The prescription agents for lipid and lipoprotein treatment fall into several broad categories. Click on any of the drugs in the table below to learn more.
PRESCRIPTION DRUG CLASS POTENTIAL BENEFIT
Statins Reduce LDL Cholesterol and Triglycerides. Increase HDL Cholesterol.
Zetia (ezetimibe) Reduce LDL Cholesterol.
Niacin Reduce LDL Cholesterol, Triglycerides, Lipoprotein(a), Increase HDL Cholesterol.
Bile Acid Resins Reduce LDL Cholesterol.
Fibrates Reduce Triglycerides, Increase HDL Cholesterol.
Thiazolidinediones Reduce Insulin Resistance
Pletal (cilostazol) Reduce LDL Cholesterol, Increase HDL Cholesterol
Experimental Drugs Under investigation
Statins
These are popular prescription drugs that lower LDL cholesterol up to 60% by increasing liver uptake of cholesterol particles. Triglycerides are also reduced moderately and HDL cholesterol increased a few points. Advantages: potency and convenience. Data consistently show a reduction in heart attack risk of about 30% over 5 years of treatment. There may be reductions in colon cancer, Alzheimer's, and stroke, as well. Side-effects include muscle damage and liver problems (evidenced by elevations in liver tests by blood draw) which occur in 1-2% of people. Much more commonly, vague muscle aches and weakness occur. The statin agents are, from most potent to least potent:
* Crestor (rosuvastatin)
* Lipitor(atorvastatin)
* Zocor (simvastatin)
* Pravachol (pravastatin)
* Mevacor (lovastatin)
* Lescol (fluvastatin)
The principal difference among the various agents is potency. For example, if your starting LDL cholesterol is 240 mg/dl, a potent agent will likely be required to reduce LDL to your target (usually 100 mg/dl or less; 60 mg/dl in the Track Your Plaque program). If your starting LDL is 135 mg/dl, then a less potent agent can be used effectively. Statins are often combined with other agents. For example:
* In the Track Your Plaque approach, a statin agent is frequently combined with niacin (usually as prescription Niaspan) because of the powerful synergistic effect of the combination, including reduction in heart attack risk of up to 90%.
* Advicor is a combination of a statin and niacin (see below).
* Caduet is a combination of atorvastatin and a blood pressure-lowering drug, Norvasc (amlodipine).
* Vytorin is a combination of atorvastatin and ezetimibe (see below).
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Zetia (ezetimibe)
Zetia is in a class of its own, though its method of action is closest to the bile acid resins (see below). Zetia blocks the absorption of cholesterol into the intestinal wall. When Zetia is prescribed by itself, LDL cholesterol is reduced around 18%, or about a third or half as potent as the statin agents. Zetia's greatest application is in combination with a statin drug. The therapeutic potency of a statin agent is tripled or quadrupled when combined with Zetia with a minimal increase in muscle ache risk. For this last reason, Zetia is a useful agent for Track Your Plaque participants for our lower target LDL cholesterol of 60 mg/dl, as well as our more aggressive lowering of apoprotein B/LDL particle number.
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Niacin
Niacin is vitamin B-3 and is an ingredient in multivitamins and food. At higher doses, however, it is an effective HDL-raising drug. Niacin also significantly lowers triglycerides, small LDL, VLDL, increases the proportion of healthy, large HDL, and is the first-line agent for reducing lipoprotein(a).
Side effects include hot flushing and itching, usually of the face, neck, and chest. Over-the-counter slow-release niacin should be avoided due to high risk of liver problems. Prescription niacin (Niaspan), and over-the-counter Slo-Niacin, as well as immediate-release niacin (non-slow-release) are very safe with minimal risk of liver problems. Immediate-release niacin, available in any health food store, is difficult to tolerate due to its marked tendency to cause the hot flush reaction. For this reason, when an agent is required to correct any of the above patterns, Niaspan or Slo-Niacin are the brands most commonly recommended to Track Your Plaque participants. Niacin is the most frequently used agent in Track Your Plaque, due to the very common low HDL and small LDL particle abnormalities. Niacin and fish oil can be a very effective combination for correction of excessive triglycerides, VLDL, intermediate-density lipoprotein (IDL), and small LDL. Combine this with weight loss (when appropriate), and full correction is nearly always achieveable. Niacin can be used safely in combination with the statin agents, though will require monitoring by your doctor.
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Bile Acid Resins
These drugs bind cholesterol in the intestine and prevent it from being reabsorbed into the circulatory system. Side effects are common and include gas, cramps, diarrhea, and constipation. Bile acid resins include:
* Questran and Questran Light (cholestyramine)
* Colestid (colestipol)
* WelChol (colesevelam)
The statin agents and Zetia have largely replaced these agents
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Fibrates
Fibrates reduce triglycerides and increase HDL cholesterol with a potency of roughly half that of niacin. Fibrates include:
* Tricor (fenofibrate)
* Lopid (gemfibrozil)
Side-effects are similar to that of the statin drugs. Clinical studies have demonstrated a reduction in heart attack risk of approximately 25% over 3-5 years of treatment. Risk of liver and muscle side-effects may be increased when these agents are used in combination with a statin agent.
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Thiazolidinediones
The thiazolidinediones, or TZD's, are actually diabetes agents to lower blood sugar modestly. They also represent a useful innovation in lipid and lipoprotein management because of their effects on reducing resistance to insulin, a crucial phenomenon in most diabetes and pre-diabetes. Improved sensitivity to insulin results in increased HDL, reduced triglycerides, reduction in small LDL and in some measures of inflammation (though these effects can be highly variable among individuals). The two available TZD's are:
* Actos (pioglitazone)
* Avandia (rosiglitazone)
Side-effects include edema (water retention) and weight gain (usually up to 5-8 lbs. in the first year of use). Insulin resistance and its associated phenomenon are extremely common, at least prior to weight loss efforts, and the TZD's have therefore been useful to address the multiple consequences of this increasingly common pattern.
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Pletal (cilostazol)
This prescription agent was originally intended for poor circulation to the legs (claudication), Pletal has proven very helpful to raise HDL cholesterol, often up to 30% or more. It also reduces small LDL quite effectively. Side-effects include headache and water retention. Because of the Track Your Plaque HDL goal of 60 mg/dl or greater, Pletal is a common part of our participants' program.
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Experimental Drugs
The following drugs are under investigation and will likely become available over the next five years
ETC-216: This investigational drug is actually a synthetic form of HDL cholesterol. Researchers discovered that a group of persons in Milan, Italy suffered few cardiac events despite very low HDL (good) cholesterol. It was determined that this group had a form of unique "super" HDL cholesterol. The drug was nicknamed "Drano for Arteries" after a group of test subjects was found to have a significant reduction in plaque after taking the drug for only five weeks. Learn More
Torcetrapib: This investigational drug is from a new class of drugs called Cholesteryl Ester Transfer Protein (CETP) inhibitors which dramatically increases HDL cholesterol. Early studies show increases in HDL of up to 91%. Unfortunately, this drug has recently been shelved after the final pre-release studies indicated it actually raised heart disease risk. This effect is currently thought to be due to a slight rise in blood pressure although this is not certain. Other CETP agents are still in early investigational stages. Learn More
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