Lipid Lowering Medications Flashcards
What is the desired outcome of lipid lowering agents?
- lower serum cholesterol
- lower serum LDLs
- prevention of CAD
How do lipid lowering agents help prevent CAD?
- protect endothelial tissue
- prevents plaque from rupturing
- slow down the progression of atherosclerosis
What is cholesterol?
a lipid that is an essential part of bile acid & cell membranes
What lipid is insoluble in blood?
cholesterol
What lipid is a precursor of the steroid hormone?
cholesterol
What is a triglyceride?
a lipid made from fatty acid & glycerol
how are triglycerides aquired?
through the diet
Where are triglycerides stored?
adipose tissue
__________ levels correlate with LDL and are inverse to HDL
triglyceride
what are lipoproteins?
are carrier proteins that aid in transportation of cholesterol & triglycerides in the blood
Where are lipoproteins produced?
by the liver
What do LDLs enter circulation as?
tightly packed cholesterol, triglycerides, & lipids fom the liver to the peripheral tissue
____ are carried by proteins; broken down for energy or stored for future use as energy
LDLs
What are know as the “bad” cholesterol?
LDLs
What are the primary transport molecules for cholesterol?
LDLs
How do HDLs enter circulation?
as loosely packed lipids
________ are used for energy; pick up remnantsof fat & cholesterol from the peripheral tissues back to the liver where it is excreted in the bile
HDLs
What is considered to be the “good” cholesterol?
HDLs
What is the desired level for total cholesterol?
less than 200
What is the desired level for LDL?
less than 130
What is the desired level for HDL?
50 or higher
What are the desired levels from triglycerides?
less than 200
What do we want LDLs to be in diabetics & those at risk?
less than 70
What are non-modifiable CV risk factors?
genetic predisposition**
age
gender
- males greater than females
- equal after menopause
What are the modifiable risk factors?
metabolic syndrome
cigarette smoking
sedentary lifestyle
high-stress levels
HTN
obesity
diabetes
untreated bacterial infection
What are modifiable CV risk factors related to?
inflammation
What medications are HMG CoA reductase inhibitors?
lovastatin
pravastatin
simvastatin
atorvastatin
rosuvastatin
What medications are fibrates?
gemfibrozil (lopid)
fenofibrate (tricor)
fenofibric acid (tripipix)
what medication is a cholesterol absorption inhibitor
ezetimibe
what medications are PCSK9 inhibitors?
evolocumab (repatha)
alirocumab (praulent)
What medications are bile acid sequestrants?
colesevelam (welchol)
cholestyramine (prevalite)
colestipol (colestid
What medication is a lipid lowering medication that is not used much anymore?
niacin
What is the suffix of that HMG-CoA reductase inhibitors have?
“statin”
What is the most effective & most prescribed lipid lowering drug?
HMG-CoA reductase inhibitors
How do HMG-CoA reductase inhibitors work?
block synthesis of cholesterol in the liver by competitively inhibiting HMG-CoA reductase activity
What do HMG-CoA reductase inhibitors affect LDLs, triglycerides & HDLs?
- decreases LDL levels by 25-65%
- modest decrease in triglycerides by 10-40%
- modest increase in HDL by 5-17%
Can you take HMG-CoA reductase inhibitors during pregnancy?
no; pregnancy category x
What do statins do in the vascular system?
- reduce smooth muscle cell changes
- reduce inflammatory c3ells inside plaque
- stabilize the endothelium
- reduce friction in the bloodflow
- reduce proteins associated with inflammation
Who should be on a statin?
- adults with a hx of CV disease
- those with LDL level greater than 190
- adults 40-75 with diabetes
- adults 40-75 with LDL of 70-189 & a 5-19.9% 10-year risk of developing CV disease
-adults 40-75 years with LDL lvel of 70-189 & a 20% or greater 10-year risk of developing CV disease
at what kind of dose should you start a HMG-CoA reductase inhibitor?
start with a lower dose & increase as needed
When should HMG-Coa reductase inhibitors be given?
should be given in the evening/bedtime
What HMG-CoA reductase inhibitors can be given in the morning
rosuvastatin
atorvastatin
When should you checkk lipid panel when starting HMG-CoA reductase inhibitors?
4-6 weeks after starting
What is the most potent of the HMG-CoA reductase inhibitors?
rosuvastatin
What are the most common side effects of HMG-CoA reductase inhibitors?
CNS effects
- headahces
- dizziness
- insomnia
- fatigue
GI effects
- flatus
- abd pain
- N/V
- constipation
What should you avoid eating when taking a HMG-CoA reductase inhibitor?
grapefruit
What drug class can cause myopathy?
HMG-CoA reductase inhibitors
What drug class may cause rhabdomyolysis?
HMG-CoA reductase inhibitors
how can the risk of myopathy with HMG-CoA reductase inhibitors be reduced?
- reduced by using the lowest effective dose
- cautiously combine statins with fibrates
What can HMG-CoA increase?
liver enzymes
How do you manage the increase in liver enzymes with HMG-CoA reductase inhibitors?
- is dose-dependent
- serious liver problems are rare
- manage by reducing the dose or stopping until levels return to normal
What is a contraindication for HMG-CoA reductase inhibitors?
active liver disease
What drug class can cause coenzyme Q10 deficiency?
HMG-CoA reductase inhibitors
What causes oxidative stress & shredding of the blood vessels?
diabetes
smoking
HTN
dyslipidemia
obesity
aging
What does oxidative stress lead to?
endothelial dysfunction & reduced nitric oxide bioavailabilty
What does endothelial dysfunction & reduced nitric oxide bioavailability cause?
- leukocyte adhesion & inflammation
- lipid deposition
- vascular smooth muscle cell proliferation
- vasoconstriction
- platelet aggregation & thrombosis
What is the result of endothelial dysfunction & reduced nitric oxide availability?
progression of atherosclerosis & CV disease
How do cholesterol absorption inhibitors work?
work in the small intestine to inhibit the absorption of cholesterol
What are indications for cholesterol absorption inhibitors?
- lower serum cholesterol levels
- those who can not tolerate statins
Can cholesterol absorption inhibitors be given in combination with statins?
yes
What are the adverse effects of cholesterol absorption inhibitors?
- abd pain & diarrhea (most common)
- upper airway infections
- arthralgias
What are contraindications for cholesterol absorption inhibitors?
- allergy
pregnancy & lactation
What are PCSK9s?
proteins produced by the liver; play a role in regulating LDL
Who are PCSK9 ibhibitors often reserved for?
people who have very high LDL levels or those who cannot tolerate statins
What are PCSK9 inhibitors often used in conjunction with?
statins
How do PCSK9 inhibitors affect LDL, cholesterol & triglycerides?
they decrease LDL, cholesterol & triglycerides
What medications are monoclonal antibodies?
PCSK9 inhibitors
How are PCSK9 inhibitors administered?
administration by SQ injection, either weekly or monthly
What are the side effects of PCSK9 inhibitors?
itching, swelling, pain or bruising at the injection site
how do bile acid sequestrants work?
- bind with cholesterol in the intestine; the complex can not be absorbed; and is excreted in the stool
- by promoting an increase in bile acid excretion, they enhance the conversion of cholesterol to bile acids by the liver
Can bile acid sequestrants be used in those with active liver disease?
yes
What do bile acid sequestrants due to LDL, triglycerides & HDL?
- decrease LDL
- may increase triglycerides
- lightly increase HDL
What medication class has a strong record of efficacy & safety?
bile acid sequestrants
Are bile acid dequestrants used routinely?
no
can bile acid sequestrants be used in pregnancy?
yes
What can bile acid sequestrants be used with?
fibrates
What are the side effects of bile acid sequestrants?
constipation
abd pain
bloating
diarrhea
heartburn
gallstones
What can bile acid sequestrants inhbit that absorption of?
fat soluble vitamins (A,D,E, & K)
What is niacin also known as?
nicotinic acid or vitamin B3
How does niacin work?
- inhbits the release of free fatty acid from adipose tissue
- increases rate of triglyceride removal from plasma
How does niacin affect total cholesterol, triglycerides, LDL & HDL?
- lowers total cholesterol, triglycerides & LDL levels
- elevates HDL
When should niacin be given?
bedtime
What are the adverse effects of niacin?
- flushing
- nausea
- abd pain
- increase uric acid levels
- liver toxicity
What are drug interactions with niacin?
- alcohol
-statins - fibrates
What is often taken with niacin to help prevent flushing?
aspirin
How do fibrates work?
- inhibition of cholesterol & synthesis
- decreases triglyceride synthesis
- inhibition of lipolysis in adipose tissue
how do fibrates affect total cholesterol, triglycerides, LDL & HDL?
- lower total cholesterol, triglycerides, & LDL levels
- elevate HDL
How often are lipid levels monitored when taking fibrates?
in 4 to 6 weeks, then every 3 to 4 months
What are adverse effects of fibrates?
- flushing of face & neck
- increased uric acid levels
- increased risk of rhabdomyolysis(rare)
- GI tract
- headaches
What are drug interactions with fibrates?
warfarin
statins
What are omega 3 fatty acids derived from?
fish oil
How do omega 3 fatty acids affect triglycerides?
decreases triglyceride levels
What are side effects of omega 3 fatty acids?
- burping
- fishy taste
- diarrhea
- change in taste
What do omega 3 fatty acids decrease the risk of?
pancreatitis
high doses of what may interfere with blood clotting?
omega 3 fatty acids
What are the drugs that are omega 3 fatty acids?
lovera
vascepa
epanova
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