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Maddy - CPR I - some pharm > Drugs for Lipid Disorders > Flashcards

Drugs for Lipid Disorders Flashcards

1
Q

Bile acid sequestrants (resins)

  • effect on LDL
  • effect on HDL
  • effect on TGs
A
  • big decrease LDL
  • slight increase HDL
  • minimal effect on TG
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2
Q

most effective drug for increasing HDL

A

niacin

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3
Q

what patients should avoid niacin

A

those with:

  • hepatic dz
  • active peptic ulcer
  • DM patients
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4
Q

adverse rxn for statins on muscle

A
  • creatinine kinase activity may increase
  • rhabdomyolosis
  • myopathy
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5
Q

why should you avoid administration of ezetimibe and bile acid sequestrants (resins)

A

due to impaired ezetimibe absorption

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6
Q

MOA of PCSK9

A

antibodies bind to PCSK9 and inhibit LDL receptor metabolism

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7
Q

what do resins treat

A

pts with primary hypercholesteremia

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8
Q

what would you give a patient with hypertriglyceridemia, dysbetalipoproteinemia, and hypertriglyceridemia that results from treatment with viral protease inhibitors (saquinavir, indinavir, or nelfinavir)

A

fibrates

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9
Q

MOA of Lomitapide

A

directly binds to and inhibits microsomal triglyceride transfer protein (MTP) which will prevent the assembly of apo-B containing lipoproteins –> reduction in chylomicrons and VLDL and LDL

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10
Q

what is the effect of niacin on fibrinogen and tissue plasminogen

A
  • fibrinogen levels are reduced

- tissue plasminogen activator levels are increased

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11
Q

adverse rxn with Lomitapide

A
  • inhibits CYP3A4 –> interactions with a number of drugs
  • GI symptoms
  • increase liver aminotransferase levels
  • hepatic fat accumulation
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12
Q

what are the two statins NOT metabolized by CYP450

A

Pitavastatin

Pravastatin

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13
Q

adverse rxn to Mipomersen

A
  • injection site reactions
  • flu like sx
  • HA
  • elevation of liver enzymes
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14
Q

MOA of ezetimibe

A

selectively inhibits intestinal absorption of cholesterol and phytosterols

  • lowers LDL by 18%
  • lowers TG by 6%
  • raising HDL by 1.3%
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15
Q

adverse rxn for statins on liver

A

elevation of serum aminotransferase activity

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16
Q

MOA of niacin

A

inhibits lipolysis of triglycerides in adipose tissue which reduces circulating free fatty acids

  • less VLDL and LDL
  • catabolism of HDL decreased
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17
Q

MOA of statins

A

inhibit HMG-CoA reductase, the rate limiting enzyme in cholesterol synthesis, increases surface LDL receptors which reduces circulating LDL levels

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18
Q

liver adverse rxn from fibrates

A

increased serum transaminases

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19
Q

most effective drug for lowering LDL

A

statins

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20
Q

therapeutic uses of ezetimibe

A
  • various causes of elevated cholesterol

- mixed hyperlipidemia

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21
Q

MOA of bile acid sequestrants (resins)

A

positively charged compounds bind to negatively charged bile acids (cholesterol) and increase bile acid excretion up to tenfold
- enhances LDL clearance and lowers levels

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22
Q

major effect of fibrates

A
  • increased oxidation of fatty acids
  • increased lipolysis of TG via lipoprotein lipase
  • intracellular lipolysis in adipose tissue is decreased
  • VLDL decreased
  • LDL decreased
  • HDL increased
23
Q

pharmacokinetics of niacin

A

niacin –> nicotinamide –> nicotinamide adenine dinucleutide (NAD)

24
Q

what dz does Mipomersen treat

A

familial hypercholestermia

25
Q

adverse rxn to resins

A
  • constipation, nausea, flatulence
  • impaired absorption of vitamins D, E, A, K
  • impaired absorption of tetracycline, phenobarbitol, digoxin, warfarin, parvastatin, fluvastatin, aspirin, and thiazide diuretics
26
Q

MOA of Mipomersen

A

targets apolipoprotein B-100 mRNA, resulting in decrease in the levels of apolipoprotein B (apo B), LDL, and total cholesterol

27
Q

weakest statin mentioned in this lecture

A

fluvastatin

28
Q

pitavastatin is metabolized by

A

undergoes limited CYP450 biotransformation

29
Q

fluvastatin and rosuvastatin are metabolized primary by

A

CYP2C9

30
Q

statins are NOT recommended for what patients

A
  • pregnant women
  • lactating women
  • children with homozygous familial hypercholesteremia
31
Q

adverse rxn to ezetimibe

A

none have been reported

32
Q

MOA of fibrates (gemfibrozil and fenofibrate)

A

agonist for peroxisome proliferator-activated receptor alpha (PPARa) which binds to DNA –> regulates the expression of genes encoding proteins involved in lipoprotein structure and function

33
Q

how does alcohol affect VLDL

A

causes hypertriglyceridemia by increasing hepatic secretions of VLDL

34
Q

Fibrates

  • effect on LDL
  • effect on HDL
  • effect on TGs
A
  • slight decrease LDL
  • bigger increase HDL
  • great decrease TG
35
Q

what patients should avoid taking fibrates

A
  • pts with biliary tree dz
  • hepatic or renal dysfunction
  • pregnant and lactating women
36
Q

most potent statins mentioned in this lecture

A

atorvastatin and rosuvastatin

37
Q

why are statins included in the management of familial hypercholesteremia when they rely on function LDL receptors to work? (FH doesn’t have functional LDL receptors)

A

statins still improve coronary endothelial function, inhibit platelet thrombus formation, and have anti-inflammatory effects

38
Q

what dz does Lomitapide treat

A

familial hypercholesteremia

39
Q

Statins

  • effect on LDL
  • effect on HDL
  • effect on TGs
A
  • greatly decrease LDL
  • increase HDL
  • decrease TG
40
Q

why is it a good idea to pair resins with statins?

A

resins enhance LDL clearance but also upregulate HMG-CoA, so by combining with a statin you block the HMG-CoA and just decrease LDL

41
Q

adverse rxn to niacin

A
  • intense cutaneous flush with uncomfortable feeling of warmth
  • pruritus
  • rashes
  • dry skin or mucous membranes
  • acanthosis nigricans
42
Q

risk of prescribe fibrates to a pt on anticoagulants

A

fibrates may potentiate the effects of anticoagulants

43
Q

GI adverse rxn from fibrates

A
  • mild GI disturbances

- increased risk of cholelithiasis

44
Q

muscle adverse rxn from fibrates

A
  • myositis can occur (muscle weakness and tenderness)
  • myopathy
  • rhabdomyolysis
45
Q

what dz does PCSK9 treat

A

familial hypercholesteremia

46
Q

most effective drug for decrease TG

A

fibrates

47
Q

Niacin

  • effect on LDL
  • effect on HDL
  • effect on TGs
A
  • decrease LDL
  • great increase HDL
  • big decrease TGs
48
Q

what pts should not take resins

A

those with:

  • diverticulitis
  • preexisting bowel dz
  • cholestasis
49
Q

Cholesterol absorption inhibitor

  • effect on LDL
  • effect on HDL
  • effect on TGs
A
  • slight decrease LDL
  • slight increase HDL
  • slight decrease TG
50
Q

adverse rxn for statins on pts taking warfarin

A

statins increase warfarin levels

51
Q

how does fat, sucrose, and fructose affect VLDL

A

increase it

52
Q

best tolerated drug for treating hyperlipidemia

A

statins

53
Q

lovastatin, simvastatin, atorvastatin are metabolized primarily by

A

CYP3A4

Maddy - CPR I - some pharm (25 decks)

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