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Statin Drugs - Cholesterol Lowering Medications


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High cholesterol happens when you get too much “bad” cholesterol in your body. For cholesterol to travel through your blood, it is coated with a layer of protein to make a lipoprotein. Two lipoproteins you may have heard of are HDL (High-density lipoprotein) and LDL (Low-density lipoprotein).

High-density lipoprotein (HDL cholesterol), is called “good cholesterol” because it is believed to remove cholesterol from the blood. High levels of HDL in your blood may help to reduce your risk of coronary heart disease. A low level can increase your risk.

Low-density lipoprotein (LDL cholesterol), is known as “bad cholesterol.” Excess LDL builds up in your arteries and may lead to heart disease. The higher the level of LDL, the higher your risk for heart disease. Bad cholesterol can be inherited from your family members or be a result of your body chemistry. It can also be the result of a diet high in saturated fats, lack of exercise or diabetes.

Why is high cholesterol a health risk?

Having high cholesterol is a risk factor for heart disease. A healthy artery has a smooth, even surface. When too much cholesterol builds up in the wall of your arteries thick deposits, called plaque, form. The buildup of plaque narrows the artery, so your heart must work harder to force blood through. Plaques can limit or block the blood flow in the artery. They can also rupture and form blood clots. When either happens in a major artery supplying the heart or brain, the blood flow can be completely blocked. The result can be a heart attack or stroke.

Statin drugs - HMG-CoA reductase inhibitors

Statin drugs (HMG-CoA reductase inhibitors) is a class of hypolipidemic agents, used to lower cholesterol levels in people at risk for cardiovascular disease because of hypercholesterolemia (high cholesterol). Statin drugs are considered a first-line therapy for the treatment of high cholesterol. The drugs in this class are associated with few side effects and are the most effective drugs for lowering total and LDL cholesterol levels. Statins also help lower the risk of heart disease, stroke, and related diseases in people at increased risk.

List of Statin drugs

  • Atorvastatin (Lipitor)
  • Fluvastatin (Lescol)
  • Fluvastatin Extended-Release (Lescol XL)
  • Lovastatin (Mevacor)
  • Lovastatin Extended Release (Altocor, Altoprev)
  • Pravastatin (Pravachol)
  • Rosuvastatin (Crestor)
  • Simvastatin (Zocor)

How effective are statins

In comparison to other classes of cholesterol lowering drugs, the statins are the most effective for lowering LDL. Statins produce about a 25% to 55% reduction in levels of LDL cholesterol, a 5% to 15% increase in HDL cholesterol levels, and a 10% to 25% reduction in triglyceride levels. The relative efficacy of the statins for lowering LDL cholesterol and triglyceride levels is as follows: rosuvastatin has the most potent effect, followed by atorvastatin, simvastatin, pravastatin, lovastatin, and fluvastatin. The ability to lower LDL cholesterol levels is usually the most important factor to consider when choosing a statin, but other considerations include a patient's level of coronary heart disease risk, differences in side effects, drug interactions, cost, results of clinical trials, and the time of day a dose should be taken.

The first results can be seen after one week of use and the effect is maximal after four to six weeks.

Statin drug side effects

The statins are well tolerated with mild upper GI disturbances, myalgias and sleep disturbances as the most common side effects (10%).

Serious side effects (contact your doctor as soon as possible):

  • Liver dysfunction. You should stop a statin if you develop liver disease.
  • Myopathy/Rhabdomyolysis (severe form of muscle inflammation). Symptoms include: unexpected muscle pains, tenderness or weakness.

Less serious side effects (usually do not need medical attention):

  • Common: constipation; diarrhea; dizziness; headache; nausea; skin rash; abdominal pain.
  • Rare: decreased sexual ability; insomnia.

Pregnancy: Pregnancy Category X. Statin drugs are contraindicated during pregnancy and in nursing mothers.

Comparison of Effects on Cholesterol Levels

Medication
Daily Dose
Total Cholesterol
Decrease
Low Density
Lipoprotein
Decrease
High Density
Lipoprotein
Increase
Triglycerides
Decrease
Altocor
(Lovastatin XR)
10-60 mg
18-29%
24-41%
9-13%
10-25%
Crestor
(Rosuvastatin)
5-40 mg
33-46%
45-63%
8-14%
10-35%
Lescol
(Fluvastatin)
20-80 mg
17-27%
22-36%
3-9%
12-23%
Lescol XL
(Fluvastatin)
80 mg
extended release
25%
33-35%
7-11%
19-25%
Lipitor
(Atorvastatin)
10-80mg
25-45%
35-60%
5-9%
19-37%
Mevacor
(Lovastatin)
10-80mg
16-34%
21-42%
2-9%
6-27%
Pravachol
(Pravastatin)
10-80mg
16-27%
22-37%
2-12%
11-24%
Zocor
(Simvastatin)
5-80mg
19-36%
26-47%
8-16%
12-33%


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