Lipid Lowering Agents

Front 1

Statins

Back 1

Structural analogs of HMG-COA

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Statins

Back 2

Inhibits 3-hydroxy 3 methylglutaryl-coA reductase

Front 3

Statins

Back 3

Upregulation of hepatic LDL receptors and increased LDL clearance

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Statins

Back 4

Reduction in LDL (20%-60%)

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Statins

Back 5

Reduction in TAG (15%-45%)

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Statins

Back 6

5-10% increase in HDL

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Statins

Back 7

Inhibits monocyte migration and adhesion to endothelium

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Statins

Back 8

Inhibit monocyte proliferation

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Statin

Back 9

Inhibit oxidation of LDL

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Statins

Back 10

Inhibit immune and inflammatory responses

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Statins

Back 11

Stabilize atherosclerotic plaque

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Statins

Back 12

Drug of Choice for patients with high plasma LDL levels

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Statins

Back 13

Taken up into the liver by OATP2

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Lovarstatin, Simvastatin, Atorvastatin

Back 14

Metabolized by CYP3A4

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Fluvastatin, Rosuvastatin

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Metabolized hy CYP2C9

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Pravastatin

Back 16

Not metabolized by CYP450

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Atorvastatin

Back 17

Half-life is 14 hours

Front 18

Rosuvastatin

Back 18

Half-life is 19 hours

Front 19

Lorvastatin, Simvastatin, Fluvastatin, Pravastatin

Back 19

Half-life is 1.5-2 hours

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Statins

Back 20

Undergoes glucorinidation

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Statins

Back 21

Elevation of creatinine kinase

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Statins

Back 22

Myalgia, myopathy, rhabdomyolysis

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Pravastatin

Back 23

Fewer muscle effects

Front 24

Rhabdomyolysis

Back 24

Fever, malaise, diffuse myalgia and tenderness

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Statins

Back 25

Elevation of transaminase levels

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Cyclosporine, Tacrolimus

Back 26

Immue suppressants CYP3AR inhibitors

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Erythromycin, Clarithromycin

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Macrolide CYP3A4 inhibitors

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Diltiazem, Verpamil

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CCB CYP3A4 inhibitors

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Amiodarone

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Antiarryhtmic CYP3A4 inhibitor

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Ketoconazole, Itraconazole

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Azole CYP3A4 inhibitor

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Warfarin

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Anticoagulant CYP3A4 inhibitor

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Amprenavir, indinavir, Neflinavir, Ritonavir

Back 32

Anti-HIV CYP3A4 inhibitor

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Grapefruit Juice

Back 33

Increase plasma concentration of LSA via inhibition of CYP3A4

Front 34

Phenytoin, Griseofulvin, Barbiturates, Rifampin, Thiazolidinedione

Back 34

Increase expression of CYP3A4

Front 35

Gemfribrozil

Back 35

Inhibits metabolism of all Statins

Front 36

Gemfibrozil

Back 36

Inhibits glucorinidation

Front 37

Gemfibrozil

Back 37

Inhibits OATP2

Front 38

Bile Acid Binding Resins

Back 38

Act as anion exchanger which binds to bile acid/salts in SI preventing absorption

Front 39

Bile Acid Binding Resins

Back 39

Disrupts normal enterohepatic recirculation of bile acids

Front 40

Bile Acid Binding Resin

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Modest 10-25% reduction in LDL

Front 41

Bile Acid Binding Resins

Back 41

Increase TAG by 3-10%

Front 42

Bile Acid Binding Resins

Back 42

Second line drugs for primary hyperlipidemia

Front 43

Bile Acid Binding Resins

Back 43

Can be used to relieve pruritus due to accumulation of bile acids

Front 44

Bile Acid Binding Resins

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Drug of choice for hypercholesterolemia in children and women of child bearing age, pregnant and lactating

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Bile Acid Binding Resins

Back 45

GI disturbances are most common side effects (Constipation, Bloating, Epigastric Fullness, Nausea a d Flatulence)

Front 46

Cholestyramine, Colestipol

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At high doses, impair absorption of fatsoluble vitamins

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Bile Acid Binding Resins

Back 47

Contraindicated to dysbetalipoprotenemia and raised trigylcerides

Front 48

Ezetimibe

Back 48

Inhibits Niemann-Pick C1-like protein

Front 49

Ezetimibe

Back 49

Reduction in hepatic cholesterol resulting on increased expression of LDL receptor, promoting increased LDL clearance

Front 50

Ezetimibe

Back 50

Reduces LDL levels by 18%

Front 51

Ezetimibe

Back 51

Significant LDL lowering effect when combined with statins

Front 52

Ezetimibe

Back 52

Undergoes entero hepatic recirculation

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Ezetimibe

Back 53

Flatulence is the most common side effect, diarrhea and myalgia may occur

Front 54

Cyclosporine

Back 54

Increases concentration of Ezetimibe

Front 55

Bile Acid Binding Resins

Back 55

Interfere with absorption of Ezetimibe

Front 56

Niacin

Back 56

Water soluble vitamin used in the synthesis of NAD and NADP

Front 57

Niacin

Back 57

Require large doses (1500-3000 mg/day)

Front 58

Niacin

Back 58

Acts via its GI-coupled GPCR expressed in adipose tissueto inhibit cAMP-induced lipolysis

Front 59

Niacin

Back 59

Significantly reduce levels of Lp(a) lipoprotein

Front 60

Niacin

Back 60

30-80% reduction in Triglycerides

Front 61

Niacin

Back 61

Most effective agent in elevating HDL levels

Front 62

Niacin

Back 62

Skin flushing, itching and sensation of warmth

Front 63

Niacin

Back 63

Inhibits tubular secretion of uric acid

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Niacin

Back 64

May cause insulin resistance and hyperglycemia

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Niacin

Back 65

Hepatic toxicity

Front 66

Niacin

Back 66

Can exacerbate peptic ulcer

Front 67

Fibrates

Back 67

Derivatives of fibric acid

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Fibrates

Back 68

Acts as ligands for nuclear hormone transcription factor: PPAR-a

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Fibrates

Back 69

Activate PPAR-a decreasing plasma triglycerides

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Fibrates

Back 70

Increase expression of lipoprotein lipase in muscles

Front 71

Fibrates

Back 71

Decreasing hepatic expression of apolipoprotein CIII

Front 72

Fibrates

Back 72

Increasing Fatty Acid Catabolism

Front 73

Fibrates

Back 73

Upregulate SR-B1 scavenger receptor in hepatocytes

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Fibrates

Back 74

40-60% reduction in TAG

Front 75

Fibrates

Back 75

Increase peripheral VLDL clearance

Front 76

Fibrates

Back 76

Undergoes extra hepatic circulation

Front 77

Gemfribozil

Back 77

Half -life is 1.5 hours

Front 78

Fenofibrate

Back 78

Half-life is 20 hours

Front 79

Fibrates

Back 79

Predisposes gallstone formation

Front 80

Fish Oils

Back 80

Inhibit hepatic triglyceride synthesis and clearance

Front 81

Fish Oils

Back 81

Lower serum Triglyceride levels by 50%

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Fish Oils

Back 82

Fishy after taste

Front 83

Fish Oils

Back 83

Reduces serum concentrations of Vitamin E

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Fish Oils

Back 84

Not associated with an incrwased risk of rhabdomyolysis when given together with Statin