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CV Pharmacology > Lipid Lowering Drugs > Flashcards

Lipid Lowering Drugs Flashcards

1
Q

Describe chylomicronemia.

A

Defect: apoCII, LPL - no removal of CM

Chylomicrons, VLDL, & TG elevated, pancreatitis, eruptive xanthomas, plasma with creamy top layer and clear infranate.

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2
Q

Describe familial hypertriglyceridemia.

A

Defective LPL - reduced metabolism of VLDL.

Elevated VLDL, hypertriglyceridemia, pancreatitis.

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3
Q

Describe familial dysbetalipoproteinemia.

A

E2 Alleles - ApoE defect - defective metabolism of VLDL & chylomicrons.

Elevated VLDL & CM remnants. Elevated cholesterol & TG. Atherosclerosis.

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4
Q

Describe familial combined hyperlipidemia.

A

Overproduction of ApoB100 for VLDLs.

Variable phenotype. Elevated VLDL, LDL, or both. Premature atherosclerosis.

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5
Q

Describe familial hypercholesterolemia (FH).

A

Defect in LDL receptor or ApoB. Decreased removal of LDL from plasma.

Elevated LDL. Premature atherosclerosis.

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6
Q

Mechanism of action of HMG-CoA Reductase Inhibitors

A
  • inhibits rate-limiting step of cholesterol synthesis
  • Increase the number of LDL receptors by promoting transport and cleavage of SREBP so it can enter the nucleus, bind to SRE (sterol regulatory element) and increase txn of the LDL receptor gene
  • Reduces LDL by 25-60%, reduces risk of CHD
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7
Q

What are the clinical uses for statins?

A

Greatly decreases LDL, increases HDL, decreases TG.

Atherosclerotic disease, acute coronary disease, high LDL

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8
Q

Which statins are lipid soluble prodrugs?

A

Lovastatin, Simvastatin

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9
Q

Which statins are metabolized by CYP3A4?

A

Simvastatin, Lovastatin, Atorvastatin

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10
Q

What statins are metabolized by CYP2C9?

A

Fluvastatin, Rosuvastatin

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11
Q

Which statin has low potentcy and efficacy?

A

Pravastatin

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12
Q

Which statins have high potentcy, high efficacy, and long half-life?

A

Atorvastatin, Rosuvastatin

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13
Q

What are the high intensity statins?

A

Atorvastatin and Rosuvastatin at high doses.

Cause > 50% reduction in LDL.

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14
Q

What drug is used for primary prevention of CVD in persons > 21 with LDL > 190?

A

High intensity statin. May add non-statin to further reduce LDL.

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15
Q

What drug is used for primary prevention of CVD in pts with diabetes aged 40-75 with LDL 70-189 mg/dL?

A

10-year risk < 7.5% = moderate intensity statin

10-year risk > 7.5% = high intensity statin

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16
Q

What drug is used for primary prevention of CVD in pts without diabetes aged 40-75 with LDL 70-189 mg/dL?

A

10-year risk > 7.5% = moderate or high intensity statin

10-year risk 5-7.4% = moderate intensity statin

17
Q

What are the moderate intensity statins?

A

Atorvastatin and Rosuvastatin at lower doses.

Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin at higher doses.

30-50% reduction in LDL.

18
Q

What are the low intensity statins?

A

Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin at lower doses.

< 30% reduction in LDL.

19
Q

What are the adverse effects of statins?

A
  • transient GI distress
  • increased liver enzymes
  • sleep disturbance, memory loss
  • pregnancy category X
  • myalgia (except Pravastatin)
  • myositis
  • rhabdomyolysis
20
Q

Mechanism of action of bile acid sequestrants/resins (Colestipol, Cholestyramine).

A
  • Bind to bile acids and prevent reabsorption
  • Requires more cholesterol to be used for bile acid synthesis - upregulates LDL receptor
  • Lowers LDL by up to 25%, does not decrease TG.
21
Q

When are bile acid sequestrants used?

A

In children, patients with liver disease, pregnant women.

Non-systemic, very safe, may cause bloating & constipation.

22
Q

What are the clinical uses for bile acid sequestrants?

A

High LDL, digitalis toxicity, pruritis

Decreases LDL, slightly increases HDL & TG.

23
Q

Adverse effects of bile acid sequestrants

A
  • bloating, nausea, flatulence, constipation, fecal impaction
  • hypertriglyceridemia
24
Q

What is the common drug interaction with bile acid sequestrants?

A

Prevention of absorption of other drugs: digoxin, beta-blockers, thyroxine, coumadin

25
Q

Bile acid sequestrants contraindications

A
  • hypertriglyceridemia
  • complex drug regimens
  • history of constipation
26
Q

Mechanism of action of Gemfibrozil & Fenofibrate

A
  • activate the PPARalpha nuclear receptor - upregulates txn of LPL, apoA, downregulates txn of apoC3
  • decreases VLDL up to 50%, LDL unchanged, increases HDL up to 15%
27
Q

Why are statins and Gemfibrozil not administered together?

A

Both are oxidized in liver via glucuronidation by UGT1A1. Gemfibrozil will reduce the metabolism of statins.

28
Q

What is the mechanism of action of fibrates?

A

Upregulate LPL to increase TG clearance.

Activates PPAR-alpha to cause HDL synthesis.

29
Q

What are the clinical uses for Fibrates?

A

High TG, low HDL

Safe to use with liver disease.

Slightly decreases LDL, slightly increases HDL, greatly decreases TG.

30
Q

Why is Fenofibrate not recommended in pts with renal disease?

A

Excreted renally. Will accumulate if GFR < 50 ml/min. Dosage reduction recommended. Contraindicated if GFR < 30.

31
Q

What are the adverse effects of fibrates?

A
  • gastroesophageal reflux, diarrhea, increased liver enzymes
  • pregnancy category C, teratogenic
  • gallstones
  • Fenofibrate: increased creatinine, HDL lowering
32
Q

Mechanism of action of Niacin

A
  • Prevents mobilization of FFA from adipocytes
  • Reduces TG synthesis in liver, ApoB synthesis, and VLDL secretion
  • Increases transfer of cholesterol from macrophages to HDL
  • Enhances LPL
  • Lowers LDL by up to 20%
  • Increases HDL 15-35%
  • Lowers TG by 20-50%
  • Reduces Lp(a) by 30%
33
Q

What are the adverse effects of Niacin?

A
  • cutaneous flushing - give aspirin
  • elevated transaminases, hepatitis, hepatic failure
  • GI irritation
  • hyperuricemia/gout
  • conjunctivitis, retinal detachment, macular edema
  • dry skin, pruritis, icthyosis, acnthosis nigricans
  • insuline resistance
  • pregnancy category C
34
Q

What are the clinical uses for Niacin?

A

Lowers LDL, increases HDL, modestly decreases TG.

Used for high VLDL, high LDL, high Lp(a), low HDL

35
Q

Mechanism of action of Ezetimibe

A
  • Prevents absorption of dietary cholesterol by inhibiting NPC1L1
  • does not effect plasma levels of drug soluble vitamins
  • Lowers LDL by up to 20% → reduced delivery of cholesterol to liver upregulates LDL receptors to cause clearance of LDL from plasma
  • distinct and complementary action to statins
36
Q

Does Ezetimibe cause a reduction in CHD risk?

A
  • no clinical trial evidence
  • modest effect on LDL, usually combined with statin or used in pts that can’t take statins
37
Q

What are the clinical uses for Ezetimibe?

A

High LDL, phytosterolemia

Reduces LDL only.

38
Q

What are the effects of omega-3 fatty acids?

A
  • reduction of CHD risk, SCD, and MI
  • antiplatelet, antiarrhythmic, lower BP
  • reduce serum TGs up to 35%
  • activates PPARalpha to increase FA oxidation
  • little to no effect on LDL or HDL cholesterol

CV Pharmacology (5 decks)

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