL

MOA:

  • bind bile acids in the intestine forming a complex that is excreted in the feces
  • this leads to an increased oxidation of cholesterol to bile acids in the liver
  • this results in an increase in the number of low-density lipoprotein receptors –> thereby decreasing serum LDL levels

Side Effects:

  • constipation
  • bad taste (may lead to compliance issues)
  • deficiency of fat-soluble vitamins (as these resins bind bile acids they may interfere with normal fit digestion and absorption and thus may prevent absorption of fat soluble vitamin such as A, D, E and K)
  • side effects can even be seen at therapeutic doses compared to toxicities which are seen at higher than therapeutic doses*

Drug Interactions:
- may delay or reduce the absorption of other concomitant oral medications i.e. digitalis, warfarin

29
Q

MOA = increase LPL and TG hydrolysis

name that drug!

A

Fibrates

gemfibrozil
fenofibrate

30
Q

MOA = decrease intestinal absorption of cholesterol

name that drug!

A

Ezetimibe

31
Q

drug causes flushing, diarrhea, hepatic dysfunction, nausea, pruritus and gout

name that drug!

A

niacin

32
Q

drug causes hepatotoxicity and myopathy

name that drug!

A

statins

33
Q

drug causes hepatotoxicity, nausea and myositis

name that drug!

A

Fibrates

gemfibrozil
fenofibrate

34
Q

drug causes GI disturbances

name that drug!

A

exetimibe

35
Q

drug causes constipation, bloating, nausea and fat soluble vitamin deficiency

name that drug!

A

Bile acid binding resins

Colestipol
Cholestyramine
colesevelam

36
Q

during drug treatment with atorvastatin it is important to routinely monitor serum concentrations of

A

alanine and aspartate transaminases and creatine kinase

37
Q

two primary adverse effects HMG CoA inhibitors

A

hepatotoxicity and myopathy

38
Q

dyslipidemia

A

general term associated with high cholesterol and/or high triglyceride (TG) levels in plasma.

39
Q

CYP450 enzyme inducers

A
  • rifampicin
  • barbiturates
  • phenytoin
  • carbamazepine
  • glucocorticoids
  • chronic alcohol use
40
Q

CYP450 enzyme inhibitors

A
  • cimetidine
  • SSRIs
  • ketoconazole
  • macrolide antibiotics
  • fluoroquinolones
  • HIV protease inhibitors
  • grapefruitjuice

Pharm (32 decks)

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