Week 4 (Exam 1) Flashcards

(53 cards)

1
Q

Statin Lipid Lowering MOA

A

blocks HMG CoA Reductase to mevalonic acid

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2
Q

Statin Inflammation reducing MOA

A

Reduces CRP and Erythrocyte Sedimentation Rate

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3
Q

Statin Reversal of Endothelial Dysfunction MOA

A
Increase in NO synthesis
Reduced oxidized LDL
Inhibition of Endothelin synthesis
Reduction in Endothelial Permeability to LDL cholesterol
Inactivation of Superoxide
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4
Q

Statin Decreased Thrombogenicity MOA

A

Reduced endothelial and atherosclerotic plaque macrophage tissue factor expression
Decreased Prothrombin activation and thrombin generation
Improved fibrinolysis
Decreased platelet activation

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5
Q

Advicor

A

Lovastatin and Niastatin

XR

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6
Q

Simcor

A

Simvistatin and Niastatin

XR

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7
Q

Vytorin

A

Simbistatin and Ezetimibe

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8
Q

Muscle related side effects of Statin

A

Bilateral, symmetrical, skeletal muscle myopathy

No rise in Creatine Kinase

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9
Q

How do statins cause liver damage?

A

Temporary depletion of intracellular cholesterol causes an increase in LDL receptor production

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10
Q

Statins and transaminase levels

A

Asx and dose-related increases 3x normal

ALT > AST (distinguishes liver from muscle AST)

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11
Q

All statins have been show to cause…

A

AKI (rhabdomyolysis, subsequent myoglobinemia)

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12
Q

The two pro-drug Statins

A

Simvistatin and Lovastatin (increases their hepatic metabolism)

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13
Q

Statins that should maybe be given at a lower dose for asian populations

A

Rosuvastatin and Simvastatin

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14
Q

Statins metabolized in CYP3A4 pathway

A

Atorvastain
Simvastatin
Lovastatin

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15
Q

Statins metabolized in CYP2C9

A

Fluvastatin

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16
Q

Ezetimibe MOA

A

Inhibits dietary and biliary cholesterol absorption at brush border via NPC1L1 so Liver has to then take more from the circulation
Also blocks chostesterol traffickers Aminopeptidase N and Cave-in 1-Annexin A2 Complex

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17
Q

NPC1A1

A

Expressed in Intestine and Liver as Sterol Transporter to mediate intestinal cholesterol absorption and counterbalances hepatobiliary cholesterol excretion
Inhibited by Ezetimibe

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18
Q

Indications for Ezetimibe

A

Homozygous Familial Hypocholeterolemia
Homozygous Sitosterolemia
Primary Hyperlipidemia

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19
Q

Ezetimibe dosing for Homozygous Familial Hypercholesterolemia

A

10mg PO qDay w/ Atorvastatin or Simvastatin

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20
Q

Ezetimibe dosing in Primary Hyperlipidemia

A

10mg PO qDay w/ HMG-CoA Reductase inhibitors in diet
Can be monotherapy
can be w/ fenofibrate
can be w/ Statins

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21
Q

Contraindications of Ezetimibe

A

Pregnancy and breastfeeding when combo w/ statin

Hepatic Disease or impairment

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22
Q

Toxicity of Ezetimibe

A

Skeletal muscle toxicity when used with statin, especially over 65 y.o., hypothyroidism, renal impairment

23
Q

PCSK9 Inhibitor MOA

A

Serine Protease: cleaves LDL receptors at Serine Residues (degrades them)
Increases Hepatic LDL-R and Decreases Plasma LDL-C

24
Q

The two PCSK9 Inhibitors

A

Alirocumab and Evolocumab

25
Indications for Alirocumab and Evolocumab
PCSK9 Inhibitors: Tx FH and Atherosclerotic CVD
26
Most common PCSK9-I side effects
Runny nose, sore throat, injection site rxn
27
Bile Acid Sequestrant MOA
Not absorbed, but bind bile acids and are excreted as a complex Cholesterol depletion increases LDL rec Activity (increases removal of LDL cholesterol from blood)
28
Bile Acid Sequestrants (3)
Colesevelam, Colestipol, Cholestyramine
29
Contraindications of Bile Acid Sequestrants
Its with Dysbetalipoproteinemia: induced Pancreatitis | Decreased GI Motility
30
Adverse Effects of Bile Acid Sequestrations
Elevated TAGs Elevated Liver Enzymes Vit D Deficiency
31
Bile Acid Sequestrant Warnings and Precautions
ADEK and Folic Acid Deficiency | Phenylketonuria (contains F)
32
Fibrate MOA
PPARa Activator: Increases liver enzymes for TAG metabolism and uptake
33
Fenofibric Acid (Fibrate) Indications
Dyslipidemia | Severe HyperTAG-emia
34
Gemfibrozil (fibrate) Indications
Severe HyperTAG-emia | Primary Prevention of Coronary Heart Disease (in type IIb patients)
35
Gemfibrozil Drug Contraindications
``` Dasabuvir Repaglinide Simvastatin (muscle toxicity with statins) Cerivastatin Enzalutamide (increases seizure risk) Selexipag ```
36
Gemfibrozil Side Effects
GI: stomach pain, nausea Increased liver enzymes (same with other Fibrates) Elevated Creatinine Kinase (like other Fibrates) Gallstones (like other Fibrates), maybe. Myopathy and Rhabdomyolysis (like other Fibrates) Kidney and Liver Dz
37
Fibrates and GFR
Do not use if GFR is below 30 ml/min | GFR between 30 - 59? Keep dose below 54 mg/day
38
Why can Fibrates cause a slight increase in serum creatinine?
They inhibit kidney Organic Cation Transporter 2
39
Gemfibrozil is a strong inhibitor of:
CYP2C8
40
Bile Acid Sequestrants and Fibrates
Can interfere with Fibrates (take 1 hour before or 4 hours after BAS)
41
Colchicine + Fibrates
Muscle Toxicity, Rhabdomyolysis
42
Fibrates + Ezetimibe
Fibrates increase the levels of Ezetimibe
43
Fibrates + Warfarin
Fibrates interfere with the warfarin
44
Fibrates + Cyclosporine / Tacrolimus
Nephrotoxicity
45
OAT1B1
Inhibited by Gemfibrozil (hepatic uptake transporter)
46
Fibrates in pregnancy
Idk, but definitely don't use them while nursing
47
Niacin MOA
Maybe increase lipoprotein lipase Maybe inhibits release of free fatty acids from adipose Maybe decreases rate of LDL/VLDL synthesis
48
Indications for Niacor
Reduction of total and LDL Cholesterol | Adjunct therapy for adults wit super high TAGs
49
Indications for Niaspan
To increase HDL | To reduce total cholesterol, LDL, Apo B, TAGs
50
Niacin Adverse Effects
Flushing, itching Blood sugar elevation Raise Uric Acid Levels, liver enzymes
51
Niacin warnings and precautions
``` Don't use with Liber Disease Can raise blood sugar: don't use with diabetes Can increase uric acid levels (gout) Can prolong bleeding time Contraindicated in PUD ```
52
Niacin metabolism
CYP2D6 Inhibitor
53
Drug interactions with Niacin
Statins and Bile Acid Sequestrants