Review of Medications for the Treatment of High Cholesterol
Cholesterol in is made by the liver and also comes from foods like meat and dairy products. There are two main types of cholesterol: ‘good’ and ‘bad’ cholesterol. High levels of bad cholesterol known as low density lipoprotein (LDL) can lead to heart attack, stroke and heart disease. Good cholesterol or high density lipoprotein (HDL) helps get rid of bad cholesterol by moving it from the arteries to the liver where it is removed from the body. Total cholesterol (TC) is the total amount of cholesterol circulating in blood. It includes LDL, HDL and VLDL (another type of ‘bad’ cholesterol). In general, a higher HDL and lower LDL and total cholesterol are preferred.
Other factors that can increase cholesterol include:
Drugs such as diuretics, glucocorticoids and amiodarone
Diseases such as biliary obstruction and nephrotic syndrome
Conditions that cause a change in metabolism such as hypothyroidism, obesity and pregnancy
Health impact of high cholesterol
71 million Americans have high LDL cholesterol and less than half are getting treatment. It is important to know your cholesterol levels in order to determine your risk of getting heart disease, the leading cause of death in the US.
Optimum cholesterol levels
Less than 100 (Optimal)
100 to 129 (Near optimal/above optimal)
130 to 159 (Borderline high)
160 to 189 (High)
Greater than 190 (Very high)
Less than 200 (Desirable)
200 to 239 (Borderline high)
Greater than 240 (High)
Less than 40 (Low)
Greater than 60 (High)
Drugs used for treating high cholesterol
(Combination drug products have not been included in this review.)
Statins or HMG-CoA inhibitors
Examples of statins:
Mechanism of action of statins: Inhibits production of HMG-CoA, an enzyme needed to make cholesterol
Side effects of statins
Drug interactions of statins
Effect of statins
18 to 55% LDL reduction
5 to 15% HDL increase
7 to 30% TG reduction
Contraindications for statins: active or chronic liver disease
Bile acid sequestrants
Examples of bile acid sequestrants
Mechanism of action of bile acid sequestrants: Cause a reduction in cholesterol levels by binding to bile acid. This increases activity of the LDL receptor, resulting in removal of more LDL from the blood.
Side effects of bile acid sequestrants
Drug interactions of bile acid sequestrants:
It also causes a decrease in absorption of other drugs when taken together
Effect of bile acid sequestrants
15 to 30% LDL reduction
3 to 5% HDL increase
No change or increase in TG
Contraindications of bile acid sequestrants
TG greater than 400 mg/dL
Fibrates (Fibric acid)
Examples of fibrates
fenofibric acid (Trilipix)
Mechanism of action: Activates PPAR alpha receptors to reduce triglycerides.
Side effects of fibrates
Drug interactions of fibrates
Effect of fibrates
5 to 20% LDL reduction (may be higher in patients with high TG)
10 to 20% HDL increase
20 to 50% TG reduction
Contraindications of fibrates: severe renal or hepatic disease
Cholesterol absorption inhibitor
Examples: ezetimibe (Zetia)
Mechanism of action of Zetia: Inhibits absorption of cholesterol from the small intestine
Side effects of Zetia
Drug interactions of Zetia: cholestyramine
Effect of Zetia
13% LDL reduction
3.5% HDL increase
8% TG reduction
active liver disease
unexplained persistent elevations in hepatic transaminase
Niacin (Nicotinic acid)
Examples of niacin
Mechanism of action: Inhibits production of LDL from the liver and raises HDL.
Side effects of niacin
hyperuricemia (or gout)
upper gastrointestinal distress
Availability: Prescription and OTC
Drug interactions of niacin: statins
Effect of niacin
5 to 25% LDL reduction
15 to 35% HDL increase
20 to 50% TG reduction
Contraindications of niacin
chronic liver disease
Omega-3 fatty acids
Mechanism of action: Inhibits production of TG in the liver
Side effects of omega-3 fatty acids
increased risk of bleeding
Availability: Prescription and OTC
Drug interactions of omega-3 fatty acids: anticoagulants
Effects of omega-3 fatty acid: 10% LDL increase
No effect on HDL
25 to 50% TG reduction
Contraindications of omega-3 fatty acids: Known hypersensitivity to omega-3 acids or any product component
Cholesterol reducing effect of various statin doses
High-Intensity Statin Therapy (50% or greater reduction in LDL)
atorvastatin 40 to 80 mg
rosuvastatin 20 to 40 mg
Moderate-Intensity Statin Therapy (30% to less than 50% reduction in LDL)
atorvastatin 10 to 20 mg
rosuvastatin 5 to 10 mg
simvastatin 20 to 40 mg
pravastatin 40 to 80 mg
lovastatin 40 mg
fluvastatin XL 80 mg
fluvastatin 40 mg twice daily
pitavastatin 2 to 4 mg
Low-Intensity Statin Therapy (less than 30% reduction in LDL)
simvastatin 10 mg
pravastatin 10 to 20 mg
lovastatin 20 mg
fluvastatin 20 to 40 mg
pitavastatin 1 mg
Percent reductions in LDL were determined by data meta-analyses by the Cholesterol Treatment Trialists (CTT) in 2010. This included data from 170,000 subjects in 26 randomized controlled trials. Individual response may vary.
There are many treatment options available for the treatment of high cholesterol. Your doctor may also recommend lifestyle changes such as regular exercise, following a diet low in saturated fat or weight management.
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