The Wellness Center Staff
This month, we feature a four-part series on cholesterol to commemorate National Cholesterol Education Month. When changes to diet and lifestyle are not enough to improve cholesterol levels, a medication might be necessary. This fourth article describes the medications that doctors routinely prescribe to modify cholesterol levels.
Not all lipid altering drugs have the same mechanism of action. Some lower undesirable lipids like LDL or “bad” cholesterol and triglycerides. Others increase desirable lipids like HDL or “good” cholesterol.
The drug(s) your doctor prescribes will depend on a number of factors including your current cholesterol levels and risk factors for cardiovascular disease. These risk factors include high cholesterol, high blood pressure, diabetes, excess weight, family history of heart disease, physical inactivity, heavy alcohol use, age, smoking, poor stress and anger management and peripheral vascular disease (narrowing of arteries in neck, arms and legs).
Classes of Lipid Altering Medications
Several classes of medications are available that improve cholesterol levels including statins, nicotinic acid, fibric acid derivatives, bile acid sequestrants and cholesterol absorption inhibitors. Each drug class is explained in greater detail below.
Statins (HMG-CoA reductase inhibitors) – As the most commonly prescribed class of lipid altering drugs, statins are most effective in lowering LDL levels. Large clinical trials have demonstrated that statins reduce heart attacks and strokes and improve survival. Statins are mildly effective in lowering triglycerides and mildly effective in increasing HDL. Statins work by blocking the enzyme in the liver that is responsible for making cholesterol. This enzyme is called hydroxy-methylglutaryl-coenzyme A reductase or HMG-CoA reductase for short. Brand names include Lipitor, Crestor, Zocor, Pravachol and Mevacor.
Nicotinic Acid – More commonly known as niacin, a type of B-vitamin, prescription based nicotinic acid is most effective in increasing HDL levels. Nicotinic acid can raise “good” cholesterol by 15 to 35 percent. It is effective in lowering trigylceride levels and just mildly to modestly effective in lowering LDL. Although niacin is available in foods, high doses of nicotinic acid per day are needed (1-3 grams) to alter cholesterol levels. To prevent skin flushing – a common occurrence when this B-vitamin is taken in high doses – sustained release nicotinic acid is available. Brand names include Niaspan, Niacor and Slo-Niacin.
Statin/Nicotinic Acid – Combines both a statin and nicotinic acid into one medication. Effective in lowering LDL and triglycerides while increasing HDL. Brand names include Advicor (Mevacor plus Niaspan).
Fibric Acid Derivatives – Fibric acid or fibrates are most effective in lowering triglycerides and are effective in increasing HDL. Fibrates lower triglyceride levels by inhibiting the production of Very Low Density Lipoprotein (VLDL) and accelerating the removal of triglycerides. They are minimally effective in lowering LDL. Brand names include Lopid and Tricor.
Bile Acid Sequestrants – Bile acid sequestrants are mildly to modestly effective in lowering LDL but have no effect on HDL and triglyceride levels. This medication binds bile acids in the intestine which results in more bile acids being eliminated in the stool. With fewer bile acids available after digestion, production is promoted in the liver. Since the liver converts cholesterol into bile acids, the result is a reduction in the amount of circulating cholesterol in the blood. Brand names include Questran, Welchol and Colestid.
Cholesterol Absorption Blockers – These medications work by blocking the absorption of cholesterol from the intestines. Cholesterol absorption blockers are mildly to modestly effective in lowering LDL but have no effect on HDL and triglyceride levels. Brand names include Zetia.
Statin/Absorption Inhibitor – Combines both a stain plus an absorption blocker to lower LDL. The advantage is that a lower dose of each drug is combined into one pill which helps to reduce side-effects. Brand names include Vytorin (Zocor plus Zetia).
Side-Effects of Statins
If your doctor prescribes a statin, you should expect that you will remain on this drug indefinitely. That is why altering your cholesterol levels first by improving your diet and lifestyle is worth trying. See Dietary & Lifestyle Modifications to Improve Cholesterol .
Although statins are very effective in lowering LDL levels, and are well-tolerated by most people, their use can cause side-effects. These include muscle and joint aches, which are the most common, but also nausea, diarrhea and constipation.
Two more serious side-effects of taking statin drugs include extreme muscle pain and liver damage. To check for liver problems, a liver enzyme test is conducted periodically. Muscle pain is more likely at higher doses. Your doctor may reduce or switch your medication if your liver enzymes are high or you are experiencing muscle pain and tenderness.
As it turns out, the same enzyme suppressed by statin drugs is also responsible for manufacturing a compound called Coenzyme Co10 or CoQ10. As a result, the use of statin drugs depletes the body’s natural store of this compound. CoQ10 plays a critical role in the reactions that generate energy within the body’s cells. Some studies have demonstrated that CoQ10 supplementation can alleviate some of the common side-effects associated with statin use such as muscular pain, weakness, fatigue and exhaustion. Typical dosing is 100 mg of CoQ10 per day.
A note of caution – if you’re taking a statin drug, you should avoid drinking grapefruit juice. A compound in grapefruit juice called narijenin interferes with the breakdown of statins in the liver. This results in more concentrated levels of the drug, leading to serious problems or a greater likelihood of the well-known side-effects to occur.
Finally, if you’re taking St. John’s Wort to relieve mild to moderate depression, this botanical can decrease the level of several statin drugs including Mevacor, Altocor and Zocor.
Children and Statin Drugs
A study published in the February 2009 issue of Circulation revealed that about 200,000 U.S. teens and preteens need to lower their cholesterol levels.
Researchers examined data from a large national survey and found that 5.2 percent to 6.6 percent of adolescents had high LDL or “bad” cholesterol and 9.6 percent to 10.7 percent had high total cholesterol. Based on their numbers, these kids met the guidelines for taking statin drugs.
Putting an adolescent or preteen on a statin drug remains controversial. However, the issue of reducing their cholesterol levels remains. Given that children learn eating habits at a very young age, it is imperative that parents intervene early to modify their kids’ eating and lifestyle habits.
The dietary and lifestyle changes that are recommended for adults are the same for kids – lose extra pounds, get more physical, eat more fruits & vegetables, and reduce consumption of saturated, partially-hydrogenated and trans-fats. By making these health promoting changes, our youth will reduce their risk of developing cardiovascular and other chronic disease in early adulthood.