16. DSA Drugs used for Lipid Disorders Flashcards
All of the following are what type of drugs for lipid disorders? Atorvastatin Fluvastatin Lovastatin Pitavastatin Pravastatin Rosuvastatin Simvastatin
HMG-CoA Reductase Inhibitors (statins)
All of the following are what type of drugs for lipid disorders?
Known as nicotinic acid/vitamin B3
Niacin
All of the following are what type of drugs for lipid disorders?
Fenofibrate
Gemfibrozil
Fibric Acid Derivatives (Fibrates)
All of the following are what type of drugs for lipid disorders?
Cholestyramine
Cholesevelam
Colestipol
Bile Acid Sequestrants (Resins)
All of the following are what type of drugs for lipid disorders?
Ezetimibe
Cholesterol Absorption Inhibitors
All of the following are what type of drugs for lipid disorders? Lomitapide Mipomersen Evolocumab Alirocumab
New treatments
The statins are most effective at reducing LDL and the best tolerated class of lipid lowering agents. What is the MOA?
they are structural analogs of HMG-CoA and inhibit HMGCoA reductase which is the rate limiting enzyme in cholesterol synthesis
What it the potency of the statins?
Atorvastatin=rosubastatin> simvastatin > pitavastatin = lovastatin = pravastatin > ?
Fluvastatin
use in atherosclerotic valvular dz/ acute coronary syndromes
Niacin decrease TGs, LDL, Lp(a) lipoproteinA and increases?
HDL
use for statin intolerant pts
The MOA of niacin is it inhibits lipolysis of TGs in adipose tissue, by reducing free fatty acids- liver produces less VLDL and?
LDL levels decrease, catabolic rate for HDL decreased
Gemfibrozil and Fenofibrate (fibric acid derivatives) are well absorbed. Which has a longer half life?
gemfibrozil has 1.5hrs
Fenofibrate is 20hrs
Fibrates MOA : they are agonists for peroxisome proliferator activated receptor alpha (PPARa - nuclear receptor), activation binds to DNA regulating expression of APO binding proteins. Leads to VLDL decrease, LDL decrease, and HDL?
increases moderately (inc. lipolysis of TGs = decrease plasma TG)
use in low HDL or hyperTG
Fibrates are useful in the management of hypertriglyeridemias where VLDL predominates, dystbetalipoproteinemia and hypertriglyceridemia that resutls from treatment with?
viral protease inhibitors
Bile acid sequestrants (resins): cholestipol, cholestyramine, and colesevelam are cationic (negative) exchange resins which bind to positively charged compounds and cause an increase in the up take of?
bile acid excretion 10 fold
Bile acid sequestrants are used to treat pts with primary hypercholesterolemia (*dec. LDL), also used to relieve pruritis in patients with bile salt?
accumulation (from obstruction)
Cholesterol absorption inhibitors such as ezetimibe block sterol transporter NPC1L1 in intestine brush border, inhibiting reabsorption of cholesterol excreted in bile, decreases LDL and phytosterols.. Good for what clinical sitch?
Elevated LDL
Phytosterolemia (characterized by hyperabsorption and decreased biliary excretion of dietary sterols)
What drugs are best to decrease LDLs?
Statins
What drugs are best to increase HDL, and the worst?
Best HDL: Niacin
Worst HDL: Bile acid
What drugs work best to decrease TGs and VLDL?
Fibrates (gemofibrozil and fenofibrate)
PCSK9 inhibitors such as (evolocumab), complec with PCSK9 and inhibit catabolism of LDL receptor. Increasing LDL receptors, decreasing LDL, Best for what situation?
Familial hypercholesterolemia not responsive to oral therapy
What is a common side effect of statins?
can cause myopathy - proximal muscle weakness and soreness (cant raise arms above head)
Which statin is the only statin that is not metabolized in the liver by CYP450?
Pravastatin
Cholestyramine, colestipol, colesevam (bile acid binding resins) causes hypertriglycemia (inc. VLDL) and can also cause constipation, bloating and?
gall stones
Common side effects of ezetimibe (cholesterol absorption inhibitor) is diarrhea and an increase in?
Liver function tests
Common side effects of fibrates is when they are combined with statins can lead to myopathy, fibrates on their own can lead to cholesterol…?
gall stones
Common side effects of niacin is cutatneous flushing and warmth, hyperglycemia, hyperuricemia, as well as elevated…?
liver function tests