Hypolipidemics Flashcards
Niacin (Niaspan) Class
Nicotinic acid
Gemfibrozil (Lopid) Class
Fibric Acid Derivatives (Fibrates)
Fenofibrate (Tricor) Class
Fibric Acid Derivatives (Fibrates)
Cholestyramine (Questran) Class
Bile acid sequestrants
Colestipol (Colestid) Class
Bile acid sequestrants
Colesevelam (Welchol) Class
Bile acid sequestrants
Lovastatin (Mevacor) Class
HMG-CoA reductase Inhibitors (statins)
Simvastatin (Zocor) Class
HMG-CoA reductase Inhibitors (statins)
Pravastatin (Pravachol) Class
HMG-CoA reductase Inhibitors (statins)
Fluvastatin (Lescol) Class
HMG-CoA reductase Inhibitors (statins)
Atorvastatin (Lipitor) Class
HMG-CoA reductase Inhibitors (statins)
Rosuvastatin (Crestor) Class
HMG-CoA reductase Inhibitors (statins)
Ezetimbe (Zetia) Class
Inhibits enterocyte absorption of cholesterol in intestine
Niacin (Niaspan) MOA
Reduction of liver triglyceride synthesis, leading to less hepatic VLDL (thus, LDL) production; decreases lipolysis in adipose tissue, leading to lowered FFA transport to liver (thus, less triglycerides); reduced hepatic clearance of ApoAI (raising HDL)
Gemfibrozil (Lopid) MOA
Unknown; may interact w/peroxisome proliferator-activated receptor (esp. PPAR_) to stimulate LPL synthesis (enhance TG-rich lipoprotein clearance); inhibit apoC III expression (enhance VLDL clearance); stimulation of apoAI and apoAII (increase HDL)
Fenofibrate (Tricor) MOA
Unknown; may interact w/peroxisome proliferator-activated receptor (esp. PPAR_) to stimulate LPL synthesis (enhance TG-rich lipoprotein clearance); inhibit apoC III expression (enhance VLDL clearance); stimulation of apoAI and apoAII (increase HDL)
Cholestyramine (Questran) MOA
Very positively charged resins binds negative charged bile acids, inhibiting reabsorption and increasing cholesterol loss; leads to increase in LDL receptors in liver (to make more cholesterol), decreasing LDL in blood
Colestipol (Colestid) MOA
Very positively charged resins binds negative charged bile acids, inhibiting reabsorption and increasing cholesterol loss; leads to increase in LDL receptors in liver (to make more cholesterol), decreasing LDL in blood
Colesevelam (Welchol) MOA
Very positively charged resins binds negative charged bile acids, inhibiting reabsorption and increasing cholesterol loss; leads to increase in LDL receptors in liver (to make more cholesterol), decreasing LDL in blood
Lovastatin (Mevacor) MOA
Inhibits HMG-CoA reductase formation of mevalonate; leads to activation of SREBP, a membrane-bound transcription factor that increases LDL-R synthesis and lessens degradation; reduction in cholesterol decreases VLDL synthesis, lowering TG
Simvastatin (Zocor) MOA
Inhibits HMG-CoA reductase formation of mevalonate; leads to activation of SREBP, a membrane-bound transcription factor that increases LDL-R synthesis and lessens degradation; reduction in cholesterol decreases VLDL synthesis, lowering TG
Pravastatin (Pravachol) MOA
Inhibits HMG-CoA reductase formation of mevalonate; leads to activation of SREBP, a membrane-bound transcription factor that increases LDL-R synthesis and lessens degradation; reduction in cholesterol decreases VLDL synthesis, lowering TG
Fluvastatin (Lescol) MOA
Inhibits HMG-CoA reductase formation of mevalonate; leads to activation of SREBP, a membrane-bound transcription factor that increases LDL-R synthesis and lessens degradation; reduction in cholesterol decreases VLDL synthesis, lowering TG
Atorvastatin (Lipitor) MOA
Inhibits HMG-CoA reductase formation of mevalonate; leads to activation of SREBP, a membrane-bound transcription factor that increases LDL-R synthesis and lessens degradation; reduction in cholesterol decreases VLDL synthesis, lowering TG
Rosuvastatin (Crestor) MOA
Inhibits HMG-CoA reductase formation of mevalonate; leads to activation of SREBP, a membrane-bound transcription factor that increases LDL-R synthesis and lessens degradation; reduction in cholesterol decreases VLDL synthesis, lowering TG
Ezetimbe (Zetia) MOA
Decreases LDL-C alone (15-20%) or in combination w/statin (60%)
Niacin (Niaspan) Therapy
Best agent to increase HDL (30-40%); as good as fibrates and statins at lowering triglycerides (35-45%); lowers LDL (20-30%); hypertriglyceridemia and low HDL
Gemfibrozil (Lopid) Therapy
Marked reduction in VLDL (thus, triglycerides); variable and small effect on LDL; small increase in HDL (10%); severe hypertriglyceridemia
Fenofibrate (Tricor) Therapy
Marked reduction in VLDL (thus, triglycerides); variable and small effect on LDL; small increase in HDL (10%); severe hypertriglyceridemia
Cholestyramine (Questran) Therapy
Decrease LDL (25%), but slight increase (5%) in TG and HDL
Colestipol (Colestid) Therapy
Decrease LDL (25%), but slight increase (5%) in TG and HDL
Colesevelam (Welchol) Therapy
Decrease LDL (25%), but slight increase (5%) in TG and HDL
Lovastatin (Mevacor) Therapy
Reduce LDL (20-55%) and TG (25%), while increasing HDL (5-10%); treatment of dyslipidemia (reduces fatal & nonfatal CHD, strokes; total mortality reduction is 20%)
Simvastatin (Zocor) Therapy
Reduce LDL (20-55%) and TG (25%), while increasing HDL (5-10%); treatment of dyslipidemia (reduces fatal & nonfatal CHD, strokes; total mortality reduction is 20%)
Pravastatin (Pravachol) Therapy
Reduce LDL (20-55%) and TG (25%), while increasing HDL (5-10%); treatment of dyslipidemia (reduces fatal & nonfatal CHD, strokes; total mortality reduction is 20%)
Fluvastatin (Lescol) Therapy
Reduce LDL (20-55%) and TG (25%), while increasing HDL (5-10%); treatment of dyslipidemia (reduces fatal & nonfatal CHD, strokes; total mortality reduction is 20%)
Atorvastatin (Lipitor) Therapy
Reduce LDL (20-55%) and TG (25%), while increasing HDL (5-10%); treatment of dyslipidemia (reduces fatal & nonfatal CHD, strokes; total mortality reduction is 20%)
Rosuvastatin (Crestor) Therapy
Reduce LDL (20-55%) and TG (25%), while increasing HDL (5-10%); treatment of dyslipidemia (reduces fatal & nonfatal CHD, strokes; total mortality reduction is 20%)
Ezetimbe (Zetia) Therapy
Inhibits cholesterol absorption by enterocytes in jejunum (70% in mice), leading to less cholesterol in chylomicrons; reduction in chylomicron remnant cholesterol delivery to liver; may also decrease atherogenesis directly (remnants very atherogenic)
Niacin (Niaspan) ISE
Flushing, pruritis of face and upper trunk, rashes, acanthosis nigricans (hyperpigmentation)
Gemfibrozil (Lopid) ISE
Potentiate oral anticoagulants (displace from albumin), increase bile lithogenicity (less than clofibrate); myositis flu-like syndrome in 5%, other effects in 10% (not serious)
Fenofibrate (Tricor) ISE
Potentiate oral anticoagulants (displace from albumin), increase bile lithogenicity (less than clofibrate); myositis flu-like syndrome in 5%, other effects in 10% (not serious)
Cholestyramine (Questran) ISE
Very safe (only hypolipidemic indicated for children) because not systematically absorbed; impairs fat soluble vitamin absorption; binds other drugs (e.g., cardiac glycosides, coumarins)
Colestipol (Colestid) ISE
Very safe (only hypolipidemic indicated for children) because not systematically absorbed; impairs fat soluble vitamin absorption, binds other drugs (e.g., cardiac glycosides, coumarins)
Colesevelam (Welchol) ISE
Very safe (only hypolipidemic indicated for children) because not systematically absorbed; impairs fat soluble vitamin absorption, binds other drugs (e.g., cardiac glycosides, coumarins)
Lovastatin (Mevacor) ISE
Very few; hepatic dysfunction in 1% (serious hepatotoxicity rare); myopathy/rhabdomyolysis (reduced if factors inhibiting statin catabolism lacking)
Simvastatin (Zocor) ISE
Very few; hepatic dysfunction in 1% (serious hepatotoxicity rare); myopathy/rhabdomyolysis (reduced if factors inhibiting statin catabolism lacking)
Pravastatin (Pravachol) ISE
Very few; hepatic dysfunction in 1% (serious hepatotoxicity rare); myopathy/rhabdomyolysis (reduced if factors inhibiting statin catabolism lacking)
Fluvastatin (Lescol) ISE
Very few; hepatic dysfunction in 1% (serious hepatotoxicity rare); myopathy/rhabdomyolysis (reduced if factors inhibiting statin catabolism lacking)
Atorvastatin (Lipitor) ISE
Very few; hepatic dysfunction in 1% (serious hepatotoxicity rare); myopathy/rhabdomyolysis (reduced if factors inhibiting statin catabolism lacking)
Rosuvastatin (Crestor) ISE
Very few; hepatic dysfunction in 1% (serious hepatotoxicity rare); myopathy/rhabdomyolysis (reduced if factors inhibiting statin catabolism lacking)
Ezetimbe (Zetia) ISE
None (rare allergies)
Niacin (Niaspan) OSE
Hepatotoxicity, hyperuricemia, hyperglycemia; dyspepsia/reactivation of peptic ulcer disease; rarely, toxic ambylopia, tachyarrhythmias, a-fib (in elderly) and myopathy
Colestipol (Colestid) OSE
Bloating, dyspepsia, constipation, gritty/unpleasant taste
Colesevelam (Welchol) OSE
Bloating, dyspepsia, constipation, gritty/unpleasant taste
Niacin (Niaspan) Misc
Water soluble B vitamin complex at [low]; hypolipidemic at [high]; side effects limit compliance (<50% eligible patients follow on it); contraindicated in DM and gout patients; prevent flushing and pruritus with ASA
Gemfibrozil (Lopid) Misc
Combination w/statin inadvisable due to higher myositis risk
Fenofibrate (Tricor) Misc
Combination w/statin inadvisable due to higher myositis risk
Cholestyramine (Questran) Misc
Contraindicated in hypertriglyceridemia; no longer prescribed
Colestipol (Colestid) Misc
Standard treatment in combo w/statin; contraindicated in hypertriglyceridemia
Colesevelam (Welchol) Misc
Standard treatment in combo w/statin; contraindicated in hypertriglyceridemia
Lovastatin (Mevacor) Misc
Lactone prodrug (modified in liver to hydroxy acid form); must be taken in evening; Advicor = niacin + lovastatin
Simvastatin (Zocor) Misc
Lactone prodrug (modified in liver to hydroxy acid form); must be taken in evening; Vytorin = ezetemibe + simvastatin
Pravastatin (Pravachol) Misc
Must be taken in evening
Fluvastatin (Lescol) Misc
Must be taken in evening
Atorvastatin (Lipitor) Misc
Due to longer half-life, can be taken anytime per day
Rosuvastatin (Crestor) Misc
Due to longer half-life, can be taken anytime per day
Ezetimbe (Zetia) Misc
Long-term decrease in endpoints not seen yet (questionable effectiveness)
