MMT: lipid drugs Flashcards
What is the target LDL for someone with no risk factors?
Less than 100
What is the target LDL for someone with multiple risk factors?
Below 55 is ideal, but up to 70
What is the primary method of controlling lipid levels?
Making personalized lifestyle changes
What is a main target for lipid lowering drugs? What is the rationale?
LDL receptor cycling; LDLR cycling removes LDL and targets it for endocytosis, so promoting this helps reduce lipids
What are the drug targetable lipoprotein mechanisms?
- Decreasing cholesterol synthesis
- Increase LDLR endocytosis
- Decrease cholesterol absorption
- Increase reverse cholesterol transport
What is the MOA of statins?
They inhibit HMG CoA reductase which inhibits cholesterol synthesis, upregulating LDLR and increasing clearance of LDL
What are the primary results of statin treatment?
- Lower LDL
- Lower triglycerides
- Increased HDL
Statins are prescribed largely in which 3 scenarios?
- Following MI
- Acute coronary syndrome
- Stroke
Where are statins metabolized?
The liver
Of the statins, which has the longest half life?
Atorvastatin
What are side effects of statins?
Hepatotoxicity, myopathy, rhabdomyolysis, increasing blood glucose, cognitive impairment
Who is at risk for statin use?
Those with liver or kidney disease, alcoholics, those with hypothyroidism
What are contraindications of statins?
Pregnant or nursing mothers and children
What drug interactions with statins are present?
CYP3A4, inhibitors of p-glycoprotein, and fibrates
How can we minimize SE of statins?
Statin switching
If statin switching isn’t working, what is another option?
A moderate-low intensity statin combined with other treatments
What is ezetimibe?
A drug that inhibits ANPEP and NPC1 in the brush border of the intestine that changes the LDLR and blocks cholesterol absorption
What is the preferred adjunct to statin for additional lipid lowering?
Ezetimibe
What are bile acid binding resins?
They bind bile acids and wipe them out of the intestine. This results in cholesterol converting to bile acids.
How do bile acid binding resins impact lipids?
Lower LDL by raising LDLR, raise TGs, raise HDL
When are bile acid binding resins often used?
Children and pregnant women/women of reproductive ages
What are the examples of bile acid sequestrants?
Colesevelam, cholestyramine
What are contraindications of bile acid binding resins?
Hypertriglyceridemia, as the medication can raise TGs
What are PCSK9 inhibitors?
They inhibit LDLR degradation, resulting in a large decrease in LDL
What is bempedoic acid?
A lipid lowering drug that inhibits ATP citrate lyase, decreasing cholesterol synthesis and increasing LDLR
How does bempedoic acid impact lipids?
Lowers LDL, does not change triglycerides, lowers HDL
What are contraindications of bempedoic acid?
Pregnancy
What are fibrates?
Drugs that lower TGs by stimulating peroxisome pathway as well as increase HDL and lower LDL
What condition are fibrates first line for?
Hypertriglyceridemia
What are SEs of fibrates?
GI issues, gallstones, rhabdomyolysis, myositis
Why is fibrate not given with statins?
Increased risk for myopathy
What is niacin/nicotinic acid?
Inhibits lipolysis to decrease TGs and LDL, and slightly increases HDL
What results in a lowering of Lp(a)?
Nicotinic acid
What is a major SE of niacin treatment?
Flushing
What dietary supplement can be used as a lipid lowering agent? What is its impact?
Omega 3. Lowers TGs, raises HDL, raises LDL
What are the guidelines for lipid lowering therapies?
- Establish LDL goal based on risk
- Determine need for lifestyle changes
- Determine level for drug consideration
