Dyslipidemia Part 2 (Exam 3) Flashcards

(85 cards)

1
Q

Main function of liver

A

bile secretion

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2
Q

Bile functions

A

Emulsifying large fat particles into minute ones
Aiding in absorption of digested fat end products through intestinal mucosal membrane

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3
Q

Bile used for excretion of waste products from blood but especially

A

bilirubin, and end product of hemoglobin destruction

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4
Q

Components of Bile

A

Bile salts
Fatty acids
Cholesterol
Proteins
Phospholipids
Bilirubin

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5
Q

Precursor of bile

A

Cholesterol

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6
Q

Primary bile acids are in the

A

liver

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7
Q

Secondary bile salts are in the

A

intestines

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8
Q

Bile salts form

A

micelles

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9
Q

Bile salts have a ____ action

A

detergent (emulsifying)

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10
Q

Micelles

A

transport medium to carry monoglycerides and free fatty acids to brush borders of intestinal epithelial cells

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11
Q

Major determinant of bile acid synthesis

A

concentration in hepatic portal blood

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12
Q

____ and _____ stimulate bile acid secretion

A

Cholecystokinin (CCK)

Secretin

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13
Q

Elevation of CCK in blood leads to

A

Release of digestive enzymes from pancreas
Contraction of gallbladder to deliver bile

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14
Q

Bile Acid Sequestrants

A

Cholestryamine (Questran)
Colestipol (Colestid)
Colesevelam (Welchol)

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15
Q

Bile Acid Sequestrants MOA

A

Bind to bile acids in intestines and prevent reabsorption

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16
Q

Bile acid sequestrants are _____ and bind ______ bile acids

A

positively charged

negatively charged

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17
Q

Are bile acid sequestrants absorbed?

A

NO
excreted in the stool

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18
Q

Bile acids are made from

A

cholesterol

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19
Q

Where are bile acids released?

A

into the small intestine

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20
Q

Reduction in available cholesterol leads to

A

LDL receptors being upregulated

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21
Q

Bile acid sequestrants are ______ that are _____

A

large polymeric cationic exchange resins

insoluble in water

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22
Q

Bile Acid Sequestrants ADRs

A

Constipation and bloating
Choking
Reduced absorption of vitamins A, D, K, E
Increase in TG

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23
Q

Which Bile Acid Sequestrant is approved for diabetes?

A

Colesevelam

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24
Q

Colesevelam MOA

A

inhibits FXR activity in L-cells and promotes GLP1 production and secretion

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25
Cholesterol Absorption Inhibitor
Ezetimibe (Zetia)
26
Ezetimibe (Zetia) MOA
inhibits cholesterol uptake by enterocytes in GI tract by inhibiting Neiman Pick C1-like protein (NPC1L1)
27
Ezetimibe is _____ and has ____
lipophilic low water solubility
28
Ezetimibe is ___ in the intestinal epithelium
glucuronidated
29
Which drugs inhibit ezetimibe absorption?
Bile acid sequestrants
30
PCSK9 Inhibitors
Alirocumab (Praluent) Evolocumab (Repatha)
31
PCSK9 Inhibitors MOA
Humanized monoclonal antibodies that bind and remove PCSK9 which leads to more LDL receptors
32
PCSK9 Inhibitors ADRs
Drug neutralizing antibodies may occur
33
Protein drugs are metabolized by _____
protease enzymes
34
How are PCSK9 Inhibitors given?
SubQ injection every 2 to 4 weeks
35
Adenosine triphosphate-citrate lyase (ACL) inhibitor MOA
Inhibits ACL leading to inhibition of cholesterol synthesis
36
ACL inhibitor is a _____ activated by _____ in ______
prodrug acyl-CoA synthetase hepatocytes
37
ECT-1002
Bempedoic acid (Nexletol)
38
ECT-1002 is converted to ____ by ____
ECT-1002-CoA acyl-CoA synthetase
39
ACL inhibitor ADRs
hyperuricemia mild increase in liver enzymes increased risk of BPH tendon rupture
40
How is ACL inhibitor metabolized?
Glucuronidation
41
Why does bempedoic acid not cause myopathy?
Not converted to active drug in muscle tissue
42
ACL inhibitor increases plasma concentrations of
simvastatin and pravastatin
43
Familial Hypercholesterolemia (FH)
genetic disorder that causes accumulation of LDL in arteries which increases risk of CV diseases (atherosclerosis)
44
HoFH LDL levels
over 400 mg/dL - 4x normal levels
45
45
46
Medications only for HoFH
Mipomersen (Kynamro) Lomitapide (Juxtapid)
46
Mipomersen (Kynamro) MOA
single-stranded oligonucleotide inhibitor of apo b-100 synthesis
47
Mipomersen (Kynamro) reduces LDL by
30-50%
48
Mipomersen (Kynamro) and Lomitapide (Juxtapid) REMS program
hepatotoxicity
49
Lomitapide (Juxtapid) MOA
inhibits microsomal trigylceride transfer protein (MTP)
50
Lomitapide (Juxtapid) reduces LDL by
40-50%
51
Fibrates
Gemfibrozil (Lopid) Fenofibrate (Tricor)
52
Fibrates MOA
Activate PPARa
53
Activation of PPARa leads to
increased lipoprotein lipase = less TG increased apoA1 + apoA2 = high HDL decreased apoCIII = low TG
54
Gemfibrozil inhibits uptake of statins by ____ and competes for ______
OATP1B1 glucuronidation
55
Which fibrate is preferred?
Fenofibrate
56
Niacin
water-soluble B-complex vitamin (B3)
57
Types of Niacin
Extended-release (ER) Sustained-release (SR) Immediate-release (IR)
58
Half-life of Niacin
SR > ER > IR
59
Which type of Niacin had quickest rate of absorption and highest rate of flushing
IR
60
Which type of Niacin has slowest absorption and highest hepatotoxicity
SR
61
Nicotinuric acid (NUA)
Prostaglandin mediated facial flushing
62
What reduces flushing?
Aspirin 30 mins before taking niacin
63
Nicotinamide (NAM)
hepatotoxicity
64
Niacin ADRs
Dyspepsia Hyperuricemia Hyperglycemia
65
Niacin undergoes ____
extensive first pass metabolism
66
Omega-3 fatty acids
polyunsaturated fatty acids obtained through diet 3rd carbon on omega side is unsaturated
67
Fatty acids
carboxylic acids with long aliphatic chain that is saturated or unsaturated
68
Alpha-linolenic acid (ALA)
Omega-3 fatty acid 9,12,15-octadecadienoic
69
Omega-3 acid ethyl esters (Lovaza and Omtryg) contains
Eicosapentaenoic acid (EPA) Docosahexaenoic acid (DHA)
70
Isocapent ethyl (Vascepa) contains
EPA ethyl ester
71
Omega-3 Acids effects
reduce synthesis of TG increase fatty acid oxidation enhanced clearance of TG reduce platelet aggregation antioxidant effects
72
EPA and DHA reduce
trigylcerides
73
DHA increases
LDL
74
Enzymes effected by omega-3 fatty acids
Diglyceride acyltransferase Lipoprotein lipase activity
75
omega-3 fatty acids are ____ that undergo ____
prodrugs hydrolysis
76
Which omega-3 has evidence for ASCVD lowering?
Icosapent ethyl
77
Pregnancy changes in cholesterol
increase cholesterol by 25-50% increase LDL up to 66% increase TG 200-400%
78
Which drugs are safe in pregnancy?
Bile acid sequestrants
79
Which drugs may be considered in pregnancy?
Miposersen and omega-3
80
Medications to lower LDL
High intensity statin, PCSK9 inhibitors > moderate statins > low statins, bile acid, ACL, cholesterol inhibitors
81
Medications to lower TG
Fibrates > nicotinic acid, omega-3 Statins
82
Nicotinic acid and fibrates have ____ effect on HDL
biggest positive
83
Medications that have negative effect on lipid levels
Lovaza/Omtryg Bile acid sequestrants