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Pharmacology & Drugs > Cardio-Lipid Disorders > Flashcards

Cardio-Lipid Disorders Flashcards

1
Q

What is the effect of fibrates with anticoagulants

A

Potentiate their effect

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2
Q

What are the adverse effects of the mipomersen

A
  • Injection site reactions
  • flu-like symptoms
  • elevation of the liver enzymes to as high as 3x normal
  • Expensive at 176,000 a year
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3
Q

How is most of the absorbed dose of statins excreted

A

In bile

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4
Q

What are the pharmacokinetics of bile acid sequestrants aka resins

A

Large cationic resins that are insoluble in water

-Completely excreted in feces as it is neither absorbed or altered/metabolized

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5
Q

What is the effect of firbrates on the muscle

A

Myositis, myopathy, rhabdomyolysis

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6
Q

What are the pharmokenetics of NIACIN

A

Converted into nicotinamide adenine dinucleotide (NAD)

  • Extensive first pass, so half life is 60 minutes (2-3 times a day)
  • Distributed to hepatic, renal, and adipose tissue
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7
Q

Which drug class will be ineffective with a patient with familial hypercholesterolemia

A

Statins because they rely on a functions LDL receptor, but that is not the cause in familial hypercholestermia

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8
Q

Which conditions can be exacerbated by niacin use

A

Gout and glucose intolerance

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9
Q

What drug class is colesevelam

A

Bile acid sequestration (resins)

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10
Q

What is the effect of firbrates on the liver

A

Elevated aminotransferases

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11
Q

What is the mechanism of metabolism for simvastatin

A

CYP3A4

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12
Q

What is the result of statins on muscle

A
  • Creatine kinase levels increased
  • Rhabdomyolysis
  • increases myopathy if taken with fibrates
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13
Q

What drug class is Ezetimibe

A

Cholesterol absorption inhibitors

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14
Q

What are the most potent statins

A

Atorvastatin and rosuvastatin

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15
Q

What are the conditions that mipomersen can be used

A

Familial hypercholesterolemia

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16
Q

What are the adverse effects of limitapide

A
  • Substrate and inhibitor of CYP3A4
  • GI symptoms
  • Increased liver aminotransferases levels
  • hepatic fat accumulation
  • Expensive at 250,000 a year
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17
Q

What are the conditions that lomitapide can be used

A

Familial hypercholesterolemia

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18
Q

When is treatment with fibrates very warranted

A

In those with very high VLDL, or those with treatment with viral protease inhibitors (such as HIV treatment)

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19
Q

What is the mechanism of metabolism for atorvastatin

A

CYP3A4

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20
Q

Which drug class has the highest effect on lowing the levels of triglycerides

A

Fibrates

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21
Q

What is the mechanism of action for mipomersen

A

-antisense oligonulceotide that targets and disrupts the ApoB100 mRNA

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22
Q

What is the mechanism of action of NIACIN

A
  • inhibits the lipolysis of TGs in the adipose tissue, which decreases free circulating free fatty acids
  • Decreased FFAs result in decreased VLDL and LDL, increased HDL
  • Fibrinogen levels are decreased and tPA are increased
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23
Q

Why are statins primarily taken at night

A

Most cholesterol synthesis occurs at night

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24
Q

Which statins are more likely to be used when using another drug affecting CYP450s

A
  • Pravastatin

- Pitavastatin

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25
Q

What is the mechanism if action for bile acid sequestrants aka resins

A

1) Because they are positively charged, binds to the negative charged bile acids and increases the excretion (almost tenfold)
2) INcreased bile acid excretion results in the increased conversation of cholesterol to bile acids via 7alpha hydroxylation
3) LDL receptors increase, along with the clearance of LDL from the blood

26
Q

Which of the drug classes has the highest effect on lowering the LDL levels

A

Statins

27
Q

What is an adverse effect seen on the liver as a result of statins

A

Elevated serum liver aminotransferases

28
Q

What is the mechanism of action for fibrates

A
  • Agonist for peroxisome proliferator-activated receptor alpha (PPARalpha), which regulates the DNA for lipoprotein structure and function
  • increases the oxidation of FFA, greatly decreases VLDL and slightly LDL
29
Q

What is the mechanism of metabolism for pitavastatin

A

Limited CYP450 activity

30
Q

What is the result of statins with warfarin

A

Increases the levels of warfarin

31
Q

What is the mechanism of action for PSCK9 monoclonal antibodies (evolocumab and alirocumab)

A

Forms complexed with the PCSK9 and inhibits the catabolism of LDL receptors, so more LDL is cleared from the blood

32
Q

What is the mechanism of metabolism for lovastatin

A

CYP3A4

33
Q

What is the mechanism of metabolism for rosuvastatin

A

CYP2C9

34
Q

What are the pharmacokinetics of ezetimibe

A
  • A cholesterol absorption inhibitor
  • Highly water insoluble,so most is excreted in the feces
  • 22 hour half life
35
Q

Which patients are statins contraindicated in

A
  • Liver failure
  • Pregnancy or lactating
  • skeletal muscle myopathies
36
Q

What drug class is gemifibrozil

A

Fibril acid derivatives (fibrates)

37
Q

What are the contraindications for fibrates

A
  • Pts at risk or with biliary tract diseases (women, obese, Native Americans)
  • Hepatic dysfunction
38
Q

What are the three statins with the longest half life

A

Atorvastatin (14 hrs)
Pitavastatin (12 hrs)
Rosuvastatin (19 hrs)

39
Q

What is the mechanism of action for Statins

A

1) Decreased production of cholesterol via inhibition of HMG-CoA reductase
2) Increased LDL receptors and LDL uptake
3) Decreased blood levels of LDL

40
Q

What are the adverse affects of bile acid sequestrants aka resins on the GI system

A
  • Constipations, nausea, and flatulence most common
  • Impaired absorption of fat soluble vitamins (A,D,E,K)
  • Impaired absorption of many common drugs
41
Q

What are the contraindications for using bile acid sequestrants aka resins

A

Pts with:

  • Diverticulitis
  • Preexisting bowel disease
  • cholestasis
42
Q

What drug class is colestipol

A

Bile acid sequestration (resins)

43
Q

What is the mechanism of metabolism for pravastatin

A

Not involved with CYP450

44
Q

What drug class is cholestryamine

A

Bile acid sequestration (resins)

45
Q

What is the result of LDL receptors levels, LDL serum levels, and activity of the HMG-CoA reductase activity as a result of administration of bile acid sequestrants aka resins

A
  • Increased LDL receptors and LDL clearance

- Increased HMG-CoA activity

46
Q

What ar ethe some of the drugs that are impacted by bile acid sequestrants aka resins

A
  • tetracycline
  • Phenobarbital
  • Digoxin
  • warfarin
  • Pravastatin, fluvastatin
  • Aspirin
  • Thiazides
47
Q

What is the mechanism of metabolism for fluvastatin

A

CYP2C9

48
Q

What are some secondary benefits of statins

A
  • Plaque stabilization
  • Improved coronary endothelial function
  • Inhibition of thrombus formation
  • Anti-inflammatory effects
49
Q

What is the mechanism of action of Exetimibe

A
  • Inhibits the intestinal absorption of cholesterol and the plant sterol, phytosterol via inhibiting the transport protein NPC1L1.
  • Works even if there is dietary cholesterol by inhibiting the uptake of cholesterol from the bile that is excreted
50
Q

What are the serum level changes with NIACIN (aka nicitinic acid, vitamin B3)

A

Decreases TGs, LDL

Increases HDL

51
Q

In a patient taking bile acid sequestrants aka resins, when should other drugs be taken

A

-at least 1 hour before or 2 hours after

52
Q

What drug class is fenofibrate

A

Fibril acid derivatives (fibrates)

53
Q

Which statins are not taken at night like the others

A
  • Atorvastatin
  • pitavastatin
  • rosuvastatin
54
Q

What are the contraindication so NAICIN

A
  • DM patients and can induce insulin resistance

- Liver or peptic ulcer disease

55
Q

Which of the statin drug in contrast to others is almost completely absorbed when taken orally

A

Fluvastatin

56
Q

What are the adverse effects of NIACIN

A
  • intense cutaneous flush when first started or dose is increased
  • rash, dry skin or mucous membranes
57
Q

What is a combination that is commonly used with bile acid sequestrants aka resins and what is the reasoning

A

Statins, because the resins increase the activity of HMG-CoA reductase activity, so statins can help limit the amount of new cholesterol synthesized

58
Q

What situations are PSCK9 monoclonal antibodies (evolocumab and alirocumab) used

A

Familial hypercholesterolemia that is not responsive to oral therapy

59
Q

What is the mechanism of action for lomitapide

A

1) binds to and inhibits the triglyceride transport protein (MTP)of the ER
2) Inhibition leads to Prevention of the Apo-B
3) Decreases the levels of LDL, VLDL

60
Q

Which drug class has the highest effect on raising the levels of HDL

A

Niacin

61
Q

What are the adverse effects of fibrates on the GI

A

Increased risk of cholelithiasis (increased bile cholesterol level)

Pharmacology & Drugs (43 decks)

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