Flashcards in Exam 2 antihyperlipidemics- Kinder Deck (73):
1
What are statins
HMG-CoA reductase inhibitors
2
what are the fibrate drugs
fenofibrate
gemfibrozil
3
what are the bile acid sequesterants
cholestyramine
colesevelam
colestipol
4
what are the cholesterol absorption inhibitors
ezetimibe
5
vytorin is a comination of what drugs
simvastatin and ezetimibe
6
what are the new Tx out for homozygous familial hypercholesterolemia
lomitapide
mipomersen
7
what are the major components of chylomicrons
dietary TGs and cholesterol
8
where are chylomicrons synthesized
intestine
9
what is the mechanism of catabolism of chylomicrons
TG hydrolysis by LPL and remant uptake by liver
10
What is LDL make up of
cholesteryl esters
11
what is HDL made up of
phospholipids, cholesteryl esters
12
what lipoproteins are made in the liver
VLDL and HDL
13
which lipoprotein has the most protein
HDL
14
which lipoprotein has the most lipid
chylomicrons
15
how do plaques form, general path sequence
LDL retention in subendothelial space leading to oxidation that increases plasminogen inhibitor and inhibits NO
massive accumulation of cholesterol with increased inflammatory response
16
What are the targe LDL choesterol levels and what is considered very high
want 190 very high
17
what is the target for total cholesterol and what is considered high
want 240 high
18
what are the normal ranges of HDL
60 is high
19
What is the LDL goal for CHD or CHD risk eqivalent?
at what LDL level do you intiate drug therapy
goal LDL 130
20
what is the LDL goal for patients with 0-1 risk factors? when do you start Tx
goal 190
21
What are the risk equivalents for CHD
symtomatic carotid artery disease
peripheral arterial disease
AAA
diabetes
22
what are the risk factors for hyperlipidemia
age
family Hx of premature CHD
cigarette smoking
HTN
low HDL
23
what are non drug Tx options for HLD
lifestyle changes, diet, exercise, smokin cessation
24
what are the drug Tx options for HLD
MHG-CoA Reductase Inhibitors (statins)
Niacin, Vit B3
Fibric Acid dervatives (fibrates)
bile acid sequestrants (resins)
cholesterol absorption inhibitors
25
non drug Tx for HLD should not be used alone in what scenarios
severe hypercholestermia
known CHD
CHD risk equivalents
PVD
26
what are the dietary recs for HLD
total fat 20-25% calories
saturated fat <200 mg
carbs 50-60% total calories
dietary fiber 20-30 g
27
What parts of diet increase TGs?
alcohol, total fat, excess caloric intae
28
what parts of diet increase LDL
cholesterol, saturated and trans fats
29
What is HMG-CoA reductase
the rate limiting enzyme in cholesterol synthesis
30
which statins have longer half lives
atorvastatin and rosuvastatin
31
What statins use CYP3A4
lovastatin, simvastatin, atorvastatin
32
what stains use CYP2C9
fluvastatin and rosuvastatin
33
What are adverse reactions of statins
LFT elevation, CPK elevation, rhabdomyolysis, myopathy
34
what are contraindications for statins
pregnancy
35
What drugs cause bad interactions with statins
increase statin: CYP inhibitors, cyclosprine, ketoconozole fibrates
decrease statin: CYP inducers (phenytoin and rifampin)
36
How does niacin work
inhibits lipolysis of TG in adipose and reduces circulatin FFA
37
what are the affects of niacin on apoA1 and plasma HDL
decrease apoA1 clearance and increase plasma HDL
38
what are the affects of niacin on clotting factors
decrease fibrinogen levels and increase tpa
39
why do you have to dose constantly with nicotinic acid, niacin
extensive first pass. t1/2 is 60 minutes
40
what are the adverse ractions with niacin
cutaneous flush (PG mediated), pruritis, acanthosis nigricans, hepatotoxicity
41
what are the contraindications with niacin
hepatic disease, active PUD, caution DM
42
how do fibrates work
PPARalpha agonists that regulate expression of proteins involved in lipoprotein structure and function, increased expression LPL
43
what is the main result of fibrates
decreased TG levels
44
what are the adverse reactions with fibrates
GI, lithiasis, myositis, myopathy
45
what are the contraindications with fibrates
avoid in hepatic or renal dysfunction, pregnancy
46
what main anticoagulant has a drug interaction with statins
warfarin, increased risk of rhabdomyolysis if used with statins
47
how do bile acid sequestrants work
bind bile acids increasing excretion in stool. so ehnaced conversion of cholesterol to BA and increased LDL clearance
48
what are the adverse reactions with bile acid sequestrants (resins)
GI constipation and nausea, impaired ADEK absorption
49
what are the contraindications with resins
caution in diverticulitis, bowel disease and cholestasis
50
what are the drug interactions with resins
impairs drug absorption- separate admin
51
how does ezetimibe work
inhibits NPC1L1 inhibits absorption of cholesterol and plant sterols
52
what is adverse reaction with ezetimibe
diarrhea
53
what are the drug interactions with resins
have to separate time of administartion by at least 4 hours because resins will bind up drugs
54
what is the overall effect of statins on lipoproteins
decrease LDL
55
what is the overall effect of niacin on lipoproteins
increase HDL
56
what is the overall effect of resins on lipoproteins
decrease LDL
57
What is the main Tx course for atherosclerotic CV disease ASCVD
maximizing statin intesnsity reduces amount of events
58
What are the 4 statin benefit groups
1) ASCVD
2) primary elevation of LDL-C >190 mg
3) age 40-75 with DM and LDL-C 70-189 mg
4) No clinical ASCVD or DM who are 40-75 y/o and LDL-C 70-189 mg with ASCVD risk >7.5%
59
if patient is above 21 and has clinical ASCVD what Tx is first line
75 moderate intensity statin
60
patient does not have ASCVD but has LDL-C >190 Tx?
high intesnsity statin
61
patient does not have ASCVD or LDL-C >190 but has DM I or II and is 40-75. Tx?
moderate intensity
high if estimated 10 y risk is >7.5%
62
what does high intesnsity statin mean
daily dose lowers LDL-C by approx 50%
63
what does moderate intesnsity statin mean
daily dose lowers LDL-C by approx 30-<50%
64
what are the high intesnsity statins available and doses
atorvastatin 40-80 mg
rosuvastatin 20 mg
65
what cause homozygous familial hypercholesterolemia
defects in LDL R gene
66
What are Tx options for homozygous familial hypercholesterolemi
Mipomersen injection
Lomitapide
67
How does mipomersen lower cholesterol
inhibits apoB 100 synthesis by binding mRNA and reducing formation
68
what are adverse reactions to mipomersen
injection site reactions, flue like symtoms, HA, elevated liver transaminases
69
what are the contraindications for mipomersen
moderate or severe hepatic impairment, active liver disease
70
what is administration method for lomitapide
once dialy oral dosew
71
what is mechanism of lomitapide
binds and inhibits microsomal TG transfer protein, lcoated in lumen of ER. prevents assembly of apoB
72
what are adverse reactions to lomitapide
GI diarrhea, nausea, increased liver transaminases, hepatic fat accumulation
73