Hypolipidemics Flashcards by Sarah Moore

Q

Niacin (Niaspan) Class

A

Nicotinic acid

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Q

Gemfibrozil (Lopid) Class

A

Fibric Acid Derivatives (Fibrates)

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Q

Fenofibrate (Tricor) Class

A

Fibric Acid Derivatives (Fibrates)

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Q

Cholestyramine (Questran) Class

A

Bile acid sequestrants

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Q

Colestipol (Colestid) Class

A

Bile acid sequestrants

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Q

Colesevelam (Welchol) Class

A

Bile acid sequestrants

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Q

Lovastatin (Mevacor) Class

A

HMG-CoA reductase Inhibitors (statins)

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Q

Simvastatin (Zocor) Class

A

HMG-CoA reductase Inhibitors (statins)

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Q

Pravastatin (Pravachol) Class

A

HMG-CoA reductase Inhibitors (statins)

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Q

Fluvastatin (Lescol) Class

A

HMG-CoA reductase Inhibitors (statins)

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Q

Atorvastatin (Lipitor) Class

A

HMG-CoA reductase Inhibitors (statins)

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Q

Rosuvastatin (Crestor) Class

A

HMG-CoA reductase Inhibitors (statins)

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Q

Ezetimbe (Zetia) Class

A

Inhibits enterocyte absorption of cholesterol in intestine

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Q

Niacin (Niaspan) MOA

A

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)

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Q

Gemfibrozil (Lopid) MOA

A

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)

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Q

Fenofibrate (Tricor) MOA

A

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)

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Q

Cholestyramine (Questran) MOA

A

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

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Q

Colestipol (Colestid) MOA

A

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

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Q

Colesevelam (Welchol) MOA

A

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

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Q

Lovastatin (Mevacor) MOA

A

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

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Q

Simvastatin (Zocor) MOA

A

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

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Q

Pravastatin (Pravachol) MOA

A

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

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Q

Fluvastatin (Lescol) MOA

A

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

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Q

Atorvastatin (Lipitor) MOA

A

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

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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)