1. Bile sequestrants
1.1. MOA: lower LDL-C by binding bile acids in the intestine preventing enterohepatic recirculation of bile acids ->
1.1.1. less cholesterol to liver->
1.1.1.1. increased LDL receptors -> lower LDL-C
1.2. drugs: cholestyramine, colestipol, colesevelam
1.2.1. colesevelam is BEST TOLERATED w/least effects
1.3. used for reducing LDL 15-30%
1.3.1. administered 2x/d w/meals
1.3.1.1. used in combo therapy and in women considering pregnancy
1.4. AE: GI, constipation, bloating, fullness, nausea, flatulence
1.4.1. lack systemic toxicity
1.4.1.1. Drug interactions: decreases absorption of other drugs, do not take at same time
1.5. CI: NOT IN PTS W/ HIGH TG levels
1.5.1. colesevalam and colestipol lower level teratogens, so cholestyramine for women considering pregnancy
2. Fibric acid derivatives (fibrates
2.1. MOA: complex but may be antagonists for nuclear transcription factor PPAR-alpha which alters transcription leading to decreased TG levels and secondary increases in HDL
2.2. Gemfibrozil, fenofibrate, clofibrate
2.3. PRIMARY USE to lower TG; TG decreased by 25-5-%
2.4. combo therapy w/statins to improve overall lipid profile
2.5. AE: GI m/c, increase cholelithiasis, renal exception, monitor INR in patients on warfarin; increased risk of myopathy w/statin and in renal pts
2.6. CI: cat C for pregnancy
3. nicotinic acid
3.1. MOA: inhibits production of VLDL by liver
3.1.1. increased HDL production by increasing Apo A I
3.1.1.1. inhibits free fatty acid release from adipose tissue
3.2. drugs include extended release nicotinic acid; crystalline
3.3. increases HDL by 15-35 % MOST EFFECTIVE TO DO THIS
3.3.1. used in combo or monotherapy
3.3.1.1. must monitor LFT, uric acid and fasting BS at baseline and 6-8 weeks after therapy
3.4. AE: flushing and HA; GI:nausea, dyspepsia, diarrhea; activation of PUD; hepatotoxicity; hyperuricemia; hyperglcemia;
3.4.1. dose dependent effects
3.4.1.1. given at bedtime to reduce AE
3.5. CI: avoid in peptic ulcer disease PUD, chronic liver disease, severe gout, DM/hyperuricemia
3.5.1. preg cat C; discontinue when nursing