Drugs for lipid disorders Flashcards
the 2 fibrates dicussed are
gemfibrozil and fenofibrate
most potent statins
Atorvastatin and rosuvastatin are equal then simvastatin
what class of drugs predominately decreases VLDL
Fibrates
Adverse effects on muscle of statins?
- CK increase (high level of physical activity)
- Rhabdo –>renal injury and myoglobinuria
- myopathy
antisense oligonucleotide that targets apolipoprotein B-100 and used to treat homozygous familial hypercholesterolemia
Mipomersen
Due to the risk of developing gallstones, Fibrates should be used with caution in what individuals?
those with biliary tract disease or in those at high risk (women, obese pts, native americans)
Which statin is NOT metabolized by CYP450s
pravastatin and pitavastatin
drug interatction for fibrates?
coumadin and indanedione anticoagulants
What patients should you use bile acid resins cautiously
diverticulitis, preexisting bowel disease, or cholestatis
What agents that inhibit CYP450 should be avoided with statins unless its pravastatin and pitavastatin
- phenytoin
- griseofulvin
Ligand for PPAR-alpha
Fibrates
Expression of what is increased when fibrates bind to PPARalpha
lipoprotein lipase which then causes decreased concentration of triglycerides
Treatment of homozygous familial hypercholesterolemia that binds to MTP
lomitapide (SUPER EXPENSIVE)
What class of drugs are useful in treating hypertriglyceridemia that results from treatment with viral protease inhibitors?
fibrates
Ezetimibe inhibits cholesterol absorption through what?
NPC1L1
intense cutaneous flush accompanied by an uncomfortable feeling of warmth
Niacin
Statins that are inactive prodrugs that must be hyrolyzed in GI to activate
Lovastatin and simvastatin
Acts by inhibiting lipolysis of triglycerides in adipose tissue which reduces free fatty acids –>liver makes less VLDL–>lower LDL
Niacin
contraindications and cautious use for niacin
- Contraindication in hepatic disease or active peptic ulcer
- caution with DM –>causes insulin resistance and hyperglycemia
When are statins not recommended but not absolute contraindication
liver disease or skeletal muscle myopathy
What is the least potent statin?
fluvastatin
Adverse effects on liver of statins?
increase in aminotransferase (liver disease or alcohol use)
Which statins have an extraordinarily long half life of 14 and 19 hours as opposed to others of around 1-3
- Atorvastatin (14)
- Rosuvastatin (19)
What time of day should statins be given?
in evening because cholesterol is synthesized at night unless you use longer acting one like Atorvastatin or Rosuvastatin