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MED233 Cardiovascular > Drugs for Lipid Disorders > Flashcards

Drugs for Lipid Disorders Flashcards

1
Q

Hyperlipoproteinemia defintion

A

Excess of lipoproteins in blood due to disorder in metabolism (acquired or familial).

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2
Q 
Hyperlipidemia definition
What class is effective at lowering all types of this?
A

Elevated concentration of any/all lipids in plasma.
Includes hyperTG, hypercholesterolemia.
Statins. (Resins for Type IIa and IIb; Ezetimibe for mixed)

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3
Q

Chylomicron - function

A

Formed in intestinal mucosa. Tranports TG to adipose/liver.

Degraded in caps of muscle and adipose tissue.

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4
Q

HDL

A

Transports cholesterol from tissues to liver for excretion in bile.
Synthesized by liver.

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5
Q

LPL

A

Lipoprotein lipase.
Located on inner surface of cap endothelial cells of muscle and adipose tissue.
Function - Hydrolzes TGs in chylomicron and VLDL&raquo_space; forms FFA+glycerol in adipose

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6
Q

Tx for Primary hypertriglyceridemias

A

Fibrates

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7
Q

Tx for Primary hypercholesterolemias

A

Niacin, statins, resins, Cholesterol Absorption Inhibitors

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8
Q

What two lipoprotein disorders will always require drug therapy?

A

Familial hypercholesterolemia and familial combined hyperlipidemia

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9
Q

What three things can result in HDL deficiency?

A

1) Tangier Disease
2) LCAT deficiency
3) Familial hypoalphalipoproteinemia

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10
Q

What are the three things that are the principle factors for increasing TGs?

A

Fat, alcohol, excess calories

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11
Q

What are the three things that are the principle factors for increasing LDL?

A

Cholesterol, saturated fat, trans fat

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12
Q

When would a child with familial hypercholesterolemia or familial combined hyperlipidemia initiate drug therapy? And what drug?

A

Age 7 or 8 after myelination of CNS is complete. Use a resin or statin.

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13
Q

What is the most effective class for reducing LDL levels? By how much?

A

Statins

reduce LDL by 20-55%

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14
Q

Statin MOA (3) and results of each.

A

1) Inhibit HMG-CoA reductase (cholest precursor). Results in decreased concentration of cholesterol within the cell.
2) Low intracellular cholesterol&raquo_space; increased LDL receptor synthesis AND decreased VLDL secretion
3) **Increased LDL receptors = promotes LDL reuptake from cell

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15
Q

Which two stains have the longest half lives?

A

Atorvastatin (14hrs)

Rosuvastatin (19hrs)

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16
Q

Primary method of metabolism of statins. Which one is not metab by CYP450s?

A 
CYPs
CYP3A4 - lovastatin, simvastatin, atorvastatin
CYP2C9 - fluvastatin and rosuvastatin
CYP450 - pitavastatin
Not mebatolized by CYP450s - pravastatin
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17
Q

Therapeutic uses (2)

A

1) In all hyperlipidemias - lower plasma cholest levels

2) Reduce LDL levels - Can be used alone or with resins, niacin, or ezetimibe.

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18
Q

Potency of statins

A

(Atorva = Rosuva) > Simva > (Pitava = Lova = Prava) > Fluva

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19
Q

What time of day should statins be taken?

A

Evening - because cholesterol is synthesized at night.

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20
Q

When are statins contraindicated (3 groups)?

A

PREGNANT WOMEN, people with liver disease, people with skeletal muscle myopathy (esp those taking antibiotics).

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21
Q

What should not be used in conjunction with statins?

A

Other agents that inhibit or compete with CYP450 - decreases their metabolism.

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22
Q

Statins are limited to use in children with what 2 hypercholesterolemia conditions?

A

Homozygous familial hypercholesterolemia and Heterozygous familial hypercholesterolemia

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23
Q

What are the two statins that penetrate the CNS?

A

Lova and Simva

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24
Q

What two things does niacin (Vitamin B3) most effective at accomplishing?

A

1) Increasing HDL by 30-40% (also lowers LDL and VLDL)

2) Significantly lowering LPL levels

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25
Q

What three tissues is niacin (NAD) distributed to and absorbed?

A

Hepatic, renal, adipose.

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26
Q

Niacin MOA

A

INHBITS LIPOLYSIS of TGs in adipose tissue&raquo_space; less circulating FFA&raquo_space; liver produces less VLDL&raquo_space; LDL levels decrease

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27
Q

When is niacin used in combo with resin or statin?

A

For heterozygous familial hypercholesterolemia, other forms of hypercholesterolemia, and nephrosis (sometimes).

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28
Q

Associate cutaneous flushing and uncomfortable warmth with what class?
What can be taken before niacin to mitigate flushing?

A

Niacin

Take aspirin or ibuprofen before.

29
Q

What are adverse effects of niacin?

A

PURITIS, rash, burning pain
Hepatoxicity
Hyperuricemia=gout
Hyperglycemia=acanthosis nigrans

30
Q

Niacin contraindicated when?

A

Liver disease or active peptic ulcer.

Precaution in DM.

31
Q

Associate acanthosis nigrans with what?

A

Niacin-induced insulin resistance

32
Q

MOA of fibrates and ultimate result.

A

Agonist ligands for nuclear transcription factor receptor PPAR-alpha.
Ultimately INCREASES LPL levels in adipose, DECREASing plasma TG.

???In muscle beds - increases LPL to breakdown more TG in circulation

33
Q

When are fibrates most effectively absorbed?

A

90% absorbed when taken with a meal. Highly bound to serum.

34
Q

Therapeutic uses of fibrin (3).

A

1) Management of hyperTGs where VLDL predominant
2) Dysbetalipoproteinemia
3) HyperTG due to tx with viral protease inhibitors

35
Q

If a person is on HIV therapy, what hyper-emia do you associate it with and what class of tx?

A

hyperTGemia

Fibrin

36
Q

Fibrates contraindicated in people with what conditions?

Indicated in what?

A

Hepatic or renal dysfunction, biliary tract disease.

Indicated in heterozygous mutation in LPL.

37
Q

People taking niacin are predisposed for forming what?

A

Cholesterol Gallstones

38
Q

Adverse effects of fibrates.

A

GI disturbances, lithiasis, cholesterol gallstones, rhabdo

39
Q

What type of drug do fibrates potentiate the actions of?

A

Anticoagulants (coumarin, indanedione anticoags)

40
Q

Which fibrate has a longer half life?

A 
Fenofibrate = 20hrs
Gemibirozil = 1.5 hours
41
Q

Bile acid sequestrants are also called what?

A

Resins

42
Q

MOA of sequesetrants

A

Positive charge, bind to neg charged bile acids, increasing bile secretion and increasing hepatic conversion of cholesterol to bile acids&raquo_space; BLOCK BILE REABSORPTION.

43
Q

Because resins decrease hepatic cholesterol, HMG-CoA reductase is upregulated. So resin effectiveness is greatly increased by combining resins with what?

A

Statins.
Statins block the enhanced cholesterol synthesis that is upregulated by the HMG-CoA reductase. ??? Why is HMG-CoA upregulated?

44
Q

What 4 therapeutic uses are Resins used for?

A

1) Primary hypercholesterolemia
2) Hyperlipidemias (type IIa and Type IIb)
3) Relieves puritis in people with bile salt accumulation
4) Tx for digitalis toxicity

45
Q

What are the adverse effects of sequestrants?

A

GI, Decreased absorption of Vitamin ADEK, drug absorption (cholestyramine and colestipol)

46
Q

What do you need to do when taking other meds with cholestyramine or colestipol?

A

Give any other med except niacin 1+ hr prior or 2hrs after sequestrant to ensure adequate absorption.

47
Q

Contraindications for sequestrant admin.

A

Diverticulitis, Preexisting bowel disease, Cholestasis

48
Q

MOA of ezetimibe

A

Inhibits intestinal absorption of cholesterol and phytosterols

49
Q

Why is ezetimibe effective even in absence of dietary cholesterol?

A

Because it inhibits reabsorption of cholesterol excreted in bile.

50
Q

Therapeutic uses of ezetimibe (3).

A

Lowers cholesterol:

1) Primary hypercholesterolemia (+/- statin)
2) Homozygous familial hypercholesterolemia (+atrova/simvastatin)
3) Mixesd hyperlipidemia (+ fenofibrate)

51
Q

Avoid concomitant admin of ezetimibe with what?

A

Bile acid sequestrants, due to inhibition of ezetimibe absorption.

52
Q

What two things combine to form Vytorin?

What two things can CAIs be absorbed with?

A

the trade name of the combo of ezemitibe and simvastatin

Fibrates or statins can be combined with CAIs.

53
Q

What 4 scenarios is combination drug therapy useful?

A

1) When VLDL significantly increased during tx of hyeprcholesterolemia with a resin.
2) When LDL and VLDL both initially elevated.
3) When LDL and VLDL not normalized by a single agent.
4) When an elevated Lp(a) or HDL deficiency coexists with other hyperlipidemias.

54
Q

Combos of lipid lowering agents (4).

A

1) Niacin and bile acid sequestrants
2) Niacin and staitns
3) Statins and fibrates
4) Statins and ezetimibe *(Vytorin)

55
Q

What class results in the largest decrease in LDL?

A

Statins (and lesser, but bile acid sequestrants)

56
Q

What class results in the largest decrease in TGs?

A

Fibrates

57
Q

What class results in the largest increase in HDL?

A

Niacin

58
Q

What is the new tx for homozygous familial hypercholesterolemia?

A

Lomitapide

Mipomersen

59
Q

Lopitamide MOA

Ultimate result

A

Oral.
Binds directly to and inhibits MTP in lumen of ER, which prevents lipoprotein contatining apo-B assembly in enteryocytes and hepatocytes.
Ultimate result is reduced VLDL and plasma LDL

60
Q

Mipomersen MOA

Ultimate result

A

SubQ.
Antisense oligonucleotide that targets apoB-100 mRNA and disrupts its function.
Ultimate result is reduced LDL-C, VLDL, apoB, non-HDL-C and total cholesterol.

61
Q

Adverse effects of lomitapide

A

GI, liver aminostransferase and fat elevation.

62
Q

Adverse effects of mipomersen

A

Injection site reaction, flu0like symptoms, HA, 3x normal liver enzyme levels

63
Q

Omega-3 PUFAs lower what?

A

Lower high plasma TGs and DON’T react with statins to increase risk of rhabdoyolysis

64
Q

Who should take Omega-3 PUFAs?

A

People recovering form recent MI - shown to decrease risk of cardiac death.

65
Q

Therapeutic benefits of statins (4).

A

Plaque stabilization, improvement of coronary endothelial function, inhibit platelet thrombus formation, anti-inflammation effects

66
Q

What labs are elevated due to statins? Presentation?

A 
Aminotransferase elevation (yellowing skin).
Creatine kinase elevation (muscle pain due to rhabdo or myopathy).
67
Q

What two drugs cause muscle pain?

A

statins and gemfibrozil

68
Q

What class increases warfarin levels? Other anticoag potentiation?

A

Warfarin increased by statins.

Anticoags potentiated by fibrates.

69
Q

Resins result in what adverse hyper-? affect? Why?

A

Resins decrease hepatic cholesterol, so there’s a compensatory mechanism of UPREGULATION of HMG-CoA reductase.
Therefore, use resin with statin.

MED233 Cardiovascular (18 decks)

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