Anti-lipids Flashcards
macromolecular complexes in the blood that transport lipids
lipoproteins
proteins on surface of lipoprtoeins
apolipoproteins
enzyme that catalyzes rate-liming step in cholesterol
HMG-CoA reducttase
enzyme found on surface of endothelial cells that release free fatty acids from triglycerides
lipoprotein lipase
what transport cholesterol and TGs from GI tract to body
chylomicrons
TG-rich lipoproteins, precursor to LDL
VLDL
What can cause high cholesterol genetically?
- familial hypercholesterolemia
- familial hypertriglyceridemia
- familial combined hyperlipidemia
What are contributing conditions for HLD
DM, alcoholism, obesity, CKD, glucocorticoids, OCPs, cyclosporine
FLP
fasting lipid profile
- total cholesterol
- LDL
- HDL
- TGs
When do you start monitoring lipids?
20+ every 4-6 years, annually for higher risk patients
frequency based on family history
Friedwald equation to
calculate LDL
LDL = TC - (HDL+(tris/5))
not accurate when tris>400
Target lipid levels
LDL: <100
HDL >60
TGS <150
Target lifestyle
reduce saturated fats, increase omega-3s
at least 150min/week of exercise
weight loss
most common and effective drug class to decrease LDL, reduce inflammation, stabilize plaques
statins (HMG-CoA reductase inhibitors)
What medications inhibit cholesterol synthesis + bind circulating LDL, stabilize plaques, inhibit thrombus, anti-inflammatory?
statins
What are ADRs of statins?
headache, arthralgia, MYALGIA, fatigue, flu-llike symptoms, myopathy and rhabdomyolysis
hepatotoxicity (monitor LFTs - if high, then severe hepatotoxicity)
signs of damage/labs persist = jaundice, light stools, dark urine, hepatomegaly
What combo with statins are not good?
macrolides, cyclosporine, azole antifungals, HIV protease inhibitors, verapamil, gemfibrozil, niacin, amiodarone
What should you monitor with statins?
Cr and CK - check baseline + with symptoms
D/C drug if CK>19 x ULN
How do you treat statin myopathy?
CoQ-10
What are DDIs with statins?
grapefruit with atorvastatin, simvastatin, lovastatin (3A4)
rosuvastatin 2C9
pravastatin = no CYP450
What are CIs of statins?
- pregnancy (no in any child-bearing age)
- liver disease
- severe illness, trauma, surgery
What med:
- lowers LDL + TGs, increases HDL
- decreased hepatic production of VLDL -> less LDL + trigs
niacin (vitamin B3): nicotinic acid
What are ADRs of niacin
lots-
flushing (can take aspirin beforehand and avoid alcohol, spicy foods, hot showers/baths after taking)
hyperglycemia
hyperuricemia
GI upset
hepatotoxicity
What are CIs of niacin?
active or chronic liver disease, severe gout, caution in DM + PUD
How do you monitor niacin?
- LFTs baseline, q2-3 months for the first year, then periodically
LFTs >/3xUNL = discontinue - glucose + uric acid levels baseline, 6-8 weeks, yearly, adverse effects
What is a cholesterol absorption inhibitor that lowers absorption in intestine>
ezetimibe (zetia)
Should you add ezetimibe to statins?
yes
Consider ____ if maximum statin dose with <50% LDL goal or LDL >100
ezetimibe
What are ADRs of zetia?
monotherapy = URI, diarrhea, arthralgias, sinusitis
w/ statin = nasopharyngitis, myalgias, everything else
What are CIs of zetia?
avoid: cyclosporine, fibrates (increase)
separate administration: bile acid sequestrants (decrease)
What do you monitor with zetia?
LFTs, CK, adverse events
What med reduces LDL but can cause GI side effects?
bile acid sequestrants
- cholesytramine (questran)
- colesevelem (welchol)
- colestipol (colestid)
Binds bile acids in intestine + impedes reabsorption
decrease LDL by 15-30%
** triglycerides may increase **
bile acid sequestrants
When
<50% reduction in LDL on max statin or LDL > 70
zetia intolerant and triglycerides <300
add bile acid sequestrants
What are ADRs of bile acid sequestrants?
GI upset, N/V, bloating, constipation, abdominal pain
bile acid sequestrants have _____ DDIs
manyyyy - decreases absorption of other drugs - should be taken 4 hours before or after other drugs
activates lipoprotein lipase which leads to reduction in triglycerides, inducing synthesis of HDL
fibrates
What to use with hypertriglyceridemia >500
fibrates
gemfibrozil (lopid), fenofibrate (tricor)
What are ADRs of fibrates?
GI upset, gallstones, constipation, myalgia, increase in LFTs
What are CIs of fibrates?
- renal impairment (CrCL <30)
- hepatic impariment
- use caution w/ Hx of gallbladder disease
- monitor: LFTs at baseline, 3 months after, annually
What are DDIs of fibrates?
increased risk of rhabdomyolysis especially gemfibrozil (less with fenofibrate)
warfarin = increases bleeding risk
sulfonylureas = increase effect, MONITOR BS
What are PCSK9 inhibitors
praluent (alirocumab) and repatha (evolocumab) - SQ q2-4 weeks
Meds that inhibit PCSK9 from degrading LDL receptors
PCSK9 inhibitors
What can you add with patient <50% LDL reduction on max statin and LDL >70 and familial hypercholesteremia?
PCSK9 inhibitors
up to 60% reduction
What are ADRs of PCSK9 inhibitors?
nasopharyngitis, injection site reactions, back pain
- expensive, SQ injection, burdensome
Who should be treated?
1) ASCVD
2) LDL >/190
3) 40-75 w/ DM
4) LDL 70-189 w/ 10 year risk >7.5%
5) assess other risk factors
Lifestyle changes for
primary first line intervention
Statins are first line for
secondary prevention of CAD
