September 2, 2014
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Cholesterol

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Using medication as directed

The lower your cholesterol levels, the better. As your "bad" cholesterol levels drop, so does your risk of developing heart disease and death. To get your cholesterol down low enough, you may need a prescription medication in addition to your healthy lifestyle changes. Here are the families of medications used to control cholesterol:

Medications have different effects and not everyone will respond the same way to medications. Ask your doctor if which medication is most appropriate for you.

Statins

Statins lower LDL-C and total cholesterol (on average, by as much as 60% and 40%, respectively), and raise HDL-C (on average, by as much as 10%). They may also lower triglycerides (TG) (on average, by as much as 18%).

Statins work by blocking cholesterol production in the liver. See Table 1 for a summary of the effects of statins on various types of cholesterol.

Table 1: Effects of statins on various types of cholesterol

Type of cholesterol Average effect
LDL cholesterol decrease by 60%
Total cholesterol (TC) decrease by 40%
HDL cholesterol increase by 10%
Triglycerides (TG) decrease by 18%

It's important to understand that the numbers listed in Table 1 are just averages. When it comes to lowering cholesterol, not all medications are the same. Some are better at lowering certain types of cholesterol, and others produce a larger cholesterol-lowering effect at lower doses than others.

Most people will be able to reach their cholesterol targets by taking a statin alone. In some cases, your doctor may decide to increase the dose, switch to a different medication, or start combination therapy (i.e., more than one medication). Statins may be combined with other cholesterol-lowering medications in the resin family or cholesterol absorption inhibitor family.

Statins available in Canada include atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin, and simvastatin.

The main side effects* of statins are mild stomach upset, headache, muscle soreness and, rarely, muscle pain. Side effects may be more likely for people taking higher statin doses or people who are already at risk of side effects due to their pre-existing medical conditions or other medications. Muscle pain, tenderness, or weakness may be a sign of muscle damage caused by these medications. Other signs include brownish or discoloured urine. People who notice muscle pain should see their doctor right away. Your doctor may suggest a simple blood test to investigate the muscle pain.

Pregnant or breast-feeding women should not use statins, as these medications may harm the baby. People with liver disease should not take statins, as they make liver damage worse. All people taking a statin need to have regular tests to check their liver function.

Since both statins and fibrates, another group of cholesterol-lowering medications, can cause muscle damage, they should only be used together with caution. Statins may also increase the effects of warfarin, a blood-thinning medication. Atorvastatin, lovastatin, and simvastatin also interact with erythromycin, cyclosporine, diltiazem, medications for people who are HIV-positive, and niacin. Fluvastatin interacts with cimetidine, ranitidine, omeprazole, and rifampin. Rosuvastatin should be taken 2 hours apart from antacids, and should not be taken with cyclosporine.

Consult your pharmacist or doctor if you are concerned that one of your medications may be interacting with your statin, and ask whether there is an alternative that does not interact.

Cholesterol absorption inhibitors

The cholesterol absorption inhibitor ezetimibe works by blocking cholesterol from being absorbed in the intestine. It may be used alone or along with a statin to lower total cholesterol, LDL-C, apoB, and TG and to increase HDL-C. It may also be used with fenofibrate to lower total cholesterol, LDL-C, non-HDL-C, and apoB.

Ezetimibe should not be used by people with severe liver disease. The effects of this medication during pregnancy are unclear, so pregnant women should not use it unless, in the opinion of their doctor, the benefits outweigh the risks. Children under 10 should not use ezetimibe.

The main side effects* are headache, abdominal pain, and diarrhea. Rarely, ezetimibe may also cause muscle pain. Muscle pain may be a sign of muscle damage caused by the medication. People who notice muscle pain should see their doctor right away. Your doctor may suggest a simple blood test to investigate the muscle pain. People with liver disease should be closely monitored by their doctors while taking ezetimibe, as this medication may cause liver damage.

Ezetimibe should not be used with fibrates other than fenofibrate. People taking cyclosporine (a medication taken after receiving an organ transplant) should have their cyclosporine levels checked if they are taking ezetimibe. People taking warfarin (e.g., Coumadin® and generics) should have their International Normalized Ratio (INR) levels checked more frequently if they are taking ezetimibe. People taking a resin (see below) should take it 2 hours before or 4 hours after ezetimibe. Otherwise, the resin will block ezetimibe from being absorbed into the body.

Resins

Resins lower LDL-C (on average, by up to 30%) and raise HDL-C (on average, by up to 3%). They work by decreasing the absorption of cholesterol and increasing the breakdown of LDL-C. The 3 resins available in Canada are cholestyramine, colesevelam, and colestipol.

The main side effects are constipation, bloating, gas, heartburn, diarrhea, nausea, headache, and a feeling of fullness. Resins also increase TG. People taking resins should have their liver function checked on a regular basis. Resins, on the advice of a physician, can be used to lower cholesterol for women who are pregnant and for children (over 2 years of age).

Resins can block the absorption of other medications and fat-soluble vitamins (vitamins A, D, E, and K). They should be taken 1 to 2 hours before or 4 hours after other medications.

Fibrates

Fibrates lower TG (on average, by up to 50%) and increase HDL-C (on average, by up to 30%). Some fibrates (such as bezafibrate and fenofibrate) also lower LDL-C (on average, by up to 10%).

There are 3 fibrates available in Canada: bezafibrate, fenofibrate, and gemfibrozil. They work by blocking cholesterol production and increasing cholesterol breakdown.

The main side effects* are nausea, abdominal pain, gas, and muscle aches. People taking a fibrate should have their liver and kidney functions checked on a regular basis. People with poor kidney function may need a lower dose. Fibrates can increase the effects of blood thinners, such as warfarin. Gemfibrozil increases the blood levels of most statins and may greatly increase the risk of muscle damage if taken with a statin. Also, because both statins and fibrates can cause muscle damage, the risk of muscle damage may be higher when these medications are taken together.

Niacin

Niacin is a type of vitamin B that raises HDL cholesterol levels and lowers triglyceride levels when taken in high doses. Doses of 1,000 mg to 2,000 mg per day can increase HDL cholesterol levels by 25% and lower triglyceride levels by 30% to 40%. Because niacin causes flushing, itching, and tingling in many people, your doctor will likely recommend that you start at a low dose and increase it slowly over time to build up your tolerance to this effect.

Although niacin is available without a prescription, it is always best to talk with a doctor first if you are planning to use it to treat your cholesterol. Be careful not to choose niacinamide to treat cholesterol; it is a relative of niacin but does not have the same effect on cholesterol.

In addition to flushing, itching, and tingling, side effects* of niacin include headache, nausea, gas, heartburn, and rash. With the use of niacin, blood sugar levels should be monitored carefully by people with diabetes when first starting the medication, and liver tests should be performed on a regular basis.

An extended-release form of niacin is available with a prescription. The niacin from this tablet is released over an 8- to 12-hour period. With daily doses between 1,000 mg and 2,000 mg it raises HDL cholesterol levels by 15% to 25% and lowers triglyceride levels by 20% to 30%.

* Please note that this is not a complete list of all possible side effects. Please consult your doctor or pharmacist to learn more about side effects.


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