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Drug Treatment for Lipid Disorders
AgentMechanism of ActionDosageBenefitsSide EffectsNotes
Colestipol (Cholestid)Interrupts bile acid reabsorption requiring bile acid synthesis from cholesterol2 scoops bid or tid. (Use bulk form). Begin with 1 scoop in a.m. 30 minutes before meal, increase to bid, then to 2 scoops bidNonabsorbed with long-term safety established. LDL cholesterol lowering 10%-15% (LRC-CPPT)Taste/texture, bloating, heartburn, constipation, drug interaction (avoidable by administration of drugs 1 hour before or 4 hours after) and triglyceride increaseDrug of choice for LDL cholesterol lowering in children and in women with childbearing potential. Often used as second line drug with statins because it acts synergistically to induce LDL receptors. Do not use in patients with triglycerides >300 or those with GI motility disorders
Colesevelam hydrochloride (WelChol)Interrupts bile acid reabsorption requiring bile acid synthesis from cholesterolThree 625-mg tablets bid (3.8 g total). 3 tablets with breakfast and 3 tablets with dinnerNonabsorbed with long-term safety established. LDL cholesterol lowering 10%-15% (LRC-CPPT)Taste/texture, bloating, heartburn, constipation, drug interaction (avoidable by administration of drugs 1 hour before or 4 hours after) and triglyceride increaseDrug of choice for LDL cholesterol lowering in children and in women with childbearing potential. Often used as second line drug with statins because it acts synergistically to induce LDL receptors. Do not use in patients with triglycerides >300 or those with GI motility disorders
Ezetimibe (Zetia)Selectively inhibits the intestinal absorption of cholesterol and related phytosterols10 mg qdDecreases the delivery of intestinal cholesterol to the liver, thereby reducing hepatic cholesterol stores and increases the clearance of cholesterol from the blood rather than inhibiting cholesterol synthesis. Reduces LDL by 18%, triglycerides by 8%, and apolipoprotein B by 16%Well tolerated with few adverse reactions similar to placeboCan use in combination with statins; however, contraindicated in patients with active liver disease or elevated LFTs. When used in combination with statins, yields an additional LDL reduction of 12%, an increase in HDL of 3%, and a triglyceride reduction of 8% (63). Statin plus ezetimibe yields a total LDL reduction of 25.8% (62; 64). Do not use in combination with resins, fibrates, warfarin, or cyclosporine. May take at the same time as statin (65)
Ezetimibe and simvastatin (Vytorin)Combination of intestinal absorption blocker and statin. Both selectively inhibits the intestinal absorption of cholesterol and partially inhibits HMG-CoA reductaseEzetimibe: 10 mg/simvastatin: 10, 20, 40, or 80 mg qhsCombination therapy fosters patient adherence with dosing. Synergistic benefits of both inhibition of intestinal cholesterol absorption by 54% and statin LDL lowering of 45%-60% depending on doseAbnormal LFTs, myositis/myalgiasContraindicated in patients with active liver disease or elevated LFTs, pregnant patients, and nursing mothers. Do not use in combination with gemfibrozil, other fibrates, >1 g niacin, amiodarone, or verapamil due to an increased risk of myopathy
Gemfibrozil (Lopid)Reduces VLDL synthesis and induces lipoprotein lipase600 mg bidBest triglyceride-reducing drugs, lowers 50% or more in many patients. Raises HDL 15%. Reduces CHD events by 24% in patients with low HDL, high triglycerides (Helsinki, VA-HIT)Nausea and skin rashDoes not lower LDL cholesterol reliably, or LDL cholesterol may increase in one-third of patients. Use in combination therapy with statins cautiously due to increased incidence of myositis/myalgias. Alters statin metabolism and causes an increase in statin plasma concentration (66). Use with caution in patients with renal insufficiency and gallbladder disease. Use with repaglinide (Prandin) may cause prolonged severe hypoglycemia
Fenofibrate (Tricor, Antara, Triglide, Lipofen, Lofibra)Reduces VLDL synthesis and induces lipoprotein lipaseTricor: 48, 145 mg/d
Antara: 43, 87, 130 mg/d
Lofibra: 54, 67, 134, 160, 200 mg/d
Best triglyceride-reducing drugs, lowers 50% or more in many patients. Raises HDL 15%. Reduces CHD in patients with low HDL, high triglycerides (Helsinki, VA-HIT)Nausea and skin rash.Does not lower LDL cholesterol reliably or LDL cholesterol may increase in one-third of patients. Used in combination therapy in combined hyperlipidemia. Need to use cautiously with statins, due to increased myositis/myalgias. Use with caution in patients with renal insufficiency and gallbladder disease
Atorvastatin (Lipitor)Partially inhibits HMG-CoA reductase, the rate-limiting step of cholesterol synthesis. This induces LDL receptor formation and removal of LDL cholesterol from blood 10-80 mg qdWell-studied for safety and efficacy in many trials. Lowers LDL cholesterol 20%-60% depending on dose and drugs. Raises HDL cholesterol 5%-10%; however, at higher doses (>=40 mg), can lower HDL cholesterol. Lowers triglycerides 15%-25%Abnormal liver function tests, myositis/myalgias Drug of choice for elevated LDL cholesterol based on safety and efficacy. Intensive lipid lowering with 80 mg of atorvastatin in patients with CHD provides significant benefit (percent reduction in CHD events) compared to 10 mg (67). Liver function abnormalities less common than previously thought. The 6 statins have different metabolism allowing substitution if side effects occur. Used in combination with bile acid binding resins to synergistically lower LDL cholesterol. Used in combination with niacin and fibrates in patients with combined hyperlipidemia. Use cautiously in patients on fibrates due to increased risk of myalgia/myositis
Amlodipine and atorvastatin (Caduet)
 
Amlodipine: 10, 20, 40, or 80 mg/atorvastatin: 5 or 10 mg qdCombination therapy fosters patient adherence with dosing. Treats both lipid disorder and hypertension concomitantly using a statin and calcium channel blockerEdema, dizziness, headache, flushing, and palpitationsDo not use in patients with congestive heart failure or severe aortic stenosis
Fluvastatin (Lescol, Lescol XL)Partially inhibits HMG-CoA reductase, the rate-limiting step of cholesterol synthesis. This induces LDL receptor formation and removal of LDL cholesterol from blood20-40 mg qhs
80 mg qhs (XL)
Well studied for safety and efficacy in many trials. Lowers LDL cholesterol 20%-30% depending on dose and drugs. Raises HDL cholesterol 5%-10%. Lowers triglycerides 15%-25%Abnormal LFTs, myositis/myalgiasDrug of choice for elevated LDL cholesterol based on safety and efficacy. Liver function abnormalities less common than previously thought. The 6 statins have different metabolism allowing substitution if side effects occur. Used in combination with bile acid binding resins to synergistically lower LDL cholesterol. Used in combination with niacin and fibrates in patients with combined hyperlipidemia. Use cautiously in patients on fibrates, due to increased risk of myalgia/myositis
Niacin and lovastatin (Advicor)Combination product of both extended release niacin (niaspan) and statin (lovastatin)Niacin: 500 mg/lovastatin: 20 mg
Niacin: 2000 mg/lovastatin: 40 mg
qhs
Combination therapy fosters patient adherence with dosing. Lowers LDL cholesterol 30%-42%. Raises HDL cholesterol 20%-30%. Reduces triglycerides 32%-44% (68)Flusing, nausea, glucose intolerance, gout, LFT abnormalities, and elevated uric acid levels. Myositis/myalgiasDrug of choice for combined hyperlipidemia and for patients who require simplified dosing. May use a nonenteric coated aspirin taken 1 hour before evening dose along with a light snack to minimize flushing. Do not take with hot beverages
Lovastatin (Mevacor, Altoprev [extended release])Partially inhibits HMG-CoA reductase, the rate-limiting step of cholesterol synthesis. This induces LDL receptor formation and removal of LDL cholesterol from blood20-80 mg qhsWell-studied for safety and efficacy in many trials. Lowers LDL cholesterol 20%-60% depending on dose and drugs. Raises HDL cholesterol 10%. Lowers triglycerides 15%-25%. (4S, West of Scotland Coronary Prevention Study [WOSCOPS], CARE)Abnormal LFTs, myositis/myalgiasDrug of choice for elevated LDL cholesterol based on safety and efficacy. Liver function abnormalities less common than previously thought. The 6 statins have different metabolism allowing substitution if side effects occur. Used in combination with bile acid binding resins to synergistically lower LDL cholesterol. Used in combination with niacin and fibrates in patients with combined hyperlipidemia. Use cautiously in patients on fibrates, due to increased risk of myalgia/myositis
Pravastatin (Pravachol)Partially inhibits HMG-CoA reductase, the rate-limiting step of cholesterol synthesis. This induces LDL receptor formation and removal of LDL cholesterol from blood10-40 mg qhsWell-studied for safety and efficacy in many trials. Lowers LDL cholesterol 20%-40% depending on dose and drugs (28% decrease in LDL in the ALLHAT-LLT trial) (69). Raised HDL cholesterol 10%. Lowers triglycerides 15%-25%. (West of Scotland Coronary Prevention Study [WOSCOPS], CARE). Reduces the risk of major CHD events by 19%-24% in patients with diabetes (LIPID trial) (70)Abnormal LFT, myositis/myalgiasDrug of choice for elevated LDL cholesterol based on safety and efficacy. Liver function abnormalities less common than previously thought. The 6 statins have different metabolism allowing substitution if side effects occur. Used in combination with bile acid binding resins to synergistically lower LDL cholesterol. Used in combination with niacin and fibrates in patients with combined hyperlipidemia. Use cautiously in patients on fibrates, due to increased risk of myalgia/myositis
Aspirin and pravastatin (Pravigard PAC)
 
Aspirin: 81 or 325 mg/pravastatin: 20, 40, or 80 mg qhs
 
 
 
Rosuvastatin (Crestor)Partially inhibits HMG-CoA reductase, the rate-limiting step of cholesterol synthesis. This induces LDL receptor formation and removal of LDL cholesterol from blood5-40 mg qhsEffective in lowering LDL cholesterol 45%-63% depending on dose and drugs. Raises HDL cholesterol 8%-14%. Lowers triglycerides 10%-35% (STELLAR trial) (71)Abnormal LFTs, myositis/myalgiasNewest of the 6 statins and therefore not as heavily studied in clinical trials to date; however, numerous industry trials have been conducted. Do not coadminister with warfarin or gemfibrozil. May be coadministered with fenofibrate and bile acid-binding resins to synergistically lower LDL cholesterol
Simvastatin (Zocor)Partially inhibits HMG-CoA reductase, the rate-limiting step of cholesterol synthesis. This induces LDL receptor formation and removal of LDL cholesterol from blood5-80 mg qhsWell-studied for safety and efficacy in many trials. Lowers LDL cholesterol 20%-60% depending on dose and drugs. Raises HDL cholesterol 10%. Lowers triglycerides 15%-25%. (4S)Abnormal LFTs, myositis/myalgiasDrug of choice for elevated LDL cholesterol based on safety and efficacy. Liver function abnormalities less common than previously thought. The 6 statins have different metabolism allowing substitution if side effects occur. Used in combination with bile acid binding resins to synergistically lower LDL cholesterol. Used in combination with niacin and fibrates in patients with combined hyperlipidemia. Use cautiously in patients on fibrates, due to increased risk of myalgia/myositis
NiacinLargely unknown. Reduces hepatic production of B-containing lipoproteins, increases HDL cholesterol production500 mg to 1 g tidLowers LDL cholesterol and triglycerides 10%-30%. Most effective drug at raising HDL cholesterol (25%-35 %). Long term efficacy studies (CDP)Flushing, nausea, glucose intolerance, gout, LFT abnormalities, and elevated uric acid levels. May potentially increase homocysteine levels.Drug of choice for combined hyperlipidemia and in patients with low HDL cholesterol. Extended release preparations limit flushing and LFT abnormalities. OTC long-acting niacin preparations are not recommended, as they increase the incidence of hepatotoxicity. Also lowers lipoprotein (a). Used in combination with statins or bile acid binding resins in combined hyperlipidemia. To minimize flushing, a nonenteric coated aspirin can be taken 1 hour before evening dose along with a light snack. Do not take with hot beverages such as tea or coffee
Niacin
Niaspan extended release
Largely unknown. Reduces hepatic production of B containing lipoproteins, increases HDL cholesterol production500 mg to 2 g qhsLowers LDL cholesterol and triglycerides 10%-30%. Most effective drug at raising HDL cholesterol (25%-35%). Long term efficacy studies (CDP)Flushing, nausea, glucose intolerance, gout, LFT abnormalities, and elevated uric acid levels. May potentially increase homocysteine levelsDrug of choice for combined hyperlipidemia and in patients with low HDL cholesterol. Extended release preparations limit flushing and LFT abnormalities. Also lowers lipoprotein (a). Used in combination with statins or bile acid binding resins in combined hyperlipidemia. To minimize flushing, a non-enteric coated aspirin can be taken 1 hour before evening dose along with a light snack. Do not take with hot beverages such as tea or coffee
Omega-3 polyunsaturated fatty acids (Lovaza)Inhibits hepatic triglyceride synthesis and augments chylomicron triglyceride clearance secondary to increased activity of lipoprotein lipase4 g/d (4 tablets)Effective in controlling triglyceride levels up to 45%. Raises HDL 13%Dyspepsia, nauseaCan increase LDL in some patients with hypertriglyceridemia. May increase bleeding time; therefore, use with caution in patients receiving anticoagulant therapy


ALLHAT-LLT = Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial; bid = twice daily; CARE = Cholesterol and Recurrent Events; CHD = coronary heart disease; GI = gastrointestinal; HDL = high-density lipoprotein; HMG-CoA = 3-hydroxy-3-methylglutaryl coenzyme A; LDL = low-density lipoprotein; LFT = liver function test; LIPID = Long-Term Intervention with Pravastatin in Ischaemic Disease; LRC-CPPT = Lipid Research Clinics Coronary Primary Prevention Trial; OTC = over the counter; qd = once daily; qhs = every night; STELLAR = Statin Therapies for Elevated Lipid Levels compared Across doses to Rosuvastatin; tid = three times daily; VA-HIT = Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial; VLDL = very-low-density lipoprotein.